Ketoconazole Pharmacology


About Ketoconazole
Imidazole derivative, A broad spectrum Antifungal.
Mechanism of Action of Ketoconazole
Ketoconazole is fungicidal or fungistatic depending on concentrations. I t inhibits the conversion of Lanosterol to 14 demethyl Lanosterol by inhibiting the cytochromeP450 enzyme 14 alpha demethylase and impair ergosterol synthesis. This will alter cell membrane and its permeability. This will results in loss of intracellular components. It also inhibits biosynthesis of triglycerides and phospholipids by fungi. It also inhibits several enzymes (e.g. Oxidative and peroxidative enzymes) which are involved in detoxification process. This will leads to cellular necrosis.

Pharmacokinets of Ketoconazole
Absorption: It is absorbed only in acidic PH.Distribution: It is distributed in the body in protein bound form. Metabolism: It is metabolised to inactive metabolite in the liver. Excretion: It is excreted mainly through faeces and also through urine.
Onset of Action for Ketoconazole
Duration of Action for Ketoconazole
1 day
Half Life of Ketoconazole
8 hour.
Side Effects of Ketoconazole
8.Loss of hair
12.Psychiatric problems
Contra-indications of Ketoconazole
1.Hypersensitivity to Ketoconazole
Special Precautions while taking Ketoconazole
Hepatic dysfunction
Pregnancy Related Information
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Children Related Information
Above 2 years:use with caution
Below 2 years:contraindicated
NEONATES: contraindicated

Indications for Ketoconazole
1.Vaginal candidiasis
2. Oral thrush
9.Tinea pedis
10.Tinea corporis
11.Tinea cruris
12.Tinea vesicolor
13.Prostatic carcinoma
15. Seborrheic dermatitis
Interactions for Ketoconazole
Antacids & Histamine H2 antagonists: Increased gastric pH may inhibit ketoconazole absorption.
Isoniazid: The bioavailability of Ketoconazole may be decreased.
Rifampicin: Decreased serum levels of either drug may occur.
Oral anticoagulants: Anticoagulants response may be enhanced.
Corticosteroids: Bioavailability of corticosteroids increased and clearance may be decreased, resulting in possible toxicity.
Cyclosporine: Efficacy of cyclosporine enhanced leading to nephrotoxicity. May be used beneficially to reduce dose of cyclosporine in some patients.
Theophelline: Serum levels of theophylline may be decreased.
Alcohol: Nausea and acute facial flushing.
Typical Dosage for Ketoconazole
Adult: 200 - 400 mg once daily
Prostate carcinoma: 1.2 g in 3 divided dose.
For the treatment of Tinea infections apply once or twice daily on the affected part for 14 days.
Seborrheic dermatitis: apply Ketoconazole twice daily for 1 month
Dandruff: Apply for 60 seconds and rinse well. Reapply for 180 seconds. Apply twice weekly for 1 month
CHILDREN>2 years: 3.3 - 6.6 mg / kg body weight / day
For the treatment of Tinea infections apply once or twice daily on the affected part for 14 days.
For Tinea pedis, apply for 1 ? month.
Seborrheic dermatitis: apply Ketoconazole twice daily for 1 month

Schedule of Ketoconazole
Storage Requirements for Ketoconazole
The drug should be stored in room temperature. Keep away from moisture and sunlight.
Effects of Missed Dosage of Ketoconazole
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose and continue the regular schedule
Effects of Overdose of Ketoconazole
Give supportive measures and treatment. Induce emesis or gastric lavage has to be done followed by activated charcoal and a cathartic.

Home Delivery for Ketoconazole in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including ketoconazole.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for ketoconazole and other medicines and health products. Home delivery services for ketoconazole may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take ketoconazole only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for ketoconazole before they complete the sale. You can get this information while placing the order for ketoconazole with the pharmacy.

Ketoconazole is a generic medicine name and there are several brands available for it. Some of the brands for ketoconazole might be better known than ketoconazole itself. If the pharmacy that's willing to deliver medicines to your home doesn't have ketoconazole in stock, you can ask for one of the branded alternatives for ketoconazole.