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Medicine LibreTexts

Glossary

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Absorption: The first stage of pharmacokinetics: medications enter the body and travel from the site of administration into the body’s circulation.

medications enter the body and travel from site of administration into the body’s circulation.

Adverse effect: An unintended and potentially dangerous pharmacological effect that occurs when a medication is administered correctly.

Affinity: The strength of binding between drug and receptor.

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Agonist: A drug or ligand that binds to a “receptor” and produces an effect. Agonists may be full or partial.

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Antagonist: A molecule that prevents the action of other molecules, often by competing for a cellular receptor; opposite of agonist. Antagonists may be further described as competitive, non-competitive, or irreversible.

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Bioavailability: The presence of a drug in the bloodstream after it is administered. Bioavailability varies with route of administration.

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Blood–brain barrier (BBB): A nearly impenetrable barricade built from a tightly woven mesh of capillaries tightly woven together to protect the brain from potentially dangerous substances such as poisons or viruses.

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Clearance: The ratio of the rate of elimination of a drug to the plasma concentration of the drug.

The ratio of the rate of elimination of a drug to the plasma concentration of the drug

Competitive antagonists: A drug that competes for the same binding site with an agonist, and their binding is mutually exclusive.

A drug that competes for the same binding site with an agonist.

CYP (Cytochrome) 450 family: Enzymes responsible for most drugs; there are many isoforms of CYP.

Distribution: The second stage of pharmacokinetics; the process by which medication is distributed throughout the body.

Dose-Response: As the dose of a drug increases, the response should also increase. The slope of the curve is characteristic of the particular drugreceptor interaction.

Dose-response curve: Graph showing the relationship between the effectiveness and drug concentration most often expressed as a log.

relationship between the effectiveness and drug concentration most often expressed as a log

Duration: The length of time that a medication is producing its desired therapeutic effect.

Efficacy: The maximum effect of which the drug is capable.

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Excretion: The final stage of pharmacokinetics; the process whereby drug byproducts and metabolites are eliminated from the body.

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First-order kinetics: When a drug follows a first-order pattern of elimination pharmacokinetics, the elimination rate depends on the plasma concentration. As the plasma concentration increases, so does the rate of elimination.

Elimination rate depends on the plasma concentration.

First-pass effect: The inactivation of orally or enterally administered drugs in the liver and intestine. Blood containing the absorbed drug passes through the liver and goes through chemical reactions that can deactivate a substantial amount of the drug and decrease its bioavailability and efficacy.

Half-life: A drug's half-life (t1/2) is the measure of time it takes for the concentration of a drug to be reduced by half.

The measure of time it takes for the concentration of a drug to be reduced by half

Induction: Increased synthesis of drug-metabolizing enzymes.

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Inhibition: Decreased synthesis of drug-metabolizing enzymes or interference with how an enzyme works

Intermediate metabolizer: Reduced metabolic activity.

LD50: Lethal dose of a drug for 50% of the population in an animal study.

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Mechanism of action: How a medication works at a cellular level within the body.

Metabolism: The breakdown of a drug molecule via enzymes in the liver (primarily) or intestines (secondarily).

Non-competitive antagonists: A drug that binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor.

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Normal metabolizer: Normal metabolic activity.

Onset: When a medication first begins to work and exerts a therapeutic effect.

P-glycoprotein: a membrane protein that transports a variety of substances, including drugs, across epithelial membranes.

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Peak: When the maximum concentration of a drug is in the bloodstream.

When the maximum concentration of a drug is in the bloodstream.

Phase I reactions: CYP450 enzyme reactions that convert the parent drug into a metabolite that is more polar and more water soluble, making the drug easier to eliminate. These enzymes are not highly selective for their substrate, so a few isoforms metabolize thousands of drugs.

Phase II reactions: Reactions that increase the water solubility of a drug.

Pharmacodynamics: The study of how drugs act at target sites of action in the body.

Pharmacogenetics: A branch of pharmacology that studies individual variation in the DNA sequence in drug metabolism and response.

Pharamacogenomics: A branch of pharmacology that studies population variation in the DNA sequence in drug metabolism and response.

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Pharmacokinetics: The study of how the body absorbs, distributes, metabolizes, and eliminates drugs.

Pharmacology: The science dealing with the actions of drugs on the body.

Pharmacy: The science of the preparation of drugs.

Poor metabolizer: Little to no functional metabolic activity.

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Potency: The drug dose required to produce a specific intensity of effect.

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Rapid metabolizer: Increased metabolic activity.

Selectivity: A “selective” drug binds to a primary and predictable site to create one desired effect. A “non-selective” drug can bind to many different and unpredictable receptor sites with potential side effects.

Side effect: Effect of a drug, other than the desired effect, sometimes in an organ other than the target organ.

Single nucleotide polymorphism (SNP): a DNA sequence variation that occurs when a single nucleotide in DNA is different from the reference sequence.

Single nucleotide in DNA is different from the reference sequence.

Steady state: When the rate of drug elimination equals the rate of administration.

Therapeutic index: A quantitative measurement of the relative safety of a drug that compares the amount of drug that produces a therapeutic effect with the amount of drug that produces a toxic effect. A medication with a large therapeutic index is safer than a medication with a small therapeutic index. TI= LD50/ED50.

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Therapeutic window: The dosing window is the safe range between the minimum therapeutic concentration and the minimum toxic concentration of a drug; the range in which the most effective treatment will occur.

Ultra-rapid metabolizer: Substantially increased metabolic activity.

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Zero-order kinetics: A process that describes how a drug's metabolism or elimination rate remains constant, regardless of the drug's concentration.

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