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Pizotifen

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Pizotifen
Clinical data
Pregnancy
category
  • AU: B1
Routes of
administration		Oral
ATC code
Pharmacokinetic data
Bioavailability78%
Protein binding91%
MetabolismGlucuronidation is the main route of biotransformation, the main metabolite is the N-glucuronide-conjugate,accounting for at least 50% of the plasma and 60-70% of urinary excreted drug.
Elimination half-life23h
Excretion18% feces, 55% urine (both as metabolites).
Identifiers
  • 4-(1-methyl-4-piperidylidine)-9,10-dihydro -4H-benzo-[4,5]cyclohepta[1,2]-thiophene
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.036.014 Edit this at Wikidata
Chemical and physical data
FormulaC19H21NS
Molar mass295.443 g/mol g·mol−1

Pizotifen (trade names Pizotyline, Sandomigran) is a benzocycloheptane based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches.[1]

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,[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]

Other applications for which pizotifen may be used include as an antidepressant, or for the treatment of anxiety or social phobia.[4][5] Animal studies also suggest that pizotyline could be used in the treatment of serotonin syndrome or MDMA overdose[6] 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.[7] 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, zakrytougolnoy glaucoma and difficulty urinating[8].

Mechanism

Pizotifen is a serotonin antagonist acting mainly at the 5-HT1, 5-HT2A and 5HT2C receptors. It also has some activity as an antihistamine.[9]

References

  1. ^ Stark RJ, Valenti L, Miller GC. Management of migraine in Australian general practice. Medical Journal of Australia. 2007 Aug 6;187(3):142-6.
  2. ^ 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.
  3. ^ 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.
  4. ^ Standal JE. Pizotifen as an antidepressant. Acta Psychiatrica Scandinavica. 1977 Oct;56(4):276-9.
  5. ^ 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.
  6. ^ 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.
  7. ^ 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.
  8. ^ Likarstwo.ru
  9. ^ 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.
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