Dose–response relationship in the context of "Pharmacological effect"

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⭐ Core Definition: Dose–response relationship

The dose–response relationship, or exposure–response relationship describes the magnitude of the response of a biochemical or cell-based assay or an organism, as a function of exposure (or doses) to a stimulus or stressor (usually a chemical) after a certain exposure time. Dose–response relationships can be described by dose–response curves, or concentration-response curves. This is explained further in the following sections. A stimulus response function or stimulus response curve is defined more broadly as the response from any type of stimulus, not limited to chemicals.

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👉 Dose–response relationship in the context of Pharmacological effect

In pharmacology, biological activity or pharmacological activity describes the beneficial or adverse effects of a drug on living matter. When a drug is a complex chemical mixture, this activity is exerted by the substance's active ingredient or pharmacophore but can be modified by the other constituents. Among the various properties of chemical compounds, pharmacological/biological activity plays a crucial role since it suggests uses of the compounds in the medical applications. However, chemical compounds may show some adverse and toxic effects which may prevent their use in medical practice.

Biological activity is usually measured by a bioassay and the activity is generally dosage-dependent, which is investigated via dose-response curves. Further, it is common to have effects ranging from beneficial to adverse for one substance when going from low to high doses. Activity depends critically on fulfillment of the ADME criteria. To be an effective drug, a compound not only must be active against a target, but also possess the appropriate ADME (Absorption, Distribution, Metabolism, and Excretion) properties necessary to make it suitable for use as a drug. Because of the costs of the measurement, biological activities are often predicted with computational methods, so-called QSAR models.

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Dose–response relationship in the context of Toxicology

Toxicology is a scientific discipline, overlapping with biology, chemistry, pharmacology, and medicine, that involves the study of the adverse effects of chemical substances on living organisms and the practice of diagnosing and treating exposures to toxins and toxicants. The relationship between dose and its effects on the exposed organism is of high significance in toxicology. Factors that influence chemical toxicity include the dosage, duration of exposure (whether it is acute or chronic), route of exposure, species, age, sex, and environment. Toxicologists are experts on poisons and poisoning. There is a movement for evidence-based toxicology as part of the larger movement towards evidence-based practices. Toxicology is currently contributing to the field of cancer research, since some toxins can be used as drugs for killing tumor cells. One prime example of this is ribosome-inactivating proteins, tested in the treatment of leukemia.

The word toxicology (/ˌtɒksɪˈkɒləi/) is a neoclassical compound from Neo-Latin, first attested c. 1799, from the combining forms toxico- + -logy, which in turn come from the Ancient Greek words τοξικός toxikos, "poisonous", and λόγος logos, "subject matter").

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Dose–response relationship in the context of PK/PD models

PKPD modeling (pharmacokinetic pharmacodynamic modeling) (alternatively abbreviated as PK/PD or PK-PD modeling) is a technique that combines the two classical pharmacologic disciplines of pharmacokinetics and pharmacodynamics. It integrates a pharmacokinetic and a pharmacodynamic model component into one set of mathematical expressions that allows the description of the time course of effect intensity in response to administration of a drug dose. PKPD modeling is related to the field of pharmacometrics.

Central to PKPD models is the concentration-effect or exposure-response relationship. A variety of PKPD modeling approaches exist to describe exposure-response relationships. PKPD relationships can be described by simple equations such as linear model, Emax model or sigmoid Emax model. However, if a delay is observed between the drug administration and the drug effect, a temporal dissociation needs to be taken into account and more complex models exist:

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