Name: Itraconazole in dermatology | Dermatology Games
Published: 2020-09-13T04:15:45+00:00

Share the knowledge

Itraconazole in dermatology

Mechanism of action

Inhibits the CYP-dependent enzyme lanosterol 14α demethlyase leading to inhibition of the conversion of lanosterol to ergosterol >> fungistatic action.

Indications

Tinea pedis (moccasin type)/tinea manuum
- adults:200–400 mg/day × 1 week.
- children:3–5 mg/kg/day (maximum 400 mg × 1 week).
Tinea unguium
- adults:200 mg/day × 6 weeks (or) 200 mg BID × 1 week/month for 2 consecutive months(fingernails) ;200 mg/day × 12 weeks (or) 200 mg BID × 1 week/month for 3–4 consecutive months(toenails).
- children: 5 mg/kg/day (<20 kg), 100 mg/day (20–40 kg), 200 mg/day (40–50 kg), (or) 200 mg BID (>50 kg) × 1 week/month for 2 (fingernails) or 3 (toenails) consecutive months.
Tinea corporis
- (extensive, adults):200 mg/day × 1 week.
- (extensive, children):3–5 mg/kg/day (maximum 200 mg)× 1 week.
Tinea capitis
- (adults):5 mg/kg/day (maximum 400 mg) ×4–8 weeks.
- (children): 5 mg/kg/day (maximum 500 mg) ×4–8 weeks.
Tinea versicolor :
- 200 mg po daily × 5–7 days.
- Single 400 mg dose of itraconazole once monthly for 6 months may be useful as prophylaxis for recurrent tinea versicolor.
Pityrosporum folliculitis :200 mg/day for 1–3 weeks.
Blastomycosis : ( mild to moderate non-CNS disease) : 200–400 mg/day.
Histoplasmosis : (immunocompetent hosts with mild to moderate, stable disease) :200–400 mg/day.
Aspergillosis :200–400 mg po daily for at least 3 months ( loading dose of 200 mg TID for first 3 days in life-threatening conditions ).
Majocchi’s granuloma : 200 mg po twice daily for 1 week per month, for 2 pulses.
Oropharyngeal candidiasis : Swish and swallow 200 mg daily for 1–2 weeks.
HIV-associated eosinophilic folliculitis :200–400 mg daily.
Tinea imbricata .
Recurrent candidiasis : 200 mg BID orally once monthly for 6 months \n
Chronic mucocutaneous candidiasis.
Cutaneous sporotrichosis :100–200 mg/day until clinical recovery (at least 3 months).
Chromoblastomycosis :200–400 mg/day for at least 6 months or until cure.

Monitoring

Liver function tests:

Side effects

Gastrointestinal
- Diarrhea (5.6%),dyspepsia(4.3%),abdominal pain (2.4%),nausea (2.6%),ﬂatulence (2.2%).
Cutaneous
- Rash (5.6%), pruritus(2.8%),urticaria(1.1%), SJS .
Neurologic
- Headache
Hepatic
- LFT ≥ 2 × upper limit of normal.
others
- Fever, edema, hypokalemia, neutropenia (rarely).

Contraindications

Ventricular dysfunction.
Hx of cardiac dysfunction (i.e. CHF).
Use of contraindicated antiarrhythmics/cardiac drugs.
known hypersensitivity to itraconazole.
caution if hypersensitive to other azoles.

Interactions

Itraconazole is contraindicated with dofetilide, levacetylmethadol (levomethadyl).
Drugs that increase gastric pH, such as proton pump inhibitors, antacids and H2 antihistamines, may reduce the absorption of Itraconazole.
It also is contraindicated with HMG -CoA-reductase inhibitors such as lovastatin and simvastatin.
Itraconazole is contraindicated with benzodiazepines midazolam and triazolam.
It is contraindicated calcium channel blocker nisoldipine, and CYP3A4 ergot alkaloids such as dihydroergotamine, ergometrine (ergonovine), ergotamine and methylergometrine (methylergonovine).
Phenytoin causes decreased levels of itraconazole.
Itraconazole reduces cyclosporine metabolism by inhibiting CYP3A4.
Itraconazole is contraindicated with methadone, disopyramide, dronedarone, quinidine, isavuconazole, irinotecan, ivabradine, lurasidone, pimozide, felodipine, ranolazine, eplerenone, cisapride, naloxegol, lomitapide, avanafil, ticagrelor.
In patients with varying degrees of renal or hepatic impairment, coadministration of itraconazole with colchicine, fesoterodine, and solifenacin are contraindicated.

Pregnancy and Lactation

Pregnancy category C.
Itraconazole is excreted in human milk and should be avoided in lactating patients.

Precautions

Itraconazole is not recommended with Abnormal LFT.
It is not recommended also with Active liver disease .
It is not recommended with hx of liver toxicity with other drugs.
Itraconazole can cause or exacerbate congestive heart failure.
Do not use for the treatment of onychomycosis in patients with ventricular dysfunction.
Monitor for sings and symptoms of CHF.
Discontinue if signs of neuropathy.
Transient or permanent hearing loss reported (concurrent administration of quinidine).
Parenteral form is incompatible with most aqueous solutions; use dedicated line, and do not mix with other drugs in any way.

Drug Info

Pulse regimen, for the treatment of onychomycosis, may help improving the adverse effects profile compared to the continuous regimen.
Although itraconazole absorption is best when the gastric pH is low, its administration with food is more important for achieving high plasma concentrations.
Absorption of itraconazole capsules is reduced when gastric acidity reduced; administer capsules with acidic beverage in patients with reduced gastric acidity and do not administer concomitantly with acid suppressive therapy; monitor for response.