Nonsteroidal Anti-Inflammatory Drugs PDF

10/19/23, 4:01 AM Realizeit for Student Nonsteroidal Anti-Inflammatory Drugs As discussed in the introduction to this module, the mechanism of action of NSAIDs involves the blocking of COX enzymes. These drugs are classified into two types, or “generations.” Firstgeneration NSAIDs block both COX-1...

10/19/23, 4:01 AM Realizeit for Student Nonsteroidal Anti-Inflammatory Drugs As discussed in the introduction to this module, the mechanism of action of NSAIDs involves the blocking of COX enzymes. These drugs are classified into two types, or “generations.” Firstgeneration NSAIDs block both COX-1 and COX-2, and second-generation NSAIDs block only COX-2. Both first- and second-generation NSAIDs have the potential to cause serious cardiovascular thrombotic events. All NSAIDs are contraindicated in the setting of coronary artery bypass graft surgery. The nonsteroidal anti-inflammatory agents ibuprofen and indomethacin are used initially in treating patent ductus arteriosus. Propionic Acid Derivatives The propionic acid derivatives are NSAIDs that inhibit prostaglandin synthesis in both the central and peripheral nervous systems. The prototype is ibuprofen (Motrin, Advil). Pharmacokinetics Ibuprofen is 80% absorbed in the GI tract. Its onset of action is 1 hour, producing antipyretic effects, reaching a peak in 1 to 2 hours. The duration of action is 6 to 8 hours. Ibuprofen is metabolized in the liver and eliminated in the urine. A small amount of the medication is eliminated in biliary excretion. Action Ibuprofen blocks prostaglandin synthesis and modulates T-cell production. It inhibits the inflammatory cells by the process of chemotaxis to destroy the cells of inflammation. A firstgeneration NSAID, it blocks COX-1 and COX-2 but is more selective with COX-1. Use Ibuprofen is used to relieve mild to moderate pain, including dysmenorrhea (painful menstruation). It is also used to treat inflammation related to rheumatoid arthritis and osteoarthritis. In addition, it is effective in reducing fever. During initial attacks of acute gout, NSAIDs such as ibuprofen may be administered. Use in Older Adults Ibuprofen is relatively safe in therapeutic doses for occasional use as an analgesic or antipyretic in older people. The incidence of musculoskeletal disorders such as osteoarthritis is higher in older adults. However, the nurse should ensure that older adults taking ibuprofen on a long- https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 1/11 10/19/23, 4:01 AM Realizeit for Student term basis are evaluated for GI blood loss, renal dysfunction, edema, hypertension, and drug– drug or drug–drug disease interactions. A gastroprotective agent is recommended for patients at risk for upper GI bleeding. Use in Patients With Renal Impairment Ibuprofen can cause or aggravate renal impairment even though it is eliminated mainly by hepatic metabolism. By inhibiting prostaglandins that dilate renal blood vessels, it can decrease the blood flow in the kidneys. When renal blood flow is normal, the activity of these prostaglandins is limited. However, when renal blood flow is decreased, synthesis of these prostaglandins is increased, and they protect the kidneys from ischemia and hypoxia by antagonizing the vasoconstrictive effects of angiotensin II, norepinephrine, and other substances. Thus, in patients who depend on prostaglandins to maintain an adequate renal blood flow, the prostaglandin-blocking effects of ibuprofen result in constriction of renal arteries and arterioles, decreased renal blood flow, decreased glomerular filtration rate, and retention of salt and water. Ibuprofen can also cause kidney damage by other mechanisms, including a hypersensitivity reaction that leads to acute renal failure, manifested by proteinuria, hematuria, and pyuria. Biopsy reports usually indicate inflammatory reactions such as glomerulonephritis or interstitial nephritis. People at highest risk from the use of ibuprofen and related drugs are those with preexisting renal impairment, those older than 50 years of age, those taking diuretics, and those with hypertension, diabetes, or heart failure. Measures to prevent or minimize renal damage include avoiding nephrotoxic drugs when possible, treating the disorders that increase risk of renal damage, stopping the ibuprofen if renal impairment occurs, monitoring renal function, reducing dosage, and maintaining hydration. Use in Patients With Hepatic Impairment Ibuprofen is metabolized in the liver, requiring that the dosage of the medication be decreased in patients with hepatic problems. The maximum daily dosage of ibuprofen in patients with hepatitis is 2 g. Use in Patients With Critical Illness The FDA has issued a BLACK BOX WARNING ♦ stating that ibuprofen is contraindicated for the treatment of perioperative pain after coronary artery bypass graft. Use in Patients Receiving Home Care It is important for the home care nurse to instruct the patient about all aspects of administration of ibuprofen. Because the medication is available in OTC preparations with many trade names, patients may not realize that they are taking an ibuprofen-containing drug. Overdosing may occur. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 2/11 10/19/23, 4:01 AM Realizeit for Student Adverse Effects The GI adverse effects of ibuprofen are many: dry mouth, gingival hyperplasia, dyspepsia, heartburn, nausea, epigastric pain, constipation, and GI ulceration with occult blood loss. The genitourinary effects include nephrotoxicity, elevated blood urea nitrogen and creatinine, and edema. The respiratory adverse effects include dyspnea, bronchospasm, hemoptysis, and pharyngitis. In addition, anaphylactic reactions may also occur. The FDA has issued a BLACK BOX WARNING stating that NSAIDs cause an increased risk of serious cardiovascular thrombotic events, including stroke or myocardial infarction. Contraindications Ibuprofen is contraindicated in patients with a known allergy to NSAIDs and salicylates. Allergic reactions are more common in patients with rhinitis, asthma, chronic urticaria, and nasal polyps (Nursing, 2019). Nursing Implications Preventing Interactions Medications and herbs interact with ibuprofen, increasing or decreasing its effects (Boxes 16.8 and 16.9). BOX 16.8 Drug Interactions: Ibuprofen Drugs That Increase the Effects of Ibuprofen Anticoagulants Increase the risk of bleeding Codeine, oxycodone, and hydrocodone Have an additive analgesic effect Corticosteroids Have additive gastric irritant and possible ulcerogenic effects https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 3/11 10/19/23, 4:01 AM Realizeit for Student BOX 16.9 Herb and Dietary Interactions: Ibuprofen Herbs and Foods That Increase the Effects of Ibuprofen Alcohol Garlic, ginger, and ginkgo Feverfew Administering the Medication Ibuprofen is administered orally, and the total daily dose should not exceed 3200 mg. When administered intravenously, it should be diluted in a concentration of 4 mg/mL or less using 0.9% sodium chloride, 5% dextrose, or lactated Ringer's. The dilution remains stable for 24 hours. Prior to the administration of the intravenous preparation, the patient should be well hydrated. Researchers have reported that the rapid infusion of ibuprofen intravenously was safe and effective in treating pain. The maximum total serum amount of IV ibuprofen was twice that of oral ibuprofen. Assessing for Therapeutic Effects When ibuprofen is administered for pain, the nurse assesses for pain. The patient should report diminished pain on a pain scale. When the drug is administered for fever, the nurse records the patient's temperature every 2 to 4 hours. Reduced fever should occur. When the drug is administered for inflammation, the nurse notes anti-inflammatory effects, particularly in the joints related to arthritis. Decreased inflammation should occur. Assessing Adverse Effects The nurse assesses the patient for dyspepsia or GI bleeding, including hemoptysis or melena. He or she also assesses complete blood count and clotting times for signs of anticoagulation. In addition, the nurse assesses for signs and symptoms of hypersensitivity to ibuprofen, including rash and bronchospasm. Patient Teaching Box 16.10 presents patient teaching guidelines for ibuprofen. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 4/11 10/19/23, 4:01 AM Realizeit for Student BOX 16.10 Patient Teaching Guidelines for Ibuprofen Take this drug with food or liquid to decrease gastric irritation. Drink 2 to 3 quarts of fluid daily when taking this drug regularly. Report any signs of bleeding (e.g., nosebleed, vomiting blood, bruising, blood in the urine or stool), difficulty breathing, severe stomach upset, swelling, or weight gain to your health care provider. Opioid Agonists Morphine sulfate (Duramorph, Infumorph, Kadian, MS Contin, Mitigo), the prototype, is an opium alkaloid used mainly to relieve moderate to severe pain. A Schedule II–controlled drug, administration is most often oral or parenteral. Patient response depends on route of administration and dosage. Pharmacokinetics