Drug Interaction:
Interacting drugs - summary
Asprin + Clopidrogrel
risk of life-threatening bleeding eg. intracranial and GI hemorrhage
may be increased in high risk patients with TIA or ischemic stroke
Macrolide antibiotics eg, erythromycin + clopidrogrel
the antiplatelet effect of clopidogrel may be inhibited by certain
macrolides and related antibiotics
NSAIDs +Clopidogrel
coadmin. of clopidogrel with naproxen was associated with increased
occult GI blood loss. Administer NSAIDs and clopidogrel with caution
Rifampicin + Clopidogrel
the antiplatelet effect of clopidogrel may be enhanced
Clopidogrel + Warfarin or Warfarin + Clopidogrel
the antiplatelet effect of clopidogrel may be enhanced
because of the increased risk of bleeding, undetake the coadmin
of warfarin and clopidogrel with caution
Clopidogrel + Bupropion
bupropion plasma concentration may be elevated increasing the
pharmacologic and adverse reactions
Indication:
U.S.FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
189. Clopidrogel 300mg tablet 02-09-08
As approved
Prophylaxis and thrombolic disorders
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Clopidogrel Anti Platelet Aggregation 2-2-2001
inhibitor
2.Clopidogrel 300mg tablet 02-09-2008
(Addl.strgth)
As approved
FIXED DOSE COMBINATIONS APPROVED BY DCG(I)
FROM JANUARY 1961 TILL NOVEMBER 2014
Name of Drug Indication Date of Approval
Clopidogrel bisulphate eq.to Clopidogrel 75mg+ 27-11-2002
Aspirin IP (as enteric coated tablets) 75mg/150mg
Capsules
For the treatment of angina, myocardial infarction and stroke
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Clopidogrel Cardiovascular Bristol-Myers 05-07-2003
Squibb & Sanofi
Adverse Reaction:
Gastrointestinal upset,diarrhoea, and rash.
Serious events include bleeding and gastrointestinal haemorrhage.
Contra-Indications:
Hypersensitivity.
Acute pathological bleeding such as peptic ulcer or intracranial hemorrhage.
Special preautions:
Pregnancy- No adequate studies of clopidigrel in pregnant women. Use with caution only if it required.
Lactation: Because of the potential side effects in the nursing infant, the physician must weigh the potential benefits against the benefits to the patient.
Dosages/ Overdosage Etc:
Date of Approval 02-09-08
Indication-
Prophylaxis and thrombolic disorders
Dosage-
Adult- 75mg once daily with or without food.
Acute coronary syndrome- For ST-elevation myocardial infaction- in combination with aspirin- 75mg once daily .
Patients > 75 years old may be given a loading dose of 300mg.
Continue treatment for upto 28 days
For unstable angina, non-ST myocardial infaction initial - 300mg loading dose followed by 75mg once daily with aspirin 75 - 325mg once daily.
Patient Information:
1.Tell patients that it may take them longer than usual to stop bleeding and they may bruise and /or bleed more easily when they take clopidrogel or clopidogrel combined with aspirin.
2.Patient should report any unusual bleeding to their health care provider
3. Instruct patients to inform their health care provider and dentist that they are taking clopidrogel and/or any other product known to bleeding before the surgery is scheduled and before a new drug is taken
Pharmacology/ Pharmacokinetics:
Pharmacology:
Clopidogrel itself is inactive, but it is converted into an active metabolite. So the activity of clopidigrel is dependent on hepatic biotransformation. Platelets that adhere to damaged vessels walls are aggravated to secrete adenosine diphosphate(ADP) from the storage granules.
ADP causes platelets in the vicinity to swell and adhere to each other, further aggravating platelet aggregation. Clopidogrel blocks ADP receptor, leading to inhibition of fibronogen binding to the platelet receptor.
Pharmacokinetics:
Cipidogrel is rapidly absorbed on oral administration. It is inactive in vivo and undergoes hepatic activation. After oral clopidrogel administration , t max of the principal metabolite is approximately 1 hour.
Steady state level of the metabolite is acheived by about 8 hours of administration.The plasma elimination half-life of the active metabolite is 8 hours .
Food and antacids do not affect the bioavailability of clopidogrel.
Interaction with Food:
Food and antacids do not affect the bioavailability of clopidogrel.
Take with or without food
Pregnancy and lactation:
Pregnancy-
No adequate studies of clopidigrel in pregnant women. Use with caution only if it required
Lactation:
Because of the potential side effects in the nursing infant, the physician must weigh the potential benefits against the benefits to the patient.
Manufacturer Details