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PubMed1976

The antiphlogistic, antinociceptive and antipyretic properties of fenclorac.

Fenclorac (a,m-dichloro-p-cyclohexlphenylacetic acid, diethylammonium salt) is a potent nonsteroidal anti-inflammatory agent with significant analgesic and antipyretic activity. Fenclorac had an ED50 of 7.9 mg/kg in the carrageenan paw edema assay and had a duration of action of 18-22 hours. Comparative tests in the carrageenan paw edema assay in the rat indicated that the potency of fenclorac was 13 times that of aspirin, 3.4 times phenylbutazone, 3 times ibuprofen and 0.3 times indomethacin. Fenclorac was less potent than indomethacin, but more potent than phenylbutazone or aspirin in treatment of developing or established adjuvant arthritis. The anti-inflammatory effectiveness of fenclorac did not depend upon the integrity of the adrenopituitary axis and was not affected by the route of administration or sex of the test animal. Fenclorac was 77 times more potent than aspirin and more than twice as potent as indomethacin in reducing fever in rats rendered hyperthermic with brewer's yeast. Fenclorac did not affect normal body temperatures. Fenclorac did not interfere with cellular immune mechanisms as measured by its lack of effectiveness in experimental allergic encephalomyelitis. Antinociceptive testing indicated that fenclorac had peripheral but not central analgesic activity. Fenclorac had an acute oral LD50 in rats and mice of 285 and 430 mg/kg, respectively. The acute gastric lesion UD50 for fenclorac was 7 mg/kg in the fasted rat. Studies using 51Cr-tagged erythrocytes indicated that fenclorac did not produce significant fecal blood loss in the rat at twice the therapeutic ED50 dose for up to 12 days after dosing. Extensive and prolonged fecal blood loss was observed with a corresponding dose of indomethacin for up to nine days after administration. Comparison of the anti-inflammatory pharmacology, Therapeutic Ratio and the data obtained from the 51Cr-fecal blood loss studies indicated that fenclorac was well tolerated after acute or subacute administration to the rat.

Adrenalectomy↗
PubMed2000

Effects of Tarchonanthus camphoratus and Eriocephalus africanus on nociception in mice and pyrexia in rats.

The affects of water extracts of the leaves of T. camphoratus and E. africanus on acetic acid- and hotplate-induced nociception and lipopolysaccharide-induced pyrexia were investigated. The writhing induced by acetic acid was significantly attenuated by T. camphoratus (50-100 mg/kg, i.p.), and E. africanus (50-200 mg/kg, i.p.). Similarly, the pain produced by the hot-plate was significantly antagonized by T. camphoratus (100 mg/kg, i.p.), and E. africanus (50-100 mg/kg, i.p.). T. camphoratus (100 mg/kg, i.p.), and E. africanus (100-200 mg/kg, i.p.) significantly attenuated the fever produced by the bacterial endotoxin (lipopolysaccharide, 50 microg/kg, i.m.). Paracetamol (500 mg/kg, i.p.), produced similar effect to T. camphoratus and E. africanus on acetic acid-induced writhes but did not affect the pain and the fever produced by the hot-plate and lipopolysaccharide respectively, to any significant extent. These results indicate that both T. camphoratus and E. africanus have analgesic and antipyretic properties.

Analgesics↗
PubMed2002

Progress in 5H[1]benzopyrano[4,3-d]pyrimidin-5-amine series: 2-methoxy derivatives effective as antiplatelet agents with analgesic activity.

A series of 2-methoxy-5H[1]benzopyrano[4,3-d]pyrimidin-5-amines were prepared and screened for their in vitro antiplatelet activity inducing the aggregation by ADP, arachidonic acid (AA) and collagen. In vivo experiments were performed in order to evaluate their antiphlogistic, analgesic and antipyretic activities. Title compounds showed antiplatelet activity in aggregation AA or collagen-induced, and a good analgesic activity without any gastric toxicity. Comparison with a number of analogue benzopyrano[4,3-d]pyrimidine derivatives and some SAR consideration were reported.

Adenosine Diphosphate↗
PubMed1999

[Hepatotoxicity caused by therapeutic doses of paracetamol in alcoholics. Report of 2 cases of fatal hepatitis in cirrhosis].

Paracetamol is a widely used medication as it is an effective analgesic and antipyretic. Because of the absence of gastro-intestinal side effects, it has been used as the analgesic of choice for alcoholic patients. Hepatotoxicity is dose-related and generally occurs in patients who absorb more than 125 mg/kg/j. However, cases of severe liver damage have been reported after absorption of therapeutic doses of paracetamol in alcoholics. We report 2 cases with a fatal outcome and discuss the mechanisms of toxicity, the prognostic factors and treatment of such event.

