Why is metabolism of a drug important to consider as part of drug development?

A drug is eliminated either by excretion or by metabolism to one or more active or inactive metabolites. When elimination occurs primarily by metabolism, the routes of metabolism can significantly affect the drug’s safety and efficacy and the directions for use.

How does metabolism affect drugs?

Drugs can be metabolized by oxidation, reduction, hydrolysis, hydration, conjugation, condensation, or isomerization; whatever the process, the goal is to make the drug easier to excrete. The enzymes involved in metabolism are present in many tissues but generally are more concentrated in the liver.

What role does drug metabolism play in making the excretion of drugs more efficient?

what role does drug metabolism play in making the excretion of drugs more efficient? it makes the drugs more polar.

Why is the study of drug metabolism and pharmacokinetics important in drug discovery and development?

The central role of DMPK in drug discovery is to contribute to the optimisation of compounds for man by balancing the properties associated with drug gastrointestinal absorption (for orally delivered therapies), distribution, clearance, elimination and DDI potential as rapidly and cost effectively as possible.

What is the desired objective of drug metabolism?

The primary goals of drug metabolism assessment at the preclinical stage are to resolve metabolic stability, identify and quantify primary metabolites, pinpoint metabolic routes by enzyme catalysis as well as inhibition and induction, and measure the potential for drug-drug interactions [12].

What is drug metabolism in medicinal chemistry?

Drug metabolism is the chemical alteration of a drug via a biological system to aid its elimination by increasing its hydrophilicity. Since drug metabolism is mediated by enzymes, there is potential for natural variability and for co-administered drugs to interact, either by enzyme inhibition or induction.

Where does drug metabolism occur in the body?

Most drugs must pass through the liver, which is the primary site for drug metabolism. Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms. The liver’s primary mechanism for metabolizing drugs is via a specific group of cytochrome P-450 enzymes.

What is metabolism and what factors affect it?

Metabolism refers to the countless chemical processes going on continuously inside the body that allow life and normal functioning. Your metabolic rate is influenced by many factors – including age, gender, muscle-to-fat ratio, amount of physical activity and hormone function.

How are drugs metabolism?

Where does drug metabolism occur in the cell?

Quantitatively, the smooth endoplasmic reticulum of the liver cell is the principal organ of drug metabolism, although every biological tissue has some ability to metabolize drugs.

What is metabolism in pharmacology?

Drug metabolism is the chemical alteration of a drug by the body. Some drugs are chemically altered by the body (metabolized). The substances that result from metabolism (metabolites) may be inactive, or they may be similar to or different from the original drug in therapeutic activity or toxicity.