Pharmacology Exam 2 Blue Print PDF

Blue-Print for Pharmacology Exam 2 2/17/2020 5Total # Questions - 50 Multiple Choice, select all that apply and calculation questions. Points Per Question: 2 Points. Time 1 hour Some of the topics you need to know: Key Terms To All Chapters - Know the prototypes: Please Remember That This Is just A...

Blue-Print for Pharmacology Exam 2 2/17/2020 5Total # Questions - 50 Multiple Choice, select all that apply and calculation questions. Points Per Question: 2 Points. Time 1 hour Some of the topics you need to know: Key Terms To All Chapters - Know the prototypes: Please Remember That This Is just A Study Guide and not inclusive of all topics; You Must Read Your Chapters and Power points. (3 math calculations included) Chapter 13 - Drug therapy to decrease Immunity - 7 Questions Blueprint: Prototype: Cyclosporine 🍄🍄🍄 Conventional Anti Rejection Agent → the first anti rejection drug used to prevent transplant rejection reactions. By selectively inhibiting proliferation of helper T cells and expression of cytokines, these anti rejection drugs reduce the activity of other immune cells involved in graft rejection. Pharmacokinetics→ PO= poor absorption. Peak plasma levels occur 4 to 5 hours after a dose. Metabolism of cyclosporine involves the CYP3A4 liver enzyme system, and elimination occurs mainly in the bile. Action→ Inhibition of the production of cytokines involved in the regulation of T-cell activation. cyclosporine inhibits the transcription of interleukin 2 (by binding with calcineurin) which inhibits the signaling of T-cell receptors (which are responsible for the inflammation that occur in organ rejection and autoimmune disease). Uses→ Blue-Print for Pharmacology Exam 2 2/17/2020 Prevent rejection reactions, prolong graft survival or to treat chronic rejection in pts previously treated with immunosuppressant drugs. The drug inhibits both cellular and humoral immunity but affects T lymphocytes significantly more than B lymphocytes. cyclosporine is useful in the prevention and treatment of GVHD, a complication of bone marrow transplantation. Cyclosporine dosing is weight based in both adults and children, with higher doses given immediately before and after the transplant and then tapered over several months to minimize adverse effects and avoid excessive immunosuppression. In children: children >6 months can have this medication PO however, they may need a higher dose due to the high metabolism rate of children. Renal Impairment: risk of nephrotoxicity increases because of the new organ. Nephrotoxicity is dose related. In kidney transplant recipients, when serum creatinine and blood urea nitrogen (BUN) levels remain elevated, an evaluation of the patient and tissue biopsy is often necessary to differentiate cyclosporine-induced nephrotoxicity from a transplant rejection reaction. Hepatic impairment: check serum bilirubin and liver enzymes prior to and during treatment. cyclosporine is associated with mild elevations of serum bilirubin, often without elevated ALT or alkaline phosphatase. Critical Illness: risk versus benefit decision making. It is necessary to balance the need to prevent transplant organ rejection against the risk of infection and associated drug toxicities, which may lead to loss of the engrafted organ. Home Care: Chronic rejection is the main priority. Promoting correct medication use is critical to maintaining therapeutic blood levels after transplantation and preventing organ rejection. Due to the variable bioavailability of cyclosporine when taken orally, 🍄 patients should consistently take the drug at the same time each day. Adverse Effects→ Nephrotoxicity, hirsutism, gingival hypertrophy, hypertension, and hyperlipidemia. Long-term adverse effects such as: an increased risk of developing malignancy (skin cancers and lymphomas, and solid organ tumors). Contraindications→ combined use of antirejection drugs that have the same mechanism of action and toxicities (e.g., tacrolimus and cyclosporine) Nursing Implications→ Preventing interactions: Drugs that increase the effects are: Aminoglycoside antibiotics and amphotericin B (Increase nephrotoxic effects). Blue-Print for Pharmacology Exam 2 2/17/2020 Drugs that decrease the effects are: Carbamazepine, phenytoin, and rifampin (Decreases therapeutic effects). Administering the medication: IV infusion several hours before transplant procedure; then PO route when applicable. Cyclosporin medications USED to be prepared in alcohol and olive oil for oral administration and in alcohol and castor oil for IV administration however this caused many anaphylaxis incidences. Assessing therapeutic effects: Monitor organ functions and any signs of rejection, assess serum blood levels (every 2 hours). Cyclosporine has a very narrow therapeutic index; therefore, prescribers use serum drug levels to regulate cyclosporine dosing Assessing adverse effects: acute nephrotoxicity to chronic nephrotoxicity to kidney failure can occur. Monitor renal function (creatinine and BUN) and urine protein. For hepatotoxicity look into liver tests such as AST and ALT. Other Drugs in Class→ (SET- acronym) Sirolimus:BLACK BOX WARNING ♦ that use of sirolimus in lung and liver transplant patients has been associated with increased morbidity and mortality. Everolimus (Zortress, Afinitor) Tacrolimus: Using tacrolimus may allow corticosteroids to be reduced or stopped, thereby decreasing the adverse effects of long-term corticosteroid therapy. Blueprint: Teaching for Immunosuppressant Drugs Summary: Teaching for immunosuppressant drugs is telling the patient that their immune response will be lowered. Meaning, they will need to be careful in the # of people who visit (want to decrease exposure to pathogens), wash hands constantly (pt and visitors), avoid eating raw foods, avoid drinking grapefruit, their body won’t be able to mount a response as it normally would which can increase the risk for infection, sepsis, and other health conditions. Depending on the drug, teach patient contraindications, adverse effects, interactions that increase/decrease drug therapy. Blue-Print for Pharmacology Exam 2 2/17/2020 Patient Teaching Guidelines Immunosuppressant Drugs (actual chart from book, but abridged) General Considerations: 🧼✋ High risk for development of infections. Everyone needs to wash their hands and practice meticulous personal hygiene. Avoid contact with infected people. Lifelong drug treatment to prevent potential organ rejection is required. Poor adherence and missed medication doses are an important cause of organ rejection and need for a subsequent transplant. Report adverse drug effects (e.g., signs or symptoms of infection such as sore throat or fever, decreased urine output if taking cyclosporine; easy bruising or bleeding if taking 😵💫🩸 methotrexate). 🚭 Maintain healthy lifestyle habits, such as a nutritious diet, adequate rest and sleep, and avoiding tobacco and alcohol. These measures enhance immunity. Carry identification that lists the drugs being taken; dosage; prescriber’s name, address, and telephone number; and instructions for emergency treatment. Use of a MedicAlert bracelet is recommended in case of an accident or other emergency situation. Maintain regular supervision by a health care provider. Take no drugs, prescription or nonprescription, without notifying prescriber who is managing immunosuppressant therapy. In addition, some vaccinations should be avoided while taking immunosuppressant drugs. People should practice safe sex during immunosuppressive drug therapy. Wear protective clothing and use sunscreens to decrease exposure of skin to sunlight and risks of skin cancers. Also, methotrexate and sirolimus increase sensitivity to sunlight and may increase sunburn. Self-Administration ⛅🔥 Blue-Print for Pharmacology Exam 2 2/17/2020 Follow instructions. If unable to take medication, report to the prescriber or other health care provider; do not stop unless advised to do so. Missed doses may lead to transplant rejection; Take medications at approximately the same time each day to maintain consistent drug levels in the blood. With cyclosporine oral solution, use the same solution consistently. The available cyclosporine solutions (Neoral, Gengraf, Sandimmune) are not equivalent and cannot be used interchangeably. If a change in formulation is necessary, the dispensing pharmacy should consult the prescriber. Measure oral cyclosporine solution with the dosing syringe provided; add to orange or apple juice that is at room temperature (avoid grapefruit juice) into a glass container, stir well, and drink at once (do not allow diluted solution to stand before drinking). Rinse the glass with more juice to ensure the total dose is taken. Do not rinse the dosing syringe with water or other cleaning agents. Rinsing ensures the entire dose is taken. Take mycophenolate on an empty stomach; food decreases drug absorption by approximately 40%. Do not crush mycophenolate tablets and do not open or crush the capsules. If also taking cyclosporine, take the sirolimus 4 hours after a dose of cyclosporine. If taking the oral solution, use the syringe that comes with the medication to measure and withdraw the dose from the bottle. Empty the dose into a glass or plastic container with at least 2 oz (1/4 cup or 60 mL) of water or orange juice. Do not use any other liquid to dilute the drug. Stir the mixture vigorously, and drink it immediately. Refill the container with at least 4 oz (1/2 cup or 120 mL) of water or orange juice, stir vigorously, and drink at once. Take tacrolimus with food to decrease stomach upset. If giving or taking an injected drug, be sure you understand how to mix and inject the medication correctly. With etanercept, for example, rotate injection sites, give a new injection at least 1 inch from a previous injection site, and do not inject the medication into areas where the skin is tender, bruised, red, or hard. When possible, practice the required techniques and perform at least the first injection under supervision of a qualified health care professional. Blueprint: Blue-Print for Pharmacology Exam 2 2/17/2020 ATG (Atgam, Thymoglobulin) [Polyclonal antibodies]: 🐴🐰🐎🐇 Summary: - type of adjuvant medication that suppresses the immune response. It is a nonspecific immunoglobulin for immunosuppression to treat rejections after kidney transplants and aplastic anemia. ATG antibodies destroy lymphoid tissues and decrease # of circulating T cells thus suppressing acute cellular and humoral response. NEED skin test before administering. Check if they are allergic to horses or rabbits. Pharm book paragraph on ATG: ATG (Atgam, Thymoglobulin) is a nonspecific immune globulin preparation used for immunosuppression. Health care providers use ATG equine (Atgam), which is obtained from horse serum Treat rejection reactions after kidney transplants and aplastic anemia in patients who are not considered candidates for bone marrow transplantation. They also use ATG rabbit (Thymoglobulin) to treat these rejection reactions. ATG contains antibodies that destroy lymphoid tissues and decrease the number of circulating T cells, thereby suppressing acute cellular and humoral immune responses. In addition to its high concentration of antibodies against T lymphocytes, the preparation contains low concentrations of antibodies against other blood cells. With Atgam, it is necessary that potential recipients have skin tests before administration to determine if they are allergic to horse serum. High risk of anaphylactic reactions in recipients previously sensitized to horse serum Positive skin tests require desensitization before therapy. Essential that emergency equipment for airway and allergy management be immediately available when ATG is administered. The FDA has issued a BLACK BOX WARNING ♦ for ATG urging that its use be restricted to experienced prescribers. 