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Pharmacology Kendi Lyles, Verna Meadows, Janet Olbert, Brooke Robinson and Olethea Tennyson July 18, 2009 OPIOID AND NONOPIOID ANALGESICS ACTIONS AND USES OF MEDICATION OPIOID CATEGORIES Natural Morphine Codeine Thebaine Video http://youtube.com/watch?v=9nQQzH4rH7o OPIOID CATEGORIES Semi-synthetic Hydromorphone Hydrocodone Oxycodone Oxymorphone Desmorphine Heroin Nicomorphine Dipropanoylmorphine Benzylmorphine Ethylmorphine OPIOID CATEGORIES Fully synthetic Fentanyl Pethidine Methadone Tramadol Propoxyphene Video http://www.youtube.com/watch?v=RCjIwHiKN4g OPIOID CATEGORIES Endogenous Opioid Peptides naturally produced by the body endorphins enkephalins dynophins endomorphins OPIOID ACTIONS Opioids work in two ways Attach to opioid receptors specific proteins on the surface of cells in the brain, spine and GI tract Work in the brain to alter the sensation of pain OPIOID USES Post-operative pain Cancer pain Non-malignant chronic pain Cough Diarrhea Loperamide does not cross the blood-brain barrier and only acts on smooth muscle (the digestive tract) OPIOID USES Painful wounds Topical morphine Detoxification Methadone and buprenorphine only Back, neck or joint pain Dental pain Painful diabetic neuropathy Migraines NONOPIOID CATEGORIES There are several different types of nonopioids they include acetaminophen, NSAIDS which are aspirin, Motrin and Advil and also naproxen. They are less potent than opioids. They are used to treat mild to moderate pain. Nonopioids are usually purchased over-thecounter, but (Cox-2 inhibitors require a prescription. NONOPIOID USES Nonopioids are effective for the dull, throbbing pain of headaches,dysmenorrhea which is menstrual pain, inflammation, minor abrasion, muscular aches and pain, and mild to moderate arthritis. Most analgesics also have an antipyretic effect and will lower an elevated body temperature. Some, such as aspirin, have antiinflammatory and antiplaelet effects as well. NSAID’S All nonsterioial anti-inflammatory drugs have an analgesic effect as well as an antipyretic and anti-inflammatory action. Some examples of NSAIDS are aspirin, ibuprofen which include (Motrin IB, nuprin, Advil, medipren) and naproxen(aleve) all of them can be purchased as OTC drugs. ASPIRIN ASPIRIN Aspirin, a salicylate NSAID, is the oldest nonopioid analgesic still in use. Aspirin is a analgesic, antipyretic, and anti-inflammatory Aspirin decreases platelet aggregation. Aspirin is in a group of drugs called salicylates. It works by reducing substances in the body that cause pain, fever, and inflammation. Aspirin is used to treat mild to moderate pain, and also to reduce fever or inflammation. It is sometimes used to treat or prevent heart attacks, strokes, and angina. NAPROXEN NAPROXEN Naproxen is rapidly and completely absorbed from the gastrointestinal tract with an in vivo bioavailability of 95%. The elimination half-life of Naproxen ranges from 12 to 17 hours. Steady-state levels of Naproxen are reached in 4 to 5 days, and the degree of Naproxen accumulation is consistent with this half-life. Absorption Peak plasma levels of Naproxen given as Naproxen suspension are attained in 1 to 4 hours. Distribution Naproxen has a volume of distribution of 0.16 L/kg. At therapeutic levels Naproxen is greater than 99% albumin-bound. At doses of Naproxen greater than 500 mg/day there is less than proportional increase in plasma levels due to an increase in clearance caused by saturation of plasma protein binding at higher doses (average trough Css 36.5 mg/L, 49.2 mg/L and 56.4 mg/L with 500 mg, 1000 mg and 1500 mg daily doses of Naproxen, respectively). The Naproxen anion has been found in the milk of lactating women at a concentration equivalent to approximately 1% of maximum Naproxen concentration in plasma NAPROXEN Metabolism Naproxen is extensively