Ketoconazole-used to treat certain serious fungal infections in the body

Ketoconazole is an oral drug that's used to treat fungal infections.

Ketoconazole-used to treat certain serious fungal infections in the body

Ketoconazole; Panfungol; Nizoral; Orifungal M; Ketoderm

Abiket, Abket Soap, Apodruff, Arclone, Arcolane Scalp Soln, At-Last, Atron, Beetoc, Beetoc Shampoo, Beetoc Soap, Can, Can Tab, Can-Z, Clinhair, Clopeta-C, Clopeta-Z, Conaderm, Cotar-K, D-Keto, Danclear, Dancure, Dandcare,

1-[4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one

• Absorption: Oral
• Distribution: Above 90% protein binding
• Metabolism: Hepatic
• Excretion: Via urine and feces.

Ketoconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability. Other mechanisms may involve the interaction with membrane phospholipids, inhibition of endogenous respiration, inhibition of yeast transformation to mycelial forms, inhibition of purine uptake, and impairment of triglyceride and/or phospholipid biosynthesis. Ketoconazole can also inhibit the synthesis of thromboxane and sterols such as aldosterone, cortisol, and testosterone.

200 to 400 mg daily by oral. Topical formulation applied on the affected area once or twice a day.

For the treatment of candidiasis, oral thrush, chronic mucocutaneous candidiasis, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.

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.

• Increased risk of cardiac arrhythmias with astemizole, cisapride, pimozide, quinidine or nilotinib.
• Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs, sucralfate.
• May reduce concentrations of isoniazid and rifampicin.
• Reduced plasma concentrations with rifampicin, isoniazid, efavirenz, nevirapine or phenytoin.
• 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 metabolism of conviptan; avoid concurrent usage.
• May reduce efficacy of oral contraceptives.
• Increased risk of dofetilide toxicity when used together.

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

Store at 59-77 ° F (15-25 ?).

Molecular weight

531.431

Molecular formula

C26H28Cl2N4O4

CAS number

65277-42-1

Precautions

• Measure LFTs before starting treatment and at frequent intervals during treatment.
• Use caution when co administering with other hepatotoxic drugs.
• Monitor liver function regularly. 
• Discontinue treatment if there is worsening or persistent of liver enzyme elevation.
• Predisposition to adrenocortical insufficiency.
• Pregnancy, lactation.