After oral application the maximum bioavailability of itraconazole observed when taking the capsules immediately after a meal.Time to maximum plasma concentration at 3-4 hours. The distribution equilibrium plasma concentration of itraconazole 3-4 hours after ingestion of 0.4 mg / ml (for receiving 100 mg once daily), 1.1 ug / ml (while taking 200 mg once a day) and 2.0 ug / ml (when receiving 200 mg twice a day).
Chronic testosterone propionate half life administration of the equilibrium concentration is achieved within 1-2 weeks. Relationship to plasma proteins -. 99.8% Itraconazole penetrates well and distributed in the tissues and organs. The concentration of drug in the lungs, kidneys, liver, spleen, stomach, bone, skeletal muscle 2-3 times greater than its concentration in plasma. The accumulation of itraconazole in keratinous tissues, particularly the skin, 4 times in the plasma, and depends on the rate of excretion of regeneration of the epidermis. In contrast, plasma concentrations that are not detectable after 7 days after stopping the treatment, the therapeutic itraconazole concentration in the skin is maintained for 2-4 weeks after stopping the 4-week course of treatment; in the vaginal mucosa – 2 days after 3 days of treatment at a dose of 200 mg per day and 3 days after the day course of treatment in a dose of 200 mg twice a day.
Therapeutic drug concentration in nail keratin determined 1 week after initiation of treatment and stored for 6 months after 3 months of therapy. Itraconazole is also determined in the secretion of sebaceous and sweat glands. Metabolism: It is metabolized testosterone propionate half life by the liver with the formation of active metabolites, one of which has a hydroxy-itrakonazol- comparable to itraconazole antifungal action-in vitro. Withdrawal Withdrawal from the plasma is biphasic with a terminal half-life of 24 – 36 hours.Elimination of the feces from 3 to 18% of the dose. Excretion by the kidneys – less than 0.03% of the dose. Approximately 35% of the dose is excreted as metabolites in the urine within 1 week.Pharmacokinetics in specific clinical situations in patients with renal failure, as well as in some patients with impaired immunity (e.g. in AIDS, organ transplantation, or in the case of neutropenia) bioavailability of itraconazole It may be reduced. In patients with cirrhosis the bioavailability of itraconazole reduced half-life is increased.
- fungal keratitis;
- onychomycosis caused by dermatophytes and / or yeasts and molds;
- systemic mycoses:
- systemic aspergillosis and candidiasis;
- cryptococcosis, including cryptococcal meningitis (immunocompromised patients and patients e cryptococcosis of the central nervous system testosterone propionate half life should be administered only in cases where the first-line treatment drugs do not apply in this case or not effective);
- other systemic or tropical mycoses;
- kandidomikoz with skin lesions and mucous membranes, including vulvovaginal candidiasis;
- deep visceral candidiasis;
Individual hypersensitivity to the drug or its components.
Concurrent with the preparation receive the following medicines:
- drugs metabolized by the enzyme, which may increase the interval (terfenadine, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide Levo, sertindole);
- inhibitors reductase, an enzyme cleavable testosterone propionate half life (simvastatin, lovastatin);
- midazolam and triazolam (oral);
- Ergot alkaloids medications (dihydroergotamine, ergometrine, ergotamine and methylene lergometrin).
Children’s age, severe heart failure, liver disease (including accompanied by liver failure), chronic renal failure.
Side effect On the part of the gastrointestinal tract: dyspepsia, nausea, vomiting, loss of appetite, abdominal pain, diarrhea, constipation. From the hepato-biliary system: a reversible increase in the activity of “liver” transaminases, hepatitis; very rarely – severe hepatotoxicity, including acute hepatic failure with a fatal outcome. From the nervous system: headache, dizziness, peripheral neuropathy. Allergic reactions: skin rash, pruritus, urticaria, angioneurotic edema, rarely – exudative erythema multiforme (Stevens-Johnson syndrome). With the skin: alopecia, photosensitivity. Other: menstrual disorders, hypokalemia, edema syndrome, congestive heart failure and pulmonary edema, giperkreatinemiya, staining of urine in a dark color.
No data. In case of accidental overdose, gastric lavage should be carried out within the first hour, designate activated carbon. Hemodialysis is not effective. There is no specific antidote.
Interaction with other drugs Drugs testosterone propionate half life affecting the absorption of itraconazole. Drugs that reduce gastric acidity reduces the absorption of itraconazole. Drugs affecting the metabolism of itraconazole.Itraconazole is mainly cleaved by the enzyme . In an application with rifampicin, rifabutin, phenytoin, carbamazepine, isoniazid, is a potent inducer enzyme, the bioavailability of itraconazole and hydroxy-itraconazole significantly reduced, which leads to a significant reduction in the effectiveness of the drug. Concomitant with these drugs, which are potential inducers of hepatic enzymes, it is not recommended.