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At least 667 records · Page 37Linked to original sources
PubMed1980

Pharmacological properties of a new anti-inflammatory agent: 2-(2-isopropyl-5-indanyl)propionic acid (UP 517-03).

2-(2-Isopropyl-5-indanyl)propionic acid (UP 517-03) is a new anti-inflammatory agent with marked analgesic and antipyretic properties. The anti-inflammatory potency is greater than that of phenylbutazone but lower than that of indometacin. This effect is observed also in adrenalectomized rats. The analgesic activity in the Randall and Selitto test is equipotent to that of indometacin, but this potency is lower in the other tests. In lowering brewer's yeast-induced fever in rats, UP 517-03 is as potent as indometacin and 10 times more effective than phenylbutazone. Considering from pharmacological index, UP 517-03 is tolerated as well as phenylbutazone and better than indometacin.

Analgesics↗
PubMed2000

Synthesis and preliminary biological evaluation of novel N-substituted 1-amino-3-[1-methyl(phenyl)-1H-indazol-4-yloxy]-propan-2-ols interesting as potential antiarrhythmic, local anaesthetic and analgesic agents.

A series of indazoloxypropanolamines 7 and 8, pindolol isosteres, were synthesized to extend the structure activity relationship (SAR) which was observed in an earlier series of related derivatives. Compounds 7, characterized by methyl substitution on the N-1 indazole nucleus, generally exhibited significant antiarrhythmic, local anaesthetic and analgesic activities. The preliminary radioligand binding assay highlighted, in compounds 7, an interesting beta 1-affinity which can be well correlated to their antiarrhyhtmic activity. Analogues 8 characterized by a phenyl group on the N-1 indazole nucleus, were generally less active as antiarrhyhtmic agents but generally interesting as local anaesthetics. Due to the importance of the indazole moiety as a carrier of antiphlogistic activity, the two classes of derivatives 7 and 8 were evaluated for their NSAID behaviour. Once again, compounds 7 resulted having more interesting analgesic and antipyretic effects than analogues 8.

Analgesics, Non-Narcotic↗
PubMed2002

Actions of paracetamol on cyclooxygenases in tissue and cell homogenates of mouse and rabbit.

BACKGROUND: Paracetamol is a potent analgesic and antipyretic drug, but has only weak anti-inflammatory activity. Unlike aspirin-like drugs, paracetamol does not damage the stomach mucosa or inhibit the aggregation of platelets. The analgesic action of paracetamol is on the central nervous system. In vitro, paracetamol inhibits cyclooxygenase (COX)-1 and -2 in high concentrations but stimulates in low doses. This study examines the stimulation and inhibition of COX-1 and COX-2 in homogenates of mouse and rabbit tissues and in J774.2 cultured mouse macrophages. MATERIAL/METHODS: Mouse and rabbit tissues were removed, homogenised and treated with different concentrations of paracetamol. Prostaglandins (PGs) E2 and I2 were measured in the homogenates to assess the activity of COX-1. Ex vivo synthesis of PGE2 was measured in tissues after treating rabbits with 100 mg/kg paracetamol. J774.2 cultured mouse macrophages treated with bacterial lipopolysaccharide (LPS) to induce COX-2, were treated with varying concentrations of paracetamol and the PGs produced were measured. RESULTS: Low doses of paracetamol stimulated PG production in J774.2 macrophages and stomach mucosa homogenates, but reduced PG production at high concentrations of paracetamol. This stimulation did not occur when co-factors were added. The order of potency of paracetamol on COX-1 or COX-2 in tissue homogenates was as follows: lungs>spleen>brain>J774.2 cells>stomach mucosa. Paracetamol, 100 mg/kg, inhibited COX-1 in stomach mucosa ex vivo much less effectively than in other tissues. CONCLUSIONS: These data support the hypothesis that paracetamol selectively inhibits a COX enzyme which is different from COX-1 or COX-2 and may be a variant of COX-1.

Acetaminophen↗
PubMed1987

Pharmacological properties of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal antiinflammatory agent.

The antiinflammatory activity of a novel pyrrolidone derivative E-5110 was investigated using anti-inflammatory, analgesic and antipyretic animal models in comparison to indomethacin (IND) and piroxicam (PIR). The acute antiinflammatory activity of E-5110 on carrageenin paw edema was similar to IND, and half of PIR. E-5110 inhibited the pleural exudate volume and leucocyte infiltration in a reversed passive Arthus reaction more potent than IND. The chronic inflammatory responses in the established adjuvant- and type II collagen-induced arthritis were suppressed by E-5110 similar to IND and PIR. The analgesic potency of E-5110 was similar to IND and PIR, but the antipyretic activity of E-5110 was more potent than that of IND, and slightly more potent than that of PIR. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than that of the reference drugs.

