The P-I-E-N-O Parkinsn's List Drug Database

flunarizine / Cinnarizine^TM

SEIZURE ANTAGONIST:

Selective calcium-entry blockade

Description: Flunarizine is an oral investigational CNS agent. It is a long-acting derivative of cinnarizine. Flunarizine is under investigation for use as an anticonvulsant, for peripheral and cerebral circulatory disorders, for prophylaxis of migraine, and vertigo.

Actions: demonstrates "selective" calcium-entry blockade; antagonizes the tonic seizure component in several seizure induction tests; inhibits the contraction of vascular smooth muscle; also exhibits antihistaminic effects; negative inotropic effect is insignificant.

Uses: unclear at this time; available on compassionate plea basis for treatment of alternating hemiplegia; has also been used in vertigo, cerebrovascular insufficiency, and prophylaxis of common or classic migraine.

Distinguishing Features: well absorbed after oral administration; highly lipophilic; protein binding >99%; extensively metabolized; minimal unchanged drug appears in urine or feces; elimination T« ranges 10-50 days (ave: 18-19 days); anticonvulsant profile of flunarizine is similar to carbamazepine and phenytoin, although flunarizine is less potent on a weight basis; antimigraine prophylaxis similar to pizotifen and cinnarizine.

Major Adverse Reactions: drowsiness is most commonly reported ADR (7% of patients); parkinsonism, tardive dyskinesia, akathisia, depression have also been reported.

Usual Adult Dosage: For migraine and cerebrovascular disorders: 10 mg/day PO in adults and 5 mg/day PO in children <40 kg. For seizure disorders: 15-20 mg/day PO in adults and 5-10 mg/day PO in children.

Administer doses at bedtime.

Manufacturer: Janssen Research Foundation, 1125 Trenton- Harbourton Road, P. O. Box 200 Office A30190, Titusville, NJ 08560-0200. (609)-730-3137 (attn: Mike Pontecorvo, PhD)

Status: no NDA has been submitted; availability on a compassionate plea-basis for treatment of alternating hemiplegia was terminated November 1994; Janssen is no longer pursuing approval of this agent; product is not available in the US (verbal communication 4/12/95).

References: *reviews: Todd PA et al. Drugs 1989;38:481-99. Bialer M. Clin Pharmacokinet 1993;24:331-52. Leppik IE. Epilepsia 1994;35(suppl 4):S29-S40.

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