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Pilot study of the antipyretic and analgesic activity of nimesulide paediatric suppositories.

The object of this study was the preliminary evaluation, in paediatric patients, of the analgesic and antipyretic effect of nimesulide given rectally. Nimesulide was studied in comparison with paracetamol, according to a double-blind technique. Forty-eight hospitalized children with fever or pain, between 1 and 8 years old, were included. The drugs were administered with a flexible posology (1 to 4 suppositories/day with an interval between administrations of at least 6 h). Monitoring of symptom intensity was scheduled in the 6 hours after each administration. At the end of the therapy the physician expressed a global judgement on the drug. Both treatments resulted in a significant decrease in body temperature at the 1 h observation. From the second hour onward, a more rapid tendency to temperature normalization was observed with nimesulide than with paracetamol. Repeated measurements with ANOVA did not show significant differences between treatments but the physicians' overall judgements were significantly more favourable to the nimesulide than to the paracetamol antipyretic activity. Good analgesic activity, favouring a rapid decrease in the painful symptomatology, was observed in both groups. No differences were found in the analgesic activity of the treatments, although in this case the clinical evidence was more favourable to paracetamol. Both drugs were very well tolerated.

Acetaminophen↗

Studies on the anti-inflammatory, antipyretic and analgesic properties of the leaves of Aegle marmelos Corr.

The serial extracts of the leaves of Aegle marmelos Corr. were investigated for anti-inflammatory property. The analgesic and antipyretic properties were also evaluated. The most of the extracts derived from the plant Aegle marmelos caused a significant inhibition of the carrageenan-induced paw oedema and cotton-pellet granuloma in rats. The extracts also produced marked analgesic activity by reduction the early and late phases of paw licking in mice. A significant reduction in hyperpyrexia in rats was also produced by the most of the extracts. This study was established anti-inflammatory, antinociceptive and antipyretic activities of the leaves of Aegle marmelos.

Acetic Acid↗

Dexamethasone fails to produce antipyretic and analgesic actions in experimental animals.

In order to explore the role of phospholipase A2 inhibition in the mechanisms of the action of glucocorticoids, it was investigated whether the steroid exhibits the analgesic and antipyretic actions as well as cyclo-oxygenase inhibitors such as indomethacin or not. Dexamethasone has been reported to produce the anti-inflammatory action with a lag time of at least 1 h at doses of up to 0.1 mg/kg in mice and rats. However, dexamethasone when given 4 h beforehand had no significant analgesic activity even at doses of 1 and 10 mg/kg i.v. in the acetic acid writhing test in rats. In mice, the significant reduction in writhes counts was seen when dexamethasone (1 and 10 mg/kg i.v.) was given 15 min or 4 h before phenylquinone injection; i.e. the activity had not the lag time. On the other hand, dexamethasone showed a strong antipyretic activity against both the fevers caused by LPS and yeast in rats. In the yeast-febrile rats, the antipyretic activity had a lag time of about 1 h, and was dose-related at doses as low as 0.03 to 0.3 mg/kg i.v.; the steroid markedly reduced the increased PGE2 content in the cerebrospinal fluid. The antipyretic activity after local injection into the cerebroventricle or the yeast pouch was stronger than that after systemic injection into the tail vein, although so large a difference in the activity between the dosage routes was not seen, suggesting that the site of the antipyretic action is in both the brain and periphery. The antipyretic activity of dexamethasone (10 mg/kg i.v.) was not seen in rabbits with fever caused by LPS.(ABSTRACT TRUNCATED AT 250 WORDS)

Analgesics↗

Studies on anti-inflammatory, analgesic and antipyretic activities of some indan acids.

A series of indan-1 acids were synthesized and screened for anti-inflammatory activity. All the reported compounds showed varying degrees of anti-inflammatory activity in carrageenin-induced paw oedema test. They also exhibited appreciable antipyretic and analgesic activity in various animal test models. Among these compounds 6-methoxy-indan-1-acetic acid (compound 11) and 5,6-dimethoxy-indan-1-acetic acid (compound 12) showed activity profile close to that of phenylbutazone having prolonged action and lower toxicity than the latter.

Animals↗

[Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83].