Animals↗
PubMed2004

Anti-inflammatory activity of methanolic extracts from Ventilago harmandiana Pierre.

Methanolic extracts from the heart wood, stem bark, and stem wood of Ventilago harmandiana Pierre (Family Rhamnaceae) were assessed for anti-inflammatory effects using both acute and chronic inflammatory models. Analgesic and antipyretic activities of the extracts were also evaluated. It was found that all extracts possessed strong inhibitory effects on the acute phase of inflammation as seen in ethyl phenylpropiolate (EPP)- and arachidonic acid (AA)-induced ear edema as well as in carrageenin-induced paw edema in rats. The extracts elicited only weak inhibitory activity on cotton pellet-induced granuloma formation, a subchronic inflammatory model. In the analgesic test, all extracts exerted pronounced inhibitory activity in acetic acid-induced writhing response but showed only weak effects in the tail-flick test. The extracts also showed excellent antipyretic activity on yeast-induced hyperthermia in rats.

Acetic Acid↗
PubMed1998

Anti-inflammatory activity of the alkaloid bukittinggine from Sapium baccatum.

The anti-inflammatory and related activities of bukittinggine were evaluated in comparison with reference drugs. The results obtained revealed that bukittinggine exhibited a significant inhibitory effect in carrageenin-induced hind paw edema and adjuvant-induced arthritis in rats. Its anti-inflammatory activity in both test models was comparable to that of acetylsalicylic acid. Bukittinggine also showed an inhibitory effect on the late proliferative phase of the inflammatory process in cotton pellet-induced granuloma formation in rats. In carrageenin-induced rat pleurisy, bukittinggine exhibited marked inhibitory activity on exudative formation, accumulation of leukocytes and on PGE2-like activity in the exudate. Furthermore bukittinggine could significantly reduce fever in yeast-induced hyperthermic rats and possessed analgesic activity comparable to that of acetylsalicylic acid when tested in acetic acid-induced writhing response in mice. However, bukittinggine exhibited only a weak effect in the tail-flick test when compared with morphine. It is likely that bukittinggine possesses a mechanism of anti-inflammatory, analgesic and antipyretic action similar to that of acetylsalicylic acid.

Abdominal Muscles↗
PubMed1979

Pharmacological study of a new non-steroidal anti-inflammatory drug: protacine (CR 604).

The pharmacological activities of 3'-(4-[2-(1-p-chlorobenzoyl-5-methoxy-2-methyl-indol-3-yl-acetoxy)-ethyl]-piperazin-1-yl)propyl-4-benzamido-N,N-dipropylglutaramate(+/-)dimaleate (protacine, CR 604), a new indolyl derivative with strong anti-inflammatory, analgesic and antipyretic activities, are described. The dose-dependent activity of protacine on inflammation has been shown both in short-term experiments, like the hind paw edema induced by carrageenin and several other irritants, and long-term tests, like the aminoacetonitrile-induced osteolathyrism, the adjuvant-induced arthritis and the cotton pellet-induced granuloma. The analgesic activity of the drug has been evidenced in the phenylquinone-induced writhing and the Randall-Selitto tests, and the antipyretic effects in the yeast-induced hyperthermia in rats. Other general pharmacological effects have been studied, too. Contrarily to several other anti-inflammatory drugs, including indometacin, showing advers effects at doses which are in the same range of those active on experimental inflammation, protacine shows these effects to a minor degree and at doses which are much larger than those pharmacologically active. The therapeutic index of protacine therefore is superior to that of other anti-inflammatory drugs.

Aminoacetonitrile↗
PubMed1977

Pharmacology of a new non-steroidal, anti-inflammatory agent: 6,11-dihydro-11-oxodibenz [b, e] oxepin-2-acetic acid (HP 549).

HP 549 is an orally effective non-steroidal anti-inflammatory agent with moderate analgesic and antipyretic activity. It is active in adjuvant-induced polyarthritis when given prophylactically or therapeutically. HP 549 also inhibits carrageenan-induced paw edema in the rat, an activity which is not altered by adrenalectomy. The analgesic activity of HP 549 was demonstrated in phenylquinone writhing. However, HP 549 produced variable results in the Randall-Selitto analgesia test. The anti-pyretic activity of HP 549 appears to be weak. HP 549, unlike other pharmacologically active anti-inflammatory drugs, does not produce gastric irritation at effective doses and is 45 times less ulcerogenic than indomethacin. Also the acute therapeutic indices for HP 549 are more favorable than for indomethacin.

