Description

Simple

A medication used to improve walking in patients with a potentially disabling disease of the brain and spinal cord, called multiple sclerosis.

Clinical

A potassium channel blocker used for the improvement of motor function in patients with multiple sclerosis (MS).

Overview

Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. This is the first drug that was specifically approved to help with mobility in these patients. FDA approved on January 22, 2010.

Pharmacology

Indication

Dalfampridine is a neurofunctional modifier that helps improve walking speed in patients with multiple sclerosis (MS).

Pharmacodynamic

Dalfampridine is a board-spectrum lipophillic potassium channel blocker and binds favourably to the open state than closed state of the potassium channel in the CNS. Its pharmacological target are the potassium channels exposed in MS patients. Does not prolong the QTc interval.

Mechanism of action

In MS, axons are progressively demyelinated which exposes potassium channels. As a result, there is a leak of potassium ions which results in the repolarization of cells and a decrease in neuronal excitability. The overall impact is the impairment of neuromuscular transmission as it is harder to tri... Read more

Absorption

Orally-administered dalfampridine is rapidly and completely absorbed from the gastrointestinal tract.
Tmax, immediate release form = 1 hour;
Tmax, extended release form = 3.5 hours;
Cmax, 10 mg extended release = 17.3 - 21.6 ng/mL;
Relative bioavailability of 10 mg extended-release tablets com... Read more

Protein binding

10 mg extended release = 1-3% protein bound

Volume of distribution

10 mg extended release = 2.6 L/kg

Clearance

Information currently not available.

Half life

Immediate release form = 3.5 hours;
Extended release form = 5.47 hours;

Route of elimination

Almost all of the dose and its metabolites are completely eliminated by the kidneys after 24 hours.
Urine (96%; 90% of total dose as unchanged drug);
Feces (0.5%)

Toxicity

LD50, oral, mouse = 19 mg/kg
LD50, oral, rat = 21 mg/kg

Adverse Effects

Contraindications

  • Lab Values:
    • CrCl≤50 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: Moderate or severe renal impairment
      • Drugbank Id: DBCOND0108446
  • Lab Values:
    • CrCl≤50 mL/min
  • Regions: US
  • Patient Conditions:
      • Name: History of seizure
      • Drugbank Id: DBCOND0108445

Food Interactions

  • Take with or without food. High-fat meals increase drug absorption, but not to a clinically significant extent.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abacavir
Abacavir may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Dalfampridine which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Aclidinium
Dalfampridine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine
Dalfampridine may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Albutrepenonacog alfa
Dalfampridine may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Aldesleukin
Aldesleukin may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Allopurinol
Allopurinol may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Allylestrenol
Allylestrenol may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Almasilate
Dalfampridine may decrease the excretion rate of Almasilate which could result in a higher serum level.
Alminoprofen
Alminoprofen may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
Almotriptan
Almotriptan may decrease the excretion rate of Dalfampridine which could result in a higher serum level.
5 References
  1. 1 . Panitch H, Applebee A: Treatment of walking impairment in multiple sclerosis: an unmet need for a disease-specific disability. Expert Opin Pharmacother. 2011 Jul;12(10):1511-21. doi: 10.1517/14656566.2011.586338. Epub 2011 Jun 2.PubMed: 21635193
  2. 2 . Pikoulas TE, Fuller MA: Dalfampridine: a medication to improve walking in patients with multiple sclerosis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1010-5. doi: 10.1345/aph.1Q714. Epub 2012 Jul 3.PubMed: 22764324
  3. 3 . Cornblath DR, Bienen EJ, Blight AR: The safety profile of dalfampridine extended release in multiple sclerosis clinical trials. Clin Ther. 2012 May;34(5):1056-69. doi: 10.1016/j.clinthera.2012.03.007. Epub 2012 Apr 11.PubMed: 22497693
  4. 4 . McDonald S, Clements JN: Dalfampridine: a new agent for symptomatic management of multiple sclerosis. Am J Health Syst Pharm. 2011 Dec 15;68(24):2335-40. doi: 10.2146/ajhp110134.PubMed: 22135060
  5. 5 . Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9.PubMed: 16472864