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Several species of the Chinese drug Angelica dahurica from different habitats have been studied in terms of anti-inflammatory, analgesic and antipyretic actions and acute toxicity. The medical value of these species is reported in this paper as a guideline for their clinic application.
Reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates 2 with phenylhydrazine gave the corresponding esters of 5-substituted 1-phenyl-1H-pyrazole-4-carboxylic acids 3 in high yields. Esters 3 were hydrolyzed to the relative carboxylic acids 4, which were converted by heating to 5-substituted 1-phenyl-1H-pyrazoles 5 in excellent yields. Reaction of methyl 5,5-dimethyl-3-dimethylaminomethylene-2,4-dioxohexanoate with phenylhydrazine afforded methyl 1-phenyl-4-pivaloyl-1H-pyrazole-5-carboxylate 8 b, which was converted as above to the corresponding carboxylic acid 10 b and this to 1-phenyl-4-pivaloyl-1H-pyrazole 11 b. Starting from 5-methoxymethyl-1-phenyl-1H-pyrazole, 1-phenyl-1H-pyrazole-5-acetic acid 18 and its alpha-methyl derivative 19 were also synthesized. Compounds 18, 19, 10 b and 11 b showed a strong antiinflammatory activity in rats; the same compounds in general as well as 8 b, showed appreciable analgesic and antipyretic activities in mice and rats, respectively.
Nonsteroidal anti-inflammatory drugs (NSAIDs) have anti-inflammatory, analgesic, and antipyretic properties. Although most NSAIDs inhibit prostaglandin synthesis, these agents also have important pharmacologic actions unrelated to their effects on prostaglandins. This review examines the evidence for diverse mechanisms of action of NSAIDs and their use in sports injuries.
One percent voltaren gel, a new drug manufactured by Ciba-Geigy [correction of Sib-Geigi], Switzerland, was used in the treatment of 57 patients with psoriasis in the progressive stage and psoriatic arthritis symptoms. The drug is characterized by antiinflammatory, analgesic, and antipyretic effects. No side effects or complications were recorded in the course of voltaren gel therapy. The drug has proved highly effective and is recommended for wide practice.
When the analgesic and antipyretic drug acetaminophen is exposed to the horseradish peroxidase/hydrogen peroxide system, light emission is observed. Both the rate of reaction and the emission intensity are increased in the presence of the cationic detergent CTAB. The emission spectrum indicates the presence of at least three emitters. The peak at 445 nm is close to the position of the only band observed in the fluorescence spectrum of the spent reaction mixture and is ascribed to excited N-acetyl-p-benzoquinoneimine. The other two emission bands (505 and 580 nm) must be due to transients. Total emission from the system increases in the presence of Triton X-100 solubilized-chlorophyll; the main donor to chlorophyll is the 445 nm emitter. The generation of excited species in this model system of acetaminophen peroxidative metabolization expands the number of candidates responsible for the deleterious effects of the drug in high doses.
Paracetamol, a widely used non-narcotic analgesic, has the same analgesic, and antipyretic efficacy as acetylsalicylic acid (ASA). In contrast to ASA, paracetamol has traditionally been claimed to have little or no anti-inflammatory effect. There is, however, increasing support for the view that paracetamol has anti-inflammatory activity and reduces pain and swelling in inflammatory conditions other than rheumatoid arthritis. Overall, paracetamol seems to be equally effective as ASA. Since ASA has a greater potential for adverse effects, paracetamol is increasingly preferred to ASA, particularly in children.
Antiinflammatory, analgesic and antipyretic activities of glycosidal fraction isolated from M. chisia were compared in battery of animal tests with known nonsteroidal antiinflammatory drugs (NSAIDs). The pharmacological activities compared favourably with NSAIDs whereas remarkable lack of toxicity was an added advantage.