Morphine is well absorbed after oral (PO), intramuscular (IM), subcutaneous, and intravenous (IV) administration. PO formulations undergo significant first-pass metabolism in the liver, which means that PO doses must be larger than injected doses to have equivalent therapeutic effects. After PO administration of fast-acting (e.g., immediate release) formulations, peak activity occurs in about 60 minutes. After IV injection, maximal analgesia and respiratory depression usually occur within 10 to 20 minutes. After IM injection, these effects occur in about 30 minutes. After subcutaneous injection, morphine effects may be delayed up to 60 to 90 minutes. Morphine is extensively metabolized in the liver, and metabolites are excreted in urine. Morphine is about 30% bound to plasma proteins, and its half-life is 2 to 4 hours. The duration of action is 5 to 7 hours. Action Morphine relieves pain by binding to receptors in the brain, spinal cord, and peripheral tissues. When bound to the drug, receptors function like gates that close and thereby block or decrease transmission of pain impulses from one nerve cell to the next. The receptors also activate the endogenous analgesia system. The major types of receptors are mu, kappa, and delta. Most of https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 5/11 10/19/23, 4:01 AM Realizeit for Student the effects of morphine (analgesia; CNS depression, with respiratory depression and sedation; euphoria; decreased gastrointestinal [GI] motility; and physical dependence) are attributed to activation of the mu receptors. Analgesia, sedation, and decreased GI motility occur with activation of kappa receptors. The endogenous analgesia system involves the delta receptors, which may not bind with opioid drugs. Use The main indication for morphine is to prevent or relieve acute or chronic pain. Specific conditions for morphine include acute myocardial infarction, biliary colic, renal colic, burns and other traumatic injuries, postoperative states, and cancer. Health care providers usually give morphine for chronic pain, such as that associated with terminal cancer, only when other measures and milder drugs are ineffective. Other clinical uses of morphine include the following: Before and during surgery to promote sedation, decrease anxiety, facilitate induction of anesthesia, and decrease the amount of anesthesia required During labor and delivery (obstetric analgesia; note that morphine crosses the placenta) Treatment of GI disorders, such as abdominal cramping and diarrhea Treatment of acute pulmonary edema Treatment of severe, unproductive cough (codeine may be used) Unlabeled use: relief of dyspnea associated with acute left ventricular failure and pulmonary edema Use in Older Adults It is necessary to use morphine cautiously in older adults, especially if they are debilitated; have hepatic, renal, or respiratory impairment; or are receiving other drugs that depress the CNS. Older adults are especially sensitive to respiratory depression, excessive sedation, confusion, and other adverse effects. However, they should receive adequate analgesia, along with vigilant monitoring. Specific recommendations for use in older adults include the following: Start with low doses and increase doses gradually, if necessary. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 6/11 10/19/23, 4:01 AM Realizeit for Student Give morphine less frequently than in younger adults because the duration of action may be longer. Monitor carefully for sedation or confusion. In addition, monitor voiding and urine output because acute urinary retention is more likely to occur in older adults. Use in Patients With Renal Impairment Patients with renal impairment should take minimal doses of morphine for the shortest effective time because usual doses may produce profound sedation and a prolonged duration of action. Morphine produces an active metabolite that may accumulate in patients with renal impairment. Use in Patients With Hepatic Impairment Morphine is extensively metabolized by the liver; therefore, morphine may accumulate and cause increased adverse effects in the presence of hepatic impairment. Drug accumulation and increased adverse effects may occur if dosage is not reduced, especially with chronic use. Adverse Effects Morphine has widespread pharmacologic effects, especially in the CNS and the GI system. These effects occur with usual doses and may be therapeutic or adverse, depending on the reason for use. CNS effects include analgesia; CNS depression, ranging from drowsiness