跳至主要内容

Factors Affecting Drug Metabolism

 Drug metabolism refers to the chemical change process of drugs in the body. Most drugs lose their activity after being metabolized, and are converted into extremely high water-soluble metabolites, which are beneficial to excretion from the body. There are also some drugs that are hardly metabolized in the body and are excreted as original drugs. For more details, please read Factors Affecting Pharmacokinetics of Drugs.

The metabolism of drugs requires the participation of enzymes. The liver is an important organ for drug metabolism. The cytochrome P-450 enzyme system of liver microsomes is the main enzyme system that promotes drug metabolism, so it is called liver drug enzymes. Some drugs can also be decomposed by related enzymes in other tissues.

The availability and content of liver drug enzymes are not unstable, and individual differences are large, and they are easily affected by certain drugs. Any drug that can enhance the activity of liver drug enzymes or accelerate the synthesis is called drug enzyme inducer, which can accelerate the metabolism of the drug itself and some other drugs, which is one of the reasons for drug tolerance. For example, phenobarbital has a strong drug-enzyme induction effect, and continuous medication can accelerate its own metabolism and that of the anticoagulant warfarin, reducing its efficacy. Any drug that can reduce the activity or synthesis of drug enzymes is called drug enzyme preparations, which can slow down the metabolism of some other drugs and enhance the drug effect. For example, chloramphenicol is a drug enzyme inhibitor, which can slow down the metabolism of phenytoin sodium. Taking the two drugs together can increase the blood concentration of phenytoin sodium, enhance the efficacy, and even cause toxic reactions. Therefore, it is necessary to pay attention to the mutual influence of the drugs when combining drugs.

Contact Us 

Email : marketing@medicilon.com

Tel : +44 1223 981 792（Europe）

        +82 (0)70-8269-5849（South Korea）

        08044216898（Japan）

        +86 021 58591500（China )

Website: https://www.medicilon.com

Related Articles:

Factors Affecting Pharmacokinetics of Drugs

Factors Affecting Metabolism

标签：

评论

发表评论

此博客中的热门博文

What is preclinical testing?

In the process of  preclinical testing  of a compound or biological agent into a drug, the compound involved must go through the testing phase. First, we need to identify potential targets that can treat the disease. Then, a variety of compounds or preparations are screened out. Any compound that has shown potential as a drug for the treatment of this disease needs to be tested for toxicity before clinical testing to reduce the possibility of injury. preclinical testing What is the basis of preclinical testing? According to US Food and Drug Administration (FDA) regulations, a series of tests are required before a new drug is approved for use. In the first stage, basic research determines a hypothetical target for the treatment of a certain disease, and then screens small molecules or biological compounds to discover any substance with the potential to treat the disease. Then, a  preclinical research  phase followed, before which, as described above, the potential toxicity of the compou
发表评论
阅读全文

Inventory of the three major in vitro pharmacokinetic research methods

  The metabolic properties of a compound are an essential factor in whether or not it can be used as a drug in the clinical setting, so pharmacokinetic studies of newly synthesized compounds are required in drug development. In vitro incubation with liver microsomes, recombinant CYP450 enzyme lines, and in vitro incubation with hepatocytes are some of the more common in vitro drug metabolism methods. 1. In vitro incubation method with liver microsomes The metabolic stability and metabolic phenotypes of candidate compounds in different species of liver microsomes are good predictors of the metabolic properties of compounds in vivo. They are practical tools for evaluating candidate compounds in the pre-development phase of drug development. Liver microsomes include rat liver microsomes, human liver microsomes, canine liver microsomes, monkey liver microsomes, and mouse liver microsomes. In in vitro incubation of the liver, microsomes are the "gold standard" for in vitro d
发表评论
阅读全文

Novel Parkinson’s Therapies Possible with New Mouse Model

Parkinson's disease (PD) is a neurodegenerative disorder that is marked by the accumulation of the protein, α-synuclein (αS), into clumps known as Lewy bodies, which diminish neural health. Now, researchers from Brigham and Women's Hospital (BWH) report the development of a mouse model to induce PD-like αS aggregation, leading to resting tremor and abnormal movement control. The mouse responds to L-DOPA, similarly to patients with PD. The team's study (“Abrogating Native α-Synuclein Tetramers in Mice Causes a L-DOPA-Responsive Motor Syndrome Closely Resembling Parkinson’s Disease”) on the use of this transgenic mouse model appears in  Neuron . “α-Synuclein (αS) regulates vesicle exocytosis but forms insoluble deposits in PD. Developing disease-modifying therapies requires animal models that reproduce cardinal features of PD. We recently described a previously unrecognized physiological form of αS, α-helical tetramers, and showed that familial PD-causing missense mutati
发表评论
阅读全文