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Tolfenamic Acid; Uses, Dosage, Side Effects, Interactions

Tolfenamic acid (TA) is one of the class of non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat the symptoms of a migraine. Tolfenamic acid, with the formula N-(2-methyl-3-chlorophenyl)-anthranilic acid, is a nonsteroidal anti-inflammatory agent. It was discovered by scientists at Medica Pharmaceutical Company in Finland. It is used in the UK as a treatment for a migraine under the name of Clotam. In the US, it presents a Status class I by the FDA. By the European Medicine Agency, it was granted in 2016 with the status of an orphan for the treatment of supranuclear palsy.

Tolfenamic acid is approved in Canada and Europe in an oral and parenteral formulation for dogs and cats. In vitro data support COX-1–sparing (COX-2–selective) activity. By studying its NSAID properties more closely, it was noted a dose-related inhibition of serum thromboxane which indicated the inhibition of COX-1. In the same line, there was noted a inhibition of prostaglandin E2 synthesis which marks a related COX-2 inhibition. The maximal inhibition of thromboxane was greater than 80% as well as is proven to be a potent prostaglandin E inhibitor.

Mechanism of Action of Tolfenamic Acid

Tolfenamic acid inhibits the biosynthesis of prostaglandins, and it also presents inhibitory actions on the prostaglandin receptors. As commonly thought, the mechanism of action of tolfenamic acid is based on the major mechanism of NSAIDs which consists of the inhibition of COX-1 and COX-2 pathways to inhibit prostaglandin secretion and action and thus, to exert its anti-inflammatory and pain-blocking action. Nonetheless, some report currently indicates that tolfenamic acid inhibits leukotriene B4 chemotaxis of human polymorphonuclear leukocytes leading to an inhibition of even 25% of the chemotactic response. This activity is a not ligand specific additional anti-inflammatory mechanism of tolfenamic acid.

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Indications of Tolfenamic Acid

headaches and migraines
a toothache
period pains
general aches and pains
In the information for tolfenamic acid, it is stated that this drug, being an NSAID, is effective in treating the pain associated with the acute attack of migraines in adults
In the information for tolfenamic acid, it is stated that this drug, being an NSAID, is effective in treating the pain associated with the acute attack of migraines in adults.
Treatment of progressive supranuclear palsy
Treatment of behavioral variant frontotemporal dementia

Contra-Indications of Tolfenamic Acid

Active peptic ulcer, aspirin/anti-inflammatory induced allergy, hepatic or renal impairment. Pregnancy (3^rd trimester).
Hypersensitivity to aspirin or other NSAID. Active or history of GI bleeding or ulceration, severe heart failure, history of GI bleeding or perforation related to previous NSAID therapy. Severe renal and hepatic impairment. Pregnancy (3rd trimester).

The Dosage of Tolfenamic Acid

Strengths: 100mg ;200 mg

Acute migraine attacks

200 mg when 1st symptoms appear, may be repeated after 1-2 hr, if necessary.

Mild to moderate pain

100-200 mg tid.

Side Effects of Tolfenamic Acid

The most common

Constipation
dizziness
drowsiness
dry mouth
chest pain
a headache
joint painPain
dizziness
nausea and vomiting
Severe stomach ache
epigastric pain,
diarrhea,
anorexia,
flatulence,
a headache,
fainting, fast or pounding heartbeats.

More common

Seizures
Syndrome of inappropriate secretion of antidiuretic hormone
Fast or irregular heartbeat
fever
Back pain
dizziness
headache
increased cough
Acid or sour stomach
decreased appetite
Agitation
chest congestion
chest pain
cold sweats
confusion
decreased sexual ability or desire
diarrhea or loose stools
heartburn
sleepiness or unusual drowsiness
stomach or abdominal cramps, gas, or pain
trouble sleeping

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Less common

Abnormal dreams
change in sense of taste
congestion
discouragement, feeling sad, or empty
Suicide attempts
Acting on dangerous impulses
Aggressive or violent behavior
Thoughts about suicide or dying
New or worse depression
New or worse anxiety or panic attacks
Agitation, restlessness, anger, or irritability
Trouble sleeping
An increase in activity or talking more than normal

Drug Interactions of Tolfenamic Acid

The tolfenamic acid may interact with following drugs, supplements & may decrease the efficacy of the drug

angiotensin converting enzyme (ACE) inhibitors (e.g., ramipril)
beta-adrenergic blockers (e.g., metoprolol, atenolol)
corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
cyclosporine
diuretics (water pills; e.g., spironolactone, triamterene)
heparin
methotrexate
“gliptin” diabetes medications (e.g.,metformin linagliptin, saxagliptin, sitagliptin)
other NSAIDs (e.g., celecoxib, ibuprofen, ketorolac, naproxen)
phenytoin
potassium supplements
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
warfarin

Pregnancy & lactation of Tolfenamic Acid

FDA Pregnancy Category C

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. The use of mefenamic acid during the last 3 months of pregnancy may result in harm to the baby or longer labour for the mother. Mefenamic acid should not be used during this time.

Lactation

This medication passes into breast milk. If you are a breast-feeding mother and are taking mefenamic acid, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.