metabolized to 6-0-desmethyl Naproxen, and both parent and metabolites do not induce metabolizing enzymes. Both Naproxen and 6-0-desmethyl Naproxen are further metabolized to their respective acylglucuronide conjugated metabolites. Excretion The clearance of Naproxen is 0.13 mL/min/kg. Approximately 95% of the Naproxen from any dose is excreted in the urine, primarily as Naproxen (<1%), 6-0-desmethyl Naproxen (<1%) or their conjugates (66% to 92%). The plasma half-life of the Naproxen anion in humans ranges from 12 to 17 hours. The corresponding half-lives of both Naproxen’s metabolites and conjugates are shorter than 12 hours, and their rates of excretion have been found to coincide closely with the rate of Naproxen disappearance from the plasma. Small amounts, 3% or less of the administered dose, are excreted in the feces. In patients with renal failure metabolites may accumulate. http://www.drugs.com/pro/naproxen.html NAPROXEN Naproxen Oral Suspension is indicated: For the relief of the signs and symptoms of rheumatoid arthritis For the relief of the signs and symptoms of osteoarthritis For the relief of the signs and symptoms of ankylosing spondylitis For the relief of the signs and symptoms of juvenile arthritis Naproxen Oral Suspension is recommended for juvenile rheumatoid arthritis in order to obtain the maximum dosage flexibility based on the patient’s weight. Naproxen Oral Suspension is also indicated: For relief of the signs and symptoms of tendonitis For relief of the signs and symptoms of bursitis For relief of the signs and symptoms of acute gout For the management of pain For the management of primary dysmenorrhea http://www.drugs.com/pro/naproxen.html IBUPROFEN IBUPROFEN Generic name Brand names include: Advil, Advil Childrens, Advil Junior Strength, Advil Liquigel, Advil Migraine, Childrens Ibuprofen Berry, Genpril, IBU-200, Midol IB, Midol Maximum Strength Cramp Formula, Motrin, Motrin Childrens, Motrin IB, Motrin Infant Drops, Motrin Junior Strength, Motrin Migraine Pain, Nuprin. IBUPROFEN Indicated for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis. Indicated for relief of mild to moderate pain. Indicated for the treatment of primary dysmenorrhea. In patients with primary dysmenorrhea, Ibuprofen tablets have been shown to reduce elevated levels of prostaglandin activity in the menstrual fluid and to reduce resting and active intrauterine pressure, as well as the frequency of uterine contractions. The probable mechanism of action is to inhibit prostaglandin synthesis rather than simply to provide analgesia. IBUPROFEN Ibuprofen tablets are rapidly absorbed. Peak serum Ibuprofen levels are generally attained one to two hours after administration. With single doses up to 800 mg, a linear relationship exists between amount of drug administered and the integrated area under the serum drug concentration vs. time curve. Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of Ibuprofen is virtually complete 24 hours after the last dose. The serum half-life is 1.8 to 2.0 hours. ACETAMINOPHEN The analgesic acetaminophen is a popular nonprescription drug for the relief of pain, discomfort, and fever in infants, children, adults, and older adults. Acetaminophen, unlike aspirin, does not have an anti-inflammatory process. ACETAMINOPHEN Acetaminophen is well absorbed fro the gastrointestinal tract. Rectal absorption may be erratic because of the presence of fecal material or a decrease in blood flow to the colon. Because of its short half-life it cam be administered every four hours as needed with a maximum dose of 4g a day. ACETAMINOPHEN Acetaminophen weakly inhibits prostaglandin synthesis, which decrease pain sensation. It is effective in eliminating mild to moderate pain and headaches and is useful for its antipyretic effect. It does not possess anti-inflammatory action. Its onset of action is rapid, and