Itraconazole

Itraconazole is a broad-spectrum antifungal agent for oral treatment of vulvovaginal candidiasis, pityriasis versicolor and dermatophytoses.itraconazole is a substituted triazole derivetive.itraconazoleactive against many Candida species, endemic mycoses and dermatophytes. Itraconazole is the most potent of available azoles, but effectiveness can be limited by reduced bioavailabilty. The requirement for intravenous administration and the toxicity of the older antifungal agents created a need for antifungal agents with a better therapeutic profile. The relatively non-toxic oral azole medications represent the first major advance in this direction. Since their introduction in the 1980s, these medications have played an increasingly important role in the systemic therapy of fungal disease.

Brands
SPORANOX ITRACON ITRAZOLE ITRACAP ROLAC ITRA ITRANEX VIGILANT ICON ITAZOL SOPRAZOLE ITROFIT ORACONE TRACONOL ITRDYM IT CAP ITROP ITRAVAL TRUCON ITRAL ITROPAN ITROTEK SPOROCID ITRADERM ITRANEU ITRAZOX SPOROKIL
Adult Dose
Dose: 200 mg
Single Dose: 200 (200)
Frequency: 24 hourly
Route: PO
Instructions: For a Week
Neonatal
Paedriatic
Dose:
Single Dose:
Frequency:
Route:
Instructions: Not recommended in this age group
Characteristics
Itraconazole also known as Oriconazole. . It is of Synthetic origin and belongs to Triazole. It belongs to Antifungals pharmacological group.The Molecular Weight of Itraconazole is 705.60. Its pKa is 3-4.
Contraindications
Itraconazole is contraindicated in conditions like Hypersensitivity.
Effects
The severe or irreversible adverse effects of Itraconazole, which give rise to further complications include Hypotension, Hepatitis, Hypotension.Itraconazole produces potentially life-threatening effects which include Dysrhythrics. which are responsible for the discontinuation of Itraconazole therapy.The symptomatic adverse reactions produced by Itraconazole are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Vertigo, Headache, Fatigue, Nausea, Vomiting, Diarrhea, Abdominal pain, Pruritus, Hallucination, Somnolence, Hair loss, Edema, Photophobia, Vasculitis, dizziness.
Indications
Itraconazole is primarily indicated in conditions like Advanced breast or prostate cancer, Antifungal prophylaxis, Candidiasis, Cryptcoccal meningitis, Dermatophytic infections, Histoplasmosis, Oculomycoses, Onychomycoses, Oral candidiasis, Oropharangeal candidiasis, Orophyrangeal candidiasis, Pityriasis versicolor, Sporotrichosis, Superficial candidiasis, Systemic mycoses, Tinea pedis, Tinae manuum, To reduce intestinal secretions and vomiting, To reduce intestinal secretions and vomiting (palliative care), and can also be given in adjunctive therapy as an alternative drug of choice in Cushing`s syndrome due to malignant disease, Fungal keratitis, Leishmaniasis, Vulvo-vaginal candidosis.
Interactions
Itraconazole is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAfatinibitraconazole may increase the level of afatinib use alternative or reduced doseAliskirenAlprazolamArtesunateConcurrent use may increase artesunate serum concentrations. AstemizoleAstemizoleBosentanPlasma concentration of Bosentan possibly increased by Itraconazole; avoid concomitant use.MajorBuspirone (HCl)BusulphanMetabolism of Busulphan inhibited by Itraconazole (increased risk of toxicity).Calcium Carbonatebinds with drugs or increase pH that effects drug solubilityantacid should not be given within two hours of the dose of these drugsCarbamazepineCarbamazepine possibly reduces plasma concentration of Itraconazole.ModerateCerivastatin SodiumCerivastatin Sodium may have its serum concentration increased by itraconazoleCisaprideCisaprideClorazepate (K)Cyclosporin ACyclosporin ADigoxinItraconazole may increase the serum concentration of digoxin.ModerateDelayedMonitor for increased serum concentrations/toxic effects of digoxin if itraconazole is initiated or the dose is increased.ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinibFelodipineFexofenadineIndinavir (Sulphate)LovastatinMidazolamMizolastineConcurrent use is contraindicated.Mometasone (Furoate)Such combination should not be used with out informing doctors/pharmacists.NizatidineNizatidine may interfere with the absorption of Itraconazole.PhenobarbitonePhenytoin (Na)QuetiapineQuinidineRifampicinRiociguatincrease the level or effects of riociguatclosely monitor/use alternativeRitonavirSaccharomycesItraconazole may inactivate Saccharomyces organisms.It has been recommended that Saccharomyces be administered at least 1 hour before or 2 hours after an antifungal dose.SildenafilClearance of Sildenafil is decreased due to inhibition of CYP450SimvastatinSunitinibmay increases sunitinib concentrations.TerfenadineTolterodine (Tartrate)TriazolamVandetanibItraconazole is a CYP3A4 inhibitor, increases vandetanib plasma exposure about 9%.Itraconazole should be administered at a dose of 400 mg OD.Vincristine (Sulphate)Warfarin (Na) These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Elevated liver enzymes
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Caps Store Between 15°C-30°C. Protect from Sunlight, Moisture and Heat. Soln Store at room temperature, Below 25°C. Do not Freeze. Protect from Sunlight and Heat.
Warnings
Itraconazole should be used with caution in patients with liver disease, heart rhythm disorders (arrhythmias) and of any drug allergies. It should be used with caution while engaging in activities requiring alertness because this medication causes dizziness or drowsiness. It should be used only when clearly needed during pregnancy or lactation. Safe use of itraconazole in the children under the age 16 has not been established. The drug should be used with caution in the patients with azole hypersensitivity. Patients who develop abnormal liver function tests during itraconazole therapy should be monitored and therapy discontinued if symptoms of the liver disease develop. Should not be administered to treat onchonycosis in pateints with ventricular dysfurution.
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