Acetaminophen↗
PubMed1977

Ibuproxam and ibuprofen. A pharmacological comparison.

The anti-inflammatory, analgesic and antipyretic effects and the tolerability of 2-(4-isobutylphenyl)-propionic acid (ibuprofen) were compared with those of its derivative 2-(4-isobutylphenyl)-propiohydroxamic acid (ibuproxam, Ibudros. Our experiments show that the interfering action of the two drugs with the reactive processes of the tibio-tarsic articulation, brought about by carrageenin, serotonin, dextrane and formalin is of the same intensity. Also, the analgesic activity is perfectly consistent with the antipyretic one. However, the tolerability of the two molecules is different; the acute toxicity is consistent in the case of the single parenteral administration and it differs in the case of a single or repeated oral treatment. When used under these conditions, ibuproxam is considerably less damaging to the gastroenteric tube than is ibuprofen. The hypothesis is put forth that the greater tolerability of ibuproxam is due to its pharmacokinetics: it is, as such, little or not toxic for the mucous membrane of the digestive apparatus, and it progressively releases ibuprofen, whose concentrations in the blood would remain below those levels that cause systemic lesions in the gastroenteric tract.

Analgesics↗
PubMed1997

Chronopharmacological study of KE-SI-TO in mice.

Influence of dosing time on pharmacological effects and toxicity of KE-SI-TO (KST), analgesic and antipyretic drug, was investigated in ICR male mice under LD (12:12) cycle. Significant circadian rhythms were demonstrated for analgesic and hypothermal effects of KST (1 g/kg, i.p.) with higher values in the dark and lower ones in the light (p<0.01, respectively). The rhythmic patterns of KST-induced analgesia and hypothermia resembled overall the rhythms occuring in the nondrugged state. Injection of KST resulted in a parallel increasing in latency to hot plate and a parallel decreasing in rectal temperature. KST (6 g/kg, i.p.)-induced toxicity also showed a significant circadian rhythm with the highest mortality at 1700 and the lowest one at 0500 (p<0.05). The principles and concepts of biological rhythm should be included in the consideration of the actions of KST.

Analgesics↗
PubMed2006

Analgesic efficacy of parenteral paracetamol (propacetamol) and diclofenac in post-operative orthopaedic pain.

BACKGROUND: Propacetamol is an injectable pro-drug of paracetamol (acetaminophen) with analgesic and antipyretic activities, especially used in the post-operative period. The aim of this study was to assess the analgesic efficacy and safety of intravenous paracetamol, administered as propacetamol, in comparison with placebo and intramuscular diclofenac in patients with post-operative pain. METHODS: This was a randomized, double-blind, double-dummy study. One hundred and twenty patients with moderate to severe pain following total hip arthroplasty received either two administrations of propacetamol 2 g intravenously, 5 h apart (n = 40), one single administration of diclofenac 75 mg intramuscularly (n = 40) or placebo (n = 40). Efficacy measures were assessed before each drug administration, for the 5 h following each study treatment administration and for the total study duration of 10 h. Safety was assessed by reporting adverse events and changes in vital signs, electrocardiogram (ECG) and biochemical investigations before and 24 h after dosing. RESULTS: Both active treatments were effective and statistically superior to placebo over the whole study period, as indicated by the total pain relief score. No significant differences were found between propacetamol and diclofenac for any measures of analgesic activity. Only minor and common adverse events were reported, with no overall differences between the groups. CONCLUSION: Both active treatments were superior to placebo, and the overall efficacy of two intravenous infusions of propacetamol 2 g (equivalent to 1 g of paracetamol), 5 h apart, was not statistically different from that provided by a single intramuscular injection of diclofenac 75 mg over the first 5 h post-dose and over the total 10-h study period. The safety was good.

