THE JUST RIGHT ANTIPLATELET
D E S C R I P T I O N / M O D E O F A C T I O N
Cidogrel is only Clopidogrel bifulphate and Cidogrel – A is combination of Clopidogrel bisulphate and Aspirin. Clopidogrel is an inhibitor of platelet aggregation and it becomes active only after hepatic metabolism by P450 – CYP enzyme. The activated metabolite blocks the P2 purinoceptors (purine receptors) located on the surface of platelets. It inhibits the ADP induced platelet aggregation acting by direct inhibition of adenosine diphosphate (ADP) binding to its receptor and of the subsequent ADP-mediated activation of the glycoprotein GP IIb / IIIa complex. This clopidogrel – sensitive purinoceptor is thought to be linked to adenylyl cyclase. Hence these receptors are also called as P2Y12receptors. Dose dependent inhibition of platelet aggregation can be seen 2 hours after single oral dose of clopidogrel. It is rapidly aborbed after oral administration and approxmately 50% was excreted in the urine and 46% in the faeces. The elimination half life of the main circulating metabolite was 8 hours with a half life of 11 days. Aspirin did not modify the clopidogrel – mediated inhibition of ADP induced platelet aggegation. Aspirn acts by inhibiting thromboxane A2 which inhibit platelet aggregation.
C O M P O S I T I O N
I N D I C AT I O N S
Cidogrel and Cidogrel – A are indicated for the reduction of atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease. It is also indicated in the treatment of unstable angina.
Cidogrel – A is synergistic combination useful in preventing ischemic episodes and for preventing restenosis of stenosed coronaries.
D O S A G E
Cidogrel : Usually 1 tablet given once daily. A loading dose upto 4 tablets may be given in specific cases.
Cidogrel – A : Usually 1 tablet given once daily.
S I D E E F F E C T S
According to CAPRIE study the following were observed – Gastro intestinal : Abdominal pain, dysepsia, gastritis, and constipation. Haemorrhgic : GI haemorrhage, neutropenia / agranulocytosis. Rash & other skindisorders : Skin and appendage disorders. Others include – Syncope, palpitation, hernia, cardiac failure, vomiting, leg cramps, increased hepatic enzymes, anxiety, insomnia, anaemia, skin ulceration, decreased platelets,sinusitis, eczema.
P R E S E N TAT I O N & PACK
Cidogrel and Cidogrel – A are presented in Alu. Strips of 3 X 10’s tablets in carton.