Pizotifen

Pizotifen

Pizotifen is a tricyclic compound having antiserotoninergic and antihistaminergic effects together with a weak anticholinergic action, but a little or no activity on kinins or their liberators. At low concentration Pizotifen may potentiate the actions of serotonin.

Mechanism of action

Pizotifen, like all triptans, is a serotonin agonist, which means it acts like serotonin. Serotonin, also known as 5-hydroxytriptamine (5-HT), is a neurotransmitter that regulates communication between nerve cells and the widening of blood vessels. It acts by activating proteins on nerve endings and blood vessels, called 5-HT receptors. Pizotifen also activates these receptors. Activation prevents the release of chemicals that mediate pain and narrows blood vessels, which reduces their leakiness.

Pharmacology

Pizotifen is characterized by its polyvalent inhibition effect on biogenic amines, such as serotonin, histamine and tryptamine. Pizotifen also possesses appetite stimulation properties.

Indication

Pizotifen is indicated for the prophylactic treatment of vascular headaches of migraine types such classical migraine, common migraine, and cluster headaches. It is also indicated in appetite loss of somatic or psychogenic organ in underweight patients as an adjuvant to treatment of the underlying condition, such as infection or parasitic diseases (including during convalescence), chronic diarrhea, anorexia nervosa, or depressive states in the elderly and mood disturbances in the elderly.

Contraindication

It is Contraindication in patient with `a history of hypersensitivity to any components of the product. Although its achlinergic activity it’s relatively weak, Pizotifen should be probably not be administered in the presence of narrow-angle glaucoma or prostate hypertrophy. Pizotifen should not be given in to children under 2 years of age.

Side effect

The most commonly occurring side effect are drowsiness and an increase in appetite, which may lead to increase in body weight. Other side effects such as dizziness, dry mouth nausea and constipation have been reported infrequency. In children, CNS stimulation may occur.

Pregnancy and lactation

As clinical data with Pizotifen in Pregnancy is very limited, although no ill effects have been reported. The drug should therefore only be given during pregnancy if the potential benefit to mother justifies the potential risk to the fetus. The safety of Pizotifen during lactation has not been established, so mother should avoid taking it when breast feeling.

Caution

Urinary retention, renal impairment, pregnancy and beast feeding should be taken in consideration. Drowsiness may affect the performance of skilled task (e.g. Dividing), effect of alcohol is enhances.

Precaution

Patient should be warned about the possibility of drowsiness and its significance in the driving of vehicle and the operation of machinery.

Drug interaction

Tolerance to alcohol may be lowered. Prolong the drowsiness that occurs as adverse effect of concurrently used tranquilizers, hypnotics and antidepressant. It should not be used in patients receiving monoamine oxidize inhibitors.

Dose and Administration

The recommended dose is as followings:

Adult: the initial dose is 1.5mg daily; this may be taken at bedtime as a single dose or in three divided dose. Dosage can be adjusted according to the individual patient requirement up to a maximum of 4.5mg daily. Up to 3mg may be given as a single daily dose.

Children: up to 1.5mg daily, usually as a divide dose. Use of 1.5mg at a time is not recommended, but up to 1mg can be given as a single daily dose at night. Children below two years of age should not be given Pizotifen.

Or, a directed by the registered physician.

Pharmaceuticals precaution

Store in a cool dry place protected from light. Keep out of reach of children.

Market competitors

Serial no.	Company Name	Brand name	Pack size	Unite per price	Selling price(per year)
01	Square	Migranil	Box containing 5×10 tablet Or 5×1 tablets in blister pack	3tk	TK. 22,751,915
02	Bexcimco	Avidro	Box containing 1×10 tablet Or 10×10 tablets in blister pack	3tk	TK. 5,938,344 tk
03	Drug International Ltd.	De-fen	Box containing 10×10 tablet Or 1×10 tablets in blister pack	2tk	TK. 6,580,221
04	Aristopharma Ltd.	Zofen	Box containing 10×10 tablet in blister pack	3tk	TK. 18,752,830
05	Opsonin Pharm	Pifen	Box containing 5×10 tablet in blister pack	2tk	TK. 2,503,136

SWOT analysis:

Seiral no.	Strength(Pizotifen)	Weakness(Rizatriptan)
01	It required low dose of Pizotifen as 1.5mg daily for acute treatment. So it active therapeutic effect at low dose	Rizatriptan required high dose as 5mg or 10mg daily for acute treatment it’s given low at high dose.
02	Children above 2 years it should be given	It is not recommended in children.
03	The bioavailability of this drug is 75%	The bioavailability of this drug is 45%
04	About 90% bound to plasma proteins. Peak plasma concentrations occur about 5 hr after a single oral dose.	About 5% bound to plasma proteins. Peak plasma concentrations occur about 10-15 hr after a single oral dose.