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Canditral 100 (Itraconazole 100 mg)
Candrtal 100 is almost certainly Canditral 100 - a brand name for Itraconazole 100 mg capsules, manufactured by Glenmark Pharmaceuticals. Each capsule contains Itraconazole pellets equivalent to 100 mg of itraconazole.
Drug Class
Triazole antifungal - inhibits fungal cytochrome P450-dependent synthesis of ergosterol, the primary sterol in fungal cell membranes. This disrupts membrane structure and function.
Uses (Indications)
| Infection | Notes |
|---|
| Dermatophytoses (tinea pedis, tinea corporis, onychomycosis) | Common indication |
| Vulvovaginal candidiasis | |
| Oropharyngeal/esophageal candidiasis | |
| Histoplasmosis (non-CNS, non-meningeal) | Mild-to-moderate disease; step-down after amphotericin B for severe disease |
| Blastomycosis | |
| Aspergillosis | Alternative for non-CNS disease |
| Sporotrichosis | |
| Coccidioidomycosis | Bone disease responds particularly well |
| Disseminated Mycobacterium avium complex | Prophylaxis |
Dosage
| Indication | Dose |
|---|
| Onychomycosis (fingernails) | 200 mg/day x 6 weeks OR pulse: 200 mg BD x 1 week/month x 2 months |
| Onychomycosis (toenails) | 200 mg/day x 12 weeks OR pulse x 3 months |
| Tinea corporis/cruris | 100 mg/day x 15 days OR 200 mg/day x 7 days |
| Tinea pedis | 100 mg/day x 30 days |
| Vulvovaginal candidiasis | 200 mg BD x 1 day |
| Oropharyngeal candidiasis | 100-200 mg/day x 7-14 days |
| Histoplasmosis (mild-moderate) | 200 mg TDS x 3 days, then 200 mg BD x 12 months |
Loading doses are recommended because steady-state levels are not reached for 4 days (and its active metabolite hydroxy-itraconazole takes 7 days).
Pharmacokinetics
- Prodrug aspect: Not a prodrug - absorbed as itraconazole directly; converted to active metabolite hydroxy-itraconazole in the liver
- Absorption: Erratic oral absorption requiring acid gastric pH; best taken with food (capsules) or in fasted state (oral solution); antacids and H2 blockers impair absorption
- Protein binding: Highly protein-bound (>99%)
- Half-life: ~30-40 hours at steady state
- Metabolism: Hepatic via CYP3A4 (both substrate AND inhibitor)
- Elimination: Primarily fecal; minimal renal excretion
Adverse Effects
- Nausea, abdominal pain, diarrhea (most common)
- Elevated liver enzymes - hepatotoxicity (monitor LFTs)
- Headache, dizziness
- Rash, pruritus
- Hypokalemia, edema (with prolonged use)
- Negative inotropic effect - can worsen congestive heart failure (contraindicated in CHF)
- Peripheral neuropathy (rare, with prolonged use)
- Hearing loss (rare)
- QT prolongation (important for drug interactions)
Contraindications
- Congestive heart failure (or history of CHF) - negative inotropic effect
- Pregnancy - teratogenic (Category D/X); women of childbearing age must use contraception
- Co-administration with: cisapride, pimozide, quinidine, dofetilide, dronedarone, methadone (risk of fatal arrhythmias via QT prolongation)
- Co-administration with lovastatin, simvastatin (risk of rhabdomyolysis)
- Hypersensitivity to itraconazole or other azoles
Key Drug Interactions
Itraconazole is a potent CYP3A4 inhibitor AND inhibits P-glycoprotein, leading to dramatically increased levels of co-administered drugs:
- Statins (lovastatin, simvastatin): rhabdomyolysis risk - avoid; use pravastatin instead
- Benzodiazepines (midazolam, triazolam, alprazolam): prolonged sedation
- Immunosuppressants (cyclosporine, tacrolimus, sirolimus): toxicity
- Calcium channel blockers (felodipine, others): hypotension, edema
- Anticoagulants (warfarin): bleeding risk - INR monitoring required
- Digoxin: increased digoxin toxicity
- Antiepileptics (carbamazepine, phenytoin): these reduce itraconazole levels (enzyme inducers)
- Rifampicin: reduces itraconazole levels significantly - avoid combination
- Antacids / PPIs / H2 blockers: reduce itraconazole absorption (need acid for absorption)
Special Warnings
- Breastfeeding: excreted in breast milk - avoid
- Liver disease: use with caution; monitor LFTs during therapy
- Immunocompromised patients: drug may be less effective; monitor serum levels
- Neuropathy: discontinue if peripheral neuropathy develops
Source references: Goodman & Gilman's Pharmacological Basis of Therapeutics (pp. 1218-1219), Medical Microbiology 9e, Katzung's Basic and Clinical Pharmacology 16e, Glenmark Pharmaceuticals Canditral 100 Patient Information Leaflet.