4-Pyridylamine

4-Pyridylamine Uses, Dosage, Side Effects, Food Interaction and all others data.

4-Pyridylamine 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.

4-Pyridylamine 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.

Trade Name 4-Pyridylamine
Availability Prescription only
Generic Dalfampridine
Dalfampridine Other Names 4-Aminopyridine, 4-Pyridylamine, Dalfampridine, Fampridina, Fampridine, Fampridinum
Related Drugs Gilenya, Tysabri, Vumerity, Copaxone, Tecfidera, Aubagio, Avonex
Type
Formula C5H6N2
Weight Average: 94.1145
Monoisotopic: 94.053098202
Protein binding

10 mg extended release = 1-3% protein bound

Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
4-Pyridylamine
4-Pyridylamine

Uses

4-Pyridylamine is a potassium channel blocker used for the improvement of motor function in patients with multiple sclerosis (MS).

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

4-Pyridylamine is also used to associated treatment for these conditions: Disseminated Sclerosis

How 4-Pyridylamine works

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 trigger an action potential. 4-Pyridylamine inhibits voltage-gated potassium channels in the CNS to maintain the transmembrane potential and prolong action potential. In other words, dalfampridine works to make sure that the current available is high enough to stimulate conduction in demyelinated axons that are exposed in MS patients. Furthermore, it facilitates neuromuscular and synaptic transmission by relieving conduction blocks in demyelinated axons.

Toxicity

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

Food Interaction

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

4-Pyridylamine Disease Interaction

Major: renal impairment, seizures

Volume of Distribution

10 mg extended release = 2.6 L/kg

Elimination Route

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 compared to aqueous oral solution = 96%

Half Life

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

Elimination Route

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%)

Innovators Monograph

You find simplified version here 4-Pyridylamine

*** Taking medicines without doctor's advice can cause long-term problems.
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