ميكونازول

BRAND NAMES:

Monistat 1 combination pack – It contains the active ingredients of miconazole. It is available in the forms of miconazole nitrate vaginal insert and miconazole nitrate vaginal cream 2%. It is used to cure most vaginal infections and relieves associated external itching and irritation.

Monist 7 -It contains the active ingredient of miconazole. It is available in the form of miconazole nitrate vaginal cream with 2% used to treat fungal infections.

Rash relief antifungal - It contains the active ingredients of miconazole nitrate, dimethicone, and petrolatum. It is available in the form of a spray used to treat jock itch, Ringworm, and athlete's foot.

Fungoid– It contains the active ingredients isoconazole nitrate and diflucortolone valerate. It is available as a cream for the treatment of fungus-related skin infections.

MECHANISM OF ACTION:

The primary mechanism of action is inhibition of the CYP450 14α-lanosterol demethylase enzyme, which results in altered ergosterol production and impaired cell membrane composition and permeability. This leads to caution phosphate and low molecular weight protein leakage.

PHARMACOKINETICS:

Absorption: Topical miconazole is poorly absorbed into the systemic circulation. Patients treated with a vaginal 1200 mg ovule had a mean Cmax of 10.71 ng/ml and a mean Tmax of 18.4 hours.

Distribution: A 100 mg vaginal cream provided an apparent volume of distribution of 10 911 L, whereas a 1200 mg miconazole vaginal suppository produced an estimated apparent volume of distribution of 95 546 L. 

Metabolism: Miconazole is metabolized in the liver but does not produce any active metabolites.

Excretion: Miconazole is eliminated in urine and feces; less than 1% of the unmodified drug is retrieved in urine.

PHARMACODYNAMICS:

Miconazole is an azole antifungal that works primarily by inhibiting a particular demethylase in the CYP450 complex. Patients who use intravaginal miconazole medications are advised not to rely on contraception to prevent pregnancy or sexually transmitted illnesses, and not to use tampons simultaneously. Miconazole is primarily used topically and is minimally absorbed into the systemic circulation after administration, hence the majority of patient reactions are limited to hypersensitivity and anaphylaxis.

DOSAGE AND ADMINISTRATION:

The topical dosage form is available in spray, cream, powder, and tincture with 2% miconazole.

Vaginal miconazole is available in the following dosage forms that are inserted into the vagina

• 2% and 4% vaginal cream

• 100mg, 120mg, and 1200mg of vaginal suppositories

A combination of 100mg, 200mg, or 1200mg of suppositories and 2% vaginal cream is also available.

Topical miconazole is available as a spray, spray powder, cream, powder, and tincture for application to the skin. It is normally administered twice daily. Topical miconazole is exclusively used on the skin. Do not let miconazole into your eyes or mouth, and do not ingest the drug. Miconazole is not effective on the scalp or nails.

Miconazole vaginal cream and suppositories are intended for use solely in the vagina. These products should not be taken by mouth. Vaginal suppositories are inserted once per dose in an applicator.

DRUG INTERACTIONS:

Drug interaction with miconazole may include

Anti-coagulant – warfarin, anisindione and dicoumarol

CONTRAINDICATIONS:

Contraindication of miconazole in individuals who have shown hypersensitivity to any of its ingredients.

Avoid contact with eyes.

SIDE EFFECTS:

Topical miconazole side effects may include

• Dry mouth

• Headache

• Sore tongue

• Tooth pain

• Itching

• Peeling

• Dry skin

• Redness of skin 

Vaginal miconazole side effects may include

• Increased burning

• Itching and

• Irritation of the vagina.

OVERDOSE:

If consumed, this medication might be hazardous. If an overdose victim exhibits life-threatening symptoms like unconsciousness or breathing difficulties.

TOXICITY:

A miconazole overdose has not been recorded. Patients who have overdosed are more likely to experience serious side effects such as headache, skin irritation, diarrhea, nausea, vomiting, stomach pain, and dysgeusia. Symptomatic and supportive measurements are recommended.