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage of diclofenac sodium are reviewed. Diclofenac, the first nonsteroidal anti-inflammatory agent (NSAID) to be approved that is a phenylacetic acid derivative, competes with arachidonic acid for binding to cyclo-oxygenase, resulting in decreased formation of prostaglandins. The drug has both analgesic and antipyretic activities. Diclofenac is efficiently absorbed from the gastrointestinal tract; peak plasma concentrations occur 1.5 to 2.0 hours after ingestion in fasting subjects. Even though diclofenac has a relatively short elimination half-life in plasma (1.5 hours), it persists in synovial fluid. The drug is metabolized in the liver and is eliminated by urinary and biliary excretion. In clinical trials, diclofenac was as effective as aspirin, diflunisal, indomethacin, sulindac, ibuprofen, ketoprofen, and naproxen in improving function and reducing pain in patients with rheumatoid arthritis. For treatment of osteoarthritis, diclofenac was equivalent in efficacy to aspirin, diflunisal, indomethacin, sulindac, ibuprofen, ketoprofen, naproxen, flurbiprofen, mefenamic acid, and piroxicam. Diclofenac was as effective as indomethacin or sulindac in treating ankylosing spondylitis. The most frequent adverse effects reported for diclofenac were gastrointestinal, but these effects were fewer and less serious than occurred with aspirin or indomethacin; in addition, diclofenac caused fewer central nervous system reactions than indomethacin. Diclofenac is administered in divided doses with meals. The recommended total daily dosage is 100 to 150 mg (osteoarthritis and ankylosing spondylitis) or 150 to 200 mg (rheumatoid arthritis). Diclofenac is effective, but no more so than other NSAIDs. It is structurally distinct and offers another choice in the treatment of rheumatological conditions.
Two series of compounds, 2,3-dihydro-9H-isoxazolo[3,2-b]quinazolin-9-ones and 3,4-dihydro-(1,2)-oxazino-[3,2-b]quinazolin-10(2H)-ones, were synthesized and evaluated for anti-inflammatory, antipyretic and analgesic activity. The isoxazolo compounds were generally more active than their oxazino homologs. Three compounds, i.e., 2,3-dihydro-9H-isoxazolo [3,2-b]quinazolin-9-one (W-2429) and its 2- and 3-methyl congeners, were the most active of all compounds tested in this study. On the basis of the biological results herein reported, W-2429 is considerably more effective than acetylsalicylic acid in inhibiting carrageenan-induced edema and in reducing brewer's yeast-induced fever in rats. Also, it was found to be more potent than propoxyphene hydrochloride in the Randall-Selitto test for analgesic activity.
The effects of acidic and nonacidic pyrazole derivatives and their metabolites on arachidonic acid metabolism have been investigated in mouse peritoneal macrophages stimulated with the calcium ionophore A 23 187 (10(-6) Mol/l). In the group of the acidic compounds with anti-inflammatory properties, phenylbutazone and butyl malonic acid mono (1-phenylhydrazide), the hydrolysis product of mofebutazone, inhibited prostaglandin production in a dose-dependent manner (10(-4)-10(-6) Mol/l). In contrast, mofebutazone itself and its hydroxylation product, 4-OH-mofebutazone, failed to show any activity. Similarly, in the case of bumadizone, an anti-inflammatory drug structurally related to phenylbutazone, no inhibitory effect on prostaglandin release was found either. The nonacidic pyrazole derivatives with antipyretic and anti-inflammatory activity, antipyrine, isopropylaminophenazone, as well as metamizol and its active metabolites 4-methylaminophenazone and 4-aminophenazone, also inhibited prostaglandin release dose-dependently. This was found to be paralleled by an increased leukotriene C4 production. Neither of the main excretory metabolites of metamizol, acetyl- and formylaminophenazone, showed any effect. The concentration levels at which the nonacidic compounds affected arachidonic acid metabolism (approx. 10(-4) Mol/l) were high enough to elicit anti-inflammatory effects. They were far higher, though, than the plasma levels producing antipyretic and analgesic effects that are reached after therapeutic doses.
In experiments on various animals glyderinine, a derivative of glycyrrhizic acid isolated from Glycyrrhiza glabra, was found to exert a pronounced anti-inflammatory effect exceeding that of hydrocortisone and amidopyrine. The mechanism of the anti-inflammatory effect was to a certain degree related to the adrenal cortex, suppression of vascular permeability and antagonism to inflammation as well. Similarly to other anti-inflammatory agents, glyderinine possesses analgesic and antipyretic properties, but unlike them it fails to suppress hemopoiesis and to cause ulceration of the gastrointestinal mucosa. The drug is of low toxicity and exerts the antiallergic effect. Glyderinine was successfully tried and recommended for a wide use as an ointment for treating skin diseases.
An experimental and comparative study was conducted on 1-(p-chlorobenzoyl)-2-methyl-5-methoxyindole-3-p-acetamidophenol acetate (Apyramide) and known anti-inflammatory agents. Apyramide was far less toxic than indomethacin in rats and mice by the oral or the i.p. route. It exhibited anti-inflammatory activity on carrageenin-induced paw oedema, cotton pellet granuloma and adjuvant arthritis, as well as analgesic and antipyretic activities. The acute ulcerogenic effect of Apyramide was lower than that of indomethacin.
