Names and pronunciation
(it-ra-con′a-zol) Onmel , Sporanox, Tolsura
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Individual generic drug information
Extracted information for itraconazole only.
(it-ra-con′a-zol) Onmel , Sporanox, Tolsura
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Func. class.: Antifungal, systemic
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Chem. class.: Triazole derivative
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ACTION: Alters cell membranes; inhibits several fungal enzymes
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USES: Histoplasmosis, blastomycosis (pulmonary and extrapulmonary), aspergillosis, onychomycosis of toenail/ fingernail
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Unlabeled uses: Dermatomycosis, histo- plasmosis, chromoblastomycosis, coccidi- oidomycosis, pityriasis versicolor, sebopso- riasis, vaginal candidiasis, cryptococcus, subcutaneous mycoses, dimorphic infec- tions, fungal keratitis, zygomycosis, superfi- cial mycoses (dermatophytosis), chronic mucocutaneous candidiasis
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Extracted information for itraconazole only.
CONTRAINDICATIONS: Hyper- sensitivity, fungal meningitis; onychomy- cosis or dermatomycosis with cardiac dysfunction, in pregnant women
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Black Box Warning: Heart failure, ven- tricular dysfunction, coadministration with other products Precautions: Pregnancy, breastfeeding, children, cardiac/renal/hepatic disease, achlorhydria or hypochlorhydria (prod- uct-induced), dialysis, hearing loss, cystic fibrosis neuropathy
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SIDE EFFECTS CNS: Headache, dizziness, insomnia, somnolence, depression CV: Hypertension, HF GI: Nausea, vomiting, anorexia, diar rhea, cramps, abdominal pain, flatu- lence, GI bleeding, hepatotoxicity GU: Gynecomastia, impotence, decreased libido INTEG: Pruritus, fever, rash, toxic epi dermal necrolysis, Stevens-Johnson syndrome MISC: Edema, fatigue, malaise, hypoka- lemia, tinnitus, rhabdomyolysis RESP: Rhinitis, sinusitis, upper respira- tory infection, pulmonary edema
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INTERACTIONS • Life-threatening CV reactions—pimo zide, quiNIDine, dofetilide, levomethadyl, dronedarone Increase: tinnitus, hearing loss—qui NIDine Increase: hepatotoxicity—other hepato toxic products Increase: edema—calcium channel blockers Increase: severe hypoglycemia—oral hypoglycemics Increase: sedation—ALPRAZolam, clo- razepate, diazePAM, estazolam, fluraze- pam, triazolam, oral midazolam Increase: levels, toxicity—busPIRone, busulfan, clarithromycin, cycloSPORINE, diazePAM, digoxin, felodipine, fentaNYL, atorvastatin, carBAMazepine, disopyra mide, indinavir, isradipine, niCARdipine, NiFEdipine, niMODipine, phenytoin, quiNI Dine, QUEtiapine, ritonavir, saquinavir, tacrolimus, warfarin Decrease: itraconazole action—antac- ids, H2-receptor antagonists, rifamycins, didanosine, carBAMazepine, isoniazid, proton pump inhibitors Drug/Food • Food increases absorption • Grapefruit juice decreases itracon- azole level Drug/Lab Test Increase: LFTs, alk phos, bilirubin, tri- glyceride, GGT
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Extracted information for itraconazole only.
DOSAGE AND ROUTES Capsules and oral solution are not inter- changeable, oral solution is used only for oral/esophageal candidiasis Pulmonary or disseminated extra- pulmonary blastomycosis Adults PO (capsules) 200 mg PO 3 times daily for 3 days followed by 200 mg PO 1 or 2 times daily for 6 to 12 months; PO (Tolsura) 130 mg PO once daily with 65 mg increment dose increases to a maximum of 260 mg/day if there is no obvious improvement or there is evi- dence of progressive fungal disease. Ad- minister doses above 130 mg/day in 2 divided doses Treatment of Serious, Life-threaten- ing Systemic Fungal Infections Adult: PO (Capsules): Loading dosage of 200 mg 3 times daily (600 mg daily) for the first 3 days, then 200–400 mg daily, usually continued for 3 months and until clinical parameters and labo- ratory tests indicate that the active fun- gal infection has subsided Treatment of Pulmonary or Extrapul- monary Aspergillosis Adult: PO (Capsules): 200–400 mg daily X at least 3 months Treatment of Pulmonary or Extrapul- monary Blastomycosis Adult: PO (Capsules): 200 mg once daily. If there is evidence of progression or no apparent improvement, increase dos- age in 100-mg increments daily up to a max 400 mg daily for 6–12 months Treatment of Oropharyngeal Candidiasis Adult PO (Oral solution): 200 mg (20 mL) daily for 1–2 weeks. Generally re- solves within several days; retreatment in patients who failed to respond to or are refractory to oral fluconazole: Manufac- turer recommends 100 mg (10 mL) twice daily. A response to itraconazole in these patients generally is evident within 2–4 weeks; relapse may be expected shortly after the drug is discontinued HIV-infected adults (oral solution): 200 mg daily X 7–14 days Treatment of Esophageal Candidiasis Adult PO Oral solution: 100 mg (10 mL) daily; depending on patient response, up to 200 mg (20 mL) daily may be given for >- 3 wks, continue for 2 weeks after symptoms resolve
