Rumycoz, capsules 100mg, 6pcs

Composition

One capsule contains:

Active ingredient:

pellets of itraconazole – 464.00 mg,

itraconazole-100.00 mg,

sugar pellets (sucrose-80.0-91.5%, corn starch-8.5-20.0%, water-maximum 1.5%) – 207.44 mg,

poloxamer 188 (Lutrol) – 25.94 mg,

poloxamer 188 (Lutrol) micronized-0.51 mg,

hypromellose-130.11 mg.

Capsule shell composition:

body: titanium dioxide E 171, gelatin;

cover: titanium dioxide E 171, dye azorubin E 122, dye sunset yellow E 110, dye quinoline yellow E 104, dye iron oxide red E 172, dye iron oxide black E 172, gelatin.

Pharmacological action

Rumycosis is a broad-spectrum antifungal agent.

Pharmacodynamics

Synthetic broad-spectrum antifungal agent derived from triazole.

Inhibits the synthesis of ergosterol, which is an important component of the fungal cell membrane.

Active against dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast-like fungi and yeasts (Cryptococcus neoformans, Pityrosporum spp., Trichosporon spp., Geotrichum spp., Candida spp., including C. albicans, C. glabrata and C. krusei), Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatitidis, Pseudallescheria boydii, Penicillium marneffei, as well as other yeast and mold fungi.

Pharmacokinetics

Suction

When administered orally, the maximum bioavailability of itraconazole is noted when taking capsules immediately after a meal. Tmax in plasma is 3-4 hours after oral use.

The distribution

of Css of itraconazole in plasma 3-4 hours after taking the drug is 0.4 mcg / ml (when taking 100 mg once a day),1.1 mcg/ml (when taking 200 mg once a day) and 2 mcg/ml (when taking 200 mg twice a day). With prolonged use, Css is achieved within 1-2 weeks. Binding to plasma proteins is 99.8%.

Itraconazole penetrates well and is distributed in tissues and organs. The concentration of the drug in the lungs, kidneys, liver, spleen, bones, stomach, skeletal muscles is 2-3 times higher than the corresponding concentration in plasma. The accumulation of the drug in keratin tissues, especially in the skin, is approximately 4 times higher than the accumulation in plasma, and the rate of elimination depends on the rate of regeneration of the epidermis. In contrast to the plasma concentration, which is not detectable as early as 7 days after discontinuation of therapy, the therapeutic concentration in the skin remains for 2-4 weeks after discontinuation of the 4-week course of treatment; in the vaginal mucosa-for 2 days after the end of the 3-day course of treatment at a dose of 200 mg once a day and for 3 days after the end of the 1-day course of treatment at a dose of 200 mg twice a day. The therapeutic concentration of the drug in nail keratin is determined 1 week after the start of treatment and persists for 6 months after the completion of a 3-month course of therapy. Itraconazole is also detected in the secretions of the sebaceous and sweat glands.

Metabolism

It is metabolized in the liver with the formation of active metabolites, one of which — hydroxyitraconazole — has an antifungal effect comparable to itraconazole in vitro.

Deduction

Elimination from plasma is two-phase with a final T1/2 — 24-36 hours.

Excretion in the faeces is from 3 to 18% of the dose, 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 special clinical cases

In patients with renal insufficiency, as well as some patients with impaired immunity (for example AIDS, post-organ transplantation, neutropenia) the bioavailability of itraconazole may decrease. In patients with cirrhosis of the liver, the bioavailability of itraconazole is reduced, T1 / 2 is increased.

Indications

• dermatomycosis;
• fungal keratitis;
• onychomycosis caused by dermatophytes and / or yeast and mold fungi;
• systemic mycoses:
• systemic aspergillosis and candidiasis;
• cryptococcosis, including cryptococcal meningitis (patients with immunodeficiency and patients e cryptococcosis of the Central nervous system Rumiko® should be administered only in cases where drugs are the first line of treatment is not applicable or not effective);
• histoplasmosis;
• sportress;
• paracoccidioidomycosis;
• blastomycosis;
• other system or tropical mycoses;
• kandidomikoz with skin lesions and mucous membranes, including vulvovaginal candidiasis;
• deep visceral candidiasis;
• pityriasis versicolor.

