Rumicosis
Medicines that affect the absorption of itraconazole. Drugs that reduce gastric acidity reduce the absorption of itraconazole. Medicines that affect the metabolism of itraconazole. Itraconazole is primarily broken down by the enzyme CYP3A4. When used simultaneously with rifampicin, rifabutin, phenytoin, carbamazepine, isoniazid, which are powerful inducers of the CYP3A4 enzyme, the bioavailability of itraconazole and hydroxy-itraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. The simultaneous use of Rumikoz® with these drugs, which are potential inducers of liver enzymes, is not recommended. Potent inhibitors of the CYP3A4 enzyme, such as ritonavir, indinavir, clarithromycin and erythromycin, may increase the bioavailability of itraconazole. Effect of itraconazole on the metabolism of other drugs: Itraconazole may inhibit the metabolism of drugs metabolized 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 Rumikoz®, the plasma concentration of itraconazole decreases gradually depending on the dose and duration of treatment (see Pharmacokinetics section). This must be taken into account when discussing the inhibitory effect of itraconazole on concomitant medications. Medicines that are not recommended to be prescribed concomitantly with Rumikoz®: • calcium channel blockers - in addition to the possible pharmacokinetic interaction associated with the common metabolic pathway involving the CYP3A4 enzyme, calcium channel blockers may have a negative inotropic effect, which is enhanced when taken simultaneously with with the drug Rumikoz®. Drugs, when administered concomitantly, it is recommended to monitor their plasma concentrations, effects, and side effects. If necessary, the dose of these drugs should be reduced. •oral anticoagulants •HIV protease inhibitors (ritonavir, indinavir, saquinavir) •some antineoplastic drugs (vinca rosea alkaloids, busulfan, docetaxel, trimetrexate) •calcium channel blockers cleaved by the CYP3A4 enzyme (verapamil and dihydropyridine derivatives) •some immunosuppressive drugs (cyclosporine, tacrolimus, sirolimus (also known as rapamycin) • some CYP3A4-digested HMG-CoA reductase inhibitors (atorvastatin) • some glucocorticosteroids (budesonide, dexamethasone and methylprednisolone) • other drugs: digoxin, carbamazepine, buspirone, alfentanil, alprazolam, brotizolam, midazolam for intravenous, rifabutin, ebastine, reboxetine, cilostazol, disopyramide, eletriptan, halofantrine, repaglinide. No interaction was found between itraconazole zidovudine and fluvastatin. There was no effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone. In vitro studies demonstrated no interaction between itraconazole and such drugs , such as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamerazine when bound to plasma proteins.
Pharmacodynamics and pharmacokinetics
Rumicosis is a triazole . It is a synthetic antifungal drug with a broad spectrum of action. The main mechanism of action of the active substance of the drug is inhibition of the synthesis of ergosterol , which is one of the important components of the fungal cell membrane.
Itraconazole is active against:
- dermatophytes: Epidermophyton floccosum, Microsporum spp., Trichophyton spp.;
- yeast and yeast-like fungi: Pityrosporum spp., Cryptococcus neoformans, Trichosporon spp., Candida spp., Geotrichum;
- Aspergillus spp., Paracoccidioides brasiliensis, Histoplasma spp., Sporothrix schenckii, Cladosporium spp., Fonsecaea spp., Blastomyces dermatitidis, Penicillium marneffei, Pseudallescheria boydii, as well as other molds and yeasts.
Itraconazole, when administered orally (internally), is well absorbed from the gastrointestinal tract, reaching peak plasma levels within 3-4 hours after administration.
To achieve maximum bioavailability of itraconazole, it is recommended to take Rumikoz capsules immediately after meals. After 7-14 days of treatment, equilibrium concentrations of the drug in plasma are observed.
The binding to plasma proteins is quite high. Itraconazole has good penetrating ability into body tissues and its biological fluids, while in some organs (lungs, stomach, kidneys, liver, skeletal muscles) its concentrations exceed plasma levels by 2-3 times.
The active substance is deposited in keratin tissues (exceeding the same indicators in plasma by 4 times), and the rate of its removal from the skin depends on the speed of regeneration of the epidermis. For 14-28 days after discontinuation of the drug, therapeutic concentrations of itraconazole in the skin remain, and in the vaginal mucosa they are detected another 48 hours after the end of a three-day course of therapy at a daily dose of 200 mg, and within 72 hours at a daily dose of 400 mg.
In the keratin of nail plates, itraconazole is determined 7 days after the start of therapy and for 6 months after the end of three months of treatment. Itraconazole is also found in the secretions of the sweat and sebaceous glands.
Metabolism of itraconazole occurs in the liver, with the release of active metabolites, and the effect of some of them is not inferior to the effect of the unchanged drug.
It is eliminated from plasma in two stages. T1/2 - 24-36 hours.
3-18% is excreted through the intestines and about 0.03% through the kidneys (unchanged), as well as 35% in the form of metabolites (over 7 days).
Bioavailability decreases with impaired immunity and renal failure. In liver cirrhosis, along with a decrease in bioavailability, the half-life increases.
Indications for use
- fungal keratitis;
- ringworm;
- onychomycosis caused by molds, yeasts and/or dermatophytes;
- systemic candidiasis and aspergillosis ;
- blastomycosis;
- cryptococcosis , including cryptococcal meningitis (for immunodeficiency and cryptococcosis, the central nervous system is prescribed only if it is impossible to use first-line therapy);
- sporotrizosis;
- histoplasmosis;
- paracoccidioidomycosis;
- other tropical and systemic mycoses ;
- pityriasis versicolor;
- deep visceral candidiasis;
- candidomycosis with damage to the skin and mucous membranes, in particular vulvovaginal candidiasis ( thrush ).
Contraindications
Hypersensitivity to itraconazole or other components of the drug.
Combined use of Rumikoz and the following groups of drugs:
- Astemizole , terfenadine , mizolastine , dofetilide , cisapride , Quinidine , levomethadone , Pimozide , Sertindole and other drugs that increase the QT interval and are metabolized by the CYP3A4 enzyme;
- Lovastatin , Simvastatin and other HMG-CoA reductase inhibitors that are broken down by the enzyme CYP3A4;
- Triazolam and midazolam for internal use (tablets);
- Ergometrine , dihydroergotamine , methylergometrine , Ergotamine and other ergot alkaloids.
Carefully:
- liver pathologies;
- childhood;
- heart failure .
Analogs
Level 4 ATC code matches:
Medoflucon
Vfend
Itracon
Mikosist
Irunin
Mikomax
Orungal
Mycoflucan
Fluconazole
Sporagal
Orungamin
Flucostat
Difluzol
Futsis
Vero-Fluconazole
Kandizol
Kanditral
Itraconazole
Diflazon
Of course, when prescribing any drug, including Rumikoz, people try to find cheaper analogues, often neglecting their effectiveness. It is worth saying that very often medicines that are half the price of the recommended one may require a double or even triple dose of use.
It depends on the raw materials from which the drug is produced, the degree of purification of the active substance, the number of foreign inclusions and much more. Therefore, before buying a cheap analogue, make sure that its effectiveness will not be inferior to the medicine prescribed to you.
Analogs of Rumikoz:
- Itrazole
- Irunin
- Orungal
- Itraconazole
- Orungamin
- Kanditral
- Orunite
- Tecnazole
Side effects
Gastrointestinal tract:
- nausea;
- dyspepsia;
- vomit;
- abdominal pain;
- decreased appetite;
- constipation or diarrhea .
Hepatobiliary system:
- hepatitis;
- increased activity of liver transaminases (reversible);
- severe toxic liver damage (cases of acute liver failure with fatal outcome have been recorded).
Nervous system:
- peripheral neuropathy;
- dizziness;
- headache.
Skin:
- photosensitivity;
- alopecia.
Allergic manifestations:
- hives;
- itching and rash on the skin ;
- angioedema;
- Stevens-Johnson syndrome.
Other:
- edema syndrome;
- hypercreatininemia;
- hypokalemia;
- irregularities in the menstrual cycle;
- pulmonary edema;
- congestive heart failure;
- dark coloration of urine.
Instructions for use of Rumikoz (Method and dosage)
The drug Rumicosis is taken orally (inside). The instructions for Rumikoz recommend swallowing the capsules whole, without chewing or crushing, immediately after eating.
The duration of therapy with Rumikoz and its dose is determined only by the attending physician, individually for each patient.
In the treatment of vulvovaginal candidiasis , there are two treatment regimens, according to one of them, treatment takes 1 day with the prescription of 200 mg of Rumikoz twice a day; according to another scheme, treatment is carried out for 3 days with a daily dose of 200 mg.
When treating oral candidiasis, a daily dose of 100 mg is recommended for 15 days.
Patients with dermatomycosis of smooth skin, fungal keratitis and pityriasis versicolor are prescribed a daily dose of 200 mg. The duration of treatment for ringworm and pityriasis versicolor is 7 days and 21 days for fungal keratitis . There is an alternative treatment regimen for dermatomycosis of smooth skin, with the prescription of 100 mg of the drug for 15 days.
Fungal infections of highly keratinized areas require taking 200 mg of Rumikoz twice a day for 7 days, or 100 mg every day for a month.
It must be remembered that in case of diseases: neutropenia , AIDS , as well as after organ transplantation , dose adjustment may be required.
For onychomycosis , a 1-week course of therapy with a daily dose of 200 mg is indicated. Then, after a 3-week break, the course is repeated. For onychomycosis of the nails, 2 courses are carried out and 3 courses for onychomycosis of the toes . In case of severe damage to the nail plates on the toes, taking Rumikoz, in the same dose, can be continuous for 3 months.
Systemic mycoses can be treated in daily doses from 100 mg to 400 mg, depending on the severity of the disease and the nature of the pathogen. The duration of treatment can take from 3 weeks to 8 months.
Below are the usual regimens for the treatment of systemic mycoses with the drug Rumicosis.
For candidiasis , 100-200 mg per day is prescribed for 1 to 7 months (for disseminated or invasive disease - 400 mg per day).
For aspergillosis, the daily dose is 200 mg for 2 to 5 months (for disseminated or invasive disease - 400 mg per day).
For cryptococcosis (with the exception of meningitis ), take 200 mg per day for 2 to 12 months.
For cryptococcal meningitis , a daily dose of 400 mg is indicated for 2 to 12 months.
For histoplasmosis , 200 mg is prescribed 1-2 times a day for 8 months.
For sporotrichosis , treatment lasts for 3 months at a daily dose of 100 mg.
For chromomycosis, it is recommended to take 100-200 mg of itraconazole per day for 6 months.
For blastomycosis, the daily dose of Rumikoz varies from 100 mg to 400 mg, depending on the severity of the condition. The course of therapy is 6 months.
For paracoccidioidomycosis, the course of treatment continues for 6 months, with a daily dose of 100 mg.
