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PubMed1994

3,3'-Bi-[1,3-thiazolidine-4-one] system. VII. Synthesis and SARS of some 2-heteroaryl derivatives with antiinflammatory and related activities.

In pursuing the research on the SARs of chiral 3,3'-Bi-[1,3-thiazolidine-4-one] system derivatives, two new structural modifications were explored, both having on chiral C atoms thienyl or 2/3 pyridyl groups which have been found to improve antiinflammatory and related activities in the previously studied 3,3'-(1,2-ethanediyl)bisthiazolidinones. In particular a trimetylene chain was introduced between N-3 and N-3' thus obtaining the 3,3'-(1,3-propanediyl) derivatives [type Ic compounds], whereas by elimination of a thiazolidinone ring the 2-heteroaryl-3-[2'(heteroarylidenamino) ethyl]-1,3-thiazolidine-4-one derivatives (type II compounds) were prepared. The new compounds were explored in vivo for their antiinflammatory, analgesic, antipyretic activities, as well as for acute toxicity and ulcerogenic effects. The results obtained don't allow us to draw any reliable SAR except that, by increasing the distance between thiazolidinonic rings, in Ic compounds, the pharmacological profile is not improved with respect to (1,2-ethanediyl) inferior homologs. Among compounds II, only the thienyl derivative 5 appears to have antiinflammatory and analgesic activities.

Acetates↗

PubMed1976

A new analgesic testing method using ultrasonic stimulation. I. Effects of narcotic and nonnarcotic analgesics.

A quantitative method for measuring pain threshold by the use of ultrasonic stimulation in mice has been designed. The method had the advantage of precision, simplicity of technique, rapidity of measurement, and the fact that the stimuli is innocuous upon repeated application. The nature of the senstaions induced by ultrasonic stimulus is somewhat like that felt with a prick type of pain. Pentazocine (30, 100, 150 mg/kg i.p.) aminopyrine (15,50, 100, 150 mg/kg i.p.), phenacetin (100,150, 200, 250 mg/kg i.p.) sodium salicylate (150, 200, 250 mg/kg i.p.) and other antipyretic analgesics were active in a wide range of doses indicating that this technique is sensitive to the narcotic antagonist and to the weak analgesics as well as to the narcotic analgesics as well as to the narcotic analgesics such as morphine (2.5, 5, 10, 15 mg/kg i.p.), codeine (10, 20, 25, 30, 50 mg/kg i.p.) and pethidine (5,10, 15, 20, 25 mg/kg i.p.). The ultrasonic method is, therefore, applicable in screening procedures when attempting to evaluate the analgesic potency of a wide variety of chemical agents.

Age Factors↗

PubMed1999

Bioactivity studies of Salvia transsylvanica (Schur ex Griseb) grown in Egypt.

Some pharmacological effects of the ethanol extract of Salvia transsylvanica (Schur ex Griseb) were experimentally investigated. The tested extract of the plant proved to be relatively nontoxic (LD50 = 4.437 g/kg b.wt.). The extract induced significant analgesic, antipyretic, antiepileptic, antiinflammatory, antiulcerogenic, as well as tranquillizing activities, besides increasing the bleeding time and exhibiting no central skeletal muscle relaxant effect compared with control groups and standard drugs.

Analgesics↗

PubMed1995

2-aryl-3-phenylamino-4,5-dihydro-2H-benz[g]indazoles with antiarrhythmic and local anaesthetic activities.

The synthesis of novel 2-aryl-3-phenylamino-4,5-dihydro-2H-benz[g]indazoles 4a-f, starting from N-phenyl-3,4-dihydro-1(2H)-oxonaphthalene-2-carbothioamide and the proper arylhydrazines, is described. Title compounds were evaluated for antiinflammatory, analgesic, antipyretic, antiarrhythmic, hypotensive, local anaesthetic and platelet antiaggregating activities; some of them showed an appreciable antiarrhythmic activity in rats and a good level of infiltration anaesthesia in mice.

Analgesics↗

PubMed1997

Formulation of an aqueous injection of flurbiprofen.

Flurbiprofen (1) is an analgesic, antipyretic and antiinflammatory agent which is practically insoluble in water. The aqueous solubility of 1 using various hydrotropes was attempted. The solubility increased up to 63 times in the case of sodium benzoate. Using selected hydrotropes, aqueous injections of 1 were formulated. Formulations were studied for physical and chemical stability. Some of the formulations showed reasonable stability which can be further enhanced by incorporation of appropriate formulation additives. These formulations were evaluated for antiinflammatory and analgesic activity and showed promising results.

