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Acticin (Permethrin) - Description and Clinical Pharmacology

 
 



DESCRIPTION

Acticin (permethrin) Cream 5% is a topical scabicidal agent for the treatment of infestation with Sarcoptes scabiei (scabies). It is available in an off-white, vanishing cream base. Acticin Cream is for topical use only.

Structural Formula:

Chemical Name:    The permethrin used is an approximate 1:3 mixture of the cis and trans isomers of the pyrethroid 3-(2,2-dichloroethyenyl)-2,2-dimethylcyclopropane carboxylic acid, (3-phenoxyphenyl) methyl ester. Permethrin has a molecular formula of C21H20Cl2O3 and a molecular weight of 391.29. It is a yellow to light orange-brown, low melting solid or viscous liquid.

Each gram of Acticin Cream 5% contains permethrin 50 mg (5%) and the inactive ingredients butylated hydroxytoluene, carbomer 934P, coconut oil, glycerin, glyceryl stearate, isopropyl myristate, lanolin alcohols, light mineral oil, polyoxyethylene cetyl ethers, purified water, and sodium hydroxide. Formaldehyde 1 mg (0.1%) is added as a preservative.

CLINICAL PHARMACOLOGY

Permethrin, a pyrethroid, is active against a broad range of pests including lice, ticks, fleas, mites, and other arthropods. It acts on the nerve cell membrane to disrupt the sodium channel current by which the polarization of the membrane is regulated. Delayed repolarization and paralysis of the pests are the consequences of this disturbance.

Permethrin is rapidly metabolized by ester hydrolysis to inactive metabolites which are excreted primarily in the urine. Although the amount of permethrin absorbed after a single application of the 5% cream has not been determined precisely, data from studies with14 C-labeled permethrin and absorption studies of the cream applied to patients with moderate to severe scabies indicate it is 2% or less of the amount applied.

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