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PubMed1976

Ketoprofen (19.583 R.P.) (2-(3-benzoylphenyl)-propionic acid). Main pharmacological properties--outline of toxicological and pharmacokinetic data.

Ketoprofen possesses the typical pharmacological properties of non-steroidal anti-inflammatory agents i.e. anti-inflammatory, analgesic and antipyretic activity, as well as antibradykinin activity and ability to inhibit prostaglandin synthesis. Ketoprofen is as potent as indomethacin in the tests for anti-inflammatory and analgesic activity, but its antipyretic and antibradykinin activities and its inhibitory activity against prostaglandin synthesis is respectively 4, 8 and 8 times greater than that of indomethacin. It seems very likely that the pituitary-adrenal axis is not involved in the mechanism of the anti-inflammatory action of ketoprofen, since in the carrageenan abscess test, the compound shows the same activity both in adrenalectomized and in normal rats and, when locally applied to the inflamed area, it is more active than when administered systemically. In the mouse the acute oral toxicity of ketoprofen is about one twentieth that of indomethacin. Like all powerful steroidal or non-steroidal antiinflammatory agents, ketoprofen shows some gastrointestinal toxicity, but its effect is mild and distinctly less than that of indomethacin. Pharmacokinetic studies in the rat, dog and monkey have shown that gastro-intestinal absorption of the drug is rapid and almost complete; the compound and its metabolites are excreted from the body fairly rapidly.

Analgesics↗
PubMed1990

[Opiates in pediatric anesthesia].

Narcotic analgesics, although frequently used in adult patients, are at present relatively minor drugs in pediatric anesthesia. This review discusses indications, clinical applications, and side effects of opiates for pre-medication, induction and maintenance of anesthesia, and postoperative pain therapy in infants and children. Opiates do not represent the agents at first choice for preoperative anxiolysis or amnesia. With the exception of certain disease states (cardiac risk, elevated intracranial pressure, malignant hyperthermia) where intravenous anesthesia including opiates is clearly indicated, inhalational anesthetics are commonly preferred to narcotics. It has been shown, however, that opiate-supplemented general anesthesia can be used for pediatric surgery in an equally effective and safe manner. Finally, there is an essential need for more narcotic analgesics in the treatment of early postoperative pain, when antipyretic-antiphlogistic analgesics alone prove ineffective. It thus seems that in pediatric anesthesia today opiates are prescribed at the wrong time and withheld when they are most urgently needed.

Adolescent↗
PubMed1997

Analgesic efficacy of a hydrocodone with ibuprofen combination compared with ibuprofen alone for the treatment of acute postoperative pain.

Hydrocodone is a semisynthetic opioid with analgesic and antitussive properties qualitatively similar to other opioid agonists. Ibuprofen is a nonsteroidal antiinflammatory agent with analgesic and antipyretic activity and is an effective, primarily peripheral-acting antiinflammatory analgesic. The objective of this clinical trial was to determine the additive analgesic effect of the combination of 15 mg hydrocodone bitartrate with 400 mg ibuprofen, relative to 400 mg ibuprofen alone and placebo, in the treatment of postoperative pain. The single-dose analgesic efficacy of the combination of hydrocodone bitartrate with ibuprofen was compared with ibuprofen alone and placebo in 120 patients with moderate or severe postoperative pain after abdominal surgery. Analgesia was measured during the 6-hour period after dosing based on onset of relief, hourly and summary variables, and duration of effect. A significantly greater proportion of patients treated with the hydrocodone/ibuprofen combination reported onset of relief compared with ibuprofen or placebo; however, the distribution functions for time to onset of relief did not differ among treatments. Hydrocodone with ibuprofen and ibuprofen alone were significantly more effective than placebo for all measures of analgesia. The combination of hydrocodone with ibuprofen was significantly superior to ibuprofen for all hourly analgesic evaluations, weighted sum of pain intensity differences (SPID), total pain relief (TOTPAR), and global rating of study medication. No patients in the hydrocodone with ibuprofen group required analgesic remedication during the 6-hour study period, compared with 25% and 82% in the ibuprofen and placebo groups, respectively. The analgesic superiority of 15 mg hydrocodone bitartrate combined with 400 mg ibuprofen compared with 400 mg ibuprofen alone was demonstrated across many efficacy variables.

Adolescent↗
PubMed2002

Free radical scavengers, anti-inflammatory and analgesic activity of Acaena magellanica.

