Itraconazole is a synthetic triazole antifungal drug, which inhibits the demethylase of fungal C14-A-ergosterol and reduces the synthesis of ergosterol (an essential component of fungal cell membrane). Itraconazole has a broad spectrum and can be used to treat fungal infections such as blastomycosis, aspergillosis, candidiasis and various superficial infections.
Pharmacology
Itraconazole works by the same mechanism as other azoles: itraconazole inhibits ergosterol synthesis mediated by P450 oxidase. Because it inhibits cytochrome P450, 3A4 and interacts with other drugs, the dose must be adjusted.
Usage and dosage
Itraconazole was approved in the United States in 1992 and is still widely used as an antifungal. Itraconazole (trade name: Sporanox) is available in a 100 mg capsule and oral suspension in a variety of generic versions. The usual dose is 100 to 400mg per day, which can be adjusted according to the type and severity of infection. Common side effects include nausea, vomiting, diarrhea, rash, and hypokalemia.
Hepatotoxicity
Transient mild to moderate elevation of serum transaminase levels occurs in 1% to 5% of patients. Most are asymptomatic and self-limited, and may even return to normal during continuous treatment. Clinically significant hepatotoxicity is rare. Liver damage usually appears within one to six months of taking the drug, with fatigue and jaundice. Elevated serum enzymes are usually cholestatic and hepatocellular in rare cases of severe hepatitis (acute liver failure). Immunohypersensitivity manifestations (rash, fever, and eosinophilia) are uncommon and the proportion of autoantibody formation is low. Recovery usually takes several weeks (typically 4 to 10 weeks) after drug withdrawal, and may be prolonged in some cases.
Injury mechanism
The mechanism of itraconazole leading to clinically significant hepatotoxicity is unknown. However, itraconazole may be related to its ability to alter sterol synthesis and inhibit P450 activity. Itraconazole is a potent inhibitor of CYP 3A4, and therefore can produce severe drug interactions that increase or decrease plasma levels of other drugs, thereby increasing their toxicity or altering their potency.
Medication hangover
Itraconazole is a relatively well tolerated drug, and its side effects are similar to those of other azoles.
It found elevated glutamic-pyruvic transaminase levels in 4% of patients taking itraconazole.
Congestive heart failure, which is "rare but at high risk of progression," occurs in less than 1 in 10,000 patients.
The preparation of cyclodextrin syrup used in oral liquid can cause diarrhea. Side effects can lead to more serious problems including: nausea, vomiting, abdominal pain, fatigue, loss of appetite, yellow skin (jaundice), yellow eyes, itching, dark urine.
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