Orungal - instructions for use, analogs, reviews and release forms (capsules or tablets 100 mg, solution or syrup for ingestion, ointment or cream) drugs for the treatment of fungal infections, candidiasis or thrush in adults, children and pregnancy

In this article, you can read the instructions for using the drug Orungal. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of experts on the use of Orungal in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Orungal Analogues in the presence of existing structural analogs.Use for the treatment of fungal infections, candidiasis or thrush in adults, children, as well as during pregnancy and lactation.

Orungal - broad-spectrum antifungal agent, triazole derivative. Inhibits the synthesis of ergosterol cell membrane of fungi, which causes the antifungal effect of the drug.

Itraconazole is active against infections caused by dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum); yeast-like and yeast fungi (Candida spp. (Candida), including Candida albicans, Candida glabrata and Candida krusei, Cryptococcus neoformans, Pityrosporum spp., Trichosporon spp., Geotrichum spp.); Aspergillus spp .; Histoplasma spp .; Paracoccidioides brasiliensis; Sporothrix schenckii; Fonsecaea spp .; Cladosporium spp .; Blastomyces dermatitidis; Pseudoallescheria boydii; Penicillium marneffei and others.

Candida glabrata and Candida tropicalis are the least sensitive to the effects of Itraconazole with Candida species.

The main types of fungi, the development of which is not inhibited by itraconazole, are Zygomycetes (Rhizopus spp., Rhizomucor spp., Mucor spp., Absidia spp.), Fusarium spp., Scedosporium spp., Scopulariopsis spp.

Composition

Itraconazole + excipients.

Pharmacokinetics

After ingestion, it is well absorbed. Absolute bioavailability of itraconazole when taking the drug with food is about 55%, with fasting, bioavailability increases by 30%. Most of itraconazole in plasma binds to proteins (99.8%), mainly with albumin (for the metabolite itraconazole - hydroxy-itraconazole, the protein is 99.6%). The affinity of itraconazole for lipids is also noted.Only 0.2% of itraconazole in plasma is unbound.

Itraconazole penetrates well into tissues, concentrations in the lungs, kidneys, liver, bones, stomach, spleen and muscles are 2-3 times higher than the corresponding concentrations in the plasma. The ratio of concentrations of itraconazole in brain tissues and plasma is approximately the same. The concentration of the drug in keratin tissues, especially in the skin, is about 4 times higher than the concentration in the plasma.

Itraconazole is biotransformed in the liver with the formation of a large number of metabolites. One of the metabolites, hydroxy-itraconazole, has an antifungal action comparable to that of itraconazole. The concentration of hydroxy-itraconazole in the plasma is almost 2 times higher than the corresponding concentrations of itraconazole.

From 3 to 18% of the administered dose is excreted with feces unchanged. Unchanged in the urine output is less than 0.03%. About 35% of the dose is excreted as inactive metabolites with urine and about 54% with feces.

Indications

Treatment of mycoses caused by susceptible pathogens, including:

• dermatomycosis;
• fungal keratitis;
• onychomycosis caused by dermatophytes and / or yeast and mold fungi;
• Systemic mycoses: systemic aspergillosis and candidiasis, cryptococcosis (including cryptococcal meningitis, in patients with immunodeficiency and in all patients with cryptocosis, the CNS Orungal should be prescribed only if the first-line drugs are not applicable or ineffective in this case), histoplasmosis, sporotrichosis, paracoccidioidomycosis, blastomycosis and other systemic and tropical mycoses;
• Candidomycosis with skin and mucous membranes (including vulvovaginal candidiasis);
• deep visceral candidiasis;
• pityriasis lichen;
• prevention of systemic fungal infections in patients with malignant blood diseases or in patients with bone marrow transplantation with a high probability of neutropenia (less than 500 cells / μl).

Forms of release

Solution for oral administration (sometimes mistakenly called syrup).

Capsules 100 mg (sometimes mistakenly called pills).

