Formulary
Isavuconazole: Indications, Dosing, Side Effects and Interactions
Isavuconazole (an active metabolite of isavuconazonium sulfate) is a triazole antifungal that blocks the synthesis of ergosterol, a key component of the...
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Isavuconazole: Indications, Dosing, Side Effects and Interactions
Isavuconazole (an active metabolite of isavuconazonium sulfate) is a triazole antifungal that blocks the synthesis of ergosterol, a key component of the...
Drug action
Isavuconazole (an active metabolite of isavuconazonium sulfate) is a triazole antifungal that blocks the synthesis of ergosterol, a key component of the fungal cell membrane.
Indications and dose
**Invasive aspergillosis,Mucormycosis in patients**
- **Adult** (By Mouth, Or By Intravenous Infusion): for whom amphotericin B is inappropriate Loading dose 200 mg every 8 hours for 48 hours (6 administrations in total), then maintenance 200 mg once daily, maintenance dose to be started at least 12 hours after the last loading dose; long-term treatment should be reviewed after 6-months.
Cautions
Elderly-limited information
Contraindications
Acute porphyrias ; short QT syndrome
Side effects
General side-effects: Common or very common Appetite decreased; asthenia; chest pain; confusion; delirium; diarrhoea; drowsiness; dyspnoea; electrolyte imbalance; gastrointestinal discomfort; headache; hepatic disorders; hyperbilirubinaemia; nausea; renal failure; respiratory disorders; skin reactions; thrombophlebitis; vomiting Uncommon Alopecia; anaemia; arrhythmias; back pain; circulatory collapse; constipation; depression; dizziness; encephalopathy; haemorrhage; hypersensitivity; hypoalbuminaemia; hypoglycaemia; hypotension; insomnia; leucopenia; malaise; malnutrition; neutropenia; palpitations; pancytopenia; paraesthesia; peripheral neuropathy; peripheral oedema; seizures; syncope; taste altered; thrombocytopenia; vertigo Frequency not known Severe cutaneous adverse reactions (SCARs) Specific side-effects: Frequency not known With intravenous use Infusion related reaction Side-effects, further information Infusion-related reactions have been reported, including hypotension, dyspnoea, dizziness, paraesthesia, nausea, and headache-manufacturer advises discontinue treatment if these reactions occur.
Interactions
**Severe interactions:**
- Contraindications of concomitant use Primidone and its main metabolite phenobarbital are strong inducers of cytochrome P450 and thus lead to life-threatening situations due to the risk of decreased...
- Moderate or weak CYP3A4 inhibitors: antifungal agents (e.g., fluconazole, isavuconazole, clotrimazole, miconazole), the macrolide antibiotics (e.g., azithromycin, calcium channel blockers (e.g.,...
**Other interactions (6):**
- Combinations requiring caution Combinations which can increase the effects of digoxin when co-administered: amiodarone, canagliflozin, daclatasvir, flibanserin, flecainide, prazosin, propafenone,...
- Ketoconazole (200 mg twice daily)/ velpatasvir (100 mg single dose) d (Inhibition of P-gp and CYPs) Itraconazole e Voriconazole e Posaconazole e Isavuconazole e Effect on ketoconazole exposure not...
- Medicinal products that affect glucuronidation (e.g.
- Isavuconazole An increase of MPA exposure (AUC 0- ) by 35% was observed with concomitant administration of isavuconazole.
- Fluconazole Isavuconazole Itraconazole Posaconazole Clotrimazole Not studied.
- Boosted darunavir may increase antifungal plasma concentrations and posaconazole, isavuconazole, itraconazole or fluconazole may increase darunavir concentrations.
Pregnancy
Manufacturer advises avoid unless severe or life-threatening infection-toxicity in animal studies.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in severe impairment (no information available)-monitor for drug toxicity.
Medicinal forms
Capsule,Solution
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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