Acetaminophen↗
PubMed1980

The pharmacological properties of fenbufen. A review.

gamma-Oxo(1,1'-biphenyl)-4-butanoic acid (fenbufen) was shown to be an orally and parenterally effective nonsteroidal antiinflammatory, analgesic and antipyretic agent in a variety of animal species. Like other clinically active antiinflammatory drugs such as acetylsalicylic acid (ASA), indometacin and phenylbutazone, fenbufen has demonstrated potent activity in a variety of laboratory test systems including carageenin edema (rats), UV erythema (guinea pigs), adjuvant arthritis (rats), urate synovitis (dogs), phenylquinone writhing (mice), and yeast-induced pyresis (rats). In general, fenbufen was less potent than indomethacin and more potent than ASA, and appeared of special interest because of its high analgetic efficacy and long duration of antiinflammatory and analgetic action. While shown to have ulcerogenic potential in rats at toxic doses, fenbufen was less potent than indometacin in this respect and had a superior margin of gastrointestinal safety in treatment of dogs with urate synovitis. One of fenbufen's major metabolites, 4-biphenylacetic acid (BPAA), was found to be potent inhibitor of prostaglandin (PG) synthesis both in vitro and in vivo with a variety of tissues tested. Fenbufen itself was devoid of this anti-PG-synthetase activity although it interacted with prostaglandins in other ways. These results, coupled with the fact that only BPAA showed pharmacological activities when applied locally, led to the conclusion that BPAA was the principle responsible for fenbufen's antiinflammatory action. Fenbufen thus appears to be a pro-drug capable of circumventing at least some of the gastric toxicity usually incurred when compounds, which are themselves capable of inhibiting PG synthesis, are introduced directly into the stomach. Fenbufen's relatively low gastric toxicity in dogs and humans seems to substantiate this hypothesis. The pharmacological evidence indicates that fenbufen should be a highly effective and clinically useful antiinflammatory, analgetic and antipyretic drug.

Analgesics↗
PubMed2002

1,5-benzodiazepines. Part XIII. Substituted 4H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-5-amines and 4H-imidazo[1,2-a][1,5]benzodiazepin-5-amines as analgesic, anti-inflammatory and/or antipyretic agents with low acute toxicity.

The reaction of proper N,N-dialkyl-4H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-5-amines (1) with N-chlorosuccinimide afforded their 4-chloroderivatives 3 which in turn were treated with cyclic amines to give the corresponding 4,5-diaminoderivatives 4. The N,N-dialkyl-4H-imidazo[1,2-a][1,5]benzodiazepin-5-amines (5) were prepared starting from suitable 4-(dialkylamino)-1,3-dihydro-2H-1,5-benzodiazepin-2-ones (8), through multistep synthetic routes. At the 200 mg kg(-1) os dose, some compounds 3 and 4 showed notable analgesic or anti-inflammatory activity but no antipyretic properties, whereas the 5-(dibutylamino) derivatives 5b and 5f proved to be significantly endowed with all these activities. Almost all the compounds 3, 4 and 5 did not show acute toxicity in mice up to 800 mg kg(-1) os dose.

Analgesics↗
PubMedDate not supplied

[Optimal dose of acetaminophen in children].

Acetaminophen is an antipyretic and analgesic drug frequently prescribed in children. Unlike aspirin, the recommended doses for acetaminophen are different in France (20-30 mg/kg/24 h) and in the USA (65 mg/kg/24 h). The authors reviewed literature data, looking for the scientific basis of these recommendations in children. The antipyretic effect of a 7-20 mg/kg single oral dose was demonstrated versus placebo. A dose-effect relationship was established: 20 mg/kg as a single oral dose was more effective than 10 mg/kg while 5 mg/kg had little antipyretic effect. More than 10 mg/kg were required to keep on average the temperature 1.5 degrees C below the starting point for 6 hours. There was no significant difference regarding the antipyretic effects of a single 10-15 mg/kg dose using suppositories or oral suspension, although there was a greater consistency of response with the oral suspension. There was no significant difference concerning the antipyretic effect between a 10-15 mg/kg acetaminophen oral dose and the same dose of aspirin. The analgesic effect of a single 10-15 mg/kg oral dose was also demonstrated versus placebo in children. Plasma concentrations between 4 and 18 mg/l seem appropriate to obtain an antipyretic effect. Half-life is 1-3.5 h. Based on these data different dose regimens including an initial loading dose have been proposed. The simplest one is as follows: 25 mg/kg loading dose and 12.5 mg/kg every 6 h as maintenance dose.

Acetaminophen↗
PubMed1978

[Analgetic and antipyretic activity of SL-573 (author's transl)].