Other medicinal forms, whether it be ointment or cream for external use, do not exist.

Instructions for use and reception scheme

Solution

In the treatment of candidiasis of the oral cavity and / or esophagus, Orungal is prescribed 200 mg (2 measuring cups) per day in 1 or 2 doses for 1 week.In the absence of a positive effect after 1 week, the course of treatment should continue for another 1 week.

In the treatment of candidiasis of the oral cavity and / or esophagus, with resistance to fluconazole, 200-400 mg (2-4 cups) are prescribed per day in 1-2 doses for 2 weeks. In the absence of a positive effect after 2 weeks, treatment should continue for another 2 weeks.

For the prevention of systemic fungal infections, the drug is prescribed at a dose of 5 mg / kg of body weight per day in 2 divided doses. The drug is taken 1 week before the start of treatment with cytostatics or a week after the bone marrow transplantation and continues until the number of neutrophils is restored (at least 1000 cells / μl).

The solution should be taken orally, on an empty stomach. The solution should be rinsed and then swallowed. After this, do not rinse your mouth with water.

Capsules

Capsules should be taken immediately after meals, swallow whole.

Bioavailability of itraconazole for oral administration may be reduced in some patients with impaired immunity, for example in patients with neutropenia, AIDS patients or with transplant organs. Therefore, a double dose increase may be required.

One course of pulse therapy is a daily intake of 2 capsules Orungala 2 times a day (200 mg twice a day) for 1 week.

For treatment of fungal lesions of the nail plates of the brushes, 2 courses are recommended. For treatment of fungal lesions of the nail plates of the feet, 3 courses are recommended. The gap between the courses, during which you do not need to take the drug, is 3 weeks.

Clinical results will become apparent after the end of treatment, as the nail grows.

In addition to pulse therapy, a continuous course is possible. The drug is prescribed 2 capsules per day (200 mg once a day) for 3 months.

Elimination of Orungala from the skin and nail tissue is slower than from the plasma. Thus, optimal clinical and mycological effects are achieved in 2-4 weeks after the end of treatment for skin infections and 6-9 months after the end of treatment for nail infections.

Side effect

• dyspepsia (nausea, vomiting, constipation, diarrhea, decreased appetite);
• stomach ache;
• hepatitis;
• toxic liver damage (including cases of acute hepatic insufficiency with a lethal outcome);
• headache;
• dizziness;
• peripheral neuropathy;
• itching;
• rash;
• hives;
• angioedema;
• Stevens-Johnson syndrome;
• anaphylactic and anaphylactoid reactions;
• alopecia;
• photosensitization;
• edema;
• congestive heart failure and pulmonary edema;
• menstrual cycle disorders;
• hypokalemia.

Contraindications

• simultaneous reception of drugs metabolized with the participation of the enzyme CYP3A4 and capable of increasing the QT-interval, incl. terfenadine, astemizole, misolastine, cisapride, dofetilide, quinidine, pimozide, sertindole, levomethadone;
• simultaneous administration of midazolam for oral administration and triazolam;
• simultaneous administration of metabolized with the enzyme CYP3A4 HMG-CoA reductase inhibitors, such as simvastatin and lovastatin;
• simultaneous reception of ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine and methylergometrine;
• hypersensitivity to itraconazole and other components of the drug.

Application in pregnancy and lactation

Orungal should be administered during pregnancy only in life-threatening systemic fungal infections, when the expected benefit for a woman exceeds the potential risk to the fetus.

Because itraconazole is excreted in breast milk, if it is necessary to use it during lactation, breastfeeding should be discontinued.

Women of childbearing age during the period of taking the drug should use adequate methods of contraception throughout the course of treatment until the onset of the first menstruation after it is completed.

Application in elderly patients

Caution should be given to elderly patients.

