ABSTRACT
14C-labelled 1-[(2-fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H- imidazole (flutrimazole, UR-4056, CAS 119006-77-8) was administered topically (dermally) in three male volunteers to normal skin and scarified skin, respectively. Blood, urine and faeces were collected and radioassayed by liquid scintillation counting techniques. After topical application to healthy skin area, less than 1% of flutrimazole was absorbed percutaneously from a 1% cream and the amount absorbed was excreted with the urine. Following administration of the drug to scarified skin, the proportions absorbed were very similar to those measured after application to normal skin. About 0.5% of the administered dose is recovered in urine. The absorbed amount of drug leads to very low concentrations in the circulation, lower than a few ng/ml.
Subject(s)
Antifungal Agents/pharmacokinetics , Cicatrix/metabolism , Clotrimazole/analogs & derivatives , Administration, Topical , Adult , Antifungal Agents/administration & dosage , Clotrimazole/administration & dosage , Clotrimazole/pharmacokinetics , Feces/chemistry , Humans , Male , Skin Absorption , Skin Physiological PhenomenaABSTRACT
The renal heamodynamic effects of a single i.v. administration of tolamolol were studied in 9 hypertensive subjects. No change of GFR and ERPF was observed after tolamolol, while urine output decreased and urine creatinine concentration increased. A reduction of the heart rate was confirmed. Blood pressure was unchanged.
