Lacosamide

Trade Names:
Vimpat
- Tablets, oral 50 mg
- Tablets, oral 100 mg
- Tablets, oral 150 mg
- Tablets, oral 200 mg
- Injection, solution 10 mg/mL

Pharmacology

User Reviews & Ratings As a treatment for... Avg User Ratings [?] Seizures 3 reviews Rate it! 5.7 Compare with other drugs.

Precise mechanism of action is unknown; however, lacosamide selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.

Pharmacokinetics

Absorption

Completely absorbed following oral administration with negligible first-pass effect and an absolute bioavailability of approximately 100%. Food does not affect the rate or extent of absorption. Following IV administration, the C _max is reached at the end of the infusion.

Distribution

Vd is approximately 0.6 L/kg. Less than 15% is bound to plasma proteins.

Metabolism

Primarily cleared from the systemic circulation by renal excretion and biotransformation. Lacosamide is a CYP2C19 substrate.

Elimination

Approximately 95% is eliminated in the urine and less than 0.5% in the feces, mainly as unchanged drug (40%), 30% as the O-desmethyl metabolite, and about 20% as a structurally unknown inactive polar metabolite. Elimination half-life is approximately 13 h.

Special Populations

AUC is increased approximately 25% in patients with mild or moderate renal function impairment and 60% in patients with severe renal function impairment. No dosage adjustment is needed in patients with mild or moderate renal function impairment.

AUC is increased by approximately 50% to 60% in patients with moderate hepatic function impairment.

In patients older than 65 yr of age, AUC and C _max are increased about 20% compared with younger subjects.

Pharmacokinetics have not been studied.

Pharmacokinetics not affected by gender.

No differences in pharmacokinetics among Asian, black, and white subjects.

Indications and Usage

Adjunctive treatment of partial-onset seizures.

Adjunctive treatment of partial-onset seizures when oral route is not feasible.

Contraindications

Standard considerations.

Dosage and Administration

PO/IV Start with 50 mg twice daily. The dosage may be increased by 50 mg twice daily at weekly intervals up to the recommended maintenance dosage of 200 to 400 mg/day, based on response and tolerability.

PO/IV Titrate the dose with caution. Max dosage of 300 mg/day is recommended in patients with mild or moderate hepatic function impairment. Not recommended in patients with severe hepatic function impairment.

PO/IV

No dosage adjustment is needed.

Max dosage is 300 mg/day. Following a 4-hour hemodialysis treatment, supplementation with up to 50% of the dose should be considered.

General Advice

• When switching from oral to IV route, administer the equivalent daily dose and frequency. Infuse the drug IV over a 30- to 60-min period.
• When switching from IV to the oral route, oral administration should be the equivalent daily dose and frequency of IV administration.
• May be taken without regards to meals.
• When discontinuing therapy, gradually withdraw over a minimum of 1 wk.

Storage/Stability

Store at 59° to 86°F. Store IV form following dilution for up to 24 h at 59° to 86°F. Store in glass or polyvinyl chloride bags. Discard any unused portion.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Dizziness (53%); ataxia, fatigue (15%); headache (14%); tremor (12%); nystagmus (10%); somnolence (8%); balance disorder, memory impairment (6%); vertigo (5%); asthenia, gait disturbance (4%); depression (2%).

Dermatologic

Contusion (4%); pruritus, skin laceration (3%).

EENT

Blurred vision, diplopia (16%).

GI

Nausea (17%); vomiting (16%); diarrhea (5%).

Local

Injection-site pain or discomfort (3%); irritation (1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 17 yr of age.

Elderly

Titrate dose with caution.

Renal Function

A max dosage of 300 mg/day is recommended for patients with severe renal function impairment or end-stage renal disease.

Hepatic Function

Titrate dose with caution in patients with mild or moderate hepatic function impairment. A max dosage of 300 mg/day is recommended for patients with mild or moderate hepatic function impairment. Not recommended in patients with severe hepatic function impairment.

Ataxia and dizziness

May occur. Patients should not drive or operate complex machinery until they are familiar with the drug's effects on their ability to perform.

Atrial fibrillation and atrial flutter

Has been reported in patients with diabetic neuropathy who received treatment with lacosamide.

Cardiac rhythm and conduction abnormalities

Dose-related PR interval prolongation may occur. Use with caution in patients with known conduction problems (eg, marked first-degree AV block, second-degree or higher AV block, sick sinus syndrome without a pacemaker), or with severe cardiac disease (eg, myocardial ischemia, heart failure).

Discontinuation

Gradually withdraw treatment over a minimum of 1 wk to minimize the potential of increased seizure frequency.

Multiorgan hypersensitivity

Has been reported rarely.

Suicide

The risk of suicidal thoughts and behavior is increased.

Syncope

Has been reported in patients with diabetic neuropathy who were treated with lacosamide.

Overdosage

Symptoms

Limited experience available. Adverse reactions in patients receiving supratherapeutic doses were not different from those of patients receiving recommended doses.

Patient Information

• Instruct patient to contact health care provider if palpitation, rapid pulse, or shortness of breath occurs.
• Advise patient or caregivers to be alert for emergence or worsening of symptoms of depression, any unusual changes in mood or behavior, or the emergence of suicidal thoughts, behavior, or thoughts about self-harm, and to immediately report any behaviors of concern to health care provider.
• Advise patient not to drive, operate complex machinery, or engage in other hazardous activities until accustomed to any dizziness, blurred vision, abnormal coordination and balance, and somnolence caused by taking lacosamide.
• Advise patient that syncope can occur, and to lie down with raised legs until they recover and to contact health care provider.

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