Itraconazole capsules 15 pcs

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Active ingredients

Itraconazole

Release form

Capsules

Composition

1 capsule contains: Active ingredient: Itraconazole 100 mg. Excipients: neutral pellets (sugar balls), sucrose, hypromellose-E (HPME-E), povidone K-30, propylene glycol 20 000, methyl, dimethylaminoethyl and butyl methacrylate copolymer (Eudragit E-100). The composition of the shell: methyl parahydroxybenzoate, propyl parahydroxybenzoate, gelatin, dye Ponso 4R (E124), dye sunsets yellow (E110), titanium dioxide (E171).

Pharmacological effect

Synthetic antifungal agent of a broad spectrum. The triazole derivative. Suppresses the synthesis of ergosterol cell membrane of fungi. Active against dermagofitov (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), and yeast fungi Candida spp. (paints, for details, for painters, for example, for paints, for paints, for paints, for example, for paints, for example, for paints, for example, for paints, for example, Cladosporium spp., Blastomyces dermatidis), Stalassezia spp. Some strains can be resistant: Candida glabrata, Candida krusei, Candida tropicalis, Absidia spp., Fusarium spp., Mucor spp., Rhizomucor spp., Rhizopus spp., Scedosporium proliferans, Scopulariopsis spp. The effectiveness of treatment is assessed after 2-4 weeks after cessation of therapy (for mycoses), after 6-9 months for onychomycosis (as nails change).

Pharmacokinetics

Absorbed from the gastrointestinal tract (GIT) quite fully. Taking itraconazole in capsules immediately after a meal increases bioavailability. Taking it in the form of a fasting solution leads to a higher rate of reaching Cmax and a higher concentration of the equilibrium phase (Css) as compared with taking after a meal (by 25%). The time to reach Cmax when taking capsules is about 3-4 hours. Css when taking 100 mg of the drug 1 time per day is 0.4 μg / ml; when taking 200 mg 1 time per day -1.1 mcg / ml, 200 mg 2 times per day - 2 mcg / ml. The time to reach Cmax when taking the solution is about 2 hours when taken on an empty stomach and 5 hours after eating. The time of occurrence of Css in plasma with prolonged use is 1-2 weeks. Communication with plasma proteins - 99.8%. It penetrates well into tissues and organs (including the vaginal mucosa) and is contained in the secretions of the sebaceous and sweat glands. The concentration of itraconazole in the lungs, kidneys, liver, bones, stomach, spleen, skeletal muscle is 2-3 times its concentration in plasma; in the tissues containing keratin - 4 times. The therapeutic concentration of itraconazole in the skin persists for 2-4 weeks after stopping the 4 week course of treatment. The therapeutic concentration in the keratin of the nails is achieved 1 week after the start of treatment and lasts for 6 months after the completion of the 3-month course of treatment. Low concentrations are found in the sebaceous and sweat glands of the skin. Metabolized in the liver to form active metabolites, including hydroxyitraconazole.It is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7. Removal from plasma is two-phase: by the kidneys for 1 week (35% in the form of metabolites, 0.03% in unchanged form) and through the intestine (3-18% in unchanged form). T1 / 2 - 1-1.5 days. Not removed during dialysis.

Indications

Mycoses of the skin, oral mucosa and eyes; onychomycosis caused by dermatophytes, yeast and mold fungi; candidiasis with lesions of the skin and mucous membranes, including vulvovaginal candidiasis; pityriasis versicolor; systemic mycoses, incl. aspergillosis (with resistance or poor tolerance to amphotericin B), cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, paracoccidioidomycosis, blastomycosis.

Contraindications

Hypersensitivity, chronic heart failure, incl. in the anamnesis (except for the treatment of life-threatening conditions); simultaneous use of CYP3A4 isoenzyme substrates that prolong the QT interval (astemizole, bepridil, cisapride, dofetilide, levacetylmethadol, mizolastine, pimozide, quinidine, sertnidol, terfenadine) HMG-CoA reductase inhibitors, metabolized by CYP3A4 isoenzyme (lovastatin, simvestatin); simultaneous oral administration of triazolam and midazolam, ergot alkaloids (dihydroergotamine, ergometrine, ergotamine, methylergotamine), nisoldipine, eletriptan; pregnancy, lactation.