the duration of action is 5 hours or less. ACETAMINOPHEN Some examples of products that have acetaminophen in it are Acephen, Actamin, Feverall, Q-Pap, Tactinal, Tempra, Tylenol, Uniserts, Vitapap. ACETAMINOPHEN TYLENOL TYLENOL Tylenol is a product that has acetaminophen. Used for the head and body pain, for colds and cough, fevers, arthritis, allergies and sinus, pain and sleepiness For children it is the product most parents used to help in fever reducer. Combined—to reduce fever and for the temporary relief of minor aches and pains due to: Headache. Muscular aches. Backache. Minor pain of arthritis. The common cold. Toothache. Premenstrual and menstrual cramps . Temporarily reduces fever. SIDE EFFECTS AND ADVERSE EFFECTS OPIOID ANALGESICS Have many more side effects than nonopioid drugs. Most severe side effect is constipation Can be avoided or reduced if a stool softener/laxative is taken while using opioid analgesics. OPIOID ANALGESICS Other possible side effects Nausea/vomiting Confusion Decrease in blood pressure/orthostatic hypotension Drowsiness Respiratory depression Sedation Urinary retention Antitussive effects NONOPIOID ANALGESICS As a group, these have one major side effect which is gastrointestinal system upset/disturbance. Other side effects can be present with nonopioid analgesic drugs. NSAIDs Can cause stomach ulcers and bleeding They break down the protective lining of the stomach NONOPIOID ANALGESICS Over use or abuse of nonopioid analgesics can also cause kidney and/or liver damage which can ultimately result in organ failure. NURSING IMPLICATIONS OPIOID ANALGESICS OPIOID ANALGESICS Nurses must increase their knowledge about pain, take every client’s pain seriously, and implement measures for treating pain effectively. Whenever a client’s pain is not controlled to his or her satisfaction, the nurse pursues better goal achievement by collaborating with pain experts. OPIOID IMPLICATIONS The nurse needs to monitor vital signs at frequent intervals to detect respiratory changes. Respirations of <10/min can indicate respiratory stress. OPIOID IMPLICATIONS Record client’s urine output because urinary retention is a side effect of morphine. Urine output should be at least 600 ml/day. NON-OPIOID ANALGESICS NONOPIOID IMPLICATIONS While liver enzymes should be monitored, nurses should be prepared to do more client teaching with nonopioid analgesics Clients should be taught to not take acetaminophen for more than 10 days in adults or 5 days with children to prevent liver damage. NONOPIOID IMPLICATIONS If it appears a client could have overdosed on these medications, toxicity levels should be checked Normal serum is 5 to 20 mcg/ml Toxic level is >50mcg/ml Levels of >200 mcg/ml are an indication of heatoxicity OPIOID OR NONOPIOID?? Evaluate client pain level Start with the lowest possible pain reliever that will help the client Monitor the client for pain relief or adverse reactions REFERENCES http://www.udel.edu/chem/theopold/chem465/c opland.udel.edu/~rmarcus/drug%20chart.gif http://www.clinicaladvisor.com/Media/Images/36 /feature1208-pain_fig1_35070_35073.gif http://www.spineunivers.com/displayarticle.php/a rticle1345.html http://en.wikipedia.org/wiki/Opioid Kee, Hayes and McCuistion (2009), Pharmacology, A Nursing Process, 6th Edition, Saunders Elsvier REFERENCES http://www.drugs.com/acetaminophen.html http://www.drugs.com/naproxen.html http://www.drugs.com/pro/naproxen.html http://everydaychemistry.suite101.com/article.cfm/how_does_aspirin_work http://health.yahoo.com/children-resources/acetaminophen-oralrectal/healthwise--d00049a1.html http://www.drugs.com/pro/ibuprofen.html http://www.drugs.com/aspirin.html http://www.migraines.org/treatment/images/tylenol.gif http://www.pharmacy-and-drugs.com/reviews/Ibuprofen.jpg http://www.tylenol.com/ http://www.pharmacy-and-drugs.com/reviews/Naproxen.jpg
