Erlosamide

Uses

Erlosamide is used for the treatment of partial-onset seizures in patients 4 years of age and older. As the safety of Erlosamide injection has not been established in pediatric patients, Erlosamide injection is used for the treatment of partial-onset seizures only in adult patients (17 years of age and older)

Erlosamide is also used to associated treatment for these conditions: Partial-Onset Seizures, Refractory seizure disorders

How Erlosamide works

It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Erlosamide may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Erlosamide binds to collapsin response mediator protein-2 (CRMP-2), a phosphoprotein which is expressed primarily in the nervous system and is involved in neuronal differentiation and control of axonal outgrowth. The role CRMP-2 of binding in seizure control is hasn't been elucidated.

Dosage

Erlosamide dosage

Adults (17 years and older): Initial dosage for monotherapy is 100 mg twice daily; initial dosage for adjunctive therapy is 50 mg twice daily; maximum recommended dosage for monotherapy and adjunctive therapy is 200 mg twice daily

Pediatric Patients 4 Years to less than 17 years: The recommended dosage is based on body weight and is administered orally twice daily. Increase dosage based on clinical response and tolerability, no more frequently than once per week

Injection: for intravenous and adult use only when oral administration is temporarily not feasible; dosing regimen is the same as oral regimen; administer over 15 to 60 minutes; obtaining ECG before initiation is recommended in certain patients

Side Effects

Adjunctive therapy: Most common adverse reactions in adults (≥10% and greater than placebo) are diplopia, headache, dizziness, nausea

Monotherapy: Most common adverse reactions are similar to those seen in adjunctive therapy studies

Pediatric patients: Adverse reactions are similar to those seen in adult patients

Precaution

Monitor patients for suicidal behavior and ideation

Erlosamide may cause dizziness and ataxia

Cardiac Rhythm and Conduction Abnormalities: Obtaining ECG before beginning and after titration to steady-state maintenance is recommended in patients with known cardiac conduction problems, taking drugs known to induce PR interval prolongation, or with severe cardiac disease; closely monitor these patients

Erlosamide may cause syncope

Erlosamide should be gradually withdrawn to minimize the potential of increased seizure frequency

Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)/Multi-Organ Hypersensitivity: Discontinue if no alternate etiology

Interaction

Strong CYP3A4 or CYP2C9 Inhibitors: Patients with renal or hepatic impairment who are taking strong inhibitors of CYP3A4 and CYP2C9 may have a significant increase in exposure to Erlosamide. Dose reduction may be necessary in these patients.

Concomitant Medications that Prolong PR Interval: Erlosamide should be used with caution in patients on concomitant medications that prolong PR interval, because of a risk of AV block or bradycardia, e.g., beta-blockers and calcium channel blockers. In such patients, obtaining an ECG before beginning Erlosamide, and after Erlosamide is titrated to steady-state, is recommended. In addition, these patients should be closely monitored if they are administered Erlosamide through the intravenous route

Food Interaction

• Take with or without food.

Erlosamide Alcohol interaction

[Moderate] GENERALLY AVOID:

Alcohol may potentiate some of the pharmacologic effects of central nervous system (CNS)-active agents.

Use in combination may result in additive CNS depression and/or impairment of judgment, thinking, and psychomotor skills.

Patients receiving CNS-active agents should be advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled against driving, operating machinery, or engaging in potentially hazardous activities requiring mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Erlosamide Drug Interaction

Moderate: duloxetine, lamotrigine, metoprolol, sertraline, cetirizineUnknown: divalproex sodium, levetiracetam, arginine, levocarnitine, pregabalin, polyethylene glycol 3350, acetaminophen, levothyroxine, carbamazepine, topiramate, acetaminophen, valproic acid, cyanocobalamin, cholecalciferol, phytonadione

Erlosamide Disease Interaction

Major: depressionModerate: CVD, hepatic impairment, renal impairment

Volume of Distribution

approximately 0.6 L/kg; thus close to the volume of total body water.

Elimination Route

Erlosamide has a negligible first pass effect with bioavailability of about 100%. The maximum Erlosamide plasma concentrations occur about 1-4 hours after oral administration, and the pharmacokinetics of Erlosamide are dose proportional. Food does not affect absorption.

Half Life

13 Hours

Clearance

95% recovered in the urine 0.5% in the feces

Elimination Route

Erlosamide is eliminated primarily from the systemic circulation by biotransformation and renal excretion.

Pregnancy & Breastfeeding use

Pregnancy: Based on animal data, may cause fetal harm

Contraindication

None

Special Warning

Dose adjustment is recommended for severe renal impairment. Dose adjustment is recommended for mild or moderate hepatic impairment; use in patients with severe hepatic impairment is not recommended

Storage Condition

Store at 20°C to 25°C

Innovators Monograph

You find simplified version here Erlosamide