Acetates↗
PubMed1983

Pharmacologic properties of fenbufen.

Fenbufen (Cinopal) is an orally active nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. Like clinically used nonsteroidal anti-inflammatory drugs, it shows activity in a wide spectrum of laboratory tests in mice, rats, guinea pigs, and dogs. Fenbufen has a long duration of anti-inflammatory and analgesic activity. Mechanistic studies indicate that fenbufen has no intrinsic effect on cyclooxygenase activity, whereas its major metabolite, biphenylacetic acid, is a potent inhibitor of prostaglandin synthesis. These observations indicate that fenbufen is a pro-drug and account for its low ulcerogenic potential. Anti-inflammatory pro-drugs that are readily metabolized to the biologically active molecule are expected to retain a favorable anti-inflammatory to ulcerogenic ratio because the gastrointestinal tract is not exposed to a large concentration of the active molecule. Comparative studies in the type II collagen arthritis model indicate that the anti-inflammatory properties of fenbufen are more potent than those of a second nonsteroidal anti-inflammatory drug, sulindac.

Animals↗
PubMed2004

Efficacy and safety of acetaminophen vs ibuprofen for treating children's pain or fever: a meta-analysis.

OBJECTIVE: To summarize studies testing the efficacy and safety of single-dose acetaminophen and ibuprofen for treating children's pain or fever. DATA SOURCES: Reports were gathered by searching computerized databases (from their inception through May 2002) and registries, relevant journals, and bibliographies of key articles. STUDY SELECTION: Seventeen blinded, randomized controlled trials with children (<18 years) receiving either drug to treat fever or moderate to severe pain. DATA EXTRACTION: Under a fixed-effects model, outcome measures for an initial single dose of ibuprofen vs acetaminophen were the risk ratio for achieving more than 50% of maximum pain relief, effect size for febrile temperature reduction, and risk ratio for minor and major harm. DATA SYNTHESIS: Ibuprofen (4-10 mg/kg) and acetaminophen (7-15 mg/kg) showed comparable efficacy (3 pain relief trials; 186 children). The risk ratio point estimates was 1.14 (95%confidence interval [CI], 0.82-1.58) at 2 hours after receiving the dose, and 1.11 (95% CI, 0.89-1.38) at 4 hours. Ibuprofen (5-10 mg/kg) reduced temperature more than acetaminophen (10-15 mg/kg) at 2, 4, and 6 hours after treatment (respective weighted-effect sizes: 0.19 [95% CI, 0.05-0.33], 0.31 [95% CI, 0.19-0.44], and 0.33 [95% CI, 0.19-0.47]) (9 fever trials; 1078 children). For ibuprofen 10 mg/kg (acetaminophen, 10-15 mg/kg), corresponding effect sizes were 0.34 (95% CI, 0.12-0.56), 0.81 (95% CI, 0.56-1.03), and 0.66 (95% CI, 0.44-0.87). There was no evidence the drugs differed from each other (or placebo) in incidence of minor or major harm (17 safety trials; 1820 children). CONCLUSIONS: In children, single doses of ibuprofen (4-10 mg/kg) and acetaminophen (7-15 mg/kg) have similar efficacy for relieving moderate to severe pain, and similar safety as analgesics or antipyretics. Ibuprofen (5-10 mg/kg) was a more effective antipyretic than acetaminophen (10-15 mg/kg) at 2, 4, and 6 hours posttreatment.

Acetaminophen↗
PubMed1992

Pharmacological studies of the new antiinflammatory agent 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-o ne. 1st communication: antiinflammatory, analgesic and other related properties.

The antiinflammatory, analgesic and antipyretic activities of 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-on e (T-614, CAS 123663-49-0) were investigated in various animal models and compared with those of nimesulide, indomethacin and ibuprofen. The antiinflammatory potency of T-614 on carrageenin-induced paw edema, paper disk granuloma and established adjuvant arthritis was greater than that of ibuprofen, but slightly lower than those of nimesulide and indomethacin. In acute inflammatory models, unlike indomethacin, T-614 suppressed the edemas provoked by dextran and bromelain in rats, but its inhibitory action on ultraviolet erythema in guinea-pigs was weak. Although the analgesic activity of T-614 was hardly demonstrated in writhing tests in mice, its potency against the inflammatory pain such as Randall-Selitto test, adjuvant-induced hyperalgesia and antigen-induced arthritic pain in rats was superior to that of ibuprofen. Moreover, it had a potent analgesic effect on urate-induced synovitis in dogs. T-614 exerted a prompt and strong antipyretic effect in both yeast-induced febrile rats and lipopolysaccharide-induced febrile rabbits. T-614 had virtually no gastrointestinal ulcerogenic action and did not affect water and sodium excretion in rats. T-614 is a novel antiinflammatory compound with different pharmacological properties from that of the reference drugs.