Use in children

Since clinical data on the use of Orungal in children is not enough, it is not recommended to prescribe it to children, except when the expected benefit exceeds the possible risk.

special instructions

When investigating the dosage form of the Orungal preparation for intravenous administration on healthy volunteers, there was a transient asymptomatic decrease in the left ventricular ejection fraction normalized to the next infusion of the drug. The clinical significance of the data obtained for oral dosage forms is unknown.

Itraconazole has been found to have a negative inotropic effect.Cases of congestive heart failure associated with Orungal administration have been reported, and therefore the drug should not be taken to patients with chronic heart failure or having a history of the disease, unless the possible benefit far exceeds the potential risk. When assessing the benefit-risk ratio individually, factors such as the severity of the indications, the dosage regimen, and individual risk factors for congestive heart failure should be taken into account. Risk factors include the presence of heart disease, such as IHD or heart valve damage; serious lung diseases, such as obstructive pulmonary disease; renal failure or other diseases accompanied by edema. Such patients should be informed about the signs and symptoms of congestive heart failure. Treatment should be done with caution, while monitoring the patient for symptoms of congestive heart failure. When they appear, Orungala should be taken off.

Caution should be exercised when taking itraconazole simultaneously and calcium channel blockers.

With a reduced acidity of gastric juice, the absorption of itraconazole is disrupted. Patients taking antacid preparations (for example, aluminum hydroxide), it is recommended to use them not earlier than 2 hours after taking Orungal. Patients with achlorhydria or using histamine H2 receptor blockers or proton pump inhibitors should take capsules with a cola drink.

In very rare cases, when applying Orungal, severe toxic liver damage developed, including. cases of acute hepatic insufficiency with lethal outcome. In most cases this was observed in patients who already had liver disease, who received itraconazole therapy according to systemic indications, or who had other serious illnesses, as well as patients receiving other drugs with hepatotoxic effect. In some patients, there were no obvious risk factors for liver damage. 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 Orungal. Patients should be warned of the need to immediately inform the doctor in case of symptoms suggestive of hepatitis (anorexia, nausea, vomiting, weakness, abdominal pain and dark urine). In the case of such symptoms it is necessary to immediately stop therapy and conduct a study of liver function. Patients with elevated levels of liver enzymes, or liver disease in its active phase, or migrated toxic liver injury when taking other medications should not be given treatment Orungalom except where the expected benefits justify the risk of liver damage. In these cases, it is necessary to control the level of hepatic enzymes during treatment.

In patients with impaired hepatic function and / or renal function, the drug is administered under the control of the level of itraconazole in plasma and, if necessary, dose adjustment Orungal is performed.

Due to pharmacokinetic characteristics, it is not recommended to administer Orungal in the form of capsules to begin treatment of systemic mycoses that are life-threatening to patients.

The attending physician should evaluate the need for supportive therapy for AIDS patients who have previously been treated for systemic fungal infections, such as sporotrichosis, blastomycosis, histoplasmosis, or cryptococcosis (both meningeal and non-meningeal) who are at risk of recurrence.

If peripheral neuropathy occurs, if it is caused by taking Orungala, the drug is canceled.

There is no evidence of cross-sensitivity to itraconazole and other azole antifungal agents.

Impact on the ability to drive vehicles and manage mechanisms

Receiving Orungal does not affect the ability to drive and work with machinery.

Drug Interactions

Medicines that affect the absorption of itraconazole

Drugs that reduce the acidity of gastric contents, reduce the absorption of itraconazole, which is due to the solubility of capsule shells.

Medicines that affect the metabolism of itraconazole

In the studies it was found,that in the interaction of Orungal with rifampicin, rifabutin and phenytoin, the bioavailability of itraconazole and hydroxy-itraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. Simultaneous use of itraconazole with these drugs, which are potential inducers of hepatic enzymes, is not recommended. Studies of interaction with other inducers of hepatic enzymes, such as carbamazepine, Phenobarbital and isoniazid, have not been carried out, however, similar results can be assumed.

