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Pizotifen
Systematic (IUPAC) name
4-(1-methyl-4-piperidylidine)-9,10-dihydro -4H-benzo-[4,5]cyclohepta[1,2]-thiophene
Identifiers
CAS number 15574-96-6
ATC code N02CX01
PubChem 27400
Chemical data
Formula C19H21NS 
Mol. mass 295.443 g/mol
Pharmacokinetic data
Bioavailability 78%
Protein binding 91%
Metabolism Glucuronidation (main route). N-glucuronide accounts for >50% of plasma and 60–70% of urinary excreted drug
Half life 23h
Excretion 18% feces, 55% urine (both as metabolites).
Therapeutic considerations
Pregnancy cat. B1(AU)
Legal status
Routes 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.[1]

Contents

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 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]

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, angle-closure 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 as well as some anticholinergic activity. [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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