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Dose-Response Relationships

By

Abimbola Farinde

, PhD, PharmD, Columbia Southern University, Orange Beach, AL

Last full review/revision Jun 2021| Content last modified Jun 2021
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Topic Resources

Regardless of how a drug effect Overview of Pharmacodynamics Pharmacodynamics (sometimes described as what a drug does to the body) is the study of the biochemical, physiologic, and molecular effects of drugs on the body and involves receptor binding... read more occurs—through binding or chemical interaction—the concentration of the drug at the site of action controls the effect. However, response to concentration may be complex and is often nonlinear. The relationship between the drug dose, regardless of route used, and the drug concentration at the cellular level is even more complex (see Pharmacokinetics Overview of Pharmacokinetics Pharmacokinetics, sometimes described as what the body does to a drug, refers to the movement of drug into, through, and out of the body—the time course of its absorption, bioavailability, distribution... read more ).

Dose-response data are typically graphed with the dose or dose function (eg, log10 dose) on the x-axis and the measured effect (response) on the y-axis. Because a drug effect is a function of dose and time, such a graph depicts the dose-response relationship independent of time. Measured effects are frequently recorded as maximal at time of peak effect or under steady-state conditions (eg, during continuous IV infusion). Drug effects may be quantified at the level of molecule, cell, tissue, organ, organ system, or organism.

  • Potency (location of curve along the dose axis)

  • Maximal efficacy or ceiling effect (greatest attainable response)

  • Slope (change in response per unit dose)

Hypothetical dose-response curve

Hypothetical dose-response curve

Biologic variation (variation in magnitude of response among test subjects in the same population given the same dose of drug) also occurs. Graphing dose-response curves of drugs studied under identical conditions can help compare the pharmacologic profiles of the drugs (see figure Comparison of dose-response curves for drugs X, Y, and Z Comparison of dose-response curves Regardless of how a drug effect occurs—through binding or chemical interaction—the concentration of the drug at the site of action controls the effect. However, response to concentration may... read more ). This information helps determine the dose necessary to achieve the desired effect.

Comparison of dose-response curves

Drug X has greater biologic activity per dosing equivalent and is thus more potent than drug Y or Z. Drugs X and Z have equal efficacy, indicated by their maximal attainable response (ceiling effect). Drug Y is more potent than drug Z, but its maximal efficacy is lower.

Comparison of dose-response curves

Dose-response, which involves the principles of pharmacokinetics and pharmacodynamics, determines the required dose and frequency as well as the therapeutic index for a drug in a population. The therapeutic index (ratio of the minimum toxic concentration to the median effective concentration) helps determine the efficacy and safety of a drug. Increasing the dose of a drug with a small therapeutic index increases the probability of toxicity or ineffectiveness of the drug. However, these features differ by population and are affected by patient-related factors, such as pregnancy Drugs in Pregnancy Drugs are used in over half of all pregnancies, and prevalence of use is increasing. The most commonly used drugs include antiemetics, antacids, antihistamines, analgesics, antimicrobials, diuretics... read more , age Pharmacodynamics in Older Adults In contrast to pharmacokinetic effects, pharmacodynamics is defined as what the drug does to the body or the response of the body to the drug; it is affected by receptor binding, postreceptor... read more , and organ function (eg, estimated GFR Renal excretion The kidneys are the principal organs for excreting water-soluble substances. The biliary system contributes to excretion to the degree that drug is not reabsorbed from the gastrointestinal ... read more ).

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