PERSANTINE- dipyridamole tablet, coated
Boehringer Ingelheim Pharmaceuticals, Inc.
DESCRIPTION
PERSANTINE� (dipyridamole USP) is a platelet inhibitor chemically described as 2,2?,2?,2?'-[(4,8- Dipiperidinopyrimido[5,4-d ]pyrimidine-2,6-diyl)dinitrilo]-tetraethanol.
ipyridamole is an odorless yellow crystalline powder, having a bitter taste. It is soluble in dilute acids, methanol and chloroform, and practically insoluble in water.
PERSANTINE tablets for oral administration contain:
Active Ingredient TABLETS 25 mg, 50 mg, and 75 mg : dipyridamole USP 25 mg , 50 mg and 75 mg, respectively.
Inactive Ingredients TABLETS 25 mg, 50 mg, and 75 mg : acacia, carnauba wax, corn starch, edible white ink, lactose monohydrate, magnesium stearate, D&C yellow #10 aluminum lake, D&C red #30, helendon aluminum pink lake, sodium benzoate, methylparaben, propylparaben, polyethylene glycol, povidone, sucrose, talc, titanium dioxide, and white wax.
CLINICAL PHARMACOLOGY
It is believed that platelet reactivity and interaction with prosthetic cardiac valve surfaces, resulting in abnormally shortened platelet survival time, is a significant factor in thromboembolic complications occurring in connection with prosthetic heart valve replacement.
PERSANTINE tablets have been found to lengthen abnormally shortened platelet survival time in a dose-dependent manner.
Mechanism of Action
Dipyridamole inhibits the uptake of adenosine into platelets, endothelial cells and erythrocytes in vitro and in vivo ; the inhibition occurs in a dose-dependent manner at therapeutic concentrations (0.5�1.9 ?g/mL). This inhibition results in an increase in local concentrations of adenosine which acts on the platelet A2 -receptor thereby stimulating platelet adenylate cyclase and increasing platelet cyclic-3?,5?-adenosine monophosphate (cAMP) levels. Via this mechanism, platelet aggregation is inhibited in response to various stimuli such as platelet activating factor (PAF), collagen and adenosine diphosphate (ADP).
Dipyridamole inhibits phosphodiesterase (PDE) in various tissues. While the inhibition of cAMP-PDE is weak, therapeutic levels of dipyridamole inhibit cyclic-3?,5?-guanosine monophosphate-PDE (cGMP-PDE), thereby augmenting the increase in cGMP produced by EDRF (endothelium-derived relaxing factor, now identified as nitric oxide).
INDICATIONS AND USAGE
PERSANTINE tablets are indicated as an adjunct to coumarin anticoagulants in the prevention of postoperative thromboembolic complications of cardiac valve replacement.
