Table of Contents
What is Ketoconazole?
Ketoconazole is an active ingredient used for the treatment of blastomycosis and chromomycosis.
Ketoconazole’s brand name is Nizoral.
Mechanism of action (MOA)
Antifungal.
Therapeutic indications, uses and benefits of Ketoconazole
Treatment for Cushing syndrome.
Ketoconazole Dosage
Oral.
Contraindications
- Hypersensitivity, acute or chronic liver disease, pregnancy and lactation.
- Co-administration with: terfenadine, sertindole, astemizole, bepridil, disopyramide, halofantrine, levacetylmethadol, mizolastine, cisapride, dofetilide, quinidine, domperidone or pimozide, for risk of prolongation of the QTc interval.
- Concomitant with: triazolam, midazolam, simvastatin and lovastatin, ergot alkaloids (e.g. dihydroergotamine, ergometrine, ergotamine and methylergometrine), nisoldipine, eplerenone, irinotecan, everolimus.
Warnings and Precautions
- Risk of hepatotoxicity, monitor liver function at baseline (rule out liver disease) and during treatment stop for liver damage, anorexia, nausea, vomiting, fatigue, jaundice, abdominal pain or dark urine.
- Monitor adrenal function in patients with adrenal insufficiency, undergoing major surgery or intensive care, or with prolonged therapy with signs of adrenal insufficiency.
- Not recommended in children < 15 kg.
Liver failure
Contraindicated in acute or chronic liver disease.
Hepatotoxic.
To monitor hepatic function at the beginning and during the treatment and to interrupt before hepatic damage.
Interactions with Ketoconazole
- Decreased bioavailability (do not associate) by: rifampicin, rifabutin, carbamazepine, isoniazid, phenytoin.
- Absorption decreased by: gastric acid reducers, H2-antagonists, proton pump inhibitors.
- Increased bioavailability by: ritonavir.
- Monitor plasma level, toxicity effect of: oral anticoagulants, indinavir, saquinavir, vinca alkaloids, busulfan, docetaxel, erlotinib, imatinib, dihydropyridines, verapamil, cyclosporine, tacrolimus, rapamycin, atorvastatin, budesonide, fluticasone, dexamethasone and methylprednisolone, digoxin, carbamazepine, buspirone, alfentanyl, sildenafil, alprazolam, brotizolam, midazolam IV, rifabutin, trimetrexate, elastin, reboxetine, quetiapine, cilostazol, eleptriptan, fentanyl, repaglinide, solifenacin, tolterodine.
- Disulfiram effect with: alcohol.
Pregnancy
Induce oligo and sindactilia in rats, no studies have been carried out in pregnant women.
Breastfeeding
Ketoconazole is excreted in milk, so women undergoing treatment should not use breast-feeding.
Adverse reactions and side effects of Ketoconazole
Nausea, headache, diarrhea, abdominal pain, altered liver function.
⭐⭐⭐⭐⭐ VIDEO OF KETOCONAZOLE/NIZORAL (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: R9400W927I
ChemIDplus
DrugPortal
PubChem CID: 47576
NCI Thesaurus: C605