Pizotifen

drugbox
IUPAC_name = 4-(1-methyl-4-piperidylidine)-9,10-dihydro -4"H"-benzo- [4,5] cyclohepta [1,2] -thiophene

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width = 140
CAS_number = 15574-96-6
ATC_prefix = N02
ATC_suffix = CX01
PubChem = 27400
DrugBank =
C = 19 | H = 21 | N = 1 | S = 1
molecular_weight = 295.443 g/mol
bioavailability = 78%
protein_bound = 91%
metabolism = Glucuronidation (main route). "N"-glucuronide accounts for >50% of plasma and 60–70% of urinary excreted drug
elimination_half-life = 23h
excretion = 18% feces, 55% urine (both as metabolites).
pregnancy_AU = B1
pregnancy_US =
pregnancy_category=
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status =
routes_of_administration = Oral

Pizotifen (INN) or pizotyline (USAN), trade name Sandomigran, is a benzocycloheptane based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches. [Stark RJ, Valenti L, Miller GC. Management of migraine in Australian general practice. Medical Journal of Australia. 2007 Aug 6;187(3):142-6.]

Uses

The main medical use for pizotifen is for the prevention of vascular headache including migraine and cluster headache. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate, valproic acid and amitryptyline. While pizotifen is reasonably effective, [Barnes N, Millman G. Do pizotifen or propranolol reduce the frequency of migraine headache? Archives of Disease in Childhood. 2004 Jul;89(7):684-5.] 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. [Pierangeli G, Cevoli S, Sancisi E, Grimaldi D, Zanigni S, Montagna P, Cortelli P. Which therapy for which patient? Neurological Sciences. 2006 May;27 Suppl 2:S153-8.]

Other applications for which pizotifen may be used include as an antidepressant, or for the treatment of anxiety or social phobia. [Standal JE. Pizotifen as an antidepressant. Acta Psychiatrica Scandinavica. 1977 Oct;56(4):276-9.] [Banki CM. Clinical observations with pizotifene (Sandomigran) in the treatment of nonmigrainous depressed women. Archiv fur Psychiatrie und Nervenkrankheiten. 1978 Mar 7;225(1):67-72.] Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose [Young R, Khorana N, Bondareva T, Glennon RA. Pizotyline effectively attenuates the stimulus effects of N-methyl-3,4-methylenedioxyamphetamine (MDMA). Pharmacology, Biochemistry and Behavior. 2005 Oct;82(2):404-10.] in a similar manner to the closely related antihistamine/antiserotonin drug cyproheptadine.

Adverse effects

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

Contraindications

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 [ [http://lekarstwo.ru/en/preparati/pizotifen.html Likarstwo.ru] ] .

Mechanism

Pizotifen is a serotonin antagonist acting mainly at the 5-HT₁, 5-HT_2A and 5HT_2C receptors. It also has some activity as an antihistamine. [Dixon AK, Hill RC, Roemer D, Scholtysik G. Pharmacological properties of 4-(1-methyl-4-piperidylidine)-9,10-dihydro-4H-benzo- [4,5] cyclohepta [1,2] -thiophene hydrogen maleate (pizotifen). Arzneimittelforschung. 1977;27(10):1968-79.]

References

External links

* [http://www.medsafe.govt.nz/Profs/Datasheet/s/Sandomigrantab.htm Sandomigran drug data sheet]