Itrazole capsules 100mg N14
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Itraconazole
Release form
Capsules
Composition
Active ingredient: Itraconazole Concentration of active ingredient (mg): 100 mg
Pharmacological effect
Antifungal medication. Itraconazole is a broad-spectrum synthetic antifungal agent derived from triazole. It inhibits the ergosterol synthesis of the cell membrane of the fungus, which causes the antifungal effect of the drug. Itraconazole is active against the scientists, which has been established by the scientists, and that yeast-like fungi and yeast (Cryptococcus neoforus scientists), which grows by the scientists, the scientists, and the yeast-like fungi and the yeast (Cryptococcus neoforus scientists). including Candida albicans, Candida glabrata, Candida krusei), Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis, as well as other yeast spp.
Pharmacokinetics
Absorption Absorbed from the digestive tract quite fully. After ingestion, Cmax in the blood plasma is reached within 3–4 hours. Intake of itraconazole immediately after a meal increases bioavailability. Distribution During long-term administration, Css is reached within 1–2 weeks. Css itraconazole in plasma 3-4 hours after taking the drug is 0.4 μg / ml (100 mg when taken 1 time / day), 1.1 μg / ml (200 mg when taken 1 time / day) and 2 μg / ml (200 mg when taken 2 times / day. Binding to plasma proteins is 99.8%. Itraconazole penetrates well into tissues and organs (including the mucous membrane of the vagina), is contained in the secretions of the sebaceous and sweat glands. Concentrations in the lungs, kidneys, liver, bones, stomach, spleen and skeletal muscles were 2-3 times higher than the corresponding concentrations in plasma; in tissues containing keratin - 4 times. Therapeutic concentrations in the skin persist for 2-4 weeks after stopping the 4-week course of treatment. Itraconazole is detected in the keratin of the nails as early as 1 week after the start of treatment and lasts for at least 6 months after the completion of the 3-month course of therapy. Low concentrations of itraconazole are also determined in the sebum and sweat glands. Metabolism Itraconazole is metabolized in the liver to form active metabolites, including hydroxyitraconazole. It is an inhibitor of isoenzymes CYP3A4, CYP3A5, CYP3A7. Excretion plasma excretion is biphasic. Excretion with feces ranges from 3% to 18% of the dose (unchanged). It is also excreted by the kidneys for 1 week (0.03% - unchanged, 35% - as metabolites). T1 / 2 - 1-1.5 days. It is not removed during hemodialysis.
Indications
dermatomycosis, fungal keratitis, onychomycosis caused by dermatophytes and / or yeasts and wild mushrooms, systemic mycoses: systemic aspergillosis and candidiasis, cryptococcosis (including cryptococcal, coccal meningitis), histoplasmosis, sporotrichosis, paracoecidomas and isotropic mycosis. with damage to the skin or mucous membranes, including vulvovaginal candidiasis, pityriasis versicolor.
Contraindications
individual hypersensitivity to the drug or its constituent parts; simultaneous administration of drugs, is metabolized with the participation of the enzyme CYP3A4: terfazadin, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide, inhibitors of the MMC - CoA reductase, such as simvastatin and lovastatin, triazazin, triacidine, lysvastatin, triazazin, triactazine, lysvastatin, trizazin, trizazin, cizaprid, dofetilide, quinidine, pimozide, triactase, HMK - CoA, such as simvastatin and lovastatin, triazazin see also the section "Interaction with other drugs"); children's age up to 3 years; pregnancy; lactation period.
Precautionary measures
Do not exceed the recommended dose. The drug should be used with caution in patients with severe heart failure, in liver diseases (including those accompanied by liver failure).
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding). Women of childbearing age, taking Itrazole, you must use adequate methods of contraception throughout the course of treatment until the first menstruation after its completion.
Dosage and administration
Inside, after eating.
Side effects
On the part of the gastrointestinal tract: dyspepsia, nausea, abdominal pain and constipation, reversible increase in liver enzymes, cholestatic jaundice, hepatitis, anorexia. In very rare cases, when Itrazole was used, severe toxic liver damage developed, including a case of fatal liver failure; Co side of the central nervous system: headache, fatigue, dizziness, peripheral neuropathy; Since the cardiovascular system: congestive heart failure and pulmonary edema; From other organs and systems: menstrual disorders, allergic reactions (such as itching, rash, urticaria, and angioedema), Stevens-Johnson syndrome, alopecia, hypokalemia, edema, dark-colored urine staining, gilercreatininemia.
Overdose
Information about cases of overdose are absent.
special instructions
In the study of intravenous dosage forms of itraconazole, conducted on healthy volunteers, a transient asymptomatic decrease in the left ventricular ejection fraction was noted, normalized until the next infusion of the drug. The clinical significance of the data obtained for oral dosage forms is unknown. Itraconazole was found to have a negative inotropic effect. Cases of heart failure associated with taking itraconazole have been reported. The drug should not be prescribed to patients with heart failure or with the presence of this disease in history, except when possible benefits far outweigh the potential risk. Calcium channel blockers may have a negative inotropic effect, which can enhance the similar effect of itraconazole; Itraconazole can reduce the metabolism of calcium channel blockers. At the same time taking itraconazole and calcium channel blockers, caution should be exercised. At low acidity of the stomach, absorption of itraconazole is impaired. Patients receiving antacid preparations (for example, aluminum hydroxide) are recommended to use them no earlier than 2 hours after administration of Itrazole capsules. Patients with achlorhydria or using histamine H2 receptor blockers or proton pump inhibitors are recommended to take Itrazole capsules with acidic drinks. With long-term use of Itraconazole (more than 1 month), when using Itraconazole in patients receiving other drugs with a hepatotoxic effect, as well as Patients with liver disease are advised to regularly monitor liver function. Patients should be warned about the need to immediately contact their physician in the event of symptoms that suggest the occurrence of hepatitis, namely anorexia, nausea, vomiting, weakness, abdominal pain and dark urine. In the event of such symptoms, it is necessary to immediately discontinue therapy and conduct a study of liver function. Patients with renal failure in case of reduced bioavailability of itraconazole may require dose adjustment of the drug. Treatment should be stopped if neuropathy occurs, which may be associated with the administration of Itrazole capsules. hypersensitivity to itraconazole and other azole antifungal agents.Itrazol should be used with caution in patients with hypersensitivity to other azoles. Patients with impaired immunity (AIDS, after organ transplantation, neutropenia) may need to increase the dose. Use in pediatrics Use of the drug in children over 3 years is recommended only if there is a possible benefit treatment exceeds the potential risk. The effect on the ability to drive motor vehicles and control mechanisms The impact on the ability to drive and work with technology was not observed s