Potency of analgetic activity of SL-573 was between that of indomethacin and aminopyrine in chemical stimulation tests. The analgetic activity of SL-573 was 3.2 times as potent as that of aminopyrine in the phenylquinone writhing test, 4.1 times as potent as aminopyrine in the acetic acid writhing test and 6.3 times as potent as aminopyrine in the Randall and Selitto test. Thus the analgetic activity of SL-573 appears to be comparable etic to that of codeine. SL-573, unlike narcotic analgesics, showed common properties to known antipyretic analgesics and anti-inflammatory agents in the following points. (1) Analgetic activity was not evident in the mechanical stimulation or in the heat stimulation tests. (2) The analgetic activity was not antagonized by naloxone. (3) SL-573 showed no antagonistic effect to morphine. (4) Tolerance to the analgetic activity of SL-573 was not observed after a one week pretreatment with this compound. (5) SL-573 had no effect on the evoked potentials recorded from cells in the pain pathway of CNS and the site of action of analgetic effect was considered to be in peripheral sites of the sensory neurons. The antipyretic activity of SL-573 was equal to that of aminopyrine in febrile rabbits and 4 times as potent as that of aminopyrine in febrile rats. This compound did not affect normal body temperature of rabbits and rats, this observation being similar to that noted with antipyretic analgesics and nonsteroidal anti-inflammatory agents.

Afferent Pathways↗
PubMed1984

Anti-inflammatory activity of Euphorbia acaulis Roxb.

From various extracts of Euphorbia acaulis , the n-hexane fraction showed marked anti-inflammatory activity in carrageenan induced oedema in rats and mice as compared to phenylbutazone and was equipotent in adrenal- ectomised rats. In chronic models of formaldehyde and adjuvant arthritis, its anti-arthritic activity was found to be superior to that of phenylbutazone. It had a diuretic effect but did not show any analgesic or antipyretic activity.

Analgesics↗
PubMedDate not supplied

Facile synthesis of fused pyrazolo[1,5-a]pyrimidinepyrazolo [1,5-a]triazines and N-sulphonamidopyrazoles as antiinflammatory.

Interaction of hydrazine hydrate with methyl (2-E)-2-cyano-3-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino]-3-(methylsulphanyl)-2-propenoate 2 which was obtained by the reaction of methyl-2-cyano-3,3-bis(methylsulphanyl) acrylate 1 with 4-amino-1-phenyl-2,3-dimethyl pyrazoline-5-one afforded methyl-5-amino-3-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino]-1H-pyrazole-4-carboxylate 3a. The pyrazolin derivative 3a is a good precursor for the synthesis of pyrazolo[1,5-a]pyrimidines which is based on the interaction of 3a with alpha,beta-unsaturated nitrile derivatives. The biological effects of some of the newly synthesized compounds were also investigated as antiinflammatory, analgesic and antipyretic drugs. Compounds 2b, 4a, 3a, 3b, 2a and 4b were found to have significant antiinflammatory activity in descending order in comparison to control groups phenylbutazone. Compounds 3a, 2a, 4b, 4a, 2b and 3b have analgesic activity in decreasing order. Compound 3a was the most potent and had 82.6% potency of Novalgin. Compounds 2b, 2a, 3b, 4b, 3a and 4a were found to have significant antipyretic activity in descending order. Compounds 2a, 4b induced no ulcerogenic activity, while compounds 3b, 2b, 4a and 3a showed only slight ulcerogenic activity.

Analgesics↗
PubMed2001

Anti-inflammatory and antipyretic effects of Trigonella foenum-graecum leaves extract in the rat.

Anti-inflammatory and antipyretic effects of the Trigonella foenum-graecum (TFG) leaves extract, an Iranian medicinal plant, were examined. For anti-inflammatory activity, the formalin-induced edema model was used. Hyperthermia was induced by intraperitoneal injection of 20% (w/v) aqueous suspension of brewer's yeast. Sodium salicylate (SS) was used as a positive control. Both TFG and SS significantly reduced formalin-induced edema in single dose (TFG 1000 and 2000 mg/kg, SS 300 mg/kg) and chronic administration (TFG 1000 mg/kg and SS 300 mg/kg). TFG and SS also significantly reduced hyperthermia induced by brewer's yeast in 1 and 2 h after their administration. The results indicate that the TFG leaves extract possess anti-inflammatory as well as antipyretic properties in both i.p. and p.o. administration. Phytochemical studies indicate that alkaloids, cardiac glycosides, and phenols are the major component in the extract. Although existence of three anti-inflammatory, analgesic and antipyretic effects in this extract suggest a NSAID-like mechanism for it, but the presence of alkaloids, the absence of other effective compounds such as flavonoids, saponins, steroids, etc., and also its analgesic effect on tail-flick test that usually is not produced by NSAIDs, suggest another mechanism for the extract. So the possibility of alkaloids as effective compounds, in this extract, increases.

Analgesics, Non-Narcotic↗
PubMed1983

[Synthesis of pyrazole and pyrazolo [4,3-d] pyrimidinone derivatives. II].

