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Levocabastine Hydrochloride

(BANM, US Adopted Name, rINNM)

Drug Nomenclature

Synonyms: Levocabastina, hidrocloruro de; Levocabastini Hydrochloridum; Levokabastiinihydrokloridi; Levokabastin-hydrochlorid; Levokabastinhydroklorid; Levokabastino hidrochloridas; Levokabasztin-hidroklorid; R-50547
BAN: Levocabastine Hydrochloride [BANM]
USAN: Levocabastine Hydrochloride
INN: Levocabastine Hydrochloride [rINNM (en)]
INN: Hidrocloruro de levocabastina [rINNM (es)]
INN: Lévocabastine, Chlorhydrate de [rINNM (fr)]
INN: Levocabastini Hydrochloridum [rINNM (la)]
INN: Левокабастина Гидрохлорид [rINNM (ru)]
Chemical name: (-)-trans-1-[cis-4-Cyano-4-(p-fluorophenyl)cyclohexyl]-3-methyl-4-phenylisonipecotic acid hydrochloride
Molecular formula: C26H29FN2O2,HCl =457.0
CAS: 79516-68-0 (levocabastine); 79547-78-7 (levocabastine hydrochloride); 79449-98-2 (cabastine)
ATC code: R01AC02; S01GX02
Read code: y09dK [Eye]; y09dL [Nose]

Note. Cabastine (rINN) is the racemate of levocabastine.

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (bevocabastine Hydrochloride). A white or almost white powder. Practically insoluble in water slightly soluble in alcohol and in a 0.2% solution of sodium hydroxide sparingly soluble in methyl alcohol. Protect from light.

The United States Pharmacopeia 31, 2008 (bevocabastine Hydrochloride). Protect from light.

Adverse Effects and Precautions

As for the antihistamines in general. The most common adverse effects reported with levocabastine eye drops are transient stinging and burning of the eyes, urticaria, dyspnoea, drowsiness, and headache. With nasal use headache, nasal irritation, somnolence, and fatigue have been noted. The use of levocabastine nasal spray is not recommended in those with significant renal impairment.

Pharmacokinetics

Levocabastine is absorbed after both nasal and ocular use. Systemic availability has been estimated at 60 to 80% after nasal doses and 30 to 60% after ocular use. However absolute peak plasma concentrations are low. Plasma protein binding is about 55%. An elimination half-life of 35 to 40 hours has been reported for all routes of delivery. Elimination of levocabastine is primarily renal with 70% excreted as unchanged drug and 10% as an inactive acetylglucuronide metabolite the remaining 20% is excreted unchanged in the faeces. Trace amounts of levocabastine have been found in breast milk after ocular and nasal use.

Uses and Administration

Levocabastine, a piperidine derivative, is a long-acting and potent antihistamine with a rapid onset of action. Levocabastine hydrochloride equivalent to 0.05% levocabastine is used topically twice daily as eye drops or as a nasal spray in the treatment of allergic conjunctivitis and rhinitis, respectively, in adults and children aged 9 years and over. The frequency of the dose in both conditions may be increased to 3 or 4 times daily if necessary. In conjunctivitis it is recommended that treatment should be stopped if there is no improvement within 3 days.

Preparations

Proprietary Preparations

Argentina: Histimet

Australia: Livostin

Austria: Livostin

Belgium: Livostin

Brazil: Livostin

Canada: Livostin

Czech Republic: Livostin

Denmark: Livostin

Finland: Livostin

France: Levophta

Germany: Levophta Livocab

Greece: Livostin

Hungary: Livostin

Israel: Livostin

Italy: Levostab Livocab Livostin

Japan: Livostin

Mexico: Livostin

The Netherlands: Livocab

Norway: Livostin

New Zealand: Livostin

Portugal: Livostin

South Africa: Livostin

Spain: Bilina Livocab

Sweden: Livostin

Switzerland: Livostin

Thailand: Livostin

Turkey: Livostin

United Kingdom: Livostin

USA: Livostin

Venezuela: Livostin


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This entry was posted on Saturday, July 24th, 2010 at 2:49 am and is filed under Antiallergic Drugs. You can follow any responses to this entry through the RSS 2.0 feed. Both comments and pings are currently closed.

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