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How Ketoconazole Works As An Antifungal Agent

Ketoconazole is an antifungal agent. Mostly used in the form of creams and shampoos and is very effective against the common problems we face like fungal infections of the skin and foot, infections of the mucous membranes and infection of the scalp. Ketoconazole is basically or chemically a synthetic imidazole which is non-steroidal, which interferes with the synthesis of Ergosterol a component of the fungal cell membrane. Ketoconazole was previously the most prescribed oral medicine for fungal infections, but due to increasing hepatotoxicity, its use is now limited to local applications only. 

Ketoconazole is the best choice of prescribed medicine for skin infections by veterinarians. Ketoconazole was discovered and patented in the United States in the late 20th Century. Ketoconazole had ruled the market for about a decade among the top-selling antifungal agents but it was only that its oral administration was banned after incidences of serious side effects. Ketoconazole is still used as an active ingredient in skincare creams and shampoos and is very famous because of its easy availability and affordable market price.

Uses of Ketoconazole

Ketoconazole came into medical use in around 1970s from then it is available in the form of generic medicine and as a formulation for local applications. Ketoconazole is used as a first-line choice of antifungal agents for the treatment of skin and mucosal membrane infections, ringworm infections, candidiasis. Topical application for dandruff, ketoconazole cream for acne and dermatitis prevailing to other parts of the body.

Side effects of Ketoconazole administration

The side effects of Ketoconazole are more pronounced in the hormonal sector. Since ketoconazole blocks the synthesis of Ergosterol in fungi, in Humans high doses inhibit the conversion of cholesterol to steroid hormones like Testosterone, Estrogen, Cortisol. The fall in the level of steroid hormones in humans is directly linked to fertility in males and females. Normal sperm count and abnormal sperm morphology are among the most counted effects of low production of steroid hormones and in females, it hampers the menstrual cycle, maturation of oocytes and proper fertilization of gametes for pregnancy. 

Oral administration has severe contraindications. Combinational drug therapy has drug-drug interactions leading to liver diseases, adrenal insufficiency and hypersensitivity to oral ketoconazole. Over abuse of Ketoconazole causes vomiting, nausea, constipation, and anaphylaxis a hypersensitivity reaction to drugs and allergens.

Modern uses of Ketoconazole

Many other drugs have replaced Ketoconazole as the primary antifungal agent but it still remains as the second choice of a drug even after thirty years after its discovery. Ketoconazole is used in shampoos to treat infections of the scalp, as a ketonic skin cream. It is also a popular choice among the veterinarians for fungal infection treatment. Its oral administration is banned but the local application is highly popular due to cost-effectiveness and better results.


Even having a wide range of difficulties associated with its administration, it is still popular among physicians and dermatologists as a potent antifungal agent. The overdose of this drug can be reduced by administering activated charcoal within the initial hours. It is a pharmacologically active drug, with better action potentials in the acidic environment.

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