Analgesic salicylates

Aspirin Salicylate Analgesic, anti-inflammatory Salix alba (white willow tree) and Filipendula ulmaria (meadowsweet)... 

This is a non-narcotic, non-salicylate analgesic with few anti-inflammatory effects that acts by inhibiting prostaglandin synthesis in the CNS (hence being antipyretic and analgesic). It is metabolized by CYP1A2. 

Many pharmaceutical compounds contain chromophores that make them suitable for analysis by UV/Vis absorption. Products that have been analyzed in this fashion include antibiotics, hormones, vitamins, and analgesics. One example of the use of UV absorption is in determining the purity of aspirin tablets, for which the active ingredient is acetylsalicylic acid. Salicylic acid, which is produced by the hydrolysis of acetylsalicylic acid, is an undesirable impurity in aspirin tablets, and should not be present at more than 0.01% w/w. Samples can be screened for unacceptable levels of salicylic acid by monitoring the absorbance at a wavelength of... 

Students determine the concentrations of caffeine, acetaminophen, acetylsalicylic acid, and salicylic acid in several analgesic preparations using both CZE (70 mM borate buffer solution, UV detection at 210 nm) and HPLC (C18 column with 3% v/v acetic acid mixed with methanol as a mobile phase, UV detection at 254 nm). 

Nonsteroidal Antiinflammatory Drugs. Nonsteroidal antiinflammatory dmgs (NSAIDs) include, among the numerous agents of this class, aspirin (acetylsaflcyhc acid), the arylacetic acids indomethacin and sulindac, and the arylpropionic acids, (5)-(147) and (R)-(148) ibuprofen, (5)-(149) and (R)- (150), flurbiprofen naproxen (41), and fenoprofen (see Analgesics, antipyretics, and antiinflammatory agents Salicylic acid and related compounds). 

Some simple benzoates are also used as antiseptic agents. Salicylic acid esters are used as antibacterial agents and pain relievers. Analgesic balms, creams. 

The popularity of aspirin has led to the preparation of a liost of relatively simple derivatives in the hope of finding a ilrug that would be either superior in action or better tolerated. i alicylamide (5), for example, is sometimes prescribed for pa-I Lents allergic to aspirin. It should be noted, however, that I his agent is not as active as the parent compound as an antiinflammatory or analgesic agent. This may be related to the fact I hat salicylamide does not undergo conversion to salicylic acid i 11 the body. 

After oral administration, acetylsalicylic acid is rapidly and almost completely absorbed but in the intestinal mucosa it is partly deacetylated to salicylic acid, which also exhibits analgesic activity. The plasma half-life of acetylsalicylic acid is 15 min whereas that of salicylic acid, at low dosages of acetylsalicylic acid, is 2-3 h. Salicylic acid is eliminated more slowly when acetylsalicylic acid is administered at high dose rates because of saturation of the liver enzymes. The metabolites are mainly excreted via the kidney. 

The next three chapters deal with dragp used in the management of pain the nonnarcotic analgesics (salicylates, nonsalicylates [acetaminophen], and the nonsteroidal anti-inflammatory dragp) and the narcotic analgesics. 

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. 

The manner in which salicylates relieve pain and reduce inflammation is not fully understood. It is thought that the analgesic action of the salicylates is due to tiie inhibition of prostaglandins. Prostaglandins are fatty acid derivatives found in almost every tissue of the body and body fluid. Release of prostaglandin is thought... 

The salicylate nonnarcotic analgesics are used for the following reasons ... 

SUM MARY DRUG TABLE NON NARCOTIC ANALGESICS SALICYLATES AND NON SALICYLATES... 

Salicylates aspirin Bayer, Ecotrin, Analgesic, Nausea, vomiting, epigastric 325-650 mg PO... 

Acetaminophen is a nonsalicylate nonnarcotic analgesic whose mechanism of action is unknown. Lake the salicylates, acetaminophen has analgesic and antipyretic activity. However, acetaminophen does not possess antiinflammatory action and is of no value in the treatment of inflammation or inflammatory disorders. 

Willow bark (weidenrinde, white willow, purple osier willow, crack willow) S lixalba, purpurea, fragilis Analgesic Adverse reactions are those associated with the salicylates Do not use with aspirin or other NSAIDs. Do not use in patients with peptic ulcers and other medical conditions in which the salicylates are contraindicated. 

Aspirin, non-acetylated salicylates, and other NSAIDs have analgesic, antipyretic, and anti-inflammatory actions. These agents inhibit cyclooxygenase (COX-1 and COX-2) enzymes, thereby preventing prostaglandin synthesis, which results in reduced nociceptor sensitization and an increased pain threshold. NSAIDs are the preferred agents for mild to moderate pain in situations that are mediated by prostaglandins (e.g., rheumatoid... 

Topical analgesics sometimes are used for mild pain or as an adjunct to systemic therapy. There are limited data to support the use of salicylate-containing rubefacients (e.g., methyl salicylate and trolamine salicylate) or other counterirritants (e.g., menthol, camphor, and methyl nicotinate) in OA.32 See Chap. 57 for more information on these products when used for musculoskeletal disorders. 

Some salicylates are specifically marketed for musculoskeletal back pain, such as magnesium salicylate. However, no studies specifically support use of these salicylates over other systemic analgesics. Magnesium salicylate should be used with caution in renal impairment because hypermagnesemia may occur.31... 

Methyl salicylate 10-60% Analgesic Balm3 BenGay Ultra Strength3 Icy Hot Chill Stick3 Caution in aspirin sensitivity May produce systemic concentrations... 

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