Precautionary measures

Renal and hepatic failure, peripheral neuropathy, risk factors: chronic heart failure (ischemic heart disease, damage to the heart valves, severe lung disease, including chronic obstructive pulmonary disease, conditions associated with edematous syndrome), hearing loss, simultaneous reception of blockers slow calcium channels, children and old age.

Use during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Dosage and administration

Inside Immediately after the meal. Capsules are swallowed whole. Removal of the drug Itraconazole from the skin and nail tissue is slower than from plasma. Thus, optimal clinical and mycological effects are achieved 2-4 weeks after the end of treatment for skin infections and 6-9 months after the end of the treatment of nail infections.The duration of treatment can be adjusted depending on the clinical picture of treatment: for vulvovaginal candidiasis - 200 mg 2 times a day for 1 day or 200 mg 1 time a day for 3 days; with ringworms - 200 mg 1 time per day for 7 days or 100 mg 1 time per day for 15 days; lesions of highly keratinized skin areas (dermatophytosis of the feet and hands) - 200 mg 2 times a day for 7 days or 100 mg 1 time a day for 30 days; with pityriasis lichen - 200 mg 1 time a day for 7 days; for candidiasis of the oral mucosa, 100 mg 1 time per day for 15 days (in some cases, immunocompromised individuals may decrease the bioavailability of itraconazole, which sometimes requires a doubling of the dose); with keratomycosis - 200 mg 1 time per day for 21 days (the duration of treatment depends on the clinical response); with onychomycosis - 200 mg 1 time per day for 3 months or 200 mg 2 times per day for 1 week per course; with the defeat of the toenails (regardless of the presence of the defeat of the nails on the hands), 3 courses are conducted with an interval of 3 weeks. With the defeat of the nails only on the hands spend 2 courses with an interval of 3 weeks; elimination of itraconazole from the skin and nails is slow; optimal clinical response in cases of ringworm is achieved 2-4 months after the completion of treatment, onychomycosis - 6-9 months; with systemic aspergillosis - 200 mg / day for 2-5 months; with the progression and dissemination of the disease, the dose is increased to 200 mg 2 times a day; with systemic candidiasis - 100-200 mg 1 time per day for 3 weeks - 7 months, with the progression and dissemination of the disease, the dose is increased to 200 mg 2 times per day; with systemic cryptococcosis without signs of meningitis - 200 mg 1 time per day for 2-12 months. When cryptococcal meningitis - 200 mg 2 times a day for 2-12 months. treatment of histoplasmosis begins with 200 mg 1 time per day, maintenance dose - 200 mg 2 times a day for 8 months; with blastomycosis - 100 mg once a day, a supporting dose of 200 mg 2 times a day for 6 months; with sporotrichosis - 100 mg 1 time per day for 3 months; with paracoccidioidosis, 100 mg once a day for 6 months; with chromomycosis -100-200 mg once a day for 6 months; children are prescribed if the expected benefit outweighs the potential risk.

Side effects

From the gastrointestinal tract: dyspepsia (nausea, vomiting, diarrhea, constipation, loss of appetite),pain in the abdomen. From the side of the hepato-biliary system: a reversible increase in “liver” enzymes, hepatitis, in very rare cases with the use of Itraconazole, severe toxic liver damage developed, including cases of acute liver failure with a fatal outcome. From the nervous system: headache pain, dizziness, peripheral neuropathy. From the immune system: anaphylactic, anaphypactoid and allergic reactions. From the skin: in very rare cases - erythema multiforme (Stevens-Johnson syndrome), skin rash, pruritus, urticaria, angioneurotic edema, alopecia, svetochuvstvitelnost.Prochie: menstrual disorders, hypokalemia, edema syndrome, chronic heart failure and pulmonary edema.

