Idebenone


Generic Medicine Info
Indications and Dosage
Oral
Leber's optic atrophy
Adult: Recommended dose: 300 mg tid.
Special Precautions
Ensure that chromaturia does not mask colour changes due to other reasons (e.g. renal or blood disorders). Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Chromaturia (reddish-brown urine discolouration).
General disorders and administration site conditions: Malaise.
Gastrointestinal disorders: Diarrhoea, nausea, vomiting, dyspepsia.
Musculoskeletal and connective tissue disorders: Back pain, pain in the extremity.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, cough.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Monitoring Parameters
Monitor patient regularly according to local clinical guidelines.
Drug Interactions
Repeated administration may increase the serum concentrations of CYP3A4 substrates (e.g. midazolam, terfenadine, cisapride, ciclosporin, fentanyl, pimozide, quinidine, tacrolimus, ergotamine). May inhibit P-glycoprotein which may increase the exposure of dabigatran etexilate, digoxin, or aliskiren.
Food Interaction
Increased bioavailability (approx 5- to 7-fold) with food.
Action
Description: Idebenone is a short-chain benzoquinone with nootropic and antioxidant properties. It is assumed to be capable of transferring electrons directly to complex III of the mitochondrial electron transport chain, bypassing complex I that is affected by mitochondrial deoxyribonucleic acid (mtDNA) Leber’s hereditary optic neuropathy (LHON) mutation thereby restoring ATP generation. It may reactivate viable, but inactive, retinal ganglion cells and promote vision recovery.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Increased bioavailability (approx 5- to 7-fold) with food. Time to peak plasma concentration: Within 1 hour (range: 0.33-2 hours).
Distribution: Crosses the blood-brain barrier. Significantly distributed into the cerebral tissues and aqueous humour of the eye.
Metabolism: Metabolised in the liver via oxidative shortening of the side chain, reduction of the quinone ring, and conjugation to glucuronides and sulphates into IDE-C and QS4+QS4-C (main metabolites). Undergoes extensive first-pass metabolism.
Excretion: Via urine as metabolites.
Chemical Structure

Chemical Structure Image
Idebenone

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3686, Idebenone. https://pubchem.ncbi.nlm.nih.gov/compound/Idebenone. Accessed Apr. 26, 2021.

Storage
Store away from the reach of children.
ATC Classification
N06BX13 - idebenone ; Belongs to the class of other psychostimulants and nootropics.
References
Amore G, Romagnoli M, Carbonelli M et al. Therapeutic Options in Hereditary Optic Neuropathies. Drugs. 2021;81(1):57-86. doi: 10.1007/s40265-020-01428-3. Accessed 19/04/2021. PMID: 33159657

Anon. Idebenone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/04/2021.

Buckingham R (ed). Idebenone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/04/2021.

Joint Formulary Committee. Idebenone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/04/2021.

Raxone 150 mg Film-Coated Tablets (Santhera Pharmaceuticals [Deutschland] GmbH). European Medicines Agency [online]. Accessed 14/04/2021.

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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
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