Pizotifen

Pizotifen (INN) or pizotyline (USAN), trade name Sandomigran, is a benzocycloheptene-based drug used as a medicine, primarily as a preventive to reduce the frequency of recurrent migraine headaches.[1]

Pizotifen
Clinical data
Trade namesSandomigran
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
    Routes of
    administration    		Oral
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability78%
    Protein binding91%
    MetabolismGlucuronidation (main route). N-glucuronide accounts for >50% of plasma and 60–70% of urinary excreted drug
    Elimination half-life23 hours
    Excretion18% feces, 55% urine (both as metabolites)
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.036.014
    Chemical and physical data
    FormulaC19H21NS
    Molar mass295.44 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    Uses

    The main medical use for pizotifen is for the prevention of migraine and cluster headache. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate, valproic acid, cyproheptadine and amitriptyline. While pizotifen is reasonably effective,[2] its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective.[3] It is not effective in relieving migraine attacks once in progress. Pizotifen has also been reported as highly effective in a severe case of erythromelalgia, a rare neurovascular disease that is sometimes refractory to the other drugs named above.[4]

    Other applications for which pizotifen may be used include as an antidepressant, or for the treatment of anxiety or social phobia.[5][6]> Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose[7] in a similar manner to the closely related antihistamine/antiserotonin medication cyproheptadine.

    Adverse effects

    Side effects include sedation, dry mouth, drowsiness, increased appetite and weight gain.[8] Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur.

    Concerning weight gain, pizotifen can be described as an appetite stimulant as for weight gain is usually of the order of 2 to 4 kg, but can be as much as 7.5 to 10 kg and is most rapid in the first few weeks of treatment. In the course of 2 or 3 months of therapy the weight stabilises itself and some patients are able to reduce weight while still on the drug. [9]

    Contraindications

    Caution is required in patients having closed angle glaucoma and in patients with a predisposition to urinary retention as the medication exhibits a relatively small anticholinergic effect. Dose adjustment is required in people who have chronic kidney disease. Liver injury has also been reported. Pizotifen treatment should be discontinued if there is any clinical evidence of liver dysfunction during treatment. Caution is advised in patients having a history of epilepsy. Withdrawal symptoms like depression, tremor, nausea, anxiety, malaise, dizziness, sleep disorder and weight decrease have been reported following abrupt cessation of pizotifen.[10] Pizotifen is contraindicated in patients who suffer from hypersensitivity to any of its components, also Pizotifen is contraindicated in gastric outlet obstruction, pregnancy, angle-closure glaucoma and difficulty urinating.[11]

    Pharmacology

    Pizotifen is a serotonin antagonist acting mainly at the 5-HT2A and 5HT2C receptors. It also has some activity as an antihistamine as well as some anticholinergic activity.[12]

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    See also

    References
    1. Stark RJ, Valenti L, Miller GC (August 2007). "Management of migraine in Australian general practice". The Medical Journal of Australia. 187 (3): 142–6. doi:10.5694/j.1326-5377.2007.tb01170.x. PMID 17680738.
    2. Barnes N, Millman G (July 2004). "Do pizotifen or propranolol reduce the frequency of migraine headache?". Archives of Disease in Childhood. 89 (7): 684–5. doi:10.1136/adc.2004.054668. PMC 1719986. PMID 15210509.
    3. Pierangeli G, Cevoli S, Sancisi E, Grimaldi D, Zanigni S, Montagna P, Cortelli P (May 2006). "Which therapy for which patient?". Neurological Sciences. 27 (Suppl 2): S153–8. doi:10.1007/s10072-006-0592-0. PMID 16688621.
    4. Cohen JS (November 2000). "Erythromelalgia: new theories and new therapies". Journal of the American Academy of Dermatology. 43 (5 Pt 1): 841–7. doi:10.1067/mjd.2000.109301. PMID 11050591.
    5. Standal JE (October 1977). "Pizotifen as an antidepressant". Acta Psychiatrica Scandinavica. 56 (4): 276–9. doi:10.1111/j.1600-0447.1977.tb00228.x. PMID 335788.
    6. Banki CM (March 1978). "Clinical observations with pizotifene (Sandomigran) in the treatment of nonmigrainous depressed women". Archiv für Psychiatrie und Nervenkrankheiten. 225 (1): 67–72. doi:10.1007/bf00367352. PMID 348154.
    7. Young R, Khorana N, Bondareva T, Glennon RA (October 2005). "Pizotyline effectively attenuates the stimulus effects of N-methyl-3,4-methylenedioxyamphetamine (MDMA)". Pharmacology, Biochemistry, and Behavior. 82 (2): 404–10. doi:10.1016/j.pbb.2005.09.010. PMID 16253319.
    8. Crowder D, Maclay WP. Pizotifen once daily in the prophylaxis of migraine: results of a multi-centre general practice study. Current Medical Research and Opinion. 1984;9(4):280-5.
    9. Speight TM, Avery GS. (1972). "Pizotifen (BC-105): a review of its pharmacological properties and its therapeutic efficacy in vascular headaches". Drugs. 3 (3–4): 159–203. doi:10.2165/00003495-197203030-00002. PMID 4403890.CS1 maint: uses authors parameter (link)
    10. "Emedicine".
    11. "Likarstwo.ru".
    12. Dixon AK, Hill RC, Roemer D, Scholtysik G (1977). "Pharmacological properties of 4(1-methyl-4-piperidylidine)-9,10-dihydro-4H-benzo-[4,5]cyclohepta[1,2]-thiophene hydrogen maleate (pizotifen)". Arzneimittel-Forschung. 27 (10): 1968–79. PMID 411500.
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