Felbamate


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Partial seizures with or without secondary generalisation
Adult: In severe cases unresponsive to other drugs: As monotherapy: Initially, 1,200 mg daily in 3 or 4 divided doses, may increase in increments of 600 mg daily every 2 weeks for up to 2,400 mg daily depending on patient response and tolerability. Max: 3,600 mg daily. As adjunctive therapy: Initially, 1,200 mg daily in 3 or 4 divided doses, may increase in increments of 1,200 mg daily at weekly intervals depending on patient response and tolerability. Reduce the dose of concomitant antiepileptic drugs (AEDs) by 1/3 (20-33%) when initiating felbamate therapy.
Child: ≥14 years Same as adult dose.

Oral
Seizures associated with the Lennox-Gastaut syndrome
Child: 2-<14 years In severe cases unresponsive to other drugs: As adjunctive therapy: Initially, 15 mg/kg daily in 3 or 4 divided doses, may increase in increments of 15 mg/kg at weekly intervals. Max: 45 mg/kg daily. Reduce the dose of concomitant AEDs by 20% when initiating felbamate therapy.
Suy thận
Reduce initial and maintenance doses by 50%.
Suy gan
Contraindicated.
Chống chỉ định
Hypersensitivity to carbamates. History of blood dyscrasia. Hepatic impairment.
Thận trọng
Avoid abrupt withdrawal. Renal impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Suicidal behaviour and ideation.
Blood and lymphatic system disorders: Leucopenia.
Cardiac disorders: Chest pain.
Ear and labyrinth disorders: Otitis media.
Eye disorders: Miosis, diplopia, visual disturbance.
Gastrointestinal disorders: Vomiting, nausea, dyspepsia, constipation, hiccups, dysgeusia, abdominal pain, diarrhoea, dry mouth.
General disorders and administration site conditions: Fatigue, fever.
Investigations: Increased liver enzymes, decreased weight.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Drowsiness, headache, dizziness, insomnia, somnolence, tremor, gait disturbance, ataxia, paraesthesia, stupor.
Psychiatric disorders: Emotional lability, anxiety, depression.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, pharyngitis, cough, rhinitis, sinusitis.
Skin and subcutaneous tissue disorders: Rash, acne, purpura.
Potentially Fatal: Aplastic anaemia, acute hepatic failure.
PO: Z (Insufficient data to conclude its safety and risk during pregnancy. Use only when benefits outweigh risks.)
Chỉ số theo dõi
Monitor therapeutic effectiveness and response (e.g. seizure activity, force, type, duration); serum levels of concomitant antiseizure therapy. Perform LFTs (at baseline, every 2 weeks after therapy initiation for the first 6-12 months of therapy, and periodically thereafter); CBC (at baseline, every 2 weeks for the first 6-12 months of therapy, periodically thereafter, and for a significant period after discontinuation). Monitor for suicidality (e.g. suicidal thoughts, depression, behavioural changes).
Quá liều
Symptoms: Mild gastric distress, resting heart rate. Management: Symptomatic and supportive treatment.
Tương tác
May increase serum concentration of phenobarbital, carbamazepine, phenytoin.
Tác dụng
Description: Felbamate is a dicarbamate derivative with unknown mechanism. It has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding. It also exhibits NMDA antagonism, and Ca and Na channel inhibition.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Bioavailability: >90%. Time to peak plasma concentration: 1-6 hours.
Distribution: Enters breast milk. Volume of distribution: 0.7-0.91 L/kg. Plasma protein binding: Approx 22-25%, mainly to albumin.
Metabolism: Partly metabolised in the liver via hydroxylation and conjugation to inactive metabolites.
Excretion: Mainly via urine (40-50% as unchanged drug, 40% as metabolites). Terminal elimination half-life: 20-23 hours.
Đặc tính

Chemical Structure Image
Felbamate

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3331, Felbamate. https://pubchem.ncbi.nlm.nih.gov/compound/Felbamate. Accessed Sept. 28, 2022.

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Thuốc chống co giật
Phân loại ATC
N03AX10 - felbamate ; Belongs to the class of other antiepileptics.
Tài liệu tham khảo
Anon. Felbamate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/08/2022.

Anon. Felbamate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/08/2022.

Buckingham R (ed). Felbamate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/08/2022.

Felbatol Tablets, Oral Suspension (Meda Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 05/08/2022.

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