Overdose

No data available. In case of accidental overdose, supportive measures should be taken. During the first hour, carry out a gastric lavage and, if necessary, prescribe activated charcoal. Itraconazole is not excreted by hemodialysis. There is no specific antidote.

Interaction with other drugs

1. Drugs that affect the absorption of itraconazole Drugs that reduce gastric acidity, reduce the absorption of itraconazole, which is associated with the solubility of the membranes of capsules. Drugs that affect the metabolism of itraconazole. Itraconazole is mainly metabolized by the CYP3A4 isoenzyme. The interaction of itraconazole with rifampicin, rifabutin and phenytoin, which are powerful inducers of the CYP3A4 isoenzyme, has been studied. The study found that in these cases, the inaccessibility of itraconazole and pyroxnitraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. The simultaneous use of itraconazole with these drugs, which are potential inducers of microsomal liver enzymes, is not recommended. Studies of interaction with other inducers of hepatic microsomal enzymes such as carbamazepine, phenobarbital and isoniazid not performed, but similar results can predpolozhit.Moschnye isoenzyme inhibitors of CYP3A4, such as ritonavir, indinavir, clarithromycin and erythromycin, can increase bioavailability itrakonazola.3. The effect of itraconazole on the metabolism of other drugs. Itraconazole may inhibit the metabolism of drugs cleaved by the CYP3A4 isoenzyme.The result of this may be an increase or prolongation of their actions, including side effects. Before you start taking concomitant medications, you should consult with your doctor about the metabolic pathways of this drug, indicated in the instructions for medical use. After cessation of treatment, concentrations of itraconazole in plasma decrease gradually, depending on the dose and duration. This should be taken into account when discussing the migratory effect of itraconazole on concomitant drugs. Examples of such drugs are: Drugs that cannot be prescribed simultaneously with itraconazole: - terfenadine, astemizole, mizolstine, cisapride, dofetilide, quinidine, pimozide, levacetylmethadol, sertindol, sertindol, levacetylmethatol, sertintol, of these drugs with itraconazole may cause an increase in the concentration of these substances in the plasma and increase the risk of prolongation of the QT interval and in rare cases the occurrence of me torsade des pointes; - inhibitors of HMG-CoA metabolized by the CYP3A4 isoenzyme, such as simvastatin and lovastatin; - midazolam for oral administration and triazolam; "Calcium channel - in addition to the possible pharmacokinetic interaction associated with the common metabolic pathway involving CYP3A4 isoenzyme, blockers of" slow "calcium channels can have a negative inotropic effect CT, which is enhanced when taken simultaneously with itraconazole. Preparations, the appointment of which is necessary to monitor their concentrations in plasma, action, side effects. In case of simultaneous administration with itraconazole, the dose of these drugs should be reduced if necessary - indirect anticoagulants; - HIV protease inhibitors, such as ritonavir, indinavir, saquinavir; - some anticancer drugs, such as the Vinca roseal alkaloids, busulfan, docetaxel, trimetrexate - CYP3A4 isoenzyme-blocking slow calcium channel blockers, such as verapamil and dihydropyridine derivatives; - some immunosuppressive drugs: cyclosporine, tacrolimus,sirolimus (also known as rapamycin); - some CYP3A4 isoenzyme-metabolized inhibitors of the substance of ancillary extracts of ancillary HMG-CoA such as atorvastatin; - some glucocorticosteroids, such as budesonide, dexamethasone, and methylprednisolone; intravenous midazolam, rifabutin, ebastine, reboxetine, cilostazol, disoliramnd, eletrnptan, halofatrin, repaglinide. Interaction between itraconazole and zidovudine and fluvastatin was not detected. The effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone was not observed.4. Effect on plasma protein binding. In vitro studies have demonstrated a lack of interaction between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide, and sulfamethazine when it binds to plasma proteins.

