Country: Afrika t’Isfel
Lingwa: Ingliż
Sors: South African Health Products Regulatory Authority (SAHPRA)
Lennon
KETAZOL Tablets SCHEDULING STATUS: S4 PROPRIETARY NAME (and dosage form): KETAZOL Tablets COMPOSITION: Each tablet contains 200 mg of ketoconazole . Antioxidant: sodium sulphite, anhydrous. PHARMACOLOGICAL CLASSIFICATION: A.20.2.2 Antimicrobial (Chemotherapeutic) agents: Fungicides. PHARMACOLOGICAL ACTION: Ketoconazole is a synthetic imidazole dioxolane derivative, active (in vitro) against dermatophytes, yeasts and other pathogenic fungi. In vitro Ketazol is fungicidal and, therefore, suppresses the formation of mycelia. In vivo, at therapeutic levels, however, it is primarily fungistatic. Ketazol acts in the case of C. albicans by inhibiting lanosterol demethylation in the biosynthesis of ergosterol, resulting in cell membrane defects. Mean peak plasma levels of approximately 3,5 mg/mL are reached within 1 - 2 hours following oral administration of a single 200 mg dose taken with a meal. Subsequent plasma elimination is biphasic with a rapid elimination phase with a half-life of 2 hours, followed by a slower elimination phase with a half-life of 8 hours. Following absorption from the gastro-intestinal tract, ketoconazole is converted into several inactive metabolites. The major identified metabolic pathways appear to be oxidation and degradation of the imidazole and piperazine rings, oxidative O-dealkylation and aromatic hydroxylation. Concentrations of active drug in the urine is very low. The major route of excretion is through the bile into the faeces. In vitro, the plasma protein binding is about 99%, mainly to the albumin fraction. Only a negligible proportion of ketoconazole reaches the cerebrospinal fluid. Ketoconazole is a weak dibasic agent and thus requires acidity for dissolution and absorption. INDICATIONS: Treatment of superficial and deep mycoses: • Systemic mycotic in Aqra d-dokument sħiħ