Rufinamide


Generic Medicine Info
Indications and Dosage
Oral
Adjunct for seizures associated with Lennox-Gastaut syndrome
Adult: Patients ≥30 kg who are not receiving valproate: Initially, 400 mg daily in 2 equally divided doses, increased in increments of 400 mg daily every 2 days according to response. Max: 30-50 kg: 1,800 mg daily; >50-70 kg: 2,400 mg daily; >70 kg: 3,200 mg daily. Patients ≥30 kg who are also receiving valproate: Initially, 400 mg daily in 2 equally divided doses, increased in increments of 400 mg daily every 2 days according to response. Max: 30-50 kg: 1,200 mg daily; >50-70 kg: 1,600 mg daily; >70 kg: 2,200 mg daily. Dosage recommendations may vary among individual products and between countries (refer to detailed product guideline).
Elderly: Initiate at the lower end of the dosing range.
Child: ≥1 to <4 years Patients who are not receiving valproate: Initially, 10 mg/kg daily in 2 equally divided doses (separated by approx 12 hours), increased in increments of up to 10 mg/kg daily every 3 days to the target dose of 45 mg/kg daily in 2 equally divided doses (separated by approx 12 hours) according to response. Max: 45 mg/kg daily; Patients who are also receiving valproate: Initially, 10 mg/kg daily in 2 equally divided doses (separated by approx 12 hours), increased in increments of up to 10 mg/kg daily every 3 days to the target dose of 30 mg/kg daily in 2 equally divided doses (separated by approx 12 hours) according to response. Max: 30 mg/kg daily; 4-17 years Patients <30 kg who are not receiving valproate: Initially, 200 mg daily in 2 equally divided doses, increased in increments of 200 mg daily every 3 days according to response. Max: 1,000 mg daily; Patients <30 kg who are also receiving valproate: Initially, 200 mg daily in 2 equally divided doses, increased in increments of 200 mg daily after a minimum of 2 days according to response. Max: 600 mg daily; Patients ≥30 kg who are not receiving or are also receiving valproate: Same as adult dose. Dosage recommendations may vary among individual products and between countries (refer to detailed product guideline).
Renal Impairment
Patients undergoing haemodialysis: Dose adjustment may be necessary.
Hepatic Impairment
Mild to moderate: Cautious dose titration may be required. Severe: Not recommended.
Administration
FC tab; oral susp: Should be taken with food. FC Tab: May be swallowed whole/split/crushed.
Contraindications
Familial short QT syndrome.
Special Precautions
Patients with history of abnormal ECG demonstrating QT interval shortening, family history of unexplained cardiac arrhythmia, risk factors for further shortening of QTc interval. Concomitant use with drugs that shorten QT interval. Avoid abrupt withdrawal. Hepatic impairment; patients undergoing haemodialysis. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Status epilepticus, shortened QT interval, leucopenia, suicidal ideation and behaviour, cognitive symptoms (e.g. somnolence, dizziness), coordination abnormalities (e.g. ataxia, gait disturbances).
Blood and lymphatic system disorders: Anaemia.
Ear and labyrinth disorders: Ear infection, vertigo.
Eye disorders: Blurred vision, diplopia, nystagmus.
Gastrointestinal disorders: Nausea, vomiting, upper abdominal pain, constipation, diarrhoea, dyspepsia.
General disorders and administration site conditions: Fatigue.
Injury, poisoning and procedural complications: Contusion, head injury.
Investigations: Decreased weight.
Metabolism and nutrition disorders: Decreased appetite, anorexia, eating disorder.
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Headache, tremor, convulsion, psychomotor hyperactivity, disturbance in attention.
Psychiatric disorders: Insomnia, anxiety, aggression.
Renal and urinary disorders: Pollakuria.
Reproductive system and breast disorders: Oligomenorrhoea.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, influenza, sinusitis, rhinitis, bronchitis, pneumonia, epistaxis.
Skin and subcutaneous tissue disorders: Rash, pruritus, acne.
Potentially Fatal: Drug reaction with eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome (SJS).
PO: Z (Insufficient data to conclude its safety and risk during pregnancy. Use only when benefits outweigh risks.)
Patient Counseling Information
This drug may cause dizziness, somnolence or blurred vision, if affected, do not drive or operate machinery. Women of childbearing potential must use proven birth control methods during therapy. Consider using other reliable contraceptive methods recommended by the doctor as hormonal contraceptives may be ineffective.
Monitoring Parameters
Obtain serum levels of the concomitant anti-seizure agents. Monitor for signs and symptoms of skin reactions (e.g. rash), suicidal ideation or behaviour, worsening depression, and/or unusual changes in mood or behaviour.
Drug Interactions
Significantly increased plasma concentrations with valproate. May decrease the effectiveness of hormonal contraceptives (e.g. ethinyl estradiol, norethisterone). May reduce the plasma concentrations of agents metabolised by CYP3A4 (e.g. triazolam), carbamazepine, and lamotrigine. May increase the risk of QT interval shortening when given with other drugs that shorten QT interval (e.g. digoxin, mexiletine, ranolazine, lamotrigine). May increase plasma concentrations of phenytoin and phenobarbital.
Food Interaction
Increased absorption with food. Alcohol may enhance the CNS effects (e.g. dizziness) of rufinamide.
Action
Description:
Mechanism of Action: Rufinamide is a triazole derivative anticonvulsant agent. The exact mechanism for its activity is unknown; however, it is suggested to modulate the activity of Na channels by prolonging their inactive state, thereby limiting the repetitive firing of Na-dependent action potentials that mediate anticonvulsant effects.
Pharmacokinetics:
Absorption: Slowly and extensively absorbed. Increased absorption with food. Time to peak plasma concentration: 4-6 hours.
Distribution: Evenly distributed between erythrocytes and plasma. Volume of distribution: Approx 50 L. Plasma protein binding: 34%, mainly to albumin (27%).
Metabolism: Extensively metabolised via carboxylesterase-mediated hydrolysis of the carboxylamide group to the inactive acid derivative, CGP 47292.
Excretion: Via urine (85%; approx 66% as CGP 47292, 2% as unchanged drug). Elimination half-life: Approx 6-10 hours.
Chemical Structure

Chemical Structure Image
Rufinamide

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 129228, Rufinamide. https://pubchem.ncbi.nlm.nih.gov/compound/129228. Accessed Aug. 25, 2022.

Storage
Tab: Store between 15-30°C. Protect from moisture. Oral susp: Store at 25°C.
MIMS Class
Anticonvulsants
ATC Classification
N03AF03 - rufinamide ; Belongs to the class of carboximide derivatives antiepileptic. Used in the management of epilepsy.
References
Anon. Rufinamide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 02/08/2022.

Anon. Rufinamide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/08/2022.

Banzel Tablet, Film Coated and Suspension (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/08/2022.

Buckingham R (ed). Rufinamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2022.

Eisai New Zealand Ltd. Inovelon 100 mg, 200 mg and 400 mg Film Coated Tablets data sheet 11 June 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 02/08/2022.

Inovelon 100 mg, 200 mg, and 400 mg Film-coated Tablets; Inovelon 40 mg/mL Oral Suspension (Eisai GmbH). European Medicines Agency [online]. Accessed 02/08/2022.

Inovelon 200 mg Film-coated Tablets (Eisai Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/08/2022.

Joint Formulary Committee. Rufinamide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2022.

Disclaimer: This information is independently developed by MIMS based on Rufinamide 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 © 2024 MIMS. All rights reserved. Powered by MIMS.com
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