acetaminophen, liver and kidney damage may result from using large doses of this medicine every day for a long time, or drinking alcohol with the usual dose. Even moderate amounts of alcohol can produce liver damage in people taking acetaminophen. Acetaminophen is administered orally with absorption associated with the rate of gastric emptying. Peak blood concentrations usually occur within one-half to one hour. In large doses, a highly active metabolite is associated with acetaminophen’s toxicity to the liver and kidneys. The half-life of this drug is two to three hours and is generally unaffected by renal function. With large doses or in the case of liver disease, the half-life duration may double. Unlike NSAIDs, acetaminophen does not have anti- inflammatory properties, so does not affect uric acid levels and platelet function. Patients allergic to aspirin, unable to take salicylates, individuals with hemophilia, a history of peptic ulcer, or those with aspirin-associated bronchospasms should not take acetaminophen. It is also often used in children with viral infections. Larger doses may cause dizziness, excitement, and disorientation. Early symptoms of hepatic damage include nausea, diarrhea, vomiting, and abdominal pain. There have also been rare cases of renal damage. The exact mechanism of action of acetaminophen is not known. Acetaminophen relieves pain by elevating the pain threshold, that is, by requiring a greater amount of pain to develop before it is felt by a person. It reduces fever through its action on the heat-regulating center of the brain. Specifically, it tells the center to lower the body’s temperature when the temperature is elevated. Acetaminophen is used for the relief of fever as well as aches and pains associated with many conditions. Acetaminophen relieves pain in mild arthritis but has no effect on the underlying inflammation, redness and swelling of the joint. If the pain is not due to inflammation, acetaminophen is as effective as aspirin. It is as effective as the non-steroidal anti-inflammatory drug ibuprofen in relieving the pain of osteoarthritis of the knee. Acetaminophen is metabolized (eliminated by conversion to other chemicals) by the liver. Therefore drugs that increase the action of liver enzymes that metabolize acetaminophen (e.g. carbamazepine, isoniazid, rifampin) may decrease the action of acetaminophen. The potential for acetaminophen to harm the liver is increased when it is combined with alcohol or drugs that also harm the liver. When used appropriately, side effects are rare. The most serious side effect is liver damage due to large doses, chronic use or concomitant use with alcohol or other drugs that also damage the liver. Acetaminophen is excreted in breast milk in small quantities. However, acetaminophen use by the nursing mother appears to be safe. Acetaminophen has been used in all stages of pregnancy. use of corticosteroids. Most corticosteroids are available only with a physician’s prescription. However, some low-strength topical creams are available over the counter. Corticosteroids are extremely helpful as short-term relief for many chronic pain conditions. They are some of the most powerful medicines available to fight inflammation. However, long-term use of corticosteroids may lead to numerous side effects. Some of the strongest side effects are associated with the oral and intravenous forms of corticosteroids, which are used for pain. Physicians may try to minimize the side effects by prescribing as low a dose as possible for pain relief and by using corticosteroids for severe pain only.
which may be prohibitive in larger dosages. Like naproxen, nabumetone has been reported to cause photosensitivity and pseudoporphyria in some users. Oxicam NSAIDs Piroxicam (Feldene) : Has a long half-life, permitting once a day dosage. At high concentrations, this COX inhibitor also inhibits leukocyte migration, decreases oxygen radical production and inhibits lymphocyte function. Toxicity includes gastrointestinal symptoms in 20 percent of users, and other adverse effects including headache, dizziness, tinnitus, and rash. Peptic ulcer and bleeding can occur at higher dosages, at a rate more than nine times that of other NSAIDs. Diflunisal (Dolobid): Although it is derived from salicylic acid, it is not reduced to salicylic acid or salicylate. Clearance is dependent on renal function and hepatic metabolism, and dosages should be limited in users with renal impairment. It is considered particularly effective for pain in cases of bone metastases and dental surgery. Ketorolac (Toradol): Used for systemic use primarily as an analgesic , rather than an anti-inflammatory, although it does have typical NSAID anti-inflammatory properties. Most typically given intramuscularly or intravenously after surgery, but an oral dose is available. When combined with an opioid, it can decrease the amount of opioid required by a much as 25- 50 percent. Toxicities are similar to other NSAIDs, with renal toxicity perhaps more common with chronic use than that of other NSAIDs. Sulindac (Clinoril): Along with its use for rheumatic disease, it may have implications for inhibiting the growth of certain cancers. Like diclofenac, may cause elevated serum aminotransferases more than most other NSAIDs. In most cases, the choice of an NSAID is based on risk of toxicity and cost-effectiveness. In general, the gastrointestinal and renal side effects of ketorolac limit its use. On a toxicity index, indomethacin and meclofenamate were associated with the greatest toxicity, while salsalate, aspirin, and ibuprofen were least toxic of all the non-selective COX inhibitors. For users with renal dysfunction, nonacetylated salicylates may have fewer side effects. Fenoprofen is used less because it is associated with interstitial nephritis. Two nonselective NSAIDs, diclofenac and sulindac, are more associated with liver function abnormalities than any other NSAIDs. In most cases, physicians seek a good fit between an individual’s needs and sensitivities and an NSAID that best suits those needs. Acetaminophen (Tylenol) Acetaminophen is a drug with antipyretic and analgesic effects similar to those of aspirin and NSAIDs, but with limited anti-inflammatory or antirheumatic effects. It is used to treat mild to moderate pain. Unlike aspirin and related drugs, acetaminophen is not irritating to the stomach. While people rarely have any side effects from the usual dose of Medications for inflammation For pain caused by swelling, glucocorticoids or steroids, like prednisone, may be useful, but because of the toxicity associated with their effects, their use has been limited, in general, to treatment for acute flare-ups of the joints. For long- term use, the NSAIDS now have the primary role in treatment. People who take corticosteroids for painful conditions such as osteoarthritis and rheumatoid arthritis may get them in the form of injections. For people with one painful joint (e.g., knee), an injection can provide pain relief and reduce swelling. Corticosteroids injected directly into a joint can concentrate the medication where it is needed and avoid potential problems such as an upset stomach. However, continued injections into specific joints may eventually damage the cartilage in the joint. People taking corticosteroids should never stop taking them abruptly because they can experience serious side effects. A physician can provide a schedule for safely discontinuing the
For further information, refer to the section under Gastrointestinal Medications (corticosteroids), above.
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Book Code: MGA1224
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