Use during pregnancy and lactation

In pregnant women, Rumycoz® should only be prescribed in life-threatening cases, if the expected benefit to the woman exceeds the potential risk to the fetus.

When prescribed during lactation, it is necessary to stop breastfeeding.

Contraindications

• individual hypersensitivity to the drug or its components;
• simultaneous use of the following drugs with Rumycoz® :
• drugs metaboliziruemami enzyme CYP3A4, which may increase the QT interval(terfenadine, astemizole, mizolastine, cisapride, dofetilide, quinidine, pimozide, levomethadone, sertindole);
• inhibitors of HMG-COA reductase that cleaves the enzyme CYP3A4 (simvastatin, lovastatin);
• midazolam and triazolam (oral);
• preparations of ergot alkaloids (dihydroergotamine, ergometrine, ergotamine and methylergometrine).

With caution:  children; severe heart failure; liver diseases (including those accompanied by liver failure); chronic renal failure.

Side effects

From the gastrointestinal tract:  dyspepsia, nausea, vomiting, decreased appetite, abdominal pain, diarrhea, constipation.

From the side of the hepatobiliary system:  reversible increase in the activity of hepatic transaminases, hepatitis; very rarely-severe toxic liver damage, including acute liver failure with a fatal outcome.

Nervous system disorders:  headache, dizziness, peripheral neuropathy.

Allergic reactions:  skin rash, pruritus, urticaria, angioedema, rarely-erythema multiforme (Stevens-Johnson syndrome).

From the side of the skin:  alopecia, photosensitivity.

Other services:  menstrual disorders, hypokalemia, edematous syndrome, congestive heart failure and pulmonary edema, hypercreatininemia, dark urine staining.

Interaction

DRUGS that affect the absorption of itraconazole

Drugs that reduce the acidity of gastric juice reduce the absorption of itraconazole.

DRUGS that affect the metabolism of itraconazole

Itraconazole is mainly broken down by the enzyme CYP3A4. When itraconazole is co-administered with rifampicin, rifabutin, phenytoin, carbamazepine, isoniazid, which are powerful inducers of CYP3A4, the bioavailability of itraconazole and hydroxyitraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. Concomitant use of Rumicose® with these drugs, which are potential inducers of liver enzymes, is not recommended.

Potent inhibitors of the CYP3A4 enzyme (e. g. ritonavir, indinavir, clarithromycin, erythromycin) may increase the bioavailability of itraconazole.

Effect of itraconazole on the metabolism of other drugs

Itraconazole can inhibit the metabolism of drugs broken down by the CYP3A4 enzyme. The result of this may be an increase or prolongation of their action, including side effects. After discontinuation of treatment with Rumycoz®, the plasma concentration of itraconazole decreases gradually, depending on the dose and duration of treatment (see “Pharmacokinetics”). This should be taken into account when discussing the inhibitory effect of itraconazole on concomitant medications.

Medications that can be prescribed simultaneously with Rumycoz® 

BCC is not recommended. In addition to the possible pharmacokinetic interaction associated with the common pathway of metabolism involving the enzyme CYP3A4, BCAAs may have a negative inotropic effect, which is enhanced when taken simultaneously with Rumycoz®.

Drugs that are recommended for simultaneous use to monitor their plasma concentrations, effects, and side effects. If necessary, the dose of these drugs should be reduced:

• oral anticoagulants;
• the HIV protease inhibitors (ritonavir, indinavir, saquinavir);
• certain anticancer drugs (the Vinca alkaloids, busulfan, docetaxel, trimetrexate);
• BPC, split by the enzyme CYP3A4 (verapamil and dihydropyridine derivatives);
• certain immunosuppressive agents (cyclosporine, tacrolimus, sirolimus (also known as rapamycin);
• some inhibitors of HMG-COA reductase that cleaves the enzyme CYP3A4 (atorvastatin);
• some corticosteroids (budesonide, dexamethasone, and methylprednisolone);
• other drugs: digoxin, carbamazepine, buspirone, was Alfentanil alprazolam, brotizolam, midazolam for/in the introduction, rifabutin, ebastine, reboxetine, Cilostazol, disopyramide, eletriptan, halofantrine, Repaglinide.

Interaction between itraconazole, zidovudine and fluvastatin was not detected.

There was no effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone.

In vitro studies have shown no interaction between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, Indometacin, tolbutamide, and sulfamerazine when binding to plasma proteins.

How to take, course of use and dosage

Inside, after eating.

Oral bioavailability of the drug may be reduced in some immunocompromised patients, such as patients with neutropenia, AIDS patients, or patients with organ transplants. In these cases, a doubling of the dose may be required. Onychomycosis caused by dermatophytes and / or yeast, mold fungi

Removal of itraconazole from the skin and nail tissue is slower than from plasma. Thus, the optimal clinical and mycological effect is achieved 2-4 weeks after the end of treatment for skin diseases and 6-9 months after the end of treatment for nail diseases.

Overdose

No data available.

Treatment:

in case of accidental overdose, gastric lavage should be performed within the first hour, if necessary, the appointment of activated charcoal. Itraconazole is not eliminated by hemodialysis.

There is no specific antidote to the drug.

Description

Capsules No. 0 are two-tone: the body is white, the cap is pink-brown. The contents of the capsules are spherical microgranules from light yellow to yellowish-beige in color.

Special instructions

Women of childbearing age who are taking Rumycoz® should use adequate contraceptive measures throughout the course of treatment until the first menstrual period occurs after its completion.

When studying the IV dosage form of itraconazole, a transient, asymptomatic decrease in the left ventricular ejection fraction was noted, which normalized until the next infusion of the drug.

Itraconazole was found to have a negative inotropic effect. Cases of heart failure associated with Rumycoz have been reported. Rumycoz®should not be used in patients with chronic heart failure or a history of this disease, unless the possible benefit significantly outweighs the potential risk.

BCAAs may have a negative inotropic effect, which may increase the similar effect of itraconazole; itraconazole may reduce the metabolism of BCAAs. Caution should be exercised when taking itraconazole and BCC at the same time.

In patients with renal insufficiency, the bioavailability of itraconazole may be reduced, which may require dose adjustment.

With low stomach acidity, the absorption of itraconazole is disrupted. Patients taking antacid medications (for example, aluminum hydroxide) are recommended to use them no earlier than 2 hours after taking Rumycoz®. Patients with achlorhydria or using H%^%2-histamine receptor blockers or proton pump inhibitors are recommended to take Rumycoz ® capsules with acidic drinks.

In very rare cases, when using the drug Rumycoz® severe toxic liver damage developed, including cases of acute liver failure with a fatal outcome.This occurred in patients who already had liver diseases, as well as in patients who received other drugs that have a hepatotoxic effect. Several such 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.

Treatment should be discontinued if neuropathy occurs, which may be associated with taking Rumycoz®capsules.

There are no data on cross-hypersensitivity to itraconazole and other azole antifungal drugs. Rumycoz ® capsules should be used with caution in patients with hypersensitivity to other azoles.

In patients with compromised immunity (AIDS, post-organ transplantation, neutropenia), an increase in the dose of Rumycoz®may be required.

Influence on the ability to drive vehicles and work with mechanisms. Not observed

Form of production

Capsules

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Itraconazole

Conditions of release from pharmacies

By prescription

Dosage form

Capsules