🐴 🐰 Blue-Print for Pharmacology Exam 2 2/17/2020 Chapter 14 - Drug Therapy for the treatment of cancer - 10 Questions Note: Cisplatin, Oxaliplatin, Methotrexate, Tamoxifen, Cytoprotective Agents, and Chemotherapy Nursing Responsibilities are in the pharmacology folder! Also notes on the beginning of the chapter! If you need any help understanding the graph let me know! -Brieanna - Cytoprotective Agents - Pg. 275 - Tamoxifen - Under Antiestrogens pg. 272 - Cisplatin - Under Alkylating Drugs - Oxaliplatin - Under Alkylating Drugs - Methotrexate - Under Antimetabolites - Chemotherapy nursing responsibilities Oxaliplatin (Eloxatin) 🧊🧊🧊 Admin: IV infusion 85 mg/m2 every 2 wk Treats: Advanced colon cancer (with 5-fluorouracil and leucovorin) Adverse: Anaphylaxis, anemia, increased risk of bleeding or infection, and cold-induced acute neurotoxicities Patient Teach: avoid exposure to cold during, and for 3 to 5 days after, drug administration. This helps prevent or minimize nerve damage that may cause numbness, tingling, and pain in the throat or hands. Swallowing and daily activities that require hand grasping may be impaired. (All the information I found on this drug in the book). Chapter 15 - Inflammation, infection and the Use of Antimicrobial agents - 3 Questions Blueprint: Blue-Print for Pharmacology Exam 2 2/17/2020 Broad Spectrum antibiotics treatment and complications ○ Broad-spectrum antibiotics are antibacterial drugs that are effective against a wide range of bacteria (e.g., both gram-positive and gram-negative bacteria), whereas narrow-spectrum antibiotics are those that are effective against a limited range or a specific type of bacteria. A narrow-spectrum antibiotic is preferred over a broad-spectrum antibiotic when possible because broad-spectrum drugs are more likely to kill some normal flora, which disrupts the microbial balance. Patients are at greater risk for an opportunistic infection when taking a broad-spectrum antibiotic. The action of an antibacterial drug is usually described as bactericidal (kills the bacteria) or bacteriostatic (inhibits growth of the bacteria). Whether a drug is bactericidal or bacteriostatic often depends on its concentration at the infection site and the sensitivity of the bacteria to the drug. Bacteriostatic antibiotics depends on the ability of the host’s immune system to eliminate the inhibited bacteria; Bactericidal drugs are preferred in serious infections, especially in people with impaired immune function. Extra information: Overusing antibiotics: leads to tolerance, unnecessary adverse drug effects, emergence of drug-resistant microorganisms, and increases in health care costs. A failure to improve within 24 to 36 hours could indicate antibiotic resistance Goal of treatment w/ antibiotics: to eradicate the causative microorganism and return the host to full physiologic functioning. Body fights infection, prevents further infection, + increases the effectiveness of antimicrobial: Eat a balanced diet and get adequate fluid intake, rest, and exercise. Serious infections of antimicrobial drugs are synergistic (more than 1 antimicrobial drug work together) to kill multiresistant bacteria. Blue-Print for Pharmacology Exam 2 2/17/2020 Can mix antibacterial w/ antiviral and/or antifungal drugs. Implement isolation procedures appropriately, teach patients to always wash their hands, + cough into the bend of their elbow, avoid crowds when ill, avoid crowds during influenza season. Recommend an annual influenza vaccine and pneumococcal vaccine to high-risk populations (e.g., people with chronic diseases such as diabetes and heart, lung, or renal problems; older adults; health care personnel who are likely to be exposed). pulmonary hygiene measures: ambulating, turning, coughing and deep breathing exercises, and incentive spirometry. Change dressing, use sterile technique, it can prevent or avoid introducing new bacteria. Clean gloves remove dressing, discard in moisture-proof bag, wash hands before apply new dressing w/ sterile gloves. Monitoring patients w/ infections: temperature for increased or decreased fever and monitor the WBC count for changes. Patients on antimicrobial therapy: need to maintain an adequate fluid intake to assist with renal clearance to decrease drug toxicity Assist the patient with hand hygiene, maintaining nutrition and fluid balance, getting adequate rest, and handling secretions correctly. These measures help the body to fight the infection, prevent further infection, and enhance the effectiveness of antimicrobial medications. Assist patients in using antimicrobial drugs safely and effectively. Instruct patient on all aspects of medication administration. Chapter 16 - Drug therapy to decrease pain, fever and inflammation - 5 Questions - NOTES FOR CH 16 IN PHARM FOLDER Introduction - Acetaminophen also decreases fever and relieves pain but DOES NOT REDUCE INFLAMMATION Blue-Print for Pharmacology Exam 2 2/17/2020 - Aspirin (acetylsalicylic acid), acetaminophen, and NSAIDS - PREVENT OR TREAT GOUT Aspirin, acetaminophen, and NSAIDs = ANTIPROSTAGLANDINS Prostaglandins - chemical mediators found in most body tissues - they help regulate many cell functions and participate in the INFLAMMATORY RESPONSE - Formed when cellular injury occurs and phospholipids in cell membranes response by releasing ARACHIDONIC ACID - CYCLOOXYGENASE (COX) ENZYMES - metabolize arachidonic acid to produce prostaglandins, act briefly in the area where produced then inactivated - COX 1 → synthesized continuously and present in all tissues and cell types - Especially in platelets, endothelial cells, GI tract and kidneys - Important in homeostatic functions and protective effects on the stomach and kidneys - In stomach → prostaglandins decrease gastric acid secretion, increase mucus secretions and regulate blood circulation - In kidneys → help maintain adequate blood flow and functions - - In cardiovascular → help regulate vascular tone (vasoconstriction and vasodilation) and platelet function DRUG INDUCED INHIBITION OF PROSTAGLANDINS = adverse effects with aspirin and nonselective NSAIDs, especially gastric irritation, ulceration and bleeding INHIBITION OF COX-1 ACTIVITY IN PLATELETS - more responsible for GI BLEEDING than INHIBITION OF COX-1 ACTIVITY IN GASTRIC MUCOSA COX-2 → in BRAIN, BONE, KIDNEYS, GI TRACT, FEMALE REPRODUCTIVE SYSTEM - Occur in SMALL AMOUNTS or INACTIVE UNTIL STIMULATED by PAIN AND INFLAMMATION - Inflamed tissues - COX-2 induced by inflammatory chemicals mediators such as IL-1 and TUMOR NECROSIS FACTOR ALPHA - In GI tract - TRAUMA and HELICOBACTER PYLORI INFECTION - common cause of peptic ulcer disease also induced COX-2 - PROSTAGLANDINS produced by COX-2 → associated with PAIN and other SIGNS OF INFLAMMATION INHIBITION OF COX-2 = therapeutic effects of analgesia and anti-inflammatory activity - COX-2 INHIBITORS DRUGS = NSAIDS Blue-Print for Pharmacology Exam 2 2/17/2020 - - designed to selectively inhibit COX-2 and relieve pain and inflammation with FEWER ADVERSE EFFECTS than those that INHIBIT BOTH COX-1 and COX-2 especially stomach damage - Long term use will cause adverse effects in GI, renal and cardiovascular Pain, fever and inflammation - Pain - Sensation of discomfort, hurt or distress - Can occur with tissue injury and inflammation - Prostaglandins sensitize pain receptors and increase pain associated with other chemical mediators of inflammation and immunity → bradykinin, histamine and leukotrienes - Bradykinin - kinin in body fluids that become active with tissue injury → INCREASE AND PROLONG the vasodilation and increased vascular permeability - caused by HISTAMINE Aggravate and prolong erythema, heat and pain of local inflammatory reactions Histamine - formed and stored in most body tissue with high concentration is mast cells, basophils and platelets - When released - it is highly vasoactive causing vasodilation and increasing permeability of capillaries and venules → producing edema - contracting smooth muscles in the bronchi (producing bronchoconstriction and respiratory distress), gastrointestinal (GI) tract, and uterus; stimulating salivary, gastric, bronchial, and intestinal secretions; stimulating sensory nerve endings to cause pain and itching; and stimulating movement of eosinophils into injured tissue Leukotrienes - mediate inflammation and immune responses - Fever - Regulating center in hypothalamus - Excessive heat = blood vessels dilate, more blood flow through skin, sweating occurs and body temperature usually stays within normal range - Fever occurs when the set point in hypothalamus is raised on response to the presence of PYROGENS (FEVER PRODUCING AGENTS) - Endogenous pyrogens - cytokines such as IL-1, IL-6 and tumor necrosis factor Blue-Print for Pharmacology Exam 2 2/17/2020 - - Exogenous pyrogens - bacteria and their toxins or other by products - Body responds to higher hypothalamic set point by vasoconstriction of blood vessels and shivering, raising core body temp to higher set point - Accompany conditions such as: dehydration, inflammation, infectious processes, brain injury, or disease involving the hypothalamus - Inflammation - Normal response to tissue damage from any source such as tissue or organ - Attempt by the body to remove the damaging agent and repair the damaged tissue - Redness, heat, edema and pain Osteoarthritis - Produces inflammation and degeneration of joints - PRIMARY OSTEO - occurs without a history of injury or disease - SECONDARY OSTEO - results from previous injury or presence of inflammatory process - Joint pain, stiffness and instability, possibly with some degree of immobility - Joints affected → carpometacarpal joint (distal joint of hand) and metatarsophalangeal joint of feet, knees, hips and cervical - or lumbar vertebrae Joint stiffness common in morning and decreases with movement Drug therapy - Aspirin, acetaminophen and NSAIDS → produce analgesic effect and reduce fever - Only aspirin and NSAIDS reduce inflammation! - Gout - Arthritic condition caused by overproduction of uric acid = hyperuricemia Caused by uric acid crystal deposits in the synovial joint lining → becomes enlarged due to infiltration of neutrophils, - monocytes and leukocytes Uric acid > 6.8 mg/dL 3 stages - 1 - acute gouty arthritis or gouty attack - Hyperuricemia, pain and swelling of 1 joint - Pain at night and goes on for 10 days - Great toe commonly affects - After 1st attack → up to 10 years may pass before permanent damage to the joints and kidneys occurs Blue-Print for Pharmacology Exam 2 2/17/2020 - - - 2 - intercritical gout - Symptoms free period of several years followed by recurrence of symptoms 3 - chronic tophaceous gout - Presence of solid deposits of urate crystals - tophi- in joints and elsewhere - In kidneys - urate deposits may form renal calculi or cause any other damage Treatment → NSAIDS and corticosteroids → reduce inflammation and uricosuric agents to increase elimination of uric acid ALLOPURINOL Blueprint: Acetaminophen nursing responsibilities Prototype: acetaminophen (APAP, Tylenol, N-acetyl-p-aminophenol) Non-prescription drug commonly used as an aspirin substitute because it does not cause nausea, vomiting, or GI bleeding and it does not interfere with blood clotting. Equivalent to aspirin as an analgesic and antipyretic but does not have the anti-inflammatory activity of aspirin. Pharmacokinetics: Oral admin absorbed well. Peak plasma concentrations are reached within 30-120min. PO or suppository: 325-650mg every 4-6hrs. IV injection Ofirmev 1000mL over 15min. Duration: 3-4 hrs Metabolized: Liver Excreted: 94% in urine as non-toxic glucuronate and sulfate conjugates, 2% excreted unchanged. 4% is metabolized by cytochrome P450 enzymes to a toxic metabolite later excreted in urine. Action: Reduce fever, acts directly on hypothalamus to increase vasodilation and sweating. Diminishes pain. Blue-Print for Pharmacology Exam 2 2/17/2020 Use: Reduce fever and decrease minor pain. Often given to children and patients at risk for seizures who are receiving diphtheria, pertussis and tetanus immunizations (unlabeled use) Use in young children: Ibuprofen also has antipyretic properties. Alternating acetaminophen and ibuprofen every 4 hours over a 3-day period to control fever in young children has been shown to be more effective than monotherapy with either agent. Use in older adults: Safe unless liver damage is present or chronic alcohol abuser. Patients with renal impairment: May accumulate in kidneys. Acetaminophen is nephrotoxic in overdose because it is a metabolite that attacks kidney cells and can cause necrosis. Patients with hepatic Impairment: Same problem as renal impairment patients, but can cause fatal liver necrosis in overdose because it forms a metabolite that destroys liver cells. It is stimulated by ingestion of alcohol, smoking and anti seizure meds so they are at a higher risk for hepatotoxicity with usual therapeutic doses. Adverse effects Hepatotoxicity and renal failure. Hypersensitivity reactions marked by rash and fever may occur in patients with allergy to drug. 