Indications
Zofen is indicated as prophylactic treatment for vascular headaches of the migraine type, such as classical migraine, common migraine, and cluster headaches. It is not effective in relieving migraine attacks once they are in progress.
Description
Zofen is a tricyclic compound that acts as a serotonin receptor antagonist. It possesses antihistamine, antibradykinin, and weak anticholinergic properties. Zofen also has appetite-stimulating properties.
Pharmacology
Pizotifen works by inhibiting the peripheral actions of serotonin and histamine, which increase the membrane permeability of cranial vessels and the transudation of plasmakinin, while altering pain thresholds in migraines. By blocking 5-HT receptors, pizotifen reduces serotonin-induced cranial vasoconstriction, serotonin-enhanced platelet function, and aggregation. There is evidence that it also inhibits the peripheral actions of bradykinin. Pizotifen may also inhibit serotonin reuptake by blood platelets, affecting the tonicity and reducing passive distension of extracranial arteries. The appetite-stimulating effects are likely due to the drug acting at the metabolic level, rather than directly stimulating the appetite center.
Dosage & Administration
- Adults: Usually 1.5 mg daily, either as a single dose at night or in three divided doses. The dosage can be adjusted based on the patient’s needs, with a maximum of 4.5 mg daily. A dose of up to 3 mg may be taken as a single dose.
- Children (aged over 2 years): Up to 1.5 mg daily, usually in divided doses, although up to 1 mg has been given as a single dose at night.
Interaction
Zofen may enhance the central effects of sedatives, hypnotics, antihistamines (including certain common cold preparations), and alcohol. Zofen also antagonizes the hypotensive effect of adrenergic neurone blockers.
Contraindications
Pizotifen is contraindicated in patients who are hypersensitive to any of its ingredients.
Side Effects
The most common side effects include appetite stimulation, weight gain, and drowsiness.
Pregnancy & Lactation
Information regarding the use of Pizotifen during pregnancy is limited, although no ill effects have been reported. It should only be used during pregnancy if the potential benefit to the mother justifies the potential risk to the fetus. The safety of Pizotifen during lactation has not been established, so breastfeeding mothers should avoid taking it.
Precautions & Warnings
Considerations for urinary retention and renal impairment should be made. Drowsiness may affect the ability to drive or operate machinery. Zofen enhances the effects of alcohol.
Therapeutic Class
Anti-histamine preparations, other drugs for migraine.
Storage Conditions
Keep in a dry place, away from light and heat. Keep out of the reach of children.
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