Mefenamic acid pharmacokinetics absorption bioavailability. Mefanamic acid has been linked to rare instances of clinically apparent, acute liver injury. Effect of magnesium hydroxide on the absorption of. Explain the meaning of the terms absorption, distribution, metabolism, and excretion. Aug 20, 2019 mefenamic acid oral capsule is a prescription drug used to treat mild to moderate pain and dysmenorrhea menstrual pain. Extract a quantity of the capsule contents or powdered tablets containing 0. Mefenamic acid is a nonsteroidal agent with antiinflammatory, analgesic and antipyretic action.
Xijing hospital,forth military medical university,shanxi xian 710032,china. No clinically meaningful effect of rifampin or mefenamic acid on the pharmacokinetics of dapagliflozin or on dapagliflozinmediated urinary glucose excretion was observed. Mefenamic acid undergoes metabolism by cyp2c9 to 3hydroxymethyl mefenamic acid, and further oxidation to a 3carboxymefenamic acid may occur 3. Modest changes in dapagliflozin exposure were seen with rifampin and mefenamic acid with minor changes in uge, none of which were considered clinically meaningful. Mefenamic acid is a white to greyishwhite, odorless, microcrystalline powder with a melting point of 230231c and water solubility of. Oct 15, 2012 rifampin reduced total exposure area under the concentration. Ketoprofen is a potent cox inhibitor without any selectivity. A novel highperformance liquid chromatographic method. Mefenamic acid standard solutionpipet a 20ml aliquot of standard stock solution into a 1 l volumetric flask. To assess the effect of multiple dose mefenamic acid on the pharmacokinetics pk of sotagliflozin and its metabolite in healthy male and female subjects.
Comparison of effects of ginger, mefenamic acid, and. The findings of the present study revealed that the pharmacokinetics of ertu may be altered by concurrent administration of mef and ket in rats. Learn about side effects, warnings, dosage, and more. The drug is almost insoluble in water, slightly soluble in ethanol 96 per cent and in methylene chloride. This study aims to establish an high performance liquid chromatography method to monitor the concentration of mefenamic acid in human serum samples, to clarify its pharmacokinetics profiles such as absorption, disposition. A paired ttest for normal and alloxan treated rabbits revealed a significant decrease in all the bioavailability and disposition kinetic parameters of mefenamic acid. Serious gastrointestinal bleeding, ulceration, and perforation. Principles of pharmacokinetics learning objectives. The newly developed method was successfully applied to investigate the pharmacokinetic interactions of ertu with mefenamic acid mef and ketoconazole ket. Although classed as a nonsteroidal antiinflammatory drug, its antiinflammatory properties are considered to be minor. Tranexamic acid is rapidly absorbed from the gastrointestinal tract.
It is a white or almost white, microcrystalline powder. Capitals indicate lifethreatening, underlines indicate most frequent. To investigate the mechanism of action of tranexamic acid txa in bleeding trauma patients, we examined the timing of its effect on mortality. They were given this dosage orally at 24 h intervals. The absorption, distribution, and excretion of drugs objectives after studying this chapter, the reader should be able to. When given at the end of anesthesia tolfenamic acid at 4 mgkg produces analgesia comparable to ketoprofen, carprofen, and meloxicam in the cat. As hepatic metabolism is a significant pathway of mefenamic acid elimination, patients with acute and chronic hepatic disease may require reduced doses of mefenamic acid compared to patients with normal hepatic function see warnings. Interaction study to evaluate the effects of mefenamic. Add 40 ml of sodium lauryl sulfate stock solution, and dilute with water to volume. Use lowest possible effective dosage and shortest duration of therapy consistent with patients treatment goals 15,2439.
We investigated the metabolism of the nsaid mefenamic acid mfa to metabolites that transacylate gsh, leading to mfa s acylgsh thioester mfasg. It is not widely used in the united states due to its side effects and high cost compared to other nsaids 334. Mefenamic acid has been reported as being greater than 90% bound to albumin. The relevant pharmacokinetic parameters maximum plasma concentration cmax, time of peak. Mefenamic acid pharmacokinetics have not been studied in patients with hepatic dysfunction. Pdf the bioavailability and pharmacokinetics of mefenamic acid. Pharmacokinetics differences of tab mefenamic acid ma 5oomg one pill and 2 50mg two pill with and without food obaid alii, roohi obaidi, noor kamif, zafar saied saify2, and syed waseemuddin ahmed3 ministry of health, government of pakistan, karachi, pakistan department of pharmaceutical chemistry, faculty of pharmacy, university. It is not widely used in the united states due to its side effects and high cost compared to other nsaid. Mefenamic acid in plasma was assayed by high performance liquid chromatography. C u is the concentration, in g per ml, of mefenamic acid in the test solution. The fenamate compounds nifhimic acid, mefenamic acid, flufenamic acid, and 4,4diisothiocyanatostilbene2,2. Mefenamic acid ponstel is an oral drug used shortterm to treat pain, including menstrual cramps. According to the british pharmacopoeia 2002 2 and indian pharmacopoeia 6, mefenamic acid in capsule and tablet preparations are identified by examination using infrared absorption spectrophotometry as the following procedure.
