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standards of non-Merck sources.
ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section and/or refer to product labeling for additional detail.
Medication Safety Issues
Sound-alike/look-alike issues:
Kuric™ may be confused with Carac®
Nizoral® may be confused with Nasarel®, Neoral®, Nitrol®
Pronunciation
(kee toe KOE na zole)
U.S. Brand Names
Generic Available
Yes: Cream, shampoo, tablet
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Systemic: Treatment of susceptible fungal infections, including candidiasis, oral thrush, blastomycosis, histoplasmosis, paracoccidioidomycosis, coccidioidomycosis, chromomycosis, candiduria, chronic mucocutaneous candidiasis, as well as certain recalcitrant cutaneous dermatophytoses
Topical:
Cream: Treatment of tinea corporis, tinea cruris, tinea versicolor, cutaneous candidiasis, seborrheic dermatitis
Foam, gel: Treatment of seborrheic dermatitis
Shampoo: Treatment of dandruff, seborrheic dermatitis, tinea versicolor
Use: Dental
Treatment of susceptible fungal infections in the oral cavity including candidiasis, oral thrush, and chronic mucocutaneous candidiasis
Use: Unlabeled/Investigational
Tablet: Treatment of prostate cancer (androgen synthesis inhibitor)
Pregnancy Risk Factor
C
Pregnancy Considerations
Teratogenic effects were noted in animal studies. There are no adequate and well-controlled studies in pregnant women.
Lactation
Enters breast milk/not recommended
Contraindications
Hypersensitivity to ketoconazole or any component of the formulation; CNS fungal infections (due to poor CNS penetration); coadministration with ergot derivatives or cisapride is contraindicated due to risk of potentially fatal cardiac arrhythmias
Warnings/Precautions
Boxed warnings:
• Cisapride: See“Concurrent drug therapy issues” below.
• Hepatic impairment: See “Disease-related concerns” below.
Concerns related to adverse effects:
• Adrenal suppression: High doses of ketoconazole may depress adrenocortical function.
Disease-related concerns:
• Hepatic impairment: [U.S. Boxed Warning]: Ketoconazole has been associated with hepatotoxicity, including some fatalities; use with caution in patients with pre-existing hepatic impairment; monitor liver function closely and dosage adjustment may be warranted.
Concurrent drug therapy issues:
• Cisapride: [U.S. Boxed Warning]:
Concomitant use with cisapride is contraindicated due to the occurrence of ventricular arrhythmias.
Dosage form specific issues:
• Foam: Formulation contains alcohol and propane/butane; do not expose to open flame or smoking during or immediately after application. Do not puncture or incinerate container.
• Topical: Formulations may contain sulfites. Avoid exposure of gel to open flames during or immediately after application.
Adverse Reactions
Oral:
1% to 10%:
Dermatologic: Pruritus (2%)
Gastrointestinal: Nausea/vomiting (3% to 10%), abdominal pain (1%)
<1%: Bulging fontanelles, chills, depression, diarrhea, dizziness, fever, gynecomastia, headache, hemolytic anemia, hepatotoxicity, impotence, leukopenia, photophobia, somnolence, thrombocytopenia
Topical cream/gel: Allergic reaction, contact dermatitis (possibly related to sulfites or propylene glycol), facial swelling, headache, impetigo, local burning, ocular irritation, paresthesia, pruritus, severe irritation, stinging (?5%)
Topical foam: Application site burning (10%), application site reaction (6%), contact sensitization, dryness, erythema, pruritus, rash
Shampoo: Abnormal hair texture, hair loss increase, irritation (<1%), itching, mild dryness of skin, oiliness/dryness of hair, scalp pustules
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Inhibits CYP1A2 (strong), 2A6 (moderate), 2B6 (weak), 2C8 (weak), 2C9 (strong), 2C19 (moderate), 2D6 (moderate), 3A4 (strong)
Drug Interactions
Alfentanil: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Alfentanil. Risk D: Consider therapy modification
Alfuzosin: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alfuzosin. Risk X: Avoid combination
Aliskiren: Ketoconazole may increase the serum concentration of Aliskiren. Risk C: Monitor therapy
Almotriptan: Ketoconazole may increase the serum concentration of Almotriptan. Risk C: Monitor therapy
Alosetron: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron. Risk C: Monitor therapy
Antacids: May decrease the absorption of Antifungal Agents (Azole Derivatives, Systemic). Risk D: Consider therapy modification
Aprepitant: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Aprepitant. Risk C: Monitor therapy
