Sporanox


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itraconazole

Sporanox

Pharmacologic class: Synthetic triazole

Therapeutic class: Antifungal

Pregnancy risk category C

FDA Box Warning

• Don't administer capsules to treat onychomycosis in patients with evidence of ventricular dysfunction, such as current or previous heart failure. If heart failure signs or symptoms occur during therapy, discontinue drug.

• Concurrent use of cisapride, dofetilide, levacetylmethadol (levomethadyl), pimozide, or quinidine with itraconazole capsules or oral solution is contraindicated. Itraconazole is a potent CYP3A4 inhibitor and may raise blood levels of drugs metabolized by this pathway. Serious cardiovascular events (including QT prolongation, torsades de pointes, ventricular tachycardia, cardiac arrest, and sudden death) have occurred in patients taking these drugs concurrently with itraconazole.

Action

Prevents ergosterol synthesis in fungal cell membranes, altering membrane permeability

Availability

Capsules: 100 mg

Oral solution: 10 mg/ml

Indications and dosages

Aspergillosis; blastomycosis; histoplasmosis

Adults: 200 to 400 mg P.O. daily for at least 3 months until patient is cured. In life-threatening infections, loading dose of 200 mg P.O. t.i.d. for 3 days, then 200 to 400 mg P.O. daily until cured.

Esophageal candidiasis

Adults: 100 to 200 mg of oral solution daily, swished in mouth for several seconds and swallowed, for at least 3 weeks; continue for 2 weeks after symptoms resolve.

Oropharyngeal candidiasis

Adults: 200 mg of oral solution daily, swished in mouth for several seconds and swallowed, for 1 to 2 weeks

Onychomycosis; tinea unguium

Adults: For toenails, 200 mg P.O. daily for 12 weeks. For fingernails, 200 mg b.i.d. for 1 week; wait 3 weeks, then repeat dosage for 1 week.

Contraindications

• Hypersensitivity to drug or its components

• Ventricular dysfunction, congestive heart failure (CHF) or history of CHF (in onychomycosis use)

• Concomitant use of astemizole, cisapride, dofetilide, ergot alkaloids (such as dihydroergotamine, ergonovine, ergotamine, and methylergonovine), lovastatin, midazolam, pimozide, quinidine, simvastatin, or triazolam

• Pregnancy or anticipated pregnancy (in onychomycosis use)

Precautions

Use cautiously in:

• hypersensitivity to other azole derivatives

• renal impairment (with I.V. use), hepatic disorders, achlorhydria, hypochlorhydria

• breastfeeding patients

• children (safety and efficacy not established).

Administration

• Obtain specimens for fungal cultures, as needed, before starting therapy.

• Administer capsule with a full meal.

• Give oral solution without food when possible.

• Be aware that liquid and tablets aren't interchangeable.

Adverse reactions

CNS: dizziness, headache, fatigue, malaise

CV: peripheral edema, tachycardia, heart failure

EENT: rhinitis, transient or permanent hearing loss

GI: nausea, vomiting, constipation, abdominal pain, flatulence, anorexia, dyspepsia, GI bleeding, pancreatitis

GU: albuminuria, erectile dysfunction

Hepatic: jaundice, hepatotoxicity (including hepatic failure and death)

Metabolic: hypokalemia

Musculoskeletal: myalgia, bursitis, rhabdomyolysis

Respiratory: pulmonary edema

Skin: flushing, rash, pruritus, urticaria, increased sweating, herpes zosterinfection

Other: fever, pain

Interactions

Drug-drug. Alfentanil, antihistamines (minimally sedating agents, such as fexofenadine, loratadine), antineoplastics (busulfan, docetaxel, vinca alkaloids), anxiolytics, benzodiazepines, cyclosporine, delavirdine, digoxin, immunosuppressants, methylprednisolone, protease inhibitors, tacrolimus, tolterodine, tretinoin: increased blood levels of these drugs

Amiodarone, anabolic steroids, androgens, antithyroid drugs, carmustine, chloroquine, dantrolene, daunorubicin, disulfiram, estrogens, gold salts, hormonal contraceptives, hydroxychloroquine, mercaptopurine, methotrexate, methyldopa, naltrexone (with long-term use), valproic acid: increased risk of hepatic damage

Amphotericin B: reduced or inhibited amphotericin B effects

Antacids, anticonvulsants, antimycobacterials, cyclobenzaprine, histamine2-receptor blockers, isoniazid, proton pump inhibitors (such as lansoprazole, omeprazole), reverse transcriptase inhibitors, sucralfate: reduced itraconazole blood level

Antipsychotics, antiarrhythmics (such as quinidine, dofetilide), anxiolytics, astemizole, cisapride: increased risk of serious cardiovascular effects

