ORUNIT CAPSULES 100MG

Active substance

Itraconazole

Composition

One capsule contains

Active substances:

Itraconazole - 100mg (in the form of pellets 22%)

Excipients:

Sugar granules, copolymer of methyl-, dimethylaminoethyl- and butyl methacrylate (Eudragit E-100), hydroxypropylmethylcellulose, polyethylene glycol.

The composition of the shell of the capsule:

Quinoline gelatin (E 104), patented blue V (E 131), diamond black (E 151), titanium dioxide (E 171), iron oxide yellow (E 172), gelatin, orange yellow (E 110).

Mechanism of action

Antifungal broad-spectrum drug, a derivative of triazole. Inhibits the synthesis of ergosterol cell membrane of fungi. It is active against dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), and yeast fungi Candida spp. (including Candida albicans, Candida glabrata, Candida krusei), mold fungi (Cryptococcus neoformans, Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecae spp., Cladosporium spp. spp. shepp, spp. spp. spp. spp. pepp.

Indications

• Dermatomycosis;
• Fungal keratitis;
• Onychomycoses caused by dermatophytes and / or yeasts and molds;
• Systemic mycoses, including systemic aspergillosis and candidiasis, cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, paracoccidioimicosis, blastomycosis;
• Candidomycosis with damage to the skin and mucous membranes, incl. vulvovaginal candidiasis;
• Visceral candidiasis;
• Pityriasis versicolor.

Contraindications

Hypersensitivity to the drug.

Side effects

On the part of the digestive system: often - dyspepsia, nausea, abdominal pain, constipation; possible anorexia, reversible increase in liver enzymes, cholestatic jaundice, hepatitis; in some cases - toxic damage to the liver, including case of acute liver failure with a fatal outcome.
On the part of the central nervous system and peripheral nervous system: possible headache, fatigue, dizziness, peripheral neuropathy.
On the part of the reproductive system: possible violations of the menstrual cycle.
On the part of the urinary system: hypercreatininemia, urine staining in a dark color.
Metabolism: edema, hyperkalemia.
Since the cardiovascular system: possible chronic heart failure and pulmonary edema.

Allergic reactions: itching, rash, urticaria, angioedema, Stevens-Johnson syndrome are possible.
Dermatological reactions: alopecia is possible.

Interaction

The simultaneous use of rifampicin, rifabutin and phenytoin, which are strong inducers of liver microsomal enzymes, is not recommended, since these drugs can significantly reduce the bioavailability of itraconazole and hydroxyitraconazole, which leads to a significant decrease in the effectiveness of the drug. Studies on the interaction of itraconazole with other inducers of hepatic enzymes, such as Carbamazepine, phenobarbital and isoniazid, have not been carried out, however, we can assume the development of a similar effect.

Since Itraconazole is mainly metabolized with the participation of CYP3A4 isoenzyme cytochrome P450, strong inhibitors of this enzyme (including ritonavir, indinavir, Clarithromycin and erythromycin) can increase the bioavailability of itraconazole.

Itraconazole can inhibit the metabolism of drugs that are biotransformed with the participation of the CYP3A4 isoenzyme. The result of this may be strengthening or prolongation of their action, incl. and side effects. After cessation of treatment, plasma concentrations of itraconazole decrease gradually, depending on the dose and duration of treatment.

Terfenadine, astemizole, mizolastine, cisapride, triazolam, midazolam (orally), dofetilide, quinidine, pimozide, metabolized by the CYP3A4 isoenzyme, HMG-CoA reductase inhibitors (simvastatin and catastrophins, and simovastin and catastrophins, and simovastin, can not be administered simultaneously with itraconazole.

Calcium channel blockers have a negative inotropic effect, which can enhance the similar effect of itraconazole; Itraconazole can reduce the metabolism of calcium channel blockers. Itraconazole should be used with caution simultaneously with calcium channel blockers.

Drugs, the use of which requires control of plasma concentrations: oral anticoagulants; HIV protease inhibitors (ritonavir, indinavir, saquinavir); some anticancer drugs (vinca pink alkaloids, busulfan, docetaxel, trimetrexate); calcium channel blockers, metabolized with the participation of the isoenzyme CYP3A4 (dihydropyridine and verapamil); some immunosuppressants (cyclosporine, tacrolimus, sirolimus); other drugs - Digoxin, carbamazepine, buspirone, alfentanil, alprazolam, brotizolam, rifabutin, methylprednisolone, ebastine, reboxetine.With simultaneous use with itraconazole, if necessary, the dose of these drugs should be reduced.

No interaction was found between itraconazole and zidovudine and fluvastatin.
No effect of itraconazole on the metabolism of ethinyl estradiol and norethisetron was noted.
In vitro studies have demonstrated a lack of interaction between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, Indomethacin, tolbutamide, and sulfamethazine when bound to plasma proteins.

How to take, the course of administration and dosage

For optimal absorption of the drug, it is necessary to take Orunit in capsules immediately after a meal.
Capsules should be swallowed whole.

Overdosage

Data overdose of the drug is not available.
Treatment: in case of accidental overdose during the first hour after taking the drug, it is necessary to do a gastric lavage, if necessary, to appoint activated charcoal.
Symptomatic and maintenance therapy is indicated.
Itraconazole is not excreted by hemodialysis. The specific antidote is not known.

Special notes

Itraconazole has a negative inotropic effect. Considering this, Orunit should not be prescribed to patients with chronic heart failure (including in history), except for cases where the expected benefit of therapy far exceeds the potential risk. This should take into account such factors as the severity of indications, dosing regimen and individual risk factors for the development of chronic heart failure (including the presence of coronary artery disease, valvular heart disease, COPD, renal failure).

At low acidity of the stomach, absorption of itraconazole is impaired. Patients receiving antacid preparations (for example, aluminum hydroxide) are recommended to take them no earlier than 2 hours after taking Irunin. For patients with achlorhydria or using histamine H2 receptor blockers or proton pump inhibitors, it is recommended to take Orunit capsules with soda.

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, as well as in patients who received other drugs with a hepatotoxic effect. In this regard, it is recommended to regularly monitor liver function in patients receiving itraconazole therapy.

In the event of the appearance of symptoms suggesting the development of hepatitis, incl. anorexia, nausea, vomiting, weakness, pain in the abdomen and darkening of the urine, you must immediately stop taking the drug and conduct a study of the function of the liver. Patients with elevated levels of liver enzymes or liver disease in the active phase should not be prescribed Orunit treatment unless the expected benefit justifies the risk of liver damage. In these cases, it is necessary to monitor the level of liver enzymes during treatment.

In the case of the development of neuropathy, which can be caused by oral administration of itraconazole, treatment should be discontinued.
There is no evidence of cross-hypersensitivity to itraconazole and other antifungal drugs derived from azole. Orunite capsules should be administered with caution to patients with hypersensitivity to other azoles.

Release form

The capsules are transparent, pink, with a blue cap.

Pharmacy sales terms

On prescription