Orunit, capsules 100 mg 15 pcs

A broad spectrum antifungal agent, a triazole derivative. Inhibits ergosterol synthesis of the cell membrane of fungi.

It is active against dermatophytes (Trichophyton spp., Microsporum spp, Epidermophyton floccosum), yeast fungi Candida spp. (including Candida albicans, Candida glabrata, Candida krusei), molds (Cryptococcus neoformans, Aspergillus spp, Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis).

Indications

Active ingredient

Composition

One capsule contains

Active ingredients:

Itraconazole – 100mg (in pellet form 22%)

Associates:

Sugar granules,

Methyl-,

dimethylaminoethyl- and butyl methacrylate copolymer (Eudragit E-100),

hydroxypropyl methylcellulose,

polyethylene glycol.

Composition of the capsule shell:

Quinoline gelatin (E 104),

proprietary blue V (E 131),

brilliant black (E 151),

titanium dioxide (E 171),

iron oxide yellow (E 172),

gelatin,

orange yellow (E 110).

How to take, the dosage

For optimal absorption of the drug, Orunit capsules should be taken immediately after meals.

The capsules should be swallowed whole.

Interaction

The concomitant use with rifampicin, rifabutin and phenytoin, which are strong inducers of microsomal liver enzymes, is not recommended because these drugs can significantly reduce the bioavailability of itraconazole and hydroxyitraconazole, which leads to a significant reduction in the effectiveness of the drug.

The studies on interaction of itraconazole with other inducers of liver enzymes, such as carbamazepine, phenobarbital and isoniazid, were not conducted, however it is possible to assume the development of similar effect.

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

Itraconazole may inhibit the metabolism of drugs that are biotransformed with the participation of CYP3A4 isoenzyme. This may result in intensification or prolongation of their action, including side effects. After discontinuation of treatment plasma concentrations of itraconazole decrease gradually depending on the dose and duration of treatment.

Terfenadine, astemizole, misolastin, cisapride, triazolam, midazolam (oral), dofetilide, quinidine, pimozide, metabolized by CYP3A4 isoenzyme, HMG-CoA reductase inhibitors (simvastatin and lovastatin) should not be used concomitantly with itraconazole.

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

Drugs during the use of which it is required to control the concentrations in plasma: oral anticoagulants; HIV protease inhibitors (ritonavir, indinavir, saquinavir); some anticancer drugs (alkaloids of periwinkle pink, busulfan, docetaxel, trimetrexate); calcium channel blockers that are metabolized with the participation of CYP3A4 isoenzyme (dihydropyridine and verapamil); some immunosuppressants (cyclosporine, tacrolimus, sirolimus); other drugs – digoxin, carbamazepine, buspirone, alfentanil, alprazolam, brotizolam, rifabutin, methylprednisolone, ebastine, reboxetine.

In concomitant use with itraconazole the dose of these drugs should be reduced, if necessary.

No interaction between itraconazole and zidovudine and fluvastatin was found.

Itraconazole has not been observed to affect the metabolism of ethinylestradiol and norethisetron.

In vitro studies have demonstrated no interaction between itraconazole and such drugs as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamethazine when bound to plasma proteins.

Special Instructions

Itraconazole has a negative inotropic effect. Taking this into account, Orunit should not be administered to patients with chronic heart failure (including in anamnesis) unless the expected benefit of therapy significantly exceeds the potential risk. Such factors as severity of indications, dosage regimen and individual risk factors of chronic heart failure development (including CHF, heart valve lesions, COPD, renal failure) should be taken into consideration.

In low acidity of stomach the absorption of itraconazole is impaired. It is recommended to patients receiving antacids (e.g. aluminum hydroxide), to take them not earlier than 2 hours after taking Irunine. It is recommended to patients with achlorhydria or who use histamine H2-receptor blockers or proton pump inhibitors to take Orunit capsules with cola.

In very rare cases severe toxic liver injury including fatal acute liver failure has developed during itraconazole use. In most cases, this was observed in patients who already had liver disease, as well as in patients who received other drugs with hepatotoxic effect. In this regard it is recommended to monitor liver function regularly in patients treated with itraconazole.

In case of symptoms, suspected hepatitis development, including anorexia, nausea, vomiting, weakness, abdominal pain and darkened urine it is necessary to stop taking the preparation and immediately conduct liver function tests. Patients with elevated liver enzymes or liver disease in the active phase should not be treated with Orunit unless the expected benefit justifies the risk of liver damage. In these cases, liver enzymes should be monitored during treatment.

If neuropathy develops, which may be caused by oral administration of itraconazole, treatment should be stopped.
No data on cross-sensitivity to itraconazole and other antifungal drugs with azole derivatives. Orunit in capsules should be prescribed with caution in patients with hypersensitivity to other azoles.

Contraindications

Hypersensitivity to the components of the drug.

Side effects

Digestive system: often – dyspepsia, nausea, abdominal pain, constipation; anorexia, reversible increase in liver enzymes activity, cholestatic jaundice, hepatitis are possible; in individual cases – toxic liver damage, including acute liver failure with fatal outcome.

CNS and peripheral nervous system disorders: headache, fatigue, dizziness, peripheral neuropathy are possible.

From the sexual system: menstrual disorders are possible.

Urinary system disorders: hypercreatininemia, dark coloring of urine.

Metabolism disorders: edema, hyperkalemia.

Cardiovascular system: chronic heart failure and pulmonary edema are possible.

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

Dermatological reactions: alopecia is possible.

Overdose

There are no data on overdose of the drug.

Treatment: In case of accidental overdose gastric lavage should be performed within the first hour after taking the drug, if necessary – administration of activated charcoal.

Symptomatic and supportive therapy is indicated.

Itraconazole is not excreted by hemodialysis.

A specific antidote is not known.

Similarities