Isavuconazole

Antifungal, Systemic · Triazole antifungal

Indications

Invasive aspergillosis. Mucormycosis in patients for whom amphotericin B is inappropriate.

Dosage

ORAL/ IV INFUSION: Adults: Loading dose 200 mg every 8 hrs for 48 hrs (total 6 administrations), then maintenance 200 mg once daily, maintenance dose to be started at least 12 hrs after the last loading dose; long-term treatment should be reviewed after 6 months. Children: Not recommended.

Administration

Administered via IV infusion. Flush line with NS or D5W before and after infusion. Do not administer as an IV bolus injection. The IV adm should be completed within 6 hrs at 20-25°C. Reconstitution: Reconstitute each 200 mg with 5 mL Water for Injection. Shake gently to dissolve. Dilute dose to conc of 0.8 mg/mL with Glucose 5% or NaCl 0.9% and give via a 0.2-1.2 micron filter over at least 1 hr. Compatibility: WFI, Glucose 5%, NaCl 0.9%. Stability: Store intact vials in a refrigerator at 2-8°C. Following reconstitution of the vial with SWFI, use the soln immediately, or stored below 25°C for a max of 1 hr prior to preparation of the admixed soln in NS or D5W. The admixed inf soln should be kept for not more than 6 hrs at 20-25°C or 24 hrs at 2-8°C prior to use. Do not freeze.

Adverse Effects

Headache, GI upset, rash, fatigue, hypokalaemia, chest pain, anorexia, delirium, somnolence, thrombophlebitis, dyspnoea, acute respiratory failure, elevated LFTs, pruritus, renal failure, inj site reactions. Reports of hepatitis.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Familial short QT syndrome. Precautions: Severe hepatic impairment. Risk of inf-related and severe skin reactions; discontinue if occur.

Interactions

CYP3A4/5 inducers (eg, rifamycins, carbamazepine, phenytoin, St John's wort), inhibitors (eg, ketoconazole, protease inhibitors) or substrates (eg, immunosuppressants). Substrates of BCRP, CYP3A4, CYP2B6, P-gp, UGT or OCT2. Drugs that shorten QT interval.

Advice to Patient

Take oral form with or without meals. Swallow whole capsule, do not chew, crush, dissolve or open. Females of childbearing potential must use effective contraception during treatment and for 28 days after the last dose.

Pharmacokinetics

Metabolism: Prodrug: Via esterases in the blood. Isavuconazole: Hepatic. Bioavailability: Oral: 98%. Half-life elimination: IV: 130 hrs. Time to peak: Oral: 2-3 hrs Excretion: Urine (<1%). Faeces (33%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.