Rufinamide

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination half-life, healthy subjects and patients with epilepsy = 6-10 hours.

Volume Distribusi Rufinamide was evenly distributed between erythrocytes and plasma. The apparent volume of distribution is dependent upon dose and varies with body surface area. The apparent volume of distribution was about 50 L at 3200 mg/day. Volume of distribution is similar between adults and children and is non-linear.

Klirens (Clearance) -

Absorpsi

The oral suspension and tablet are bioequivalent on a mg per mg basis. Rufinamide is well absorbed but the rate is slow and the extent of absorption decreases as dose is increases. Based on urinary excretion, the extent of absorption was at least 85% following oral administration of a single dose of 600 mg rufinamide tablet under fed conditions. Bioavailability= 70%-85% (decreases with increasing doses); Tmax, fed and fasted states= 4-6 hours; Cmax, 10 mg/kg/day= 4.01 µL/mL; Cmax, 30mg/kg/day= 8.68 µL/mL; AUC (0h-12h), 10mg/kg/day= 37.8±47 µg·h/mL; AUC (0h-12h), 30mg/kg/day= 89.3±59 µg·h/mL.

Metabolisme

Rufinamide is extensively metabolized but has no active metabolites. Metabolism by carboxyesterases into inactive metabolite CGP 47292, a carboxylic acid derivative, via hydrolysis is the primary biotransformation pathway. A few minor additional metabolites were detected in urine, which appeared to be acyl-glucuronides of CGP 47292. The cytochrome P450 enzyme system or glutathiones are not involved with the metabolism of rufinamide. Rufinamide is a weak inhibitor of CYP 2E1. Rufinamide is a weak inducer of CYP 3A4 enzymes.

Rute Eliminasi

Renally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated.

