Itrakon

Itrakon – antifungal drug.

Form of release and structure

Itrakon release in the form of capsules: gelatinous, the case – pink color, a lid – blue; contents of capsules – spherical granules of cream or white color (on 5 or 6 capsules in blisters, on 3 blisters in a cardboard pack).

Is a part of 1 capsule:

• Active agent: итраконазол – 100 mg;
• Auxiliary components: gidropropilmetiltsellyuloza or gipromelloza, gelatin, sucrose, dyes azoruby (E122) and "sunset" (E110).

Indications to use

• The mycoses caused by the dermatophytes and yeast showing sensitivity to effect of active agent (itrakonazola);
• Dermatomycoses, chromophytosis, keratitis of a fungal origin, candidosis defeats of an oral cavity, fungal infections of nail plates (onychomycoses);
• Vulvovaginal candidiasis;
• Cryptococcal damages of the central nervous system at patients with the weakened immunity in cases when therapy by other medicines was not productive;
• System mycoses, system aspergillomycosis or candidiases, and also cryptococcoses (including cryptococcal meningitis);
• Rare system and tropical mycoses, including histoplasmosis, a sporotrichosis, a paracoccidioidosis, a zymonematosis and other fungal infections.

Contraindications

• Simultaneous use with the drugs which are metabolized with CYP3A4 enzyme participation, extending QT interval (because of possible increase in level of an itrakonazol in a blood plasma that can lead to lengthening of an interval of QT with development of ventricular tachycardia);
• Simultaneous use with drugs, metabolizirovanny with participation of CYP3A4 enzyme of inhibitors of GMG-KOA-reduktazy, and also with the medicines containing ergot alkaloids;
• Instructions in the anamnesis on an acute heart failure or other displays of ventricular dysfunction of heart (except states, life-threatening the patient, or in the presence of the disease-producing factors showing resistance to therapy by other drugs);
• Hypersensitivity to drug components.

The feeding and pregnant women, and also children Itrakon can accept only according to strict indications after ratio assessment advantage/risk.

Route of administration and dosage

Itrakon accept inside, without chewing. Drug is recommended to be accepted after food (high-calorific food promotes the best absorption).

The scheme of use of drug is defined by indications:

• Fungal keratitis: once a day on 2 capsules, a course – 21 days;
• Oral candidiasis: on 1 capsule once a day, a course – 15 days. Itrakon's bioavailability can be lowered at pathologies of immune system, in this case can demand increase in a dose twice;
• Chromophytosis: on 2 capsules once a day, a course – 7 days;
• Vulvovaginal candidiasis: reception on one of schemes – 2 times a day on 2 capsules, a course – 1 day, or once a day on 2 capsules, a course – 3 days is possible;
• Dermatomycoses: reception on one of schemes – once a day on 2 capsules, a course – 7 days, or once a day on 1 capsule, a course – 15 days is possible. An epidermophitia of feet and hands, and also other defeats with high keratinization: reception on one of schemes – 2 times a day on 2 capsules, a course – 7 days, or once a day on 1 capsule, a course – 30 days is possible;
• The onychomycoses caused by dermatophytes and/or yeast (defeats of nail plates on toes with simultaneous defeat on hands or without it, defeat of nail plates only on hands) reception on one of schemes – once a day on 2 capsules, a course – 7 days which needs to be repeated in 21 days, or once a day on 2 capsules, a course – 3 months is possible. In certain cases the doctor appoints the scheme of use of drug individually. Because of slow removal of Itrakon from nails and tissues of skin, the therapeutic effect is reached only in 14-28 days after the termination of a course of therapy of damages of skin and in 6-9 months after the termination of a course of treatment of diseases of nail plates.

At treatment of system mycoses usually appoint:

• Aspergillosis – once a day on 2 capsules, a course – 2-5 months. At the invasive or disseminated disease increase in frequency rate of administration of drug up to 2 times a day is possible;
• Candidiasis: once a day on 1-2 capsules, a course – from 3 weeks to 7 months. At the invasive or disseminated disease increase in frequency rate of administration of drug up to 2 times a day is possible;
• Cryptococcosis (without meningitis symptoms): once a day on 2 capsules, a course – 2-12 months;
• Cryptococcal meningitis: 2 times a day on 2 capsules, a course – 2-12 months;
• Histoplasmosis: 1-2 times a day on 2 capsules, a course – 8 months;
• Sporotrichosis: once a day on 1 capsule, a course – 3 months;
• Paracoccidioidomycosis: once a day on 1 capsule, a course – 6 months (patients with AIDS have not enough data on efficiency of the specified dosing mode);
• Chromomycosis: once a day on 1-2 capsules, a course – 6 months;
• Zymonematosis: 1-2 times a day on 1-2 capsules, a course – 6 months.

Side effects

During Itrakon's reception the following disturbances which are shown with various frequency can develop:

• Central nervous system: headache, peripheral neuropathy, paresthesias, hypesthesia, dizzinesses;
• Digestive tract: often – dyspepsia, nausea, a meteorism, abdominal pains, a lock, a dysgeusia, diarrhea, vomiting;
• Immune system: serum disease, anaphylactic and anaphylactoid reactions;
• Allergic reactions: skin itch, papular rash, small tortoiseshell, Quincke's disease, Stephens-Johnson's syndrome, inflammatory diseases of upper respiratory tracts, sinusitis, rhinitis, fluid lungs, congestive heart failure;
• Lymphatic system and blood: in rare instances – a leukopenia, a neutropenia, thrombocytopenia;
• Musculoskeletal system and connecting fabric: mialgiya, arthralgias;
• Reproductive system: women have frustration of a menstrual cycle, men have an erectile dysfunction;
• Metabolic frustration: giperglitseridemiya, hypopotassemia;
• Organ of sight: vision disorders, including a diplopia, opacification or feeling of a grid before eyes;
• Acoustic organ: sonitus, temporary or constant hearing loss;
• Gepatobiliarny system: crushing toxic damages of a liver with development of isolated cases of an acute liver failure, reversible increase in activity of liver enzymes, hepatitis;
• Kidneys and urinary tract: pollakiuria and incontience of urine;
• Skin and hypodermic fabrics: a toxic epidermal necrolysis, a multiformny erythema, exfoliative dermatitis, a leykotsitoklastichesky vasculitis, the raised photosensitivity, an alopecia;
• Others: hypostases.

Special instructions

Sugar is Itrakon's part that needs to be considered at its appointment as a sick diabetes mellitus.

At the lowered acidity of a stomach absorption of active agent in digestive tract worsens. At simultaneous use of Itrakon with antiacid drugs (for example, with aluminum hydroxide) it is necessary to observe a break not less than 2 hours.

The patient with an achlorhydria or at simultaneous use of H2 blockers or inhibitors of the proton pump Itrakon is recommended to accept with drinks like stake.

Drug is not recommended to be used for primary treatment of medical emergencies which cause system fungal infections.

Need of carrying out a maintenance therapy at patients with AIDS who were treated for system mycoses (a sporotrichosis, a zymonematosis, histoplasmosis or a cryptococcosis, including cryptococcal meningitis) and are in risk group of development of a recurrence, the doctor defines individually.

Women of reproductive age during all course of therapy (before the first periods after its end) need to apply well-tried remedies of contraception.

Itrakon patients should not accept with congestive heart failure or with the instruction on this disease in the anamnesis except cases when the expected advantage is much higher than potential risk. At individual assessment of a ratio advantage/risk it is necessary to consider the following factors: the mode of dosing, the indication, individual risk factors of development of congestive heart failure (coronary heart disease, defeat of valves, a chronic obstructive pulmonary disease, a renal failure or other diseases which are followed by hypostases). Treatment needs to be carried out with care, controlling symptoms of congestive heart failure. At development of these symptoms Itrakon's use should be stopped.

It is necessary to be careful at simultaneous use of Itrakon with blockers of calcium channels.

During Itrakon's reception it is recommended to carry out monitoring of function of a liver. At development of symptoms of hepatitis (anorexia, vomitings, nausea, increased fatigue, dark coloring of urine or abdominal pains) needs to interrupt treatment and to see a doctor.

Itrakon's bioavailability at oral administration at patients with cirrhosis and a renal failure goes down a little therefore dose adjustment can be required.

At development of neuropathy therapy should be interrupted.

To elderly patients Itrakon appoint only in cases when the expected advantage is higher than risk from drug use.

The most frequent side effect of Itrakon – diarrhea which can cause decrease in absorption of active agent and change intestinal microflora, promoting development of fungal colonization. In these cases it is necessary to be careful at the treatment termination.

The patients accepting Itrakon or Itrakon along with quinidine have messages on a temporary or resistant hearing loss (the combination of these medicines is contraindicated). As a rule, after drug withdrawal hearing is recovered, however in certain cases the hearing loss can be irreversible.

As at Itrakon's use there can be dizziness, for the period of therapy it is recommended to abstain from control of motor transport and performance of other works demanding high concentration of attention.

Medicinal interaction

Simultaneous use of Itrakon with some drugs demands control of level of their concentration in plasma a shelter. At purpose of such combinations of medicines control of a condition of the patient and development of side effects is required. Also dose adjustment can be required. With care Itrakon appoint at the same time with the following medicines:

• HIV protease inhibitors (индинавир, ритонавир, саквинавир);
• Peroral anticoagulants;
• Some antineoplastic drugs (the methotrexate, alkaloids of a periwinkle of pink (Vinca), dotsetakset, бусульфан);
• Blockers of calcium channels which are split by CYP3A4 enzyme (verapamil, dihydropyridine);
• Some immunosuppressors (такролимус, cyclosporine, рапамицин);
• Some glucocorticosteroids (dexamethasone, будесонид, Methylprednisolonum);
• Some cardiac glycosides (digoxin);
• Other drugs relating to different pharmaceutical groups (буспирон, carbamazepine, alfentanil, цилостазол, fentanyl, галофантрин, Disopyramidum, to alprazola, рифабутин, brotiozolam, midazolam, эбастин, репаглинид, ребоксетин, loperamide).

At simultaneous use of Itrakon with some medicines there can be undesirable effects:

• Rifampicin, Phenytoinum, рифабутин: considerable decrease in efficiency of Itrakon because of decrease in bioavailability (the combination with the drugs inducing enzymes of system of cytochrome is not recommended);
• Inhibitors of CYP 3A4 enzyme (кларитромицин, индинавир, ритонавир, erythromycin and other antibacterial drugs): increase in bioavailability of an itrakonazol;
• Blockers of calcium channels: decrease in their metabolism, strengthening of a negative inotropic effect (such combination demands care).

Itrakonazol does not exert impact on metabolism of Norethisteronum and ethinylestradiol and does not interact with the following drugs: флувастатин, zidovudine, Tolbutamidum, Imipraminum, diazepam, propranolol, indometacin, Cimetidinum, Sulfamethazinum.

Terms and storage conditions

To store in protected from light, the place, dry, unavailable to children, at a temperature up to 25 °C.