Flunarizine

404.49

404.49

257-937-5

R7PLA2DM0J

DTXSID6045616

N07CA03|N - Nervous system

6.5

5.78

Solid

1.17 g/cm3

251.5

511.3ºC at 760 mmHg

1.606

1.68e-03 g/L

211.5 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

-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.

99% bound to plasma proteins

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.

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

Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)|Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood. (See all compounds classified as Histamine H1 Antagonists.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

85% following oral administration.

Hepatic, to two metabolites via N-dealylation and hydroxylation.|Flunarizine has known human metabolites that include 1-[bis(4-fluorophenyl)methyl]piperazine, bis(4-fluorophenyl)methanone, and p-Hydroxyflunarizine.

18 days

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.

Dihydrochloride, Flunarizine

Pharmaceuticals