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 |
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 Drug Interaction
Unknown: naproxen, calcium / vitamin d, duloxetine, omega-3 polyunsaturated fatty acids, flax, fluticasone nasal, furosemide, pregabalin, metoprolol, mirabegron, armodafinil, ocrelizumab, bifidobacterium infantis / lactobacillus acidophilus, dimethyl fumarate, acetaminophen, natalizumab, cyanocobalamin, ascorbic acid, ergocalciferol, cholecalciferol
4-Pyridylamine Disease Interaction
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
