Tolfenamic acid

Indications

Tolfenamic acid is used-
  • Specifically for relieving the pain of migraine headache and
  • Recommended for use as an analgesic in post-operative pain and fever.

Pharmacology

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.

Dosage & Administration

Adult:
  • Acute migraine attacks: 200 mg when symptoms appear may be repeated once after 1-2 hour.
  • Mild to moderate pain: 100-200 mg tid
  • Renal impairment: Dose adjustments may be needed.
  • Severe renal impairment: Avoid.
Children: A pediatric dosage regimen has not yet been established.

Tolfenamic acid should be taken with food. Take water during or immediately after meals.
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Interaction

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

Contraindications

Active gastro-intestinal bleeding, active gastro-intestinal ulceration, history of gastro-intestinal bleeding related to previous NSAID therapy, history of gastro-intestinal haemorrhage, history of gastro-intestinal perforation related to previous NSAID therapy, history of recurrent gastro- intestinal ulceration, severe heart failure.

Side Effects

Side effects which include rare alveolitis, hepatic damage, pancreatitis, pulmonary eosinophilia, Stevens-johnson syndrome, angioedema, blood disorder, depression, diarrhea, dizziness, drowsiness, dysuria, euphoria, gastro-intestinal bleeding, gastro-intestinal discomfort, hallucination, insomnia, malaise, nausea, hearing disturbances, rash, visual disturbances , vertigo, raised blood pressure. Overdose: Symptoms include headache, nausea, vomiting, gastro-intestinal bleeding, drowsiness, dizziness, occasionally convulsion. In case of significant poisoning acute renal failure and liver damage are possible.

Pregnancy & Lactation

This medicine is not recommended for using during pregnancy unless considered essential by doctor Not to be given during the third trimester of pregnancy. NSAID's can appear in breast milk in very low concentrations NSAID's should, if possible, be avoided when breastfeeding.

Precautions & Warnings

Precaution should be needed for patients with asthma bronchospasm, bleeding disorders, cardiovascular diseases, peptic ulceration, hypertension, liver infection, cardiac or renal function impairment and elderly. Increase water intake or dose reduction to reduce dysuria.

Overdose Effects

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.

Therapeutic Class

Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs), Other drugs for migraine

Storage Conditions

Store in a cool and dry place, away from light Keep out of the reach of children.

Chemical Structure

Molecular Formula : C14H12ClNO2
Chemical Structure : Chemical Structure of Tolfenamic acid

Common Questions about Tolfenamic acid

What is Tolfenamic acid?

Tolfenamic acid 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.

What are the uses of Tolfenamic acid?

Tolfenamic acid is used for the treatment of acute migraine attacks and Mild to moderate pain.

Quick Tips

  • Tolfenamic acid should be taken with food or milk to avoid getting an upset stomach.
  • Tolfenamic acid can cause serious complications like stomach bleeding and kidney problems if taken for a long time.
  • Tolfenamic acid can raise your risk of blood clots, heart attack, or a stroke.
  • Inform your doctor if you are pregnant or planning to conceive or breastfeeding.
  • Inform your doctor if you have ever been diagnosed with kidney or liver problems.
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Available Brand Names