Flunarizine
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| Clinical data | |
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| Trade names | Sibelium |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Protein binding | >99% |
| Metabolism | Mainly CYP2D6 |
| Metabolites | ≥15 |
| Biological half-life | 5–15 hrs (single dose) 18–19 days (multiple doses) |
| Excretion | Faeces, <1% urine |
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| Synonyms | 1-[bis(4-fluorophenyl)methyl]-4-cinnamyl-piperazine |
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| ChEMBL | |
| ECHA InfoCard | 100.052.652 |
| Chemical and physical data | |
| Formula | C26H26F2N2 |
| Molar mass | 404.495 g/mol |
| 3D model (Jmol) | |
| Melting point | 251.5 °C (484.7 °F) (dihydrochloride) |
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Flunarizine (trade name Sibelium and many others) is a drug classified as a calcium antagonist. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. It has been shown to significantly reduce headache frequency and severity in both adults and children.
Flunarizine is not available by prescription in the U.S. or Japan. It was discovered at Janssen Pharmaceutica in 1968.
Flunarizine is contraindicated in patients with depression, in the acute phase of a stroke, and in patients with extrapyramidal symptoms or Parkinson's disease. It is also contraindicated in hypotension, heart failure and arrhythmia.
Common side effects include drowsiness (20% of patients), weight gain (10%), as well as extrapyramidal effects and depression in elderly patients.
The effects of other sedating drugs and alcohol, as well as antihypertensives, can be increased. No relevant pharmacokinetic interactions have been described.
Flunarizine is a non-selective calcium antagonist with moderate other actions including antihistamine, serotonin receptor blocking and dopamine D2 blocking activity. Compared to other calcium channel blockers such as dihydropyridine derivatives, verapamil and diltiazem, flunarizine has low affinity to voltage-dependent calcium channels. It has been theorised that it may act not by inhibiting calcium entry into cells, but rather by an intracellular mechanism such as antagonising calmodulin, a calcium binding protein.
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