💔 Myocardial damage may develop in patients when doses of 5 to 8 g/d are ingested over several weeks or when 4 g/d have been ingested over 1 year. ASSESS For: Jaundice, urinary output, BUN, creatine, rash, fever. If rash develops stop drug. Contradictions hypersensitivity, caution with impaired hepatic and renal function. CROSSES PLACENTA and BREASTMILK. INCREASE EFFECT: Carbamazepine, phenytoin, rifampin. 🌿🌿HERBS: Willow, meadow root and Ginkgo. TOXICITY: Early symptoms (12–24 hours after ingestion) of toxicity are nonspecific (e.g., anorexia, nausea, vomiting, diaphoresis) and may not be considered serious or important enough to report or seek treatment. At 24 to 48 hours, symptoms may subside, but tests of liver function (e.g., aspartate aminotransferase, alanine aminotransferase, bilirubin, prothrombin time) begin to show increased levels. Later manifestations may include jaundice, vomiting, and CNS stimulation with excitement and delirium, followed by vascular collapse, coma, and Blue-Print for Pharmacology Exam 2 2/17/2020 death. Peak hepatotoxicity occurs in 3 to 4 days; recovery in nonfatal overdoses occurs in 7 to 8 days. Gastric lavage and activated charcoal. 😢 Antidote: Acetylcysteine can be administered by inhalation, oral or IV but does not reverse damage. Blueprint: Aspirin indications, contraindications and nursing responsibilities Prototype: aspirin (Asaphen) Relieves pain by acting both centrally and peripherally to block the transmission of pain impulses. They act peripherally to prevent sensation of pain receptors to various chemical substances released by damaged cells. These antipyretic agents also reduce fever by acting on hypothalamus to decrease its response to pyrogens and setting the body temp to a lower level. These drugs diminish inflammation by preventing prostaglandins from increasing the pain and edema produced by other substances released by damaged cells. These class drugs can suppress platelet aggregation. Low aspirin is used for patients who have experienced an ischemic stroke, TIA, angina and acute MI, reducing the risk of death and/or recurring event. Pharmacokinetics Action 🔬 Admin ORALLY or RECTALLY Onset of action 5 - 30 mins orally and 1 - 2 hours rectally Oral peaks in 15 - 120 mins & duration of action 3 - 6 hrs Rectal peaks in 4 - 5 hrs & duration of action 6 - 8 hrs Metabolized: liver Half-life: 15 min - 12 hrs Excretion: urine CROSSES PLACENTA AND ENTERS BREAST MILK → intrauterine growth retardation, increased bleeding, neonatal acidosis, low birth weight, still birth 🏃 Blue-Print for Pharmacology Exam 2 2/17/2020 Use Inhibit prostaglandins produces inflammatory effects needed for analgesia and antirheumatic effects Acts on thermoregulatory center of hypothalamus blocking the effects of endogenous pyrogens and inhibiting synthesis of prostaglandins Antiplatelet effects → low doses blocks thromboxane A2 to inhibit platelet aggregation 👾 Alert Analgesic agent → relieve mild to moderate pain Antipyretic agent → ONLY FOR ADULTS!!! Anti-inflammatory agent → decrease inflammation in pt with osteoarthritis, juvenile rheumatoid arthritis and spondyloarthropathies Pregnant and with polycythemia vera → low dose aspirin Use in older adults: safe in low doses prescribed for prevention of MI and cerebrovascular accidents Use in pt with renal failure: NEPHROTOXIC in high doses ○ decrease the blood flow in the kidneys by inhibiting the synthesis of prostaglandins that dilate renal blood vessels ○ blood flow is normal, these prostaglandins have limited activity. However, when renal blood flow is decreased, synthesis of these prostaglandins is increased ○ they protect the kidneys from ischemia and hypoxia by antagonizing the vasoconstrictive effects of angiotensin II, norepinephrine 😮 Do not admin on children with chickenpox or influenza Not recommended in children causes Reye’s syndrome → encephalopathy, hepatic damage Adverse Effects 💀 GI adverse effects: nausea, dyspepsia, heartburn and epigastric discomfort Decreases platelet aggregation = GI blood loss and hemorrhage Petechiae and bruising Toxic at levels > 300 mcg.mL ○ Acute toxicity → respiratory alkalosis, hyperpnea, tachypnea, hemorrhage, confusion, pulmonary edema, seizures, tetany, metabolic acidosis, fever, coma and cardiovascular collapse ○ Renal and respiratory failure - 20 -25 g in adults & 4 g in children ○ Salicylism - toxicity → dizziness, tinnitus, difficulty hearing and mental confusion Therapeutic serum- 100 - 300 mcg/mL Toxicity- > 300 mcg/mL Blue-Print for Pharmacology Exam 2 2/17/2020 Nurse should assess for bleeding tendencies, GI irritation, nausea, vomiting and diarrhea ○ Assess skin for signs of decreased coagulation ○ Perform pulmonary and integumentary assessment looking for dyspnea, bronchospasm, and rash 🌿🌿Herbs and foods: INCREASE the effects alcohol, ginkgo Administering the Medication Take with full glass of water or other fluid and with food Admin med with food decreases gastric irritation Crushing of tablets or capsules = faster absorption → destroys long-acting feature and increases risk of adverse effects and toxicity Low doses - start with 325 mg then 75 - 81 mg daily → prevent MI and stroke Larger doses for anti-inflammatory effects - max 8000 mg Watch for bleeding, ringing in ears or diminished hearing Don’t take if have a fever Avoid 2 weeks before and after major surgery or dental procedures or before giving birth Assessing for Therapeutic Effects 💉 💖 Given for pain - nurse use pain scale to assess intensity, should decrease Given for fever - check temp every 2 -4 hrs, should decrease Given for inflammation - assess signs of inflammation, should decrease Pt using for MI or TIA → no chest pain or confusion Treatment of overdose - - Mild salicylate toxicity - stop drug or reduce dose Severe salicylate toxicity - treatment is symptomatic and prevent further absorption from GI tract, increasing urinary excretion and correcting fluid, electrolyte and acid base imbalances In GI tract - gastric lavage and activated charcoal reduces absorption IV sodium bicarbonate → produces alkaline urine where salicylates are excreted more rapidly Blueprint: Blue-Print for Pharmacology Exam 2 2/17/2020 Allopurinol- nursing responsibilities & patient teachings Prototype: Allopurinol (Zyloprim) Gout drug. Pharmacokinetics: ○ Absorbed in the GI tract ○ Onset: 24 to 48 hours ○ Peak of action of 2 to 6 hours ○ Half-life: 1 to 3 hours ○ Metabolized: active metabolite oxypurinol ○ Excretion: Slowly in the urine, also excreted in the breast milk Action: Inhibits the enzyme responsible for the conversion of purines to uric acid. The result is the reduction of the symptoms of gout. Use: Management of the signs and symptoms of primary and secondary gout. Also used in acute and chronic tophaceous gout to reduce uric acid concentrations. Other indications include leukemia, lymphoma, and malignancies that result in elevated serum uric acid levels. Use in Older Adults: The initial dose is 100 mg/d, which can be increased until the desired uric acid level is obtained. It is necessary to maintain fluid intake to produce a urine output of at least 2000 mL/d. The dosage should be reduced in the event of diminished renal function. Renal Impairment: The dosage of allopurinol is reduced based on the patient’s creatinine clearance. Hepatic Impairment: Allopurinol is administered cautiously in patients with hepatic impairment. The dosage does not need to be adjusted, but it is important to monitor liver function. Adverse Effects: CNS include drowsiness, headache, and vertigo. Hematologic: agranulocytosis, aplastic anemia, and bone marrow depression. GI: (most common) are nausea, vomiting, diarrhea, abdominal pain, and indigestion. ○ Hepatotoxicity and renal insufficiency are risk factors with the use of allopurinol. Contraindications: hypersensitivity. Patients with a family history or history of idiopathic hemochromatosis should not receive the drug. Assess for Adverse Effects: Assess for diminished urine output or cloudy urine, could mean build up of uric acid kidney stones. GI effects: such as nausea, vomiting, diarrhea, and abdominal pain. Bruising, bleeding, and anemia, also check aspartate Blue-Print for Pharmacology Exam 2 2/17/2020 aminotransferase and alanine aminotransferase levels for hepatotoxicity and creatinine clearance for renal insufficiency. Interactions: Several medications, including azathioprine, mercaptopurine, cyclophosphamide, cyclosporine, and thiazide diuretics, increase the risk of uricosuric-associated toxicity. ○ ampicillin and amoxicillin with allopurinol increases the risk of developing a rash ○ Anticoagulation effects are increased when combined with warfarin and aspirin. ○ Alcohol combined with allopurinol decreases the excretion of uric acid. Chapter 18 - Drug therapy with Beta-lactam Antibacterial agents-3 Questions Blueprint: Penicillin uses, nursing responsibilities Prototype: Ampicillin Pharmacokinetics After absorption, ampicillin is widely distributed. Penetration into the cerebrospinal fluid (CSF) occurs only with inflamed meninges. The kidneys rapidly excrete ampicillin, largely as unchanged drug, and it produces high drug concentrations in the urine. It is present in breast milk, and the volume of distribution increases during pregnancy, when the half-life, generally 1-2 hours, is increased. Action Ampicillin, like all penicillin, inhibits bacterial cell wall synthesis by binding to one or multiple penicillin-binding proteins Use Clinical indications for use of ampicillin include bacterial infections caused by susceptible microorganisms. Health care providers use the drug in the treatment or prophylaxis of infective endocarditis. The drug’s broad spectrum is often useful in skin, soft tissue, respiratory, GI, and genitourinary infections. The broad-spectrum coverage of ampicillin extends its activity against gram-negative Blue-Print for Pharmacology Exam 2 2/17/2020 bacilli. Note that the incidence of resistance among streptococci, staphylococci, and other microorganisms continues to increase. Use in Children o Widely used to treat infections and are generally safe. Caution is necessary in neonates because immature kidney function slows drug elimination. Dosage should be based on age, weight, severity of infection being treated, and renal function. Use in Older Adults o Relatively safe but decreased renal function/other disease processes with concurrent drug therapies increase risks of adverse effects. o Prior to administration of any antibiotic, verify if the dosage should be adjusted based on the patient’s creatinine clearance. Elderly patients are susceptible to superinfections when given any anti-infective agent. Use in Patients with Renal Impairment o Ampicillin is excreted primarily by kidneys, use caution Use in Patients with Hepatic Impairment o Can be used, as can almost all penicillins. o Caution is necessary when using amoxicillin-clavulanate (Augmentin) in patients with hepatic injury/destruction. o Development of cholestatic jaundice and hepatic dysfunction with previous use of drug are contraindications. Cholestatic liver impairment usually subsides when drug is stopped Use in Patient with Critical Illness o The extended-spectrum drugs (piperacillin, which is a derivative of ampicillin) and penicillin-beta-lactamase inhibitor combinations (Zosyn), which have bactericidal activity against a wide range of bacteria, are most likely to be used in critical care units for the treatment of respiratory diseases such as pneumonia, blood, or other infections. o With cephalosporins, third- and fourth-generation drugs are commonly used and usually given by intermittent IV infusion every 8-12 hours. o Blood levels of penicillins need to be maintained above the minimum inhibitory concentration (MIC) of the microorganisms causing the infection. Continuous or extended infusions may be of benefit w/ serious infections, especially Pseudomonas/Acinetobacter. ▪ Necessary to monitor function of kidneys, liver, and other organs in critically ill patients and reduce drug dosages when indicated Adverse Effects Most common AE is hypersensitivity rxns, including rash/anaphylactic