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Details

Stereochemistry ABSOLUTE
Molecular Formula C13H18N2O3
Molecular Weight 250.2941
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LACOSAMIDE

SMILES

CC(=N[C@]([H])(COC)C(=NCc1ccccc1)O)O

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 250.2941
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

1.225152E12
Palliative
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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 (max)
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
n = 21
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 21
Sources:
Other AEs: Vomiting, Dizziness...
Other AEs:
Vomiting (4.8%)
Dizziness (4.8%)
Sources:
5.82 mg/kg 1 times / day multiple, oral (mean)
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
n = 47
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 47
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
Co-administed with::
zonisamide
topiramate
gabapentin
Sources:
unhealthy
n = 1
Health Status: unhealthy
Population Size: 1
Sources:
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
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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 (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 270
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 270
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 471
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 471
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
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
n = 203
Health Status: unhealthy
Condition: partial-onset seizures
Age Group: adult
Population Size: 203
Sources:
Dizziness 4.8%
12 mg/kg 1 times / day multiple, oral (max)
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
n = 21
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 21
Sources:
Vomiting 4.8%
12 mg/kg 1 times / day multiple, oral (max)
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
n = 21
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 21
Sources:
Dizziness 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral (mean)
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
n = 47
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 47
Sources:
Gait disturbance 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral (mean)
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
n = 47
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 47
Sources:
Somnolence 6.4%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral (mean)
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
n = 47
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 47
Sources:
Vomiting 8.5%
Disc. AE
5.82 mg/kg 1 times / day multiple, oral (mean)
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
n = 47
Health Status: unhealthy
Condition: focal seizures
Age Group: ≥1 month ≤17 years
Sex: M+F
Population Size: 47
Sources:
Coma
12 g single, oral
Overdose
Dose: 12 g
Route: oral
Route: single
Dose: 12 g
Co-administed with::
zonisamide
topiramate
gabapentin
Sources:
unhealthy
n = 1
Health Status: unhealthy
Population Size: 1
Sources:
Aphasia severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Coordination abnormal severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Dysarthria severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Dysphemia severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Negative thoughts severe, 1 patient
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Muscle weakness severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Nausea severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
Sources:
Vomiting severe, 2 patients
800 mg single, oral
Studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy
n = 34
Health Status: healthy
Sex: M+F
Population Size: 34
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 72
Health Status: unhealthy
Condition: Migraine
Population Size: 72
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 78
Health Status: unhealthy
Condition: Fibromyalgia Syndrome
Population Size: 78
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
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
n = 74
Health Status: unhealthy
Condition: Migraine
Population Size: 74
Sources:
Fatigue below serious, 4 patients
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Vertigo below serious, 8 patients
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Angina pectoris serious, 1 patient
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Breast cancer in situ serious, 1 patient
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Hypoglycaemic shock serious, 1 patient
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Liver disorder serious, 1 patient
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
Sources:
Sick sinus syndrome serious, 1 patient
400 mg steady, oral (total daily dose)
Dose: 400 mg
Route: oral
Route: steady
Dose: 400 mg
Sources:
unhealthy
n = 72
Health Status: unhealthy
Condition: Osteoarthritis
Population Size: 72
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
Pregabalin for the management of partial epilepsy.
2008 Dec
Lacosamide.
2008 Dec
New epilepsy treatment receives FDA approval.
2008 Dec 15
Lacosamide for the treatment of diabetic neuropathic pain.
2008 Nov
[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
Paroxysmal extreme pain disorder M1627K mutation in human Nav1.7 renders DRG neurons hyperexcitable.
2008 Sep 19
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
Lacosamide: in partial-onset seizures.
2009
Gateways to clinical trials.
2009 Apr
Lacosamide in painful diabetic neuropathy: an 18-week double-blind placebo-controlled trial.
2009 Aug
What is the promise of new antiepileptic drugs in status epilepticus? Focus on brivaracetam, carisbamate, lacosamide, NS-1209, and topiramate.
2009 Dec
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
Clinical perspectives on lacosamide.
2009 Jan-Feb
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
Transitional polytherapy: tricks of the trade for monotherapy to monotherapy AED conversions.
2009 Jun
Antiepileptic drug monotherapy: the initial approach in epilepsy management.
2009 Jun
Efficacy and safety of lacosamide in diabetic neuropathic pain: an 18-week double-blind placebo-controlled trial of fixed-dose regimens.
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
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions.
2009 Mar-Apr
Status epilepticus: a critical review.
2009 May
Schedules of controlled substances: placement of lacosamide into schedule V. Final rule.
2009 May 21
New drugs: Febuxostat, lacosamide, and rufinamide.
2009 May-Jun
Gateways to clinical trials.
2009 Nov
Painful diabetic neuropathy: advantage of novel drugs over old drugs?
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
Efficacy and safety of lacosamide in painful diabetic neuropathy.
2010 Apr
A high-performance liquid chromatography assay to monitor the new antiepileptic drug lacosamide in patients with epilepsy.
2010 Aug
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
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
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
Intravenous lacosamide as short-term replacement for oral lacosamide in partial-onset seizures.
2010 Jun
Epileptic seizures in AD patients.
2010 Mar
Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activities.
2010 May 13
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 Fri Jun 25 21:08:55 UTC 2021
Edited
by admin
on Fri Jun 25 21:08:55 UTC 2021
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
LACOSAMIDE [EMA EPAR]
Common Name English
LACOSAMIDE [VANDF]
Common Name English
SPM 927
Code English
ERLOSAMIDE
Common Name English
LACOSAMIDE [USAN]
Common Name English
PROPANAMIDE, 2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)-, (2R)-
Systematic Name English
(+)-(2R)-2-(ACETYLAMINO)-N-BENZYL-3-METHOXYPROPANAMIDE
Systematic Name English
LACOSAMIDE [WHO-DD]
Common Name English
VIMPAT
Brand Name English
LACOSAMIDE [MART.]
Common Name English
LACOSAMIDE CV [USP-RS]
Common Name English
LACOSAMIDE [INN]
Common Name English
ADD 243037
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 Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
DEA NO. 2746
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
EMA ASSESSMENT REPORTS VIMPAT (AUTHORIZED: EPILEPSY)
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
LIVERTOX 537
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
NDF-RT N0000175753
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
WHO-VATC QN03AX18
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
WHO-ATC N03AX18
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
NCI_THESAURUS C264
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
Code System Code Type Description
LACTMED
Lacosamide
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
IUPHAR
7472
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
NCI_THESAURUS
C83859
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
MERCK INDEX
M6651
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
LACOSAMIDE
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
RXCUI
623400
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY RxNorm
ChEMBL
CHEMBL58323
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
INN
8094
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
CAS
175481-36-4
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
FDA UNII
563KS2PQY5
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
MESH
C403507
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
DRUG BANK
DB06218
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
EVMPD
SUB25407
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
EPA CompTox
175481-36-4
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
USP_CATALOG
1357103
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY USP-RS
PUBCHEM
219078
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
PRIMARY
DRUG CENTRAL
4310
Created by admin on Fri Jun 25 21:08:55 UTC 2021 , Edited by admin on Fri Jun 25 21:08:55 UTC 2021
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
URINE
METABOLITE INACTIVE -> PARENT
Lacosamide does not inhibit or induce the cytochrome P450 enzyme family at therapeutic concentrations.
MAJOR
FECAL
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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