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Nizoral is a synthetic antifungal drug given to treat several fungal skin infections like athlete's foot, ringworm, candidiasis which are hard to treat with other medications. It may also be prescribed for other conditions as determined by your doctor.

Brand: Ketoconazole

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: June 2024
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Nizoral 200 mg
270 pills - 200 mg
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$346.99 $1.29 $515.66 Add to cart
180 pills - 200 mg
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120 pills - 200 mg
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90 pills - 200 mg
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10 pills - 200 mg $31.95 $3.20 No Add to cart

Product description

Drug Title

Nizoral (Ketoconazole)

Pharmacological action

Antifungal agent. It has fungicidal and fungistatic action. The mechanism of action is inhibition of ergosterol synthesis and changes in lipid composition of the membrane. It is active against the causative agent of variegated lichen Malassezia furfur, causative agents of some dermatomycoses (Trichophyton, Epidermophyton floccosum, Microsporum), causative agents of candidiasis (Candida), as well as causative agents of systemic mycoses (Cryptococcus).

It is also active against Gram-positive cocci: Staphylococcus spp., Streptococcus spp.


Ketoconazole is a weak bivalent compound, which dissolves and is absorbed in an acidic environment. Cmax of ketoconazole in plasma is about 3.5 µg/ml and is reached 1-2 hours after a single oral dose of 200 mg with meal. Bioavailability of ketoconazole is maximal when taken with food. Absorption of ketoconazole is reduced in patients with decreased acidity of gastric juice, such as those taking antacids, such as aluminum hydroxide, and antisecretory drugs such as histamine H2-receptor blockers and proton pump inhibitors, as well as in patients with achlorhydria caused by a particular disease.

Binding to plasma proteins, mainly to the albumin fraction, is 99%. Nizoral (Ketoconazole) is widely distributed in the tissues, but only a small part of the drug penetrates into the cerebrospinal fluid.

After absorption from the gastrointestinal tract ketoconazole is metabolized in the liver with the formation of a large number of inactive metabolites.

In vitro studies have shown that CYP3A4 isoenzyme is involved in metabolism of ketoconazole. The main pathways of metabolism are oxidation and cleavage of imidazole and piperazine rings, oxidative O-dealkylation and aromatic hydroxylation. Ketoconazole is not an inducer of its own metabolism. Excretion from plasma is biphasic: during first 10 h T1/2 is 2 h, and 8 h thereafter.

About 13% is excreted with urine, of which 2-4% is unchanged. It is excreted mainly with bile in the gastrointestinal tract and about 57% is excreted with feces.

Contraindications to use

Acute and chronic liver diseases, pregnancy, lactation, children under 3 years of age, hypersensitivity to ketoconazole, concomitant use with the following CYP3A4 substrates (increase in plasma concentration of these drugs, caused by co-administration with ketoconazole, may increase or prolong both therapeutic and adverse effects and develop potentially dangerous effects, including prolongation of QT interval and development of ventricular arrhythmia of "pirouette" type): analgesics (levacetylmetadol, methadone); antiarrhythmics (disopyramide, dofetilide, dronedarone, quinidine); anthelmintic and antiprotozoal drugs (halofantrine); antihistamines (astemizole, misolastine, terfenadine) migraine medications (dihydroergotamine, ergometrine, ergotamine, methylergometrine); anticancer drugs (irinotecan); antipsychotics, anxiolytics and hypnotics (oral lurazidone, oral midazolam, pimozide, sertindol, triazolam) calcium channel blockers (bepridil, felodipine, lercanidipine,nisoldipine); cardiovascular drugs of different groups (ivabradine, ranolazine); diuretics (eplerenone); immunosuppressants (everolimus); gastrointestinal drugs (cisapride, domperidone); hypolipidemic drugs (lovastatin, simvastatin); other (colchicine in treatment of patients with liver and kidney disorders).

Administration during pregnancy and lactation

Contraindicated for use during pregnancy and lactation (breast-feeding).

Administration with liver dysfunction

Contraindicated in cases of severe hepatic impairment.

Usage in impaired renal function

Contraindicated in cases of marked impairment of renal function.

Indications of active substances of Ketoconazole DS

For oral administration (when other therapies are unavailable and intolerant): blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis.

Dosing regimen

For oral administration in adults and children weighing more than 30 kg - 200-400 mg/day. For children with body weight less than 30 kg - 4-8 mg/kg/day. It is taken 1 time/day with meals.