Idebenone


Concise Prescribing Info
Indications/Uses
Listed in Dosage
Dosage/Direction for Use
Adult : PO Symptomatic treatment of Friedreich's ataxiaLower dose therapy: Patients ≤45kg: 150 mg 3 times/day; >45kg: 300 mg 3 times/day; for at least 6 mth. If tolerated and clinical benefit is observed, may move to higher dose therapy: Patients ≤45kg: 450 mg 3 times/day; >45kg: 750 mg 3 times/day. Cosmetic treatment of wrinkles As a 1% cream: Apply a pea-sized amount of cream to dry, clean face and neck once daily for 1 wk; then increase to twice daily if well tolerated.
Dosage Details
Oral
Friedreich's ataxia
Adult: For symptomatic treatment: Lower dose therapy: Patients ≤45 kg: 150 mg tid; >45kg: 300 mg tid. After at least 6 mth of low dose therapy, may increase to higher dose if clinical benefit and tolerability are observed. Higher dose therapy: Patients ≤45 kg: 450 mg tid; >45kg: 750 mg tid. Return to lower dose if no additional improvement is observed after 6 mth on high dose therapy.

Topical/Cutaneous
Cosmetic treatment of wrinkles
Adult: As a 1% cream: Apply a pea-sized amount of cream to clean, dry face and neck once daily for the first wk. If tolerated, may increase to twice daily.
Contraindications
Moderate or severe hepatic impairment; severe renal impairment.
Special Precautions
Oral preparation: Leucocytopenia and agranulocytosis have been reported (rarely) from post-marketing experience. Monitor CBC count before initiation of treatment; after dosage increment, and regularly thereafter. Use with caution in mild hepatic impairment; mild to moderate renal impairment. May cause increases in liver function test (LFT) values, monitor LFT before initiation of therapy; after dosage increment, and regularly thereafter. Safety and efficacy have not been established in pediatric patients <8 yr and in elderly patients >65 yr. Not recommended in pregnancy and lactation. Topical preparation: Allergic reactions including itching, burning, redness, or swelling may occur.
Adverse Reactions
Oral: Nausea, diarrhoea, abdominal pain, dyspepsia, headache, leucocytopenia, agranulocytosis, abnormal LFT values, and increased BUN. Topical: Allergic reactions, rashes, and contact dermatitis.
Overdosage
In the event of overdose, provide general supportive treatment. No known specific antidotes for Idebenone.
Drug Interactions
Concurrent use with CYP2C19, CYP1A2, CYP3A4 inhibitors and inducers may affect metabolism of Idebenone, but clinical relevance is unknown.
Food Interaction
Administration with a high fat meal increases Idebenone bioavailability.
Action
Description: Idebenone is a benzoquinone derivative with structural similarity to ubiquinone (coenzyme Q10). Exact mechanism of action is unknown, it is thought to have antioxidant activity and is believed to facilitate electron flow through respiratory chain, thus improving energy production by body cells.
Pharmacokinetics:
Absorption: Rapidly absorbed following oral admin. Tmax: Within 1 hr.
Distribution: Widely distributed with relatively high levels in the gut, liver and kidney. Enters the brain; with significant amount present in the mitochondria. Protein binding: About 96%.
Metabolism: Undergoes first pass metabolism to conjugated Idebenone, Phase I metabolites (QS10, QS6, and QS4) and their corresponding Phase II metabolites (glucuronide and sulphates). Conjugated Idebenone and QS4 are the main metabolites in plasma.
Excretion: Mainly excreted in urine.
Storage
Oral:
Store at 15-30°C.
Disclaimer: This information is independently developed by MIMS based on Idebenone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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