Bendamustine: CYP1A2 Inhibitors (Strong) may increase the serum concentration of Bendamustine. Concentrations of the active metabolites of bendamustine may be decreased. Risk C: Monitor therapy
Benzodiazepines (metabolized by oxidation): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Benzodiazepines (metabolized by oxidation). Exceptions: Quazepam. Risk D: Consider therapy modification
Bosentan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Bosentan. Risk C: Monitor therapy
BusPIRone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of BusPIRone. Risk D: Consider therapy modification
Busulfan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Busulfan. Risk C: Monitor therapy
Calcium Channel Blockers: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Exceptions: Clevidipine. Risk D: Consider therapy modification
CarBAMazepine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of CarBAMazepine. Risk C: Monitor therapy
Cardiac Glycosides: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Cardiac Glycosides. Risk D: Consider therapy modification
Ciclesonide: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ciclesonide. Specifically, concentrations of the active des-ciclesonide metabolite may be increased. Risk C: Monitor therapy
Cilostazol: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Cilostazol. Risk D: Consider therapy modification
Cinacalcet: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Cinacalcet. Risk C: Monitor therapy
Cisapride: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Cisapride. Risk X: Avoid combination
Codeine: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk C: Monitor therapy
Conivaptan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Conivaptan. Risk X: Avoid combination
Corticosteroids (Orally Inhaled): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Corticosteroids (Orally Inhaled). Exceptions: Beclomethasone; Flunisolide; Triamcinolone. Risk C: Monitor therapy
Corticosteroids (Systemic): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
CycloSPORINE: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of CycloSPORINE. Risk D: Consider therapy modification
CYP1A2 Substrates: CYP1A2 Inhibitors (Strong) may decrease the metabolism of CYP1A2 Substrates. Risk D: Consider therapy modification
CYP2A6 Substrates: CYP2A6 Inhibitors (Moderate) may decrease the metabolism of CYP2A6 Substrates. Risk C: Monitor therapy
CYP2C19 Substrates: CYP2C19 Inhibitors (Moderate) may decrease the metabolism of CYP2C19 Substrates. Risk C: Monitor therapy
CYP2C9 Substrates (High risk): CYP2C9 Inhibitors (Strong) may decrease the metabolism of CYP2C9 Substrates (High risk). Risk D: Consider therapy modification
CYP2D6 Substrates: CYP2D6 Inhibitors (Moderate) may decrease the metabolism of CYP2D6 Substrates. Exceptions: Tamoxifen. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Substrates: CYP3A4 Inhibitors (Strong) may decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dabigatran Etexilate: P-Glycoprotein Inhibitors may increase the serum concentration of Dabigatran Etexilate. Risk X: Avoid combination
Didanosine: May decrease the absorption of Antifungal Agents (Azole Derivatives, Systemic). Enteric coated didanosine capsules are not expected to affect these antifungals. Risk D: Consider therapy modification
Docetaxel: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Docetaxel. Risk D: Consider therapy modification
Dofetilide: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Dofetilide. Risk X: Avoid combination
Eletriptan: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Eletriptan. Risk D: Consider therapy modification
Eplerenone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Eplerenone. Risk D: Consider therapy modification
Erlotinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Erlotinib. Risk C: Monitor therapy
Eszopiclone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Eszopiclone. Risk C: Monitor therapy
Fexofenadine: Ketoconazole may increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
Fosaprepitant: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Fosaprepitant. Specifically, concentrations of aprepitant are likely to be increased. Risk C: Monitor therapy
Gefitinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Gefitinib. Risk C: Monitor therapy
Grapefruit Juice: May increase the metabolism of Antifungal Agents (Azole Derivatives, Systemic). This specifically applies to oral antifungal administration. Risk D: Consider therapy modification
H2-Antagonists: May decrease the absorption of Antifungal Agents (Azole Derivatives, Systemic). Risk D: Consider therapy modification
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
