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Pizotifen(BC-105): A Review of its Pharmacological Properties and its Therapeutic Efficacy in Vascular Headaches

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Summary

Synopsis: Pizotifen2 is a benzocycloheptathiophene derivative possessing a strong antagonistic action against certain biogenic amines. It is indicated in the prophylactic treatment of severe and recurrent vascular headaches, but is of no value in the treatment of acute attacks.

Pizotifen is structurally similar to cyproheptadine and the tricyclic antidepressants, and has been shown to exert strong antiserotonin and antihistaminic effects, together with a weak anticholinergic activity. These antagonistic effects are evidently related to the drug’s mode of action in reducing the occurrence of migrainous attacks, as it is now considered that the pathogenesis of migraine involves the action of a number of vasoactive substances (including serotonin, histamine, noradrenaline, acetylcholine and bradykinin) on the microcirculation. Most, but not all, therapeutic trials have obtained reasonably good results in patients suffering from either classic or common migraine and also in patients with cluster headache (migrainous neuralgia). Controlled studies have in general shown pizotifen to be significantly more effective than a placebo, but usually less effective than methysergide. In some cases however, patients who have failed to respond to methysergide have responded to pizotifen. In other forms of headache, such as tension or muscle contraction headache, post-traumatic headache, inflammatory headache and trigeminal neuralgia, pizotifen has generally had little effect. With usual therapeutic doses (1.5 to 3 mg daily) drowsiness and increased appetite (with weight gain) frequently occur. In the majority of patients, these symptoms usually prove mild and tend to diminish during prolonged therapy.

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  1. Australasian Drug Information Services, Auckland, Australia

    T. M. Speight & G. S. Avery

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  1. T. M. Speight
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  2. G. S. Avery
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‘Sandomigran’ or BC-l 05 (Sandoz).

Manuscript reviewed by: M. Anthony, Neurologist, Prince Henry and Prince of Wales Hospitals, Sydney, Australia; J.R. Bianchine, Division of Clinical Pharmacology, The Johns Hopkins University, Baltimore, Md, USA; J.A.K. Cuningham, Neurologist, Christchurch Hospital, Christchurch, New Zealand; M.J. Eadie, Neurologist, Royal Brisbane Hospital, Brisbane, Australia; K. Ekbom, Department of Neurology, Södersjuk-huset, Stockholm, Sweden; J.W. Lance, Division of Neurology, Prince Henry and Prince of Wales Hospitals, Sydney, Australia; M.J. Rand, Department of Pharmacology, University of Melbourne, Parkville, Australia; O. Sjaastad, Department of Neurology, Rikshospitalet, Oslo, Norway; D.N. Wade, Department of Clinical Pharmacology, St. Vincents Hospital, Sydney, Australia; W.E. Waters, Faculty of Medicine, The University of Southampton, Highfield, Southampton, England

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Speight, T.M., Avery, G.S. Pizotifen(BC-105): A Review of its Pharmacological Properties and its Therapeutic Efficacy in Vascular Headaches. Drugs 3, 159–203 (1972). https://doi.org/10.2165/00003495-197203030-00002

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