Be Careful When Using Antifungal Drugs Ketoconazole

Mushrooms are creatures commonly found on the skin. Hot and humid climate is the condition for the fungus to grow. When the skin is damaged or frequently wet or when the normal bacterial flora of the body is changed due to prolonged antibiotic treatment, fungi can proliferate causing dermatitis on the body especially those thin, damp skin.

Fungi can also cause infections of the lungs and other body tissues, especially in patients with weakened immune systems. When it is necessary to use antifungal drugs, the current choice is ketoconazole

. Currently, ketoconazole has many dosage forms such as oral tablets, creams, oral suspension, shampoos .. These are synthetic anti-fungal drugs that help prevent and treat fungal poisoning in general and on the skin, especially cases of immunocompromised patients such as AIDS patients.



Although newer antifungal drugs have fewer side effects, such as fluconazole and itraconazole, the mechanism of action is similar to that of ketoconazole. Ketoconazole usually works to suppress fungi but the drug can also kill fungi in high concentrations. The fungicidal effects of ketoconazole in high concentrations may be due to the direct physicochemical effects of the drug on the fungal cell membrane.
With Candida albicans, azol-type antifungals inhibit the transformation from shoot-conid spores to potentially invasive filaments. Ketoconazole is a broad-spectrum antifungal drug, effective on many fungal pathogens such as Candida, Blastomyces dermatitidis, Coccidioides immitis .. The drug also works on some gram-positive bacteria.




Ketoconazole is rapidly absorbed from the gastrointestinal tract, preferably at acidic pH. After oral administration, the drug dissolves in gastric juice and converts to hydrochloride salt and is absorbed in the stomach. The bioavailability of oral medications depends on gastric pH, increasing pH will reduce drug absorption, so if used concurrently with drugs that increase gastric pH will reduce absorption of ketoconazole.
The effect of food on the rate and extent of drug absorption in the stomach has not been clearly determined, but the manufacturer believes that taking ketoconazole with food will increase the level of drug absorption and make the concentration The drug in plasma is more concentrated, that is because food increases the speed and the solubility of the drug.
Maximum plasma concentration is achieved 1-2 hours after ingestion. Ketoconazole is distributed into inflamed joints, saliva, bile, urine, milk, tendons, skin, soft tissues, testes ...



The drug crosses the placenta but does not cross the blood-brain barrier, so it only reaches a certain amount. negligible in cerebrospinal fluid. Partially metabolized ketoconazole in the liver produces inactive derivatives through oxidation and degradation of imidazole and piperazole rings. The main pathway for elimination of drugs and its metabolites is via bile and faeces.

Ketoconazole is indicated in systemic mycosis, candidiasis of the skin, severe, chronic mucous membranes, persistent fungal infections of the vagina, fungal infections of the mouth, throat and stomach, intestines or other internal organs. Fungal infections of the body that choose the appropriate dosage form.
Ketoconazole can be toxic to the liver and should not be used by people with liver disease. Liver complications are more common in the elderly, women, alcoholics or impaired liver function due to other causes.




Because ketoconazole also has the ability to inhibit the synthesis of steroids and metabolism of vitamin D, so when prolonged treatment in children should be very careful.
Prolonged use of ketoconazole to prevent fungal diseases for immunocompromised individuals can cause serious hormonal changes.
Ketoconazole crosses the placenta, but there are no adequate human studies. The drug is only used for pregnant women when the benefits outweigh the risks that can be caused to the fetus. The drug can be secreted into milk, so mothers treated with ketoconazole should not breastfeed.
Some harmful effects

Unwanted effects (ADR) of ketoconazole common on the digestive system are nausea, vomiting, abdominal pain, constipation, flatulence, gastrointestinal bleeding, diarrhea. These effects are dose-related and can be minimized if taken with food. Most cases of hepatotoxicity have been reported in patients treated with onychomycosis and in others with chronic persistent skin fungus.



Although the toxic effects of ketoconazole on the liver can usually recover after a few months of drug discontinuation, rare rare cases of acute liver necrosis, hepatic fat changes or death have also occurred. If prolonged treatment is required, before taking the drug, it is necessary to perform liver function tests and during the treatment every 1 or 2 months, check at least once, especially patients who are taking other toxic drugs. Strong against the liver as anti-tuberculosis drugs, antibiotics.
When the results of the liver function test changes significantly, or the abnormality persists or worsens, or is accompanied by other manifestations of liver dysfunction, the drug should be discontinued. Ketoconazole may be taken with or after meals to reduce nausea and vomiting.
Because ketoconazole is highly toxic to the liver.

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