Three new series of pyrazolic and pyrazolo-pyrimidinonic derivatives (II a-g), (III a-g) and (IV a-g), containing the substituted phenyl-hydrazide moiety were prepared and studied in order to check some information on the analgesic and antipyretic activity of an analogous series obtained in a previous work. Some derivatives (II b), (II d), (II f), (III b), (III c) and (IV d) show interesting analgesic activity.

Animals↗
PubMed2005

1,8-Naphthyridines v. novel N-substituted 5-amino-N,N-diethyl-9-isopropyl [1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamides, as potent anti-inflammatory and/or analgesic agents completely devoid of acute gastrolesivity.

Most N,N-disubstituted 5-amino-N,N-diethyl-9-isopropyl [1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamides 9 (compounds 9a, c-i) and the N-monosubstituted one 8c were obtained by treating with excess amine the corresponding 5-chloroderivative 7a, which was in turn prepared by cyclocondensation of the 2,4-dichloro-N,N-diethyl-1,8-naphthyridine-3-carboxamide (4a) with isobutyrohydrazide. Compounds 8a,b and 9b,j-m were obtained according with the methods shown in Scheme 1. The above now synthesized compounds, along with the previously described 8d and 8e, were tested for their anti-inflammatory, analgesic and antipyretic properties, and most compounds also for their effect on spontaneous mice locomotor activity and their acute gastrolesivity in rats. Several compounds showed potent anti-inflammatory and/or analgesic activities, and all the compounds tested proved to be completely lacking in acute gastrolesivity. In many cases compounds 8 and 9 produced hypothermic effect, usually at high doses. On the whole, the N-monosubstituted 5-aminoderivatives 8 appeared to be more potent anti-inflammatory agents than the corresponding N,N-disubstituted 9, whereas these latter compounds exhibited higher analgesic activity.

Analgesics↗
PubMed2006

Effects of anti-inflammatory [1, 2, 4]triazolo[4, 3-a] [1, 8]naphthyridine derivatives on human stimulated PMN and endothelial cells: an in vitro study.

BACKGROUND: 124 triazolo [4, 3-a]18naphthyridine derivatives (including NF161 and NF177) were tested for anti-inflammatory, analgesic and antipyretic properties and for their effects on spontaneous locomotor activity in mice and acute gastrolesivity in rats. Both NF161 and NF177 appeared to be anti-inflammatory and analgesic agents without toxic effects or acute gastrolesivity, but NF161 showed stronger anti-inflammatory activity, whereas NF177 was more active as analgesic. METHODS: An EIA kit was used to investigate the ability of NF161 and NF177 to affect prostaglandin E2 (PGE2) and prostacyclin (PGI2) production by human umbilical vascular endothelial cells (HUVEC). The compounds' effects on the production of reactive oxygen species (ROS) by human polymorphonuclear cells (PMNs) were studied in an in vitro cell model, evaluating inhibition of superoxide anion (O2-*) production induced by N-formylmethionyl-leucyl-phenylalanine (FMLP). Their effects on PMN adhesion to HUVEC were also investigated; they were incubated with PMNs and endothelial cells (EC) and challenged by stimuli including Platelet Activating Factor (PAF), FMLP, Phorbol Myristate Acetate (PMA), Tumor Necrosis Factor-alpha (TNF-alpha) and Interleukin-1beta (IL-1beta). Adhesion was quantitated by computerized micro-imaging fluorescence analysis. RESULTS: Neither compounds modified PGE2 or PGI2 production induced by IL-1alpha. O2-* production and myeloperoxidase release from PMNs stimulated by FMLP was inhibited in a dose- but not time-dependent manner by both 18naphthyridine derivatives, NF161 being statistically more active than NF177 (P < 0.01). The compounds inhibited adhesion evoked by the pro-inflammatory stimuli PAF, FMLP, TNF-alpha and IL-1beta in a concentration-dependent manner in the 10(-6)-10(-4)M range, being more active when PAF was used as stimulus and inactive when cells were challenged by PMA. Both compounds acted both on PMN and HUVEC. CONCLUSION: Considering the interesting anti-inflammatory effects of these compounds in in vivo models and the absence of acute gastrolesivity, the study improved knowledge of anti-inflammatory properties of NF161 and NF177, also demonstrating their potential in vitro, through inhibition of O2-* production, myeloperoxidase release and PMN adhesion to HUVEC. Negative results on PG production suggest a cyclooxygenase (COX)-independent mechanism.

Journal Article↗