Ketoconazole (When ATH D01AC08)

When ATH:
D01AC08

Characteristic.

White powder;, soluble in acids in. Molecular weight 531,44.

Pharmacological action.
Antifungal, fungistatic, fungicidnoe, anti-androgenic.

Application.

Mycosis of the skin, hair and nails, caused by dermatophytes and / or yeast (dermatophytoses, onixomikoz, kandidoznaja paronixija, pityriasis versicolor, folliculitis, trihofitii), gastrointestinal mycosis, mycosis eyes, juccuya, seborrheic dermatitis, caused Pityrosporum ovale, systemic mycosis (candidiasis, parakokcidiomikoz, histoplasmosis, coccidiomycosis, blastomycosis), hrybkovыy sepsis, vaginal candidiasis (acute and chronic recurrent); mycoses in immunocompromised patients (prevention).

Contraindications.

Hypersensitivity, acute liver disease, pregnancy, lactation.

Restrictions apply.

Reduced function of the adrenal cortex and pituitary, severe renal and hepatic failure, concomitant use of potentially hepatotoxic drugs, childhood (to 2 years).

Pregnancy and breast-feeding.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Side effects.

Decreased appetite, nausea, vomiting, diarrhea, abdominal pain, toxic hepatitis, increase in liver enzymes in the blood, jaundice, hepatitis (high mortality, the risk increases with the use of more 14 Nights), thrombocytopenia, headache, dizziness, drowsiness, paresthesia, photophobia, gynecomastia, decreased libido, impotence, oligospermatism, menstrual irregularities, hair loss, allergic reactions (hives, itching), arthralgia, fever; Local reactions - redness and irritation of the vaginal mucosa, itching of the vagina (suppozitorii); local skin irritation, burning, rash, contact dermatitis (cream, ointment); irritation, itching and burning of the skin, Increased oiliness or dryness of hair, hair loss (shampoo).

Cooperation.

It weakens the effect of amphotericin B. Incompatible with terfenadine, astemizolom, alcohol. Antacids, anticholinergics, H₂-blockers significantly reduce the absorption, rifampicin and isoniazid - concentration in the blood. It inhibits microsomal oxidation both prescribed drugs and increases their concentration, enhances the toxicity fenitonina. It reduces the stimulating effect on the adrenal corticotropin. Co-administration of oral contraceptives with low hormone levels cause breakthrough bleeding.

Dosing and Administration.

Inside, while eating, adults and children weighing more than 30 kg - for 200 mg 1 once a day, the ineffectiveness - 400 mg 1 once a day; children weighing from 15 to 30 kg - 100 mg 1 time. When prophylactic use in immunocompromised patients prescribed for adults 400 mg / day, Children - 4-8 mg / kg / day. Outwardly, cream or ointment applied to the affected areas 1 once a day. The shampoo is applied to the affected skin and hair, then after 3-5 minutes wash off with water. Intravaginal - By 1 supp. within 3-5 days. Treatment continues for at least a week after the disappearance of all symptoms of the disease.

Cooperation

Active substance	Description of interaction
Akarʙoza	FMR: synergism. Against the background of ketoconazole, retarding biotransformation, enhanced effect.
Algeldrat + Magnesium hydroxide	FKV. Slows absorption (the interval between doses should be at least 2 no).
Amphotericin B	FMR: antagonizm. Against the background of ketoconazole, retarding the synthesis of ergosterol (captures polyenes to the membrane of fungi), attenuated effect and increases the likelihood of emergence of resistant strains. Combination therapy should be administered with caution, especially in immunocompromised patients.
Atropyn	FKV. It reduces the acidity of gastric contents and slows absorption; should not be taken before 2 hours after ketoconazole tablets.
Biperiden	FKV. It reduces the acidity of gastric contents and slows absorption; should not be taken before 2 hours after ketoconazole.
Glimepiride	FMR: synergism. Against the background of ketoconazole, retarding biotransformation, enhanced effect.
Glipizide	FMR: synergism. Against the background of ketoconazole, retarding biotransformation, enhanced effect.
Digoxin	FKV. Against the background of increasing ketoconazole (sometimes) The plasma concentration (it needs monitoring).
Isoniazid	FKV. It reduces the concentration in the blood.
Ipratropiya bromide	FKV. It reduces gastric acidity and slows absorption; should not be taken before 2 hours after ketoconazole tablets.
Carbamazepine	FKV. FMR. Against the background of ketoconazole (inhibits CYP3A4) zamedlyaetsya biotransformation, increased plasma concentrations and increases the risk of toxic effects.
Clonazepam	FKV. Against the background of ketoconazole (CYP3A4 inhibitor) slows elimination; with a joint appointment caution.
Methylprednisolone	FKV. Against the background of ketoconazole (Inhibits CYP3A) slowing biotransformation and reduced clearance (toxic effects may occur).
Metformin	FKV. Against the background of ketoconazole, retarding biotransformation, enhanced effect.
Midazolam	FKV. FMR. Against the background of increasing with ketoconazolemax (more than 300%), AUC (almost 1500%), reduced plasma clearance, amplified and prolonged sedation.
Natriya carbonate	FKV. It inhibits the absorption; should not be taken before 2 hours after ketoconazole tablets.
Nevirapine	FKV. Significantly reduces the plasma concentration. Against the background of ketoconazole, inhibiting microsomal oxidation, significantly reduced the formation of hydroxylated metabolites. Combined use not recommended.
Omeprazole	FKV. It reduces the acidity of gastric contents and slows absorption.
Paclitaxel	FKV. Against the backdrop of slowing ketoconazole biotransformation.
Pioglitazone	FKV. In the presence of ketoconazole significantly inhibited the degradation (data in vitro).
Repaglinide	FKV. FMR. Against the backdrop of slowing ketoconazole biotransformation and increases the effect.
Rifampicin	FKV. It accelerates biotransformation and significantly reduces the concentration in the blood.
Rosiglitazone	FMR: synergism. Against the background of ketoconazole, retarding biotransformation, enhanced effect.
Siʙutramin	FKV. Against the background of ketoconazole (inhibits CYP3A4) zamedlyaetsya biotransformation, moderate increases in AUC and Cmax, reduced clearance.
Simvastatin	FKV. FMR. Against the background of ketoconazole (CYP3A4 inhibitor) zamedlyaetsya biotransformation, increased plasma levels and increases the risk of myopathy and rhabdomyolysis.
Fexofenadine	FKV. Against the backdrop of increased absorption of ketoconazole, slowing biotransformation and increases plasma levels.
Phenytoin	FKV. FMR. Against the background of ketoconazole (inhibits CYP3A4) zamedlyaetsya biotransformation, increased plasma concentrations and increases the risk of toxic effects.
Celecoxib	FKV. Against the background of ketoconazole (It inhibits CYP3A4) zamedlyaetsya biotransformation, increased plasma concentration; In sharing caution.
Cyclosporine	FKV. FMR. Against the background of ketoconazole (an inhibitor of CYP3A4) zamedlyaetsya biotransformation, increasing concentration in the tissues, It increases the likelihood of renal impairment.
Eʙastin	FMR. Against the background of ketoconazole (CYP3A4 inhibitor) biotransformation slows and increases the concentration in the blood; with a joint appointment (not recommended) It may prolong the QT interval.
Ethanol	FMR. Against the background of ketoconazole may cause reactions disulfirampodobnyh (redness and rashes, peripheral edema, nausea, headache and so on.).