Extracts of the whole plant Acaena magellanica (Rosaceae) were assessed for anti-inflammatory, antipyretic and analgesic activity in animal models. At 600 mg kg(-1), the global ethanolic extract (GEE), dichloromethane (DCM) and defatted methanol (MeOH) fractions showed a mild anti-inflammatory effect in the carrageenan-induced guinea-pig paw oedema. The GEE, DCM and defatted MeOH fractions significantly reduced inflammation by 43.2, 40.5 and 42.1%, respectively. The GEE did not showed any significant antipyretic activity in doses up to 600 mg kg(-1). A 20% w/v infusion administered orally at 16 mL kg(-1) presented analgesic effect in the acetic acid-induced abdominal constriction test in mice. The GEE and MeOH extract of A. magellanica showed free radical scavenging activity in the diphenylpicrylhydrazyl decolouration assay. Assay-guided isolation led to quercetin, Q-3-O-beta-glucoside, Q-3-O-beta-D-galactoside, ellagic acid and catechin as the free radical scavengers. The saponins tormentic acid 28-O-beta-D-galactopyranoside and 28-O-beta-D-glucopyranoside were isolated from the polar extract. The structures were determined by spectroscopic methods.

Administration, Oral↗
PubMed1985

The antiinflammatory activity of the immunomodulator Wy-18,251 (3-(p-chlorophenyl)thiazolo[3,2-a]benzimidazole-2-acetic acid).

The antiinflammatory activity of the immunomodulatory agent Wy-18,251 (3-(p-chlorophenyl)thiazolo-[3,2-a]benzimidazole-2-acetic acid) was examined using a variety of antiinflammatory, analgesic and antipyretic animal models in comparison to aspirin, levamisole and indomethacin. The acute antiinflammatory and analgesic activity of Wy-18,251 (ED50 = 100-200 mg/kg, p.o.) was similar to aspirin, but in contrast to aspirin Wy-18,251 failed to demonstrate antipyretic activity. Wy-18,251 (10-100 mg/kg, p.o.) also inhibited chronic inflammatory responses in the adjuvant- and collagen-induced arthritis models. Wy-18,251 was a modest inhibitor of prostaglandin biosynthesis but did not inhibit either 5- or 15-lipoxygenase enzymes. Wy-18,251 (up to 480 mg/kg, p.o.) produced little gastrointestinal pathology in 16 h fasted rats. The combined immunomodulatory and antiinflammatory activity of Wy-18,251 suggests that this agent may have therapeutic promise in certain immunoinflammatory diseases including rheumatoid arthritis.

Adjuvants, Immunologic↗
PubMed1993

Synthesis of new 5-substituted pyrazolo[1,5-d][1,2,4]-triazine derivatives and their analgesic, anti-inflammatory and antipyretic properties.

A series of 2-aryl-4-oxo-pyrazolo[1,5-d][1,2,4]triazines substituted in the 5-position by aminoalkyl or benzoyl moieties was synthesized and evaluated for analgesic activity. The structures of new triazine derivatives were confirmed by IR, 1H-NMR spectra and by elementary analysis. In the phenylbenzoquinone induced writhing test, only 3,3a-dihydropyrazolo triazines substituted by an arylpiperazinylmethyl group exhibited potent analgesic effect. In addition, these compounds possessed significant anti-inflammatory and antipyretic properties. A desaturation in 3,3a positions or other groups than arylpiperazinylmethyl moieties notably decreased analgesic effects.

Animals↗
PubMed2003

COX-1 and COX-3 inhibitors.

Low doses of aspirin reduce both pain and fever, whereas the anti-inflammatory action of aspirin requires a much higher dose. It is possible that inhibition of cyclooxygenase (COX)-1 is the major action of aspirin involved in its analgesic and antipyretic effects, and inhibition of COX-2 is responsible for its anti-inflammatory action. We compared the analgesic effects of an aspirin-like drug (diclofenac) and a centrally acting analgesic (paracetamol) in the mouse stretching test and confirmed that the analgesic action of the aspirin-like drug was peripheral. Two possible sites have been postulated for the antipyretic action of non-steroid anti-inflammatory drugs; (a) inhibition of COX in endothelial cells of hypothalamic blood vessels or (b) inhibition of COX synthesising prostaglandins near sensory receptors of sub-diaphragmatic vagal afferents. The antipyretic action of aspirin may be mediated by inhibition of COX-3 in hypothalamic endothelial cells or by inhibition of COX-1 localised close to sensory receptors of peripheral vagal afferents. It is also possible that both enzymes are involved in the antipyretic action of aspirin. Whereas lipopolysaccharide (LPS)-induced fever is attenuated in COX-2 gene-deleted mice, suggesting that COX-2 is responsible for this type of fever, the COX-1 gene may also be important in temperature regulation and in mediating the pyresis that occurs in the absence of infection.

