Active Substance: Ketoconazole.
Overview
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This medicine contains an important and useful components, as it consists of
Ketoconazoleis available in the market in concentration
Ketoconazole
Hepatic impairment; monitor liver function regularly. Pregnancy, lactation. Predisposition to adrenocortical insufficiency. Discontinue treatment if there is persistent or worsening of liver enzyme elevation.
Candidiasis, Fungal infections, Pityriasis versicolor, Seborrhoeic dermatitis
Hypersensitivity; preexisting liver disease, porphyria. Concurrent use with cisapride, terfenadine or astemizole.
1-10% Nausea and vomiting (3-10%),Pruritus (2%),Abdominal pain (1%) <1% Alopecia,Headache,Dizziness,Hyperlipidemia,Somnolence,Fever,Chills,Bulging fontanelles,Depression,Gynecomastia,Diarrhea,Impotence,Thrombocytopenia,Leukopenia,Hemolytic anemia,Erythema multiforme,Orthostatic hypotension,Jaundice,Dyspepsia,Dysgeusia,Hepatotoxicity,Decreased platelet count,Xeroderma,Photophobia Potentially Fatal: Hepatotoxicity.
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Ketoconazole interferes w/ biosynthesis of triglycerides and phopholipids by blocking fungal CYP450, thus altering cell membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen peroxide.
Reduced absorption w/ antimuscarinics, antacids, H2-blockers, PPIs, sucralfate. Reduced plasma concentrations w/ rifampicin, isoniazid, efavirenz, nevirapine, phenytoin. May also reduce concentrations of isoniazid and rifampicin. May reduce efficacy of oral contraceptives. May increase serum levels of CYP3A4 substrates e.g. digoxin, oral anticoagulants, sildenafil, tacrolimus. Potentially Fatal: May potentiate and prolong sedative and hypnotic effects of midazolam and triazolam. Increased plasma levels and prolonged QT intervals of astemizole, cisapride, dofetilide, pimozide, quinidine and terfenadine which may lead to torsade de pointes. Increased risk of myopathy w/ HMG-CoA reductase inhibitors (e.g. lovastatin, simvastatin). Markedly increased plasma levels of nisoldipine. Increased risk of hyperkalaemia and hypotension w/ eplerenone. Increased risk of vasospasm potentially leading to cerebral ischaemia w/ ergot alkaloids (e.g. ergotamine, dihydroergotamine).
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