special instructions

- Women of childbearing age who take Itraconazole must use reliable methods of contraception throughout the entire course of treatment until the first menstruation begins. - Itraconazole has been found to have a negative inotropic effect. At the same time taking itraconazole and calcium channel blockers, which can have the same effect, care must be taken. Cases of chronic heart failure associated with taking itraconazole have been reported. Itraconazole should not be taken in patients with chronic heart failure or with the presence of this disease in history, except in cases where the potential benefits far outweigh the potential risk. In an individual assessment of the balance between benefits and risks, factors such as the seriousness of the indications, the dosing regimen and individual risk factors for the occurrence of chronic heart failure should be taken into account. Risk factors include the presence of heart disease, such as coronary heart disease or valve disease; serious lung diseases such as obstructive pulmonary lesions; renal failure or other diseases associated with edema. Such patients should be informed about the signs and symptoms of congestive heart failure.Treatment should be carried out with caution, and the patient should be monitored for symptoms of congestive heart failure. When they appear, it is necessary to stop taking Itraconazole. - At low acidity of the stomach: in this state, the absorption of Itraconazole from the capsules is impaired. Patients taking antacid preparations (for example, aluminum hydroxide) are recommended to use them no earlier than 2 hours after taking Itraconazole capsules. Patients with achlorhydria or using histamine H1 receptor blockers and proton pump inhibitors are recommended to take Itraconazole capsules with drinks containing cola. - In very rare cases, when Itraconazole was used, severe toxic liver damage developed, including cases of acute liver failure with a fatal outcome. In most cases, this was observed in patients who already had liver disease, in patients with other serious illnesses who received systemic therapy with Itraconazole, as well as in patients who received other drugs with a hepatotoxic effect. Some patients did not identify obvious risk factors for liver damage. Several of these cases occurred in the first month of therapy, and some in the first week of treatment. In this regard, it is recommended to regularly monitor liver function in patients receiving itraconazole therapy. Patients should be warned about the need to immediately contact their physician in the event of symptoms that suggest the occurrence of hepatitis, namely: anorexin, 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 the function of the liver. Patients with elevated concentrations of liver enzymes or liver disease in the active phase, or when toxic liver damage is tolerated while taking other drugs should not be given treatment with Itraconazole unless the expected benefit justifies the risk of liver damage. In these cases, it is necessary to control the concentration of “liver” enzymes during treatment. Liver dysfunction: itraconazole is metabolized primarily in the liver.Since the total half-life of itraconazole is slightly increased in patients with impaired liver function, it is recommended to monitor plasma concentrations of itraconazole and adjust the dose if necessary. Renal dysfunction: Because patients with renal insufficiency have a slightly increased half-life of itraconazole, concentration control is recommended Itraconazole in plasma and, if necessary, adjust the dose of the drug. - Patients with immunodeficiency: bio-dose If it is orally ingested, it can be reduced in some immunocompromised patients, for example, in patients with neutropenia, AIDS patients or organ transplants. Patients with systemic fungal infections that pose a life-threatening: Due to pharmacokinetic characteristics Itraconazole is not capsules It is recommended to start treatment of systemic mycoses that pose a threat to the lives of patients. - AIDS patients. - The attending physician should evaluate the need for a prescription. ivayuschey therapy to AIDS patients who have received prior treatment for systemic fungal infections such as sporotrichosis, blastomycosis, histoplasmosis or cryptococcosis (meningeal how and nemeningealnogo), in which there is a risk retsidiva.- Clinical data on the use of Itraconazole capsules in pediatric patients is limited. Itraconazole capsules should not be given to children, unless the expected benefit exceeds the possible risk. - Treatment should be stopped if peripheral neuropathy occurs, which may be associated with taking Itraconazole capsules. Impact on the ability to drive a car and work with appliances. Itraconazole may cause dizziness and other side effects that may affect the ability to drive vehicles and other equipment that requires increased attention when working.

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