Last Updated on June 3, 2023
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Fluconazole
The active ingredient Fluconazole is a member of the azole antifungals, is therefore a means to treat fungal infections. He acts – as well as other members of this group – against a broad spectrum, so relatively many different types of infectious fungi. Here you can read more about the impact and use of Fluconazole, side effects and other interesting facts.
How Fluconazole works
Cholesterol is usually mentioned only in negative context: as blood lipid value that can “clog up” the receptacles. In certain amounts of cholesterol, however, is essential for the body. Among other things, it is an important component of the cell membrane. Without cholesterol and thus without a functioning membrane body cells could no longer meet many tasks.
The membrane of fungal cells comprising a block which is structurally related to cholesterol: the ergosterol (also called ergosterol). Without this substance, the fungal membrane loses its stability, and the fungus is no longer growing in a position. Azole antifungals such as Fluconazole inhibit a specific fungal enzyme (14-alpha-demethylase), which is involved in the production of ergosterol. The growth of the fungus is braked. Thus Fluconazole acts “fungistatic” (“fungal growth”).
Pharmacokinetics and metabolism of Fluconazole
After taking over her mouth Fluconazole is well absorbed through the intestinal wall into the bloodstream and reaches after half an hour and a half to the highest blood levels. The drug passes into all areas of the body, even in the brain and in skin and nails. It degrades only a small part of the body and mostly excreted unchanged in the urine. Approximately 30 hours after taking the blood levels of Fluconazole has fallen by half.
When is Fluconazole used?
The active ingredient Fluconazole is used to treat fungal infections. Examples include the infection of the oral, nasal and vaginal mucosa with the yeast Candida albicans, fungal skin infections (dermatomycosis) and the infection of the meninges with Coccidioides immitis(coccidioidomycosis, also known as known valley or desert fever).
The therapy with Fluconazole can also be done as a precaution to prevent in immunocompromised patients (re) fungal infection. This would, for example, transplant patients, cancer and HIV patients.
The treatment is usually carried out over a limited period as a developing resistance in fungi is not excluded. In individual cases, but may is also a long-term treatment with Fluconazole needed.
How Fluconazole is used
Fluconazole is often via the mouth (oral) administered, for example in the form of capsules. The dosage is determined individually and is often between 50 milligrams daily (or 150 milligrams per week) and 400 milligrams daily. In very severe cases, a Fluconazole dosage is possible up to 800 milligrams a day. Usually a double dose of Fluconazole is the first day of treatment taken to quickly achieve a high drug concentration in the body.
In some cases, the agent is administered directly into a vein (intravenously).
What are the side effects of Fluconazole?
In a step down from ten to one hundred patients treated side effects such as vomiting, rash, and an increase in liver enzymes in the blood.
Fluconazole side effects in an are from hundreds to thousands of patients anemia, decreased appetite, drowsiness, skin rash and itching.
What should I watch for while taking Fluconazole?
The active ingredient Fluconazole inhibits the liver specific drug-degrading enzymes (especially CYP2C9, CYP2C19 and CYP3A4). If other drugs administered concomitantly with Fluconazole, whose levels can rise significantly due to the reduced degradation and reach toxic (toxic) concentrations. Examples include the antiallergic agent terfenadine, pimozide (medicines for psychoses), antibiotics such as Erythromycin and certain agents against cardiac arrhythmias. Concomitant use should be avoided or require a dose adjustment. The latter is also in combination with other agents may be required:
- The antidepressants Amitriptyline and nortriptyline
- amphotericin B (another antifungal; it is combined may be applied in severe infections)
- anticoagulant such as warfarin and phenprocoumon
- sedatives like midazolam and triazolam
- remedy for epilepsy and seizures such as Carbamazepine and Phenytoin
- calcium channel blockers such as Nifedipine, Amlodipine, Verapamil (about high blood pressure and angina pectoris)
- very strong opioid painkillers like methadone, fentanyl and alfentanil
- cholesterol-lowering agents (statins) such as Atorvastatin and Simvastatin
- asthma medications such as Theophylline
- non-steroidal anti-inflammatory drugs (NSAIDs, commonly used as painkillers) such as Ibuprofen, Naproxen, Diclofenac
Pregnancy and lactation
The long-term and high-dose intake of Fluconazole during pregnancy can lead to damage in the development of the child. As a precaution, pregnant women should therefore only take in urgent cases under medical supervision shortly Fluconazole.
The active ingredient Fluconazole passes into breast milk, which is why when taking more than 200 milligrams should be discontinued (as a single dose).
Children and the elderly
In accordance with low-dose Fluconazole is also approved for the treatment of newborns, children and adolescents. In elderly and patients with kidney disease, the dose may need to be adapted to the renal function.
How to get Fluconazole
In Germany funds are with the drug Fluconazole in any dosage form and dosage prescription.
Since when Fluconazole is known?
The newer antifungals of the azole group were developed from about 1969th A major disadvantage of the first active ingredients of this group such as clotrimazole was that they could only be administered orally rather than by injection. Therefore, the pharmaceutical company Janssen Pharmaceutica developed in 1978 ketoconazole, which can be administered by injection, but is very toxic to the liver. Then developed based on its structure, the pharmaceutical company Pfizer, a new antifungal agent both orally and works very well by injection and well tolerated – in 1990 was the active ingredient Fluconazole issued its authorization
.