Tolfenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase inhibitor. It is used for the management of both acute and chronic pain in dogs and acute pain for cats. The pharmacologic effects of tolfenamic acid are similar to those of aspirin.
Anthranilic Acid Derivative; Anti-inflammatory
Tolfenamic acid (N-(2-methyl-3-chlorophenyl) anthranilic acid) belongs to the fenamate group and is a potent inhibitor of cyclooxygenase enzyme, thus it inhibits the synthesis of important inflammatory mediators such as thromboxane (TX) B2 and prostaglandin (PG) E2. Prostaglandins are responsible for causing swelling pain and inflammation associated with these conditions. It acts not only by inhibiting prostaglandin synthesis, but it also has direct antagonistic action on its receptors.
Pharmacokinetic properties: Absorption Readily absorbed from GI tract. Peak plasma concentration: 60-90 min. Bioavailability 85%. Distribution: Protein-binding: 99% Plasma half-life 2 hours. Metabolism: Metabolised in the liver. Tolfenamic acid undergoes enterohepatic circulation. Excretion: Excreted in urine (90%) and faces.
Acute migraine attacks: Adult: 200 mg when 1st symptoms appear may be repeated once after 1-2 hr. Renal impairment: Dose adjustments may be needed. Severe: Avoid. Mild to moderate pain: Children: A pediatric dosage regimen has not yet been established. Adult: 100-200 mg tid.
The rate of absorption of Tolfenamic acid increases with Metoclopramide and Magnesium hydroxide but decreases with Aluminium hydroxide. Risk of bleeding with anticoagulants and other NSAIDS increases when use with Tolfenamic acid. It decreases antihypertensive response to loop diuretics, B-blockers and ACE Inhibitors. Co-administration increases plasma concentration of Lithium Methotrexate and cardiac glycosides. It also increases the risk of nephrotoxicity with ACE inhibitors, Ciclosporin, Tacrolimus or diuretics
Hypersensitivity to aspinn or other NSAID. Active peptic ulceration. Severe renal or hepatic impairment. Pregnancy (3rd trimester). Asthma, bronchospasm, bleeding disorders, CV diseases, history of peptic ulceration, hypertension, patients w/ infections, liver, cardiac, or renal function impairment. Increase water intake or dose reduction to reduce dysuria. CHF; elderly; lactation.
Dysuria esp in males; diarrhoea, nausea, epigastric pain, vomiting, dyspepsia, erythema, headache. Tremor, euphoria, fatigue, pulmonary infiltration. Blood dyscrasias, toxic hepatitis.
Pregnancy: This medicine is not recommended for use during pregnancy unless considered essential by your doctor. This is particularly important in the first and third trimesters. Not to be given during the third trimester of pregnancy. Lactation: In limited studies so far available, NSAIDs can appear in breast milk in very low concentrations. NSAIDs should, if possible, be avoided when breastfeeding.
Symptoms include headache, nausea, vomiting, epigastric pain. gastrointestinal bleeding, diarrhoea excitation, coma, drowsiness dizziness, tinnitus, fainting and convulsions. In cases of significant poisoning, acute renal failure and liver damage are possible. Patients should be treated symptomatically as required.
Store in a cool and dry place, away from light Keep out of the reach of children.