Pizotifen is a [[serotonin antagonist]] acting mainly at the [[5-HT1 receptor|5-HT<sub>1</sub>]], [[5-HT2A receptor|5-HT<sub>2A</sub>]] and [[5-HT2C receptor|5HT<sub>2C</sub>]] [[serotonin receptor|receptors]]. It also has some activity as an [[antihistamine]].<ref>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.</ref>
Pizotifen is a [[serotonin antagonist]] acting mainly at the [[5-HT1 receptor|5-HT<sub>1</sub>]], [[5-HT2A receptor|5-HT<sub>2A</sub>]] and [[5-HT2C receptor|5HT<sub>2C</sub>]] [[serotonin receptor|receptors]]. It also has some activity as an [[antihistamine]].<ref>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.</ref>
Glucuronidation 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.
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]
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.
^Stark RJ, Valenti L, Miller GC. Management of migraine in Australian general practice. Medical Journal of Australia. 2007 Aug 6;187(3):142-6.
^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.
^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.
^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.
^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.
^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.
^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.