rxn. GI adverse effects: abdominal pain, diarrhea, gastritis, and nausea and vomiting Blue-Print for Pharmacology Exam 2 2/17/2020 Nephropathy, such as interstitial nephritis, has occurred with all penicillins. Most often associated with high dosages of parenteral penicillins and attributed to hypersensitivity rxn. Penicillin G irritates the CNS. AE r/t CNS toxicity includes confusion, lethargy, twitching, dysphagia, seizures, and coma Penicillinase-resistant penicillins may result in hepatotoxicity Extended-spectrum penicillins may lead to hypokalemia and hypernatremia BBW♦: alert healthcare provider that inadvertent IV administration of PENICILLIN G BENZATHINE may result in cardiopulmonary arrest/death. Long-acting repository forms have additives that decrease their solubility in tissue fluids and delay absorption. Contraindications Include hypersensitivity/allergic reactions to any penicillin formulation (an allergic rxn to one penicillin = rxn to all penicillins) Cephalosporins and carbapenems each have a bicyclic core structure. This chemical unity is thought to be most responsible for beta-lactam hypersensitivity. Nursing Implications Preventing Interactions o Ampicillin inhibits renal tubular secretion of methotrexate, which may lead to prolonged and higher drug concentrations of methotrexate. o Penicillins are often given with aminoglycosides for serious infections (caused by Pseudomonas aeruginosa). They are not to be admixed in a syringe, given in IV solution, or administered via Y-site, because the penicillin inactivates the aminoglycoside. Dose separation is ideal! o Drugs That Increase the Effects of Ampicillin ▪ Allopurinol: Increases the incidence of skin rash ▪ Clavulanic acid: Overcomes resistance in bacteria that secrete beta-lactamase ▪ Probenecid: Inhibits the renal tubular secretion ▪ Uricosuric drugs: Block renal excretion o Drugs That Decrease the Effects of Ampicillin ▪ Chloroquine: Decreases the serum concentration ▪ Fusidic acid: Diminishes the therapeutic effect ▪ Tetracycline derivatives: Diminish the therapeutic effect Administering the Medication Blue-Print for Pharmacology Exam 2 2/17/2020 o Necessary to give ampicillin (like most oral penicillins) on empty stomach, approximately 1 hour before or 2 hours after a meal; with a full glass of water to promote absorption and decrease inactivation (can occur in acidic environment). Can be taken with food but absorption decreases. Oral suspensions are stable for 7 days at room temp and 14 days refrigerated. o When diluted with 0.9% NaCl, ampicillin is stable for 8 hours for concentrations up to 30 mg/mL. only stable for 1 hour when diluted with dextrose solutions for concentrations of 10-20 mg/mL. it is necessary to give IV penicillins for full, prescribed course of treatment to prevent complications such as rheumatic fever, endocarditis, and glomerulonephritis; IV concentrations should NOT exceed 30mg/mL. Assessing for Therapeutic Effect o Not necessary to obtain drug levels o It is recommended that serum creatinine and BUN be monitored Assessing for Adverse Effects o Assess characteristics of rash if present o Distinguish hypersensitivity from a nonallergic ampicillin rash Patient Teaching o General considerations ✅ ▪ Do not take any penicillin if you have ever had an allergic reaction to penicillin in which you had difficulty breathing, swelling, or skin rash. However, some people call a minor stomach upset an allergic reaction, which is incorrect, and they are not given penicillin when that is the best antibiotic in a given situation. ▪ Complete the full course of drug treatment for greater effectiveness and prevention of secondary infection with drug-resistant bacteria. ▪ Follow instructions carefully about how much of the drug you are supposed to take and how often you are supposed to take it. Drug effectiveness depends on maintaining adequate blood levels. Penicillins often need more frequent administration than some other antibiotics, because they are rapidly excreted by the kidneys. o Self- or Caregiver Administration ▪ Take most penicillins on an empty stomach, 1 hour before or 2 hours after a meal. ▪ Penicillin V, amoxicillin, and Augmentin can be taken with food. 🍲 (Take Augmentin with meals to increase absorption and decrease GI upset.) Blue-Print for Pharmacology Exam 2 2/17/2020 ▪ Take each dose with a full glass of water; do not take with orange juice or with other acidic fluids (they may destroy the drug). ▪ Take at even intervals, preferably around the clock. ▪ Shake liquid penicillins well, so they are mixed thoroughly, and measure the dose accurately. ▪ Discard liquid penicillin after 1 week if it is stored at room temperature or after 2 weeks if it is refrigerated. Liquid forms deteriorate and should not be taken after their expiration dates. ▪ Report skin rash, hives, itching, severe diarrhea, shortness of breath, fever, sore throat, black tongue, or any unusual bleeding to your health care provider. These symptoms may indicate an allergy to penicillin. 🌿🌿Herb Interactions: o Food: decreases absorption o Khat 🐈🐱 decreases absorption Other prototypes included in Ch 18: 🙀 Cephalosporins (Prototype: Cefazolin) Pharmacokinetics · After absorption, they achieve cephalosporins achieve therapeutic concentrations in most body fluids and tissues with maximum concentrations in liver and kidneys. Most do not reach therapeutic levels in CSF (most 3rdgens are consistent with CSF penetrations in patients with inflamed meninges) · Distributed into most body tissues and crosses placenta. Onset of action is rapid with IV and IM administration. Peaks at the end of IV infusion and within 1-2 hours with IM injection. Duration of action is 6-12 hours. Drug is largely excreted unchanged via the kidneys, concentrates in the urine. Metabolism is not hepatic, no dosage adjustments needed with hepatic impairment Action · Cefazolin inhibits the third and last step of bacterial wall synthesis by binding to one of more penicillin-binding proteins Blue-Print for Pharmacology Exam 2 2/17/2020 Use · Cefazolin is a frequently used parenteral agent. Reaches higher serum concentration, is more protein bound and has a slower rate of elimination than other 1stgen drugs. These factors prolong serum half-life, can be given less frequently. · Indications for cephalosporins include surgical prophylaxis and treatment of infections of respiratory tract, skin and soft tissues, bones and joints, urinary tract, brain and spinal cord, and bloodstream (septicemia). In infections caused by MRSA, cephalosporins are not clinically effective even if in vitro testing indicates susceptibility. Infections caused by Neisseria gonorrhoeae, at one time susceptible to penicillin, are now treated with a third-generation cephalosporin such as ceftriaxone. · Use in Children o Commonly safe. Should be used cautiously in neonates because immature kidney function slows their elimination. Dosages should be based on weight, age, severity of infection, and renal function. · Use in Older Adults o Decreased renal function, other disease processes, and concurrent drug therapies increase risk of complications · Use in Patients with Renal Impairment o All parenteral cephalosporins, except ceftriaxone, require dosage adjustment in patients with renal impairment. Usual dose may produce high and prolonged serum drug levels, and therefore a lower dose or increased period between doses is necessary. Cefazolin is moderately dialyzable and normal dose or supplemental dose should be administered after dialysis. · Use in Patients with Critical Illness o First-generation cephalosporins, mainly cefazolin, are used for procedures associated with gram-positive postoperative infections because of activity against streptococci and methicillin-susceptible staphylococci. o Second-generation cephalosporins, mainly cefotetan and cefoxitin, are often used for abdominal procedures, especially gynecologic and colorectal surgery, in which enteric gram-negative postoperative infections may occur. o Third-generation cephalosporins should not be used for surgical prophylaxis because they are less active against staphylococci than Blue-Print for Pharmacology Exam 2 2/17/2020 cefazolin and the gram-negative organisms they are most useful against are rarely encountered in elective surgery. o A single dose is usually sufficient, although repeat doses are necessary in patients undergoing a surgical procedure exceeding 4 hours or procedures involving major blood loss. · Use in Patients Receiving Home Care o Teach accurate administration, observation for therapeutic effects, and adverse effects with oral agents (cephalexin and cefprozil). For parenterals, teach about not using drug if it is cloudy/discolored or if the vial is damaged. Adverse Effects · Abdominal pain, gastritis, nausea, vomiting. Contraindications · Previous severe anaphylaxis rxn to a penicillin, there is a risk of cross-sensitivity because they are chemically similar. · Cephalosporin allergy. Immediate reactions with anaphylaxis, bronchospasm, and urticaria occur less often than delayed reactions with skin rash, drug fever, and eosinophilia. · Drugs That Increase the Effects of Cephalosporins o Aminoglycosides: Increase the risk of nephrotoxicity o Entecavir: Leads to competitive inhibition of transporters in renal tubules o Furosemide: Increases the risk of nephrotoxicity o Nimodipine: Increases the risk of nephrotoxicity o Vancomycin: Increases the risk of nephrotoxicity Nursing Implications · Preventing Interactions o Cephalosporins associated with decrease in prothrombin activity, may be due to depletion of Vitamin K in gut flora. Necessary to monitor patients previously stabilized on anticoagulants. Each gram of cefazolin has 46 mg (2 mEq) of sodium,15 may have negative effects on patients with heart failure! · Administering the Medication o The nurse should not mix ceftriaxone and IV solutions of calcium-containing salts or administer these drugs simultaneously, because of the potential for ceftriaxone–calcium precipitation. It is Blue-Print for Pharmacology Exam 2 2/17/2020 · possible to minimize adverse effects by administering most oral cephalosporins with food or milk. Assessing for Therapeutic Effects o If the patient is experiencing renal impairment, monitoring of serum creatinine and BUN is recommended, because adjustment for renal dysfunction may be necessary. NO HERB INTERACTIONS Carbapenems (Prototype: Imipenem-cilastatin) Pharmacokinetics · Imipenem-cilastatin is given parenterally, distributed in most body fluids/tissues. Rapid onset of action, peaks at end of infusion, duration is 6-8 hours. Enzyme dehydropeptidase in renal tubules breaks down imipenem component; low concentration in urine. Cilastatin inhibits destruction of imipenem, increasing urinary concentration and reducing renal toxicity. Action · Inhibits synthesis of bacterial wall by binding with penicillin-binding proteins Use · Effective in infections by wide range of bacteria, including penicillinase-producing staphylococci, E. coli, Proteus species, Enterobacter–Klebsiella–Serratia species, P. aeruginosa, and Enterococcus faecalis. Main use is treatment of infections caused by organisms resistant to other drugs. Considered broad-spectrum antibiotic; covers a range of gram-negative and gram-positive aerobes and anaerobes. · Used to treat infections of the lower respiratory tract, urinary tract, intra-abdominal infections, bone and joints, and skin and skin structures. It can also be used to treat polymicrobial infections (caused by multiple microorganisms), bacterial septicemia, and endocarditis. · Use in Children o Children with CNS infections should not use; risk of seizures. Caution with neonates, immature kidneys. Dosages calculated based on age, weight, severity, and renal function. · Use in Older Adults o Relatively safe, except if patient has decreased renal function, other diseases, and concurrent drug therapies (increased risk of AE) Blue-Print for Pharmacology Exam 2 2/17/2020 · Use in Patients with Renal Impairment o Reduce the dosage of imipenem–cilastatin and all other carbapenems in most patients with renal impairment, and caution is warranted in patients with creatinine clearance ≤20 mL/min because of the increased risk of seizures. Patients with severe renal impairment (≤5 mL/min) should not receive imipenem–cilastatin unless hemodialysis is