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Details

Stereochemistry ABSOLUTE
Molecular Formula C13H18N2O3
Molecular Weight 250.2936
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Lacosamide

SMILES

COC[C@@H](NC(C)=O)C(=O)NCC1=CC=CC=C1

InChI

InChIKey=VPPJLAIAVCUEMN-GFCCVEGCSA-N
InChI=1S/C13H18N2O3/c1-10(16)15-12(9-18-2)13(17)14-8-11-6-4-3-5-7-11/h3-7,12H,8-9H2,1-2H3,(H,14,17)(H,15,16)/t12-/m1/s1

HIDE SMILES / InChI

Molecular Formula C13H18N2O3
Molecular Weight 250.2936
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including: https://www.drugs.com/pro/lacosamide.html | http://www.wikidoc.org/index.php/Lacosamide | https://www.ncbi.nlm.nih.gov/pubmed/17461888 | https://www.ncbi.nlm.nih.gov/pubmed/19552484

Lacosamide is an anticonvulsant that is FDA approved for the treatment of partial-onset seizures. The precise mechanism by which lacosamide exerts its antiepileptic effects in humans remains to be fully elucidated. In vitro electrophysiological studies have shown that lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing Common adverse reactions include diplopia, headache, dizziness, nausea. Patients with renal or hepatic impairment who are taking strong inhibitors of CYP3A4 and CYP2C9 may have a significant increase in exposure to Lacosamide tablets.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
164.0 µM [EC50]
1797.0 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VIMPAT

Approved Use

VIMPAT is indicated for: Partial-onset seizures (1.1): Tablets and oral solution are indicated for adjunctive therapy in patients ≥17 years. Injection is indicated as short term replacement when oral administration is not feasible in these patients. 1.1 Partial-Onset Seizures VIMPAT (lacosamide) tablets and oral solution are indicated as adjunctive therapy in the treatment of partial-onset seizures in patients with epilepsy aged 17 years and older. VIMPAT (lacosamide) injection for intravenous use is indicated as adjunctive therapy in the treatment of partial-onset seizures in patients with epilepsy aged 17 years and older when oral administration is temporarily not feasible.

