Copy of PHARM DRUGS EXAM 1.pdf
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Salicylate: Aspirin (prototype) - Indication: treatment of mild to moderate pain, fever, inflammatory conditions; reduction of risk of TIA, or stroke; reduction of risk of myocardial infarction - Action: inhibits the synthesis of prostaglandins; blocks the effects of pyrogens at the...
Salicylate: Aspirin (prototype) - Indication: treatment of mild to moderate pain, fever, inflammatory conditions; reduction of risk of TIA, or stroke; reduction of risk of myocardial infarction - Action: inhibits the synthesis of prostaglandins; blocks the effects of pyrogens at the hypothalamus; inhibits platelet aggregation by blocking thromboxane A2 - Given orally or rectally; absorbed by stomach, metabolized liver, excreted in urine - Adverse effects: nausea. Vomiting, heartburn, epigastric discomfort, occult blood loss, dizziness, tinnitus, acidosis; salicylism toxicity, Reye’s syndrome in children and adolescents with viral illness, vasoconstriction → helps with reduction of blood clots - 20-25g for adult 4g in children→ toxicity s/s: tetany, confusion, pulmonary edema, CV, renal, respiratory collapse - Contraindications: pt will have surgery within a week, known allergy (NSAIDs, salicylates, tartrazine), pregnant, lactating bleeding disorders - Evaluate CNS status, eighth cranial nerve - Monitor lab tests: CBC, liver and renal function - Nursing conclusion - Impaired comfort related to CNS and GI effects, altered breathing because of toxicity - Older pt’s have a higher risk, of hepatotoxicity, kidney function, GI bleeding (ulcers), neurotoxicity (lethargy, confusion) NSAID: Ibuprofen (prototype) → propionic acid - Indicated for relief f s/s of RA and OA, and fever reduction; relief of mild-moderation pain; treatment of primary dysmenorrhea; fever reduction - Block COX1 and COX2 receptors - Pharmacokinetics: absorbed through GI tract, metabolized in liver and excreted in urine. Cross the placenta and cross into human milk - contraindications : allergy to NSAID, salicylates, celecoxib, pt with CV dysfunction or hypertension, peptic ulcer/GI bleeding, renal/hepatic dysfunction, pregnant or lactating - Adverse effects: headache, dizziness, somnolence, fatigue, rash, nausea, dyspepsia, bleeding, constipation, bone marrow suppression, MI, stroke// heartburn, GI bleeding, and peptic ulcer - ginkgo biloba, garlic and ginger, can increase risk of bleeding and so can ibuprofen// so LOOK AT SUPPLEMENTS - Drug-drug: decreased diuretic effect when drugs are taken with loop diuretics, inhibit beta blocker (metoprolol) effectiveness - IF DRUGS ARE COMBINED, WITH IBUPROFEN = REPORTED RISK OF LITHIUM TOXICITY - Be aware of alcohol intake and glucocorticoids (increases risk) NSAID: Ketorolac (can be given IM or IV, or orally)// acetic acid NSAIDS ARE MOST ASSOCIATED WITH GI IRRITATION AND BLEEDING - Renal impairment is especially risky for this drug, this medication should not be used if a pt has advanced renal disease - Short term management of pain in adults, topically to relieve ocular itching - Should be used only short-term (5 days or fewer) - Can be given PO or IM, switching to oral form as soon as possible - Increased risk of toxicity in older adults, so should be avoided if possible Acetaminophen (aka tylenol) DOES NOT TREAT INFLAMMATION - Treat moderate to mild pain, and fever in place of NSAID or salicylate - Extremely toxic in high doses// severe liver toxicity - 4 g/d for most pt’s/ → alc. Abuse and hepatic injury lower maximum dose - Pharmacokinetics: absorbed from GI tract, extensively metabolized in liver, excreted in urine// available IV for ppl older than 2 yrs old if oral not possible - ANTIDOTE: acetylcysteine - Drug-drug: increased risk of bleeding with oral anticoagulants, carbamazepine, rifampin - Indications: treatment of mild to moderate pain, fever, signs and symptoms of the common cold, or flu; musculoskeletal pain associated with arthritis and rheumatic disorder. - Actions: works directly on hypothalamus to cause VASODILATION AND HEAT RELEASE, reducing fever, - Adverse effects: can cause liver failure and hepatotoxicity, rash, fever, chest pain, bone marrow suppression - Helps relieve musculoskeletal pain so OA - Contraindications And cautions: pregnancy and lactation; hepatic dysfunction or chronic alcoholism Antiarthritis: Gold Compound:- auranofin (prototype) - Rheumatic inflammatory conditions - Gold compound// prevent and suppress arthritis in selected patients with rheumatoid arthritis - Used for pt who doesn’t respond to NSAIDs - Gold salts: gold is taken up by macrophages, inhibiting phagocytosis; lysosomal enzymes are inhibited → available in auranofin - May not prevent further damage; needs to be used early in disease - prevent some arthritis and synovitis - Pharmacokinetics: absorption varies based on route of administration; widely distributed throughout the body; excreted in the URINE AND FECES(specifically auranofin) ; crosses placenta and enters human milk - Barrier contraceptives should be recommended→ another form of feeding infant - Contraindications: allergy to gold, severe diabetes, congestive heart failure, hypertension, recent radiation, pregnant or lactating, toxic levels of heavy metals, blood dyscrasia bc of bone marrow suppression - Adverse effects: bone marrow suppression, renal toxicity, dermatitis, nausea, vomiting, stomatitis, hepatitis, rashes - Penicillamine, antimalarials, cytotoxic drugs, or immunosuppressive agents other than low-dose corticosteroids DMARD: Etanercept (prototype) - Treats arthritis, especially RA, aggressively affects inflammation process - Adverse effects could be severe or life threatening - Dr. pick DMARDs early to alter inflammation process - TNF blockers: are biological// release cytokines that cause death of tumor cells - MUST BE GIVEN SUBQ - Used for treatment of RA, polyarticular juvenile arthritis, psoriatic arthritis, plaque psoriasis, and ankylosing spondylitis - Contraindications: anyone with acute infection, cancer, sepsis, tb, hepatitis, myelosuppression, or demyelinating disorders; pregnancy or lactation, hepatic and renal disorders; heart failure; latex allergies - BLACK BOX WARNING: DEVELOPMENT OF LYMPHOMAS AND OTHER CANCERS→ so pt must be screened accordingly - Adverse: fatal reacts with pt who have cancer and lymphoma(don't give it to pt that already has it either), demyelinating disorders - ex. Dementia, MI, heart failure, hypotension (so don’t give it to someone that is already hypotensive) → effects are SERIOUS AND FATAL CONDITIONS - Drug-drug interactions: Immunosuppressant drugs; live vaccines - Other dmards: allergy to drug or animal products, pregnant, lactating, acute inf. Antigout/hyperuricemia: Colchicine (prototype) - Seen with flare ups (treat gout attacks) - Caused by build up of uric acid crystals in the joints - Gouty arthritis: occurs when uric acid crystals are deposited in kidneys and joints, causing inflammation and pain - Pharmacokinetics: absorbed orally; administration with food makes no difference - Contraindications: used with caution and requires dose reduction in pt’s with severe renal and hepatic disease (hemodialysis patients need dosage adjustment) - Indications: treatment of gout flares and Familial Mediterranean fever (FMF) - Actions: prevent of actions on neutrophils that facilitate inflammation - Adverse: GI disturbances (may need do take with antidiarrheal), nausea, vomiting, abdominal pain, muscle pain and RHABDOMYOLYSIS (CAUSING COCA COLA COLORED URINE), blood dyscrasias - Elevated CK in rhabdomyolysis Antigout/hyperuricemia: Allopurinol - Designed to lower blood levels of uric acid in symptomatic pt’s. - for treatment - Pharmacokinetics: absorbed orally, excreted renally and via feces, GIVEN PO - Contraindications: discontinue if rash or allergic reaction, renal insufficiency, pt receiving thiazide medications (pt may have increased gout attacks when starts, so may be put on colchicine prophylactically ) - Indication: treatment of gout and symptomatic hyperuricemia - Adverse effects: fever, rash, hepatic and renal dysfunction, nausea, vomiting, increase in gout attack - Drug-drug: may slow down metabolism of warfarin and increase risk of bleeding - PT/INR levels need to be monitored! Immune stimulants// Interferons Interferon alfa-2b (prototype)// treat various cancers and warts - Absorbed well in sub q or IM, takes some time to work - Indications: hairy cell leukemia, malignant melanoma, AIDS-related Kaposi, sarcoma, chronic Hep B and C, follicular lymphoma, intralesional treatment of condylomata acuminata in pt 18 or older - Actions: inhibits the growth of tumor cells and enhances immune response - Contraindications: pregnancy and lactation, use with caution if cardiac disease with myelosuppression, and with CNS dysfunction (also reactions at the site) - related to immune or inflammatory reaction that is being stimulated - Other common effect: headache, dizziness, bone marrow depression, depression and suicidal ideation, photosensitivty, liver impairment (GET FLU LIKE SYNDROME), monitor for suicidal thoughts - Drug-drug: theophylline; zidovudine or other myelosuppressive treatment Immune stimulant// interleukins Aldesleukin // used to treat specific cancers - Indications: metastatic cell carcinoma in adults, treatment of metastatic melanomas - Actions: activates human cellular immunity and inhibits tumor growth through increase - Rapidly distributed after injection; primarily excreted by the kidneys - Assess mental status, and cardiac function, usually faster rhythm and CNS changes, - Adverse effects: hypotension, itching GI issues, GI bleeding, bone marrow suppression may also occur, fever chills and pain, sinus tachycardia, arrhythmias, pruritus, nausea, anorexia, respiratory difficulties - Drug-drug: concurrent use with medications that are either cardio or neurotoxic, other antineoplastic medications Immune stimulants// colony stimulating factors Filgrastim - Help with neutrophil production if pt has bone marrow suppression ex. Bone marrow transplant, receiving chemotherapy - Increase production of WBC, decrease neutropenia associated with bone marrow transplants and chemotherapy - Help treat many blood related cancers - Actions: increase production of neutrophils in bone marrow - Pharmacokinetics: given IV or subq, metabolism and excretion unknown - Adverse effects: GI effects, dermatitis, anorexia, alopecia, deep bone pain, stomatitis - Contraindications: allergic to anything in drug, caution with pregnancy or lactation, pt with bone marrow cancer or sickle cell disease - Drug-drug interactions: increase in the myeloproliferative effects of sargramostim when combined with lithium or corticosteroids Immunosuppressant// immune modulator Thalidomide - Action and indication: inhibit the secretion of proinflammatory cytokines - Used to treat: multiple myeloma and myelodysplastic syndrome - Pharmacokinetics: slowly absorbed via GI, metabolism not known, excreted in urine - Usual indication: treatment of erythema, nodosum following treatment for leprosy, newly diagnosed multiple myeloma Immunosuppressant// T and B cell suppressors Cyclosporine (prototype) CANT HAVE WITH GRAPEFRUIT JUICE - Indications: often be used with someone who has had an organ replacement, or organ transplant , or sometimes RA or psoriasis - Pharmacokinetics: PO or IV, metabolized in liver, excreted in bile and urine - Adverse effects: tremors, hypertension, gingival hyperplasia (need good mouth care), renal dysfunction, diarrhea, hirsutism, acne, bone marrow, suppression, interleukin receptor antagonist, pulmonary edema, - DEVELOP NEOPLASM, don’t give it to pt who has cancer or tumor!! - Assess pt for this before giving it → get baseline EKG - Drug-drug: Other drugs that are hepatotoxic or nephrotoxic Immunosuppressants// T & B cell Tacrolimus - Given PO or IV - Usual indications: prophylaxis for organ injection in lover, kidney, or heart transplants; topical treatment of atopic dermatitis - Pharmacokinetics: absorbed GI, extensively metabolized in liver, excreted in urine Immunosuppressants// T & B cell suppressors - Indications: used mostly with different types of lung cancer, renal, cervical, and ovarian cancer - Adverse effects: thrombotic events, pulmonary edema, headache, back pain, hypertension, can have hemorrhage, cytokine release syndrome, can have thrombotic events, GI perforation, surgery and wound complications - Drug-drug combination with other immunosuppressant drugs, others vary by drug; consult drug guide - Contraindications: allergy, pt who have previous administration of monoclonal antibody, not be used during pregnancy or lactating unless benefits weigh out risks MMR vaccine live → viral vaccine (prototype) - Indication: active immunization against measles, mumps, and rubella in children older than 15 months and adults - Actions: attenuated MMR viruses produce a modified infection and stimulate an active immune reaction wit the production of antibodies to these viruses - Given subq, metabolized in tissues, excretion unknown - Adverse effects: moderate fever, rash or burning or stinging, wheal or flare at site of injection; rarely, febrile convulsions and high fever, vision and hearing impairment; numbness, pain, and tingling; altered balance - Contraindications: known allergies, person is immunodeficient stopping them from making AB, pregnant women, - Delay vaccine for pt’s who are receiving immune globulin or who have received blood or blood products, history of immune deficiency, evidence of acute infection, - Assessment: evaluate range of motion of patient, perform physical assessment before beginning therapy Influenza vaccine dead - Beginning at age 6 months, then yearly after than - Contraindications: children younger than 6 months, people taking aspirin/salicylates, people with severe allergies, previous bad reaction to flu vaccine Immune globulin, IM - Indications: prophylaxis against hep A, measles, varicella, rubella; prophylaxis for pt with immunoglobulin deficiency - Provides passive, short-term immunity - Pharmacokinetics: IM, unknown; metabolized in the tissues; excretion unknown - Adverse effects: tenderness, muscle stiffness at site of injection; urticaria, angioedema, nausea, vomiting, chills, fever, chest tightness - Contraindications: someone with a history of severe immunoglobulin sensitivity or with other ingredients being used, thrombocytopenia or coagulation disorders, pregnant women, previous exposure to serum (hypersensitivity worse after exposure again) TDAP (Tetanus, Diphtheria, and Pertussis,) dead - Occurance of encephalopathy within 7 days prior dose of the vaccine, a previous dose or vaccine component can cause a severe allergic reaction, such as anaphylaxis - Contraindications; Has had an allergic reaction after a previous dose of any vaccine that protects against tetanus or diphtheria, or has any severe, life-threatening allergies. Has ever had Guillain-Barré Syndrome Aminoglycosides// Gentamicin (broad spectrum) → bactericidal (prototype) - Used primarily for aerobic-negative bacilli// can be toxic so have been replaced recently - Used for treatment of serious G- infections ex. urinary tract infection, pyelonephritis - Available ophthalmic, topical, IV, IM, intrathecal - Indications: treatment of serious infectious caused by susceptible bacteria - Inhibits protein synthesis in susceptible strains of G- bacteria, disrupting functional integrity of cell membrane and causing cell death - Pharmacokinetics, IM, IV → excreted in urine - Adverse effects: hypersensitivity, sinusitis, dizziness, rash, fever, risk of nephrotoxicity and ototoxicity - Hypersensitivity: subsequent sinusitis, report change in mucus, pain in face or teeth, dizzy, fever, can cause GI disturbance and superinfections - Look for changes in urine, can get immune suppression bc of bone marrow suppression, stomatitis, - Contraindications and cautions - Known allergies to any aminoglycosides, renal disease, preexisting hearing loss, myasthenia gravis, or parkinsonism - Use caution during pregnancy; use lower doses with pt who have renal impairment, RISK FOR NEPHRO AND OTOTOXICITY - Drug-drug - Synergistic bactericidal effect with penicillins or cephalosporins - Use caution with nephrotoxic medications - Increased neuromuscular blockade with certain drugs ex. Someone who is going in for surgery, or intubated - Assess for pre existing hearing loss, pregnant, lactating, myasthenia gravis Carbapenem// Ertapenem (prototype) → broad spectrum - Works on both gram bacteria - Bactericidal, inhibits cell membrane synthesis, leading to cell death - Indications: Treatment of serious infectious, treatment of serious intra-abdominal, urinary tract, skin, bone joint, and gynecological infections, community acquired pneumonia - Pharmacokinetics: Rapidly absorbed IM, given IV a lot → widely distributed, crosses placenta and human milk - Contraindications: known allergy to carbapenems, or beta lactams// use with caution in pregnant and lactating women// TEST RENAL FUNCTION REGULARLY - Adverse effects: pseudomembranous colitis (C.diff) → leading to electrolyte imbalance, superinfection, headache, dizziness, nausea, pain at injection site - Drug-drug interactions: consider alternative if pt is taking valproic acid, avoid concurrent use of imipenem with ganciclovir Cephalosporins→ Cefaclor (prototype) → broad spectrum second gen. - Type of beta-lactam antibiotic, Similar to penicillin in structure and activity// if they are allergic to one, they are prob allergic to the other - Indications: treatment of respiratory, dermatological, urinary tract, and middle ear infection caused by susceptible strains of bacteria - Action: inhibits synthesis of bacterial cell walls, causing cell death in susceptible bacteria - Pharmacokinetics// given ORAL - Primarily excreted unchanged in urine, eliminated primarily by liver, cross placenta and enter human milk (look at liver function, look for signs of renal dysfunction, liver AST and ALT, jaundice) - Contraindications: allergies to cephalosporins, penicillins, hepatic or renal impairment, pregnant or lactating, ONLY USE WHEN NEEDED bc of change of resistance - Given IM but hurts, usually given IV - Adverse effects: nausea, vomiting, diarrhea, rash, superinfection (fungal growth on tongue, yeast infection), bone marrow depression, pseudomembranous colitis - Drug-drug: increased nephrotox if used with aminoglycosides, increased possible bleeding with warfarin - Assess for: currently pregnant, renal disease, examine skin for rash or lesions, do culture and sensitivity - CHECK BUN AND CREATININE FREQUENTLY - Bactericidal and bacteriostatic depending on dose and drug Cephalosporins// Cephalexin (first gen) - Most are administered IV or IM because of decreased absorption from GI tract - Each subsequent gen is more likely to reach cerebrospinal fluid, less susceptible to destruction of beta-lactamase, more effective against G- organisms and anaerobes - Dosage route (according to textbook, PO) - Indication: treatment of respiratory, skin, bone, and GU infections; used for otitis media in children Cephalosporins// Ceftriaxone (third gen) - Given IV or IM - Indications: treatment of moderate to severe skin, urinary tract, and respiratory tract infections; pelvic inflammatory disease; intra-abdominal infections; peritonitis; septicemia; bone infections; CNS infections; preoperative prophylaxis - Pharmacokinetics: eliminated primarily by the liver - Frequently monitor BUN and creatinine levels - TEACH PT HOW TO MONITOR FOR BLOOD LOSS EX. BLEEDING GUMS, EASY BRUISING Cephalosporins// Cefepime (fourth gen) - Given IM or IV - Indications: treatment of moderate to severe skin, urinary tract, and respiratory tract infections - Active against G-/ G+ organisms Fluoroquinolones// Ciprofloxacin (prototype) → broad spectrum - bactericidal// interfere with action of DNA enzymes, leading to cell death// susceptible strains in G-/G+ - Indications: treatment of respiratory, dermatological, urinary tract, ear,eye,bone, and joint infections; treatment after anthrax exposure, typhoid fever, plague - **prolong QT interval// drug can cause heart conduction to slow down, end up with torsades:ventricular tachycardia —> given IV might get EKG - Look out for bruising or petechiae - Indications: treatment of respiratory, dermatological, urinary tract, ear, eye, bone, and joint infections; treatment after anthrax exposure, typhoid fever, plague - Pharmacokinetics: metabolized in liver, excreted in bile and urine - Adverse effects: headache, dizziness, hypotension, nausea, vomiting, diarrhea, fever, rash// PROLONGED QT INTERVAL - known allergy, pregnant or lactating pt (in specific circumstances), renal dysfunction, liver dysfunction, c.diff, associated with damage to developing cartilage, interfere with thinning blood drugs - Adverse effects - Most serious: tendonitis, tendon rupture, peripheral neuropathy, CNS, prolonged QT interval, C. Diff, liver toxicity - Drug-drugTherapeutic effect decreased with iron salts, sucralfate, multivitamins, calcium, or magnesium supplements, antacids, drugs that increase QT interval: warfarin NSAID Fluoroquinolones// Levofloxacin - Available on oral and IV forms - PO or IV - Indications: treatment of respiratory, urinary tract, skin, and sinus infectious caused by susceptible G- bacteria in adults; treatment after exposure to anthrax, plague - REDUCE DOSE IN RENAL IMPAIRMENT Penicillins// Amoxicillin (aminopenicillins) → (prototype) - More narrow spectrum - Bactericidal, interfere with the ability of susceptible bacteria to build their cell walls - INTERFERE WITH STREP AND STAPH - Indications: Antipseudomonal penicillin have widest spectrum - Indications: treatment of infectious diseases caused by susceptible strains of bacteria, and treatment of helicobacter infections as part of combination therapy. Off label uses include post exposure prophylaxis for anthrax and prophylaxis for endocarditis - Pharmacokinetics: absorbed from GI, excreted unchanged in urine, enter human milk - Contraindications: allergies to penicillin and cephalosporins, renal disease, pt who are pregnant or lactating - Adverse effects GI, superinfections, glossitis, stomatitis, bone marrow suppression, superinfections, lethargy - Drug-drug interactions: parenteral aminoglycosides - Hairy tongue= secondary, opportunistic infection Penicillins// Amoxicillin- Clavulanate, aka Augmentin (aminopenicillin) - GIven PO - Treatment of lower respiratory tract, acute bacterial otitis media, sinusitis, skin and skin structure, and urinary tract infections Penicillin// natural Penicillin - some pt who have valves or heart replaced, take it before they get dental work done - Given PO, used prophylaxis for bacterial endocarditis, Lyme disease, UTIs Penicillin// Piperacillin-tazobactam (antipseudomonal) - Given IV - Treatment of infections caused by intra-abdominal, Urinary tract, gynecological, lower respiratory, skin and skin structure, and bone and joint infections. - Treatment of septicemia and uncomplicated gonococcal urethritis. Prophylaxis against infection from surgical procedures Sulfonamides **broad → sulfa // Trimethoprim- sulfamethoxazole/ cotrimoxazole - Drugs that inhibit folic acid synthesis in susceptible bacteria //Medications: bactrim// pt who have E.coli, influenza, UTI → bacteriostatic - Treatment of both Gram - Inexpensive and effective treatment for UTIs and trachoma - teratogenic MAKE SURE TO TEACH ABOUT CONTRACEPTIVES - Contraindications and cautions - Known allergy to any sulfonamide, or to thiazide or loop diuretics, Pregnancy and lactation, Renal disease or history of kidney stones, Older adults - Drug-drug: antidiabetic, medications that increase hyperkalemia risk, cyclosporine (increases risk of nephrotoxicity) - Indications: treatment of urinary tract infection, acute otitis media in children, exacerbations of chronic bronchitis in adults, traveler’s diarrhea in adults - Given oral, excreted in urine - Adverse effects: SJS, center perception issues, photophobia hepatocellular necrosis, hematuria Tetracycline// Tetracycline - Bacteriostatic - Inhibit protein synthesis in wide range of bacteria, TOXIC TO HUMANS AT HIGH CONCENTRATIONS - Pharmacokinetics: absorbed GI tract, concentrated in liver, excreted unchanged in the urine, cross placenta and pass into human milk - Contraindications: known allergy to tetracycline, pregnancy and lactation, children under 8 years old (can permanently stain teeth), can lead to bone marrow suppression → leading to superinfection - Indications: treatment of various infections caused by susceptible strains of bacteria acne; when penicillin is contraindicated for eradication of susceptible organisms - Given ORAL - Adverse effects: PHOTOSENSITIVITY, DISCOLORATION