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Ketoconazole information from DrugsUpdate  

See Available Brands of Ketoconazole in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Ketoconazole is a synthetic antifungal drug used to prevent and treat skin and fungal infections, especially in immunocompromised patients such as those with AIDS. Ketoconazole is sold commercially as an anti-dandruff shampoo, topical cream, and oral tablet, under the trademark name Nizoral by Johnson & Johnson. Ketoconazole is very lipophilic, which leads to accumulation in fatty tissues. The less toxic and more effective triazole compounds fluconazole and itraconazole have largely replaced ketoconazole for internal use. Ketoconazole is best absorbed at highly acidic levels, so antacids or other causes of decreased stomach acid levels will lower the drug's absorption when taken orally.

Pharmacodynamics

Pharmacokinetics

Ketoconazole interferes with biosynthesis of triglycerides and phopholipids by blocking fungal cytochrome P450, thus altering cell membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen peroxide.


Absorption Variably absorbed from the GIT (oral), may be increased with decreasing gastric pH. Minimally absorbed systemically (topical or vaginal). Peak plasma concentrations after 2 hr (oral).


Distribution Widely distributed, CSF (poor penetration); enters breast milk. Protein-binding: >90%, mainly to albumin.


Metabolism Hepatic; converted to inactive metabolites.


Excretion Via faeces (as metabolites and unchanged drug), via urine; 2 hr (initial half-life), 8 hr (terminal half-life).

Ketoconazole Indications / Ketoconazole Uses

Information Not Available

Ketoconazole Adverse Reactions / Ketoconazole Side Effects

GI disturbances e.g. nausea and vomiting; rash, dermatitis, burning sensation, pruritus; headache, dizziness, somnolence, fever and chills; thrombocytopenia; gynaecomastia, impotence; raised intracranial pressure; photophobia; transient elevations in LFTs. Potentially Fatal: Hepatotoxicity.

Precautions

Warnings When used orally, hepatotoxicity has been reported and included fatalities; use caution when coadministering with other hepatotoxic drugs. Monitor Measure LFTs before starting treatment and at frequent intervals during treatment.

Special Precautions

Hepatic impairment; monitor liver function regularly. Pregnancy, lactation. Predisposition to adrenocortical insufficiency. Discontinue treatment if there is persistent or worsening of liver enzyme elevation.

Other Drug Interactions

Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs, sucralfate. Reduced plasma concentrations with rifampicin, isoniazid, efavirenz, nevirapine or phenytoin. May reduce concentrations of isoniazid and rifampicin. May increase plasma concentrations of CYP3A4 substrates such as benzodiazepines, mirtazapine, nefazodone, tacrolimus, oral anticoagulants, rosiglitazone, sertindole, sildenafil. Disulfiram-like reaction with alcohol. May reduce efficacy of oral contraceptives. Potentially Fatal: Increased risk of cardiac arrhythmias with astemizole, cisapride, pimozide, quinidine or nilotinib. May reduce metabolism of conviptan; avoid concurrent usage. Increased risk of dofetilide toxicity when used together.

Other Interactions

Information Not Available

Dosage

Oral Fungal infections Adult: 200 mg once daily. Increase to 400 mg once daily if clinical response is insufficient. Treatment duration: 14 days and for at least 1 wk after symptoms have cleared and cultures have become negative. Child: ≥2 yr: 3.3-6.6 mg/kg daily as a single dose. Treatment duration: 1-2 wk for candidiasis; at least 4 wk in recalcitrnt dermatophyte infections and up to 6 mth for other systemic mycoses. Oral Chronic vaginal candidiasis Adult: 400 mg once daily for 5 days. Topical/Cutaneous Seborrhoeic dermatitis Adult: As 2% cream: Apply to the affected area bid for 4 wk or until clinical clearing. As 2% foam: Apply to the affected area bid for 4 wk. As 1 or 2% shampoo: Apply on the scalp twice wkly for 2-4 wk; continue for a few days until symptoms disappear. For prophylaxis: 2% shampoo is used once every 1-2 wk. Topical/Cutaneous Skin fungal infections Adult: As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine. Topical/Cutaneous Pityriasis versicolor Adult: As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine.

Food(before/after)

Should be taken with food.

List of Contraindications

Ketoconazole and Pregnancy

Caution when used during pregnancy. Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Ketoconazole and Lactation

Caution when used during lactation

Ketoconazole and Children

Cream/Shampoo 2%/Tablets Safety and efficacy not established. Foam/Gel/Shampoo 1% Safety and efficacy not established in children younger than 12 yr of age.

Ketoconazole and Geriatic

Information Not Available

Ketoconazole and Other Contraindications

Hypersensitivity; preexisting liver disease, porphyria. Concurrent use with cisapride, terfenadine or astemizole.

Storage

Oral Store at 15-25 ℃ (59-77 ° F). Topical/Cutaneous Store below 25 ℃ (77 ° F).

Lab interference

Oral Store at 15-25 ℃ (59-77 ° F). Topical/Cutaneous Store below 25 ℃ (77 ° F).

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