Launch Date

2008
Palliative
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
13285.5 ng/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12730.8 ng/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
13.13 μg/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2935.3 ng/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
225522.2 ng × h/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
230511.9 ng × h/mL
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
112.35 μg × h/mL
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
59120 ng × h/mL
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
16.68 h
200 mg 2 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
14.47 h
100 mg 1 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
LACOSAMIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Disc. AE: Dizziness, Ataxia...
AEs leading to
discontinuation/dose reduction:
Dizziness (>1)
Ataxia (>1)
Vomiting (>1)
Diplopia (>1)
Nausea (>1)
Vertigo (>1)
Vision blurred (>1)
Sources:
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Disc. AE: Dizziness, Ataxia...
AEs leading to
discontinuation/dose reduction:
Dizziness (>1)
Ataxia (>1)
Vomiting (>1)
Diplopia (>1)
Nausea (>1)
Vertigo (>1)
Vision blurred (>1)
Sources:
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Disc. AE: Dizziness, Ataxia...
AEs leading to
discontinuation/dose reduction:
Dizziness (>1)
Ataxia (>1)
Vomiting (>1)
Diplopia (>1)
Nausea (>1)
Vertigo (>1)
Vision blurred (>1)
Sources:
12 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 12 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Other AEs: Vomiting, Dizziness...
Other AEs:
Vomiting (4.8%)
Dizziness (4.8%)
Sources:
5.82 mg/kg 1 times / day multiple, oral
Dose: 5.82 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 5.82 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Disc. AE: Vomiting, Gait disturbance...
AEs leading to
discontinuation/dose reduction:
Vomiting (8.5%)
Gait disturbance (6.4%)
Dizziness (6.4%)
Somnolence (6.4%)
Sources:
12 g single, oral
Overdose
Dose: 12 g
Route: oral
Route: single
Dose: 12 g
Sources:
unhealthy
Other AEs: Coma...
1200 mg 1 times / day multiple, oral
Overdose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
unhealthy
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Other AEs: Dysarthria, Dysphemia...
Other AEs:
Dysarthria (severe, 1 patient)
Dysphemia (severe, 1 patient)
Aphasia (severe, 1 patient)
Negative thoughts (severe, 1 patient)
Coordination abnormal (severe, 1 patient)
Muscle weakness (severe, 2 patients)
Nausea (severe, 2 patients)
Vomiting (severe, 2 patients)
Sources:
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Myocardial infarction, Knee operation...
Other AEs:
Myocardial infarction (serious, 1 patient)
Knee operation (serious, 1 patient)
Diarrhoea (below serious, 4 patients)
Fatigue (below serious, 5 patients)
Nasopharyngitis (below serious, 12 patients)
Bronchitis (below serious, 2 patients)
Sinusitis (below serious, 4 patients)
Upper respiratory tract infection (below serious, 7 patients)
Dizziness (below serious, 5 patients)
Oropharyngeal pain (below serious, 3 patients)
Sources:
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Vision blurred, Constipation...
Other AEs:
Vision blurred (below serious, 4 patients)
Constipation (below serious, 5 patients)
Hypoaesthesia oral (below serious, 4 patients)
Nausea (below serious, 13 patients)
Vomiting (below serious, 5 patients)
Back pain (below serious, 4 patients)
Pain in extremity (below serious, 4 patients)
Balance disorder (below serious, 4 patients)
Dizziness (below serious, 18 patients)
Somnolence (below serious, 5 patients)
Pruritus (below serious, 7 patients)
Sources:
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Coronary artery dissection, Vaginal infection...
Other AEs:
Coronary artery dissection (serious, 1 patient)
Vaginal infection (serious, 1 patient)
Fatigue (below serious, 11 patient)
Nasopharyngitis (below serious, 11 patient)
Bronchitis (below serious, 4 patients)
Sinusitis (below serious, 3 patients)
Oropharyngeal pain (below serious, 4 patients)
Sources:
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Angina pectoris, Sick sinus syndrome...
Other AEs:
Angina pectoris (serious, 1 patient)
Sick sinus syndrome (serious, 1 patient)
Liver disorder (serious, 1 patient)
Hypoglycaemic shock (serious, 1 patient)
Breast cancer in situ (serious, 1 patient)
Vertigo (below serious, 8 patients)
Fatigue (below serious, 4 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Ataxia >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Diplopia >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Dizziness >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Nausea >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vertigo >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vision blurred >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vomiting >1
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Ataxia >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Diplopia >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Dizziness >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Nausea >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vertigo >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vision blurred >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vomiting >1
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Ataxia >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Diplopia >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Dizziness >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Nausea >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vertigo >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vision blurred >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Vomiting >1
Disc. AE
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
Dizziness 4.8%
12 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 12 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Vomiting 4.8%
12 mg/kg 1 times / day multiple, oral
Studied dose
Dose: 12 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 12 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Dizziness 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral
Dose: 5.82 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 5.82 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Gait disturbance 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral
Dose: 5.82 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 5.82 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Somnolence 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral
Dose: 5.82 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 5.82 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Vomiting 8.5%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral
Dose: 5.82 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 5.82 mg/kg, 1 times / day
Sources:
unhealthy, ≥1 month ≤17 years
Health Status: unhealthy
Age Group: ≥1 month ≤17 years
Sex: M+F
Sources:
Coma
12 g single, oral
Overdose
Dose: 12 g
Route: oral
Route: single
Dose: 12 g
Sources:
unhealthy
Aphasia severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Coordination abnormal severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Dysarthria severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Dysphemia severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Negative thoughts severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Muscle weakness severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Nausea severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Vomiting severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
Health Status: healthy
Sex: M+F
Sources:
