Pharmacokinetics and tolerance of sertaconazole in man after repeated percutaneous administration

Arzneimittelforschung. 1992 May;42(5A):752-4.

Abstract

The local and systemic tolerance of 7-chloro-3-[1-(2,4-dichlorophenyl)-2-(1H- imidazol-1-yl)ethoxy-methyl]benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) 2% cream was studied in healthy volunteers after cutaneous application in an increasing-dose schedule during 13 days. Blood and urine samples were collected after the application of 16 g of cream. Percentage of absorption was determined in eight 3 x 3 cm areas of the volar arm skin after 2 mg cream topical application. No changes on vital signs (blood pressure, heart rate and body temperature) or in the ECG were found during the trial. Sertaconazole did not produce skin irritation nor systemic side effects. Sertaconazole was not detected in either the serum and urine samples obtained. The percentage of cutaneous absorption at 24 h after administration reached 72% of the applied dose.

MeSH terms

  • Administration, Cutaneous
  • Adolescent
  • Adult
  • Antifungal Agents / administration & dosage
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics*
  • Body Temperature / drug effects
  • Drug Tolerance
  • Hemodynamics / drug effects
  • Humans
  • Imidazoles / administration & dosage
  • Imidazoles / adverse effects
  • Imidazoles / pharmacokinetics*
  • Injections, Subcutaneous
  • Irritants
  • Male
  • Skin Absorption
  • Thiophenes / administration & dosage
  • Thiophenes / adverse effects
  • Thiophenes / pharmacokinetics*

Substances

  • Antifungal Agents
  • Imidazoles
  • Irritants
  • Thiophenes
  • sertaconazole