Aspirin anti-inflammatory effect

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. 

The salicylates include aspirin (acetylsalicylic acid) and related drugp, such as magnesium salicylate and sodium salicylate. The salicylates have analgesic (relieves pain), antipyretic (reduces elevated body temperature), and anti-inflammatory effects. All the salicylates are similar in pharmacologic activity however, aspirin has a greater anti-inflammatory effect than the other salicylates. Specific salicylates are listed in the Summary Drug Table Nonnarcotic Analgesics Salicylates and Nonsalicylates. 

Unlike aspirin and other cyclooxygenase inhibitors that work on the COX-1 and COX-2 enzymes, acetaminophen works on the COX-3 enzyme, which is present in the spinal column and brain. This helps it to avoid shutting down prostaglandin function elsewhere in the body, which is why it has no anti-inflammatory effects and does not affect blood platelets or the stomach lining. 

Yamashita reported anti-inflammatory effect of astaxanthin when administered with aspirin. An oral preparation has been developed by Alejung and Wadstroem for the treatment of Helicobacter infections of the mammalian gastrointestinal tract. Strong evidence suggested that astaxanthin modulated the humoral and non-humoral immune systems. It enhanced the release of interleukin-1 and tumor necrosis factor-... 

Aspirin is acetylsalicylic acid and is used as an antiplatelet agent and for pain relief. Its use for anti-inflammatory effects is limited by the occurrence of side-effects, which include tinnitus and deafness, both features of salicylate poisoning. 

Reduction of inflammation with nonsteroidal anti-inflammatory drugs (NSAIDs) often results in relief of pain for significant periods. Furthermore, most of the nonopioid analgesics (aspirin, etc) have anti-inflammatory effects, so they are appropriate for the treatment of both acute and chronic inflammatory conditions. 

Ibuprofen is a simple derivative of phenylpropionic acid (Figure 36-1). In doses of about 2400 mg daily, ibuprofen is equivalent to 4 g of aspirin in anti-inflammatory effect. Pharmacokinetic characteristics are given in Table 36-1. 

The anti-inflammatory effect of aspirin appears to be due to the acetylation of a serine residue at the active site of the cyclooxygenase, which irreversibly inactivates the enzyme (fig. 19.18). Aspirin has no effect on the peroxidase activity of the enzyme. 

The eicosanoids have been implicated as mediators of tissue inflammation since aspirin s anti-inflammatory effect was shown to be the result of its inactivation of cyclooxygenase. How eicosanoids cause tissue inflammation is the focus of much current research. 

Generic Name Aspirin Trade Name(s) Many trade names Specific Comments—Comparison to Other NSAIDs Most widely used NSAID for analgesic and anti-inflammatory effects also used frequently for antipyretic and anticoagulant effects. 

Diflunisal Dolobid Has potency 3-4 times greater than aspirin in terms of analgesic and anti-inflammatory effects but lacks antipyretic activity. 

Oxaprozin Daypro Analgesic and anti-inflammatory effects similar to aspirin may produce fewer side effects than other NSAIDs. 

Aspirin is employed for mild to moderate pain of varied origin but is not effective for severe visceral pain. Aspirin and other NSAIDs have been combined with opioid analgesics for treatment of cancer pain, where their anti-inflammatory effects act synergistically with the opioids to enhance analgesia. High-dose salicylates are effective for treatment of rheumatic fever, rheumatoid arthritis, and other inflammatory joint conditions. 

Aspirin has some beneficial effects when mixed with caffeine, because caffeine increases the pain-relieving and anti-inflammatory effects of aspirin. Brand names of pain relievers that combine aspirin and caffeine include Alka-Seltzer , Anacin , and Cope Analgesic Pain Reliever. 

Mechanism of action The antipyretic and anti-inflammatory effects of the salicylates are due primarily to the blockade of prostaglandin synthesis at the thermoregulatory centers in the hypothalamus and at peripheral target sites. Furthermore, by decreasing prostaglandin synthesis, the salicylates also prevent the sensitization of pain receptors to both mechanical and chemical stimuli. Aspirin may also depress pain stimuli at subcortical sites (that is, the thalamus and hypothalamus). 

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. 

Aspirin produces an antipyretic and anti-inflammatory effect primarily by irreversibly inhibiting cyclooxygenase (thus having similar effects to NSAIDs). It possesses an antiplatelet effect that may have additive effect with other drugs with a similar effect (e.g, selective serotonin reuptake inhibitors) and those which affect other aspects of blood clotting. The risk of interactions and adverse effects are reduced by using a lower dose (e.g. 75 mg) fortunately, a full antiplatelet effect is seen at this dose. This is considered in Part 1, Cardiovascular Drugs. 

Aspirin is often given in a buffered form. The addition of small amounts of antacids decreases GI irritation and increases the dissolution and absorption rate of the aspirin. Nonacetylated salicylates, including salsalate, sodium salicylate, choline salicylate, magnesium salicylate, and various salicylate combinations, are usually more expensive but can be effective. Although these aspirin substitutes provide less anti-inflammatory effects than aspirin, they exhibit minimal antiplatelet properties and have fewer GI side effects.They can therefore be useful for patients who cannot tolerate aspirin or other NSAIDs. 

The analgesic efficacy and safety profiles of the nonsalicylate NSAIDs make them appropriate alternatives to aspirin for treatment of mild to moderate pain. Most NSAIDs are used primarily for their anti-inflammatory effects, but they are also effective analgesics that relieve pain associated with a variety of ocular conditions. The nonsalicylate NSAIDs consist of the propionic acid derivatives, cyclooxygenase-2 (COX-2) inhibitors, and several other less commonly used agents (Table 7-2). 

Acetaminophen is a potent analgesic drug, but it lacks the anti-inflammatory effects of aspirin. It also is less likely to cause stomach irritation. 

---