Trapidil
Trapidil Uses, Dosage, Side Effects, Food Interaction and all others data.
Trapidil, a platelet-derived growth factor antagonist, was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.
Trapidil exerts vasodilatory and antiplatelet effects . It also inhibits the activity of platelet derived growth factor (PDGF) .
Trade Name | Trapidil |
Generic | Trapidil |
Trapidil Other Names | Trapidil |
Type | |
Formula | C10H15N5 |
Weight | Average: 205.265 Monoisotopic: 205.132745503 |
Groups | Experimental |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Used in the treatment of chronic stable angina .
How Trapidil works
Trapidil is thought to inhibit cyclic adenosine monophosphate (cAMP) phosphodiesterase enzymes . The resultant increase in cAMP potentiates the inhibition of platelets by adenosine . The reduction in platelet activation is likely responsible for the decrease in thromboxane A2 generation seen with trapidil . The increase in cAMP is also likely responsible for the vasdilatory action of trapidil. The increase in protein kinase A activity due to increased cAMP activated L-type calcium channels in the heart leading to increased depolarization and a positive inotropic effect . Lastly, PKA inactivates Raf-1, an activator of mitogen activated protein kinase (MAPK), which leads to a reduction in MAPK activation. This reduction in MAPK prevents mitogenesis due to PDGF binding to PDGF receptors .
Elimination Route
Trapidil has a Tmax of 1 h .
Half Life
The half life of elimination is 1.31 h for a single dose and 1.14 h for steady state dosing .
Clearance
The apparent clearance is 179 mL/min for a single dose and 273 mL/min for steady state dosing .
Innovators Monograph
You find simplified version here Trapidil