initiated within 48 hours. · Use in Patients with Hepatic Impairment o May cause abnormalities in liver function test results (elevated alanine and aspartate aminotransferases, alkaline phosphatase), but hepatitis and jaundice rarely occur. · Use in Patients with Critical Illness o Typically used for critical illnesses. Carbapenem-resistant strains of P. aeruginosa are arising due to the altered permeability to this class of drugs and specific changes that occur on the protein outer membranes. · Use in Patients Receiving Home Care o Not typically given in home settings Adverse Effects · Risk of cross-sensitivity in patients with penicillin hypersensitivity and gastric disturbances. · Have been reports of CNS toxicity, including seizures. Seizures are more likely in patients with a preexisting seizure disorder or when recommended doses are exceeded; however, they have occurred in other patients as well. Contraindications · Hypersensitivity to carbapenems. Patients with severe shock or atrioventricular block should not receive the IM formulation (containing lidocaine). Nursing Implications · Preventing Interactions o Drugs That Increase the Effects of Imipenem–Cilastatin Cyclosporine: May increase central nervous system effects Ganciclovir: May lead to generalized seizures Probenecid: Increases drug level and half-life Blue-Print for Pharmacology Exam 2 2/17/2020 o All carbapenems may decrease the serum concentrations of divalproex. The drug may cause positive Coombs test results. · Administering the Medication o IM administration of imipenem–cilastatin is not recommended for people with severe or life-threatening infections such as endocarditis, shock, or septicemia. To prepare imipenem–cilastatin for IM injection, lidocaine, a local anesthetic, is added to decrease pain. The solution is contraindicated in people allergic to this type of local anesthetic. The IM formulation is not for IV use · Assessing for Therapeutic Effects o Drug levels are not required. Monitor serum creatinine and BUN. · Assessing for Adverse Effects o Assess any rash · Patient Teaching o Important to report any adverse effects NO HERB INTERACTIONS Monobactam (Prototype: Aztreonam) Pharmacokinetics · Given parenterally, is distributed in most body fluids and tissues, including the lungs, liver, kidney, bone, uterus, intestine, sputum, bile, pleural fluid, and synovial fluids. The drug also crosses the placenta and is excreted in breast milk. · Peak action within 1 hour, duration 4-14 hours; onset depends on organism and dose. Metabolized in liver to inactive metabolites, which are excreted in urine Action · Synthesis of bacterial cell walls by binding to penicillin-binding proteins. Considered safe to administer to patients with penicillin allergy Use · Effective in infections caused by N. gonorrhoeae, H. influenzae, and most Enterobacter–Klebsiella–Serratia species, and it is often active against P. aeruginosa. Lacks gram-positive coverage, anaerobes are not susceptible. · Indications for use include infections of the urinary tract, skin and skin structures, and lower respiratory tract. Other indications include intra-abdominal and gynecologic infections as well as gram-negative septicemia. FDA considers aztreonam solution for inhalation as an orphan drug for control of gram-negative bacteria in the respiratory tracts of patients diagnosed with cystic fibrosis. Blue-Print for Pharmacology Exam 2 2/17/2020 · Aztreonam may cause an elevation in hepatic enzymes; however, on discontinuation of the drug, most enzymes return to pretherapy levels. · Use in Children o Used for those older than 1 month of age. AE occur more frequently in children. · Use in Older Adults o Relatively safe, although decreased renal function, other disease processes, and concurrent drug therapies increase the risks of adverse effects in older adults. · Use in Patients with Renal Impairment o Necessary to reduce the dosage of aztreonam in patients with renal impairment. Aztreonam is moderately dialyzable, and patients with life-threatening infections should receive a supplemental dose after each hemodialysis session. · Use in Patients with Critical Illness o Typically reserved for those patients with a severe penicillin allergy. Monotherapy with aztreonam may lead to resistant P. aeruginosa infections. · Use in Patients Receiving Home Care o Typically not given at home Adverse Effects · Most common adverse effects include rash, diarrhea, nausea, vomiting, and localized thrombophlebitis. · Prolonged use may cause fungal or bacterial superinfections. Clostridium difficile–associated diarrhea and pseudomembranous colitis should be concerned with extended use. Contraindications · Hypersensitivity to any component of aztreonam. Nursing Implications · Preventing Interactions o No identified food/herb interactions. Aztreonam and aminoglycosides, when used in combination, can demonstrate synergistic effects against some strains of organisms, specifically P. aeruginosa and some Enterobacteriaceae. Potential for false-positive reactions in urine glucose tests using Benedict’s solution, Clinitest, or Fehling’s solution. o Drugs That Increase the Effects of Aztreonam Aminoglycosides: Increase the risk of nephrotoxicity Blue-Print for Pharmacology Exam 2 2/17/2020 Furosemide: May increase serum levels o Drugs That Decrease the Effects of Aztreonam Cefoxitin: Induces the production of beta-lactamases Chloramphenicol: May antagonize bactericidal activity · Administering the Medication o Given IV or IM · Assessing for Therapeutic Effects o Drug levels are not required. Monitor serum creatinine, BUN, and liver function tests. · Assessing for Adverse Effects o Assess any rash Patient Teaching · Importance of reporting any AE NO HERB INTERACTIONS Chapter 20 - Drug therapy with Tetracyclines, Sulfonamides and Urinary antiseptics - 5 Questions By: Kevin These older, broad-spectrum, bacteriostatic drugs are rarely used for systemic infections because of antimicrobial resistance and the development of more effective or less toxic drugs. Blueprint: Tetracyclines-indications, patient teachings, nursing responsibilities Blue-Print for Pharmacology Exam 2 Class: TETRACYCLINES 🦷🐄🥛🧀 🚴 2/17/2020 Prototype: Tetracycline Hydrochloride Antibiotics Derived from chlortetracycline, that may be used to treat a broad variety of infections. The drugs in this class have similar pharmacologic properties and antimicrobial activity. Although tetracyclines are effective against both gram-negative and gram-positive microorganisms, they are usually not drugs of choice. Many gram-negative microorganisms have developed resistance to tetracyclines. However, prescribers still order them for bacterial infections caused by Brucella and Vibrio cholerae. The drugs also remain effective against rickettsiae, chlamydia, some protozoa, spirochetes, and others. Pharmacokinetics 🔬 Administration of tetracycline is oral, and the stomach absorbs 75% of the medication Peak of action is 2 to 4 hours Widely distributed to the tissues, with 65% of the drug protein bound Cross the placenta Half-life in patients with normal renal function is 8 to 11 hours. Action 🏃 Tetracycline penetrates microbial cells by passive diffusion and an active transport system. Intracellularly, it binds to the 30S ribosomes and possibly the 50S ribosomes and inhibits microbial protein synthesis 🥩 With acne, it suppresses the growth of Propionibacterium acnes with sebaceous follicles, reducing the free fatty acid content in the sebum. Blue-Print for Pharmacology Exam 2 Use 2/17/2020 👾 Treating Mycoplasma, Chlamydia, and Rickettsia. Treatment of chronic bronchitis, gonorrhea, and syphilis in patients with a known allergy to penicillin Helicobacter pylori Treating small animal bites and Lyme disease Acute intestinal amebiasis and acne vulgaris Klebsiella, Neisseria gonorrhoeae, Treponema pallidum, Listeria monocytogenes, Clostridium, Bacillus anthracis, Fusobacterium fusiforme, and Actinomyces Alert 😮 🦷💔 CHILDREN. Children younger than 8 years of age should not take tetracyclines because of their effects on teeth and bones. RENAL. Patients with renal impairment should not take tetracyclines. High concentrations of these drugs inhibit protein synthesis in human cells. RENAL. Causes azotemia, increased blood urea nitrogen (BUN), hyperphosphatemia, hyperkalemia, and acidosis. Adverse Effects 🥩 💀 Hypersensitivity such as rash, urticaria, serum sickness, or anaphylaxis. Maculopapular and erythematous rashes may also occur. Central nervous system (CNS) conditions such as intracranial hypertension Gastrointestinal (GI) conditions such as flatulence, diarrhea, nausea, vomiting, and epigastric distress Candidiasis: sore throat Increased pigmentation, photosensitivity reactions Administering the Medication 💉 Adults. 250–500 mg PO every 6 h 🌞🔥🔥🔥 Blue-Print for Pharmacology Exam 2 2/17/2020 Children. Older than 8 y: 25–50 mg/kg/d PO in four divided doses. The medication is most effective when taken on an empty stomach 1 hour before meals or 2 hours after meals. DO NOT to take it with dairy products, antacids, or iron supplements Metallic ions such as aluminum, calcium, iron, or magnesium inhibits tetracycline Withhold tetracycline for 2 hours if taken any of the above. Beware: 🐄🥛🧀 Contraindications Renal failure and known hypersensitivity to the drug Permanent discoloration of teeth, defects in tooth enamel, and retardation of bone growth Interactions Administering oral anticoagulants with tetracycline enhances the effect of vitamin K. Digoxin toxicity interferes with the bactericidal effects of the penicillins Dairy products, which decrease the absorption of the antibiotic. Drugs that Increase the Effects of Tetracycline Methoxyflurane (Increases the risk of nephrotoxicity) Drugs that Decrease the Effects of Tetracycline Blue-Print for Pharmacology Exam 2 2/17/2020 Aluminum, antacids, bismuth subsalicylate, didanosine, ferrous sulfate, calcium, kaolin, laxatives, magnesium, pectin, zinc (Decrease antibiotic absorption) Blueprint: Patient Teaching Guidelines for Tetracycline Take tetracycline around the clock because it inhibits bacteria rather than kill the bacteria. Avoid sunlamps, tanning beds, and intense or prolonged exposure to sunlight. Wear sunscreen and protective clothing when in the sun. Report severe nausea, vomiting, diarrhea, skin rash, or perineal itching to your health care provider. These symptoms may indicate a need to change or stop the drug. Take the drug on an empty stomach, at least 1 hour before or 2 hours after meals. Do not take the drug with or within 2 hours of taking dairy products, antacids, or iron supplements. If you must take an antacid, take it at least 2 hours before or 4 hours after tetracycline. Take each dose with 8 ounces of water. If you are taking an oral contraceptive, use another form of birth control for the duration of therapy. The effectiveness of oral contraceptives is decreased when combined with tetracycline. Never take outdated tetracycline due to the risk of severe reactions. Intravenous (IV) administration of minocycline requires slow infusion. Prolonged IV administration of minocycline may be associated with thrombophlebitis. The drug is stable in all IV solutions but is incompatible with calcium-containing solutions. Blue-Print for Pharmacology Exam 2 2/17/2020 Blueprint: Trimethoprim-Sulfamethoxazole - nursing process Class: SULFONAMIDES 🧬🧬🧬 Prototype: trimethoprim–sulfamethoxazole (TMP-SMZ) Sulfonamides are bacteriostatic drugs that were once effective against a wide range of gram-positive and gram-negative bacteria. However, increasing resistance is making them less useful. It is important to document susceptibility with culture and sensitivity testing, but sulfonamides may be active against S. pyogenes, some staphylococcal strains, H. influenzae, Nocardia, C. trachomatis, and toxoplasmosis. The trimethoprim–sulfamethoxazole (TMP-SMZ) combination (Bactrim, Septra) is useful in UTIs due to Enterobacteriaceae and Pneumocystis jiroveci infection (in high doses), and it serves as the prototype. The combination of drugs demonstrates synergistic antimicrobial activity that is greater than the dose of either drug used alone. Other drugs in the class vary in extent of systemic absorption and clinical indications. Some sulfonamides are well absorbed and can be used in systemic infections; others are poorly absorbed