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Pharmacokinetics: Overview

Pharmacokinetics: Overview

Pharmacokinetics is a scientific discipline that focuses on the journey of a drug within the body, encompassing four key stages: absorption, distribution, metabolism, and elimination. The first stage, absorption, involves the drug's transfer into the bloodstream. Several factors dictate the extent and speed of this process. For example, the liver often metabolizes oral drugs before they reach systemic circulation, leading to only partial absorption. In contrast, intravenous (IV) administration...

Pharmacokinetic–Pharmacodynamic Relationship: Problems

Pharmacokinetic–Pharmacodynamic Relationship: Problems

The empirical approach to drug therapy optimization relies on correlating pharmacological response with administered dosage. Such an approach can be costly, time-consuming, and often yields poor correlation due to variables like formulation factors and drug elimination characteristics. A more precise approach correlates response with plasma drug concentration or the amount of drug in the body, rather than dosage. This is achieved through pharmacokinetic-pharmacodynamic (PK/PD) modeling, which...

Nonlinear Pharmacokinetics: Role of Transporters

Nonlinear Pharmacokinetics: Role of Transporters

A drug's nonlinear kinetics can be influenced by a diverse range of transporter proteins that serve as crucial players in drug distribution. These transporters, found within cells, can enhance or reduce local drug concentrations by facilitating the influx or efflux of drugs. For instance, the expression of xenobiotic transporters can be influenced by factors such as age and gender, potentially impacting the linearity of drug response.
Polymorphisms occurring in drug transporters can alter...

Biopharmaceutics and Pharmacokinetics: Overview

Biopharmaceutics and Pharmacokinetics: Overview

Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the appropriate...

Nonlinear Pharmacokinetics: Overview

Nonlinear Pharmacokinetics: Overview

Nonlinear or dose-dependent pharmacokinetics is a phenomenon that occurs when the pharmacokinetic parameters of certain drugs deviate from linear pharmacokinetics at higher doses. These drugs do not follow the expected first-order kinetics, where the rate of drug elimination is directly proportional to the drug concentration. Instead, they exhibit a nonlinear relationship, which can be attributed to several factors.
Nonlinearity can arise due to the saturation of plasma protein-binding or...

Toxicokinetics: Overview

Toxicokinetics: Overview

Studies that assess how a drug is absorbed, distributed, metabolized, and excreted (ADME) at toxic doses are termed toxicokinetics. Understanding toxicokinetics helps predict adverse drug reactions (ADRs) and manage toxicity in humans.Toxicokinetics differs from pharmacokinetics mainly in the dose levels studied, with toxicokinetics focusing on higher toxic doses. The kinetics at these levels can be non-linear due to altered physiological processes. Toxicodynamics examines the relationship...

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Updated: Jun 21, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

Published on: December 3, 2020

From pharmacokinetics to therapeutics.

Martin K Church¹, Michel Gillard, Maria Laura Sargentini-Maier

¹Charité - Universitätsmedizini Berlin, Germany. mkc@ southampton.ac.uk

Drug Metabolism Reviews

|July 16, 2009

Summary

Pharmacokinetic-pharmacodynamic (PK-PD) models integrate drug dose, concentration, and response over time. This review focuses on PK-PD models for allergic disease therapies, including receptor occupancy and adverse effects, to optimize dosing and benefit-risk assessment.

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Area of Science:

Pharmacology
Pharmacometrics
Drug Development

Background:

Pharmacokinetics (PK) relates drug dose to concentration-time profiles.
Pharmacodynamics (PD) links drug concentration to response.
Pharmacokinetic-pharmacodynamic (PK-PD) models integrate PK and PD for a comprehensive understanding of drug behavior.

Purpose of the Study:

To review PK-PD models for drugs used in treating allergic diseases.
To emphasize the role of receptor occupancy in clinical response.
To discuss PK-PD models for adverse effects.

Main Methods:

Literature review of PK-PD modeling in allergic diseases.
Analysis of receptor occupancy in relation to drug effects.
Evaluation of PK-PD models for both therapeutic and adverse effects.

Main Results:

PK-PD models provide a framework for understanding the time course of drug response.
Receptor occupancy is a key factor linking drug concentration to clinical outcomes.
Models for adverse effects are also crucial for comprehensive drug evaluation.

Conclusions:

Integrated PK-PD modeling aids in selecting optimal dosing regimens.
These models facilitate objective benefit-risk assessment of medications.
Application of PK-PD principles enhances therapeutic strategies for allergic diseases.