Itraconazole

When ATH:
J02AC02

Characteristic.

Antimycotic means of a group of triazole derivatives. White or slightly yellowish powder. Insoluble in water, very little is soluble in alcohols, easily soluble in dihlormetane. Lipophilic, distribution coefficient (октанол/вода при pH 8,1) - 5,66. Molecular weight - 705,64.

Pharmacological action.
Broad spectrum antifungal.

Application.

Mycosis of the skin, mucous membrane of the mouth and eyes; onychomycosis, caused by dermatophytes, yeasts and molds; candidiasis with the defeat of the skin and mucous membranes, incl. vulvovaginal candidiasis; chromophytosis; systemic mycosis, incl. aspergillosis (resistance or poor tolerability amphotericin b), kryptokokkoz (incl. cryptococcal meningitis), histoplasmosis, sporotrichosis, Paracoccidioidomycosis, blastomycosis.

Contraindications.

Hypersensitivity.

Restrictions apply.

Congestive heart failure, incl. history (use only in cases, the expected benefit outweighs the potential risk), cirrhosis of the liver, renal failure, childhood (safety and effectiveness in children have not identified).

Pregnancy and breast-feeding.

Application of pregnancy is possible only in systemic mikozah in cases, When the expected effect outweighs the potential risk to the fetus.

Nursing mothers should abandon breastfeeding (itraconazole enters breast milk).

Side effects.

From the digestive tract: dyspepsia, nausea, abdominal pain, anorexia, vomiting, constipation, increased activity of liver transaminases, hepatitis, in very rare cases — heavy toxic liver damage, incl. a case of acute hepatic failure fatal.

From the nervous system and sensory organs: headache, dizziness, peripheral neuropathy, fatiguability, drowsiness.

Cardio-vascular system and blood (hematopoiesis, hemostasis): arterial hypertension. Reported cases of chronic heart failure, associated with the acquisition of itraconazole.

With the genitourinary system: dysmenorrhoea, edematous syndrome, albuminuria, staining of urine a dark color.

Allergic reactions: itching, rash, hives, angioedema, Syndrome Stevens - Johnson.

Other: alopecia, kaliopenia, pulmonary edema, decreased libido, impotence.

Cooperation.

Incompatible with terfenadine, astemizolom, cizapridom, lovastatin, oral forms midazolama and triazolama. Enhances and/or prolong the action of oral anticoagulants (incl. varfarina), cyclosporine, digoksina, methylprednisolone, vinchristina, calcium channel blockers. Rifampicin and phenytoin reduce bioavailability itrakonazola, inhibitors zitohroma CYP3A4 (ritonavir, indinavir, clarithromycin) increase its bioavailability. Antacids reduce absorption of itraconazole (interval, separating their admission, must be at least 2 no).

Overdose.

Treatment: gastric lavage, administration of activated charcoal, simptomaticheskaya therapy. Is not removed during dialysis. No specific antidote.

Dosing and Administration.

Inside, after meal (capsules), fasting (oral solution). Onychomycosis is 200 mg 1 once a day for 3 months or 200 mg 2 twice a day for 1 weeks, followed by a break 3 Sun; onihomicose 3 treatment, brushes- 2 exchange rate; vulvowaginalny candidiasis-on 200 mg 2 times during 1 day or 200 mg 1 once a day for 3 days; Tinea Versicolor- 200 mg 1 once a day for 7 days; dermatomikozy and candidiasis of the oral cavity is 100-200 mg 1 Once a day for 7-15 days (If necessary, repeat); gribkovi keratit- 200 mg 1 once a day for 21 day; mikozy system — for 100-200 mg 1-2 times a day for 2-12 months (depending on the pathogen).

Precautions.

In patients with impaired immunity (AIDS, state after organ transplantation, neutropenia) You may need to increase the dose (as a result of reduced bioavailability of itraconazole).

In appointing patients with chronic heart failure require individual assessment ratio of benefits and risks, taking into account such factors as the seriousness of the evidence, dosing regimen, individual risk factors (the presence of heart disease, incl. CHD, defeat valves), chronic obstructive pulmonary disease, renal failure. If you experience signs or symptoms of congestive heart failure, as well as neuropathy treatment itrakonazolom should be discontinued.

During treatment itrakonazolom it is necessary to monitor liver function (especially in the long admission). With the increased level transaminaz shall appoint, If the effect of therapy outweighs the potential risk to liver. In patients with cirrhosis of the liver and/or kidney dysfunction must be monitored itrakonazola concentration in the plasma and adjust dose.

Women of childbearing age should use adequate contraception throughout treatment, until the onset of first menstruation after its completion.

Cooperation