Ketoconazole


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult: PO Cushing's syndrome Initial: 400-600 mg daily, may be increased by 200 mg/day increments every 7-28 days if tolerated, according to patient's urinary free or plasma cortisol levels. Maintenance dose range: 600-800 mg daily. Max: 1,200 mg/day. All doses are given in 2 or 3 divided doses. Dose reduction or discontinuation may be required based on patient adrenal or liver function (refer to detailed product guideline). Systemic fungal infection In patients who have failed or who are intolerant to other therapies: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis: 200 mg once daily, may increase to 400 mg once daily if clinical response is not obtained. Continue treatment until fungal infection is resolved. Topical/Cutaneous Cutaneous candidiasis; Tinea corporis; Tinea cruris; Tinea manuum; Tinea pedis As 2% cream: Apply onto affected and immediate surrounding area 1-2 times daily. Duration of treatment: Yeast infections: 2-3 weeks; tinea cruris: 2-4 weeks; tinea corporis: 3-4 weeks; tinea pedis: 4-6 weeks. Pityriasis versicolor As 2% cream: Apply onto affected and immediate surrounding area 1-2 times daily for 2-3 weeks. As 2% shampoo: Treatment: Apply on wet scalp once daily for Max 5 days. Prophylaxis: Apply on wet scalp once daily for Max 3 days before exposure to sunlight. Seborrhoeic dermatitis As 2% cream: Apply 1-2 times daily on the affected area. Initial duration of treatment: 2-4 weeks. Maintenance treatment: Apply once weekly on affected area. As 2% shampoo: Treatment: Apply on wet scalp twice weekly for 2-4 weeks. Prophylaxis: Apply on wet scalp once every 1-2 weeks. Leave for 3-5 minutes then rinse thoroughly. Continue treatment until a few days after symptoms have resolved. As 2% foam: Apply on the affected area bid for 4 weeks. Dandruff As 2% shampoo: Treatment: Apply on wet scalp twice weekly for 2-4 weeks. Prophylaxis: Apply on wet scalp once every 1-2 weeks. Leave for 3-5 minutes then rinse thoroughly. Continue treatment until a few days after symptoms have resolved.
Administration
Should be taken with food.
Contraindications
Hypersensitivity. Concomitant use with CYP3A4 substrates (e.g. cisapride, dofetilide, dronedarone, quinidine, disopyramide, pimozide, sertindole, mizolastine, lurasidone, quetiapine, methadone, ranolazine, eplerenone, halofantrine, triazolam, alprazolam, midazolam, nisoldipine, felodipine, irinotecan, everolimus, sirolimus, paritaprevir/ombitasvir, saquinavir/ritonavir), HMG-CoA reductase (e.g. simvastatin, lovastatin), ergot alkaloids (e.g. ergotamine, ergometrine); colchicine, telithromycin, clarithromycin, fesoterodine and solifenacin. Acute or chronic hepatic impairment. Pregnancy (with Cushing syndrome) and lactation (oral).
Special Precautions
Patients with achlorhydria, prostate cancer, CNS infection, adrenal insufficiency; under prolonged stress (e.g. major surgery, intensive care). Children. Pregnancy and lactation (topical). Patient Counselling Oral: This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery. Topical: Avoid use of shampoo within 48 hours of applying hair dye, straightening or waving preparations. Avoid exposure to open flame or other source of ignition during or after application. Avoid contact with eyes and other mucous membrane. Monitoring Parameters Monitor LFT, bilirubin, adrenal function and QTc interval at baseline and at frequent intervals during therapy; serum Ca and phosphorus periodically (long-term use). Assess signs and symptoms of hepatotoxicity and hypocortisolism.
Adverse Reactions
Significant: Adrenal suppression, QT prolongation, bone fragility, abnormal LFTs, hypersensitivity reactions (e.g. anaphylaxis, angioedema). Blood and lymphatic system disorders: Thrombocytopenia. Eye disorders: Photophobia. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, dyspepsia, constipation, abdominal pain, flatulence. General disorders and administration site conditions: Asthenia, malaise, hot flush; topical: oily/dry hair, application site reactions (e.g. irritation, burning sensation, erythema, swelling). Hepatobiliary disorders: Jaundice, hepatitis. Immune system disorders: Urticaria. Investigations: Increased hepatic enzymes, decreased platelet count. Metabolism and nutrition disorders: Alcohol intolerance, anorexia, peripheral oedema. Musculoskeletal and connective tissue disorders: Myalgia, arthralgia. Nervous system disorders: Headache, dizziness, somnolence, dysgeusia, paraesthesia. Psychiatric disorders: Insomnia, nervousness. Reproductive system and breast disorders:Menstrual disorder, erectile dysfunction, azoospermia, gynaecomastia. Skin and subcutaneous tissue disorders: Pruritus, rash, alopecia, photosensitivity, dermatitis, xeroderma. Vascular disorders: Epistaxis, orthostatic hypotension.
Potentially Fatal:
 Hepatotoxicity e.g. hepatic necrosis, cirrhosis and failure or requiring liver transplantation.
Drug Interactions
Increased risk of hyperkalaemia and hypotension with eplerenone. Increased risk of hepatotoxicity and QTc interval prolongation with telithromycin and clarithromycin Increased risk of oedema and CHF with felodipine and nisoldipine. Increased risk of liver damage with paracetamol. May reduce absorption with antacids, antimuscarinics, PPIs, H2-receptor antagonists. May decrease plasma concentration with CYP3A4 inducers (e.g. rifampicin, rifabutin, carbamazepine, phenytoin, isoniazid, nevirapine, mitotane). May increase serum level with CYP3A4 inhibitors (e.g. ritonavir-boosted darunavir and fosamprenavir). May increase plasma concentrations of buprenorphine, alfentanil, fentanyl, oxycodone, digoxin, apixaban, warfarin, cilostazol, repaglinide, praziquantel, saxaliptin, isavuconazole, eletriptan, buspirone, aripiprazole, reboxitine, risperidone, midazolam (IV), maraviroc, indinavir, nadolol, verapamil, aliskiren, bosentan, domperidone, naloxegol, ciclosporin, budesonide, dexamethasone, fluticasone, sildenafil, vardenafil, cinacalcet, ibrutinib, busulfan, docetaxel, vinca alkaloids (e.g. vincristine, vinblastine). May increase risk of QTc interval prolongation with haloperidol, salmeterol, ebastine, pasireotide and tolterodine.
ATC Classification
J02AB02 - ketoconazole ; Belongs to the class of imidazole derivatives. Used in the systemic treatment of mycotic infections.
G01AF11 - ketoconazole ; Belongs to the class of imidazole derivative antiinfectives. Used in the treatment of gynecological infections.
D01AC08 - ketoconazole ; Belongs to the class of imidazole and triazole derivatives. Used in the topical treatment of fungal infection.
Disclaimer: This information is independently developed by CIMS based on ketoconazole from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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