Luhan Pharmachem Co., Ltd.

Luhan pharmachem Co., Ltd. supplies Clopidogrel Bisulfate bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Clopidogrel Bisulfate is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Clopidogrel Bisulfate?

Clopidogrel (INN) is an oral, cheap thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, sale peripheral vascular disease, order and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi under the trade name Plavix. The drug works by irreversibly inhibiting a receptor called P2Y12, an adenosine diphosphate (ADP) chemoreceptor on platelet cell membranes.

Pharmacology

Clopidogrel is a prodrug, the action of which may be related to an ADP receptor on platelet cell membranes. The drug specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in activation of platelets and eventual cross-linking by the protein fibrin. Platelet inhibition can be demonstrated two hours after a single dose of oral clopidogrel, but the onset of action is slow, so that a loading-dose of 300 mg is usually administered.

Clinical Use

Clopidogrel is indicated for:

• Prevention of vascular ischemic events in patients with symptomatic atherosclerosis
• Acute coronary syndrome without ST-segment elevation (NSTEMI)
• ST elevation MI (STEMI)

It is also used, along with acetylsalicylic acid (ASA, brand name Aspirin), for the prevention of thrombosis after placement of intracoronary stent or as an alternative antiplatelet drug for patients who are intolerant to ASA.

Pharmacokinetics

After repeated 75 mg oral doses of clopidogrel (base), plasma concentrations of the parent compound, which has no platelet inhibiting effect, are very low and are generally below the quantification limit (0.258 µg/L) beyond two hours after dosing.

Clopidogrel is a pro-drug activated in the liver by cytochrome P450 enzymes, including CYP2C19. Due to opening of the thiophene ring, the chemical structure of the active has three sites that are stereochemically relevant, making a total of eight possible isomers. These are: a stereocentre at C4 (attached to the ¡ªSH thiol group), a double bond at C3¡ªC16, and the original stereocentre at C7. Only one of the eight structures is an active antiplatelet drug. This has the following configuration: Z configuration at the C3¡ªC16 double bond, the original S configuration at C7, and although the stereocentre at C4 can’t be directly determined, as the thiol group is too reactive, work with the active metabolite of the related drug prasugrel suggests that R-configuration of the C4 group is critical for P2Y12 and platelet-inhibitory activity.

What are the side effects of Clopidogrel Bisulfate?

Serious adverse drug reactions associated with clopidogrel therapy include:

Severe neutropenia (low white blood cells) (Incidence: 1/2,000)Thrombotic thrombocytopenic purpura (TTP) (Incidence: 4/1,000,000 patients treated)

Hemorrhage – The annual incidence of hemorrhage may be increased by the co-administration of aspirin.

• Gastrointestinal hemorrhage (Incidence: 2.0% annually)
• Cerebral Hemorrhage (Incidence: 0.1 to 0.4% annually)

Use of non-steroidal anti-inflammatory drugs is discouraged in those taking clopidogrel due to increased risk of digestive tract hemorrhage

Bleeding in the postoperative period. This is especially a problem for patients after heart surgery where Clopidogrel is associated with a more than double the take back for bleeding rate, as well as other complicatons. The take back for bleeding occurs when there is chest tube clogging in the setting of ongoing bleeding in early postoperative period. Often, if chest tube clogging can be avoided, and the chest tubes drain, the patient can be given platelets until the platelet defect is corrected and the bleeding ceases. But if the bleeding continues, and the chest tubes occlude, then the patient will become hemodynamically unstable and may require an emergency take back to the operating room. This impacts outcomes and costs of care.

Most studies researching clopidogrel do not compare patients on clopidogrel to patients taking placebo, rather clopidogrel use is compared to aspirin use. Thus attributing side effects directly to clopidogrel is difficult.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.