Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: Pfizer Healthcare Ireland, 9 Riverwalk, National Digital Park, Citywest Business Campus, Dublin 24, Ireland
Pharmacotherapeutic group: Imidazole and triazole derivatives
ATC Code: D01AC07
Tioconazole is an imidazole which is active against commonly occurring dermatophyte and yeast-like fungal species. It is fungicidal in murine models vs. Candida spp., T. rubrum and T. mentacrophytes. In vitro it is fungicidal to pathogenic dermatophytes, yeasts and other fungi. All dermatophytes and Candida spp. were inhibited by 6.25 or 12.5 mg/l respectively. It is also inhibitory vs. Staph. spp. and Strep. spp. at 100 mg/l or less.
Oral doses (200 mg/kg) did not affect behaviour in rats but 25 mg/kg i.v. produced dose-related respiratory distress, gasping, tremors and prostration. Slight but dose-related impairment of performance of mice on the rotating rod occurred from 25 mg/kg. Slight anti-cholinergic and anti-histamine (H1) activity was recorded in vitro but no effect on mice pupil size in vivo. Oral tioconazole prolonged alcohol and pentobarbital sleeping time at 150 and 37.5 mg/kg respectively.
In the anaesthetised cat i.v. tioconazole 2.5-10 mg/kg produced brief falls in blood pressure and increased heart rate, haematuria, tremors and twitches.
Absorption is rapid and extensive on oral administration to rats, monkeys and man, the major metabolite being a glucuronide conjugate of tioconazole. Tissue uptake in rat and monkey was highest in liver, kidney and intestinal tract with excretion in all species mainly in faeces.
Rat studies using oral, dermal and vaginal administration of C14 labelled tioconazole confirm significantly lower absorption via the topical route.
In man, oral formulations of tioconazole (500mg) gave plasma concentrations of 1300ng/ml. Topical administration of dermal cream 1% (20mg/day) for 28 days, or vaginal cream 2% (100mg/day) for 30 days gave negligible mean peak plasma levels, i.e. 10.1 and 11.5ng/ml respectively.
After single dose administration of tioconazole vaginal ointment 6.5% w/w (tioconazole 300mg) the mean peak plasma concentration was 18ng/ml in humans, achieved approximately 8 hours post dose.
None relevant to the prescriber.
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