May 25, 2016 prostaglandins are mediators of inflammation. We investigated the metabolism of the nsaid mefenamic acid mfa to metabolites that transacylate gsh, leading to mfa s acylgsh thioester mfasg formation in incubations with rat and. Etamsylate drug information, uses, adverse effects. Pdf effect of dehydration on the pharmacokinetics of.
Pdf the bioavailability and pharmacokinetics of mefenamic. List two physiologic factors that can alter each of the processes of absorption, distribution, and excretion. Modest changes in dapagliflozin exposure were seen with rifampin and mefenamic acid with minor changes in uge, none of which were considered clinically. Uses and administration mefenamic acid, an anthranilic acid derivative, is an nsaid p. Enhancement of dissolution and absorption of mefenamic. The pharmacokinetic properties and bioavailability of mefenamic acid was studied in normal and dehydrated rabbits. Synthesis, biological evaluation and pharmacokinetic studies.
Page 2 of 16 pharmacokinetics absorption mefenamic acid is rapidly absorbed after oral administration. Each bluebanded, ivory capsule contains 250 mg of mefenamic acid for. Overview primary characterstics indications pharmacokinetics contraindications drug interactions side effects dosage high risk groups warning precautions storage conditions interference in pathology brands of mefenamic acid manufacturers of mefenamic acid. Methods mefenamic acid dispersible tablets and mefenamic acid tablets were given to 18 health volunteers in an open randomized two period crossover test single oral dose500 mg. We hypothesised that if txa reduces mortality by decreasing blood loss, its effect should be greatest on the day of the injury when bleeding is most profuse. Following a single 1gram oral dose, mean peak plasma levels ranging from 10. Objective to study the pharmacokinetics and bioequivalence of mefenamic acid dispersible tablets and mefenamic acid tablets. Mefenamic acid is rapidly absorbed after oral administration. Estimation and analysis of mefenamic acid suspension. To assess total 24 hour urinary glucose excretion uge after 400 mg sotagliflozin alone and in combination with mefenamic acid in healthy male and female subjects. The pharmacokinetics of mefenamic acid ma, 2 mgkg, were studied in 17 preterm infants with symptomatic patent ductus arteriosus.
Tranexamic acid indications, pharmacology, dosage, side. Consider potential benefits and risks of mefenamic acid therapy as well as alternative therapies before initiating therapy with the drug. Asif husain, department of pharmaceutical chemistry, faculty of pharmacy, hamdard university, new delhi110062, india. In a patient with decreased acid sec retion leading to a higher than normal gastric ph, weakly basic drugs can have lower bioavailability due to poor dissolution rates. High perfomance liquid chromatography hplc was used for the assay of mefenamic acid in plasma samples. In vitroin vivo correlation of fast release mephenamic acid. Many different brands and dosage forms of mefenamic acid are available in the omani market that places health practitioners in a dilemma of drug substitution in case of non availability of a particular. No clinically meaningful effect of rifampin or mefenamic acid on the pharmacokinetics of dapagliflozin or on dapagliflozin. Each bluebanded, ivory capsule contains 250 mg of mefenamic acid for oral administration. The safety and scientific validity of this study is the responsibility of the study sponsor and investigators.
Halflife 5 times longer in preterm infants compared with adults. In patients with renal or hepatic impairment, clearance of metabolites may be decreased. Mefenamic acid 500 mg and asa 650 mg four times a day both caused significant further lowering of the prothrombin concentration mefenamic acid 3. Tolfenamic acid is a cox1selective nsaid that should not be used preoperatively. To compare the effects of ginger, mefenamic acid, and ibuprofen on pain in women with primary dysmenorrhea. Feb 14, 2017 trace amounts of ponstel mefenamic acid may be present in breast milk and transmitted to the nursing infant.
Mefenamic acid has been reported as being greater than 90% bound to. Pharmacokinetics and bioequivalence study of mefenamic acid dispersible tablets in health volunteers wu yin1,wen aidong1,luo xiaoxing2,xie li1,yang zhifu1,chen pingjun1,li wei1,zhao lei11. Mefenamic acid oral capsule is a prescription drug used to treat mild to moderate pain and dysmenorrhea menstrual pain. Synthesis, biological evaluation and pharmacokinetic studies of mefenamic acid nhydroxymethylsuccinimide ester prodrug as safer nsaid authors. Bioequivalent study provides a biologic standard for the drug formulation and direct proof for the clinic effect ion. Pharmacokinetics of mefenamic acid in preterm infants with patent ductus arteriosus. Synthesis, biological evaluation and pharmacokinetic. After oral administration, about 40% of the dose is excreted in the urine during the first 24 hours. Mefenamic acid, an anthranilic acid derivative, is a nonsteroidal antiinflammatory drug used to treat pain of different etiology. Effect of dehydration on the pharmacokinetics of mefenamic acid article pdf available in turkish journal of medical sciences 292. A paired ttest for normal and alloxan treated rabbits revealed a significant. It dissolves in dilute solutions of alkali hydroxides.
Menorrhagia and its management the pharmaceutical journal. Ponstel mefenamic acid is a member of the fenamate group of nonsteroidal antiinflammatory drugs nsaids. Effect of dehydration on the pharmacokinetics of mefenamic acid. The bioavailability and pharmacokinetics of mefenamic acid was studied in alloxandiabetic rabbits.
This study aims to establish an high performance liquid chromatography method to monitor the concentration of mefenamic acid in human serum samples, to clarify its pharmacokinetics profiles such as absorption, disposition, metabolism and elimination in health body, and evaluate the bioequivalence of mefenamic acid dispersible tablets and conventional tablets to provide. Oct 11, 2018 mefenamic acid pharmacokinetics have not been studied in patients with hepatic dysfunction. Pharmacokinetics and bioequivalence study of mefenamic acid. Parameterparameter biokeperolehan dan farmakokinetik asid mefenamik telah dikaji dan dibandingkan antara amab normal dengan amab febril. The normal dose is 500mg three times a day, starting on the. Describe the physicochemical and physiological factors that influence the absorption of drugs from enteral and parenteral routes of administration, their distribution within the body, and their routes and mechanisms of elimination. This was a doubleblind comparative clinical trial conducted from september 2006 to february 2007. The bioavailability and pharmacokinetics of mefenamic acid. The effect of various antacids on the absorption of tolfenamic and mefenamic acids has been investigated in three separate crossover studies, each consisting of four phases. Ponstel mefenamic acid is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft surgery see warnings. Mefenamic acid dosing, indications, interactions, adverse. Interaction study to evaluate the effects of mefenamic acid on the pharmacokinetics and pharmacodynamics of sotagliflozin in healthy male and female subjects.
In one small, randomized trial, the prevalence of preterm labor was significantly reduced by mefenamic acid compared with placebo. Mefenamic acid is a nonsteroidal antiinflammatory drug nsaid used largely for acute treatment of pain. Nsaids cause an increased risk of serious gastrointestinal gi adverse events, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. However, if txa reduces mortality via an antiinflammatory mechanism its effect should be. Given that mefenamic acid, its metabolites and conjugates are primarily excreted by the kidneys, the potential exists for mefenamic acid metabolites to accumulate.
Mefenamic acid is contraindicated in the setting of coronary artery bypass graft cabg surgery. In two 500mg single oral dose studies, the mean extent of absorption was 30. View enhanced pdf access article on wiley online library html view download pdf for offline viewing. Given that mefenamic acid, its metabolites and conjugates are primarily excreted by the kidneys, thepotentialexistsformefenamic acidmetabolitestoaccumulate. Pharmacokinetics differences of tab mefenamic acid ma 5oomg. Mefenamic acid is an aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3dimethylphenyl group. Listing a study does not mean it has been evaluated by the u. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and.
There are no adequate reports or wellcontrolled studies of mefenamic acid in pregnant women. Mefenamic acid is one of the fenamate series of nonsteroidal antiinflammatory agents. Carboxylic acid containing nonsteroidal antiinflammatory drugs nsaids can be metabolized to chemically reactive acyl glucuronide andor s acylcoa thioester metabolites capable of transacylating gsh. Pdf the bioavailability and pharmacokinetics of mefenamic acid was studied in alloxandiabetic rabbits. Single doses of magnesium hydroxide 85 mg, 425 mg and 1700 mg or of water 150 ml were given by mouth to 6 healthy volunteers immediately after tolfenamic acid 400 mg study 1. Mefenamic acid pharmacokinetics have not been investigated in subjects with renal insufficiency. Ponstel mefenamic acid is contraindicated in patients with acute active ulceration or chronic inflammation of either the upper or lower gastrointestinal tract. International journal of current pharmaceutical research innovare. Mefenamic acid is a member of the anthranilic acid derivatives or fenamate class of nsaid drugs, and is used to treat mild to moderate pain, including menstrual pain, and is sometimes used to prevent migraines associated with menstruation.
In two 500 mg single oral dose studies, the mean extent of absorption was 30. It is not widely used in the united states due to its side effects and high cost compared to other nsaid drugs. Pharmacokinetics of mefenamic acid in preterm infants with. History of asthma, urticaria, or other sensitivity reaction precipitated by aspirin or other nsaias. Known hypersensitivity to mefenamic acid or any ingredient in the formulation. Effect of food on rate and extent of absorption not known. The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug. The bioavailability and pharmacokinetics of mefenamic acid in. Pharmacokinetic and bioequivalent study of mefenamic acid. Nov 30, 2014 mefenamic acid is a white to greyishwhite, odorless, microcrystalline powder with a melting point of 230 to 231c and water solubility of 0. Because mefenamic acid is an inhibitor of prostaglandin synthesis, its mode of action may be due to a decrease of prostaglandins in peripheral tissues. Voltagegated channels, 1999 positive regulation by stabilization of open isk channels by chloride channel blockers.
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