Analgesics/antipyretics acetaminophen

Moreover, COX-2 expression seems to be regulated by synaptic activity [36]. Recently, COX-3 was characterized as generated from COX-1 intron-1 retention [37]. COX-3 is expressed in brain [37], brain microvasculature [38] and has been proposed to be a target of the analgesic/ antipyretic acetaminophen [37,39]. 

Chandrasekharan, N. V., Dai, H., Roos, K. L. et al. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs cloning, structure, and expression. Proc. Natl Acad. Sci. U.S.A. 99 13926-13931,2002. 

Another analgesic, acetaminophen, is a derivative of /7-aminophenol. Although it is an analgesic and antipyretic, acetaminophen shows little if any... 

Acetaminophen (APAP, N-Ace l-o-Aminophenol) (Tylenol, Other Generic) [OTC] [Analgesic, Antipyretic] Uses MUd-mod pain, HA, fevCT Action Nonnarcotic analgesic X CNS synth of prostaglandins hypothalamic heat-regulating center Dose Adults. 650 mg PO or PR q4-6h or... 

Correct choice = D. Acetaminophen does not antagonize the uricosuric agent probenecid and therefore may be used in patients with gout. Acetaminophen has little anti-inflammatory effect, but has analgesic and antipyretic activities equal to those of aspirin. It is the analgesic-antipyretic of choice for children with viral infections aspirin can increase the risk for Reye s syndrome in children. Acetaminophen is a suitable substitute for the analgesic and antipyretic effects of aspirin in those patients with gastric complaints. 

Mild analgesic-antipyretic therapy is often helpful in relieving the associated lethargy, malaise, and fever. Aspirin or acetaminophen (650 mg in adults or 10-15 mg/kg per dose in children maximum daily pediatric dose 60 mg/kg maximum daily adult dose 4 g) or ibupro-fen (200-800 mg in adults or 10 mg/kg per dose in children maximum daily pediatric dose 40 mg/kg maximum daily adult dose 3.2 g) should be administered every 4 to 6 hours. In children, aspirin should be avoided and acetaminophen used as the preferred agent because of the possible association between aspirin use and the development of Reye s syndrome. ... 

Acetaminophen (paracetamol JV-acetyl-p-aminophenoF, TYLENOL, others) is an effective alternative to aspirin as an analgesic-antipyretic agent however, its anti-inflammatory effects are much weaker. While it is indicated for pain relief in patients with noninflammatory osteoarthritis, it is not a suitable substitute for aspirin or other NSAIDs in chronic inflammatory conditions such as rheumatoid arthritis. Acetaminophen is well tolerated and has a low incidence of GI side effects. It is available without a prescription. Acute overdosage can cause severe hepatic damage, and the number of accidental or deliberate poisonings with acetaminophen continues to grow. Chronic use of less than 2 g/day is not typically associated with hepatic dysfunction. 

Acetaminophen (Tylenol) Mechanism not yet clear. Weak inhibitor of prostaglandin synthesis. Analgesic antipyretic effects equal those of aspirin. Anti-inflammatory effects much weaker. Mild to moderate pain and fever. Preferred over aspirin in children because it is less likely to cause Reye s Syndrome. Does not cause Gl upset or bleeding. Rash, occasionally with fever. Overdose may cause severe hepatic necrosis leading to coma and death. 

Recent research in dogs has revealed a slice variant of COX-1 that was sensitive to inhibition by acetaminophen. This novel variant of the cyclooxygenase system was named COX-3, and it was hypothesized that inhibition of COX-3 could represent a primary CNS mechanism by which acetaminophen and phenacetin exerted their analgesic and antipyretic effects (30). The ability of selected analgesic/antipyretic drugs to inhibit COX-1, COX-2, and COX-3 is... 

Non-narcotic analgesics (see chart) are used to treat mild to moderate pain. Many of these medications are not addictive and available over-the-counter. Non-narcotic analgesics are used to treat headaches, menstmal pain (dysmenor-rheal), pain from inflammation, minor abrasions, muscular aches and pain, and mild-to-moderate arthritis. Non-narcotic analgesics also lower elevated body temperature (antipyretic). Non-narcotic analgesics include acetaminophen and NSAIDs (aspirin, ibuprofen, and COX-2 inhibitors), which were discussed in Chapter 12. 

Acetaminophen Analgesic antipyretic derivative of acetanUide. It has weak antiinflammatory properties and is used as a common analgesic, but may cause Ever, blood cell,... 

Anilides are simple acetamides of aniline, which may or may not contain a 4-hydroxy or 4-alkoxy group (Figure 13.13). Acetanilide is ring hydroxylated after administration to yield acetaminophen, the active analgesic/antipyretic, whereas phenacetin (rarely used) undergoes oxidative-O-dealkylation to produce acetaminophen. Anilides do not possess carboxylic acid functionality and, therefore, they are classified as neutral drugs and possess little, if any, inhibitory activity against COX. 

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