Pharmacological properties of LFP83, a non-steroidal analgesic and antipyretic drug, were studied in mice, rats and rabbits. LFP83 is a prodrug of flurbiprofen (FP) which is its active major metabolite in vivo. In experimental models of acetic acid writhing, the Randall and Selitto method, arthritic pain, yeast fever, LPS fever, carrageenin edema and adjuvant arthritis, LFP83 (i.v.) showed remarkable analgesic, antipyretic and antiinflammatory activities; and it was more potent than ketoprofen (i.m.) and aspirin DL-lysine (i.v.). The analgesic activity of LFP83 was equal to or more potent than that of pentazocine, and its duration was longer than those of aspirin DL-lysine and pentazocine. In addition, the analgesic potency of LFP83 was approximately the same or more potent than that of FP (p.o.), and the onset of this analgesic effect began earlier. On the other hand, the ulcerogenic activity of LFP83 on rat gastric mucosa was less than that of FP (p.o.) in both single and consecutive (7 days) administrations. The safety index (UD50/ED50) of LFP83 was three to ten-fold higher than that of FP (p.o.). As mentioned above, LFP83 is a potent analgesic, antipyretic and antiinflammatory drug; and in comparison to oral FP, it has a more potent and immediate effect, weak gastric irritation and high safety index.

Analgesics↗

Interactions of analgesics with other drugs.

Antipyretic analgesics, such as salicylates, acetaminophen, and pyrazolones, are often given concomitantly with a variety of other drugs. Drug interactions that occur at the receptors are known as pharmacodynamic interactions; alterations in absorption (bioavailability), distribution (plasma protein-binding), and elimination (renal excretion, hepatic metabolism) are termed pharmacokinetic interactions. For example, antacids and food both delay the absorption of analgesics. Highly protein-bound drugs (such as phenylbutazone, phenytoin, or warfarin) can compete with the common binding sites of salicylates. Hepatic elimination of salicylates can be influenced by drugs such as beta-blockers and cimetidine. Clinically important interactions involving salicylates, acetaminophen, and other antipyretic analgesics are discussed.

Acetaminophen↗

[4-(3-Oxo-1,2-benzisothiazolin-2-yl)alkanoic, phenyl and phenoxyalkanoic acids: synthesis and anti-inflammatory, analgesic, and antipyretic properties].

Based on previous observations, the preparation, some physicochemical (partition coefficient, pKa) and pharmacological properties of 4-(3-oxo-1,2-benzisothiazolin-2-yl)alkanoic, benzoic, phenyl, phenoxyalkanoic acids and of some of their functional derivatives are reported. All new compounds were biologically examined for their antiphlogistic, analgesic and antipiretic actions, in comparison with those of 1,2-benzisothiazolin-2-one and with those of ibuprofen as the antiphlogistic, analgesic, antipyretic arylalkanoic prototype. Structure-activity relationships showed that the 1,2-benzisothiazolin-2-one and its new alkanoic and arylalkanoic derivatives have strong actions which are however specific for some of the tested pharmacological properties. From this point of view, the synthesized substances have a narrow spectrum of activity, if compared with ibuprofen which is at the same time an antiphlogistic, analgesic and antipiretic substance. The antiphlogistic and antipyretic activities of 4-(3-oxo-1,2-benzisothiazolin-2-yl)benzoic, phenylacetic and phenylmethylacetic acids and the antipyretic and analgesic actions of 3-oxo-1,2-benzisothiazolin-2-ylacetic acid, which are comparable or higher in "potency" than those of ibuprofen, are noteworthy.

Animals↗

Preliminary studies on antipyretic and analgesic properties of Taverniera abyssinica.

In an attempt to ascertain the pharmacological basis of the use of the marketed traditional drug Taverniera abyssinica A. Rich. (Amharic name Dingetegna), crude extracts as well as purified substances of this plant were tested for their antipyretic and analgesic properties. Antipyretic activity was determined on rats made hyperthermic by yeast injection and analgesic activity was determined by the hot plate, as well as the acetic acid induced writhing, methods. The study showed that the plant possesses significant antipyretic and analgesic activities.

Animals↗

[Combination of antibiotics with analgesic and antipyretic substances (author's transl)].

1. We suggest a combination of analgesic and antipyretic medicaments in medical treatments with antibiotics. Thus, the antibiotic is increased and microorganisms, resistant to antibiotics, are converted into sensitive forms. 2. The results of the in vitro used method (diffusion plate test) are in accordance with the results obtained using these combinations in therapy. 3. This method should not be applied to strains that are sufficiently sensitive to antibiotics, since the results would be contrary to the afore mentioned. 4. The effects of a combination are additionally synergistic in the case of strains originally sensitive. 5. This method offers great possibilities for multiplying treatments with antibiotics. We recommend to give standardized combinations of antibiotics with analgesic and antipyretic medicaments per os.

Analgesics↗