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PubMed1979

Pharmacological profile of mangostin and its derivatives.

Mangostin (M), a naturally occurring xanthone in the rinds of the fruits of Garcinia mangostana Linn. (Guttiferae) and its derivatives such as 3-0-methyl mangostin (MM), 3,6-di-O-methyl mangostin (DM), 1-isomangostin (IM), mangostin triacetate (MT), mangostin 3,6-di-O-(tetra acetyl) glucoside (MTG) and mangostin-6,6-di-O-glucoside (MOG) were screened for various pharmacological effects in experimental animals. With the exception of DM all the test compounds produced CNS depression characterised by ptosis, sedation, decreased motor activity, potentiation of pentobarbital sleeping time and ether anaesthesia in mice and rats. None of the compounds exhibited analgesic, antipyretic and anticonvulsant effects. With the exception of MOG, none of the test compounds produced significant effects on the cardiovascular system of frogs and dogs. MOG produced myocardial stimulation and a rise in blood pressure which was partially blocked by propranolol. M, IM and MT produced pronounced antiinflammatory activity both by intraperitoneal and oral routes in rats as tested by carrageenininduced hind paw oedema, cotton pellet implantation and granuloma pouch techniques. Antiinflammatory activity for M, IM and MT was observed even in bilaterally adrenalectomised rats. M, IM and MT did not produce any mast cell membrane stabilising effect and the degranulation effect of polymyxin B, diazoxide and Triton X-100 on rat peritoneal mast cells in vitro was not prevented. M, IM and MT did not alter the prothrombin time of albino rats. M alone produced significant antiulcer activity in rats.

Analgesics↗

PubMed2000

Paracetamol (acetaminophen) hypersensitivity.

BACKGROUND: Acetaminophen (paracetamol) is an analgesic antipyretic drug with no antiinflammatory effects and is widely used worldwide. Earlier clinical studies reported IgE-mediated adverse reactions to acetaminophen, but in vivo and in vitro tests have been inconclusive. OBJECTIVE: We propose to demonstrate an IgE-mediated mechanism in four patients with adverse reactions to acetaminophen (paracetamol). Tolerance to aspirin and other nonsteroidal antiinflammatory drugs are present in all patients. METHODS: We studied four patients with anaphylactic reactions to acetaminophen who tolerated aspirin and other nonsteroidal antiinflammatory drugs. Skin tests, oral challenges and immunoassay for allergen-specific IgE antibodies with acetaminophen were performed in all patients. RESULTS: All patients tolerated the aspirin oral challenge without adverse effects. In contrast, the oral challenge with acetaminophen produced adverse effects in all patients. Skin tests with acetaminophen were positive in two patients (3-mm wheal and flare) and IgE antibodies acetaminophen were detected in serum from two patients. CONCLUSION: We describe four patients with adverse reactions to acetaminophen but with tolerance to aspirin and other nonsteroidal antiinflammatory drugs. Skin tests, oral challenges, and serum IgE results with acetaminophen suggest that an IgE-mediated mechanism is responsible for these reactions.

Acetaminophen↗

PubMed2002

Effects of dipyrone on inflammatory infiltration and oxidative metabolism in gastric mucosa: comparison with acetaminophen and diclofenac.