OF TEETH due to inadequate calcification of primary teeth of fetus when used in ppl who are pregnant or of secondary teeth when used in children, - drug-drug interactions, concurrent tetracycline use, oral combinations that decrease absorption - administer on empty stomach with water Antimycobacterials// Isoniazid (prototype) - Given PO - treatment/prevention of M. Tuberculosis - Pharmacokinetics: Generally well absorbed from GI tract, metabolized in liver, excreted in urine, cross placenta and enter human milk - Contraindications: Known allergy to these agents, severe renal or hepatic failure, pregnancy - Drug-drug: combinations that increase risk of hepatotoxicity, histamine reactions - **pt could get peripheral neuropathy: numbness or tingling in extremities, also cause GI and hepatitis, hold medication if they already have liver failure - gynecomastia: abnormal breast tissue growth in men - Orange tint to body fluids** ex. Tears, urine - Indications: treatment of tb as part of combination therapy; prophylactic treatment of household members of recently diagnosed tb - Pharmacokinetics: ORAL, metabolized in liver, excreted in urine - Adverse: gynecomastia, lupus syndrome, nausea, vomiting, - Normal for it to cause organ stain to urine or tears Antimycobacterials// Ethionamide - Given PO, second-line treatment of M. Tuberculosis (antituberculosis drug) Lincosamides// Clindamycin (prototype ) - used in anaerobic infectious, pt with infection in joint spaces, or cant have penicillin, seen a lot with dental pt’s// does cross placenta, contraindication: hepatic impairment - Indications: treatment of serious infections caused by susceptible strains of bacteria, including some anaerobes; useful in septicemia and chronic bone and joint infections - Pharmacokinetics: oral, IM, IV, Topical// metabolized in liver, excreted in urine and feces - Adverse effects: nausea, vomiting, diarrhea, pseudomembranous colitis, bone marrow suppression Lipoglycopeptide// Vancomycin (prototype) - Vancomycin: used for SERIOUS LIFE THREATENING MRSA, broad spectrum to treat more serious infections - Indications: treatment of c. diff, enterocolitis caused by S. aureus - Pharmacokinetics: IV, no known metabolism; excreted in urine(IV) or feces (oral) - Adverse effects: abdominal pain, nausea, nephrotoxicity, hypokalemia, ototoxicity (PO or IV), C. Diff, phlebitis, flushing, sweating, hypotension (IV). - Oral for C. diff, given IV used more for systemic infections INCREASE QT INTERVAL→ cardiac dysrhythmia, hypokalemia**, don’t give it to pt already taking diuretics?, ototoxicity, phlebitis (looking for red line) can be HYPOTENSIVE Macrolides// Erythromycin (prototype) - indications : treatment of respiratory, dermatological, UTI, or GI infection caused by bacterial - Pharmacokinetics: Oral, IV - Adverse effects: abdominal cramping, vomiting, diarrhea, rash, superinfection, liver toxicity, risk of pseudomembranous colitis, potential for hearing loss with high doses and prolonged QT interval Oxazolidinones// Linezolid (prototype) - Indications: treatment of infections caused by resistant strains, pneumonias, skin and skin structure infections, diabetic foot infections. - Pharmacokinetics: Oral, IV// excreted in urine - Adverse effects: headache, dizziness, vomiting, diarrhea - a lot with diabetics that get foot ulcers, can get c. diff, thrombocytopenia, optic neuritis, big GI, and bone marrow suppression, hypertension, pseudomembranous colitis Monobactams// Aztreonam (prototype) narrow spectrum - lower respiratory, UTI, anaphylaxis can be a big one, can be given IV, IM - Indications: treatment of lower respiratory, dermatological, intra-abdominal, infections caused by susceptible strains of G- bacteria - Pharmacokinetics: given IM or IV, excreted, unchanged in urine - Adverse effects: nausea, vomiting, diarrhea, rash, superinfection, anaphylaxis, local discomfort at injection sites Influenza A and respiratory virus agents// Oseltamivir (prototype) - Indications: treatment of Influenza A and B in pt 2 weeks of age or older who have had symptoms no more than 48 hours. Prophylaxis of influenza A and B in patients 1 year and older - Inhibit viral enzyme in order to slow spread of virus - Route: Oral - Adverse effects: headache, nausea, rash, vomiting Herpes virus and cytomegalovirus agents// Acyclovir (prototype) - Indications: treatment of herpes simplex virus (HSV) 1 and 2 infections; treatment of severe genital HSV infections; treatment of HSV encephalitis; acute treatment of varicella-zoster viruses; ointment for the treatment of genital herpes infections; cream for the treatment of cold sores - Actions: inhibit viral DNA replication - Adverse effects: headache, vertigo, tremors, nausea, vomiting, rash nephrotoxicity, - Contraindications: allergy, renal dysfunction, someone with severe CNS disorders, pregnant and or lactating - Some drugs are highly toxic; extreme caution with pregnancy or lactation - Known allergies; renal disease, CNS disorders - Adverse effects: nausea, vomiting, headache, depression, paresthesia, neuropathy, rash, hair loss; renal dysfunction - Drug-drug: nephrotoxic drugs, zidovudine HIV and AIDS agents// Nevirapine (prototype) - Non Nucleoside reverse transcriptase inhibitors - Indications: treatment of HIV-1 infected patients who have experienced clinical or immunological deterioration, in combination with other antiretrovirals - Pharmacokinetics: oral, metabolized in liver, excreted in urine - Adverse effects: headache, nausea, vomiting, diarrhea, rash, liver dysfunction, chills, fever - Action: bind directly to HIV reverse transcriptase; blocking both RNA and DNA dependent DNA polymerase activities - Rapidly absorbed from the GI tract, metabolized in liver, excreted in urine/and or feces - Contraindications and cautions: pregnancy and lactation - Adverse effects: GI related; dizziness, blurred vision, headache, flu like syndrome (may be related to disease) - Drug-drug interaction: Delavirdine: antiarrhythmics, clarithromycin, dapsone, anti-TB drugs, calcium channel blockers, warfarin, quinine, Indinavir, saquinavir, dapsone - Efavirenz: midazolam, Rifabutin, Triazolom, ergot derivatives - St. john's wort HIV and AIDS// Zidovudine (prototype) - Nucleoside reverse transcriptase inhibitors - Actions: compete with naturally occurring nucleosides within the cell that the virus would use to build the DNA chain - Pharmacokinetics: rapidly absorbed form the GI tract, metabolized by liver, excreted in urine and or/feces - Contraindications and cautions: pregnancy and lactating - Pregnancy and breast or chestfeeding - Hepatic dysfunction: bone marrow suppression - Adverse effects: hypersensitivity, pancreatitis, hepatomegaly, neurological problems, bone marrow suppression - Drug-drug: tenofovir, lamivudine and zalcitabine, didanosine and antibiotics or antifungals, stavudine, and didanosine, other interactions - Indications: management of adults with symptomatic HIV infection in combination with other antiretrovirals; prevention of maternal-fetal HIV transmission - Pharmacokinetics: oral, metabolized in liver and excreted in urine - Adverse effects: headache, insomnia, dizziness, nausea, diarrhea, fever, rash, bone marrow suppression HIV and AIDS// Fosamprenavir (prototype) - Protease inhibitor - Action: block protease activity to render HIV particles unable to fuse with and inject itself into a cell - Pharmacokinetics: varies by particular drug - Contraindications and cautions: hepatic dysfunction, treatment with antidiabetic drugs - Adverse effects: GI effects, changes in liver function, elevated cholesterol and triglyceride levels, redistribution of fat, SJS - Drug- drug interactions: interact with many drugs; check drug guide - Indications: management of symptomatic HIV infection in adults in combination with other antiretrovirals - Pharmacokinetics: oral, metabolized in lover, and excreted in feces and urine - Adverse effects: headache, mood changes, SJS, redistribution of body fat (increase of fat to the face, back of neck, and upper back; thinning of arms and legs) HIV and AIDS// Enfuvirtide (prototype) - Fusion inhibitor - Prevents the fusion of the virus with the human cellular membrane - Given subq, metabolized in liver; recycled in tissues and not excreted - Contraindications and cautions: hypersensitivity to any drug component, pregnancy, breast or chestfeeding, lung disease - Adverse effects: insomnia, depression, peripheral neuropathy, nausea, diarrhea, pneumonia, injection site reactions - Indications: treatment of patients with HIV-1 who have experienced clinical or immunological deterioration after treatment with other agents, in combination with other antiretrovirals - Pharmacokinetics: given Subq, metabolized in live, tissues recycle the amino acids, not excreted - Adverse: headache, nausea, vomiting, diarrhea, rash, anorexia, pneumonia, cills, injection site reactions HIV and AIDS// Maraviroc (prototype) - CCR5 coreceptor antagonist - Blocks receptor site on cell membrane with which the HIV virus needs to interact to enter the cell - Pharmacokinetics: rapidly absorbed from GI tract, metabolized in liver, excreted primarily through feces - Contraindications and cautions: Hypersensitivity to any component of the drug, breast feeding, liver disease - Adverse effects: severe hepatotoxicity, CNS effects, URIs - drug-drug : changes in serum levels and toxicity when combined with cytochrome P-450 CYP3A inhibitors and inducers; St. John’s wort - Indications: combination antiretroviral treatment of adults infected with CCR5- tropic HIV-1 who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents - Pharmacokinetics: oral, metabolized in liver, excreted in feces and urine - Adverse: dizziness, paresthesia, nausea, vomiting, diarrhea, cough, URI, fever, musculoskeletal symptoms, hepatotoxicity HIV and AIDS// Raltegravir (prototype) - Integrase Strand Transfer Inhibitors - Inhibit the activity of the virus- specific enzyme integrase, an encoded enzyme needed for viral replication - Pharmacokinetics: rapidly absorbed from the GI tract, metabolized in liver, excreted in urine and feces - Contraindications and cautions: known hypersensitivity; risk for rhabdomyolysis or myopathy; pregnant - Adverse effects: liver failure, renal impairment; suicidal ideation, headache, dizziness, insomnia, weight gain - Drug-drug: decreased serum levels if combined with rifampin, St. Johns wort - Indication: combination with other antiviral agents for the treatment of HIV-1 infection in treatment experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents - Pharmacokinetics: oral, metabolized in liver, excreted in feces and urine - Adverse: headache, dizziness, nausea, vomiting, diarrhea, fever, rhabdomyolysis Anti- hepatitis B agents// Adefovir (prototype) - Inhibit reverse transcriptase in the Hep B virus and causes DNA chain termination - Pharmacokinetics: rapidly absorbed from GI tract, metabolized in liver and excreted in the urine - Contraindications and cautions: known allergy, renal impairment, severe liver disease, pregnancy, HIV infection (tenofovir alafenamide) - Adverse effects: headache, dizziness, nausea, diarrhea, and elevated liver enzymes, hepatomegaly with steatosis; renal impairment - Drug-drug interactions: increased risk for renal toxicity if these drugs are taken with other nephrotoxic drugs - Indications: treatment of chronic HBV in adults with evidence of active viral replication and either evidence of persistent elevations in alanine aminotransferase and aspartate aminotransferase or histologically active disease - Pharmacokinetics: oral, excreted in urine - Adverse effects: headache, asthenia, nausea, severe to fatal hepatomegaly with steatosis, nephrotoxicity, lactic acidosis, exacerbation of HBV when discontinued Antifungals Systemic antifungals// Fluconazole (prototype) - Indications: treat systemic and topical fungal infections - Bind to sterols and can cause cell death or interfere with cell replication depending on type of fungus and concentration of drug - Pharmacokinetics: varies by drug - Contraindications: hepatic and renal dysfunction, endocrine or fertility problems, pregnancy or lactation - Adverse effects: liver toxicity; severe effects on fetus or nursing baby - Drug-drug: Many; consult drug guide - Indication: treatment of oropharyngeal, esophageal, and vaginal candidiasis, prophylaxis to decrease the