HMG-CoA Reductase Inhibitors: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of HMG-CoA Reductase Inhibitors. Exceptions: Fluvastatin; Rosuvastatin. Risk D: Consider therapy modification
Imatinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Imatinib. Risk C: Monitor therapy
Irinotecan: Antifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Irinotecan. Risk D: Consider therapy modification
Ixabepilone: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ixabepilone. Risk D: Consider therapy modification
Losartan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Losartan. Risk C: Monitor therapy
Macrolide Antibiotics: May decrease the metabolism of Antifungal Agents (Azole Derivatives, Systemic). Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Macrolide Antibiotics. Exceptions: Azithromycin; Dirithromycin [Off Market]; Spiramycin. Risk D: Consider therapy modification
Maraviroc: CYP3A4 Inhibitors may increase the serum concentration of Maraviroc. Risk D: Consider therapy modification
Methadone: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Methadone. Risk C: Monitor therapy
Nebivolol: CYP2D6 Inhibitors (Moderate) may increase the serum concentration of Nebivolol. Risk C: Monitor therapy
Nilotinib: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nilotinib. Risk X: Avoid combination
P-Glycoprotein Substrates: P-Glycoprotein Inhibitors may increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Phenytoin: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Phenytoin. Phenytoin may decrease the serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Risk D: Consider therapy modification
Phosphodiesterase 5 Inhibitors: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Phosphodiesterase 5 Inhibitors. Risk D: Consider therapy modification
Pimecrolimus: CYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy
Pimozide: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Pimozide. Risk X: Avoid combination
Praziquantel: Ketoconazole may increase the serum concentration of Praziquantel. Management: Praziquantel dose may need to be reduced when used with ketoconazole. Risk D: Consider therapy modification
Protease Inhibitors: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Protease Inhibitors. Protease Inhibitors may increase the serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Management: Limit indinavir to 600mg every 8 hours with itraconazole or ketoconazole. When used with ritonavir, limit ketoconazole to 200mg/day. Tipranavir labeling recommends limiting fluconazole, itraconazole, and ketoconazole to 200mg with tipranavir/ritonavir. Risk D: Consider therapy modification
Proton Pump Inhibitors: May decrease the absorption of Antifungal Agents (Azole Derivatives, Systemic). Risk D: Consider therapy modification
QuiNIDine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of QuiNIDine. Management: Itraconazole, voriconazole, and posaconazole are specifically contraindicated with quinidine. Use of quinidine with any azole antifungal may require quinidine dose adjustment and should be done with caution and close monitoring. Risk X: Avoid combination
Ramelteon: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ramelteon. Risk C: Monitor therapy
Ranolazine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ranolazine. Risk X: Avoid combination
Repaglinide: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Repaglinide. Management: Concurrent use of an azole antifungal with both repaglinide and gemfibrozil should be avoided. Risk C: Monitor therapy
Rifamycin Derivatives: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Rifamycin Derivatives. Only rifabutin appears to be affected. Rifamycin Derivatives may decrease the serum concentration of Antifungal Agents (Azole Derivatives, Systemic). Risk D: Consider therapy modification
Saccharomyces boulardii: Antifungal Agents may diminish the therapeutic effect of Saccharomyces boulardii. Risk D: Consider therapy modification
Salmeterol: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol. Risk X: Avoid combination
Sirolimus: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Sirolimus. Management: Sirolimus dose reductions of up to 50-90% may be necessary when starting an azole antifungal. Use of sirolimus with the azole antifungals voriconazole and posaconazole is contraindicated. Risk D: Consider therapy modification
Solifenacin: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Solifenacin. Risk D: Consider therapy modification
Sorafenib: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sorafenib. Risk C: Monitor therapy
Sucralfate: May decrease the absorption of Antifungal Agents (Azole Derivatives, Systemic). Risk C: Monitor therapy
Sunitinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Sunitinib. Risk D: Consider therapy modification
Tacrolimus: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Tacrolimus. Risk D: Consider therapy modification
Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease the metabolism of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the formation of highly potent active metabolites. Risk D: Consider therapy modification
Temsirolimus: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Temsirolimus. Concentrations of the active metabolite, sirolimus, are likely to be increased more substantially than those of the parent temsirolimus. Risk D: Consider therapy modification
Thioridazine: CYP2D6 Inhibitors may decrease the metabolism of Thioridazine. Risk X: Avoid combination
Tolterodine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Tolterodine. This is likely only of concern in CYP2D6-deficient patients (ie, "poor metabolizers") Risk D: Consider therapy modification
Topotecan: P-Glycoprotein Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
TraMADol: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy
VinCRIStine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of VinCRIStine. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Vitamin K Antagonists. Risk D: Consider therapy modification
Ziprasidone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ziprasidone. Risk C: Monitor therapy
Zolpidem: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Zolpidem. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Food: Ketoconazole peak serum levels may be prolonged if taken with food.
Herb/Nutraceutical: St John's wort may decrease ketoconazole levels.
Storage
Cream: Store at <25°C (<77°F).
Foam: Store at 20°C to 25°C (68°F to 77°F). Do not refrigerate. Do not store in direct sunlight. Contents are flammable.
Gel: Store at 15°C to 30°C (59°F to 86°F).
Shampoo: Store between 2°C to 30°C (35°F to 86°F); protect from freezing. Protect from light.
Tablet: Store at 15°C to 25°C (59°F to 77°F).
Mechanism of Action
Alters the permeability of the cell wall by blocking fungal cytochrome P450; inhibits biosynthesis of triglycerides and phospholipids by fungi; inhibits several fungal enzymes that results in a build-up of toxic concentrations of hydrogen peroxide; also inhibits androgen synthesis
Pharmacodynamics/Kinetics
Absorption: Oral: Rapid (?75%); Shampoo: None; Gel: Minimal
Distribution: Well into inflamed joint fluid, saliva, bile, urine, breast milk, sebum, cerumen, feces, tendons, skin and soft tissue, and testes; crosses blood-brain barrier poorly; only negligible amounts reach CSF
Protein binding: 93% to 96%
Metabolism: Partially hepatic via CYP3A4 to inactive compounds
Bioavailability: Decreases as gastric pH increases
Half-life elimination: Biphasic: Initial: 2 hours; Terminal: 8 hours
Time to peak, serum: 1-2 hours
Excretion: Feces (57%); urine (13%)
Dosage
Oral:
Fungal infections:
Children ?2 years: 3.3-6.6 mg/kg/day as a single dose for 1-2 weeks for candidiasis, for at least 4 weeks in recalcitrant dermatophyte infections, and for up to 6 months for other systemic mycoses
Adults: 200-400 mg/day as a single daily dose for durations as stated above
Prostate cancer (unlabeled use): Adults: 400 mg 3 times/day
Shampoo: Seborrheic dermatitis, tinea versicolor: Children ?12 years and Adults: Apply twice weekly for 4 weeks with at least 3 days between each shampoo
Topical:
Tinea infections: Adults: Cream: Rub gently into the affected area once daily. Duration of treatment: Tinea corporis, cruris: 2 weeks; tinea pedis: 6 weeks
Seborrheic dermatitis: Children ?12 years and Adults:
Cream: Rub gently into the affected area twice daily for 4 weeks or until clinical response is noted
Foam: Apply to affected area twice daily for 4 weeks
Gel: Rub gently into the affected area once daily for 2 weeks
Dosing adjustment in hepatic impairment: Dose reductions should be considered in patients with severe liver disease
Hemodialysis: Not dialyzable (0% to 5%)
Dosage: Combination Regimens
Prostate cancer:
Doxorubicin + Ketoconazole
Doxorubicin + Ketoconazole/Estramustine + Vinblastine
Dental Usual Dosing
Oral fungal infections: Oral:
Children ?2 years: 3.3-6.6 mg/kg/day as a single dose for 1-2 weeks for candidiasis, for at least 4 weeks in recalcitrant dermatophyte infections, and for up to 6 months for other systemic mycoses
Adults: 200-400 mg/day as a single daily dose for durations as stated above
Administration: Oral
Administer oral tablets 2 hours prior to antacids to prevent decreased absorption due to the high pH of gastric contents.