to sleep to unconsciousness; decreased mental and physical activity; respiratory depression; nausea and vomiting; and pupil constriction. Sedation and respiratory depression are major adverse effects and potentially life threatening. In the GI tract, morphine slows motility, and it may cause constipation and smooth muscle spasms in the bowel and biliary tract. Contraindications Contraindications and cautions are respiratory depression, acute or chronic lung disease, liver or kidney disease, prostatic hypertrophy, pregnancy, increased intracranial pressure and head injury, seizure disorders, or hypersensitivity reactions to morphine. Lactation is a consideration (it may be safer to wait 4 to 6 hours after opioid administration to nurse an infant). Additional contraindications may include Addison’s disease, severe alcoholism, and toxic psychosis. Nursing Implications Preventing Interactions Naloxone is known to reverse the effects of morphine. Herbs such as kava, valerian, and St. John’s wort may increase the sedative effect of morphine. The FDA has issued a BLACK BOX WARNING for the combined use of morphine and other opioid analgesics with the benzodiazepines and other drugs that depress the CNS. The risk of serious adverse reactions, including slowed or difficult breathing and death, has been reported. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 7/11 10/19/23, 4:01 AM Realizeit for Student Administering the Medication Although the dose of morphine can be titrated upward for adequate analgesia, unacceptable adverse effects (e.g., excessive sedation, respiratory depression, nausea, and vomiting) may limit the dose. With PO administration, patients may take the drug without regard to food. However, if GI upset occurs, food is acceptable. It is essential that PO forms are not broken or crushed. The nurse dilutes and administers IV doses slowly to minimize likelihood of adverse effects. It is necessary to monitor respiration closely in neonates. The antagonist naloxone should be readily available (see “Opioid Antagonists”). Other guidelines for morphine administration include: Assess for pain on a regular schedule around the clock (e.g., every 1 to 2 hours). It is important to use a consistent method for assessing severity, such as a visual analog or numeric scale. If the patient is able to communicate, the nurse asks about the location, severity, and so forth. If the patient is unable to communicate needs for pain relief, as is often the case during critical illnesses, the nurse must evaluate posture, body language, risk factors, and other possible indicators of pain. In patients with trauma and other critical illnesses, administer morphine by IV infusion over a prolonged period. Health care providers may also give the drug by transdermal patch or by epidural infusion, depending on the patient’s condition. For information about the use of PCA, see Box 49.2. As previously stated, the nurse administers morphine by the recommended routes (e.g., PO, IV, epidural) rather than IM injections, because IM injections are painful and frightening for children. For any child receiving parenteral medications, it is essential to assess vital signs and level of consciousness regularly. Assessing for Therapeutic Effects The nurse assesses for decreased pain (patient reports) and general feeling of well-being. The nurse ensures that the patient is free from adverse effects. Tolerance (the initial dose of a substance loses its effectiveness over time) occurs with morphine and other opioids. Assessing for Adverse Effects The nurse should assess for increases in respiratory distress, cardiac rhythm disturbances, and increasing somnolence. The FDA has issued BLACK BOX WARNING for all opioid analgesics because of the potentially fatal adverse effects of respiratory depression, coma, and death, as well as the risks of drug abuse and dependence. Assessing for pruritus and urticaria, which may indicate an allergic reaction, is also important. Sweating may be a sign of tolerance and dependence in some patients taking morphine. Box 49.4 presents measures to recognize and manage toxicity. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 8/11 10/19/23, 4:01 AM Realizeit for Student BOX 49.4 Recognition and Management of Toxicity With Opioid Use Acute toxicity or overdose can occur from therapeutic use or from abuse by drugdependent people. Overdose may produce severe respiratory depression and coma. The main goal of treatment is to restore and maintain adequate respiratory function. Managed by inserting an endotracheal tube and starting mechanical ventilation or by giving an antagonist, such as naloxone. Emergency supplies should be readily available in any setting where opioids are used. Patient Teaching Box 49.6 presents patient teaching guidelines for morphine sulfate and other opioids. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99af… 9/11 10/19/23, 4:01 AM Realizeit for Student BOX 49.6 Patient Teaching Guidelines for Opioid Analgesics General Considerations For acute episodes of pain that occur at irregular intervals, most opioids may be taken as needed; for acute pain that occurs daily and for chronic pain, the drugs should be taken on a regular schedule, around the clock. When a choice of pain-relieving medication is available, use the least amount of the mildest drug that is likely to be effective in a particular situation. Take only as prescribed. If desired effects are not achieved, report to your health care provider. Do not increase the dose and do not take medication more often than prescribed. Although these principles apply to all medications, they are especially important with opioid analgesics because of potentially serious adverse effects and because analgesics may mask pain for which medical attention is needed. Do not drink alcohol or take other drugs that cause drowsiness (e.g., some antihistamines, sedative-type drugs for nervousness or anxiety, sleeping pills) while taking opioids for pain. Combining drugs with similar effects may lead to excessive sedation and difficulty in breathing. Do not smoke, cook, drive a car, or operate machinery when drowsy or dizzy or when vision is blurred from medication. Sit or lie down at least 30 to 60 minutes after receiving an opioid by injection. Injected drugs may cause dizziness, drowsiness, and falls when walking around. If it is necessary to stand up, ask someone for assistance. If hospitalized, ask a health care provider about methods of pain management. For example, if anticipating surgery, ask how postoperative pain will be managed, how you need to report pain and request pain medication, and so on. It is better to take adequate medication and be able to cough, deep breathe, and walk around than to avoid or minimize pain medication and be unable to perform activities that promote recovery and healing. Do not object to having bed rails up or asking for assistance when receiving a strong narcotic analgesic. These are safety measures to prevent falls or other injuries because these drugs may cause drowsiness, weakness, unsteady gait, and blurred vision. Avoid constipation, a common adverse effect of opioid analgesics. It may be prevented or managed by eating high-fiber foods, such as whole-grain cereals, fruits, and vegetables; drinking 2 to 3 quarts of fluid daily; and being as active as tolerated. If you take these medicines for more than a few days, or if you are the caregiver for someone who takes them, ask a health care provider about a bowel program to prevent constipation. A possible regimen is a daily stool softener (e.g., docusate) and a daily or every other day laxative (e.g., bisacodyl), preferably started at the same time as the narcotic. Docusate and bisacodyl are available over the counter. Self-administration Take oral opioid analgesics with 6 to 8 ounces of water, with or after food to reduce nausea. Do not crush or chew long-acting tablets (e.g., MS Contin, OxyContin). The tablets are formulated to release the active drug slowly, over several hours. Crushing or chewing causes immediate release of the drug, with a high risk of overdose and adverse effects, and shortens the duration of pain-relieving effects. You may experience these side effects: nausea, loss of appetite (take the drug with food and lie quietly), constipation (notify your health care provider if this is severe; a laxative https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99… 10/11 10/19/23, 4:01 AM Realizeit for Student may help), dizziness, sedation, drowsiness, and impaired visual acuity (avoid driving or performing other tasks requiring alertness, visual acuity). Omit one or more doses if severe adverse effects occur, and report to a health care provider. Also, report a skin rash. Take these drugs exactly as prescribed. Avoid alcohol, antihistamines, sedatives, tranquilizers, and over-the-counter drugs. Do not take any leftover medication for other disorders, and do not let anyone else take your prescription. https://herzing.realizeithome.com/RealizeitApp/Student.aspx?Token=0Dn26kXyU%2f6F5gOCz4%2f2IcdpKuauTn1W0lrWmCsonBYnaQIwEDgwdbmVgOEy99… 11/11