Generic
Pizotifen
27 brands available in the market
At a glance
Pizotifen is a serotonin antagonist used for prophylactic treatment of vascular headache of migraine type, including classical migraine, common migraine, and cluster headache. It is not effective in relieving migraine attacks once in progress.
Description
Pizotifen is a tricyclic compound that competitively antagonizes serotonin receptors. It possesses antihistamine, antibradykinin, and weak anticholinergic properties. It works by inhibiting peripheral actions of serotonin and histamine in increasing cranial vessel membrane permeability and transudation of plasmakinin, while altering pain thresholds in migraines.
Indications
- Classical migraine
- Common migraine
- Cluster headache (prophylaxis)
Therapeutic class
Anti-histamine Preparations, Other drugs for migraine
Pharmacological class
Serotonin Antagonist (Antihistamine)
Pharmacology
Pizotifen inhibits peripheral actions of serotonin and histamine, reducing cranial vessel membrane permeability and plasmakinin transudation, and alters pain thresholds in migraines. It blocks 5-HT receptors, attenuating serotonin-induced cranial vasoconstriction and serotonin-enhanced platelet function and aggregation. It also inhibits peripheral actions of bradykinin.
Mechanism of action
Prevents migraine by blocking 5-HT (serotonin) receptors and reducing platelet function.
Dosage
Adult Dose (Oral):
- Initial: 0.5 mg; gradually increase as needed
- Maintenance: 1.5 mg daily (single night dose or in 3 divided doses)
- Max: 4.5 mg daily (max 3 mg/dose)
- Hepatic impairment: Dose adjustment may be needed
Pediatric Dose (>2 years):
- Initial: 0.5 mg
- May increase gradually up to 1.5 mg daily in divided doses (max 1 mg/dose)
Administration
- May be taken with or without food; preferably at night
- Take at the same time each day
- Swallow tablet whole; do not chew, crush or break
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Drowsiness
- Dry mouth
- Increased appetite
- Weight gain
- Dizziness
- Nausea
Precautions & warnings
- May decrease alertness; do not drive if drowsy or dizzy
- May cause sleepiness initially; do not drive until you know how it affects you
- May cause weight gain; eat a balanced diet, avoid high-calorie snacking, exercise regularly
- Inform doctor if skin rash, muscle aches, tremors, difficulty moving
- Avoid alcohol (increased sedation)
- Long-term use: monitor liver function and vision
Contraindications
- Hypersensitivity to pizotifen or any ingredient
- Premature infants or neonates
- Postural giddiness
Drug interactions
- CNS depressants (sedatives, hypnotics, antihistamines, alcohol): Enhanced sedative effects
- Other antimuscarinic drugs: Additive antimuscarinic action
- Ototoxic drugs (aminoglycosides): May mask warning signs of damage
Food interactions
Caution is advised when consuming alcohol with Pizotifen.
Use in pregnancy
Use in Pregnancy: Limited information; no ill effects reported; use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Safety not established; avoid in nursing mothers.
Pediatric use
Safety not established in children under 2 years.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store in a dry place, away from light and heat; keep out of reach of children.
Chemical structure
Pizotifen