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
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
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 |
DescriptionCurator'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
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.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Voltage-gated sodium channels |
164.0 µM [EC50] | ||
Target ID: P47942 Gene ID: 25416.0 Gene Symbol: Dpysl2 Target Organism: Rattus norvegicus (Rat) |
|||
Target ID: CHEMBL3622 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22850102 |
1797.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | VIMPAT Approved UseVIMPAT 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 Date2008 |
|||
Palliative | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
13285.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38513537/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38513537/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22437449/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
225522.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38513537/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/38513537/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22437449/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/22437449/ |
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
Dose | Population | Adverse 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) Sources: Ataxia (>1) Vomiting (>1) Diplopia (>1) Nausea (>1) Vertigo (>1) Vision blurred (>1) |
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) Sources: Ataxia (>1) Vomiting (>1) Diplopia (>1) Nausea (>1) Vertigo (>1) Vision blurred (>1) |
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) Sources: Ataxia (>1) Vomiting (>1) Diplopia (>1) Nausea (>1) Vertigo (>1) Vision blurred (>1) |
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... |
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%) Sources: Gait disturbance (6.4%) Dizziness (6.4%) Somnolence (6.4%) |
12 g single, oral Overdose Dose: 12 g Route: oral Route: single Dose: 12 g Sources: |
unhealthy Health Status: unhealthy 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 Health Status: unhealthy Sources: |
|
800 mg single, oral Studied dose |
healthy |
Other AEs: Dysarthria, Dysphemia... Other AEs: Dysarthria (severe, 1 patient) Sources: 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) |
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 |
Other AEs: Myocardial infarction, Knee operation... Other AEs: Myocardial infarction (serious, 1 patient) Sources: 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) |
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 |
Other AEs: Vision blurred, Constipation... Other AEs: Vision blurred (below serious, 4 patients) Sources: 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) |
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 |
Other AEs: Coronary artery dissection, Vaginal infection... Other AEs: Coronary artery dissection (serious, 1 patient) Sources: 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) |
400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Other AEs: Angina pectoris, Sick sinus syndrome... Other AEs: Angina pectoris (serious, 1 patient) Sources: 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) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 Health Status: unhealthy Sources: |
|
Aphasia | severe, 1 patient | 800 mg single, oral Studied dose |
healthy |
Coordination abnormal | severe, 1 patient | 800 mg single, oral Studied dose |
healthy |
Dysarthria | severe, 1 patient | 800 mg single, oral Studied dose |
healthy |
Dysphemia | severe, 1 patient | 800 mg single, oral Studied dose |
healthy |
Negative thoughts | severe, 1 patient | 800 mg single, oral Studied dose |
healthy |
Muscle weakness | severe, 2 patients | 800 mg single, oral Studied dose |
healthy |
Nausea | severe, 2 patients | 800 mg single, oral Studied dose |
healthy |
Vomiting | severe, 2 patients | 800 mg single, oral Studied dose |
healthy |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
Fatigue | below serious, 4 patients | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Vertigo | below serious, 8 patients | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Angina pectoris | serious, 1 patient | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Breast cancer in situ | serious, 1 patient | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Hypoglycaemic shock | serious, 1 patient | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Liver disorder | serious, 1 patient | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Sick sinus syndrome | serious, 1 patient | 400 mg steady, oral Dose: 400 mg Route: oral Route: steady Dose: 400 mg Sources: |
unhealthy |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
PubMed
Title | Date | PubMed |
---|---|---|
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 |
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Adjunctive lacosamide for partial-onset seizures: Efficacy and safety results from a randomized controlled trial. | 2009 Mar |
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Long-term oral lacosamide in painful diabetic neuropathy: a two-year open-label extension trial. | 2009 May |
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Gateways to clinical trials. | 2009 Nov |
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Painful diabetic neuropathy: advantage of novel drugs over old drugs? | 2009 Nov |
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Lacosamide: an adjunctive agent for partial-onset seizures and potential therapy for neuropathic pain. | 2009 Nov |
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Six months of postmarketing experience with adjunctive lacosamide in patients with pharmacoresistant focal epilepsy at a tertiary epilepsy center in Germany. | 2009 Nov |
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Lacosamide isothiocyanate-based agents: novel agents to target and identify lacosamide receptors. | 2009 Nov 12 |
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Lacosamide: new drug. Refractory partial epilepsy: optimise existing combinations. | 2009 Oct |
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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 |
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Lacosamide: what can be expected from the next new antiepileptic drug? | 2009 Sep-Oct |
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Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs. | 2010 Apr |
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Gateways to clinical trials. | 2010 Apr |
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Lacosamide intoxication in attempted suicide. | 2010 Apr |
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Efficacy and safety of lacosamide in painful diabetic neuropathy. | 2010 Apr |
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No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers. | 2010 Apr |
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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 |
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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 Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17461888
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
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NDF-RT |
N0000008486
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DEA NO. |
2746
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EMA ASSESSMENT REPORTS |
VIMPAT (AUTHORIZED: EPILEPSY)
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LIVERTOX |
NBK547940
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NDF-RT |
N0000175753
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WHO-VATC |
QN03AX18
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WHO-ATC |
N03AX18
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NCI_THESAURUS |
C264
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Code System | Code | Type | Description | ||
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Lacosamide
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RR-116
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m6651
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LACOSAMIDE
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623400
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100000089434
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CHEMBL58323
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219078
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METABOLIC ENZYME -> SUBSTRATE | |||
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
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BINDER->LIGAND |
BINDING
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE INACTIVE -> PARENT |
Lacosamide does not inhibit or induce the cytochrome P450 enzyme family at therapeutic concentrations.
MAJOR
FECAL
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
MINOR
URINE
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Volume of Distribution | PHARMACOKINETIC |
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