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Indications and Dosage
Oral
Prophylaxis of cluster headache, Prophylaxis of migraine Adult: Initially, 0.5 mg, increase gradually as necessary. Maintenance: 1.5 mg daily as a single dose at night or in 3 divided doses. Max: 4.5 mg daily (max ≤3 mg/dose).
Child: ≥2 yr Initially, 0.5 mg. May increase gradually up to 1.5 mg daily in divided doses (max 1 mg/dose). |
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Renal Impairment
Dose adjustment may be needed.
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Hepatic Impairment
Dose adjustment may be needed.
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Administration
May be taken with or without food.
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Special Precautions
Patient w/ angle-closure glaucoma, urinary retention, epilepsy. Avoid abrupt withdrawal. Renal and hepatic impairment. Childn. Pregnancy and lactation.
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Adverse Reactions
Increased appetite, nausea, wt gain, drowsiness, dizziness, dry mouth, fatigue, muscle pain or cramps, heavy or restless legs, fluid retention, facial flushing, reduced libido, exacerbation of epilepsy, dreaming, hepatic injury.
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Patient Counseling Information
This drug may cause drowsiness, somnolence and dizziness, if affected, do not drive or operate machinery.
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Monitoring Parameters
Monitor hepatic function (prolonged use), wt gain, BP.
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Overdosage
Symptoms: Drowsiness, dizziness, hypotension, dry mouth, confusion, excitatory states (in childn), ataxia, nausea, vomiting, dyspnoea, cyanosis, tachycardia, convulsions (particularly in childn), coma, and resp paralysis. Management: Symptomatic treatment. Perform gastric lavage followed by admin of activated charcoal. Convulsions may be treated w/ short-acting barbiturates or benzodiazepines.
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Drug Interactions
Enhances the central effects of sedatives, hypnotics, antihistamines including certain common cold preparations. May reduce the efficacy of cisapride. MAOIs may prolong or intensify the anticholinergic effect of pizotifen.
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Food Interaction
Enhances the CNS effects of alcohol.
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Action
Description: Pizotifen is a sedating antihistamine which is known to inhibit the reuptake of serotonin by blood platelets, thereby preventing loss of tone of intracranial vessels. It has weak antimuscarinic properties and it also antagonises the action of tryptamine.
Pharmacokinetics: Absorption: Well absorbed from the GI tract. Absolute bioavailability: Approx 78%. Time to peak plasma concentration: Approx 5 hr. Distribution: Extensively and rapidly distributed throughout the body. Volume of distribution: 833 L (pizotifen); 70 L (N-glucuronide). Plasma protein binding: >90%. Metabolism: Extensively metabolised in the liver via glucuronidation. Excretion: Via urine, mainly as metabolites; faeces (approx 18%). Elimination half-life: Approx 23 hr (N-glucuronide conjugate). |
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Storage
Store between 15-30°C. Protect from light and moisture.
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MIMS Class
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ATC Classification
N02CX01 - pizotifen ; Belongs to the class of other antimigraine preparations.
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References
Anon. Pizotifen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 17/05/2016. Buckingham R (ed). Pizotifen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 17/05/2016. Joint Formulary Committee. Pizotifen. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 17/05/2016.
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