MODE OF ACTION OF TOLMETIN:
Tolmetin is an arylalkanoic acid and non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic activities. Although the exact mechanism through which tolmetin exerts its effects has yet to be fully elucidated, this agent appears to inhibit the enzyme prostaglandin synthase.
Drug Label Information | Brands:
BRANDS OF TOLMETIN IN KENYA:
No brands of Tolmetin is registered in Kenya
Tolmetin is indicated for the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis. Tolmetin is indicated in the treatment of acute flares and the long-term management of the chronic disease.
Tolmetin is also indicated for treatment of juvenile rheumatoid arthritis. The safety and effectiveness of tolmetin sodium capsules have not been established in pediatric patients under 2 years of age
Tolmetin is contraindicated in patients with known hypersensitivity to tolmetin sodium.
Tolmetin should not be given to patients who have experienced asthma, urticaria or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients
TOLMETIN ADVERSE DRUG REACTIONS:
Gastrointestinal: nausea , dyspepsia, gastrointestinal distress, abdominal pain, diarrhea, flatulence, vomiting, constipation, gastritis, and peptic ulcer.
Body as a Whole: headache, asthenia, chest pain
Cardiovascular: elevated blood pressure, edema
Central Nervous System: dizziness, drowsiness, depression
Metabolic/Nutritional: weight gain, weight loss
Dermatologic: skin irritation
Special Senses: tinnitus, visual disturbance
Hematologic: Small and transient decreases in hemoglobin and hematocrit not associated with gastrointestinal bleeding have occurred. These are similar to changes reported with other nonsteroidal anti-inflammatory drugs.
Urogenital: elevated BUN, urinary tract infection
TOLMETIN DRUG INTERACTINS:
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE Inhibitors. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE Inhibitors.
As with other NSAIDs, concomitant administration of tolmetin sodium and aspirin is not generally recommended because of the potential of increased adverse effects.
Clinical studies, as well as post-marketing observations have shown that NSAIDs can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with NSAIDs, the patient should be observed closely for signs of renal failure, as well as to assure diuretic efficacy.
NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.
NSAIDs have been reported to competitively inhibit methotrexate accumulation in rabbit kidney slices. This may indicate that they could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.
The in vitro binding of warfarin to human plasma proteins is unaffected by tolmetin, and tolmetin does not alter the prothrombin time of normal volunteers. However, increased prothrombin time and bleeding have been reported in patients on concomitant tolmetin and warfarin therapy. Therefore, caution should be exercised when administering tolmetin to patients on anticoagulants.
In adult diabetic patients under treatment with either sulfonylureas or insulin there is no change in the clinical effects of either tolmetin or the hypoglycemic agents.
Drug/Laboratory Test Interactions
The metabolites of tolmetin sodium in urine have been found to give positive tests for proteinuria using tests which rely on acid precipitation as their endpoint (e.g., sulfosalicylic acid). No interference is seen in the tests for proteinuria using dye-impregnated commercially available reagent strips (e.g., Albustix®, Uristix®, etc.).
In a controlled single-dose study, administration of tolmetin with milk had no effect on peak plasma tolmetin concentrations, but decreased total tolmetin bioavailability by 16%. When tolmetin was taken immediately after a meal, peak plasma tolmetin concentrations were reduced by 50% while total bioavailability was again decreased by 16%.
Tolmetin is contraindicated in the setting of coronary artery bypass graft (CABG) surgery
Routes of Administration:
Elimination Half life:
Routes of Administration:
Elimination Half life: