Lacosamide

250.29

250.29

1308068-626-2

563KS2PQY5

2746

DTXSID1057666

C83859

N03AX18|N - Nervous system

2924296000

67.4

0.728

1.120±0.06 g/cm3(Predicted)

142-143 °C @ Solvent: Ethyl acetate

536.447

2℃

1.520

Lacosamide is a white to light yellow powder. It is sparingly soluble in water and slightly soluble in acetonitrile and ethanol.

Refrigerator

1.4E-11mmHg at 25°C

D23 +16.0° (c = 1 in CH3OH)

UN 1648 3 / PGII

2

11-20/21/22-36

16-26-36/37

F,Xn

P210-P280-P305 + P351 + P338

H225-H302 + H312 + H332-H319

|Danger|H301 (95.31%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P280, P301+P310, P305+P351+P338, P321, P330, P337+P313, P405, and P501|Aggregated GHS information provided by 65 companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H301 (20%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P301+P312, P304+P312, P304+P340, P305+P351+P338, P312, P321, P330, P337+P313, P405, and P501|Aggregated GHS information provided by 5 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

In prelicensure clinical trials, addition of lacosamide to standard anticonvulsant therapy was reported to be associated with ALT elevations above 3 times the upper limit of normal (ULN) in 7 of 935 patients (0.7%) compared to none of 356 treated with placebo. A single case of hepatitis with jaundice during lacosamide therapy was also reported. Since approval, there have been rare isolated reports of clinically apparent liver injury associated with lacosamide used, but the clinical features suggested that hepatic ischemia or other anticonvulsants combined with lacosamide may have been responsible. The onset was within a few days to several months after starting and the presentation was with a hepatocellular pattern of serum enzyme elevations, one case being asymptomatic and mild and the other severe. In both instances, there was rapid recovery.

<15%

Lacosamide is indicated for adjunctive therapy for partial onset seizures in patients with epilepsy over 17 years old. Injection is indicated for short term use when oral therapy is not feasible.|FDA Label|Vimpat is indicated as monotherapy and adjunctive therapy in the treatment of partial-onset seizures with or without secondary generalisation in adults, adolescents and children from 4 years of age with epilepsy.|Lacosamide Accord is indicated as monotherapy in the treatment of partial-onset seizures with or without secondary generalisation in adults, adolescents and children from 4 years of age with epilepsy.Lacosamide Accord is indicated as adjunctive therapy•         in the treatment of partial-onset seizures with or without secondary generalisation in adults, adolescents and children from 4 years of age with epilepsy.•         in the treatment of primary generalised tonic-clonic seizures in adults, adolescents and children from 4 years of age with idiopathic generalised epilepsy.|Lacosamide UCB is indicated as monotherapy and adjunctive therapy in the treatment of partial-onset seizures with or without secondary generalisation in adults, adolescents and children from 4 years of age with epilepsy.|Treatment of epilepsy with partial-onset seizures|Treatment of generalised epilepsy and epileptic syndromes

Lacosamide is an amino acid derivative with a unique anticonvulsant activity that is used in combination with other agents as therapy of partial onset seizures. Lacosamide therapy is associated with a low rate of transient serum enzyme elevations and has been linked to rare instances of clinically apparent liver injury.

Anticonvulsants

Lacosamide therapy is correlated with a decrease in seizure frequency. It should be noted that in group analyses, dosages above 400 mg/day do not appear to result in additional benefit.

A class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS. (See all compounds classified as Voltage-Gated Sodium Channel Blockers.)|Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)

Lacosamide has a negligible first pass effect with bioavailability of about 100%. The maximum Lacosamide plasma concentrations occur about 1-4 hours after oral administration, and the pharmacokinetics of Lacosamide are dose proportional. Food does not affect absorption.|Lacosamide is eliminated primarily from the systemic circulation by biotransformation and renal excretion.|approximately 0.6 L/kg; thus close to the volume of total body water.|95% recovered in the urine 0.5% in the feces

Lacosamide is a CYP2C19 substrate. The relative contribution of other CYP isoforms or non-CYP enzymes in the metabolism of lacosamide is not known. Primary compounds excreted were unchanged lacosamide (approximately 40% of the dose), its O-desmethyl metabolite (approximately 30%), and a structurally unknown polar fraction (~20%). The plasma exposure of the major human metabolite, O-desmethyl-lacosamide, is approximately 10% of that of lacosamide. This metabolite has no known pharmacological activity.

13 Hours

It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Lacosamide may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Lacosamide binds to collapsin response mediator protein-2 (CRMP-2), a phosphoprotein which is expressed primarily in the nervous system and is involved in neuronal differentiation and control of axonal outgrowth. The role CRMP-2 of binding in seizure control is hasn't been elucidated.

lacosamide

Lacosamide|Vimpat|2746|Schedule V - Substances in the DEA Schedule V have a low potential for abuse relative to substances listed in Schedule IV and consist primarily of preparations containing limited quantities of certain narcotics.|No

Human drugs -> Vimpat -> EMA Drug Category|Antiepileptics -> Human pharmacotherapeutic group|Human drugs -> Lacosamide Accord -> EMA Drug Category|Human drugs -> Lacosamide UCB -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients