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SPORANOX
(generic name: intraconazole)

Pharmacological category: antifungal

Reviews
Int J Clin Pharmacol Ther. 2005 Feb;43(2):109-16.
Simultaneous itraconazole bioequivalence assessment and CYP3A phenotyping in South American subjects.
Estevez-Carrizo FE, Ruiz S, Bellocq B, Leal C, Siri MT, del Campo MJ.
Center for Biomedical Sciences, University of Montevideo, Montevideo, Uruguay. festeve2@adinet.com.uy.

OBJECTIVE: The present study evaluates the acute effect of a single-dose itraconazole administration on CYP3A phenotype, as measured by cortisol MR ratio in urine. METHODS: Twenty-four healthy Uruguayan subjects recruited according to strict inclusion criteria participated in an open-label, randomized, two-period, crossover study designed to evaluate the bioequivalence of an itraconazole formulation (Traconal 100 mg, Ache Labs, Sao Paulo, Brazil). The study comprised two treatment periods separated by a wash-out period of 14 days. In each period a series of venous blood samples were drawn over 48 hours. Three urine samples were obtained for CYP3A phenotyping: pre-dose, 24 and 48 hours after dosing. Blood and urine samples were assayed for itraconazole, beta-hydroxycortisol and cortisol using a validated chromatographic method. RESULTS: The ratio of the mean AUC0-inf. T/AUC0-inf. R was included in the bioequivalence range, however, due to high variability, the CI90% was not. It was found that the cortisol metabolic ratio (MR) showed inhibition relative to basal activity in a proportion of subjects 24 hours (68 +/- 6.1%, mean +/- CI95%) and 48 hours (80 +/- 7.3%, mean +/- CI95%) after ingestion of itraconazole. A significant correlation was found between itraconazole AUC0-inf. and normalized basal CYP3A MR for the reference (r = 0.62, t = 3.72, p = 0.001) and the test product (r = 0.74, t = 5.22, p = 0.00003). A good correlation existed between basal cortisol MR and the elimination half-life of itraconazole. CONCLUSIONS: The findings are in line with the hypothesis that the determination of the bioavailability of highly variable CYP3A substrates might be improved by simultaneous non-interfering phenotyping. If this is confirmed, a new methodological paradigm may need to be developed in order to take account of metabolic variability in bioequivalence evaluation of this group of drugs.
J Dermatolog Treat. 2003 Jun;14(2):95-8
Itraconazole pulse therapy improves the quality of life of patients with toenail onychomycosis
Firooz A, Khamesipour A, Dowlati Y
Center for Research & Training in Skin Diseases and Leprosy, Tehran University of Medical Sciences, 79 Taleghani Avenue, Tehran 14166, Iran

BACKGROUND: Toenail onychomycosis is a common disease that can have serious adverse effects on the quality of life (QOL) of patients. AIM: To evaluate the impact of itraconazole pulse therapy on the QOL of patients with toenail onychomycosis. METHODS: A total of 20 patients with disto-lateral subungual toenail onychomycosis were treated with itraconazole 200 mg twice daily for 1 week every 4 weeks for 12 weeks. The patients were asked to complete a QOL questionnaire before treatment and on the last follow-up visit (week 48). A score of 0-4 was given according to the five possible responses to each question and these were summed to give the final score of the patient. The mean of the final scores of the patients before and after treatment were compared using the Wilcoxon matched-pairs test. RESULTS: At 48 weeks after commencing treatment, 14 patients (70%) responded to treatment (nine patients were cured with almost totally clear toenails and five patients improved), and 16 patients (80%) were mycologically cured (negative KOH smear and culture). The mean of the QOL scores of the patients before treatment was 18.0+/-7.8, which reduced to 13.1+/-11.3 after treatment (two-tailed, p=0.009). CONCLUSION: Itraconazole pulse therapy is an effective treatment and can improve the QOL of patients with toenail onychomycosis.
Akush Ginekol (Sofiia). 1999;38(3):56-8
The treatment of vaginal mycosis with Orungal
Pekhlivanov B, Markova R

(Janssen-Cilag). Twenty two sexually active women are included in the study, all with clinical signs of fungal vaginitis. Microscopic examination of vaginal secretions and fungal cultures are performed for all of the patients. Twenty cultures show C.albicans as causing agent and 2-non-C.albicans. One-day treatment with Orungal 2 x 200 mg is prescribed. Control examination and mycologic cultures are performed on day 7-10 and 30 after treatment. In 20 patients (91%) there is not clinical signs and the cultures remains negatives. In 2 (9%) the signs of fungal vaginitis persists which evoke the giving of the same dose once again. Adverse reaction (nausea) has been notify by one woman. CONCLUSION: The treatment with Orungal of the vaginal mycosis is highly effective, with minimal adverse reactions and very good acceptance by women.
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Drug information

GENERIC NAME: itraconazole
BRAND NAME: Sporanox


DRUG CLASS AND MECHANISM: Itraconazole is a drug used in the treatment of fungal infections, such as aspergillosis, blastomycosis, histoplasmosis, and fungal infection localized to the toenails and fingernails (onychomycosis).

PREPARATIONS: Capsule 100 mg.

STORAGE: Itraconazole should be stored at room temperature in a tight container. Protect from light and moisture.

PRESCRIBED FOR: The treatment of fungal infections which are isolated to a small area of the body (localized) or throughout the body (systemic). It is active against fungal infections such as aspergillosis, blastomycosis, histoplasmosis, and fungal infection localized to the toenails and fingernails (onychomycosis).

DOSING: Should be taken with a full meal. It is important to report any signs or symptoms that may suggest liver dysfunction so that the appropriate laboratory testing can be done. These signs include unusual fatigue, poor appetite, nausea and/or vomiting, yellowing of the eyes (jaundice), dark urine or pale stool.

DRUG INTERACTIONS: Liver tests are monitored periodically in most patients, especially if receiving continuous treatment for more than one month. Itraconazole is used with caution in any patient with liver dysfunction.

The use of itraconazole in children is not recommended because it's safety has not been established.

Itraconazole is not used with following medications: terfenadine (Seldane), cisapride (Propulsid), astemizole (Hismanal), triazolam (Halcion) or midazolam (Versed).

PREGNANCY: There are no studies in pregnant women. Therefore, itraconazole is used for the treatment of systemic fungal infections in pregnancy only if it is felt that the benefit outweighs the potential risk. Itraconazole is not, however, used for the treatment of isolated onychomycosis (local fungal nail infections) in pregnant women or for those contemplating pregnancy.

NURSING MOTHERS: Itraconazole is excreted in human milk and therefore should not be administered to nursing women.

SIDE EFFECTS: The most common side effects of itraconazole are minor and include nausea, vomiting, diarrhea, rash, edema, fatigue, dizziness. Less common but more serious side effects are liver enzyme elevation, hepatitis, and high blood pressure (hypertension).


Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.

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SPORANOX - ORUNGAL
Generic name: Itraconazole
Manufacturer: Janssen-Cilag


Dosage
Packing
Price
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100 mg
15 tab
USD 75.00
100 mg
28 tab
USD 137.00
 

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