Administration, Oral↗

PubMedDate not supplied

Pharmacology, clinical efficacy, and adverse effects of the nonsteroidal anti-inflammatory agent benoxaprofen.

Benoxaprofen is a nonsteroidal anti-inflammatory agent that belongs to the arylalkanoic acid class of antirheumatic drugs. Animal studies have demonstrated that it has analgesic, antipyretic, and anti-inflammatory properties. Although benoxaprofen is a relatively weak inhibitor of cyclo-oxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation, it has not been established that it is unique with regard to these actions. Benoxaprofen undergoes hepatic metabolism via glucuronidation as the primary route of elimination and has a half-life of 28-35 hr. Clinical trials have demonstrated that its analgesic and anti-inflammatory properties are useful in the management of the signs and symptoms of rheumatoid arthritis and osteoarthritis. Once daily dosing of 300-600 mg is effective for many patients. In addition to gastrointestinal intolerance, photosensitivity and onycholysis are the most frequent adverse effects encountered. Recent reports of fatal cholestatic jaundice often associated with nephrotoxicity led to the withdrawal of benoxaprofen from world markets. It is uncertain whether it will once again be available for clinical use.

Animals↗

PubMed2002

Acetaminophen (paracetamol)-induced anaphylactic shock.

Acetaminophen (paracetamol) is a widely prescribed analgesic-antipyretic drug. Adverse allergic reactions to this drug are rare. We report a case of anaphylactic shock due to acetaminophen. Results of skin prick tests and intradermal tests were negative. Oral rechallenge resulted in generalized urticaria associated with an increased plasma level of histamine. Acetaminophen should be added to the list of causes of anaphylaxis.

Acetaminophen↗

PubMed2006

Prevalence and characteristics of adverse drug reactions in neurosurgical intensive care patients.

OBJECTIVE: To evaluate the prevalence and characteristics of adverse drug reactions (ADRs) in neurosurgical intensive care patients. METHODS: Retrospective analysis of ADR data obtained from a spontaneous reporting system in a tertiary care university hospital. Reports of suspected ADRs in adult patients admitted emergently or electively to the neurosurgical service were included. RESULTS: Over the 3 year period, 3496 neurosurgical intensive care unit (ICU) patient admissions accounted for 5% of all hospital admissions. A total of 10% of all neurosurgical patients developed a suspected ADR, with three patients experiencing multiple reactions. Other adult ICU patients developed ADRs at a comparable rate (9%, P > 0.05). Overall, neurosurgery patients accounted for 12% of all spontaneously reported ADRs. Preventable reactions were observed in 43 (13%) cases, and treatment was required for 76%. The majority (96%) of ADRs resolved or improved at the time of the ADR report. Nausea, pruritus, thrombocytopenia, and vomiting were most frequently noted. Therapies most often associated with reported events were analgesics, antipyretics, antibiotics, anticonvulsants, and histamine H2 antagonists. The relationship between central nervous system disease and adverse event occurrence is not clear. CONCLUSION: Despite the narrow scope of drug regimens in neurosurgical ICU patients, ADRs can complicate therapy in this critically ill population. Neurosurgical ICU patients seem to experience ADRs no more frequently than their adult ICU counterparts.

Adult↗

PubMed1982

Hospital admissions for adverse effects of medicinal agents (mainly self-poisoning) among adolescents in the Oxford Region.

Hospital statistics for episodes coded as adverse effects of medicinal agents' were used to study deliberate self-poisoning among people aged 12-20 years in the Oxford Region. Admission rates rose sharply from the age of 12 years, more so for females than males, up to the age of 16 years in females and 18 years in males. Analgesics, antipyretics and psychotropic drugs were the agents most commonly used by both sexes and accounted for three-quarters of all admissions. Admission rates varied from year to year, but increased overall between 1974 and 1979, notably among people under 16 years of age. Admissions for 'adverse effects of medicinal agents' accounted for 4.7 per cent of all general admissions among people aged 12-20 years.

Adolescent↗

PubMed1991

[Acute myocardial injury and repeated angina pectoris-like attacks in a young patient with Churg-Strauss syndrome].

A 23-year-old male with bronchial asthma developed eosinophilia (eosinophils greater than 2,000/mm3) and was observed at our hospital. After using a prescribed indomethacin suppository for fever at home, he experienced an attack of acute chest pain and severe dyspnea. He suffered cardiac arrest while being transferred to the ward. After resuscitation, he was diagnosed as having acute myocardial infarction on the basis of electrocardiographic and ultrasonic cardiographic findings, and marked elevation of serum concentrations of myocardial enzymes. Thereafter, he often complained of precordial pain and abdominal pain. When he was administered an analgesic in another hospital, he developed severe precordial pain, and marked ST elevation was recorded on the electrocardiogram. Coronary angiography revealed no stenosis nor atherosclerotic changes, suggesting that severe spasm of the coronary arteries and direct myocardial injury by eosinophils were the causes of the myocardial infarction-like symptoms and angina pectoris-like attacks. He was diagnosed as having Churg-Strauss syndrome (allergic granulomatous angiitis) on the basis of the clinical findings; skin biopsy and transbronchial lung biopsy findings were consistent with the diagnosis. Following steroid administration, his angina-like attacks and abdominal pain ceased. This patient developed two episodes of acute cardiovascular symptoms upon administration of antipyretic analgesics. This suggests that in cases of Churg-Strauss syndrome with aspirin-induced asthma, physicians must be aware of the cardiovascular complications, and such drugs should be administered with caution.

Adult↗

PubMed1989

Ethnopharmacologic investigation of ginger (Zingiber officinale).

An ethanolic extract of the rhizomes of Zingiber officinale was investigated for anti-inflammatory, analgesic, antipyretic, antimicrobial and hypoglycaemic activities. In rats, the extract reduced carrageenan-induced paw swelling and yeast-induced fever but was ineffective in suppressing the writhing induced by intraperitoneal acetic acid. The extract produced blood glucose lowering in rabbits. The growth of both Gram-positive and Gram-negative bacteria was significantly inhibited. A dose-dependent inhibition of prostaglandin release effect was observed using rat peritoneal leucocytes.

Analgesics↗

PubMedDate not supplied

Adverse reaction of acetaminophen as an alternative analgesic in A.A.S. Triad.

The syndrome of A.A.S. Triad consisting of an intolerance to analgesics such as aspirin, bronchial asthma and nasal polyps, is every day more frequent. During the last years, the use of acetaminophen as an analgesic-antipyretic alternative in patients with A.A.S. Triad has been imperative. However, there are already publications that show reversible bronchial obstruction symptoms similar to the ones produced by A.A.S., though of less intensity. A study was performed in 32 patients diagnosed of A.A.S. Triad by our allergy specialized office with a challenge test of acetaminophen and placebo. Basal spiromentry, physical examination and control of medication before the test, were noted. Of the 32 patients studied, six of them showed a positive provocation test. We maintain the need to perform a provocation test with acetaminophen at the hospital under medical observation before the medication is used by the patient. In terms of practical medicine, this study with acetaminophen as medications of common use in A.A.S. Triad underlies the importance of more caution in prescribing analgesic drugs to patients sensitive to aspirin and A.I.N.E.

Acetaminophen↗

PubMed2001

Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; partial final rule for combination drug products containing a bronchodilator. Final rule.

The Food and Drug Administration (FDA) is issuing a final rule establishing that cough-cold combination drug products containing any oral bronchodilator active ingredient in combination with any analgesic(s) or analgesic-antipyretic(s), anticholinergic, antihistamine, oral antitussive, or stimulant active ingredient are not generally recognized as safe and effective and are misbranded for over-the-counter (OTC) use. FDA is issuing this final rule after receiving no public comments on the agency's proposed nonmonograph status of these specific combination drug products, which was issued in the form of a tentative final monograph for OTC cough-cold combination drug products. This final rule is part of the ongoing review of OTC drug products conducted by FDA.

Analgesics↗

PubMed1998

[Treatment of acute otitis media in children].

Acute otitis media in children have to be treated by analgesics, antipyretics and antibiotics. The choice of the antibiotic depends on the child's age, associated clinical symptoms such as conjonctivitis, and any recent history of antibiotic treatment. Children over 2 are treated by amoxicillin or CG1, children with conjunctivitis are treated by amoxicillin + clavulanate acid, infants attending day care centers and with recent history of antibiotic treatment have to be treated by cefuroxim-axetil, cefpodoximproxetil or high dosages of amoxicillin. In case of unsatisfactory course of the disease, the infecting organism has to be identified by tympanocentesis.

Acute Disease↗

PubMed1977

Pharmacological properties of the anti-inflammatory agent pyridyl-biphenylyl-acetamide (diphenpyramide).