Animals↗
PubMed1987

Pharmacological properties of the novel non-steroidal antiinflammatory agent N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2 -one.

The antiinflammatory activity of the novel pyrrolidin-2-one derivative N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-o ne (E-5110) was investigated and compared with those of indomethacin and piroxicam in various antiinflammatory, analgesic and antipyretic animal models. The acute antiinflammatory activity of E-5110 on the carrageenin paw edema was similar to that of indomethacin, and half that of piroxicam. The chronic inflammatory responses in established adjuvant- and type II collagen-induced arthritis, which are widely used models of rheumatoid arthritis, were suppressed as effectively by E-5110 as by indomethacin and piroxicam. E-5110 decreased the pleural exudate volume and inhibited leucocyte infiltration in a reversed passive Arthus reaction more potently than indomethacin, suggesting that mediators other than prostaglandin E2 may play an important role in this inflammatory process. The analgesic potency of E-5110 against inflammatory pain was similar to that of indomethacin or piroxicam, but the antipyretic activity of E-5110 was more potent than that of the reference drugs. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than those of indomethacin and piroxicam. In conclusion, E-5110 is a very potent antiinflammatory compound acting against various types of inflammation, and has a favorable therapeutic index.

Animals↗
PubMed1995

[Efficacy of propacetamol in postoperative pain based on two modes of intravenous administration].

The analgesic and antipyretic efficacy of propacetamol is identical to paracetamol. Because the propacetamol is injectable and its side effects are uncommon and mild, it is the drug commonly used in France for postoperative pain relief. The aim of this prospective study was to compare the analgesic efficacy of propacetamol after breast surgery or thyroidectomy when it was administered either systematically or on the patients demand. After informed consent, 119 patients having undergone breast surgery or thyroidectomy, having received the same general anaesthesia and scheduled for receiving propacetamol postoperatively, were included in the study. Two groups of patients were compared, those who received propacetamol on demand (D Group) and those who received propacetamol systematically (S Group). During the first 24 hours, analgesia was evaluated on a visual analogical scale graded from 0 to 100 mm, at rest and during mobilization; the efficacy was also evaluated by the amount of additional analgesic drug injected. Side effects were also compared between the 2 treatment groups. In the 2 groups, demographic data, type of anaesthesia and type of surgery were identical. Postoperative pain relief and supplemental injection of morphine were not statistically different between the 2 groups. Propacetamol doses were statistically higher in the S group than in the D group (7.8 +/- 0.7 g and 3.9 +/- 2.3 g respectively, p < 0.05). Pain during propacetamol infusion was more frequent in the D group than in the S group (30% and 13% respectively, p < 0.05). No other adverse effects were observed during the study. Propacetamol alone is sufficient for pain relief after peripheral surgery; more than 90% of patients need no supplemental analgesic, and adverse effects are rare.

Acetaminophen↗
PubMed1997

Use of carprofen for the treatment of pain and inflammation in dogs.

Most studies of nonsteroidal anti-inflammatory drugs (NSAID) do not demonstrate appreciable differences in efficacy. As awareness of the adverse effects associated with NSAID use increases, safety is becoming the primary concern among physicians when selecting NSAID for use by their human patients. However, veterinarians may be less aware of the safety concerns associated with NSAID use. A wide range of NSAID is used to treat human beings with osteoarthrits; however, it is imperative to remember that dogs are especially sensitive to these drugs, and reports of serious, and occasionally fatal, complications are numerous. Carprofen is a propionic acid-derived NSAID that has anti-inflammatory, analgesic, and antipyretic activity. In animals, carprofen is as potent as indomethacina and more potent than aspirin or phenlbutazone, but carprofen appears to be safer than most other NSAID.

Acetaminophen↗
PubMed2000

[Specific cyclooxygenase-2 inhibitors. Basis and options of a pharmacotherapeutic concept].

