Reumophan 40 tabs, Ketoprofen, chlorzoxazone
INDICATIONS: Muscle relaxant, analgesic and anti-inflammatory useful in patients with a history or gastrointestinal intolerance to NSAIDs (nonsteroidal anti-inflammatory drugs) such as: NSAID-induced gastritis, gastric ulcer, duodenal. Prophylaxis of acid peptic disease induced by NSAIDs and patients sensitive to them. Arthralgia and musculoskeletal pain. Rheumatoid arthritis and osteoarthritis. Painful vertebral syndromes, lumbago, lumbosciatic. Muscle spasms. Acute gout. Bursitis, tendinitis and tenosynovitis.
Description and therapeutic uses: REUMOPHAN ALKA * is the combination of ketoprofen, a nonsteroidal antiinflammatory drug (NSAID) with analgesic, chlorzoxazone having muscle relaxant effect and calcium carbonate which may attenuate or prevent gastrointestinal intolerance induced gastritis expressed as NSAIDs and peptic ulcer, gastric or duodenal ulcers in patients with chronic-degenerative diseases.
Pharmacokinetics in humans: The peak serum concentrations achieved ketoprofen 0.5 to 2 hours after oral administration. Ketoprofen is metabolized in the liver and 60 to 75% of the dose appears in the urine, mainly as the glucuronide metabolite and less than 10% is excreted as unchanged drug. The elimination half-life of ketoprofen is 2 to 4 hours.
Ketoprofen is an NSAID that has anti-inflammatory and analgesic properties. Inhibits prostaglandin synthesis, besides the factor inhibit leukocyte migration especially neutrophils and macrophages which are the constituents of the cellular factor of inflammation. It is excreted mainly in urine and in other ways completely after 24 hours.
Chlorzoxazone is rapidly absorbed from the gastrointestinal tract is metabolized to 6-hydroxychlorzoxazone. Is excreted in urine in 1.1 hours. It is a muscle relaxant and does not exert a direct effect on the muscles. Chlorzoxazone can act on the spinal cord and brain subcortical level to inhibit reflections associated with muscle spasm. Much of the therapeutic effect of chlorzoxazone is related to its sedative properties.
Chlorzoxazone attenuates muscle spasm internuciales acting on spinal neurons, induces muscle relaxation, decreased muscle tone, does not produce neuromuscular blockade hence its muscle relaxant effect is of central origin. Chlorzoxazone in man is able to decrease muscle tone abnormally exaggerated nervous disorders, rheumatic and contracturales.
It is absorbed orally easily excreted in urine in 6 hours and 24 hours totally. It is used as a muscle relaxant, to break the vicious cycle associated with anti-inflammatory, analgesic and antirheumatic.
At the recommended dose of calcium carbonate is 0.5 to 1.5 g. The bioavailability of commercially available calcium carbonate is reasonably good. The calcium carbonate antacids neutralize HCl secreted by the parietal cells. Empty stomach is removed from approximately 30 minutes to be administered.
Food prolonged neutralizing effect in approximately two hours. The alkalization of gastric contents increases gastric motility by action of gastrin although antacids absorption is variable.
Hypersensitivity to the components of the formula, rhinitis, urticaria, asthma or allergy to aspirin (aspirin) or other anti-inflammatory.
PRECAUTIONS: History of gastrointestinal ulceration, bleeding or perforation, renal failure, hypertension or heart disease aggravated by fluid retention and edema, history of coagulation defects.
RESTRICTIONS OF USE DURING PREGNANCY AND LACTATION: Not ketoprofen established safety during pregnancy and breast-feeding is therefore not recommended.
ADVERSE REACTIONS: Ketoprofen may cause dyspepsia and other gastrointestinal effects usually mild and diminish if taken with food, milk or antacids. May cause fluid retention and higher plasma creatinine which are transient and occur without any symptoms.
Chlorzoxazone is usually well tolerated, but may cause drowsiness, dizziness and overstimulation.
DRUG INTERACTIONS AND OTHER GENDER: Oral anticoagulants require close monitoring of coagulation parameters. The use of alendronate has been associated with gastrointestinal irritation, so that concomitant administration may increase this effect. NSAIDs may diminish the antihypertensive and natriuretic.
The concurrent use of aspirin and ketoprofen can produce reduced levels of serum ketoprofen, but the clinical relevance of this observation is indeterminate.
The concurrent use of NSAIDs can produce beta-adrenergic blocking the rise in blood pressure. This effect has been reported for flurbiprofen (400 mg daily), ibuprofen (more than 400 mg daily), indomethacin (more than 50 mg daily), naproxen (1,000 mg daily) and piroxicam.
By altering both gastric and urinary pH, antacids can do the same with the rate of dissolution, absorption, bioavailability and renal clearance of various drugs.
In general, it is prudent to avoid concomitant use. This effect can be avoided by administering antacids if taken two hours before or two hours after other drugs.
This decrease may have clinical significance in the case of iron, theophylline, antibiotics from the group of quinolones, tetracyclines, isoniazid and ketoconazole (dissolution reduces with increasing pH) antacids can also decrease the bioavailability of ethambutol, some antimuscarinic, benzodiazepines, phenothiazines, ranitidine, indomethacin, phenytoin, nitrofurantoin, vitamin A, prednisone, procainamide, propranolol and atenolol.
Antacids increase the bioavailability of metoprolol.
CHANGES IN RESULTS OF LABORATORY TESTS Ketoprofen may interfere with studies of albumin, bile salts and 17 ketosteroids.
PRECAUTIONS IN RELATION TO EFFECTS Carcinogenesis, Mutagenesis, Impairment of Fertility: The use of ketoprofen in humans has not been associated with carcinogenesis or teratogenic effects, but should be avoided in late pregnancy because of its effect of inhibiting prostaglandins in fetal circulatory system. It also has been linked to impaired fertility.
DOSAGE AND ADMINISTRATION: Oral. Two tablets every 8 hours, preferably after meal.
MANIFESTATIONS AND MANAGEMENT OF OVERDOSE OR ACCIDENTAL INGESTION: To reach toxic levels of ketoprofen is required to take a dose greater than 486 mg / kg corresponding to the LD50 in mice. In some individuals have reported nausea, abdominal pain and drowsiness. In case of overdose, it is recommended to induce vomiting and gastric lavage.
PRESENTATION: Box with 20 tablets in blister pack.
RECOMMENDED STORAGE: Store at room temperature not exceeding 30 ° C and dry.
Drug Name: Reumophan
Comparative Brand: Reumophan
Active substance: Ketoprofen / Chlorzoxazone
Concentration: 50mg / 250mg
time release tablets: No
Laboratory: Grisi Hermanos
Box with 40 tablets
Made in Mexico