Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties

Pharmacotherapeutic group: Pyrethrines, incl. synthetic compounds
ATC code: P03AC04

The principle physiological action in insects (lice) exposed to permethrin is induction of electrochemical abnormalities across the membranes of excitable cells, leading to sensory hyperexcitability, in co-ordination and prostration. It is assumed that the mode of action against arachnids (mites) is similar.

Paediatric population
Newborns and infants:
The safety and efficacy of permethrin in newborns and infants under 2 months of age have not been established since no data are available from prospective trials or larger case series. A limited number of case reports in the treatment of children under 2 months of age presenting with scabies do not suggest specific safety concerns for the use of topical permethrin in this age group, but no definite conclusion can be drawn.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

Investigations with the 5 % cream in humans revealed an average percutaneous absorption rate of 0.47 ± 0.3 % in healthy subjects and of 0.52 ± 0.3 % in patients. Pharmacokinetic properties were studied in adult subjects only (6 healthy volunteers and 6 patients with scabies). Absorbed permethrin is rapidly broken down by esterases as well as hydrolases. After oral administration, peak plasma concentrations are reached in approximately 4 hours. The isomeric mixture is then excreted in the urine in the form of glucuronides, sulfates etc as cis- trans CI2CA [(3- (2,2-dichlorovinyl)-2,2- dimethylcyclopropane-1-carboxylic acid)] and after oxidation to 3 PBA (3- phenoxybenzoic acid).
After oral application, up to 6 % is excreted unchanged in the faeces whilst on dermal application, unchanged permethrin is virtually undetectable.