incidence of candidiasis in bone marrow transplants - Pharmacokinetics: oral or IV, metabolized in liver, excreted in urine - Adverse: headache, nausea, vomiting, diarrhea, abdominal pain, rash Topical antifungal// clotrimazole (prototype) - Indications: local treatment of a variety of mycoses of the skin and mucous membrane - Actions: work to alter the cell permeability of the fungus, preventing replication and causing fungal death - Pharmacokinetics: not absorbed systemically - Contraindications: limited to known allergy to any of these drugs; open lesions - Adverse effects: irritation, burning, rash, and swelling at the site: GI, hepatic, urinary effects when used as suppository - Indication: treatment of tinea cruris, tinea pedis, tinea corporis - NOT ABSORBED SYSTEMICALLY, PHARMACOKINETICS IS UNKNOWN - Adverse effects: troche: nausea, vomiting, abnormal liver function tests. Topical: stinging, redness, urticaria, edema. Vaginal: lower abdominal pain, urinary frequency burning or irritation in sexual partner Antiprotozoal agents - Children: follow up with precautions, hand washing, antiseptic, think about potential with hepatic issue and if they are pregnant and traveling, need to be cautious - prophylaxis for malaria, so traveling to certain areas of world, may be given - Visual and auditory disturbances, retinal changes, hypotension, nausea, vomiting, diarrhea// GI AND SENSORY ISSUES Chloroquine (prototype) - Indications: treatment and prophylaxis of acute attacks of malaria - Pharmacokinetics: oral, metabolized in liver, excreted in urine - Adverse effects: visual and auditory disturbances, retinal changes, hypotension, nausea, vomiting, diarrhea - Contraindications: pt with liver disease, or alcoholism, lactating mother - Drug-drug: antacids may reduce absorption of chloroquine, ampicillin may have reduce bioavailability when used with these medications Metronidazole (prototype) AKA flagyl - “Flagyl has no friends”// When hanging as IV anti protozoan, not able to be given with other medication - NEUROLOGICAL CNS ISSUES// headache, dizziness, **seizures, ataxia (difficulty with muscles) - ALCOHOL IS VERY CONTRAINDICATED, also warfarin, disulfiram - Make sure pt tells you if they are having other infections ex. Whitening of the tongue - METALLIC TASTE IN MOUTH (SIDE EFFECT), DARKENING OF THE URINE (ALSO NORMAL, JUST EDUCATE THEM ) - Excreted in urine and feces, neurologic effects - Contraindications and cautions: known allergy or hypersensitivity, pregnancy, CNS disease, hepatic disease, renay dysfunction - Pharmacokinetics: oral, IV, metabolized in liver, excreted in urine and feces - Adverse effects: headache, dizziness, ataxia, seizures, nausea, vomiting, metallic taste diarrhea, darkening or urine (this is a harmless effect) Antihelminthic Mebendazole (prototype - Indications: treatment of diseases caused by pinworms, roundworms, whipworms, and hookworms - Action: interferes with ability to use glucose, leading to inability to reproduce and cell death - Pharmacokinetics: very little is absorbed systemically, metabolized by liver, and most is excreted unchanged in feces - Contraindications: known allergy, pregnancy, and lactation, renal and hepatic disease - Adverse effects: abdominal discomfort, diarrhea, pain; few other effects - Drug-drug: consult drug guide - PT teaching: keep nails short, especially with pinworms, good hygiene(shower in AM) - Indication: treatment if whipworm, pinworm, roundworm, and hookworm - Pharmacokinetics: oral, metabolized in liver, excreted in feces - Adverse effects: transient abdominal pain, diarrhea, fever ASPIRIN IS ANTIPLATELET Antiplatelet// Clopidogrel - Antiplatelet: stop clumping of platelet, avoiding clot from occurring - Given PO - Indications: treatment of patients who are at risk for ischemic events, pt with history of MI, peripheral artery disease, or ischemic stroke; and pt’s with acute coronary syndrome - Pharmacokinetics: metabolized in liver, excreted in urine, tend to enter human milk - Contraindications: presence of allergy, caution with pt who has bleeding disorder, or actively bleeding, recent surgery, caution during pregnancy and lactation - BOX WARNING FOR PEOPLE WHO POORLY METABOLIZE THE LIVER ENZYME CYP2C1 - Drug-drug: risk of excessive bleeding increases if any of these drugs are combined with another drug that affects blood clotting Anticoagulant// Heparin → look at aPPT/ PTT - Interfere with clotting cascade and thrombin formation - Indications: prevention and treatment of venous thrombosis and PE, treatment of AF with embolization, treatment of DIC, prevention of clotting in blood samples and heparin lock sets, adjunct in the treatment of MI and stroke - Pharmacokinetics: given IV or subq, metabolized in cells, excreted in urine - Adverse effects: bleeding, epidural or spinal hematoma, heparin- induced thrombocytopenia, hypersensitivity reactions, loss of hair, bruising, chills, fever, osteoporosis, suppression of renal function (with long timer use) - LOOK AT INR LEVEL AND MAKE SURE THEY ARE FOLLOWING UP WITH THEIR PROVIDER - Contraindications - allergy , conditions that could be compromised by increased bleeding tendencies - Warfarin: pregnancy (heparin is generally safer) - Contraindications: hemorrhagic disorders, recent trauma, spinal puncture, GI ulcers, intrauterine device placement, tb, indwelling catheters Anticoagulant// Enoxaparin - Sub q injection → dosing varies based on indication and renal function - Indication: prophylaxis of DVT in abdominal surgery, hip replacement, knee surgery etc. prophylaxis of ischemic complications of unstable angina and non-Q- wave MI Anticoagulant// Warfarin - Given PO→ dosing based on INR - Indication: treatment of pt with AF, artificial heart valves, or valvular damage (makes it more susceptible to thrombus and embolus formation ) - Causes decrease in production of Vitamin-K dependent clotting factors in liver - Given orally, but can also be given IV - Absorbed through GI tract, metabolized in lover, excreted in urine and feces - Contraindications:pt who are pregnant, unless need anticoag, due to artificial heart valve Thrombolytic// Alteplase (prototype) - Break down the thrombus that has been formed by