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 Date1.225152E12 |
|||
Palliative | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
---|---|---|---|---|
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 |
---|---|---|---|---|
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 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) 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 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) 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 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) Sources: Ataxia (>1) Vomiting (>1) Diplopia (>1) Nausea (>1) Vertigo (>1) Vision blurred (>1) |
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... |
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%) 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 Co-administed with:: zonisamide Sources: topiramate gabapentin |
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 Health Status: unhealthy Sources: |
|
800 mg single, oral Studied dose |
healthy n = 34 |
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 n = 72 Health Status: unhealthy Condition: Migraine Population Size: 72 Sources: |
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 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) 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 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) 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 (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) 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 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 Sources: topiramate gabapentin |
unhealthy n = 1 Health Status: unhealthy Population Size: 1 Sources: |
|
Aphasia | severe, 1 patient | 800 mg single, oral Studied dose |
healthy n = 34 |
Coordination abnormal | severe, 1 patient | 800 mg single, oral Studied dose |
healthy n = 34 |
Dysarthria | severe, 1 patient | 800 mg single, oral Studied dose |
healthy n = 34 |
Dysphemia | severe, 1 patient | 800 mg single, oral Studied dose |
healthy n = 34 |
Negative thoughts | severe, 1 patient | 800 mg single, oral Studied dose |
healthy n = 34 |
Muscle weakness | severe, 2 patients | 800 mg single, oral Studied dose |
healthy n = 34 |
Nausea | severe, 2 patients | 800 mg single, oral Studied dose |
healthy n = 34 |
Vomiting | severe, 2 patients | 800 mg single, oral Studied dose |
healthy n = 34 |
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Drug as victim
PubMed
Title | Date | PubMed |
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Management of painful diabetic neuropathy: what is new or in the pipeline for 2007? | 2007 Dec |
|
Pharmacological management of epilepsy: recent advances and future prospects. | 2008 |
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The effectiveness of anticonvulsants in psychiatric disorders. | 2008 |
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Pregabalin for the management of partial epilepsy. | 2008 Dec |
|
Lacosamide. | 2008 Dec |
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New epilepsy treatment receives FDA approval. | 2008 Dec 15 |
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Lacosamide: an investigational drug for adjunctive treatment of partial-onset seizures. | 2008 Jan |
|
The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels. | 2008 Jan |
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Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepine. | 2008 Jul |
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Lacosamide, the new anticonvulsant, effectively reduces harmaline-induced tremors in rats. | 2008 Jul 28 |
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Gateways to clinical trials. | 2008 Mar |
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Intravenous lacosamide as replacement for oral lacosamide in patients with partial-onset seizures. | 2008 Mar |
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Painful diabetic neuropathy: treatment and future aspects. | 2008 May-Jun |
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Lacosamide for the treatment of diabetic neuropathic pain. | 2008 Nov |
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[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: in partial-onset seizures. | 2009 |
|
Gateways to clinical trials. | 2009 Apr |
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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 |
|
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 |
|
Clinical perspectives on lacosamide. | 2009 Jan-Feb |
|
Efficacy and safety of lacosamide in diabetic neuropathic pain: an 18-week double-blind placebo-controlled trial of fixed-dose regimens. | 2009 Jun |
|
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 |
|
Long-term oral lacosamide in painful diabetic neuropathy: a two-year open-label extension trial. | 2009 May |
|
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 |
|
Lacosamide: an adjunctive agent for partial-onset seizures and potential therapy for neuropathic pain. | 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 |
|
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs. | 2010 Apr |
|
Lacosamide intoxication in attempted suicide. | 2010 Apr |
|
No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers. | 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 |
|
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 |
|
Lacosamide as treatment of epileptic seizures - cost utility results for Sweden. | 2010 Jun |
|
Intravenous lacosamide as short-term replacement for oral lacosamide in partial-onset seizures. | 2010 Jun |
|
Recommendations for the pharmacological management of neuropathic pain: an overview and literature update. | 2010 Mar |
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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Wed Jul 05 23:40:50 UTC 2023
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563KS2PQY5
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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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1357103
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7472
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C83859
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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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175481-36-4
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DB06218
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SUB25407
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DTXSID1057666
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563KS2PQY5
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219078
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4310
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Related Record | Type | Details | ||
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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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PARENT->INACTIVE ISOMER |
Related Record | Type | Details | ||
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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
|
Related Record | Type | Details | ||
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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 |
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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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