Arquel - General Information
A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.
Pharmacology of Arquel
Arquel is a nonsteroidal agent which has demonstrated anti-inflammatory, analgesic, and antipyretic activity in laboratory animals.
Arquel for patients
Patients should be advised that nausea, vomiting, diarrhea, and abdominal pain have been associated with the use of meclofenamate sodium. The patient should be made aware of a possible drug connection and accordingly should consider discontinuing the drug and contacting his or her physician if any of these conditions are severe.
Women who are taking meclofenamate sodium for heavy menstrual flow should be advised to consult their doctor if they have spotting or bleeding between cycles or worsening of their menstrual blood flow. These symptoms may be signs of the development of a more serious condition that is not appropriately treated with meclofenamate sodium.
Meclofenamate sodium may be taken with meals or milk to control gastrointestinal complaints. Concomitant administration of an antacid (specifically, aluminum and magnesium hydroxides) does not interfere with the absorption of the drug.
Meclofenamate sodium, like other drugs of its class, is not free of side effects. The side effects of these drugs can cause discomfort, and rarely, there are more serious side effects, such as gastrointestinal bleeding, which may result in hospitalization and even fatal outcomes.
NSAIDs (nonsteroidal anti-inflammatory drugs) are often essential agents in the management of arthritis and have a major role in the treatment of pain, but they also may be commonly employed for conditions which are less serious.
Physicians may w.s. to discuss with their patients the potential risks and likely benefits of NSAID treatment, particularly when the drugs are used for less serious conditions where treatment without N. A.D. may represent an acceptable alternative to both the patient and physician.
Meclofenamate sodium enhances the effect of warfarin. Therefore, when meclofenamate sodium is given to a patient receiving warfarin, the dosage of warfarin should be reduced to prevent excessive prolongation of the prothrombin time.
Concurrent administration of aspirin may lower meclofenamate sodium plasma levels, possibly by competing for protein-binding sites. The urinary excretion of meclofenamate sodium is unaffected by aspirin, indicating no change in meclofenamate sodium absorption. Meclofenamate sodium does not affect serum salicylate levels. Greater fecal blood loss results from concomitant administration of both drugs than from either drug alone.
The concurrent administration of propoxyphene hydrochloride does not affect the bioavailability of meclofenamate sodium.
Concomitant administration of aluminum and magnesium hydroxides does not interfere with absorption of meclofenamate sodium.
Meclofenamate sodium should not be used in patients who have previously exhibited hypersensitivity to it.
Cross-sensitivity to aspirin or other nonsteroidal anti-inflammatory drugs: meclofenamate sodium should not be given to patients in whom these drugs induce symptoms of bronchospasm, allergic rhinitis, or urticaria.
Additional information about Arquel
Arquel Indication: For the relief of mild to moderate pain, for the treatment of primary dysmenorrhea and for the treatment of idiopathic heavy menstrual blood loss. Also for relief of the signs and symptoms of acute and chronic rheumatoid arthritis and osteoarthritis.
Mechanism Of Action: The mode of action, like that of other nonsteroidal anti-inflammatory agents, is not known. Therapeutic action does not result from pituitary-adrenal stimulation. In animal studies, meclofenamic acid was found to inhibit prostaglandin synthesis and to compete for binding at the prostaglandin receptor site. In vitro meclofenamic acid was found to be an inhibitor of human leukocyte 5-lipoxygenase activity. These properties may be responsible for the anti-inflammatory action of meclofenamic acid. There is no evidence that meclofenamic acid alters the course of the underlying disease.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Meclofenamic acid
Synonyms: Acidum meclofenamicum [INN-Latin]; Acido meclofenamico [INN-Spanish]; Acide meclofenamique [INN-French]; Meclophenamic acid; Meclomen (free acid); Meclofenamate
Drug Category: Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Meclofenamic acid: Arquel;
Absorption: Rapidly absorbed in man following single and multiple oral doses with peak plasma concentrations occurring in 0.5 to 2 hours. The concomitant administration of antacids (aluminum and magnesium hydroxides) does not interfere with absorption of meclofenamic acid. Unlike most NSAIDs, which when administered with food have a decrease in rate but not in extent of absorption, meclofenamic acid is decreased in both. It has been reported that following the administration of meclofenamic acid capsules one-half hour after a meal, the average extent of bioavailability decreased by 26%, the average peak concentration (Cmax) decreased fourfold and the time to Cmax was delayed by 3 hours.
Toxicity (Overdose): After a massive overdose, CNS stimulation may be manifested by irrational behavior, marked agitation and generalized seizures. Following this phase, renal toxicity (falling urine output, rising creatinine, abnormal urinary cellular elements) may be noted with possible oliguria or anuria and azotemia. A 24 year-old male was anuric for approximately one week after ingesting an overdose of 6 to 7 grams of meclofenamate sodium. Spontaneous diuresis and recovery subsequently occurred.
Protein Binding: Greater than 99% bound to plasma proteins over a wide drug concentration range.
Biotransformation: Hepatic. Meclofenamic acid is extensively metabolized to an active metabolite (Metabolite I; 3-hydroxymethyl metabolite of meclofenamic acid) and at least six other less well characterized minor metabolites. Only Metabolite I has been shown in vitro to inhibit cyclooxygenase activity with approximately one fifth the activity of meclofenamic acid.
Half Life: In a study in 10 healthy subjects following a single oral dose the apparent elimination half-life ranged from 0.8 to 5.3 hours. Metabolite I (3-hydroxymethyl metabolite of meclofenamic acid) has a mean half-life of approximately 15 hours.
Dosage Forms of Arquel: Capsule Oral
Chemical IUPAC Name: 2-[(2,6-dichloro-3-methylphenyl)amino]benzoic acid
Chemical Formula: C14H11Cl2NO2
Meclofenamic acid on Wikipedia: http://en.wikipedia.org/wiki/Meclofenamic_acid
Organisms Affected: Humans and other mammals