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As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate , which is the rate-limiting step in hepatic cholesterol biosynthesis.
As noted above, statins exhibit action beyond lipid-lowering activity in the prevention of atherosclerosis through so-called "pleiotropic effects of statins". [147] The pleiotropic effects of statins remain controversial. [154] The ASTEROID trial showed direct ultrasound evidence of atheroma regression during statin therapy. [155]
In studies using standard doses, statins have been found to lower LDL-C by 18% to 55%, depending on the specific statin being used. A risk exists of muscle damage (myopathy and rhabdomyolysis) with statins. Hypercholesterolemia is not a risk factor for mortality in persons older than 70 years and risks from statin drugs are more increased after ...
The action of drugs on the human body (or any other organism's body) is called pharmacodynamics, and the body's response to drugs is called pharmacokinetics. The drugs that enter an individual tend to stimulate certain receptors, ion channels, act on enzymes or transport proteins. As a result, they cause the human body to react in a specific way.
Ezetimibe, sold under the brand name Zetia among others, is a medication used to treat high blood cholesterol and certain other lipid abnormalities. [3] [4] Generally it is used together with dietary changes and a statin. [5]
Ezetimibe/atorvastatin (trade names Liptruzet, Atozet) is a cholesterol lowering combination drug. In the United States, it was approved in May 2013, by the Food and Drug Administration for the treatment of elevated low-density lipoprotein (LDL) in patients with primary or mixed hyperlipidemia as adjunctive therapy to diet. [ 1 ]
The statins differ with respect to their ring structure and substituents. These differences in structure affect the pharmacological properties of the statins, such as: [6] Affinity for the active site of the HMGR; Rates of entry into hepatic and non-hepatic tissues; Availability in the systemic circulation for uptake into non-hepatic tissues
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. [2] A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor . [ 3 ]