and have more local effects. Pharmacokinetics 🔬 TMP-SMZ is rapidly and nearly completely absorbed in the GI tract Half-life of the medication is 6 to 11 hours Crosses the placental and blood–brain barriers Action 🏃 Blue-Print for Pharmacology Exam 2 2/17/2020 TMP-SMZ and other sulfonamides act as antimetabolites of para-aminobenzoic acid (PABA), which microorganisms require to produce folic acid Folic acid is necessary for the production of bacterial intracellular proteins Sulfonamides enter into the reaction instead of PABA, compete for the enzyme involved, and cause formation of nonfunctional derivatives of folic acid. Sulfonamides halt multiplication of new bacteria but do not kill mature, fully formed bacteria The presence of pus, serum, or necrotic tissue interferes with sulfonamide action because these materials contain PABA Some bacteria can change their metabolic pathways to use precursors or other forms of folic acid and thereby develop resistance Use 👾 TMP-SMZ acts by inhibiting bacterial synthesis of essential nucleic acids and proteins treatment of P. jiroveci pneumonitis, severe UTIs, Shigella enteritis, and Enterobacteriaceae. Streptococcus viridans, Staphylococcus epidermidis, Salmonella, Klebsiella, Nocardia, and Pseudomonas also is used to treat S. aureus and Escherichia coli, significant resistance Alert 😮 CHILDREN. Younger than 2 months of age should not receive TMP-SMZ. CHILDREN. Displaces bilirubin from binding sites on albumin. CHILDREN. bilirubin may accumulate in the bloodstream (hyperbilirubinemia) and CNS (kernicterus), resulting in life-threatening toxicity. RENAL. Acute renal failure has occurred when the drugs or their metabolites precipitated in renal tubules and caused obstruction RENAL. Preventive measures include intake of 1.5 to 3 L of fluid daily to reduce the formation of crystals and stones in the urinary tract. Monitor potassium level as hyperkalemia Adverse Effects 💀 Blue-Print for Pharmacology Exam 2 2/17/2020 GI effects: abdominal pain, nausea, vomiting, diarrhea, anorexia, and pancreatitis Hematological effects: aplastic anemia, agranulocytosis, eosinophilia, thrombocytopenia, and leukopenia Dermatological effects: pruritus, urticaria, Stevens-Johnson syndrome, and skin photosensitivity Renal effects: increased blood urea nitrogen and serum creatinine, renal failure, and interstitial nephritis Administering the Medication 💉 Adult. UTI: 1 double strength tablet PO twice daily for 3 d Children. UTI and otitis media: PO 8-mg/kg trimethoprim and 40-mg/kg sulfamethoxazole in two divided doses every 12 h for 10 d administered orally, with or without food take it with a full glass of water In patients with severe pneumonia caused by P. jiroveci, the drug is administered parenterally. 🧬 Drugs that Increase the Effects of TMP-SMZ Alkalinizing agents such as sodium bicarbonate Increase the rate of urinary excretion, raising the levels of sulfonamides in the urinary tract and increasing effectiveness in urinary tract infections Methenamine compounds such as urinary acidifiers Increase the risk of nephrotoxicity Salicylates, nonsteroidal anti-inflammatory agents, oral anticoagulants, phenytoin, methotrexate Increase the risk of nephrotoxicity by displacing sulfonamides from plasma protein binding sites Sulfonylureas Increase hypoglycemic reactions Blue-Print for Pharmacology Exam 2 2/17/2020 Preventing Interactions Both inhibit specific cytochrome P450 enzymes, leading to concurrent multiple drug and herb interactions, increasing or decreasing the effects The drug inhibits warfarin metabolism and is associated with a three-fold increased risk of GI bleeding when compared with other antibiotics. Other interactions include sulfonylureas (hypoglycemia), anticonvulsants (toxicity), and methotrexate (pancytopenia). 🌿🌿🌿🌿 Herbs and Foods that Increase the Effects of TMP-SMZ Garlic, ginseng, ginger, St. John’s wort 🌿🌿🌿🌿 Patient Teaching Guidelines for TMP-SMZ Take TMP-SMZ with 8 ounces of water. Take the drug before or after meals. Drink a minimum of 2 to 3 L of fluid per day. Effectiveness of oral contraceptives is decreased when combined with TMP-SMZ. 👶👶👶👶👶👶👶👶 🌞🔥🔥🔥 Avoid sunlamps, tanning beds, and intense or prolonged exposure to sunlight. When in the sun, wear sunscreen and protective clothing. 💫😵💫 If you have diabetes, be sure to monitor your blood sugar values. Reduced blood sugar levels can occur. Blueprint: Blue-Print for Pharmacology Exam 2 2/17/2020 Nitrofurantoin –Urinary antiseptics & nursing responsibilities Class: URINARY ANTISEPTICS 🚨NOTE: This is a very small section so it won’t be as detailed as the previous ones.🚨 The adjuvant medications used to treat UTIs are trimethoprim and the urinary antiseptic agents. Urinary antiseptics may be bactericidal for sensitive organisms in the urinary tract because these drugs are concentrated in renal tubules and reach high levels in urine. They are not used in systemic infections because they do not attain therapeutic plasma levels. The adjuvant medications include nitrofurantoin, phenazopyridine, and trimethoprim. Prototype: Nitrofurantoin Use 👾 Anti-infective agent that is administered for the treatment and prophylaxis of UTIs. The drug is effective for UTIs caused by E. coli, S. aureus, Enterobacter, Enterococcus, and Klebsiella. Administration of nitrofurantoin with food aids in absorption and decreases the onset of adverse effects. Alert 😮 renal, pulmonary, and hepatic toxicities may cause the urine to turn brown Blue-Print for Pharmacology Exam 2 2/17/2020 magnesium-containing antacids may reduce absorption and subsequent urinary secretion Adverse Effects 💀 Fetal malformations, and between week 38 and delivery, there is a risk of hemolytic anemia (1) nonspecific ST- and T-wave changes and bundle branch block 🧠💫 💔💔🖤 (2) CNS changes such as fever, malaise, depression, headache, lethargy, and vertigo. Administering the Medication 💉 Macrobid: 100 mg every 12 h for 7 d Macrodantin: 100 mg PO two times daily for 5 d Prophylaxis of recurrent urinary tract infection (UTI) in women. Macrodantin: 50–100 mg PO at bedtime Children older than 12 y: dual-release capsules: 100 mg every 12 h for 7 d Children 1 mo and older: macrocrystal capsules, 5–7 mg/kg/d PO in four divided doses for 7 days 🚨These last two are NOT on the Blueprint. Don’t focus too hard on these last two.🚨 Other Drugs: Phenazopyridine Phenazopyridine hydrochloride (Azo-Standard, Pyridium) is a urinary analgesic that is administered to provide pain relief related to burning, urgency, frequency, and irritation of the lower urinary tract mucosa The pain is a result of infection, trauma, cystoscopic examinations, surgery, or catheter insertion acts directly on the urinary tract mucosa to provide analgesia administer the medication with food to decrease GI distress urine will turn reddish orange BLACK BOX WARNING ♦ cautioning that if the patient’s skin turns yellow, it is important to report this to the health care provider immediately. This is a sign that phenazopyridine is accumulating in the patient’s system report a sore throat, fever, bruising, or bleeding Blue-Print for Pharmacology Exam 2 2/17/2020 Contraindications to phenazopyridine include renal insufficiency and hepatitis. Other Drugs: Trimethoprim Trimethoprim (Primsol) is a folate antagonist that is a urinary tract anti-infective. Most commonly administered in combination with sulfamethoxazole or as an adjuvant agent with the sulfonamides (see Sulfonamides) For susceptible infections and UTIs CDC has recommended that trimethoprim be used (unlabeled use) in the treatment of P. jiroveci pneumonia inhibits folic acid reduction to tetrahydrofolate, thus interfering with the bacterial cell growth Contraindications include a known folate deficiency, fragile X syndrome, and a creatinine clearance less than 15 mL/min Have a sufficient fluid intake (2000–3000 mL/24 hours report symptoms such as sore throat, fever, bruising, or rash Rash and pruritus are the most common adverse effects occasional reports of nausea, vomiting, thrombocytopenia, and leukopenia Chapter 23 - Drug Therapy for Viral Infections - 3 Questions HSV-1 = causes fever blisters or cold sores on the lips, mouth, or face HSV-2= genital warts Blueprint: Drug class: antiviral Prototype: Acyclovir (Zovirax) DRUGS FOR HERPES VIRUS INFECTIONS Pharmacokinetics Can be given oral, parenteral, IV or topical! Blue-Print for Pharmacology Exam 2 2/17/2020 Action This drug interrupts viral DNA replication and reduces viral shedding and prevents formation of new lesions. Use Immunocompromised patients take acyclovir for initial and recurrent cutaneous and mucosal herpes simplex virus (HSV), varicella-zoster virus (VZV) (chicken pox), and cytomegalovirus (CMV) Treatment of genital herpes Does not eliminate the inactive virus in your body so if you're not continuously taking the drug, it may reoccur However if you take this drug too long you make become resistant (especially the immunocompromised patients) IV= immunocompromised/ non compromised patients and for severe genital herpes Oral= HSV and VZV Use for children= HSV gingivostomatitis Adverse effects Most common= malaise, headache, nausea, vomiting, and diarrhea Parenteral can cause phlebitis, rash, hives, encephalopathy (rare, but serious) Contraindications heart failure, renal disease, and lactation. Caution is necessary in patients who are receiving nephrotoxic agents. And of course, sensitivity to the drug Nursing implications Interactions The most significant interactions with acyclovir include increased serum concentrations with probenecid, drowsiness with zidovudine, and renal insufficiency when combined with medications that cause renal toxicity. Administration WASH HANDS before application of topical meds with a gloved hand These meds should be given ASAP (once the symptoms arise) With oral meds take the drug without respect to food intake With parenteral, infuse OVER AN HOUR to prevent renal damage Patient needs to be well hydrated 2 to 3 L of fluid per 24 hours Blue-Print for Pharmacology Exam 2 2/17/2020 Do not give with other blood products or protein products (in iv) Assessing for therapeutic effects nurse assesses for the healing of lesions, decreased pain, and itching. When administering acyclovir prophylactically (prevention) for genital herpes, assess for fewer recurrences. Assessing for Adverse Effects topical drug- assess for burning, stinging, and pruritus. parenteral drug- assess for phlebitis at the injection site. It is also necessary to assess for confusion, coma, seizures, and tremors. assess the aspartate aminotransferase (AST) and alanine aminotransferase (ALT) for elevations, as well as blood urea nitrogen (BUN) and serum creatinine for increases. LABS BUN: Normal is 7-18 mg/dL AST: Normal is 10-40 units ALT: 7-56 units per liter Crcl: PATIENT TEACHING Prevention is better than treatment, partly because medications used to treat viral infections may cause serious adverse effects. Thus limit exposure with those infected with a viral illness. Wash hands frequently and thoroughly; this helps prevent most infections. immunizations against viral infections as indicated. With genital herpes, avoid sexual intercourse when visible lesions are present and always wash hands after touching any lesion. Understand that drugs may relieve symptoms but do not cure viral infections. For example, treatment of genital herpes does not prevent transmission to others, and treatment of cytomegalovirus (CMV) retinitis may not prevent disease progression. Ask a health care provider for information about managing adverse drug effects. If taking foscarnet or ganciclovir for CMV retinitis, have eye examinations approximately every 6 weeks. If taking ganciclovir maintain regular appointments for the assessment of the complete blood count and renal function. Blue-Print for Pharmacology Exam 2 2/17/2020 Administer antiviral agents for recurrent genital herpes lesions as soon as signs and symptoms begin. Use gloves to apply topical antiviral ointment to lesions. Question: An 80-year-old patient with chronic renal failure is admitted to the hospital with herpes simplex. The acyclovir (Zovirax) is to be administered parenterally. When preparing to administer this medication, what would the nurse expect in regard to the dose? Answer: The dose is smaller based on the patient's kidney function. Blueprint: Prototype: