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Brand Name :
Nizoral
Synonyms :
ketoconazole
Class :
Antifungals
Brand Name :
Nizoral
Synonyms :
ketoconazole
Class :
Antifungals
Dosage forms and strengths
Tablet
200 mg
The recommended dose is 200 to 400 mg orally daily
The recommended dose is 600 to 800 mg orally daily
The recommended dose is 400 mg orally in a month
Dosage forms and strengths
Tablet
200 mg
Children below two years of age:
Safety and efficacy are not established
Children age ≥2 years:
The recommended dose is 3.3 to 6.6 mg/kg orally daily
Refer adult dosing
ketoconazole: they may diminish the serum concentration of antacids
ketoconazole: they may diminish the serum concentration of antacids
ketoconazole: they may diminish the serum concentration of antacids
ketoconazole: they may diminish the serum concentration of antacids
ketoconazole: they may diminish the serum concentration of antacids
when both drugs are combined, there may be an increased effect of nilotinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
Sucralfate may diminish the serum concentration of ketoconazole
rifabutin: they may diminish the serum concentration of ketoconazole
It may enhance the effect when combined with pemigatinib by affecting CYP3A4 metabolism
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be a reduced metabolism of abemaciclib
when both drugs are combined, there may be a reduced metabolism of erlotinib
the effect of ketoconazole is increased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
ketoconazole increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
ketoconazole increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
ketoconazole increases the effect of encorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
ketoconazole increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
ketoconazole increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
it increases the effect or level of palbociclib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it will increase the impact or level of regorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may increase the level of effectiveness through P-glycoprotein MDR1 efflux transporter
may increase the serum concentration
may diminish the serum concentration of antacids
This may increase the serum concentration when both drugs are combined
it increases the concentration of rilpivirine in the serum
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may enhance toxicity when combined with cholic acid by diminishing the elimination
it may enhance the risk of QTc prolongation when combined with amifampridine
when ajmaline is used together with ketoconazole, the risk or seriousness of QTc prolongation is enhanced
When encainide is used together with ketoconazole, this leads to a reduction in the encainide’s metabolism
increase the therapeutic effects of busulfan by inhibiting metabolism
when both drugs are combined, there may be a decreased metabolism of paclitaxel
has a synergistic effect over brentuximab vedotin by showing altered intestinal/hepatic CYP3A4 enzyme metabolism.
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
ketoconazole increases the effect of gefitinib by altering the intestinal/ hepatic CYP3A4 enzyme metabolism
it may increase the hepatotoxic effects of ketoconazole
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporteridarub
it increases the effect or level of finasteride by altering the intestinal/hepatic enzyme CYP3A4 metabolism
it may increase the toxicity of each other
the rate of metabolism of tocofersolan may be reduced with ketoconazole
the risk of QTc prolongation may be increased
ketoconazole has the potential to modify the metabolism of propoxyphene, resulting in increased levels of propoxyphene in the bloodstream
When ketoconazole is aided by hesperetin, it reduces hesperetin’s metabolism
it increases the effect or level of osimertinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the efficacy of sorafenib by altering the hepatic CYP3A4 enzyme metabolism
it increases by affecting the hepatic enzyme CYP3A4 metabolism
Actions and Spectrum:
Action: It works by blocking ergosterol biosynthesis, which is an essential component in the fungal cell membrane. It interferes with the stability of the fungal cell membrane and consequently makes it to break, so the death of the fungal cell occurs. The antifungal action is helps in treatment of several fungal skin infections.
Adverse Reaction
Frequency defined
1-10%
Abdominal pain (1%)
Pruritus (2%)
Nausea and vomiting (3-10%)
<1%
Hyperlipidemia
Dizziness
Headache
Alopecia
Black Box Warning
Hepatotoxicity
Contraindication/Caution:
Hypersensitivity
Pre-existing liver disease
Pregnancy and breast-feeding
Drug interactions
Pregnancy/Lactation
Pregnancy warnings:
Pregnancy category: C
Lactation: Excreted into human milk is known
Pregnancy Categories:
Pharmacology: Ketoconazole is an antifungal medication.
Pharmacodynamics:
It works through interfering the synthesis of ergosterol; this is an element that is needed for formation of cell walls of fungi. Its specificity is on one enzyme known as lanosterol 14α-demethylase that is involved in the conversion of lanosterol to ergosterol. Ketoconazole interferes with the proper formation and function of the fungal cell membrane by inhibiting this enzyme, which ultimately causes the fungal demise.
Pharmacokinetics:
Absorption
The drug absorption is rapid.
After taken oral form, peak plasma concentration is usually obtained in one to two hours.
Distribution
Ketoconazole protein binding is 93-96%.
Metabolism
The drug metabolism occurs in liver.
Excretion and Elimination
The terminal half-life is two to eight hours.
Most of the drug is excreted through feces 57% and minor through urine 13%.
Administration:
The tablet form of the drug is taken orally.
Patient information leaflet
Generic Name: ketoconazole
Why do we use ketoconazole?
Ketoconazole is used in treating yeast infections like oral candidiasis.
Ketoconazole is used in treating cushing syndrome but used as off-label in this instance.
It is also used in treatment of systemic mycoses.
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