flunarizine (Sibelium)
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Introduction
Tradename: Sibelium
Indications
- migraine prophylaxis, including children[2] (NOT for aborting migraine)
- symptomatic treatment of vestibular vertigo
Contraindications
Dosage
Capsules: 5 mg
Pharmacokinetics
- well-absorbed from GI tract
- peak plasma levels in 2-4 hours; steady state in 5-6 weeks
- protein binding 99%
- hepatic metabolism; metabolites excreted in bile & feces
- terminal 1/2 life is 18 days
Adverse effects
- drowsiness
- fatigue
- depression, especially females with a history of depression
- extrapyramidal effects (especially elderly)
- uncommon
- sedation, agitation, tachycardia
- charcoal, gastric lavage, supportive therapy; no antidote
- drug adverse effects of calcium channel blockers
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- galactorrhea in women taking oral contraceptives
- sedatives & CNS depressants
- carbamazepine & phenytoin may increase metabolism of flunarizine
- drug interaction(s) of calcium channel blockers with ARBs
- drug interaction(s) of calcium channel blockers with ACE inhibitors
- drug interaction(s) of calcium channel blockers with diuretics
- drug interaction(s) of calcium channel blockers with erythromycin
- drug interaction(s) of calcium channel blockers with clarithromycin
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- calcium channel antagonist
- reduces excessive transmembrane Ca+2 fluxes
More general terms
References
- ↑ http://home.intekom.com/pharm/janssen/sibelium.html
- ↑ Jump up to: 2.0 2.1 Prescriber's Letter 12(3): 2005 Drug Therapy for Children and Adolescents with Migraine Headaches Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210307&pb=PRL (subscription needed) http://www.prescribersletter.com
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3378
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=941361
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3377
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=35353
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5282407
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657260