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  • Sumatriptan succinate : pharmacokinetics of different formulations in clinical practice.

Sumatriptan succinate : pharmacokinetics of different formulations in clinical practice.

Expert opinion on pharmacotherapy (2012-09-28)
Luana Lionetto, Andrea Negro, Barbara Casolla, Maurizio Simmaco, Paolo Martelletti
ABSTRACT

Migraine is a common neurovascular disorder characterized by recurrent episodes of disabling headache, autonomic nervous system dysfunction, and in some patients, neurological aura symptoms. Triptans are frequently prescribed drugs for the treatment of the acute migraine attack, considering their capability to provide wide efficacy and tolerability. This review discusses pharmacodynamics and pharmacokinetics of sumatriptan succinate, considering the clinical impact of new drug formulations in the treatment of acute migraine and cluster headache. The data were obtained by searching the following keywords in MEDLINE: sumatriptan succinate, pharmacokinetics, pharmacodynamics, triptans, migraine, new delivery systems, relative to the period 1989 - 2012. Subcutaneous sumatriptan has been considered as the most efficacious treatment in the acute phase of migraine both on pain alone as well as on associated autonomic symptoms. Pharmacologically, pharmacokinetic parameters, in particular bioavailability, T(max) and C(max) are responsible for the wide efficacy of the compound and the limited adverse effect (AE) profile. The new drug formulations that are the most similar to the pharmacokinetics parameters of the subcutaneous one are promising because they both improve pharmacokinetic bioavailability bypassing the first-pass metabolism and increase patient compliance.

MATERIALS
Product Number
Brand
Product Description

Sumatriptan for system suitability, European Pharmacopoeia (EP) Reference Standard
Sumatriptan succinate, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Sumatriptan succinate, ≥98% (HPLC), solid
USP
Sumatriptan succinate, United States Pharmacopeia (USP) Reference Standard