Interaksi Makanan

1 Data

1. Take with food. Food can increase the absorption of rufinamide.

Interaksi Obat

948 Data

Buprenorphine	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine	Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Dronabinol	Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Droperidol	Droperidol may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Hydrocodone	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine	Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Magnesium sulfate	The therapeutic efficacy of Rufinamide can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine	Rufinamide may increase the sedative activities of Metyrosine.
Minocycline	Minocycline may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Mirtazapine	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone	Nabilone may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Orphenadrine	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde	Rufinamide may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Pramipexole	Rufinamide may increase the sedative activities of Pramipexole.
Ropinirole	Rufinamide may increase the sedative activities of Ropinirole.
Rotigotine	Rufinamide may increase the sedative activities of Rotigotine.
Botulinum toxin type B	The risk or severity of adverse effects can be increased when Rufinamide is combined with Botulinum toxin type B.
Botulinum toxin type A	The risk or severity of adverse effects can be increased when Rufinamide is combined with Botulinum toxin type A.
Tryptophan	The risk or severity of adverse effects can be increased when Rufinamide is combined with Tryptophan.
Fluvoxamine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Fluvoxamine.
Baclofen	Baclofen may increase the central nervous system depressant (CNS depressant) activities of Rufinamide.
Lorazepam	The risk or severity of adverse effects can be increased when Rufinamide is combined with Lorazepam.
Ethchlorvynol	The risk or severity of adverse effects can be increased when Rufinamide is combined with Ethchlorvynol.
Succinylcholine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Succinylcholine.
Reserpine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Reserpine.
Citalopram	The risk or severity of adverse effects can be increased when Rufinamide is combined with Citalopram.
Eletriptan	The risk or severity of adverse effects can be increased when Rufinamide is combined with Eletriptan.
Enflurane	The risk or severity of adverse effects can be increased when Rufinamide is combined with Enflurane.
Temazepam	The risk or severity of adverse effects can be increased when Rufinamide is combined with Temazepam.
Reboxetine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Reboxetine.
Butabarbital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Butabarbital.
Butalbital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Butalbital.
Methysergide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Methysergide.
Cabergoline	The risk or severity of adverse effects can be increased when Rufinamide is combined with Cabergoline.
Clemastine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Clemastine.
Venlafaxine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Venlafaxine.
Etomidate	The risk or severity of adverse effects can be increased when Rufinamide is combined with Etomidate.
Morphine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Morphine.
Talbutal	The risk or severity of adverse effects can be increased when Rufinamide is combined with Talbutal.
Pentobarbital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Pentobarbital.
Zolmitriptan	The risk or severity of adverse effects can be increased when Rufinamide is combined with Zolmitriptan.
Codeine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Codeine.
Dihydroergotamine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Dihydroergotamine.
Amitriptyline	The risk or severity of adverse effects can be increased when Rufinamide is combined with Amitriptyline.
Tolcapone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Tolcapone.
Hydromorphone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Hydromorphone.
Olanzapine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Olanzapine.
Cetirizine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Cetirizine.
Protriptyline	The risk or severity of adverse effects can be increased when Rufinamide is combined with Protriptyline.
Trimethadione	The risk or severity of adverse effects can be increased when Rufinamide is combined with Trimethadione.
Clobazam	The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Rufinamide.
Chlorzoxazone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorzoxazone.
Clozapine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Clozapine.
Meprobamate	The risk or severity of adverse effects can be increased when Rufinamide is combined with Meprobamate.
Thiethylperazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Thiethylperazine.
Palonosetron	The risk or severity of adverse effects can be increased when Rufinamide is combined with Palonosetron.
Sulpiride	The risk or severity of adverse effects can be increased when Rufinamide is combined with Sulpiride.
Alprazolam	The risk or severity of adverse effects can be increased when Rufinamide is combined with Alprazolam.
Dexbrompheniramine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Dexbrompheniramine.
Loxapine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Loxapine.
Remoxipride	The risk or severity of adverse effects can be increased when Rufinamide is combined with Remoxipride.
Metocurine iodide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Metocurine iodide.
Secobarbital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Secobarbital.
Promazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Promazine.
Methocarbamol	The risk or severity of adverse effects can be increased when Rufinamide is combined with Methocarbamol.
Triprolidine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Triprolidine.
Prochlorperazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Prochlorperazine.
Cyproheptadine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Cyproheptadine.
Meperidine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Meperidine.
Imipramine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Imipramine.
Metharbital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Metharbital.
Quinine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Quinine.
Methohexital	The risk or severity of adverse effects can be increased when Rufinamide is combined with Methohexital.
Chlordiazepoxide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Chlordiazepoxide.
Duloxetine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Duloxetine.
Chlorpromazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorpromazine.
Gallamine triethiodide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Gallamine triethiodide.
Entacapone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Entacapone.
Oxycodone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Oxycodone.
Triflupromazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Triflupromazine.
Dextromethorphan	The risk or severity of adverse effects can be increased when Rufinamide is combined with Dextromethorphan.
Nortriptyline	The risk or severity of adverse effects can be increased when Rufinamide is combined with Nortriptyline.
Amoxapine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Amoxapine.
Adinazolam	The risk or severity of adverse effects can be increased when Rufinamide is combined with Adinazolam.
Cisatracurium	The risk or severity of adverse effects can be increased when Rufinamide is combined with Cisatracurium.
Fenfluramine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Fenfluramine.
Mazindol	The risk or severity of adverse effects can be increased when Rufinamide is combined with Mazindol.
Fluticasone propionate	The risk or severity of adverse effects can be increased when Rufinamide is combined with Fluticasone propionate.
Lisuride	The risk or severity of adverse effects can be increased when Rufinamide is combined with Lisuride.
Ethosuximide	The risk or severity of adverse effects can be increased when Rufinamide is combined with Ethosuximide.
Thiopental	The risk or severity of adverse effects can be increased when Rufinamide is combined with Thiopental.
Cisapride	The risk or severity of adverse effects can be increased when Rufinamide is combined with Cisapride.
Butorphanol	The risk or severity of adverse effects can be increased when Rufinamide is combined with Butorphanol.
Furazolidone	The risk or severity of adverse effects can be increased when Rufinamide is combined with Furazolidone.
Paramethadione	The risk or severity of adverse effects can be increased when Rufinamide is combined with Paramethadione.
Fluphenazine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Fluphenazine.
Efavirenz	The risk or severity of adverse effects can be increased when Rufinamide is combined with Efavirenz.
Clorazepic acid	The risk or severity of adverse effects can be increased when Rufinamide is combined with Clorazepic acid.
Dexmedetomidine	The risk or severity of adverse effects can be increased when Rufinamide is combined with Dexmedetomidine.

Target Protein

Sodium channel protein type 9 subunit alpha SCN9A

Metabotropic glutamate receptor 5 GRM5

Referensi & Sumber

Synthesis reference: Emanuele ATTOLINO, Lino COLOMBO, Ilaria MORMINO, Pietro ALLEGRINI, "METHOD FOR THE PREPARATION OF RUFINAMIDE." U.S. Patent US20100234616, issued September 16, 2010.

Artikel (PubMed)

PMID: 17199032
Arroyo S: Rufinamide. Neurotherapeutics. 2007 Jan;4(1):155-62.
PMID: 17696794
Hakimian S, Cheng-Hakimian A, Anderson GD, Miller JW: Rufinamide: a new anti-epileptic medication. Expert Opin Pharmacother. 2007 Aug;8(12):1931-40.
PMID: 15991887
Authors unspecified: Rufinamide: CGP 33101, E 2080, RUF 331, Xilep. Drugs R D. 2005;6(4):249-52.
PMID: 21351809
Wier HA, Cerna A, So TY: Rufinamide for pediatric patients with Lennox-Gastaut syndrome: a comprehensive overview. Paediatr Drugs. 2011 Apr 1;13(2):97-106. doi: 10.2165/11586920-000000000-00000.

Contoh Produk & Brand

Produk: 50 • International brands: 0

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Menampilkan 8 dari 50 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.

Peringatan Keamanan

Deskripsi

Struktur Molekul 2D

Deskripsi metode visualisasi

1. Pendahuluan & Konsep

2. Sumber Data (Validasi)

3. Algoritma Visualisasi

4. Legenda Visual