| 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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| Other Sizes |
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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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The oral suspension and tablets are bioequivalent on a mg/mg basis. Lufedipine is well absorbed, but at a slow rate, and the extent of absorption decreases with increasing dose. Based on urinary excretion, a single oral dose of 600 mg lumfedipine tablets in a fed state results in at least 85% absorption. Bioavailability = 70%-85% (decreasing with increasing dose); Time to peak concentration (Tmax), in both fed and fasting states = 4-6 hours; Peak plasma concentration (Cmax), 10 mg/kg/day = 4.01 µL/mL; Peak plasma concentration (Cmax), 30 mg/kg/day = 8.68 µL/mL; AUC (0-12 hours), 10 mg/kg/day = 37.8 ± 47 µg·h/mL; AUC (0-12 hours), 30 mg/kg/day = 89.3 ± 59 µg·h/mL. Primarily excreted via the kidneys (91%; of which 66% is CGP 47292 and 2% is the original drug) and feces (9%). Lufedipine is uniformly distributed in erythrocytes and plasma. The apparent volume of distribution is dose-dependent and varies with body surface area. At 3200 mg/day, the apparent volume of distribution is approximately 50 L. The volume of distribution is similar in adults and children and exhibits a non-linear variation. Metabolism/Metabolites Lufedipine is extensively metabolized, but has no active metabolites. Its primary biotransformation pathway is hydrolysis by carboxylesterases to the inactive metabolite CGP 47292 (a carboxylic acid derivative). Small amounts of other metabolites have been detected in urine, suspected to be acylglucuronide of CGP 47292. Cytochrome P450 enzyme systems or glutathione are not involved in the metabolism of lufedipine. Lufedipine is a weak inhibitor of CYP 2E1 and a weak inducer of CYP 3A4 enzymes. Biological Half-Life The elimination half-life in healthy subjects and patients with epilepsy is 6-10 hours. |
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| Toxicity/Toxicokinetics |
Hepatotoxicity
In premarket clinical trials, the addition of rufinamide to standard antiepileptic treatment regimens was reported to be associated only with rare ALT elevations (more than 3 times the upper limit of normal). Rufinamide was not associated with clinically significant liver injury cases, but a pooled analysis of over 200 children indicated that two patients required early discontinuation of treatment due to liver-related adverse events, one of which was described as "toxic hepatitis." Since its approval, there have been no reports of clinically significant liver injury associated with rufinamide use, but its use in epilepsy treatment is limited. Rufinamide has been associated with cases of severe skin reactions, including Stevens-Johnson syndrome, which is often accompanied by some degree of liver injury. Therefore, rufinamide may cause liver injury, but this is rare. Probability score: E (Unproven but suspected cause of clinically significant liver injury). Effects during pregnancy and lactation ◉ Overview of medication use during lactation Since there is currently no information on the use of rufenamide during lactation, and this drug may be toxic to breastfed infants, alternative medications should be preferred, especially for breastfed newborns or premature infants. ◉ Effects on breastfed infants As of the revision date, no relevant published information was found. ◉ Effects on lactation and breast milk As of the revision date, no relevant published information was found. Protein binding rate 26.3% - 34.8%, of which 90% is bound 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 heteroaryl hydrocarbon and aromatic amide. Lufedipine is a triazole derivative and an anticonvulsant used to treat epileptic seizure disorders, such as childhood epilepsy—Lennox-Gastaut syndrome. Clinical trials have shown its effectiveness in treating partial seizures. Lufedipine is a unique anticonvulsant, often used in combination with other drugs to treat severe epileptic seizure disorders. Lufedipine treatment is associated with a low incidence of transient serum enzyme elevations and rare cases of clinically significant liver injury. Drug Indications For adjunctive treatment of seizures associated with Lennox-Gastaut syndrome. FDA Label Inovelon is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut syndrome in patients aged 4 years and older.
Treatment of Lennox-Gastaut Syndrome Mechanism of Action Lufedipine is a triazole derivative antiepileptic drug that prolongs the inactive state of voltage-gated sodium channels, thereby stabilizing the cell membrane and ultimately preventing the spread of partial seizures. |
| 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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