Quick Answer: 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. Drug metabolism occurs in two phases: Phase 1 includes oxidative reactions such as those undertaken by the cytochrome P450s, but also includes reduction and hydrolysis.

What is meant by drug metabolism?

Drug metabolism is the metabolic breakdown of drugs by living organisms, usually through specialized enzymatic systems.

What is drug metabolism in pharmacology?

Drug metabolism is the term used to describe the biotransformation of pharmaceutical substances in the body so that they can be eliminated more easily. The majority of metabolic processes that involve drugs occur in the liver, as the enzymes that facilitate the reactions are concentrated there.

What is the main purpose of drug metabolism?

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.

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How is drug metabolized in 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 are the phases of drug metabolism?

Drug metabolism reactions comprise of two phases: Phase I (functionalization) reactions such as oxidation, hydrolysis; and Phase II (conjugation) reactions such as glucuronidation, sulphate conjugation. Oxidation reactions are the most common and vital.

What is first pass metabolism of drug?

The first-pass metabolism or the first-pass effect or presystemic metabolism is the phenomenon which occurs whenever the drug is administered orally, enters the liver, and suffers extensive biotransformation to such an extent that the bioavailability is drastically reduced, thus showing subtherapeutic action (Chordiya …

What organs are involved in drug metabolism?

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.

What are the four stages of drug metabolization?

The four stages are absorption, distribution, metabolism, and excretion.

What factors can affect drug metabolism in an elderly?

Aging results in a number of significant changes in the human liver including reductions in liver blood flow, size, drug-metabolizing enzyme content, and pseudocapillarization. Drug metabolism is also influenced by comorbid disease, frailty, concomitant medicines, and (epi)genetics.

What are the importance and consequences of drug metabolism?

In general, the metabolism of a drug decreases its therapeutic effect. The majority of drugs are metabolized to increase their water solubility to allow elimination in urine or bile. However some drugs are metabolized into active compounds first before subsequent metabolism to inactive compounds and be excreted.

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What factors affect metabolism of a drug?

Many factors affect the rate and pathway of metabolism of drugs, and the major influences can be sub-divided into internal (physiological and pathological) and external (exogenous) factors as indicated below: Internal: species, genetic (strain), sex, age, hormones, pregnancy, disease. External: diet, environment.

What causes slow drug metabolism?

Underlying health conditions can also influence your drug metabolic rate. Some concerning ones are chronic liver disorders, kidney dysfunction, or advanced heart failure. Drug and Food Interactions. CYP450 enzymes can be impacted by the foods you eat and other drugs you take.

What is oxidation in drug metabolism?

In most cases, an oxygen atom is retained in the metabolite, although some reactions, such as dealkylation, result in loss of the oxygen atom in a small fragment of the original molecule. Oxidation reactions are catalysed by a diverse group of enzymes, of which the cytochrome P450 system is the most important.

What is drug distribution?

Drug distribution refers to the movement of a drug to and from the blood and various tissues of the body (for example, fat, muscle, and brain tissue) and the relative proportions of drug in the tissues.

Where are drugs absorbed?

For these reasons, most drugs are absorbed primarily in the small intestine, and acids, despite their ability as un-ionized drugs to readily cross membranes, are absorbed faster in the intestine than in the stomach (for review, see [1]).

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