Nasopharyngitis below serious, 12 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Bronchitis below serious, 2 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Oropharyngeal pain below serious, 3 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Diarrhoea below serious, 4 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Sinusitis below serious, 4 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dizziness below serious, 5 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Fatigue below serious, 5 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Upper respiratory tract infection below serious, 7 patients
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Knee operation serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Myocardial infarction serious, 1 patient
100 mg 2 times / day steady, oral
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nausea below serious, 13 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dizziness below serious, 18 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Back pain below serious, 4 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Balance disorder below serious, 4 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hypoaesthesia oral below serious, 4 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pain in extremity below serious, 4 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Vision blurred below serious, 4 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Constipation below serious, 5 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Somnolence below serious, 5 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Vomiting below serious, 5 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pruritus below serious, 7 patients
200 mg 2 times / day steady, oral
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Fatigue below serious, 11 patient
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nasopharyngitis below serious, 11 patient
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Sinusitis below serious, 3 patients
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Bronchitis below serious, 4 patients
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Oropharyngeal pain below serious, 4 patients
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Coronary artery dissection serious, 1 patient
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Vaginal infection serious, 1 patient
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Fatigue below serious, 4 patients
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Vertigo below serious, 8 patients
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Angina pectoris serious, 1 patient
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Breast cancer in situ serious, 1 patient
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hypoglycaemic shock serious, 1 patient
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Liver disorder serious, 1 patient
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
Sick sinus syndrome serious, 1 patient
400 mg steady, oral
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
Health Status: unhealthy
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
inconclusive
inconclusive
inconclusive
inconclusive
inconclusive
inconclusive
likely (co-administration study)
Comment: POP-PK results showed that lacosamide exposure decreased 20% in the presence of carbamazepine, phenytoin, or phenobarbital
Page: 46.0
no
yes
no (co-administration study)
Comment: lacosamide had no effect on omeprazole PK
Page: 10, 46
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Pharmacological management of epilepsy: recent advances and future prospects.
2008
Lacosamide.
2008 Dec
New epilepsy treatment receives FDA approval.
2008 Dec 15
Lacosamide, the new anticonvulsant, effectively reduces harmaline-induced tremors in rats.
2008 Jul 28
Gateways to clinical trials.
2008 Mar
[Lacosamide. A new antiepileptic drug as adjunctive therapy in patients with partial-onset seizures].
2008 Oct
Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives.
2008 Oct 1
Lacosamide as treatment for partial epilepsy: mechanisms of action, pharmacology, effects, and safety.
2009
Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders.
2009
Gateways to clinical trials.
2009 Apr
The anti-epileptic drug lacosamide (Vimpat) has anxiolytic property in rodents.
2009 Dec 10
Intravenous lacosamide as successful treatment for nonconvulsive status epilepticus after failure of first-line therapy.
2009 Feb
Lacosamide: pharmacology, mechanisms of action and pooled efficacy and safety data in partial-onset seizures.
2009 Jan
Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX).
2009 Jan
Minimizing AED adverse effects: improving quality of life in the interictal state in epilepsy care.
2009 Jun
Truly "rational" polytherapy: maximizing efficacy and minimizing drug interactions, drug load, and adverse effects.
2009 Jun
Antiepileptic drug monotherapy: the initial approach in epilepsy management.
2009 Jun
Lacosamide for epilepsy.
2009 Jun 29
Adjunctive lacosamide for partial-onset seizures: Efficacy and safety results from a randomized controlled trial.
2009 Mar
Long-term oral lacosamide in painful diabetic neuropathy: a two-year open-label extension trial.
2009 May
Gateways to clinical trials.
2009 Nov
Painful diabetic neuropathy: advantage of novel drugs over old drugs?
2009 Nov
Lacosamide: an adjunctive agent for partial-onset seizures and potential therapy for neuropathic pain.
2009 Nov
Six months of postmarketing experience with adjunctive lacosamide in patients with pharmacoresistant focal epilepsy at a tertiary epilepsy center in Germany.
2009 Nov
Lacosamide isothiocyanate-based agents: novel agents to target and identify lacosamide receptors.
2009 Nov 12
Lacosamide: new drug. Refractory partial epilepsy: optimise existing combinations.
2009 Oct
Pharmacology and treatment of neuropathic pains.
2009 Oct
Effects of lacosamide, a novel sodium channel modulator, on dorsal horn neuronal responses in a rat model of neuropathy.
2009 Sep
Lacosamide: what can be expected from the next new antiepileptic drug?
2009 Sep-Oct
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs.
2010 Apr
Gateways to clinical trials.
2010 Apr
Lacosamide intoxication in attempted suicide.
2010 Apr
Efficacy and safety of lacosamide in painful diabetic neuropathy.
2010 Apr
No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers.
2010 Apr
In silico docking and electrophysiological characterization of lacosamide binding sites on collapsin response mediator protein-2 identifies a pocket important in modulating sodium channel slow inactivation.
2010 Aug 13
New Drugs2010, PART 1.
2010 Feb
Successful treatment for refractory convulsive status epilepticus by non-parenteral lacosamide.
2010 Feb
Drug interactions involving the new second- and third-generation antiepileptic drugs.
2010 Jan
Comparative study of five antiepileptic drugs on a translational cognitive measure in the rat: relationship to antiepileptic property.
2010 Jan
The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors.
2010 Jan 28
Update on anticonvulsant drugs.
2010 Jul
Lacosamide: new adjunctive treatment option for partial-onset seizures.
2010 Jun
Lacosamide as adjunctive therapy for partial-onset seizures: a randomized controlled trial.
2010 Jun
Intravenous lacosamide as short-term replacement for oral lacosamide in partial-onset seizures.
2010 Jun
Proteomic searches comparing two (R)-lacosamide affinity baits: An electrophilic arylisothiocyanate and a photoactivated arylazide group.
2010 Jun 21
Epileptic seizures in AD patients.
2010 Mar
[Antiepileptic drugs in North America].
2010 May
Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.
2010 May 13
[The use of oral lacosamide in a patient with refractory partial epileptic status].
2010 May 16
Emerging drugs for partial onset seizures.
2010 Sep
Patents

