Harkoseride
Harkoseride Uses, Dosage, Side Effects, Food Interaction and all others data.
It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Harkoseride may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Harkoseride 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.
Harkoseride therapy is correlated with a decrease in seizure frequency. It should be noted that in group analyses, dosages above 400 mg/day do not appear to result in additional benefit.
Trade Name | Harkoseride |
Availability | Prescription only |
Generic | Lacosamide |
Lacosamide Other Names | Erlosamide, Harkoseride, Lacosamida, Lacosamide |
Related Drugs | gabapentin, clonazepam, lamotrigine, diazepam, pregabalin, Lyrica, topiramate, levetiracetam, Keppra, Topamax |
Type | |
Formula | C13H18N2O3 |
Weight | Average: 250.2936 Monoisotopic: 250.131742452 |
Protein binding | <15% |
Groups | Approved |
Therapeutic Class | Atypical anti-depressant drugs |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Harkoseride is used for the treatment of partial-onset seizures in patients 4 years of age and older. As the safety of Harkoseride injection has not been established in pediatric patients, Harkoseride injection is used for the treatment of partial-onset seizures only in adult patients (17 years of age and older)
Harkoseride is also used to associated treatment for these conditions: Partial-Onset Seizures, Refractory seizure disorders
How Harkoseride works
It is proposed that lacosamide's inhibition of sodium channels is responsible for analgesia. Harkoseride may be selective for inhibiting depolarized neurons rather than neurons with normal resting potentials. Pain and nociceptor hyperexcitability are associated with neural membrane depolarization. Harkoseride 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
Harkoseride 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
Harkoseride 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
Harkoseride may cause syncope
Harkoseride 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 Harkoseride. Dose reduction may be necessary in these patients.
Concomitant Medications that Prolong PR Interval: Harkoseride 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 Harkoseride, and after Harkoseride is titrated to steady-state, is recommended. In addition, these patients should be closely monitored if they are administered Harkoseride through the intravenous route
Food Interaction
- Take with or without food.
Harkoseride 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.
Harkoseride 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
Harkoseride 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
Harkoseride has a negligible first pass effect with bioavailability of about 100%. The maximum Harkoseride plasma concentrations occur about 1-4 hours after oral administration, and the pharmacokinetics of Harkoseride 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
Harkoseride 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 Harkoseride
Harkoseride contains Lacosamide see full prescribing information from innovator Harkoseride Monograph, Harkoseride MSDS, Harkoseride FDA label