Lacosamide

Lacosamide
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [2]; Associate Editor(s)-in-Chief: Stefano Giannoni [3]

Disclaimer

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Overview

Lacosamide is an anticonvulsant that is FDA approved for the treatment of partial-onset seizures. Common adverse reactions include diplopia, headache, dizziness, nausea.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

There is limited information regarding Lacosamide FDA-Labeled Indications and Dosage (Adult) in the drug label.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lacosamide in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lacosamide in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Lacosamide FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lacosamide in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lacosamide in pediatric patients.

Contraindications

• None

Warnings

There is limited information regarding Lacosamide Warnings' in the drug label.

Adverse Reactions

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

In the premarketing development of adjunctive therapy for partial onset seizures, 1327 patients received lacosamide in controlled and uncontrolled trials, of whom 1000 were treated for longer than 6 months, and 852 for longer than 12 months. The monotherapy development program included 425 patients, 310 of whom were treated for longer than 6 months, and 254 for longer than 12 months.

lacosamide Tablet and Oral solution

Monotherapy Historical-Control Trial (Study 1)

In the monotherapy trial, 16% of patients randomized to receive lacosamide at the recommended doses of 300 and 400 mg/day discontinued from the trial as a result of an adverse event. The adverse reaction most commonly (≥1% on lacosamide) leading to discontinuation was dizziness.

Adverse reactions observed in this study were generally similar to those observed and attributed to drug in adjunctive placebo-controlled studies. One adverse reaction, insomnia, was observed at a rate of ≥2% and was not reported at a similar rate in previous studies. This adverse reaction has also been observed in postmarketing experience [see ADVERSE REACTIONS (6.2)]. Because this study did not include a placebo control group, causality could not be established.

Dizziness, headache, nausea, somnolence, and fatigue were all reported at lower incidences during the AED Withdrawal Phase and Monotherapy Phase, compared with the Titration Phase [see CLINICAL STUDIES (14.1)].

Adjunctive Therapy Controlled Trials (Studies 2, 3, and 4)

In adjunctive therapy controlled clinical trials, the rate of discontinuation as a result of an adverse event was 8% and 17% in patients randomized to receive lacosamide at the recommended doses of 200 and 400 mg/day, respectively, 29% at 600 mg/day, and 5% in patients randomized to receive placebo. The adverse events most commonly (>1% on lacosamide and greater than placebo) leading to discontinuation were dizziness, ataxia, vomiting, diplopia, nausea, vertigo, and vision blurred.

Table 2 gives the incidence of treatment-emergent adverse events that occurred in ≥2% of adult patients with partial-onset seizures in the lacosamide total group and for which the incidence was greater than placebo. The majority of adverse events in the lacosamide patients were reported with a maximum intensity of 'mild' or 'moderate'.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of lacosamide. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Blood and lymphatic system disorders: Agranulocytosis

Psychiatric disorders: Aggression, agitation, hallucination, insomnia, psychotic disorder

Skin and subcutaneous tissue disorders: Angioedema, rash, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Drug Interactions

There is limited information regarding Lacosamide Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Lacosamide in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lacosamide in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Lacosamide during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Lacosamide in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Lacosamide in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Lacosamide in geriatric settings.

Gender

There is no FDA guidance on the use of Lacosamide with respect to specific gender populations.

Race

There is no FDA guidance on the use of Lacosamide with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Lacosamide in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Lacosamide in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Lacosamide in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Lacosamide in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Lacosamide Administration in the drug label.

Monitoring

There is limited information regarding Lacosamide Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Lacosamide and IV administrations.

Overdosage

There is limited information regarding Lacosamide overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Lacosamide Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Lacosamide Mechanism of Action in the drug label.

Structure

There is limited information regarding Lacosamide Structure in the drug label.

Pharmacodynamics

There is limited information regarding Lacosamide Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Lacosamide Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Lacosamide Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Lacosamide Clinical Studies in the drug label.

How Supplied

There is limited information regarding Lacosamide How Supplied in the drug label.

Storage

There is limited information regarding Lacosamide Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Lacosamide Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Lacosamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Lacosamide Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Lacosamide Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Lacosamide

File:Lacosamide.svg
Clinical data
Trade names	lacosamide
Synonyms	(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide
AHFS/Drugs.com	Monograph
MedlinePlus	a609028
Routes of administration	Oral, intravenous
ATC code	N03AX18 (WHO)
Legal status
Legal status	Schedule V (U.S.)
Pharmacokinetic data
Bioavailability	High
Elimination half-life	13 hours
Identifiers
IUPAC name N2-acetyl-N-benzyl-D-homoserinamide
CAS Number	175481-36-4 N
PubChem CID	219078
ChemSpider	189902 Y
UNII	563KS2PQY5
KEGG	D07299 Y
ChEMBL	ChEMBL58323 Y
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C13H18N2O3
Molar mass	250.294 g/mol
3D model (JSmol)	Interactive image
SMILES O=C(N[C@@H](C(=O)NCc1ccccc1)COC)C
InChI 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 Y Key:VPPJLAIAVCUEMN-GFCCVEGCSA-N Y
NY (what is this?)  (verify)

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [4]

Overview

Lacosamide (INN, formerly known as erlosamide) is a medication developed by UCB for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain marketed under the trade name lacosamide.

The U.S. Food and Drug Administration accepted UCB's New Drug Application for lacosamide as of November 29, 2007, beginning the approval process for the drug. UCB also filed for marketing approval in the European Union; the European Medicines Agency accepted the marketing application for review in May 2007.

The drug was approved in the EU on September 3, 2008. It was approved in the US on October 29, 2008. Lacosamide release was delayed owing to an objection about its placement into schedule V of the Controlled Substances Act. The FDA issued their final rule of placement into Schedule V on June 22, 2009.

Mechanism of action

Lacosamide is a functionalized amino acid that has activity in the maximal electroshock seizure test, like antiepileptic drugs that are believed to act through voltage-gated sodium channels. However, lacosamide does not act in a conventional way to stabilize fast sodium channel inactivation. Rather, recent studies indicate that it enhances slow inactivation . During an action potential voltage gated sodium channels undergo fast inactivation. This inactivation prevents the channel from opening, and helps end the action potential. Many antiepileptic drugs, like carbamazepine or lamotrigine, slow the recovery from inactivation and hence reduce the ability of neurons to fire action potentials. Inactivation only occurs in neurons firing action potentials, this means that drugs that modulate fast inactivation selectively reduce the firing in active cells. Slow inactivation is similar but does not produce complete blockade of voltage gated sodium channels, with both activation and inactivation occurring over hundreds of milliseconds or more. Lacosamide makes this inactivation happen at less depolarized membrane potentials. This means that lacosamide only affects neurons which are depolarized or active for long periods of time, typical of neurons at the focus of an epileptic focus.

Lacosamide does not affect AMPA, kainate, NMDA, GABA_A, GABA_B or a variety of dopaminergic, serotonergic, adrenergic, muscarinic or cannabinoid receptors and does not block potassium or calcium currents

Clinical trials

In a large double-blind, randomized clinical trial of people with poorly controlled partial-onset seizures, lacosamide was found to significantly reduce seizure frequency when given in addition to other antiepileptics, at doses of 400 and 600 milligrams a day. In a smaller trial of people with diabetic neuropathy, lacosamide also provided significantly better pain relief when compared to placebo.

Tolerability

Lacosamide was generally well tolerated in adult patients with partial-onset seizures. Dizziness was the most common treatment-related adverse event.

Chemistry

File:Lacosamide.png

J.A. McIntyre, J. Castaner, Drugs Future 29, 992 (2004).