Clopidogrel

Clopidogrel is an oral antiplatelet agent (thienopyridine class) to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi-Aventis under the trade name Plavix, by Sun Pharmaceuticals under the trade name Clopilet, by Ranbaxy Laboratories under the trade name Ceruvin. It works by irreversibly inhibiting a receptor called P2Y12. Adverse effects include hemorrhage.

Clinical use

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Indications

Clopidogrel is indicated for:[2]
Prevention of vascular ischaemic events in patients with symptomatic atherosclerosis
Acute coronary syndrome without ST-segment elevation (NSTEMI),
ST elevation MI (STEMI)

It is also used, along with aspirin, for the prevention of thrombosis after placement of intracoronary stent. [2]

International guidelines granted the highest grade of recommendation for NSTE-ACS, PCI and stent,[clarification needed] for Clopidogrel in addition to Aspirin. Consensus-based therapeutic guidelines recommend also the use of clopidogrel, instead of aspirin, in patients requiring antiplatelet therapy but with a history of gastric ulceration, as inhibition of the synthesis of prostaglandins by aspirin (acetylsalicylic acid) can exacerbate this condition. A study has shown that in patients with healed aspirin-induced ulcers, however, patients receiving aspirin plus the proton pump inhibitor esomeprazole had a lower incidence of recurrent ulcer bleeding than patients receiving clopidogrel. [3] However, a more recent study suggested that prophylaxis with proton pump inhibitors along with clopidogrel following acute coronary syndrome may increase adverse outcomes, possibly due to inhibition of CYP2C19 which is required for activation of clopidogrel, itself a pro-drug.[4]

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Dosage forms

Clopidogrel is marketed as clopidogrel bisulfate (clopidogrel hydrogen sulfate), most commonly under the trade names Plavix, as 75 mg oral tablets.

Atorvastatin

Atorvastatin (INN) (pronounced /əˌtɔrvəˈstætən/) (Lipitor, Pfizer), is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammatory and other mechanisms.

Atorvastatin inhibits HMG-CoA reductase, the rate-determining enzyme located in hepatic tissue that produces mevalonate, a small molecule used in the synthesis of cholesterol and other mevalonate derivatives. This lowers the amount of cholesterol produced which in turn lowers the total amount of LDL cholesterol. Atorvastatin was first synthesized in 1985 by Bruce Roth while working at Parke-Davis Warner-Lambert Company (now Pfizer). With 2008 sales of US$12.4 billion, Lipitor is likely the top-selling drug in the world.[1] US patent protection is scheduled to expire in June 2011.[2] However, Pfizer made an agreement with Ranbaxy Laboratories to delay the generic launch in the US until November 2011.[1]

Lipitor is not the only statin; there are several other statins on the market.[3][4]

Contraindications
Active liver disease: cholestasis, hepatic encephalopathy, hepatitis, and jaundice.
Unexplained elevations in AST or ALT levels
Pregnancy.
Breast-feeding.

Fluvastatin

Fluvastatin (Lescol, Canef, Vastin) is a member of the drug class of statins, used to treat hypercholesterolemia and to prevent cardiovascular disease. It has also been shown to exhibit antiviral activity against Hepatitis C.[1]

Pravastatin

Pravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used for lowering cholesterol and preventing cardiovascular disease. Initially known as CS-514, it was originally identified in a bacterium called Nocardia autotrophica by researchers of the Sankyo Pharma Inc..[1] It is presently being marketed outside Japan by the pharmaceutical company Bristol-Myers Squibb.

The U.S. Food and Drug Administration approved generic pravastatin for sale in the United States for the first time on April 24, 2006. Generic pravastatin sodium tablets (10 mg, 20 mg and 40 mg) are manufactured by TEVA Pharmaceuticals in Kfar Sava, Israel.[2]

Simvastatin

Simvastatin (INN) (pronounced /ˈsɪmvəstætɨn/), (marketed under the trade names Zocor, Simlup, Simcard, Simvacor, and others) is a hypolipidemic drug belonging to the class of pharmaceuticals called "statins". It is used to control hypercholesterolemia (elevated cholesterol levels) and to prevent cardiovascular disease. Simvastatin is a synthetic derivate of a fermentation product of Aspergillus terreus.

Simvastatin is a powerful lipid-lowering drug that can decrease low density lipoprotein (LDL) levels by up to 50%. It is used in doses of 5 mg up to 80 mg. Higher doses (160 mg) have been found to be too toxic, while giving only minimal benefit in terms of lipid lowering. There is no real effect on HDL and triglyceride levels.

From recent research it has become apparent that simvastatin and other statins inhibit the progression of atherosclerosis beyond their effects on LDL. Many explanations have been proposed, for example its inhibitory effect on macrophages in the atherosclerotic plaque lesions.

In one non-randomized study, simvastatin halved the risk of developing dementia or Parkinson's disease.[3]

Lovastatin

Lovastatin is a member of the drug class of statins, used for lowering cholesterol (hypolipidemic agent) in those with hypercholesterolemia and so preventing cardiovascular disease. Lovastatin is a naturally occurring drug found in food such as oyster mushrooms[1] and red yeast rice[2].

Lovastatin is an inhibitor of 3-hydroxy-3methylglutaryl-coenzyme A reductase (HMG-CoA reductase), an enzyme which catalyzes the conversion of HMG-CoA to mevalonate.[20] Mevalonate is a required building block for cholesterol biosynthesis and lovastatin interferes with its production by acting as a reversible competitive inhibitor for HMG-CoA which binds to the HMG-CoA reductase. Lovastatin, being inactive in the native form, the form in which it is administered,is hydrolysed to the β-hydroxy acid form in the body and it is this form which is active.

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