Pyridyl-biphenylyl-acetamide (diphenpyramide, Z-876) is a new bisphenylalcanoic derivative with marked anti-inflammatory, analgesic, antipyretic and uricosuric properties. It is more active than phenylbutazone in the adjuvant polyarthritis in the rat when given prophylactically or therapeutically. It is thrice as active as phenylbutazone and ten times as active as acetylsalicylic acid (ASA) on the carrageenin-induced edema of the hind-paw. Diphenpyramide is characterized by low acute toxicity and by weak ulcerogenic activity. On the carrageenin-induced edema the therapeutic index of diphenpyramide is 30 times higher than that of indometacin and the ratio between the ED50 and the UD50 (ulcerogenic dose in 50% of the treated rats) is 39 times higher than that of ASA.

Acetamides↗

PubMed1997

[Legal format and costs of prescriptions at the Central Hospital in Yaounde, Cameroon].

Prescribing treatment is the last act of a medical visit. A prescription is a written document that engages the medical and legal responsibility not only of the physician but of all those subsequently involved in its execution. In countries with weaker economies and more limited health care insurance the costs of filling a prescription can place a heavy financial burden on the families. In the present study we analyzed 285 prescriptions written in the Emergency Room and Outpatient Clinic of Central Hospital in Yaounde, Cameroon. In most cases prescribers were in compliance with legal requirements regarding their identity, but in 20 to 30% of cases neither the name nor function of the prescriber was mentioned. Most prescriptions were written legibly and coherently for both paramedical personnel and the patient. The number of products prescribed ranged from 2 to 5 depending on the issuing department. Practitioners in the outpatient clinic prescribed few brand-name products from the public outlet of the hospital pharmacy (16% of the prescriptions). In 68% of the cases a generic replacement was available. Practitioners in the emergency room were more apt to prescribe brand-name products (73% of the prescriptions). Five classes of drugs accounted for two thirds of prescriptions, i.e. analgesics-antipyretics, usual antibiotics, antimalarials, non-steroid anti-inflammatory drugs, and vitamins. Lawfully required information (drug presentation, route of administration, dose unit, directions and duration of treatment) was stated on 85% of prescriptions from the outpatient clinic and 50% from the emergency room. Although there were large variations, the mean cost of filling a prescription at the town pharmacy was identical in the two groups, i.e. 9500 CFA francs. The cost was 50% lower at the hospital pharmacy. All prescribers and in particular medical students should receive instruction in prescription writing. Careful selection of brand and non-brand-name drugs in agreement with practitioners should achieve further reductions in the cost of filling a prescription in hospital pharmacy.

Analgesics↗

PubMed1976

Analgesic and anti-inflammatory activity of 6-chloro-alpha-methyl-carbazole-2-acetic acid (C-5720).

The carbazole, C-5720, has the same order of analgesic, antipyretic and anti-inflammatory activity as indomethacin and is more potent than phenylbutazone and acetylsalicylic acid in the yeast inflamed paw, the carrageenin foot edema, the Mycobacterium butyricum-induced pyrexia, and the acute and chronic adjuvant arthritis tests. In chronic adjuvant arthritis in rats, C-5720 lowers the elevated serum mucopolysaccharide and plasma fibrinogen levels, and partially restores the depressed liver N-demethylase activity. C-5720 is 16 times less active than indomethacin in the production of gastric ulcers in rats and is about 70 times less active than indomethacin in blocking arachidonic acid-induced diarrhea in mice. C-5720 has a greater safety margin than indomethacin with respect to the production of gastric ulcers or the blockade of diarrhea and the reduction of inflammation in adjuvant-induced polyarthritis.

Analgesics↗

PubMedDate not supplied

Drug interactions with paracetamol.

Paracetamol (acetaminophen) is one of the most commonly used analgesic antipyretic drugs worldwide, and it is widely available by prescription and over the counter (OTC). Fortunately, few clinically significant drug interactions have been documented. There is probable potentiation of hepatotoxicity following an overdose from the paracetamol metabolite NAPQI by enzyme-inducing drugs. There is considerable controversy regarding the possible interaction with warfarin in its potential to increase its anticoagulant effects because of discrepancies between observational studies and those in healthy volunteers. Otherwise, no serious adverse drug interactions with therapeutic doses of paracetamol have been confirmed in humans. Because the absorption of paracetamol is so dependent on gastric emptying, other drugs that alter gastric emptying can change its pharmacokinetics; but this would not cause serious adverse effects. Although animal experiments have demonstrated that many compounds can modify paracetamol hepatotoxicity, these are unlikely to be important at therapeutic doses.

Acetaminophen↗