Miconazole - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antifungal means

Included in the formulation

Ginezole 7®

suppositories the vagina.

BAYER, AO Russia

Mikozone®

cream externally

Agio Pharmaceuticals Ltd. India

АТХ:

D.01.A.C Imidazole derivatives

Pharmacodynamics:

Inhibition of sterol-14-demethylase fungal cells: a violation of the synthesis of ergosterol involved in the construction of membranes of fungi; violation of dense packing of hydrocarbon chains of phospholipids, necessary for normal functioning of membrane proteins, including adenosine triphosphatases and respiratory chain enzymes. AT C. albicans - inhibition of the transformation of blastophores into an invasive mycelium.

Pharmacokinetics:

It penetrates well into the stratum corneum of the epidermis and remains in it until 4 days. Absorption from the skin is less than 1%, with a vagina of less than 1.3%. The connection with plasma proteins is more than 90%. Biotransformation in the liver to inactive metabolites. Half-life 24 hours. It is excreted by the kidneys (10-20% in the form of metabolites) and with feces (up to 50% unchanged). It is poorly removed during hemodialysis.

Indications:

Inside: candidiasis of the oral cavity (prevention and treatment in cancer patients receiving radiation or chemotherapy), candidiasis of the pharynx, candidiasis of the gastrointestinal tract.

Outwardly: dermatomycoses caused by fungi that are sensitive to the drug (including with secondary infection by Gram-positive microorganisms).

Intravaginal: vaginal and vulvovaginal candidiasis (including in pregnant women, nystatin is more effective, all imidazoles are comparable in effectiveness), superinfection caused by gram-positive microorganisms, fungal balanitis.

ICD-10

I.B35-B49.B35 Dermatophytosis

I.B35-B49.B35.1 Mycosis of nails

I.B35-B49.B35.6 Epidermophytosis inguinal

I.B35-B49.B37.3 Candidiasis of the vulva and vagina (N77.1 *)

I.B35-B49.B37.2 Candidiasis of skin and nails

I.B35-B49.B37.0 Candidiasis stomatitis

I.B35-B49.B37 Candidiasis

I.B35-B49.B49 Mycosis, unspecified

XIV.N70-N77.N76 Other inflammatory diseases of the vagina and vulva

XIV.N70-N77.N77.1 * Vaginitis, vulvitis and vulvovaginitis in infectious and parasitic diseases classified elsewhere

Contraindications:

Individual intolerance.

Hepatic and / or renal insufficiency.

Children under 12 years (for vaginal forms).

Pregnancy (first trimester).

Carefully:

Diabetes.

Disorders of microcirculation.

Pregnancy (II and III trimesters for vaginal forms).

Pregnancy and lactation:

The category of FDA recommendations is not defined. It is forbidden in the first trimester of pregnancy, with caution in the second and third trimester of pregnancy and with breastfeeding.

Dosing and Administration:

Inside 62 mg (¹/₂ dosage spoon) 4 times a day or lubricate the mouth and denture, leaving the gel for the night (keep in the mouth for as long as possible). Treatment continues for 4-5 days after the disappearance of clinical symptoms.

Outwardly the cream is applied 2 times a day until the symptoms disappear completely and for several consecutive days to prevent recurrence; with onychomycosis - continuously for 3 months, with fungal lesions of the skin and fingernails stop - externally 2 times a day for 4-6 weeks.

Intravaginally one candle (100 mg, 200 mg) at night, deep into the vagina. After the disappearance of the symptoms, treatment is continued for another 14 days.

Side effects:

Allergies (cross with all azoles), other anaphylactic, anaphylactoid and allergic reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria).

Nervous system: dizziness, headache, drowsiness.

Digestive system: nausea, vomiting, constipation, diarrhea, loss of appetite, abdominal pain, increased activity of aminotransferases, hepatitis, hepatic insufficiency, heart failure.

Local: itching, burning sensation in the vagina, rashes in the external genital organs; allergic reactions.

Overdose:

In case of an overdose, cardiopulmonary insufficiency may develop. Treatment is symptomatic.

Interaction:

Alprazolam, diazepam, midazolam, triazolam - increasing their concentration in the blood, strengthening and lengthening their sedative and hypnotic activity.

Alfentanil, eletriptan - decrease in their clearance.

Astemizole, pimozide, terfenadine, cisapride - increasing their concentration in the blood, lengthening the interval QT (sudden death due to arrhythmia is possible); concomitant use is contraindicated!

Buspirone - a significant increase in the concentration of buspirone in the blood.

Warfarin - strengthening of anticoagulant action.

Hydrochlorothiazide - decreased elimination by the kidneys, increased concentration in the blood (by 40%) and toxicity of fluconazole.

Hypoglycemic agents (sulfonylurea preparations, for example glibenclamide) - increasing their concentration in the blood, the development of hypoglycemia.

Carbamazepine, phenytoin, phenobarbital - reduction of miconazole in the blood, therapeutic inefficiency or exacerbation of the infection.

Macrolides (clarithromycin, erythromycin) - increased concentration and toxicity of miconazole, concomitant use is undesirable.

Polyene antifungal agents (including amphotericin B) - a decrease in the activity of polyene antibiotics.

Rifampicin - a decrease in the concentration of azoles in the blood, inefficiency, exacerbation of infection.

Tacrolimus, ciclosporin - increase of their toxicity.

Special instructions:

The use of suppositories with miconazole reduces the reliability of mechanical contraception (latex-containing drugs: condoms, vaginal diaphragms).

Instructions

Miconazole (Miconazolum)