Zidovudine Drug class: antiretroviral drug, to fight HIV GOALS of ANTIRETROVIRAL DRUGS Antiretroviral therapy assists in improving patients’ quality of life and suppressing conversion to AIDS. a reduction in morbidity and mortality The prevention of drug resistance is accomplished by the administration of combination drug therapy. most effective regimens contain two different NRTIs and integrase strand transfer inhibitors A specific type of antiretroviral drug is NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS----which includes zidovudine. These drugs are similar to our DNA (A,C,G,T) which is how they get into our human cells. more specifically the T component (thymidine) Pharmacokinetics quickly absorbed in the GI tract, reaching a peak of action in ½ to 1 ½ hours Crosses placenta Oral or iv Action Blue-Print for Pharmacology Exam 2 2/17/2020 This drug does a reverse on DNA ( reverse transcriptase) because HIV needs the normal conversion of RNA to DNA to replicate itself, so viral reverse transcriptase prevents this from happening. Zidovudine blocks the addition of further nucleotides and terminates viral replication. Use The drugs are more active in slowing the progression of acute infection rather than in treating chronically infected cells. do not cure HIV infection or prevent transmission of the virus through sexual contact or blood contamination. Used in treatment of HIV infection—in combination with two or more other antiretroviral agents. Infected Pregnant women take this drug to prevent transmission to the fetus!!! If they don't take this then during labor they receive through IV. MUST give within 6-12 hrs after birth and the baby should continue to receive for the next 6 weeks Contraindications History of lactic acidosis Assessing for adverse effects assesses for malaise, CNS depression, and GI symptoms such as nausea, vomiting, and diarrhea. assess for myalgia and hepatomegaly. Development of anemia usually occurs 2 to 4 weeks after the start of therapy. Neutropenia is most likely to occur in 6 to 8 weeks. It is important to obtain the patient’s CBC as a baseline measure before therapy begins and then every 2 weeks from then on. Hgb, Hct, and granulocyte count for hematologic toxicity. If the hemoglobin level is less than 7.5 g/dL or the reduction is greater than 25% of the baseline value, it may be necessary to interrupt therapy and administer transfusions. This is also the case if the granulocyte count is less than 750/mm3 or greater than 50% of the baseline measure. *** LABS: CBC Hgb (normal= 12-18) Hct ANC (normal= 1500-8000) Assess for therapeutic effects Blue-Print for Pharmacology Exam 2 2/17/2020 Monitors the patient’s CD4 and cell count for increase or decrease in viral load. An increase in the CD4 count indicates a decrease in viral load and the ability to fight viral infections Patient Teaching Because lactic acidosis may develop, the nurse teaches the patient the signs and symptoms of this condition, including musculoskeletal pain Prevention is key Use condoms Wash hands frequently Have immunizations Use clean needles Drugs relieve symptoms, but do not cure Adherence is also key Do not use St. John’’s Wort while on antiretroviral drugs. It can decrease serum drug levels. Have regular blood tests (check on CD4) When administering antiretroviral agents, it is important to distinguish whether the patient has taken antiretroviral agents in the past. Patients who have received antiretroviral agents are treatment experienced, whereas those who have not received them are treatment naïve. 🌿 Another antiviral drug not mentioned in the blueprint is ribavirin. Its main use is for the treatment of respiratory syncytial virus (RSV) infections in children. (inhaled) also used for the treatment of cytomegalovirus Another drug is indinavir sulfate (Crixivan)- used to treat HIV: patient teaching--- drink 48oz of water per day with regards to renal function Hope I covered all 3 questions !!! Chapter 35 - Nutritional Support Products, Vitamins and Mineral Supplements Blue-Print for Pharmacology Exam 2 2/17/2020 6 Questions Blueprint: Hypokalemia, hyperkalemia, hyponatremia, & lead poisoning NORMAL POTASSIUM LEVELS 3.5-5.0 HYPOKALEMIA→ less than normal amounts of potassium in the blood. Potassium chloride is usually the drug of choice for preventing or treating because if potassium is low, so is chloride (cation and anion reaction). Health care providers will give this medication to those who are taking potassium-depleting diuretics, those receiving digoxin, and those who are receiving IV fluids because of surgical procedures, GI disease, and also replace chloride in patients with hypochloremic metabolic acidosis. Hypokalemia increases the risk of digoxin toxicity!!! In IV therapy the serum potassium level and urine output are measured before giving potassium chloride IV. PREVENTION/ TREATMENT OF HYPOKALEMIA DOSES IN ADULTS: 20-40 mEq PO daily in 1-2 divided doses, 40-100 mEq PO daily in 2-4 divided doses, MAX DOSE FOR IV is 40 mEq/L infused at 10 mEq/h (do not exceed 200 mEq daily). MONITOR EKG AND POTASSIUM LEVELS. IN CHILDREN: 1-2 mEq/kg/d in 1 to 2 divided doses, IV 0.5-1 mEq/kg/dose (max dose 40 mEq) if infusion exceeds 0.5 mEq/kg/hr the patient will need continuous EKG monitoring with physician at bedside. Final note: Give potassium chloride by IV infusion only. NEVER IM or IV push, rapid infusion can cause fatal hyperkalemia. Signs and symptoms of hypokalemia: palpitations, confusion, dizziness, muscle weakness, abdominal distension, frequent voiding of large amounts of urine HYPERKALEMIA→ greater than normal amounts of potassium in the blood. Dysrhythmia, heart block, cardiac arrest, respiratory paralysis and death can occur. Blue-Print for Pharmacology Exam 2 2/17/2020 Situations to look out for are in patients who use potassium chloride with angiotensin-converting enzyme inhibitors or potassium sparing diuretics. Patients taking salt substitutes that contain potassium instead of sodium are used with potassium supplements (I remember Voss talked about this one). And Patients taking penicillin G potassium. WELL-DILUTED PREPARATIONS IN IV ROUTE PREVENT SUDDEN HYPERKALEMIA. Treatment for hyperkalemia is Sodium polystyrene In adults: 15g PO 1-4 times per day or 30-50 g rectal q6h. In children: 1g/kg/dose PO q6h or 1g//kg/dose rectal every 2-6h; in infants and small children use lower dose. Signs and symptoms of hyperkalemia: muscle weakness, palpitations, slow pulse, fatigue, shortness of breath. Insulin & glucagon Insulin & glucagon are a treatment for hyperkalemia. Infusion causes potassium to move into the cells. Glucose, given with insulin, prevents hypoglycemia. Regular insulin 10-20 units in 10% dextrose 500 mL infused over 1 hr. Bolus regular insulin 10 units followed immediately by 50 mL of 50% dextrose Blood glucose must be monitored every hour for 5-6 hrs. HYPONATERMIA (0.9% NaCl) only used in initial treatment of severe hyponatremia Maintenance 3-4 mEq/kg/d Max 100-150 mEq/d dose varies based on condition LEAD POISONING 💀💀💀 SUCCIMER (Chemet, Category C) ○ Succimer chelates lead to form water-soluble complexes that can be excreted in urine ○ Indication: lead poisoning ○ Peak blood levels = 1-2 hrs ○ Metabolized in liver ○ Excreted in urine and feces ○ Most common adverse effects: Anorexia, nausea, vomiting, and diarrhea ○ ½ life = 2 days ○ Dosages for adults and children: 10 mg/kg/dose or 350 mg/m2/dose PO q8h for 5 days Then q12h for 14 days Max dose = 500 mg/dose Blue-Print for Pharmacology Exam 2 2/17/2020 Treatment course may be repeated; 2 week interval in between courses is recommended Capsule comes in 100 mg Capsule can be sprinkled on soft food or given in food for young children Other Drug: PENICILLAMINE (Cupermine) ○ This is a chelating agent which binds to copper, lead, mercury, and zinc to form soluble complexes that are excreted in the urine. Class: Fat Soluble Vitamins Prototype: Vitamin A or retinol Not soluble in blood, so is distributed by attaching to protein carriers in the blood. Pharmacokinetics 🔬 Absorbed from GI tract, stored in liver. Metabolized in liver. Eliminated in feces and urine. Use 👾 Replacement in deficiency states. Alert 😮 Serum levels of vitamin A>1200 international unit/dL is TOXIC. Large doses may increase the anticoagulant effects of warfarin. Adverse Effects 💀 Toxicity: hair loss, double vision, headaches, vomiting, bone abnormalities, and liver damage. Contraindications: allergic reaction, malabsorption syndrome, caution with pregnancy. Blue-Print for Pharmacology Exam 2 Administering the Medication 2/17/2020 💉 Oral: take before meals, on an empty stomach. After meals to prevent nausea. (IM administration may be necessary) Do not take with mineral oil because it prevents systemic absorption. Assessing for Therapeutic Effects 💖 Improved vision, less dryness in eyes, improvement in skin lesions. Prototype: Vitamin E, or alpha-tocopherol Pharmacokinetics 🔬 Absorbed from GI tract. Stored in adipose tissue. Metabolized in liver. Eliminated in bile. Use 👾 Alert Vitamin E replacement in deficiencies. 😮 Large amounts can interfere with vitamin K action (blood clotting) by decreasing platelet aggregation and producing a risk of bleeding! May increase the anticoagulant effect of warfarin. Mineral oil and cholestyramine decrease absorption. Adverse Effects 💀 Excessive: fatigue, headache, blurred vision, nausea, diarrhea. Contraindications: allergic, hypervitaminosis E, history of bleeding disorders or thrombocytopenia. Administering the Medication 💉 Oral: before meals on an empty stomach. Blue-Print for Pharmacology Exam 2 2/17/2020 After meals to prevent nausea. Assessing for Therapeutic Effects 💖 Decreased signs and symptoms of vitamin E deficiency. Prototype: Vitamin K, or phytonadione Pharmacokinetics 🔬 Concentrated in liver. Crosses placenta and enters breast milk. Metabolism occurs rapidly in liver. Elimination in the bile and urine. Action 🏃 Onset: after oral dose is 6-12 hours, subcutaneous dose is 1-2 hours. Use 👾 To correct hypoprothrombinemia caused by inadequate levels of vitamin K. To reverse the effects of warfarin (Coumadin) overdose. Alert 😮 IV administration may result in an anaphylactic type of reaction with risks of shock, cardiorespiratory arrest, and death. Avoid use when patient is receiving warfarin. Adverse Effects 💀 Facial flushing, alterations in taste, redness and pain at the injection site. In Contraindications: allergic, allergic to benzyl alcohol or castor oil. Administering the Medication 💉 Oral and subcutaneous routes are preferred. IM and IV route associated with severe hypersensitivity reactions. Protect preparations from light. Blue-Print for Pharmacology Exam 2 Assessing for Therapeutic Effects 💖 2/17/2020 Decreased signs and symptoms of vitamin K deficiency. Decreased bleeding and more normal blood coagulation tests. Class: Water Soluble Vitamins Prototype: Vitamin B complex: vitamin B1 (thiamine), vitamin B3 (niacin), and vitamin B6 (pyridoxine) (presented together because they have much in common) Pharmacokinetics 🔬 Absorbed from GI tract. Niacin and pyridoxine metabolized in liver. All eliminated by kidneys in urine. Thiamine widely distributed and enters breast milk. Niacin crosses placenta and enters breast milk. Pyridoxine stored in liver and crosses placenta. Alert 😮 Thiamine: history of an allergic reaction to the vitamin Niacin: hepatic impairment, active peptic ulcer disease, arterial bleeding, and lactation. Administration causes vasodilation, which may result in dizziness, hypotension, and injury from falls. Pyridoxine (IV form): cardiac disease. Caution is warranted with renal impairment. Use 👾 Vitamin B complex deficiencies. Adverse Effects 💀 Niacin and thiamine (parenteral): hypotension and anaphylactic shock Niacin (oral): anorexia, nausea, vomiting, diarrhea, and postural hypotension Blue-Print for Pharmacology Exam 2 Administering the Medication 2/17/2020 💉 Thiamine: preferred route of administration is by mouth; people may take it without regard to food. Niacin: people may take oral niacin, except for timed-release forms, with or after meals, which decreases anorexia, nausea, vomiting, diarrhea, and flatulence. Pyridoxine: the general route of administration is oral. Assessing for Therapeutic Effects 💖 Decreased signs and symptoms of deficiency. Prototype: Vitamin B12 (cyanocobalamin) and folic acid Pharmacokinetics 🔬 Vitamin B12: requires intrinsic factor for absorption. Widely distributed and stored in liver. Crosses placenta and enters breast milk. Eliminated slowly in urine. Folic acid: absorbed from small intestine. Distributed to all body tissue, high in cerebrospinal fluid. Stored in liver. Crosses placenta, breast milk. Metabolized in liver. Eliminated in urine. Use 👾 Deficiencies in vitamin B12 and folic acid. Both= megaloblastic anemia. Vitamin B12= pernicious anemia. Alert 😮 Vitamin B12: history of a sensitivity to vitamin B12, other cobalamins, or cobalt. Vitamin B12 should be used with caution when treating folic acid deficiency. Folic acid: undiagnosed anemia because the vitamin may mask pernicious anemia. Adverse Effects 💀 Vitamin B12: rare. Hypokalemia sometimes results. There is a slight risk of anaphylactic shock and sudden death. Blue-Print for Pharmacology Exam 2 2/17/2020 Folic acid: uncommon. The most serious potential adverse effect is bronchospasm. Administering the Medication 💉 Vitamin B12: use of the oral form is most convenient, and administration with food increases absorption. Not safe for IV administration. Folic acid: oral administration is preferable unless severe malabsorption is present, and people may take the vitamin without regard to food. Also available in subcutaneous, IM, or IV forms. Assessing for Therapeutic Effects 💖 Increased appetite, strength, and feeling of well-being; increased reticulocyte counts; and increased number of normal red blood cells, hemoglobin, and hematocrit. Prototype: Vitamin C (ascorbic acid) Pharmacokinetics Use 🔬 Absorbed from GI tract. Crosses placenta, enters breast milk. Metabolized in liver. Eliminated by kidneys. 