An open trial of piroxicam, a new nonsteroidal anti-inflammatory agent with long-lasting analgesic and antipyretic activities, was carried out on 49 children as outpatients with viral rhinopharyngitis. Piroxicam administered once daily as an oral suspension gave significant improvement in all parameters, both respiratory (nasal obstruction and discharge, hoarseness, sore throat) and general (headache, dysphagia). A lowering in body temperature was also observed. Recovery seemed to have a more favourable trend in patients treated with piroxicam than to previous treatments. Tolerability of piroxicam was satisfactory in all but six patients who showed only slight transitory side-effects.
Optical resolution of (+/-)-2-(4-dimethylvinylphenyl)propionic acid (I) was performed through fractional crystallization of its salts with (S)-(-)- and (R)-(+)-alpha-phenylethylamine. 2-(4-Dimethylvinylphenyl)propionic acid, in comparison to ibuprofen, has greater antiinflammatory, analgesic and antipyretic activities, as well as a higher therapeutic index. Absolute configuration was determined by comparison of the (S)-(-)-alpha-phenylethylamide 1H-N.M.R. spectra of the enantiomers of (I) and of the enantiomers of ibuprofen whose configuration was already known. Thus, the absolute configuration (S) was assigned to (+)-(I).
Twenty-six cases of Reye syndrome from The Children's Hospital, Camperdown, Australia, occurring between 1973 and 1982 were reviewed. Of these, 20 cases met the US Public Health Service Centers for Disease Control criteria for the diagnosis of Reye syndrome. Aspirin or salicylate ingestion had occurred in only one of the 20 cases (5%), and paracetamol (acetaminophen) had been administered in only six of the cases (30%). Pathologic confirmation of the diagnosis of Reye syndrome was accomplished in 90% of the cases. The incidence of Reye syndrome in New South Wales, Australia, is estimated from this study to be approximately nine cases per 1 million children compared with recent US data of ten to 20 cases per 1 million children and three to seven cases per 1 million children in Great Britain. The mortality for these Reye syndrome cases in Australia was 45% as compared with a 32% case-fatality rate in the United States. In Australia, the pediatric usage of aspirin has been extremely low for the past 25 years (less than 1% of total dosage units sold), with paracetamol (acetaminophen) dominating the pediatric analgesic and antipyretic market. Reye syndrome may be disappearing from Australia despite a total lack of association with salicylates or aspirin ingestion, since there were no cases found at The Children's Hospital in 1983, 1984, or 1985.
Acetaminophen is a popular analgesic and antipyretic medication that has few side effects and little toxicity when used in recommended doses. With ingestion of overdose quantities, accumulation of toxic metabolites may cause hepatotoxicity. Acetylcysteine is an effective antidote when used early in the course of an acute overdose. An accurate history of the time of ingestion and an acetaminophen plasma level will determine which patients require treatment with acetylcysteine.
Analgesics containing dipyrone continue to be available throughout Africa, including South Africa and Zimbabwe. Although an effective analgesic and antipyretic, dipyrone may cause severe side-effects, including agranulocytosis. The mechanism of this hypersensitivity reaction has been well documented, and many reports of agranulocytosis associated with dipyrone use have been published. Use of this drug has been prohibited or restricted in several countries. Dipyrone is known by a variety of official names, which may contribute to confusion in deciding whether a particular preparation contains this drug. The prescribing information contained in the Monthly Index of Medical Specialities (MIMS) (South Africa) and the MIMS Desk Reference is inadequate for some of the products available, although the package inserts do provide more detailed information. The continued use of these products is difficult to justify when safer alternatives are available.
In Thailand, 5 years ago, the Ministry of Public Health set up the National Adverse Drug Reaction Monitoring Center for collecting, analysing and compiling all evidence related to drug hazards. Between March 1983 and December 1985, 790 reports on adverse drug reactions have been received, of which 711 could be analysed. Adverse drug reactions are commonly reported with the antibiotics, other anti-infective agents, analgesics and antipyretics, and anti-inflammatory drugs. Most of the reported reactions are related to skin reactions and gastrointestinal disorders. It is unquestionable that such voluntary reporting is more useful qualitatively than quantitatively. Even though there are a lot of problems facing us in assessing adverse drug reactions, it is a necessity to have the programme running and improving as time goes by. There is an urgent need for well-trained personnel to perform such tasks.