| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Rufinamide (also known as CGP-33101; E-2080; RUF-331; BANZEL; Inovelon) is a voltage-gated sodium channel blocker approved as an antiepilepic agent for seizure treatment. It is a board spectrum anticonvulsant that is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other seizure disorders. Rufinamide has efficacy for partial seizures. Rufinamide prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons.
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| ln Vivo |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
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. Renally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated. 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. Metabolism / Metabolites 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. Biological Half-Life Elimination half-life, healthy subjects and patients with epilepsy = 6-10 hours. |
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| Toxicity/Toxicokinetics |
Hepatotoxicity
In prelicensure clinical trials, addition of rufinamide to standard anticonvulsant therapy was reported to be associated with only rare elevations in ALT above 3 times the upper limit of normal (ULN). Rufinamide was not linked to instances of clinically apparent liver injury, but a pooled analysis of more than 200 children mentioned that two patients needed to discontinue therapy early because of liver related adverse events, one of which was described as “toxic hepatitis”. Since approval, there have been no reports of clinically apparent liver injury associated with rufinamide use, but it has had limited use in epilepsy. Rufinamide has been linked to instances of severe cutaneous reactions, including Stevens Johnson syndrome which often has some degree of associated liver injury. Thus, rufinamide may cause liver injury, but it is rare. Likelihood score: E* (unproven but suspected cause of clinically apparent liver injury). Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Because no information is available on the use of rufinamide during breastfeeding and because it is potentially toxic to the breastfed infant, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding 26.3% - 34.8% with 90% binding to albumin (27%). |
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| References |
Int J Clin Pract.2006Nov;60(11):1497-501;J Vet Pharmacol Ther.2012 Dec;35(6):529-33
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| Additional Infomation |
Rufinamide is a heteroarene and an aromatic amide.
Rufinamide is a triazole derivative and an anticonvulsant medication to treat seizure disorders like Lennox-Gastuat syndrome, a form of childhood epilepsy. Clinical trials suggest its efficacy in the treatment of partial seizures. Rufinamide is a unique anticonvulsant that is used in combination with other agents as therapy of severe forms of seizure disorders. Rufinamide therapy is associated with a low rate of transient serum enzyme elevations and with rare instances of clinically apparent liver injury. Drug Indication Adjunct therapy for treatment of seizures associated with Lennox-Gastaut syndrome. FDA Label Inovelon is indicated as adjunctive therapy in the treatment of seizures associated with Lennox Gastaut syndrome in patients 4 years of age and older. Treatment of Lennox-Gastaut syndrome Mechanism of Action Rufinamide is a triazole derivative antiepileptic that prolongs the inactive state of voltage gated sodium channels thus stabilizing membranes, ultimately blocking the spread of partial seizure activity. |
| Molecular Formula |
C10H8F2N4O
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|---|---|
| Molecular Weight |
238.19
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| Exact Mass |
238.066
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| CAS # |
106308-44-5
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| Related CAS # |
Rufinamide-d2;1129491-38-8;Rufinamide-15N,d2;1795037-48-7
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| PubChem CID |
129228
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
473.8±55.0 °C at 760 mmHg
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| Melting Point |
232-234?C
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| Flash Point |
240.4±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.635
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| LogP |
0.05
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
282
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
POGQSBRIGCQNEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17)
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| Chemical Name |
1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
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| Synonyms |
E-2080; RUF-331; E2080; CGP-33101; RUF331; CGP 33101; E 2080; RUF 331; CGP33101; Trade names: BANZEL; Inovelon.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1983 mL | 20.9916 mL | 41.9833 mL | |
| 5 mM | 0.8397 mL | 4.1983 mL | 8.3967 mL | |
| 10 mM | 0.4198 mL | 2.0992 mL | 4.1983 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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