Since itraconazole is mainly metabolized by the CYP3A4 isoenzyme, potential inhibitors of this enzyme (ritonavir, indinavir, Clarithromycin and erythromycin) can increase the bioavailability of itraconazole.

Effect of itraconazole on the metabolism of other drugs

Itraconazole can inhibit the metabolism of drugs metabolized by the CYP3A4 isoenzyme. The result of this may be an increase or prolongation of their action (including side effects). Before you start taking concomitant medications, you should consult your doctor about the ways of metabolism of this drug, indicated in the instructions for medical use.After discontinuation of treatment, the concentrations of itraconazole in the plasma are reduced gradually depending on the dose and duration of treatment. This should be taken into account when assessing the inhibitory effect of itraconazole on the metabolism of concomitantly prescribed drugs.

When conducting a course of treatment Orungal can not be appointed:

• terfenadine, astemizole, misolastine, cisapride, dofetilide, quinidine, pimozide, sertindole, levometadone, the use of which together with Orungal can lead to an increase in the concentration of these substances in the plasma, which in turn can cause an increase in the QT interval and, in rare cases, paroxysmal ventricular tachycardia type "pirouette" (torsade de pointes);
• midazolam for oral administration and triazolam;
• metabolized by the enzyme CYP3A4 inhibitors of HMG-CoA reductase, such as simvastatin and lovastatin;
• preparations of ergot alkaloids, such as dihydroergotamine, ergometrine, ergotamine and methylergometrine;
• calcium channel blockers - in addition to the possible pharmacokinetic interaction associated with a common metabolic pathway involving the enzyme CYP3A4, calcium channel blockers have a negative inotropic effect, which can enhance the similar effect of itraconazole.

With a simultaneous appointment with Orungal should be monitored levels in the plasma, the effect, side effects of oral anticoagulants; HIV protease inhibitors (such as ritonavir, indinavir, saquinavir); some antitumor drugs (such as vinca alkaloids pink, busulfan, docetaxel, trimetrexate); metabolized by the isoenzyme CYP3A4 calcium channel blockers (dihydropyridine and verapamil); some immunosuppressive agents (such as cyclosporine, tacrolimus, sirolimus); some metabolized by the enzyme CYP3A4 inhibitors of HMG-CoA reductase, such as atorvastatin; some GCS, such as budesonide, Dexamethasone and methylprednisolone; as well as digoxin, carbamazepine, buspirone, alfentanil, alprazolam, brothisolam, midazolam (w / w), rifabutin, methylprednisolone, ebastin, reboxetine, repaglinide, disopyramide, cilostazol, eletriptan, halofantrine. With a simultaneous application with Orungal dose of the above drugs, if necessary, should be reduced.

Interactions between itraconazole and zidovudine and fluvastatin were not detected.

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

Effect on binding to proteins

Studies have demonstrated the lack of interaction due to competition for binding to plasma proteins, between itraconazole and such drugs as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamethasine.

Analogues of medicinal preparation Orungal

Structural analogs for the active substance:

• Irunin;
• Itrazole;
• Itraconazole;
• Itramikol;
• Canditral;
• Miconiol;
• Orungamine;
• Orunite;
• Rumikoz;
• Tecnazol.

Analogues for therapeutic effect (drugs for the treatment of mycosis nails):

• Amphotericin B;
• Atitis;
• Batrafen;
• Binafin;
• Bifonazole;
• Griseofulvin;
• Dactanol;
• Diflason;
• Diflucan;
• Lamisyl;
• Lamican;
• Loceril;
• Mikozolone;
• Mycosorrhal;
• Mycomomax;
• Mycospores;
• Mycoflucan;
• Nizoral;
• Nofung;
• Terbisyl;
• Thermic;
• Trozid;
• Fluconazole;
• Flucostat;
• Fungolon;
• Fungoterbine;
• Exifin;
• Exodermil.

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