Idebenone

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.

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.

Monitor patient regularly according to local clinical guidelines.

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.

Increased bioavailability (approx 5- to 7-fold) with food.

Description:
Mechanism of Action: 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.

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.

Store away from the reach of children.

Thuốc hướng thần kinh & thuốc bổ thần kinh

N06BX13 - idebenone ; Belongs to the class of other psychostimulants and nootropics.

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.