Itraconazole, effect

Toxicological studies have demonstrated that there are no important problems with fluconazole. Therapeutic doses of fluconazole may cause enzyme induction in the Hver. This suggests that interactions with other dmgs cannot be excluded. The side effects are similar to those of itraconazole and include nausea, headache, and vertigo. Occasionally, increased Hver enzymes may be noted. Like itraconazole, fluconazole is contraindicated during pregnancy. 

The effects of buspirone are decreased when the drug is administered with fluoxetine Increased serum levels of buspirone occur if the drug is taken with erythromycin or itraconazole Should any of these combinations be required, the dosage of buspirone is decreased to 2.5 mg BID, and the patient is monitored closely. Venlafaxine blood levels increase with a risk of toxicity when administered witii MAOIs or cimetidine There is an increased risk of toxicity when trazodone is administered with the phenothiazines and decreased effectiveness of trazodone when it is administered with carbamazepine Increased serum digoxin levels have occurred when digoxin is administered with trazodone There is a risk for increased phenytoin levels when phenytoin is administered witii trazodone... 

Theoretically buprenorphine metabolism could be inhibited by itraconazole, ketoconazole, grapefruit juice, and erythromycin or any other CYP3A4 inhibitor the effects may be greater than expected for the dose of buprenorphine being given may need to decrease buprenorphine dose. 

Buspirone generally is well tolerated and does not cause sedation. Most common side effects include dizziness, nausea, and headaches. Drugs that inhibit CYP3A4 (e.g., verapamil, diltiazem, itraconazole, fluvoxamine, nefa-zodone, and erythromycin) can increase buspirone levels. Likewise, enzyme inducers such as rifampin can reduce buspirone levels significantly. Bupirone may increase blood pressure when coadministered with an monoamine oxidase inhibitor (MAOI). 

The goal of treating recurrent WC is control of the infection, rather than cure. First, any acute episodes are treated, followed by maintenance therapy. For the treatment of acute episodes, intravaginal or oral azoles can be utilized. Although acute episodes of recurrent WC will respond to azole therapy, some patients may require prolonged therapy in order to achieve remission. To achieve remission, a second dose of oral fluconazole 150 mg repeated 3 days after the first dose or 14 days of topical azole therapy can be used. The practitioner should consider that non-albicans infections are more common in recurrent WC therefore fluconazole and itraconazole resistance may make these agents less effective. 

Two to three weeks of fluconazole or itraconazole solution are highly effective and demonstrate similar clinical response rates.32 Doses of 100 to 200 mg are effective in immunocompetent patients but doses up to 400 mg are recommended for immunocompromised patients. Due to variable absorption, ketoconazole and itraconazole capsules should be considered second-line therapy. In severe cases, oral azoles may prove ineffective, warranting the use of amphotericin B for 10 days. Although echinocandins and voriconazole are effective in treatment of esophageal candidiasis, experience remains limited. 

Onychomycosis is a chronic infection that rarely remits spontaneously. Adequate treatment is essential to prevent spread to other sites, secondary bacterial infections, cellulitis, or gangrene. Due to the chronic nature and impenetrability of nails, topical agents have low efficacy rates for treating onychomycosis. Oral agents that can penetrate the nail matrix and nail base, such as itraconazole and terbinafine, are more effective than ciclopirox lacquer. Itraconazole and terbinafine demonstrate mycological cure rates of 62%37 and 76%,38 respectively, while ciclopirox has a cure rate of 29% to 36%.39... 

Mild to moderate Observation or itraconazole 200 mg PO Itraconazole is less effective for CNS infections... 

Itraconazole 200 mg PO daily for 6-12 weeks Lipid formulation may be more effective... 

Although more invasive, esophageal candidiasis does not typically evolve into a life-threatening infection. However, topical therapy is ineffective. Azoles (fluconazole, itraconazole solution, or voriconazole), echinocandins, or intravenous amphotericin B (in cases of unresponsive infections) are effective treatment options. Parenteral therapy should be used in patients who are unable to take oral medications.20... 

