Antipyretic effects

The different furanones 104 were tested for their potency as inhibitors of PGE2 production both in transfected Chinese hamster ovarian (CHO) cells expressing human COX-2 and in human whole blood. Compound 104r proved to be an orally active and selective COX-2 inhibitor that is devoid of the ulcerogenic effect at >100 times the dose for antiinflammatory, analgesic, and antipyretic effects (99BMC3187). 

Age does not significantly affect plasma concentrations or disposition of ibuprofen however, investigators have determined that the onset of antipyresis and maximum antipyretic effect is greater in children less than one year old as compared to children older than 6 years [43]. The authors hypothesized that this accelerated response was related to the greater relative body surface area of the young child. It should be noted that cystic fibrosis patients do have a higher clearance of ibuprofen [43a]. 

Amabeoku GJ, Eagles P, Scott G, Mayeng I, Springfield E. Analgesic and antipyretic effects of Dodonaea angustifolia and Salvia africana-lutea. J Ethnopharmacol 2001 75 117-124. 

Similarly, where a stimulation action (e.g., antipyretic effect of NSAIDS through thermolysis or production of cAMP by bronchodilator beta-2 agonisU ) is involved, the stimulation response... 

Propoxyphene (Darvon ) is a stronger analgesic but has no antipyretic effects. It is sometimes taken in combination with aspirin and... 

Adults - Initially, 50 mg every 3 or 4 hours increase to 100 mg if necessary. Do not exceed a total daily dosage of 600 mg. When anti-inflammatory or antipyretic effects are desired in addition to analgesia, aspirin can be administered concomitantly. 

The enumeration of these effects of prostaglandins makes it understandable that the inhibition of the cycloxigenases will result in antiinflammatory, analgesic and antipyretic effects. Another important function of PGE2 is the vasodilatation it can induce in the renal circulation. Locally produced PGE2 increases the renal perfusion. 

Diclofenac Voltaren) is a phenylacetic acid derivative that is a potent inhibitor of COX and that has analgesic, antiinflammatory, and antipyretic effects. Its use is accompanied by side effects similar to those of other NSAIDs. Indications for the drug include rheumatoid arthritis, osteoarthritis, and ophthalmic inflammation (use of an ophthalmic preparation). 

Hydrocodone (Hycodan), oxycodone (Roxicodone), dihydrocodeine, hydromorphone (Dilaudid), and oxy-morphone (Numorphan) are derivatives of codeine and morphine. All are indicated for the relief of mild to severe pain or for their antipyretic effects they are often used in combination with nonopioid analgesics. The drugs vary in potency, but their pharmacological effects do not differ significantly from those of codeine or morphine. 

It is a para-amino phenol derivative, acts on CNS to produce analgesia and antipyretic effect. It has negligible antiinflammatory action peripherally in therapeutic uses. It is poor inhibitor of PG synthesis in peripheral tissues, but more active on COX in brain. It also raises the pain threshold. 

Clinical use Salicylamide has analgesic and antipyretic effects and is used in multidrug combinations for the treatment of a variety of mild pain conditions including musculoskeletal, soft tissue and joint disorders. 

The action of endogenous pyrogens on the hypothalamus produces fever, because of a readjustment ill the central set point controlling the body s internal temperature. Salicylates and other NSAIDs achieve their antipyretic effect by controlling the prostaglandin-induced release of pyrogens. 

SAM-dependent methylation of salicylic acid. The salicyl alcohol derivative salicin, found in many species of willow (Salix species Salicaceae), is not derived from salicylic acid, but probably via glucosylation of salicylaldehyde and then reduction of the carbonyl (Figure 4.27). Salicin is responsible for the analgesic and antipyretic effects of willow barks, widely used for centuries, and the template for synthesis of acetylsalicylic acid (aspirin) (Figure 4.27) as a more effective analogue. 

Aspirin does not alter the normal body temperature, which is maintained by a balance between heat production and dissipation. In a fever associated with infection, increased oxidative processes enhance heat production. Aspirin acts by causing cutaneous vasodilation, which prompts perspiration and enhances heat dissipation. This effect is mediated via the hypothalamic nuclei, as proved by the fact that a lesion in the preoptic area suppresses the mechanism through which aspirin exerts its antipyretic effects. The antipyretic effects of aspirin may be due to its inhibition of hypothalamic prostaglandin synthesis. Although aspirin-induced diaphoresis contributes to its antipyretic effects, it is not an absolutely necessary process, because antipyresis takes place in the presence of atropine. 

Aspirin reduces elevated temperature, whereas normal body temperature is only slightly affected. Aspirin s antipyretic effect is probably mediated by both COX inhibition in the central nervous system and inhibition of IL-1 (which is released from macrophages during episodes of inflammation). 

Studies in animals clearly indicate that prostaglandins can produce fever when injected into the central nervous system and that Cox-2 induction is responsible for the fever that occurs with bacterial endotoxin and cytokines. To address the potential for an antipyretic effect in humans, Schwartz et al. (1999) administered rofecoxib or ibuprofen to young adults who presented to an infirmary for acute, nonbacterial... 

A decoction of dried twigs of cinnamon can produce an antipyretic effect in mice. Studies conducted in anaesthetized dogs and guinea pigs indicated that cinnamaldehyde, or sodium cinnamate, also produced the hypothermic and antipyretic effects (Chinese Materia Medica, 1996). It also causes a hypotensive effect, which is due mainly to vasodilation of peripheral vessels. Cinnamaldehyde produced an analgesic effect in mice (Wang, 1985). 

Fenugreek leaves possess anti-inflammatory and antipyretic effect. The leaf extract reduces formalin-induced oedema in single dose (fenugreek 1000 and 2000 mg/ kg, sodium salicylate 300mg/kg). It also reduces hyperthermia induced by Brewer s yeast 1-2 h after administration (Ahmadiani et al., 2001). 

Ahmadiani, A., Javan, M., Semnanian, S., Barat, E. and Kamalineyad, M. (2001) Antiinflammatory and antipyretic effects of Trigonella foenum graecum leaf extracts in rats. Journal of Ethnopharmacology 75, 283-286. 

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. 

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