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Available forms: Caps 100 mg; oral sol 10 mg/mL; tab 200 mg Pulmonary or disseminated extra- pulmonary blastomycosis Adults: PO (capsules) 200 mg PO 3 times daily for 3 days followed by 200 mg PO 1 or 2 times daily for 6-12 mo; PO (Tolsura) 130 mg PO once daily with 65-mg-increment dose increases to a maximum of 260 mg/day if there is no obvious improvement or there is evidence of progressive fungal disease. Administer doses above 130 mg/day in 2 divided doses Treatment of serious, life-threatening systemic fungal infections Adult: PO (capsules) Loading dosage of 200 mg 3 times daily (600 mg daily) for the first 3 days, then 200-400 mg daily, usually I continued for 3 mo and until clinical pa- rameters and laboratory tests indicate that the active fungal infection has subsided Treatment of pulmonary or extra- pulmonary aspergillosis Adult: PO (capsules) 200-400 mg daily for at least 3 mo Treatment of pulmonary or extra- pulmonary blastomycosis Adult: PO (capsules) 200 mg once daily. If there is evidence of progression or no apparent improvement, increase dosage in 100-mg increments daily up to a max 400 mg daily for 6-12 mo Treatment of oropharyngeal candidiasis Adult: PO (oral solution) 200 mg (20 mL) daily for 1-2 wk. Generally resolves within several days; retreatment in pa- tients who failed to respond to or are refractory to oral fluconazole: Manufac- turer recommends 100 mg (10 mL) twice daily. A response to itraconazole in these patients generally is evident within 2-4 wk; relapse may be expected shortly after the drug is discontinued HIV-infected adults (oral solution) 200 mg daily ×7-14 days Treatment of esophageal candidiasis Adult: PO (oral solution) 100 mg (10 mL) daily; depending on patient response, up to 200 mg (20 mL) daily may be given for ≥3 wk, continue for 2 wk after symp- toms resolve
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Administer: • In the presence of acid products only; do not use alkaline products, antacids within 2 hr of product; may give coffee, tea, acidic fruit juices PO route • Swallow caps whole; do not break, crush, or chew caps • Give caps after full meal to ensure ab- sorption • Oral sol: patient should swish in mouth vigorously, use on empty stomach • Oral sol and caps are not interchange- able on mg/mg basis • Store in tight container at room tem- perature, do not freeze
Source page 732
Extracted information for itraconazole only.
Assess: • HF: if present, discontinue product • Type of infection; may begin treatment before obtaining results • Infection: temperature, WBC, sputum at baseline and periodically • I&O ratio, potassium levels • Hepatic studies (ALT, AST, bilirubin) if patient receiving long-term therapy • Allergic reaction: rash, photosensitiv- ity, urticaria, dermatitis • Hepatotoxicity: nausea, vomiting, jaundice, clay-colored stools, fatigue • Pregnancy/breastfeeding: do not use in onychomycosis; use for other condi tions only if benefits outweigh fetal risk; do not use in breastfeeding
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Evaluate: • Therapeutic response: decreased fever, malaise, rash, negative C&S for in- fecting organism
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That long-term therapy may be needed to clear infection (1 wk-6 mo, depending on infection) • To avoid hazardous activities if dizzi- ness occurs • To take 2 hr before administration of other products that increase gastric pH (ant- acids, H2-blockers, omeprazole, sucralfate, anticholinergics); to avoid grapefruit juice; to notify health care provider of all medications taken; to take after a full meal (caps) or on empty stomach (oral sol) • About the importance of compliance with product regimen; to use alternative methods of contraception • To notify prescriber of GI symptoms; signs of hepatic dysfunction (fatigue, jaundice, nausea, anorexia, vomiting, dark urine, pale stools); heart failure (trouble breathing, unusual weight gain, fatigue, swelling); hearing changes
Source pages 732, 733
Extracted information for itraconazole only.
PHARMACOKINETICS PO: Peak 3-4 hr; half-life 21 hr, IV 35.4 hr; metabolized in liver; excreted in bile, feces, urine 40%; requires acid pH for absorption; distributed poorly to CSF; 99.8% protein bound; inhibits CYP3A4
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Filter the extracted dose blocks for this individual drug.