Lacosamidee (Tablets) Instructions for Use

Marketing Authorization Holder

LIFE SCIENCES OHFK, LLC (Russia)

Manufactured By

OHFK, JSC (Russia)

ATC Code

N03AX18 (Lacosamide)

Active Substance

Lacosamide (Rec.INN registered by WHO)

Dosage Forms

	Lacosamide	Film-coated tablets 50 mg
		Film-coated tablets 100 mg
		Film-coated tablets 150 mg
		Film-coated tablets 200 mg

Dosage Form, Packaging, and Composition

Film-coated tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – By prescription
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – blister packs (6 pcs.) – cardboard packs (60 pcs.) – By prescription
14 pcs. – jars – cardboard packs (14 pcs.) – By prescription
56 pcs. – jars – cardboard packs (56 pcs.) – By prescription

Film-coated tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – By prescription
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – blister packs (6 pcs.) – cardboard packs (60 pcs.) – By prescription
14 pcs. – jars – cardboard packs (14 pcs.) – By prescription
56 pcs. – jars – cardboard packs (56 pcs.) – By prescription

Film-coated tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – By prescription
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – blister packs (6 pcs.) – cardboard packs (60 pcs.) – By prescription
14 pcs. – jars – cardboard packs (14 pcs.) – By prescription
56 pcs. – jars – cardboard packs (56 pcs.) – By prescription

Film-coated tablets

10 pcs. – blister packs – cardboard packs (10 pcs.) – By prescription
10 pcs. – blister packs (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – blister packs (6 pcs.) – cardboard packs (60 pcs.) – By prescription
14 pcs. – jars – cardboard packs (14 pcs.) – By prescription
56 pcs. – jars – cardboard packs (56 pcs.) – By prescription

Clinical-Pharmacological Group

Anticonvulsant drug

Pharmacotherapeutic Group

Antiepileptic drugs; other antiepileptic drugs

Pharmacological Action

Antiepileptic drug. Electrophysiological studies have shown that Lacosamide selectively enhances the slow inactivation of voltage-gated sodium channels, which leads to a reduction in the hyperexcitability of neuronal membranes.

Moreover, Lacosamide has the potential to interact with the collapsin response mediator protein-2 (CRMP-2), a phosphoprotein that is expressed mainly in the nervous system and is involved in the processes of neuronal differentiation and the control of axonal growth.

Pharmacokinetics

After oral administration, Lacosamide is rapidly and completely absorbed from the gastrointestinal tract. T_max is approximately 0.5-4 hours. After intravenous administration, C_max is reached at the end of the infusion. V_d is about 0.6 L/kg. Plasma protein binding is less than 15%.

It is metabolized in the liver by the CYP2C19 isoenzyme to form a pharmacologically inactive O-desmethyl metabolite. An interaction study with omeprazole (a CYP2C19 inhibitor) showed no clinically significant changes in lacosamide plasma concentration, so the significance of this metabolic pathway is minimal.

T_1/2 is about 13 hours. It is excreted in the urine unchanged (about 40%), as the O-desmethyl metabolite (less than 30%) and other metabolites; less than 0.5% is found in feces.

Indications

As adjunctive therapy for the treatment of partial-onset seizures with or without secondary generalization in patients with epilepsy aged 16 years and older.

ICD codes

Dosage Regimen

Administer lacosamide orally twice daily with or without food.

Initiate therapy at a starting dose of 50 mg twice daily (100 mg total per day).

Increase the dose based on therapeutic response and patient tolerability.

Titrate the dose at weekly intervals by increasing the twice-daily dose by 50 mg increments.

The recommended maintenance dose is 100 mg to 200 mg twice daily (200 mg to 400 mg total per day).

Do not exceed the maximum recommended daily dose of 400 mg.

For patients with severe renal impairment (CrCl ≤30 mL/min) or those undergoing hemodialysis, a maximum dose of 300 mg daily is recommended.

In patients with mild to moderate hepatic impairment, do not exceed a maximum daily dose of 300 mg.

Avoid use in patients with severe hepatic impairment.

When discontinuing treatment, gradually reduce the dose over at least one week.

Adverse Reactions

From the central and peripheral nervous system:dizziness, headache, impaired coordination, drowsiness, tremor, nystagmus, memory impairment, cognitive disorders, depression, hypoesthesia, dysarthria, impaired concentration.

From the digestive system:nausea, vomiting, constipation, flatulence, dyspepsia, dry mouth.

From the cardiovascular system:prolongation of the PR interval, AV block, syncope, bradycardia.

From the sensory organs:labyrinthine vertigo, diplopia, blurred vision, tinnitus.

Other:asthenia, gait disturbance, weakness, skin abrasions, increased trauma, skin itching, muscle spasms.

Contraindications

Second- and third-degree AV block, hypersensitivity to lacosamide.

Use in Pregnancy and Lactation

The use of lacosamide during pregnancy is not recommended, except in cases of extreme necessity, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

If it is necessary to use lacosamide during lactation, the issue of discontinuing breastfeeding should be considered.

Special Precautions

When using antiepileptic drugs, including Lacosamide, the risk of suicidal attempts and suicidal behavior increases, regardless of the indications for which the drug is used.

Effect on ability to drive vehicles and operate machinery

During treatment, patients should avoid driving vehicles and other potentially hazardous activities, because Lacosamide may cause dizziness and diplopia.

Drug Interactions

Lacosamide should be used with caution in patients receiving drugs that can cause prolongation of the PR interval (including carbamazepine, lamotrigine, pregabalin) and in patients receiving class I antiarrhythmic drugs.

With simultaneous use with inducers of liver microsomal enzymes (carbamazepine, phenytoin, phenobarbital in various doses), a 25% decrease in the AUC of lacosamide was noted.

With simultaneous use of lacosamide with 1-3 antiepileptic drugs, patients experienced impaired liver function tests (increased activity of liver transaminases).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.