stimulating the plasmin system ex. Pt who had MI, stroke - Given for pt who are having MI, acute pulmonary embolism, acute stroke - Action: convert plasminogen → plasmin: breaking down the clot// DISSOLUTION OF FORMED THROMBUS Know that it is going to cause bleeding - Pharmacokinetics: cleared from the body after liver metabolism, cross placenta; unknown if they enter human milk - Contraindications: allergy - Cautions: Any condition that could be worsened by dissolution of clots, pregnancy and lactation - Adverse effects: Bleeding, cardiac arrhythmias, hypotension, mental status change, Gi bleeding, hypersensitivity reaction - Cardiac monitor! - Monitor blood values: CBC, H&H, and platelets, and hypersensitivity (hives, can’t breath) - Indications: treatment of MI, acute PE, and acute ischemic stroke, restoration of function in occluded central venous access devices - Pharmacokinetics: IV, metabolized in plasma, excretion unknown - Adverse: bleeding, hypersensitivity Antihemophilic// Antihemophilic factor (prototype) - Intrinsic pathway, extrinsic pathway (854-855) - Intrinsic: looking at cascade of clotting leading to clot in injured vessel itself - Extrinsic: cascade of clotting factors outside the vessels - Platelet aggregation: could acclude vessel, leading to stroke or heart attack - IndicationL treatment of classic hemophilia to provide temporary replacement of clotting factors to correct or prevent bleeding episodes or to allow necessary surgery - Pharmacokinetics: IV, cleared from body by normal protein metabolism - Adverse effects: allergic reaction, stinging at injection site, headache, rash, chills, nausea Hemostatic agents// Aminocaproic acid (prototype) - Inhibit plasminogen activating substances - Systemic: prevent body-wide or systemic clot breakdown to prevent blood loss - Topical: for surface injuries that involve so much damage to the small vessels in the area that clotting does not occur and blood is slowly and continually lost - Contraindications: Can cause systemic effects, injury to kidneys, liver, and issues with cardiac system, excessive clotting - Drug-drug interactions: Heparin, oral contraceptives or estrogen - Indication: treatment of excessive bleeding resulting from hyperfibrinolysis, decrease need for platelet administration - Pharmacokinetics: oral, IV, excreted unchanged in urine - Adverse: dizziness, tinnitus, headache, weakness, hypotension, nausea, cramps, diarrhea, fertility problems, malaise, and elevated serum creatine phosphokinase - Contraindications: present of allergy, pt with acute DIC, cardiac disease, pregnancy and breastfeeding not recommended Erythropoiesis- stimulating agent// epoetin alfa - Pt who have chronic kidney disease → someone who is on dialysis, pt on chemo, pt who are on medications for HIV - Make sure pt has adequate levels of components required to make RBCs, including adequate iron - Given subq - Boxed warnings: increased risk of death, myocardial infarction, stroke, venous thromboembolism, thrombosis of vascular access, tumor progression or recurrence - Therapeutic actions: acts like the natural glycoprotein erythropoietin to stimulate the production of RBCs in the bone marrow - Indications: treats anemia associated with chronic renal failure or kidney disease, other indications specific to each drug → better than getting transfusions - Contraindications: uncontrolled hypertension (bc it causes hypertension), known hypersensitivity, no adequate studies in pregnancy or lactation, pt with certain blood disorders - Adverse effects: CNS effects, nausea, vomiting, diarrhea, CV symptoms, serious and increased risk of DVT when hemoglobin is higher than 11g/dL - Drug-drug: should never be mixed into solution with other drugs - Report painful lumps, swelling of legs Agents for iron deficiency// Ferrous sulfate (prototype) - Look for nausea, constipation in older adults (increase fluid intake), does cause GI upset, - Not absorbed with taken with antacids, eggs, milk, anything with calcium, coffee or tea - You do not want them to take it first thing in the morning, not with certain foods - Indications: increase iron - Pharmacokinetics: Primarily absorbed from the small intestine by an active transport system. Transported in the blood, bound to transferrin - Contraindications: allergies, hemochromatosis (build up iron in blood), anemias that are not iron deficiency anemias, normal iron balance, - peptic ulcer, colitis, or regional enteritis// bc can cause GI effects - Adverse effects: CNS toxicity with increasing serum levels, Oral iron: effects related to GI irritation Parental iron: severe anaphylactic reactions, local irritation, staining of the tissues, phlebitis - Drug-drug: antacids, substances with calcium and magnesium, tetracyclines, cimetidine, fluoroquinolones or tetracyclines, chloramphenicol, levodopa - CAN GET DARK TARRY OR GREEN STOOLS (USE STRAW CAN DISCOLOR/ stain teeth Agents used for megaloblastic anemia// Folic Acid (prototype) - necessary for production of DNA, RBC, WBC, platelets - Indications: treatment of megaloblastic anemia due to folate deficiency, malabsorption, or nutritional deficiency; prevention of neural tube defects - Pharmacokinetics: Oral, IM, subq, IV, metabolized in liver and excreted in urine - Adverse: allergic reactions, pain and discomfort at injection site Agents for megaloblastic anemia// Hydroxocobalamin (prototype) - Indications: treatment of Vitamin B12 deficiency; to meet increased vitamin B12 requirements related to disease, pregnancy, or blood loss; treatment of pernicious anemia - Pharmacokinetics: IM, metabolized in liver, excreted in urine - Adverse effects: itching, transitory exanthema, mild diarrhea, anaphylactic reaction, heart failure, pulmonary edema, hypokalemia, pain at injection site Agents used for sickle cell anemia - Indications: reduction of frequency of painful crisis and need for blood transfusions in adult patients with sickle cell anemia - Pharmacokinetics: oral, metabolized in liver and excreted in urine - Adverse effects: dizziness, headache, rash, erythema, anorexia, nausea, vomiting, stomatitis, bone marrow depression, cancer - Contraindications: being on antivirals may heighten adverse effects