👾 Prevention and treatment of scurvy. Deficiency. Alert 😮 Dialysis removes vitamin C, and patients receiving dialysis require vitamin C replacement. Patients with renal failure: imperative to avoid large doses of vitamin C because of impaired urinary excretion. Adverse Effects 💀 Abdominal cramps, nausea, vomiting, and diarrhea. Blue-Print for Pharmacology Exam 2 2/17/2020 Contraindications: prone to kidney stones, glucose-6-phosphate deficiency or sickle cell anemia. Administering the Medication 💉 Available in various oral forms. Oral solutions may need mixing with food. Effervescent tablets may need dissolving in water immediately before use. Parenteral forms are also available. Assessing for Therapeutic Effects 💖 Decreased or absent malaise, irritability, and bleeding tendencies. Class: Minerals Prototype: Iron- ferrous sulfate (Feosol) Pharmacokinetics 🔬 About 10% to 15% of ingested dietary iron is absorbed. Stored in the small intestine (and in certain other cells) as ferritin as well as in the liver. Crosses the placenta. Not metabolized. Eliminated daily in urine, sweat, sloughing of intestinal mucosal cells, excreted in feces. Use 👾 Supplement during periods of increased iron use and as treatment for iron deficiency. Alert 😮 Contraindications to ferrous sulfate include peptic ulceration, ulcerative colitis, regional enteritis, and repeated blood transfusions. Vitamin C increases iron absorption. Adverse Effects 💀 GI discomfort, nausea, constipation, diarrhea, and black stools. Liquid forms of iron may temporarily stain the teeth. In iron overload, excess iron is deposited in the heart, liver, and endocrine glands resulting in organ damage and, if untreated, death. Blue-Print for Pharmacology Exam 2 Administering the Medication 2/17/2020 💉 Take iron tablets or capsules before meals, with 8 ounces of water or juice, if tolerated. Better absorbed if taken on an empty stomach. With liquid preparations, it is necessary to dilute them, take with a straw, and then rinse the mouth afterward to prevent temporary staining of teeth. Assessing for Therapeutic Effects 💖 Increased vigor and feeling of well-being, improved appetite, less fatigue, and increased red blood cells, as well as hemoglobin, hematocrit, and reticulocyte count. Therapeutic effects are usually evident within a month. Other drugs: Iron dextran (Dexferrum, INFeD) is a parenteral form of iron useful for treating iron deficiency anemia when oral supplements cannot be used. Risk of anaphylactic reactions and death. Iron sucrose (Venofer) is a parenteral iron supplement given by IV infusion. This supplement is indicated for patients with chronic kidney disease who are not on dialysis and for those who are peritoneal dialysis dependent or hemodialysis dependent. Prototype: potassium chloride or KCl Pharmacokinetics Use 🔬 Absorbed from GI tract. Level maintained by kidneys. 👾 Prevent or treat hypokalemia. Replace chloride in patients with hypochloremic metabolic acidosis. Alert 😮 Caution is necessary in cardiac disease or renal impairment. Intravenous (IV) potassium chloride is indicated when a patient cannot take an oral preparation or has severe hypokalemia. It is essential to never give undiluted drug by the IV route or give it by the IV push route. Blue-Print for Pharmacology Exam 2 Adverse Effects 2/17/2020 💀 Nausea, vomiting, abdominal pain, and diarrhea. Adverse effects of IV potassium include postinfusion phlebitis at the IV site. Overdosage with oral or IV forms or rapid infusion of IV preparations produces hyperkalemia (greater than normal amount of potassium in the blood), dysrhythmias, heart block, cardiac arrest, respiratory paralysis, and death. Administering the Medication 💉 Take oral preparations with or after meals; this decreases gastric irritation. It is necessary to mix oral liquids, powders, and effervescent tablets in at least 120 mL of water, juice, or carbonated beverage to disguise the taste. Adjuvant Minerals: Magnesium: useful for mild hypomagnesemia. Oral magnesium salts may cause diarrhea. Contraindications to magnesium include impaired renal function or being comatose. Oral preparations of magnesium oxide or hydroxide act in 3 to 6 hours, and are excreted in urine. With parenteral magnesium sulfate, IM injections act in 1 hour and last 3 to 4 hours; IV administration produces immediate action that lasts 30 minutes. Zinc: given orally as a dietary supplement to prevent or treat zinc deficiency. Adverse effects of zinc sulfate are dizziness, restlessness, nausea, vomiting, gastric ulcers, and diarrhea. Do not use intranasally. Multiple-Mineral-Electrolyte Preparations (Pedialyte): contain several electrolytes and a small amount of dextrose. Used to supply maintenance amounts of fluids and electrolytes when oral intake is restricted. Should not be mixed with other electrolyte-containing fluids, such as milk or fruit juices. Chapter 61 - Drug Therapy to Disorders of skin - 5 Questions Blueprint: Blue-Print for Pharmacology Exam 2 2/17/2020 Class: RETINOIDS Prototype: Isotretinoin (aka Accutane) (Absorica, Amnesteem, Claravis, Myorisan) 🥕🥕🥕🥕 Vitamin A derivatives that are active in proliferation and differentiation of skin cells Use 🌋🌋🌋 Treatment of severe recalcitrant nodular acne that is unresponsive to other treatments in adolescents and adults. Pharmacokinetics Isotretinoin dissolves slowly in the GI tract, and the drug is then absorbed rapidly. It crosses the placenta. Isotretinoin is metabolized in the liver and excreted in equal amounts in the feces and urine. Action The antiacne effects of isotretinoin include suppression of sebum production, inhibition of comedone formation, and inhibition of inflammation. The drug normalizes keratinization, reversibly decreases the size of sebaceous glands, and makes sebum less viscous and less likely to plug follicles. The decrease in sebum results in the inhibition of the sebum-dependent bacterium P. acnes, which is a key promoter of inflammation in acne vulgaris. Adverse Effects 😱 Isotretinoin has severe adverse effects These adverse effects, which may limit its use, include: Reproductive effects: severe life-threatening congenital malformations and spontaneous abortions. Blue-Print for Pharmacology Exam 2 2/17/2020 👿 Psychiatric effects (serious): depression, psychosis, aggressive or violent behavior, and changes in mood; rarely, suicidal thoughts and actions have been reported. Dermatologic effects (most common): dryness and swelling of the lips (cheilitis), dry skin and mucous membranes, nasal dryness, epistaxis, dry mouth, conjunctivitis, peeling skin, skin fragility, rash, and pruritus GI effects (potential): nausea, vomiting, and, rarely, inflammatory bowel disease and pancreatitis. Musculoskeletal effects (common): arthralgia, myalgia (particularly with vigorous exercise), weakness, increased creatine phosphokinase (CPK), and back pain in some children and also bone abnormalities, decreased bone mineral density, and premature epiphyseal closure. Metabolic effects: hyperlipidemia (elevated triglycerides in 45% of patients, elevated total cholesterol, and low-density lipoprotein in 30% of patients: usually transient elevations) Other effects: decreased night vision, corneal opacities, hepatotoxicity, and bone marrow suppression. Contraindications Contraindications to isotretinoin include hypersensitivity to the drug, parabens (used as a preservative), vitamin A, or other retinoids, as well as pregnancy. As reported earlier, the FDA has issued a BLACK BOX WARNING ♦ stating that isotretinoin, in pregnancy category X, causes both spontaneous abortions and severe life-threatening congenital malformations. In addition, women of childbearing potential should not take isotretinoin unless they have had two negative pregnancy test results before beginning therapy, will begin drug therapy on the 2nd or 3rd day of the next menstrual period, and will comply with stringent contraceptive measures for 1 month before therapy, during therapy, and for 1 month after therapy. (iPLEDGE) Drugs That Increase the Effects of Isotretinoin Alcohol Increases triglycerides Corticosteroids Increase the risk of osteoporosis Phenytoin Increases the risk of osteomalacia Tetracycline Increases the risk of cerebri pseudotumor Vitamin A Produces toxic effects associated with isotretinoin 💀 Blue-Print for Pharmacology Exam 2 2/17/2020 Assessing for Therapeutic Effects The nurse assesses for a decrease in total cyst count. The ideal value is a 70% decrease. Assessing for Adverse Effects With oral retinoids the nurse observes for hypervitaminosis. Nausea and vomiting; headache; blurred vision, eye irritation, and conjunctivitis; skin disorders; musculoskeletal pain (any evidence of osteoporosis, osteopenia, or fractures); and depression and suicidal ideation are common signs of hypervitaminosis. Most adverse effects can be managed without stopping the drug. Also, the nurse monitors laboratory tests. It is important to conduct repeat tests (CBC, lipid profile, liver function tests) at 4 and 8 weeks. If the repeat tests are normal and the dose is stable, monitoring is no longer necessary. Other Drugs in the Class Adapalene and tazarotene are effective topical retinoids used to treat both non inflammatory and inflammatory acne. Adapalene is the only topical retinoid available without a prescription. A combination gel product (Epiduo, Epiduo Forte) containing adapalene and benzoyl peroxide is available by prescription. Traditionally, administration of most topical retinoids takes place at bedtime because of initial reports of drug instability in the presence of light; newer formulations are less affected by exposure to light. Patient Teaching Guidelines for Isotretinoin 💬 Understand that acne is not caused by dirt, that washing does not improve acne, and that vigorous scrubbing may worsen acne lesions. No evidence that acne is caused by eating chocolate or other foods. If you are a woman of childbearing age, it is essential that you adhere to all requirements of the iPLEDGE program. Use two forms of birth control. Adhere to mandatory pregnancy testing requirements. Take the drug with or shortly after meals. Report bone, muscle, or joint pain or visual disturbances immediately, as well as persistent headaches or GI pain. Report depression or suicidal thoughts immediately. Do not take oral vitamin A supplements. Avoid using abrasives, medicated soaps and cleansers, acne preparations containing peeling drugs, and topical products containing alcohol (e.g., cosmetics, aftershave). These products will exacerbate skin dryness and irritation. Avoid prolonged sun exposure. Use sun block. Do not donate blood during therapy and up t