K

ketoconazole

kee-toe-kon-a-zol

(Apo-Ketoconazole , Extina, Nizoral, Nizoral AD, Novo-Ketoconazole , Xolegel)

BLACK BOX ALERT Potentially fatal hepatotoxicity has occurred. Concurrent cisapride, terfenadine, astemizole contraindicated; serious cardiovascular events (QT prolongation, torsade de pointes, ventricular tachycardia, ventricular fibrillation, fatalities) have occurred.

Do not confuse Nizoral with Nasarel, Neoral, or Nitrol.

classification

PHARMACOTHERAPEUTIC: Imidazole derivative. CLINICAL: Antifungal (see pp. 48C, 49C).

Action

Inhibits synthesis of ergosterol, a vital component of fungal cell formation. Therapeutic Effect: Damages fungal cell membrane, altering its function. Fungistatic.

Pharmacokinetics

Well absorbed from GI tract following PO administration. Protein binding: 93%–96%. Metabolized in liver. Primarily excreted in bile with minimal elimination in urine. Negligible systemic absorption following topical absorption. Ketoconazole is not detected in plasma after shampooing, topical administration. Half-life: 8 hrs.

Uses

PO: Treatment of susceptible fungal infections including histoplasmosis, blastomycosis, candidiasis, chronic mucocutaneous candidiasis, coccidioidomycosis, paracoccidioidomycosis, chromomycosis, oral thrush, candiduria. Shampoo: Treatment of dandruff. Treatment of tinea versicolor. Topical: Treatment of tineas, pityriasis versicolor, cutaneous candidiasis, seborrhea dermatitis, dandruff. Xolegel: Treatment of seborrheic dermatitis. OFF-LABEL: Systemic: Treatment of prostate cancer.

Precautions

Contraindications: Concurrent use with ergot derivatives, triazolam, CNS fungal infections. Cautions: Hepatic impairment.

 ​Lifespan considerations

Pregnancy/Lactation: Oral form distributed in breast milk. Unknown if topical form crosses placenta or is distributed in breast milk. Pregnancy Category C. Children: Cream, shampoo: Safety and efficacy not established. Oral form: Safety and efficacy not established in those younger than 2 yrs. Elderly: No age-related precautions noted.

Interactions

DRUG: May increase concentration/toxicity of cyclosporine, digoxin, ergot alkaloids, midazolam, protease inhibitors (e.g., indinavir, ritonavir, saquinavir), sirolimus, tacrolimus, triazolam, warfarin. Isoniazid, rifampin may decrease concentration/effects. Antacids, H₂ antagonists, proton pump inhibitors (e.g., omeprazole) may decrease absorption. HERBAL: St. John’s wort may decrease concentration. FOOD: None known. LAB VALUES: May increase serum alkaline phosphatase, bilirubin, AST, ALT. May decrease serum corticosteroid, testosterone.

Availability (Rx)

Foam (Extina): 2%. Gel (Xolegel): 2%. Shampoo (Nizoral AD [OTC]): 1%. Tablets (Nizoral): 200 mg.

Administration/handling

PO

• Give with food to minimize GI irritation. • Tablets may be crushed. • Ketoconazole requires acidity; give antacids, anticholinergics, H₂ blockers at least 2 hrs following dosing.

Shampoo

• Apply to wet hair, massage for 1 min, rinse thoroughly, reapply for 3 min, rinse.

Topical

• Apply, rub gently into affected/surrounding area.

Indications/routes/dosage

Usual dosage

PO: ADULTS, ELDERLY: 200–400 mg/day. Maximum: 800 mg/day in 2 divided doses. CHILDREN 2 YRS AND OLDER: 3.3–6.6 mg/kg/day.

Topical: ADULTS, ELDERLY: Apply to affected area 1–2 times a day for 2–4 wks.

Shampoo: ADULTS, ELDERLY: Use twice weekly for 4 wks, allowing at least 3 days between shampooing. Use intermittently to maintain control.

Side effects

Occasional (10%–3%): Nausea, vomiting. Rare (less than 2%): Abdominal pain, diarrhea, headache, dizziness, photophobia. Topical: Burning, irritation, pruritus.

Adverse effects/toxic reactions

Hematologic toxicity (thrombocytopenia, hemolytic anemia, leukopenia) occurs occasionally. Hepatotoxicity may occur within first wk to several mos after starting therapy. Anaphylaxis occurs rarely.

Nursing considerations

Baseline assessment

Confirm culture or histologic test for accurate diagnosis; therapy may begin before results known. Receive full medication history and screen for contraindications.

Intervention/evaluation

Monitor hepatic function tests; be alert for hepatotoxicity: dark urine, pale stools, jaundice, fatigue, anorexia, nausea, or vomiting (unrelieved by giving medication with food). Monitor CBC for hematologic toxicity. Monitor daily pattern of bowel activity, stool consistency. Assess for dizziness, provide assistance as needed. Evaluate skin for rash, urticaria, pruritus. Topical: Check for localized burning, pruritus, irritation.

Patient/family teaching

• Prolonged therapy (wks or mos) is usually necessary. • Avoid alcohol. • May cause dizziness; avoid tasks that require alertness, motor skills until response to drug is established. • Take antacids, antiulcer medications at least 2 hrs after ketoconazole. • Report dark urine, pale stool, yellow skin or eyes, vomiting, increased irritation in topical use, onset of other new symptoms. • Topical: Rub well into affected areas. • Avoid contact with eyes. • Keep skin clean, dry; wear light clothing for ventilation. • Separate personal items in direct contact with affected area. • Shampoo: Initially, use 2 times a wk for 4 wks with at least 3 days between shampooing; frequency then determined by response to medication.

ketoprofen

kee-toe-proe-fen

(Apo-Keto )

BLACK BOX ALERT Increased risk of serious cardiovascular thrombotic events, including myocardial infarction, CVA. Increased risk of severe GI reactions, including ulceration, bleeding, perforation.

classification

PHARMACOTHERAPEUTIC: NSAID. CLINICAL: Antirheumatic, analgesic, antidysmenorrheal, vascular headache suppressant (see p. 130C).

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