Sample Use Guides

Initially, give 50 mg twice daily (100 mg/day). The dose may be increased, based on clinical response and tolerability, at weekly intervals by 100 mg/day given as two divided doses to a daily dose of 200 to 400 mg/day.
Route of Administration: Other
In recombinant systems the effect of LCM on the potassium current mediated by the human hERG channel was studied. Inhibition of this channel has been associated with fatal arrhythmias. LCM only minimally affected hERG current at concentrations as high as 3000 uM/L.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:22:20 GMT 2025
Edited
by admin
on Mon Mar 31 18:22:20 GMT 2025
Record UNII
563KS2PQY5
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Lacosamide
DASH   EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
MOTPOLY
Preferred Name English
Lacosamide [WHO-DD]
Common Name English
LACOSAMIDE [EMA EPAR]
Common Name English
LACOSAMIDE [VANDF]
Common Name English
LACOSAMIDE [USP MONOGRAPH]
Common Name English
SPM927
Code English
ERLOSAMIDE
Common Name English
Propanamide, 2-(acetylamino)-3-methoxy-N-(phenylmethyl)-, (2R)-
Systematic Name English
LACOSAMIDE [USAN]
Common Name English
(+)-(2R)-2-(ACETYLAMINO)-N-BENZYL-3-METHOXYPROPANAMIDE
Systematic Name English
(2R)-2-(Acetylamino)-3-methoxy-N-(phenylmethyl)propanamide
Systematic Name English
VIMPAT
Brand Name English
LACOSAMIDE [MART.]
Common Name English
LACOSAMIDE [USP-RS]
Common Name English
lacosamide [INN]
Common Name English
ADD243037
Code English
LACOSAMIDE [MI]
Common Name English
LACOSAMIDE [EP MONOGRAPH]
Common Name English
LACOSAMIDE [ORANGE BOOK]
Common Name English
ADD-243037
Code English
(R)-LACOSAMIDE 1
Common Name English
SPM-927
Code English
LACOSAMIDE [JAN]
Common Name English
Classification Tree Code System Code
NDF-RT N0000008486
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
DEA NO. 2746
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
EMA ASSESSMENT REPORTS VIMPAT (AUTHORIZED: EPILEPSY)
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
LIVERTOX NBK547940
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
NDF-RT N0000175753
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
WHO-VATC QN03AX18
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
WHO-ATC N03AX18
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
NCI_THESAURUS C264
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
Code System Code Type Description
LACTMED
Lacosamide
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
USAN
RR-116
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
RS_ITEM_NUM
1357103
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
IUPHAR
7472
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
NCI_THESAURUS
C83859
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
MERCK INDEX
m6651
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY Merck Index
WIKIPEDIA
LACOSAMIDE
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
RXCUI
623400
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY RxNorm
SMS_ID
100000089434
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
ChEMBL
CHEMBL58323
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
INN
8094
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
CAS
175481-36-4
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
FDA UNII
563KS2PQY5
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
MESH
C403507
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
DRUG BANK
DB06218
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
EVMPD
SUB25407
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
EPA CompTox
DTXSID1057666
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
DAILYMED
563KS2PQY5
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
PUBCHEM
219078
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
DRUG CENTRAL
4310
Created by admin on Mon Mar 31 18:22:20 GMT 2025 , Edited by admin on Mon Mar 31 18:22:20 GMT 2025
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
BINDER->LIGAND
BINDING
PARENT->INACTIVE ISOMER
Related Record Type Details
METABOLITE -> PARENT
MINOR
URINE
METABOLITE -> PARENT
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METABOLITE -> PARENT
MINOR
URINE
METABOLITE INACTIVE -> PARENT
Lacosamide does not inhibit or induce the cytochrome P450 enzyme family at therapeutic concentrations.
MAJOR
FECAL
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
MINOR
URINE
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CHROMATOGRAPHIC PURITY (HPLC/UV)
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IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
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Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC