Itraconazole

Chemical name

4-[4-[4-[4-[[2-(2,4-Дихлорфени л)-2-(1Н-1,2,4-триазол-1-илм етил)-1,3-диоксолан-4-ил] метокси]фенил]-1-пипер��зинил]фенил]-2,4-дигидр о-2-(1-метилпропил)-3Н-1,2, 4-триазол-3-он

Gross

C35-H38-Cl2-N8-O4

Characteristics

White with a slightly yellowish white powder, insoluble in water and poorly soluble in alcohol and dissolves easily in dihlormetane.

Of drugs

The drugs-antimycotic. Ingibiruet цитохром-Р450-зависимы�� synthesis fungal ergosterola necessary component of cell membranes fungus, and it was fungizidnyi effect. Extracted from the blood adequately. Admission after eating increases bioavailability. C_max achieved in 3-4 hours equilibrium concentration in plasma (with a 200 mg 1-2 times a day), in 1-2 weeks and the amount of (in 3-4 h after administration of the last dose) : 0.4 µ g / ml (to 100 mg once a day); 1.1 µ g / ml or 2 µ g / ml (200 mg one or two times a day). Associated with the plasma protein at 99.8%. Penetrates into tissues and organs (including the vagina), in secret and sebaceous glands port, accumulate in the lungs, kidneys, liver, bones, stomach, spleen, skeletal muscle : itrakonazola concentration in the tissues exceeds plasma (especially in the skin), in 2-4 times. Therapy (protivogribkovi) level keratine nails achieved within 1 week and remains about 6 months months after treatment, the skin for a period of 2-4 weeks after 4-nedelnogo reception. Biotransformiroetsa in the liver with the formation of a large number of metabolites, including active (гидроксиитраконазол��). Return plasma dwuhfaznoe, T_1/2 - 24-36 h. Place in 1 hour gastrointestinal (3-18%) and kidneys (35%). Active against dermatomycosis (Trichophyton spp. , Microsporum spp. , Epidermophyton floccosum), yeast fungi, including Candida spp. (including C.albicans, C.glabrata, C.krusei), mould fungi (Cryptococcus neoformans, Aspergillus spp. , Histoplasma spp. , Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp. , Cladosporium spp. , Blastomyces dermatitidis), etc.

Indications

Onihomikoz, mikozy skin, mouth and eyes caused by dermatofitami, yeast and plesnevami mushrooms, tropical system mikozy, vulvowaginalny candidiasis.

Restrictions on the use of

Application of pregnancy is allowed only in systemic mikozah when the expected effect outweighs the potential risk to the fetus. Nursing mothers should abandon breastfeeding.

Contraindications

Гиперчувствительност ь.

Side-Effects

Neuralgia, pain in the abdomen, constipation, hepatitis, increased appetite, headache, dizziness, peripheral neuropathy, dismenorea, raising transaminaz plasma blood, skin, thrombocytopenia, lakopenia, prolonged bleeding, swelling, gipokaliemia, increased body mass index, giperammoniemia, alopecia, fatigue Stevens-Johnson, angioneuroticeski swelling, urticaria, skin.

Patient interaction

Incompatible with terfenadine, astemizolom, lovastatinom, oral forms midazolama and triazolama. Enhance and / or prolong the oral anticoagulants, cyclosporine A, digoxin, metilprednizolona, racumin, vinchristina, blocking calcium channels. Rifampicin and phenytoin reduce bioavailability itrakonazola, antatsidnye drugs-induction (interval separating their admission should not be less than two hours).

Precautions

If increased level transaminaz shall, if the effect of therapy over the risk of liver damage. In patients with cirrhosis and / or in violation of kidney function should be monitored itrakonazola concentration in the plasma and, if necessary, adjust the dose. In the case of low acidity gastric juice that made with drunk. Women of child-bearing age at the time of treatment should be to use contraception.

Dosing and Administration

The inside is not liquid, after food. Onihomikoz-200 mg / day for 3 months or 200 mg twice a day for one week, followed by a break three weeks; Onihomicose to stop to three days of treatment, case-2 course; vulvowaginalny candidiasis-200 mg twice in one day or 200 mg once a day for 3 days; otrubevidnyi zoster - 200 mg once a day for 7 days; dermatomikozy and candidiasis of the oral cavity is 100 mg once a day for 15 days (if necessary repeat rate); gribkovi keratit-200 mg once a day for 21 days; mikozy system for the 200 mg 1-2 times a day for 2-12 months (depending on the cause).

Directory → Antimicrobials, and protivoparazitarnae protivoglistnae funds → Antifungal funds → Itraconazole