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Clopidogrel

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Overview

What is Clopidogrel?

Clopidogrel bisulfate, USP is a thienopyridine class inhibitor of P2Y12 ADP platelet receptors. Chemically it is methyl (+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H) acetate sulfate (1:1). The empirical formula of clopidogrel bisulfate is CHClNOS•HSO and its molecular weight is 419.9.

The structural formula is as follows:

Clopidogrel bisulfate, USP is a white to off-white powder. It is practically insoluble in water at neutral pH but freely soluble at pH 1. It also dissolves freely in methanol, dissolves sparingly in methylene chloride, and is practically insoluble in ethyl ether. It has a specific optical rotation of about +56°. Clopidogrel tablets USP, 75 mg for oral administration is provided as either pink, round, biconvex, debossed, film-coated tablets containing 97.875 mg of clopidogrel bisulfate which is the molar equivalent of 75 mg of clopidogrel base. Each tablet contains lactose monohydrate, low substituted hydroxypropyl cellulose, colloidal silicon dioxide, dimethicone and hydrogenated castor oil as inactive ingredients. The pink film coating contains hypromellose 2910, polyethylene glycol 400, titanium dioxide and iron oxide red.



What does Clopidogrel look like?



What are the available doses of Clopidogrel?

Tablets: 75 mg. ()

What should I talk to my health care provider before I take Clopidogrel?

Nursing mothers: Discontinue drug or nursing. () 

How should I use Clopidogrel?

• Clopidogrel is indicated to reduce the rate of myocardial infarction (MI) and stroke in patients with non-ST-segment elevation ACS (unstable angina [UA]/non-ST-elevation myocardial infarction [NSTEMI]), including patients who are to be managed medically and those who are to be managed with coronary revascularization. Clopidogrel should be administered in conjunction with aspirin. • Clopidogrel is indicated to reduce the rate of myocardial infarction and stroke in patients with acute ST-elevation myocardial infarction (STEMI) who are to be managed medically. Clopidogrel should be administered in conjunction with aspirin.

In patients who need an antiplatelet effect within hours, initiate clopidogrel with a single 300-mg oral loading dose and then continue at 75 mg once daily. Initiating clopidogrel without a loading dose will delay establishment of an antiplatelet effect by several days [].


What interacts with Clopidogrel?

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What are the warnings of Clopidogrel?

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What are the precautions of Clopidogrel?

Sorry No Records found


What are the side effects of Clopidogrel?

Sorry No records found


What should I look out for while using Clopidogrel?

• Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage () • Hypersensitivity to clopidogrel or any component of the product ()

The effectiveness of Clopidogrel results from its antiplatelet activity, which is dependent on its conversion to an active metabolite by the cytochrome P450 (CYP) system, principally CYP2C19 []. Clopidogrel at recommended doses forms less of the active metabolite and so has a reduced effect on platelet activity in patients who are homozygous for nonfunctional alleles of the CYP2C19 gene, (termed “CYP2C19 poor metabolizers”). Tests are available to identify patients who are CYP2C19 poor metabolizers []. Consider use of another platelet P2Y12 inhibitor in patients identified as CYP2C19 poor metabolizers.


What might happen if I take too much Clopidogrel?

Platelet inhibition by clopidogrel is irreversible and will last for the life of the platelet. Overdose following clopidogrel administration may result in bleeding complications. A single oral dose of clopidogrel at 1500 or 2000 mg/kg was lethal to mice and to rats and at 3000 mg/kg to baboons. Symptoms of acute toxicity were vomiting, prostration, difficult breathing, and gastrointestinal hemorrhage in animals.

Based on biological plausibility, platelet transfusion may restore clotting ability.


How should I store and handle Clopidogrel?

