The drug Sureptil® contained two active principles: (i) the piperazine derivative cinnarizine which has antihistaminic, antiserotoninergic, antidopaminergic, and calcium channel-blocking activities, and (ii) the synthetic molecule heptaminol acefyllinate (a theophylline derivative) which is a peripheral vasodilator. The drug combination was used to improve blood circulation and tissue oxygenation. Sureptil® was removed from the market in 2003. The drug was Sureptil® in France, and Stugeron® in other countries, mainly used to control travel sickness.
Cinnarizine is an anti-histaminic agent (antagonist of H1-histamine receptors) but its has also antiserotonergic, antidopaminergic, and calcium channel-blocking activities. This compound has been used for the treatment of nausea and motion sickness, as well as vertigo associated with Ménière’s syndrome, taking advantage of its anti-vasoconstrictor activity and its capacity to reduce blood viscosity. Cinnarizine represents an efficacious and well-tolerated prophylactic antimigraine medication, notably in adults with migraine-associated vertigo such as vestibular migraine. It remains used today in a few countries (not in the US). The treatment benefit of this compound should be balanced with its adverse effects because the long-term use of this compound has been suspected to increase the risk for Parkinsonism, dyskinesia, and dystonia. It has shown extrapyramidal side effects.
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Sureptil was used to treat cerebral circulatory insufficiency. The cover image was intended to illustrate the improved brain flow upon treatment with Sureptil, with a type of extended blueish brain, like waves or clouds.