Pizotifen

Dosage adjustment may be needed.

Dosage adjustment may be needed.

May be taken with or without food.

Patient with epilepsy, closed angle glaucoma; at risk of or with current urinary retention (e.g. prostate hypertrophy). Obese patient. Not indicated for the treatment of migraine attacks or tension headaches. Avoid abrupt withdrawal. Renal and hepatic impairment. Children. Pregnancy and lactation.

Significant: CNS depression, hepatotoxicity, increased appetite, weight gain. Rarely, seizures.
Gastrointestinal disorders: Nausea, vomiting, dry mouth.
General disorders and administration site conditions: Fatigue.
Musculoskeletal and connective tissue disorders: Arthralgia, muscle cramps.
Nervous system disorders: Somnolence, dizziness, drowsiness, tremor.
Psychiatric disorders: Rarely, depression, anxiety, insomnia.
Skin and subcutaneous tissue disorders: Rarely, rash, urticaria.

This drug may cause dizziness, somnolence, or vertigo; if affected, do not drive or operate machinery.

Monitor LFTs (prolonged use), renal function, blood pressure, weight gain, visual disturbance.

Symptoms: Nausea, vomiting, xerostomia, drowsiness, dizziness, hypotension, tachycardia, pyrexia, confusion, ataxia, dyspnoea, cyanosis, respiratory paraylysis, coma; excitatory states, convulsions (particularly in children). Management: Symptomatic treatment. Administer activated charcoal; may perform gastric lavage in case of very recent intake. Short-acting barbiturates or benzodiazepines may be given for excitatory states or convulsions. Correct severe hypotension.

May diminish the therapeutic effect of cisapride. Increased central effects of sedatives, hypnotics, antihistamines. Decreased hypotensive effect of adrenergic neurone blockers (e.g. debrisoquine, guanethidine).

Increased central effects of alcohol.

Description:
Mechanism of Action: Pizotifen is a potent serotonin and tryptamine inhibitor with weak antihistamine, anticholinergic, and antikinin effects; it also possesses appetite-stimulating and sedative properties. The mechanism of action by which it exerts its prophylactic effect on migraine has not been fully explained but has been associated with its capability to modify the humoral mechanisms of headache. It prevents the permeability-increasing effect of serotonin and histamine on the affected cranial vessels, thereby regulating the transudation of plasmakinin which maintains the pain threshold of receptors at the normal levels. It inhibits serotonin reuptake by platelets which affects tonicity and reduces the passive distension of extracranial arteries.
Onset: Weeks of therapy may be needed.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability: Approx 78%. Time to peak plasma concentration: Approx 5 hours.
Distribution: Extensively and rapidly distributed throughout the body. Volume of distribution: 833 L (parent drug); 70 L (N-glucuronide metabolite). Plasma protein binding: Approx 91%.
Metabolism: Extensively metabolised in the liver via glucuronidation into its major metabolite N-glucoronide-conjugate.
Excretion: Mainly via urine (approx 55% as metabolites, <1% as unchanged drug); faeces (approx 33% of dose). Elimination half-life: Approx 23 hours (parent drug and metabolite).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 27400, Pizotifen. https://pubchem.ncbi.nlm.nih.gov/compound/Pizotifen. Accessed Apr. 27, 2023.

Store between 15-30°C. Protect from light and moisture.

Thuốc trị đau nửa đầu

N02CX01 - pizotifen ; Belongs to the class of other antimigraine preparations.

AFT Pharmaceuticals Pty Ltd. Sandomigran 500 mcg Coated Tablets data sheet 21 June 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 16/03/2023.

Anon. Pizotifen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/03/2023.

Buckingham R (ed). Pizotifen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/03/2023.

Joint Formulary Committee. Pizotifen. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/03/2023.

Pizogran 0.5 Tablets (Eucogen Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 16/03/2023.

Pizotifen 0.5 mg Tablets (Tillomed Laboratories Ltd). MHRA. https://products.mhra.gov.uk. Accessed 16/03/2023.

Pizotifen 1.5 mg Tablets (Genethics Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 16/03/2023.