Tolfenamic acid

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Tolfenamic acid is a non-steroidal anti-inflammatory drug (NSAID) used primarily for its analgesic, anti-inflammatory, and antipyretic properties. It is commonly prescribed for the treatment of migraines and other forms of headaches. Tolfenamic acid is part of the fenamate class of NSAIDs, which also includes drugs like mefenamic acid and flufenamic acid.

Pharmacology

Tolfenamic acid works by inhibiting the synthesis of prostaglandins, which are compounds involved in the mediation of inflammation, pain, and fever. It achieves this by blocking the enzyme cyclooxygenase (COX), specifically COX-1 and COX-2. This inhibition reduces the formation of prostaglandins, thereby alleviating symptoms associated with inflammation and pain.

Medical Uses

Tolfenamic acid is primarily used for the treatment of acute migraine attacks. It is also effective in managing other types of headaches and pain conditions, including dysmenorrhea (painful menstruation) and musculoskeletal pain.

Dosage and Administration

The typical dosage for adults is 200 mg at the onset of a migraine attack, followed by an additional 200 mg if needed. The maximum recommended dose is 400 mg per day. It is usually taken orally in the form of tablets.

Side Effects

Common side effects of tolfenamic acid include gastrointestinal issues such as nausea, vomiting, diarrhea, and abdominal pain. Less common but more serious side effects can include gastrointestinal bleeding, ulceration, and renal impairment. Patients are advised to use the drug under medical supervision, especially if they have a history of peptic ulcer disease or kidney disease.

Contraindications

Tolfenamic acid is contraindicated in individuals with known hypersensitivity to NSAIDs, active peptic ulcer disease, severe heart failure, and renal impairment. It should be used with caution in patients with a history of asthma or allergic reactions to other NSAIDs.

Interactions

Tolfenamic acid can interact with other medications, including anticoagulants, antihypertensives, and other NSAIDs. These interactions can increase the risk of adverse effects such as bleeding and renal impairment. Patients should inform their healthcare provider of all medications they are taking to avoid potential interactions.

Mechanism of Action

The primary mechanism of action of tolfenamic acid is the inhibition of the cyclooxygenase (COX) enzymes, which are crucial for the conversion of arachidonic acid to prostaglandins. By inhibiting COX-1 and COX-2, tolfenamic acid reduces the production of prostaglandins, leading to decreased inflammation, pain, and fever.

History

Tolfenamic acid was first introduced in the 1970s and has since been used in various countries for the treatment of migraines and other pain conditions. It is available under several brand names and formulations.

See Also

• Non-steroidal anti-inflammatory drug
• Migraine
• Analgesic
• Prostaglandin
• Cyclooxygenase