In patients who have failed initial therapy (i.e., salvage), liposomal amphotericin products, itraconazole, or the echinocandin caspofungin can be used. Itraconazole has a response rate of approximately 40%.100 Oral itraconazole exhibits erratic absorption the IV formulation is suspended in cyclodextrin, which is eliminated renally, and thus IV itraconazole should be avoided in patients with a creatinine clearance of less than 30 mL/minute (0.29 mL/s m2).103 Itraconazole also has negative inotropic cardiac effects and increases the serum concentrations of medications (e.g., cyclophosphamide, etopo-side, calcineurin inhibitors, and sirolimus). 

PPIs are usually well tolerated. Potential adverse effects include headache, dizziness, somnolence, diarrhea, constipation, nausea, and vitamin B12 deficiency. All PPIs can decrease the absorption of drugs such as ketoco-nazole or itraconazole that require an acidic environment for absorption. Other drug interactions vary with each agent. 

Itraconazole and ketoconazole (200-800 mg/day orally for 1 year) are effective in 74% to 86% of cases, but relapses are common fluconazole 200-400 mg daily is less effective (64%) than ketoconazole or itraconazole, and relapses are seen in 29% of responders Severe disease Amphotericin B 0.7 mg/kg/day for a minimum total dose of 35 mj kg is effective in 59% to 100% of cases and should be used in patients who require hospitalization or are unable to take itraconazole because of drug interactions, allergies, failure to absorb drug or failure to improve clinically after a minimum of 12 weeks of itiaconazole therapy... 

Itraconazole, 200 to 400 mg/day, is effective as a first-line agent in the treatment of non-life-threatening, non-CNS blastomycosis. 

Itraconazole is a triazole antifungal causing side-effects, such as nausea, abdominal pain, dizziness and headache. Itraconazole does not lead to palpitations however, it may lead to heart failure and hence itraconazole is administered with caution to patients at risk of heart failure. 

Fluconazole and itraconazole are newer, orally effective triazole derivatives. The topically active allylamine naftidine and the morpholine amorolfine also inhibit ergosterol synthesis, albeit at another step. 

CHF Do not administer itraconazole for the treatment of onychomycosis in patients with evidence of ventricular dysfunction, such as CHF or a history of CHF. Discontinue if signs and symptoms of CHF occur during treatment. If signs and symptoms of CHF occur during treatment, reassess the continued use of itraconazole. When itraconazole was administered IV to dogs and healthy human volunteers, negative inotropic effects were seen. 

Interchangeability Do not use itraconazole capsules and oral solution interchangeably. Drug exposure is greater with the oral solution than with the capsules when the same dose of drug is given. Additionally, the topical effects of mucosal exposure may be different between the two formulations. 

Children Safety and efficacy have not been established. A small number of patients from 3 to 16 years of age have been treated with 100 mg/day for systemic fungal infections and no serious adverse effects have been reported. Itraconazole oral solution was given to 26 pediatric patients 6 months to 12 years of age. Itraconazole was dosed at 5 mg/kg once daily for 2 weeks, and no serious unexpected adverse events were reported. 

Decreased gastric acidity Under fasted conditions, itraconazole absorption was decreased in the presence of decreased gastric acidity. The absorption of itraconazole may be decreased with coadministration of antacids or gastric acid secretion suppressors. Studies conducted under fasted conditions demonstrated that administration with 8 oz of a cola beverage resulted in increased absorption of itraconazole in AIDS patients with relative or absolute achlorhydria. This increase relative to the effects of a full meal is unknown. 

Both itraconazole and its major metabolite, hydroxyitraconazole, are inhibitors of the cytochrome P450 3A4 enzyme system. Coadministration of itraconazole and drugs primarily metabolized by the cytochrome P450 3A4 enzyme system may result in increased plasma concentrations of the drugs that could increase or prolong therapeutic and adverse effects. 

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