Administration: Topical
Cream, foam, gel, and shampoo are for external use only. Avoid exposure to flame or smoking immediately following application of gel or foam; do not apply directly to hands.
Monitoring Parameters
Liver function tests
Dietary Considerations
Tablet: May be taken with food or milk to decrease GI adverse effects.
Patient Education
Do not take any new prescription or OTC medications or herbal products during therapy without consulting prescriber. Oral formulations may be taken with food, at least 2 hours before any antacids. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. Cream, foam, gel, and shampoo are for external use only. Use full course of medication as directed; some infections may require long periods of therapy. If you have diabetes, test serum glucose regularly; may impact effectiveness of oral hypoglycemics. May cause nausea and vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). Report unresolved headache, rash or itching, yellowing of eyes or skin, changes in color of urine or stool, chest pain or palpitations, sense of fullness or ringing in ears, or if condition worsens. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.
Cream, foam, and gel: Apply exactly as directed. Wash hands thoroughly before and after applying; keep away from eyes or mouth. Keep Extina foam can away from open fire, flame, or direct heat (Extina foam is flammable). You may experience some burning, dryness, irritation, or rash at site of application. Report severe or persistent adverse effects or if condition worsens.
Shampoo: Use as directed. May cause some temporary hair loss, scalp irritation, itching, or change in hair texture. Report severe or persistent adverse effects or if condition worsens.
Geriatric Considerations
No specific recommendations.
Cardiovascular Considerations
Ketoconazole may increase cyclosporine levels by up to 50% at high doses. It may also potentiate the anticoagulant effect of warfarin and can increase lovastatin and simvastatin levels. Concomitant administration with cisapride is contraindicated.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness, dizziness, or depression
Mental Health: Effects on Psychiatric Treatment
May cause leukopenia; use caution with clozapine and carbamazepine
Nursing: Physical Assessment/Monitoring
Evaluate hepatic function prior to beginning therapy. Assess potential for interactions with other pharmacological agents or herbal products patient may be taking (eg, anything that reduces gastric acidity may result in treatment failures with ketoconazole, concurrent use of ergot derivatives or cisapride increases the risk of potentially fatal cardiac arrhythmias, oral contraceptive efficacy may be reduced). Assess liver function, therapeutic effect (resolution of viral infection), and adverse reactions on a regular basis. Instruct patients with diabetes to monitor glucose levels closely; may impact effectiveness of oral hypoglycemics. Teach patient proper use (administration or application) and necessity of completing full therapy, possible side effects/appropriate interventions (eg, importance of adequate hydration), and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Aerosol, topical [foam]:
Extina®: 2% (50 g, 100 g)
Cream, topical: 2% (15 g, 30 g, 60 g)
Kuric™: 2%: (75 g)
Gel, topical:
Xolegel™: 2% (15 g) [contains dehydrated alcohol 34%]
Shampoo, topical: 1% (120 mL), 2% (120 mL)
Nizoral®: 2% (120 mL)
Nizoral® A-D: 1% (120 mL, 210 mL)
Tablet: 200 mg
Pricing: U.S. (www.drugstore.com)
Cream (Kuric)
2% (25): $45.99
2% (75): $92.77
Foam (Extina)
2% (100): $296.98
Shampoo (Ketoconazole)
2% (120): $27.98
Shampoo (Nizoral)
2% (120): $37.99
Tablets (Ketoconazole)
200 mg (14): $30.99
Tablets (Nizoral)
200 mg (14): $64.27
Extemporaneously Prepared
A 20 mg/mL suspension may be made by pulverizing twelve 200 mg ketoconazole tablets to a fine powder; add 40 mL Ora-Plus® in small portions with thorough mixing; incorporate Ora-Sweet® to make a final volume of 120 mL and mix thoroughly; refrigerate (no stability information is available)
Allen LV, “Ketoconazole Oral Suspension,” US Pharm, 1993, 18(2):98-9, 101.
References
Como JA and Dismukes WE, “Oral Azole Drugs as Systemic Antifungal Therapy,” N Engl J Med, 1994, 330(4):263-72.
Ginsburg AM, McCracken GH Jr, and Olsen K, “Pharmacology of Ketoconazole Suspension in Infants and Children,” Antimicrob Agents Chemother, 1983, 23(5):787-9.
Gorman SE, Dela Cruz F, and Paloucek F, “Ketoconazole and Zidovudine Overdose,” Am J Emerg Med, 1995, 13(1):115-6.
Greenblatt DJ, von Moltke LL, Harmatz JS, et al, “Interaction of Triazolam and Ketoconazole,” Lancet, 1995, 345(8943):191.
Herrod HG, “Chronic Mucocutaneous Candidiasis in Childhood and Complications of non-Candida Infection: A Report of the Pediatric Immunodeficiency Collaborative Study Group,” J Pediatr, 1990, 116(3):377-82.
Hwang WL, Gau JP, Young JH, et al, “Ketoconazole and High-Dose Methylprednisolone Predisposing to Cyclosporine-Induced Seizures: A Report of Three Cases,” Acta Haematol, 1992, 88(2-3):139-41.
Janssen PA and Symoens JE, “Hepatic Reactions During Ketoconazole Treatment,” Am J Med, 1983, 74(1B):80-5.
Lyman CA and Walsh TJ, “Systemically Administered Antifungal Agents. A Review of Their Clinical Pharmacology and Therapeutic Applications,” Drugs, 1992, 44(1):9-35.
Small EJ, Halabi S, Dawson NA, et al, “Antiandrogen Withdrawal Alone or in Combination With Ketoconazole in Androgen-Independent Prostate Cancer Patients: A Phase III Trial (CALGB 9583),” J Clin Oncol, 2004, 22(6):1025-33.
Terrell CL, “Antifungal Agents. Part II. The Azoles,” Mayo Clin Proc, 1999, 74(1):78-100.
Trachtenberg J and Pont A, “Ketoconazole Therapy for Advanced Prostate Cancer,” Lancet, 1984, (8400):433-5.
Varhe A, Olkkola KT, and Neuvonen PJ, “Oral Triazolam Is Potentially Hazardous to Patients Receiving Systemic Antimycotics Ketoconazole or Itraconazole,” Clin Pharmacol Ther, 1994, 56(6 Pt 1):601-7.
Wynn RL, “Erythromycin and Ketoconazole (Nizoral®) Associated With Terfenadine (Seldane®)-Induced Ventricular Arrhythmias,” Gen Dent, 1993, 41(1):27-9.
International Brand Names
Lexi-Comp.com
Last full review/revision September 2008
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