Store VPRIV at 2 °C to 8°C (36°F to 46°F). Do not use VPRIV after the expiration date on the vial. Do not freeze.Protect vial from light.Store VPRIV at 2 °C to 8°C (36°F to 46°F). Do not use VPRIV after the expiration date on the vial. Do not freeze.Protect vial from light.Clopidogrel Tablets USP, 75 mg are available as pink colored, circular, biconvex, film-coated tablets debossed with "L 11" on one side and plain on other side. Tablets are provided as follows:NDC 33342-060-07           Bottle of 30 tablets NDC 33342-060-10           Bottle of 90 tabletsNDC 33342-060-15           Bottle of 500 tabletsNDC 33342-060-12           Blister pack of 100 tablets (10 x 10 Unit Dose)Store at 20° to 25°C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature].Clopidogrel Tablets USP, 75 mg are available as pink colored, circular, biconvex, film-coated tablets debossed with "L 11" on one side and plain on other side. Tablets are provided as follows:NDC 33342-060-07           Bottle of 30 tablets NDC 33342-060-10           Bottle of 90 tabletsNDC 33342-060-15           Bottle of 500 tabletsNDC 33342-060-12           Blister pack of 100 tablets (10 x 10 Unit Dose)Store at 20° to 25°C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature].Clopidogrel Tablets USP, 75 mg are available as pink colored, circular, biconvex, film-coated tablets debossed with "L 11" on one side and plain on other side. Tablets are provided as follows:NDC 33342-060-07           Bottle of 30 tablets NDC 33342-060-10           Bottle of 90 tabletsNDC 33342-060-15           Bottle of 500 tabletsNDC 33342-060-12           Blister pack of 100 tablets (10 x 10 Unit Dose)Store at 20° to 25°C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature].Clopidogrel Tablets USP, 75 mg are available as pink colored, circular, biconvex, film-coated tablets debossed with "L 11" on one side and plain on other side. Tablets are provided as follows:NDC 33342-060-07           Bottle of 30 tablets NDC 33342-060-10           Bottle of 90 tabletsNDC 33342-060-15           Bottle of 500 tabletsNDC 33342-060-12           Blister pack of 100 tablets (10 x 10 Unit Dose)Store at 20° to 25°C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature].Clopidogrel Tablets USP, 75 mg are available as pink colored, circular, biconvex, film-coated tablets debossed with "L 11" on one side and plain on other side. Tablets are provided as follows:NDC 33342-060-07           Bottle of 30 tablets NDC 33342-060-10           Bottle of 90 tabletsNDC 33342-060-15           Bottle of 500 tabletsNDC 33342-060-12           Blister pack of 100 tablets (10 x 10 Unit Dose)Store at 20° to 25°C (68° to 77° F); excursions permitted to 15° to 30° C (59° to 86° F) [see USP Controlled Room Temperature].


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Clinical Information

Chemical Structure

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Clinical Pharmacology

Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y class of ADP receptors on platelets.

Non-Clinical Toxicology
• Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage () • Hypersensitivity to clopidogrel or any component of the product ()

The effectiveness of Clopidogrel results from its antiplatelet activity, which is dependent on its conversion to an active metabolite by the cytochrome P450 (CYP) system, principally CYP2C19 []. Clopidogrel at recommended doses forms less of the active metabolite and so has a reduced effect on platelet activity in patients who are homozygous for nonfunctional alleles of the CYP2C19 gene, (termed “CYP2C19 poor metabolizers”). Tests are available to identify patients who are CYP2C19 poor metabolizers []. Consider use of another platelet P2Y12 inhibitor in patients identified as CYP2C19 poor metabolizers.

The administration of local anesthetic solutions containing vasopressors, such as Levonordefrin, Epinephrine or Norepinephrine, to patients receiving tricyclic antidepressants or monoamine oxidase inhibitorsproduce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential. Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.

Phenothiazines and butyrophenones may reduce or reverse the pressor effect of Epinephrine.

Solutions containing a vasoconstrictor should be used cautiously in the presence of disease which may adversely affect the patient's cardiovascular system. Serious cardiac arrhythmias may occur if preparations containing a vasoconstrictor are employed in patients during or following the administration of potent inhalation anesthetics.

MEPIVACAINE SHOULD BE USED WITH CAUTION IN PATIENTS WITH KNOWN DRUG ALLERGIES AND SENSITIVITIES. A thorough history of the patient's prior experience with Mepivacaine or other local anesthetics as well as concomitant or recent drug use should be taken (see). Patients allergic to methylparaben or para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to agents of the amide type such as Mepivacaine. Since Mepivacaine is metabolized in the liver and excreted by the kidneys, it should be used cautiously in patients with liver and renal disease.

Clopidogrel is a prodrug. Inhibition of platelet aggregation by clopidogrel is achieved through an active metabolite. The metabolism of clopidogrel to its active metabolite can be impaired by genetic variations in CYP2C19 [].

The metabolism of clopidogrel can also be impaired by drugs that inhibit CYP2C19, such as omeprazole or esomeprazole. Avoid concomitant use of clopidogrel with omeprazole or esomeprazole because both significantly reduce the antiplatelet activity of clopidogrel [].

The following serious adverse reactions are discussed below and elsewhere in the labeling:

•         Bleeding

•         Thrombotic thrombocytopenic purpura

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Interactions

Interactions

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