2010/06/05

ITRACONAZOLE

Pharmacological action

Antifungal, triazole derivatives. The mechanism of action associated with the ability to inhibit cytochrome P 450-dependent enzymes of sensitive fungi, which leads to disruption of the synthesis of ergosterol of the cell wall of the fungus. It has a broader spectrum anti-fungal activity than ketoconazole. It is active against Aspergillus spp., Blastomyces dermatitidis, Candida, Coccidioides immitis, Cryptococcus neoformans, Epidermophyton, Microsporum, Trichophyton, Histoplasma capsulatum, Malassezia furfur, Paracoccidioides brasiliensis, Sporothrix schenckii.


Pharmacokinetics

Therapeutic concentrations in the skin persist for 2-4 weeks after the end of a 4-week course of treatment. Itraconazole is defined in the keratin of nails in a week after the start of treatment and lasts for 6 months after the end of the 3-month course of therapy.


Statement

Vulvovaginal candidiasis, mycoses of the skin, mouth, eyes, onychomycosis caused by dermatophytes and / or yeast, systemic mycosis (including systemic aspergillosis, candidiasis, cryptococcosis, histoplasmosis, sporotrichosis, parakoktsidioidoz, blastomycosis, and other rare tropical and systemic mycoses).


Dosage regimen

Inside of 100 mg 1 time / d or 200 mg 1-2 times / day, duration of treatment depends on the etiology of disease.


Side effect

Co of the digestive system: stomach aches, nausea, vomiting, constipation, increased activity of liver enzymes, cholestatic jaundice, and in some cases - hepatitis.

The part of the CNS and peripheral nervous system: headache, dizziness, and in some cases - peripheral neuropathy.

Since the cardiovascular system: in some cases - edema, congestive heart failure and pulmonary edema.

Allergic reactions: skin rash, itching, urticaria, angioedema, Stevens-Johnson syndrome.

Other: long-term use - dysmenorrhea, hair loss, hypokalemia.


Contraindications

Simultaneous ingestion terfenadina, astemizola, mizolastina, tsizaprida, dofetilida, quinidine, pimozida, simvastatin, lovastatin, midazolam, or triazolama; sensitivity to itraconazole.


Application of pregnancy and breastfeeding

Itraconazole is used during pregnancy only if systemic mycosis when the expected effect of therapy outweighs the potential risk to the fetus.

Women of childbearing age in the period of itraconazole is recommended to use contraceptives.

If necessary, use during lactation should decide on the termination of breastfeeding.

In experimental studies found that itraconazole has embryotoxicity and causes abnormal development of the fetus.


Cautions

Should not be used in patients with symptomatic ventricular dysfunction and indications in history to congestive heart failure.

You should not use itraconazole in patients with liver disease. However, in cases of extreme necessity in liver cirrhosis and / or breach of renal function itraconazole treatment is performed under the control of its level in plasma and with appropriate dose adjustment.

When the activity of liver transaminases Itraconazole is used in cases where the expected benefit of therapy exceeds the potential risk of liver damage.

In the case of itraconazole over 1 month is necessary to monitor liver function.

With the development during the treatment of symptoms of heart failure, abnormal liver function, peripheral neuropathy itraconazole should be abolished.

With careful use itraconazole sensitivity to other derivatives of Asola.

Use in Pediatrics

Currently, insufficient data on the use of itraconazole in children.


Drug Interactions

Vehicles causing an induction of liver enzymes (rifampicin, phenytoin) may decrease the concentration of itraconazole in plasma.

When applied simultaneously with drugs that reduce gastric acidity (including m-holinoblokatory, antacid, histamine blockers H 2-receptor), may decrease absorption of itraconazole.

With the simultaneous use of drugs, the metabolism of which involve the participation of isozymes 3A cytochrome P 450 may increase in intensity and / or duration of their effects. These drugs include terfenadin, astemizol, tsizaprid, midazolam, triazolam (Oral), indirect anticoagulants, cyclosporine, digoxin, calcium channel blockers, quinidine, vincristine.