Oral treatment and prevention of fungal infections of the oropharynx and gastrointestinal tract, and of super infections due to Gram-positive bacteria.
Aural Anti-fungal preparations
Pharmacodynamics: Miconazole possesses an antifungal activity against the common dermatophytes and yeasts as well as an antibacterial activity against certain gram-positive bacilli and cocci. Its activity is based on the inhibition of a demethylation step in the ergosterol biosynthesis. Ergosterol, the end-product of the biosynthetic pathway and the main sterol in yeast and fungi. The disruption in production of ergosterol disrupts the fungal cell membrane, causing holes to appear in it. These holes allow the essential constituents of the fungal cells to leak out and ultimately the fungal cells die.
Pharmacokinetics: The oral bioavailability of Miconazole is low (25-30%) because there is little absorption of Miconazole from the intestinal tract. Miconazole is systemically absorbed after administration as the oral gel. Absorbed Miconazole is bound to plasma proteins (88.2%), primarily to serum albumin and red blood cells (10.6%). The absorbed portion of Miconazole oral gel is largely metabolized; less than 1% of the administered dose is excreted unchanged in the urine. The terminal plasma half-life is 20-25 hours in most patients. The elimination half-life of Miconazole is similar in any renal impaired patient.
For oral administration: Dosage is based on 15 mg/kg/day. Adults: 1-2 tea-spoonfuls of gel four times daily Children aged 6 years and over: One tea-spoonful of gel four times daily Children aged 2-6 years: One tea-spoonful of gel twice daily Infants under 2 years: Half tea-spoonful of gel twice daily. For localised lesions of the mouth: A small amount of gel may be applied directly to the affected area with a clean finger. For topical treatment of the oropharynx, the gel should be kept in the mouth for as long as possible. Treatment should be continued for up to 2 days after the symptoms have cleared. For oral candidasis, dental prostheses: Should be removed at night and brushed with the gel.
Concomitant treatment with Terfenadine, Astemizole and Cisapride should be avoided because in vitro studies suggest that Miconazole may inhibit their metabolism, so these products miqht precipitated.
Miconazole may delay Phenytoin and Cyclosporine metabolism and this might precipitate Phenytoin and Cyclosporine toxicity, respectively.
Miconazole is contraindicated in patients with known hypersensitivity to the active drug. If the concomitant use of Miconazole and anticoagulants is envisaged, the anticoagulant effect should be carefully monitored and titrated. It is advisable to monitor Miconazole and phenytoin levels, if they are used concomitantly. Particularly in infants and young children, caution is required to ensure that the gel does not obstruct the throat. Hence, the gel should not be applied to the back of the throat and the full dose should be divided into smaller portions. Observe the patient for possible choking.
Occasionally, nausea and vomiting have been reported, and with long term treatment, diarrhoea. In rare instances, allergic reactions have been reported. There are isolated reports of hepatitis, for which the causal relationship with Miconazole has not been established.
In animals, Miconazole has shown no teratogenic effects but is foetotoxic at high oral doses. The significance of this to man is unknown. However, as with other imidazoles, Miconazole Oral Gel should be avoided in pregnant women if possible. The potential hazards should be balanced against the possible benefits. It is not known whether Miconazole is excreted in human milk. Caution should be exercised when prescribing Miconazole Oral Gel to nursing mothers.
Accidental overdosage may cause vomiting and diarrhea. Treatment is symptomatic and supportive. A specific antidote is not available.
keep in a dry place away from light and heat. Keep out of the reach of children.
.png&w=384&q=75)