The therapeutic and unwanted side effects of non-steroidal antiinflammatory drugs (NSAIDs) are attributable to inhibition of the cyclooxygenase (COX) enzyme which catalyzes the first step of the synthesis of prostanoids. In the early 1990s, COX was demonstrated to exist as two distinct isoforms. COX-1 is constitutively expressed as a 'housekeeping' enzyme in most tissues. In contrast, COX-2 can be upregulated by various proinflammatory agents, including endotoxin, cytokines and growth factors. Whereas many of the side effects of NSAIDs (e.g. gastrointestinal ulceration and bleeding, platelet dysfunctions) are due to a suppression of COX-1 activity, inhibition of COX-2-derived prostanoids facilitates the anti-inflammatory, analgesic and antipyretic effects of NSAIDs. Thus, the hypothesis that specific inhibition of COX-2 might have therapeutic actions similar to those of NSAIDs, but without causing the unwanted side effects, was the rationale for the development of specific inhibitors of the COX-2 enzyme as a new class of anti-inflammatory and analgesic agents with improved gastrointestinal tolerability. However, the simple concept that COX-2 is an exclusively proinflammatory and inducible enzyme cannot be supported any longer. Recently, COX-2 was shown to be also expressed under basal conditions in organs such as the ovary, uterus, brain, spinal cord, kidney and bone, suggesting that this isoenzyme may play a more complex physiological role than was expected. The present review assesses concept and molecular mechanism underlying specific COX-2 inhibition as well as indications, pharmakokinetics and unwanted side effects of the recently approved specific COX-2 inhibitors celecoxib and rofecoxib. Moreover, recent advances in COX-2 research, with particular emphasis on new insights into physiological functions of this isoenzyme will be discussed.

Animals↗
PubMed2004

Does paracetamol potentiate the effects of oral anticoagulants?: a literature review.

Paracetamol (acetaminophen) is the analgesic and antipyretic therapy of choice for patients receiving oral anticoagulation. It is widely used by patients in both prescription and over-the-counter products, resulting in frequent co-prescription with oral anticoagulants, especially in elderly patients. Indeed, older patients are the most likely to receive this combination of drugs because indications for both oral anticoagulation and analgesic therapy increase with age. For many years reports have presented evidence both for and against the idea that paracetamol may potentiate the anticoagulant effect of oral anticoagulants, thus increasing haemorrhagic risk in patients receiving this combination of drugs. This issue has continued to be a matter of debate in recent publications. No clear practical conclusion can be drawn from the studies because of methodological bias and the lack of clinical relevance. No prospective, randomised study assessing the effect of paracetamol on the anticoagulant effect of oral anticoagulants as used in clinical practice (i.e. the types of patients and dosages used in clinical practice) are available in the literature. The implications are considerable since on the one hand, the ingestion of paracetamol may be a cause of altered anticoagulation in patients who regularly take oral anticoagulation and who may have a haemorrhagic risk factor; and on the other hand, paracetamol might be the analgesic drug of choice that can be used without the need for any restrictions in patients receiving oral anticoagulant drugs. A comprehensive search of Medline and EMBASE for studies and case reports from 1966-2002 was performed in order to review the available literature on the interaction between paracetamol and oral anticoagulant drugs. In conclusion, the potential interaction between oral anticoagulant drugs and paracetamol is an important unanswered question, due to the growing incidence of the concomitant use of these drugs and the possible bleeding implications. The association between paracetamol and the occurrence of excessive INR values remains controversial due to lack of prospective clinical studies assessing the effect of the prescription of paracetamol in patients receiving long-term oral anticoagulation in clinical conditions. Such a study is currently ongoing.

Acetaminophen↗
PubMed1982

Pharmacological studies of a new non-steroidal antiinflammatory drug: 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043).

2-(5-Ethylpyridin-2-yl)benzimidazole (KB-1043) is a new benzimidazole derivative with marked antiinflammatory, analgesic and antipyretic properties. KB-1043 possesses potent inhibitory activities on the acute inflammatory edema induced by chemical and physical irritants in the hind paw of rats, but almost ineffective (similar to tiaramide) against adjuvant-induced polyarthritis in the rat. The antagonistic effects of KB-1043 on increased vascular permeability are more potent than those of phenylbutazone, and the analgesic effects of KB-1043 on the pain induced by chemical and mechanical stimulations were nearly equal to, or slightly less potent than, those of tiaramide and phenylbutazone. The fevers induced by brewer's yeast and polysaccharide from Pseudomonas fluorescens (T.T.G.) were lowered by KB-1043. THe ulcerogenic activity of KB-1043 was weaker than those of tiaramide and phenylbutazone. The therapeutic index of KB-1043 therefore is superior to those of tiaramide and phenylbutazone.

Analgesics↗