Analgesics, Non-Narcotic↗
PubMed2004

Antiinflammatory, lack of central analgesia and antipyretic properties of Acanthus montanus (Ness) T. Anderson.

Aqueous leaves extract of Acanthus montanus (Nees) T. Anderson (Acanthaceae) were tested for antiinflammatory, analgesic and antipyretic properties. This was done using standard methodologies following oral administration of the extract. The results showed that the extract significantly reduced the oedema induced by carrageenan within 30 min with 200 mg/kg being the most potent. On the analgesia front, acetic acid writhing test was significant. The extract reduced only the number of paw licks of phase 2 and not phase 1 of formalin test. The results on hotplate and tail immersion tests excluded central acting analgesic properties of the extract. In overall, the analgesic tests conducted revealed that the extract had only peripheral analgesic properties. Its effect on pyresis was also observed to be appreciable. It significantly reduced fever at doses greater than 100 mg/kg within 6 h.

Acanthaceae↗
PubMed1979

Study of two new non-steroid anti-inflammatory drugs having a pyrazole structure (LM 22070 and LM 22102).

Two derivatives from a new heteroarylacetic series, 1,3,4-triphenylpyrazole-5-acetic acid (LM 22102) and 1-isobutyl-3,4-diphenylpyrazole-5-acetic acid (LM 22070), were selected on the basis of their anti-inflammatory, analgesic and antipyretic properties. In the mouse, LM 22102 and LM 22070 were respectively 15 and 30 times less active than indomethacin in Koster's test, but they were 9 and 13 times less toxic than the reference drugs. In contrast, they were very active in the rat and the guinea-pig. LM 22102 appeared to be as active as indomethacin in the various tests performed: Randall and Selitto's test for analgesic activity, hyperthermic rat, experimental models of inflammation (UV erythema, carrageenin-induced oedema, cotton granuloma, adjuvant-induced arthritis). In vitro, its inhibition of prostaglandin-synthetase in guinea-pig lung was appreciably more powerful than that of indomethacin. Like all potent non-steroid anti-inflammatory drugs it has ulcerogenic activity, similar to that of indomethacin, which accounts for its acute oral toxicity in the rat. The activity of LM 22070 is either the same as (antipyretic action) or inferior to (analgesic and anti-inflammatory activity and inhibition of prostaglandin-synthetase) that of indomethacin, but always markedly superior to that of phenylbutazone. Its ulcerogenic activity and oral acute toxicity in the rat are respectively 2.5 and 3 times weaker than those of indomethacin.

Animals↗
PubMed1985

Rigid congeners of arylpyridazinones. IV. Synthesis and activity of derivatives of the new heterocyclic system 9H-indeno[2,1-c]pyridazine.

Representative terms of the new heterocyclic system 9H-indeno[2,1-c]pyridazine have been synthesized. Their antiinflammatory, analgesic and antipyretic activities were evaluated, in order to compare the pharmacological profiles with those of the isomeric series of 5H-indeno[1,2-c]pyridazine previously investigated. The new compounds were, in general, equiactive as analgesic but less active as antiinflammatory and antipyretic agents with respect to their 5H-isomers.

Animals↗
PubMed2000

Effects of caffeine and paracetamol alone or in combination with acetylsalicylic acid on prostaglandin E(2) synthesis in rat microglial cells.

Paracetamol has mild analgesic and antipyretic properties and is, along with acetylsalicylic acid, one of the most popular "over the counter" analgesic agents. However, the mechanism underlying its clinical effects is unknown. Another drug whose mechanism of action is unknown is caffeine, which is often used in combination with other analgesics, augmenting their effect. We investigated the inhibitory effect of paracetamol and caffeine on lipopolysaccharide (LPS)-induced cyclooxygenase (COX)- and prostaglandin (PG)E(2)-synthesis in primary rat microglial cells and compared it with the effect of acetylsalicylic acid, salicylic acid, and dipyrone. Furthermore, combinations of these drugs were used to investigate a possible synergistic inhibitory effect on PGE(2)-synthesis. Both paracetamol (IC(50)=7.45 microM) and caffeine (IC(50)=42.5 microM) dose-dependently inhibited microglial PGE(2) synthesis. In combination with acetylsalicylic acid (IC(50)=3.12 microM), both substances augmented the inhibitory effect of acetylsalicylic acid on LPS-induced PGE(2)-synthesis. Whereas paracetamol inhibited only COX enzyme activity, caffeine also inhibited COX-2 protein synthesis. These results are compatible with the view that the clinical activity of paracetamol and caffeine is due to inhibition of COX. Furthermore, these results may help explain the clinical experience of an adjuvant analgesic effect of caffeine and paracetamol when combined with acetylsalicylic acid.

Acetaminophen↗