In the last several years, it has been proposed that neutrophil- and oxygen-dependent microvascular injuries may be important factors in the gastrointestinal toxicity of nonsteroidal antiinflammatory drugs (NSAIDs). In addition, after oral administration, reduced levels of gastric mucosal adenosine triphosphate in response to mitochondrial damage constitute the earliest event on topical mucosal erosions. In these experiments, we compared the implication of active oxygen, lipid peroxidation levels and neutrophil infiltration in gastric mucosal injury induced by the analgesic-antipyretic drugs, dipyrone (pyrazolone derivative) and acetaminophen (nonacidic drug), both with relatively weak antiinflammatory effects, with diclofenac (an acidic NSAID). After 6 hr of oral administration, dipyrone (120 and 500 mg/kg) did not provoke macroscopic lesions on rat gastric mucosa. Only the highest dose (1000 mg/kg) induced slight erosions similar to the same dose of acetaminophen without modifications in lipid peroxidation levels or myeloperoxidase activity. The area of mucosa with lesions, the increase in neutrophil infiltration, and concentration of TBA-reactive substances was significantly higher with diclofenac (50 mg/kg). By contrast, inhibition in superoxide dismutase activity was observed. In a dose-dependent manner, dipyrone and diclofenac decreased the levels of endogenous gluthatione, and the highest dose (1000 mg/kg) also inhibited glutathione peroxidase activity. None of treatments induced changes in xanthine oxidase activity, an index of ischemic condition. These findings confirm the favorable gastric tolerability of dipyrone, since only the highest dose produced weak mucosal lesions similar to that obtained with acetaminophen, and this effect only could be related to a diminished glutathione metabolism. In contrast, diclofenac induced significant erosions, and the data obtained indicate that the enhancement of oxidative stress plays an important role in the pathogenesis of damage.

Acetaminophen↗

PubMed1996

Nonrenal toxicities of acetaminophen, aspirin, and nonsteroidal anti-inflammatory agents.

Approximately 2% of the United States population consumes an analgesic, antipyretic, or nonsteroidal antiinflammatory drug (NSAID) each day. Aspirin and acetaminophen have been available to the public without a prescription (over-the-counter) for decades, while most NSAIDs are still only available with a prescription from a physician. The recent trend of switching NSAIDs from prescription to over-the-counter status may be perceived by some as an indication of their inherent safety. However, all these agents have been associated with a unique but overlapping safety profile. In fact, significant adverse events (AEs) on multiple organ systems, including the kidney and gastrointestinal tract, have been reported with most of these agents. In this review, the incidence of the nonrenal AEs of aspirin, acetaminophen, and selected NSAIDs are tabulated. The strengths of the causative associations are highlighted, the relative risks for the gastrointestinal and cardiovascular AEs are discussed, and the relationship to patient risk factors and drug characteristics, such as dose and half-life, are reviewed. The selection of the optimal agent for an individual patient depends on the balance between the desired pharmacodynamic response, the patient's pharmacotherapy history, and the degree of AE risk one is willing to accept. Therapy should be initiated in all settings with the lowest possible dosage since the incidence of the major AEs is dose related.

Acetaminophen↗

PubMed1999

[Aspirin].

Acetylsalicylic acid (aspirin) was the first synthetized drug 100 years ago. Whereas other drugs have disappeared a long time ago, aspirin has stood the test of time and is one of the most important drugs at the turn of this century. Initially it was used for its analgesic, antipyretic and antiphlogistic properties. They are due to the acetylation of the cyclooxygenase and hence an inhibition of prostaglandin synthesis. At higher doses aspirin inhibits interleukin expression induced by nuclear factor-kappa B. Aspirin is the prototype of nonsteroidal antiinflammatory drugs, which are currently challenged by the development of specific inhibitors of cyclooxygenase isoform 2 (COX-2), which must, however, first prove their efficacy and safety in clinical trials. The inhibition of platelet aggregation by aspirin has only been recognized in the second half of the century. It is due to an inhibition of thromboxane A2 synthesis because of an irreversible cyclooxygenase blockade in platelets. Aspirin has been found to reduce the incidence and death rate of cardiovascular and cerebrovascular events and is nowadays the cornerstone of any secondary prevention in vascular diseases. Newer antiaggregatory agents such as ticlopidine, clopidogrel or IIb/IIIa-blockers have been developed. Most often they are used in conjunction with aspirin and their place has yet to be defined. New modes of action of aspirin continue to be found. Recent examples are an improvement of endothelial dysfunction or a reduced incidence of colorectal cancers. It is therefore likely that aspirin will continue to be a very useful and cheap drug for a very large population and will meet the interest of researchers for many more decades.

Analgesics↗

PubMed2005

Does dipyrone have any effect on respiratory function in COPD patients?

OBJECTIVE: Dipyrone (Novalgin) is an effective analgesic, antipyretic agent also with spasmolytic effects on various types of smooth muscles. It has recently been reported that dipyrone relaxes tracheal smooth muscle of guinea pig. In this present study, we aimed to investigate whether this and previously reported in vitro results have any consequences on the respiratory function of normal healthy volunteers and chronic obstructive pulmonary disease (COPD) patients. METHODS: In this one-centered, non-randomized, non-comparative, open labelled study, 15 normal healthy volunteers and 15 stable COPD patients, with partially reversible bronchospasm, diagnosed according to the Global Initiative for Chronic Obstructive Lung Disease (GOLD) criteria were enrolled in the study at the time they had any indication of dipyrone use. The spirometric tests were performed by a portable notebook and Medikro Spiro2000 spirometry programme-software 1.6 version, before 30, 60, 90, and 120 min after 20 mg/kg of orally dipyrone intake. Groups were compared with the General Linear Model Repeated Measures analysis of variance. RESULTS: None of the spirometric parameters evaluated showed any significant differences when compared with the baseline values in both groups. CONCLUSION: While dipyrone had no bronchodilator effects on either COPD patients or normal volunteers, it also did not impair the spirometric parameters. Since COPD is a disease characterized by a progressive and largely irreversible airflow limitation, dipyrone has no observable bronchodilator effect. However, since dipyrone does not impair the pulmonary function, it can be used safely in COPD patients when there is an indication.

Adult↗

PubMed2005

Shift from biliary to urinary elimination of acetaminophen-glucuronide in acetaminophen-pretreated rats.

Despite its toxicity, acetaminophen (APAP) is used increasingly as an analgesic, antipyretic, and anti-inflammatory agent. We examined the effect of prior exposure to APAP on its biliary and urinary elimination. The biliary and urinary elimination of a test dose of APAP (150 mg/kg i.v.) was determined in male Wistar rats 24 h after pretreatment with vehicle, a single dose (1.0 g/kg i.p.), or increasing daily doses (0.2, 0.3, 0.6, and 1.0 g/kg/day i.p.) of APAP. Although elimination of the parent APAP was minimally affected, biliary excretion of APAP glucuronide was significantly decreased 70 and 80%, whereas urinary excretion was significantly increased 90 and 100% in the groups pretreated with single and repeated doses of APAP, respectively, relative to vehicle controls. Western analysis and confocal immunofluorescent microscopy indicated a marked increase in hepatic expression of multidrug resistance-associated protein 3 (Mrp3) in both groups pretreated with APAP, relative to expression of Mrp2. ATP-dependent transport of [3H]taurocholate, an Mrp3 substrate, was significantly increased in basolateral liver plasma membrane vesicles from rats pretreated with repeated doses of APAP relative to controls. Enterohepatic recirculation of APAP glucuronide after administration of the same test dose of the drug was significantly decreased in rats pretreated with repeated doses of APAP. These data indicate that APAP pretreatment induced a shift from biliary to urinary elimination of APAP glucuronide, consistent with the increased expression of Mrp3 in the basolateral domain of the hepatocyte. We postulate that decreased enterohepatic recirculation contributes to decreased APAP hepatotoxicity by reducing liver exposure.

Acetaminophen↗

PubMed2000

Paracetamol: past, present, and future.

Paracetamol (acetaminophen) is one of the most widely used of all drugs, with a wealth of experience clearly establishing it as the standard antipyretic and analgesic for mild to moderate pain states. First used clinically by von Mering in 1893, paracetamol did not appear commercially until 1950 in the United States and 1956 in Australia. During the 1960s and 1970s, increasing concern was raised about the toxicity of nonprescription analgesics, but in normal use paracetamol exhibited a consistent safety profile. Its exemplary safety record was marred by the discovery in 1966 that a major overdose could be complicated by severe and sometimes fatal liver damage. Fortunately, early treatment with N-acetylcysteine prevents liver toxicity. A turning point in the choice of pediatric analgesic came in the 1980s when aspirin was linked to Reye's syndrome. As a consequence, paracetamol became the mainstay analgesic and antipyretic for children with a subsequent reduction in the incidence of Reye's syndrome. Currently, paracetamol is a first-line choice for pain management and antipyresis in a variety of patients, including children, pregnant women, the elderly, those with osteoarthritis, simple headaches, and those with noninflammatory musculoskeletal conditions. With proper use, paracetamol seldom causes adverse events and reports of serious side effects are rare. It has a broad tolerability and is of particular value in the treatment of patients in whom nonsteroidal anti-inflammatory drugs are contraindicated such as aspirin-sensitive asthmatics and people at risk of gastrointestinal complications. In the future, a better insight into the mechanism of action of paracetamol may be gained from a fuller understanding of the cyclooxygenase enzymes. In the meantime, paracetamol may find applications in other therapeutic areas, such as the prevention of atherosclerosis via a potential antioxidant activity. In summary, although it is more than a century since the first clinical use of paracetamol, it continues to be a first-line therapy of choice in adults and children with fever and pain. In addition, current research suggests that paracetamol may have a much broader clinical utility in years to come.

Acetaminophen↗

PubMed1981

Comparative pharmacokinetics of aspirin and acetaminophen.

Aspirin is extensively hydrolyzed to salicylic acid during absorption after oral administration. This hydrolysis is completed systemically. Salicylic acid, an effective analgesic, antipyretic, and anti-inflammatory agent, is eliminated by renal excretion and by metabolic conversion to conjugates with glycine and glucuronic acid, respectively, and to gentisic acid. Two of these metabolic processes are easily saturable, causing systemic clearance of salicylate to decrease with increasing dose. Acetaminophen metabolism during absorption is minor, and the drug is eliminated primarily by conjugation with glucuronic acid and with sulfate to pharmacologically inactive products. These processes become saturated only in the supertherapeutic dose range, thereby causing an increase in the fraction in the dose converted to a minor but potentially hepatotoxic metabolite. In the usual therapeutic dose range, acetaminophen is much more rapidly eliminated from the body than is salicylic acid.

Acetaminophen↗

PubMed1997

Prescribing patterns at primary health care level in the Asir region, Saudi Arabia: an epidemiologic study.

Out of 208 primary health care centres (PHCCs) in the Asir region, southwestern Saudi Arabia, a stratified random sample of 23 PHCCs was randomly chosen. Data regarding all the medical consultations (66,438) provided by all PHCCs physicians (49) and their prescriptions were collected to study prescribing patterns. The data were collected from the health information system of the PHCCs without the physicians' knowledge. The study showed that more than two-thirds of medical consultations (71.5%, 47,494) ended by prescribing medications. The average number of drug items prescribed for the individual patient was 1.44. The leading missing items in the studied prescriptions were, for how long should medication be taken (32.9%), the patient's name (15.8%) and the family health record number (6.5%). Prescribing drugs by generic name is very minimal among physicians (2.9%). The groups of drugs commonly prescribed were analgesics-antipyretics (61.9%), antibiotics (56.2%), cough medications (26.6%) and vitamins (22.7%). The observed defects identify fields to be addressed in continuing medical education programmes aimed at encouraging more rational prescribing among PHC physicians.

Journal Article↗

PubMed1987

Description, mechanisms and control of reactions to treatment in the human filariases.

Since diethylcarbamazine at the dosages used to treat filarial infections has little direct toxicity, most of the post-treatment reactions (termed Mazzotti reactions in onchocerciasis) result from the immunological inflammatory mechanisms activated in the process of clearing and killing the skin-swelling or blood-borne microfilariae. These reactions may be either localized to the skin, eyes or lymphatics or generalized systemically (e.g. headache, fever, adenopathy, arthralgia, tachypnoea, tachycardia, hypotension and even death). The occurrence and intensity of such reactions can be shown to be related to the intensity of infection. It had previously been speculated that the best candidates for triggering these post-treatment reactions were activation of complement, immediate hypersensitivity responses mediated by immunoglobulin E, and degranulation of eosinophils with resultant inflammatory reactivity. Recent detailed studies have given little support to the primacy of either complement or immediate hypersensitivity responses in triggering such reactions, but eosinophil degranulation with the release of inflammatory mediators into the tissues and peripheral blood is extremely prominent in all patients undergoing post-treatment reactions and develops with a time course generally consistent with what would be required of an initiator of such reactions. Other inflammatory mediators and pathways may be involved (e.g. kinins, prostaglandins, immune complexes, leukotrienes, platelets and parasite-derived inflammatory molecules), but there is currently no evidence to implicate any of these mechanisms as initiators of the response. Symptomatic treatment of these post-treatment reactions with analgesics, antipyretics, antihypotensive agents etc. has been successful, but their prevention has been achieved only with the broadly anti-inflammatory corticosteroids.

Animals↗

PubMed1985

Research on heterocyclic compounds. XVIII. Imidazo[2,1-b]-1,3,4-thiadiazole derivatives.

The synthesis of a series of 6-carbethoxy-, 6-carbethoxy-methyl-, and 5-carbethoxy-6-methylimidazo[2,1-b]-1,3,4-thiadiazoles was accomplished by reacting some 2-amino-1,3,4-thiadiazoles with ethyl bromopyruvate, 4-chloroacetoacetate, and 2-chloroacetoacetate, respectively; such carbethoxy derivatives afforded the corresponding carboxylic acids by hydrolysis. The antiinflammatory, analgesic, antipyretic and ulcerogenic activities were studied on three of the new acidic compounds.

Animals↗

PubMed2003

Pharmacological and toxicological properties of Nigella sativa.

The seeds of Nigella sativa Linn. (Ranunculaceae), commonly known as black seed or black cumin, are used in folk (herbal) medicine all over the world for the treatment and prevention of a number of diseases and conditions that include asthma, diarrhoea and dyslipidaemia. This article reviews the main reports of the pharmacological and toxicological properties of N. sativa and its constituents. The seeds contain both fixed and essential oils, proteins, alkaloids and saponin. Much of the biological activity of the seeds has been shown to be due to thymoquinone, the major component of the essential oil, but which is also present in the fi ed oil. The pharmacological actions of the crude extracts of the seeds (and some of its active constituents, e.g. volatile oil and thymoquinone) that have been reported include protection against nephrotoxicity and hepatotoxicity induced by either disease or chemicals. The seeds/oil have antiinflammatory, analgesic, antipyretic, antimicrobial and antineoplastic activity. The oil decreases blood pressure and increases respiration. Treatment of rats with the seed extract for up to 12 weeks has been reported to induce changes in the haemogram that include an increase in both the packed cell volume (PCV) and haemoglobin (Hb), and a decrease in plasma concentrations of cholesterol, triglycerides and glucose. The seeds are characterized by a very low degree of toxicity. Two cases of contact dermatitis in two individuals have been reported following topical use. Administration of either the seed extract or its oil has been shown not to induce significant adverse effects on liver or kidney functions. It would appear that the beneficial effects of the use of the seeds and thymoquinone might be related to their cytoprotective and antioxidant actions, and to their effect on some mediators of inflammation.

Animals↗

PubMed1975

[Controlled research of the influence of Neoston on tracking performance, heart rate, sinus arrhythmia and on subjective rating of healthy subjects].

The influence of Neoston--a relatively new analgesic, antipyretic, and anti-inflammatory agent--on performance in different tracking tests, on heart rate, on sinus arrhythmia and on subjective rating was objectivated. 15 healthy male and female subjects, aged from 19 to 27 years, took part in the sessions lasting about 2 1/2 hrs each. Two times two pills Neoston or a placebo were taken orally 2 and 5 hrs before the tests, making a total of 2 g. Performance in tracking was poorer on the whole with Neoston than with placebo, but only up to a maximum of 5%. Except one measurement point out of 10 all differences between the tests with the active drug and placebo were not statistically significant at the level of 5%. Yet a relatively uniform trend suggests a certain but only a small damping effect of Neoston. When relating the data of the second and third session on the data of the first session of each day, damping effects could be made more obvious. Hereby the influence of Neoston on tracking performance could be demonstrated to exist also statistically significant but to be practically almost irrelevant. In physiological variables as well as in subjective rating only small differences between the drug and placebo condition were measured. When relating the results to comparable research on the effects of alcohol, tranquilizers and stimulants, it is concluded that with Neoston in the relatively high dosage as used here, no real detrimental effects on traffic safety are to be expected.

Adult↗

PubMed1983

Effect of oxametacin on endogenous uric acid clearance rate in healthy volunteers.

Oxametacin, a new non steroidal anti-inflammatory compound, with analgesic, antipyretic and anti-inflammatory properties comparable to those of indomethacin, has been claimed to be effective in treatment of acute attacks of gout. The present study comprises an investigation in 8 healthy volunteers of the effect on the endogenous uric acid clearance rate, of oxametacin administered alone or in combination with the conventional hypouricaemic agents benzbromarone or allopurinol. Whether given alone or in combination with these drugs, oxametacin failed to alter the clearance rate of endogenous uric acid. In view of its good tolerance and its possible efficacy in treatment of acute attacks of gout, the present data help to validate use of oxametacin in acute gout.

Adult↗

PubMed1983

Close correlation of acetaminophen clearance with that of conjugated benzodiazepines but not oxidized benzodiazepines.

The clearance of the antipyretic-analgesic drug acetaminophen, biotransformed in humans by glucuronide and sulfate conjugation, was evaluated in 32 healthy young and elderly volunteers. Subjects received a single 650-mg dose of acetaminophen, and multiple plasma concentrations measured over the next 12 h. Random subgroups of subjects also participated in studies of the oxidized benzodiazepines diazepam, desmethyldiazepam and alprazolam, and of the conjugated benzodiazepines lorazepam, oxazepam and temazepam. Acetaminophen clearance was not related to that of the oxidized benzodiazepines, but was highly correlated with clearance of lorazepam (r = 0.70, n = 11, p less than 0.02), oxazepam (r = 0.76, n = 14, p less than 0.005) and temazepam (r = 0.63, n = 16, p less than 0.01). Thus acetaminophen may serve as a probe or marker compound to evaluate drug conjugating capacity in humans.

Acetaminophen↗

PubMed1998

The early clinical history of salicylates in rheumatology and pain.

The first clinical reports on the treatment of fever and pain with salicylate-containing natural willow bark remedies were made by the English clergyman Edward Stone in 1763. The pharmacologically active principles were isolated from natural sources by Italian, German and French scientists between 1826 and 1829. Salicylic acid was first synthesised by the German Gerland in 1852 and a year later the Frenchman Gerhardt synthesised acetylsalicylic acid. The first reports on the clinical use of salicylic acid in rheumatic disorders were made independently by the two German physicians Stricher and Reiss in 1876. Acetylsalicylic acid was rediscovered by Hoffmann in 1897 and by the turn of the century it had gained worldwide recognition in the treatment of pain and rheumatological disorders. Reports on adverse events relating to gastrointestinal intolerance and bleeding appeared early, but were largely neglected until the 1950s. Today, salicylates are still widely used as analgesic, antipyretic and anti-inflammatory drugs. New indications, such as thrombosis prophylaxis, have emerged during the last decades, and yet others are being explored.

Europe↗

PubMed1983

Non-acidic pyrazoles: inhibition of prostaglandin production, carrageenan oedema and yeast fever.

Prostaglandin production from mouse peritoneal macrophages was elicited by the tumour promoter 12-O-tetradecanoyl-phorbol-13-acetate (TPA). The inhibitory potency (IC50) of metamizole and its major metabolites as well as other non-acidic pyrazoles was defined in this system. A reliable IC50-value could not be assigned to metamizole. Isopropylaminophenazone was as active as acetylsalicylic acid while aminophenazone and methylaminophenazone, the major metabolites of metamizole, were about 10 times and phenazone 100 times less potent than acetylsalicylic acid. The major excretion products of metamizole, 4-formyl- and 4-acetyl-aminophenazone were inactive. The IC50-values obtained agree with those necessary for manifestation of anti-inflammatory effects in rats but are up to 10 times higher than those measurable in human plasma after administration of analgesic-antipyretic doses.

Animals↗