Extina, Kuric, Nizoral, Nizoral A-D, Xolegel
Classifications: antibiotic; azole antifungal; Therapeutic: azole antifungal antibiotic
Pregnancy Category: C
200 mg tablets; 2% cream; 2% shampoo; 2% foam; 2% gel
Fungistatic; may also be fungicidal depending on concentration. Interferes with formation of ergosterol, the principal sterol
in the fungal cell membrane that, when depleted, interrupts membrane function by increasing its permeability.
Antifungal properties are related to the drug effect on the fungal cell membrane functioning.
OralSevere systemic fungal infections including candidiasis (e.g., oral thrush, candiduria), chronic mucocutaneous candidiasis,
pulmonary and disseminated coccidioidomycosis, histoplasmosis, paracoccidioidomycosis, blastomycosis, and chromomycosis.
TopicalTinea corporis and tinea cruris (caused by Epidermophyton floccosum, Trichophyton mentagrophytes, and Trichophyton rubrum) and in treatment of tinea versicolor (pityriasis) caused by Malassezia furfur (Pityrosporum obiculare), seborrheic dermatitis.
OralOnychomycosis, vaginal candidiasis, Cushing's syndrome associated with adrenal or pituitary adenoma; precocious puberty,
dysfunctional hirsutism, and as swish and swallow preparation for prophylaxis against fungal infections in patients with
neutropenia induced by cancer chemotherapy and in patients with AIDS.
Hypersensitivity to ketoconazole or any component in the formulation; chronic alcoholism, fungal meningitis; onychomycosis;
ocular exposure, ophthalmic administration; pregnancy (category C).
Azole antifungal hypersensitivity; achlorhydria, hypochlorhydria; history of hepatic disease, HIV infection; alcoholism;
azole antifungal hypersensitivity. Safe use in children <2 y is not established.
Route & Dosage
Adult: PO 200400 mg once/d Topical Apply 12 times/d to affected area and surrounding skin
Child (>2 y): PO 3.36.6 mg/kg/d as single dose
Adult/Child: Topical Shampoo twice a week for 4 wk with at least 3 d between shampoos Topical (Extina) Apply b.i.d. x 4 wk (Xolegel) Apply q.d. x 2 wk
- Give with water, fruit juice, coffee, or tea; drug requires an acid medium for dissolution and absorption.
- Relieve nausea and vomiting during early therapy by taking drug with food and dividing into 2 daily doses.
- Do not give with antacids.
- Store in tightly covered container at 15°30° C (59°86° F) unless otherwise directed.
- Apply sufficient shampoo to produce lather to wash scalp and hair and gently massage over entire scalp area for 1 min, rinse
hair thoroughly and repeat, leaving shampoo on scalp for 3 min. Rinse thoroughly.
Adverse Effects (≥1%)OralBody as a Whole:
Skin rash, erythema
, urticaria, pruritus, angioedema, anaphylaxis. GI: Nausea, vomiting,
anorexia, epigastric or abdominal pain, constipation
, transient elevation in serum
liver enzymes, fatal hepatic necrosis
With high doses, lowers serum testosterone
and ACTH-induced corticosteroid serum
levels, transient decreases in serum
and triglycerides; hyponatremia (rare). Urogenital:
Gynecomastia (males), breast pain; uterine bleeding, loss of libido, impotence, oligospermia, hair loss. Other: Acute hypoadrenalism (reduction of adrenal stress syndrome), renal hypofunction. TopicalSkin:
Mild transient erythema
, severe irritation, pruritus, stinging.
may cause sunburnlike reaction; antacids
, h2-receptor antagonists
decrease ketoconazole absorption; isoniazid, rifampin
increase ketoconazole metabolism
, thus decreasing its activity; levels of phenytoin
and ketoconazole decreased; may increase levels of cyclosporine
increasing the risk of toxicity
may potentiate hypoprothrombinemia; may increase ergotamine toxicity
of dihydroergotamine, ergotamine;
may increase concentration and toxicity
of trazodone. Herbal: Echinacea
may increase risk of hepatotoxicity.
Erratically from GI tract (needs an acid pH); minimal absorption topically. Peak:
12 h. Distribution:
Distributed to saliva, urine, sebum, and cerumen; CSF levels unpredictable; distributed into breast milk. Metabolism:
In liver (CYP3A4). Elimination:
Primarily in feces, 13% in urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Monitor baseline liver function tests (AST, ALT, alkaline phosphatase, and bilirubin) and repeat at least monthly
- Monitor for S&S of hepatotoxicity (see Appendix F). Discontinue drug immediately to prevent irreversible liver damage and
report to physician.
Patient & Family Education
- Report S&S of hepatotoxicity promptly to physician (see Appendix F).
- Note: Drowsiness and dizziness are early and time-limited adverse effects.
- Do not drive or engage in potentially hazardous activities until response to drug is known.
- Avoid OTC drugs for gastric distress, such as Rolaids, Tums, Alka-Seltzer and check with physician before taking any other
- Do not alter dose or dose interval and do not stop taking ketoconazole before consulting the physician.
- Notify physician if skin condition fails to respond to topical therapy or worsens or if signs of irritation or sensitivity