Calcium channel blockers: increased risk of edema, possible increase in itraconazole's effect

Carbamazepine, carbidopa, levodopa: altered blood levels of these drugs

Didanosine, vinblastine, vincristine, xanthine bronchodilators: decreased efficacy of these drugs

Digoxin: increased digoxin blood level, possible digoxin toxicity

HMG-CoA reductase inhibitors, miconazole: inhibited metabolism of these drugs, increased risk of skeletal muscle toxicity (including rhabdomyolysis)

Macrolide antibiotics: increased itraconazole blood level

Oral hypoglycemics: severe blood glucose decrease

Quetiapine, sildenafil: increased efficacy of these drugs

Warfarin: enhanced anticoagulant effect

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, gamma-glutamyltransferase, serum creatinine: increased levels

Potassium, magnesium: decreased levels

Drug-food. Any food, cola: increased itraconazole blood level

Grapefruit juice: decreased blood level and reduced therapeutic effects of itraconazole

Drug-herbs. Chaparral, comfrey, germander, jin bu huan, kava: increased risk of hepatic damage

Drug-behaviors. Alcohol consumption: toxic reaction, hepatic damage

Patient monitoring

• In patient with hepatic dysfunction, monitor hepatic enzyme levels.

Monitor for signs and symptoms of hearing loss, pancreatitis, hepatic dysfunction (jaundice, fatigue, nausea, vomiting, dark urine, pale stools), heart failure, muscle disorder, and pulmonary or peripheral edema.

• Monitor potassium level. Stay alert for hypokalemia.

Patient teaching

• Tell patient he may take capsule with a full meal. If he's using oral solution, advise him to take it without food.

• Inform patient that drug interacts with many other drugs. Advise him to tell all prescribers he's taking it.

Teach patient to recognize and immediately report signs and symptoms of hearing loss, pancreatitis, hepatic dysfunction, persistent muscle pain, and heart failure.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Advise female patient of childbearing potential to use effective contraception during and for 1 month after therapy. Caution her not to breastfeed.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

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Sporanox

(spôr′ə-nŏks′)
A trademark for the drug itraconazole.

Sporanox

A brand name for ITRACONAZOLE.
References in periodicals archive ?
Total systemic exposure over 24 hours (AUC0-24h) and maximum plasma concentration were approximately 85-fold and 250-fold lower compared to AUC0-24h and Cmax following 200 mg of oral Sporanox, respectively.
The best is the oral anti-fungal medicine Sporanox, a medicine available only by prescription.
This myopathy might also be seen with Mevacor and Zocor when erythromycin, Biaxin, Nizoral, Sporanox, cyclosporine, Serzone, protease inhibitors (for AIDS) or grapefruit juice are used with them.
The Department of Health has told GPs to be careful how they prescribe Sporanox and Lamisil - used to treat toe nail fungus - after they were linked with 22 deaths from heart and liver failure.
Drugs affected by levels of stomach acidity like ketoconazole (Nizoral) or itraconazole (Sporanox) should be taken at least 2 hours prior to didanosine.
Ortho Biotech, Inc., Raritan, NJ, announced SPORANOX (itraconazole) Injection is now available for treatment of potentially life-threatening fungal infections, including blatomycosis, histoplasmosis, and aspergillosis in patients who are intolerant of or refractory to amphotericin B, a first line therapy.
It's a hot one, the war against fungus, pitting Lamisil against Janssen Pharmaceutical's Sporanox and Pfizer's Diflucan for shares in a market estimated to be worth hundreds of millions of dollars a year.
"People have seen television ads for Sporanox and are going into their doctors saying 'I've got ugly toenails.
Pharmaceutical anti-fungal drugs like Nystatin, Ketoconazol, Monistat, Lamisil (Terbinafine HCl), Diflucan (Fluconazole), Sporanox (Itraconazole), etc.
For those with unsightly fungal infections of toenails (or fingernails), two new drugs approved by the FDA may spell relief: itraconazole (Sporanox) and terbinafine (Lamisil).
Additionally, summary data for systemic pharmacokinetics from Part 2 following 14 days of daily inhalation of Pulmazole at doses ranging between 10 and 35 mg inhaled itraconazole suggest that total systemic exposure over 24 hours is approximately 100- to 400-fold lower that what would be expected following administration of 200 mg of oral Sporanox. These results support the potential of Pulmazole to improve the safety profile of oral Sporanox, as there is a progressive increase in the probability of toxicity occurring with increasing concentrations of itraconazole after oral administration.
Bayer, Kiel, Germany), and itraconazole (5 mg/kg PO q12h, Sporanox 100-mg capsules, Janssen-Cilag, High Wycombe Bucks, UK) were administered to control and prevent infection.