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Pharmacotherapeutic Group: Gynaecological antiinfectives and antiseptics, excluding combinations with corticosteroids.
Combinations of imidazole derivatives.
Pharmacology: Pharmacodynamics: Metronidazole + Miconazole nitrate (METINDAZ FORTE) contains miconazole nitrate for antifungal and metronidazole for antibacterial and antitrichomonal effects. Miconazole nitrate which is a synthetic imidazole derivative antifungals has a wide spectrum of activity and is particularly effective against pathogen fungi including Candida albicans. In addition, miconazole nitrate is effective against Gram-positive bacteria. Miconazole shows its effect by inhibiting ergosterol synthesis in the cytoplasmic membrane. Miconazole nitrate changes the permeability of the fungal cell of Candida species and inhibits glucose utilization in vitro. Metronidazole, a 5-nitroimidazole derivative is an antiprotozoal and an antibacterial agent and is effective against several infections caused by anaerobic bacteria and protozoa, such as Trichomonas vaginalis, Gardnerella vaginalis and anaerobic bacteria including anaerobic Streptococci.
Pharmacokinetics: Absorption: Metronidazole: Bioavailability of metronidazole by this route is 20% compared to the oral route. Steady state levels of metronidazole in plasma ranged from 1.1 to 5.0 μg/mL after daily intravaginal application of Metronidazole + Miconazole nitrate (METINDAZ FORTE).
Miconazole nitrate: Absorption of miconazole nitrate by the intravaginal route is very low (approximately 1.4% of dose).
Following intravaginal application of Metronidazole + Miconazole nitrate (METINDAZ FORTE), miconazole nitrate was not detected in plasma.
Distribution: Metronidazole: It is widely distributed in body tissues and fluids including bile, bone, breast milk, cerebral abscesses, cerebrospinal fluid, liver and liver abscesses, saliva, seminal fluids and vaginal secretion, and achieves concentrations similar to those in plasma. It crosses the placenta and rapidly enters the fetal circulation. No more than 20% is bound to plasma proteins.
Distribution volume is 0.25-0.85 L/kg. Miconazole nitrate: The protein binding is 90%-93%. Its distribution to cerebrospinal fluid is poor; however, it is widely distributed to other tissues. Distribution volume is 1400 L.
Biotransformation: Metronidazole: It is metabolized in the liver by oxidation. The hydroxy metabolite is active. Major metabolites of metronidazole, hydroxy and acetic acid metabolites, are excreted in urine. The hydroxy metabolite has a 30% of biological activity of metronidazole.
Miconazole nitrate: It is metabolized in liver. Two non-active metabolites are found (2,4-dichlorophenyl-1 H imidazole ethanol and 2,4-dichloromandelic acid).
Elimination: Metronidazole: Half-life is equal to 6-11 hours. About 6%-15% of metronidazole dose is excreted with feces, 60%-80% is unchanged and excreted in urine as its metabolites. Approximately 20% of metronidazole is excreted in the urine as unchanged drug.
Miconazole nitrate: Half-life is equal to 24 hours. Less than 1% is excreted in the urine. Approximately 50%, usually unchanged, is excreted by feces.
