Product Details

Flunarizine

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. 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.

Indication

Used in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Associated Conditions

• Severe Migraine

Pharmacodynamics

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.

Mechanism of action

Flunarizine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Absorption

85% following oral administration.

Volume of distribution

Not Available

Protein binding

99% bound to plasma proteins

Metabolism

Hepatic, to two metabolites via N-dealylation and hydroxylation.

• Flunarizine
   
  Flunarizine metabolite M1
• Flunarizine
   
  Flunarizine metabolite M2
• Flunarizine
   
  Flunarizine metabolite M3

Route of elimination

Not Available

Half life

18 days

Clearance

Not Available

Toxicity

-Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects. -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia. -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.

Affected organisms

• Humans and other mammals

source: drugbank