Pizotifen, also known aspizotyline and sold under the brand namesSandomigran andMosegor among others, is anantimigraine agent of thetricyclic group which is used primarily as apreventative to reduce the frequency of recurrentmigraine headaches.[1]
The main medical use for pizotifen is for the prevention ofmigraine andcluster headache. Pizotifen is one of a range of medications used for this purpose, other options includepropranolol,topiramate,valproic acid,cyproheptadine andamitriptyline. While pizotifen is effective in adults,[2] evidence of efficacy in children is limited,[3] and 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.[4] It is not effective in relieving migraine attacks once in progress.
Pizotifen has also been reported as highly effective in a severe case oferythromelalgia, a rare neurovascular disease that is sometimes refractory to the other drugs named above.[5]
Caution is required in patients having closed angleglaucoma and in patients with a predisposition tourinary retention as the medication exhibits a relatively small anticholinergic effect. Dose adjustment is required in people who havechronic 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 ofepilepsy.Withdrawal symptoms like depression, tremor, nausea, anxiety, malaise, dizziness, sleep disorder and weight decrease have been reported following abrupt cessation of pizotifen.[11]
Pizotifen is contraindicated in patients who suffer from hypersensitivity to any of its components or havegastric outlet obstruction, angle-closure glaucoma, and difficulty urinating.[12] In addition, women who arepregnant should not take pizotifen.[12]
Side effects includesedation,dry mouth, drowsiness, increased appetite and weight gain.[13] Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur.
Pizotifen is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name andBANTooltip British Approved Name, whilepizotyline is itsUSANTooltip United States Adopted Name.[21][22][23] Brand names of pizotifen include Sandomigran, Mosegor, and Litec, among others.[21][22][23][24]
^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.PMID348154.S2CID13510725.
^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):404–410.doi:10.1016/j.pbb.2005.09.010.PMID16253319.S2CID20885754.
^ab"Pizotifen".Universal Reference Book of Medicines – via Likarstwo.ru.
^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.
^Moritomo A, Yamada H, Watanabe T, Itahana H, Akuzawa S, Okada M, Ohta M (December 2013). "Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists".Bioorg Med Chem.21 (24):7841–7852.doi:10.1016/j.bmc.2013.10.010.PMID24189186.
^abNewman-Tancredi A, Conte C, Chaput C, Verrièle L, Audinot-Bouchez V, Lochon S, Lavielle G, Millan MJ (June 1997). "Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy".Naunyn Schmiedebergs Arch Pharmacol.355 (6):682–688.doi:10.1007/pl00005000.PMID9205951.
^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):1968–1979.PMID411500.