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.

Miconazole Nitrate oral gel is indicated-

• For the treatment of oral and gastrointestinal candidiasis.
• For eradication of fungal colonization in the mouth and gastrointestinal tract.
• For the treatment of super infections due to gram-positive bacteria.

Oropharyngeal candidosis-

• Infants 4-24 months: 1.25 ml (1⁄4 measuring spoon) of gel, applied 4 times day after meals.
• Adult and children 2 years of age and older: 2.5 ml (1⁄2 measuring spoon) of gel, applied 4 times a day after meals.

Gastrointestinal tract candidosis-

• Infants (4 months of age or above): Children and adults who have difficulty swallowing tablets: 20 mg per kg body weight per day, in four divided doses. The daily dose should not exceed 250 mg (10 ml gel) four times daily.

Missed Dose: Apply the missed dose as soon as you remember. In case of next dosing time, omit the missed

dose and continue your usual course.

Administration

In case of localized lesions of the mouth, a small amount of gel may be applied 2-4 times a day directly to the affected area with a clean finger. For best results, Miconazole oral gel should be kept in contact with the affected area as long as possible. The treatment should be continued for at least a week after symptoms have disappeared. For oral candidosis, dental prosthesis should be removed at night and brushed with the gel.

Miconazole is contraindicated in patients with known hypersensitivity to the active ingredient.

Occasionally nausea and vomiting, diarrhea with long term use and rarely allergic reactions.

Overdose Effects

Accidental overdosage may cause vomiting and diarrhea. Treatment is symptomatic and supportive. A specific antidote is not available.

If the concomitant use of Miconazole and anticoagulant is considered, the anti-coagulant effect should be monitored and titrated. Miconazole and phenytoin plasma level should also be monitored when used concomitantly. In infants and young children, caution must be taken to ensure that the gel does not obstruct the throat.

Pregnancy & Lactation

There is no information regarding the safety of Miconazole oral gel during pregnancy. So Miconazole oral gel should be avoided in pregnant women if possible or the potential hazards should be balanced against the possible benefits. As many drugs are excreted in human milk, caution should be exercised when Miconazole is administered to a nursing woman.