Drug Elimination

Drug elimination is the irreversible removal of a drug and its metabolites from the body, a process that determines how long pharmacological effects persist and helps guide safe dosing. It occurs mainly through hepatic metabolism, which converts many compounds into more water-soluble products, and renal excretion, which filters, secretes, and sometimes reabsorbs substances in the nephron; biliary and pulmonary routes also contribute. Pharmacologists assess elimination using clearance, elimination rate, and half-life to predict drug concentrations over time. These principles support dose selection, dosing-interval design, evaluation of drug interactions, and adjustment of therapy when liver or kidney function changes.

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JoVE Core - Pharmacology

Kinetics of Drug Elimination

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2023

Eliminating drugs from the body is a vital process that occurs through excretion or metabolism. Understanding the kinetics of drug elimination is crucial for drug development, dosage determination, and optimizing patient outcomes. Drug clearance depends on the rate of drug elimination and its plasma concentration. Another important parameter is the half-life of a drug, which is the time required for its concentration to decrease by half. In most cases, drug clearance follows first-order...

Drug Elimination: Overview

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2025

Drug elimination involves many complex processes and does not necessarily differentiate between distribution and elimination. It is divided into two primary components: excretion and biotransformation. Excretion refers to removing a drug from the body, either in its unchanged form or as its metabolites. Nonvolatile and polar drugs are primarily excreted through the kidneys, with other pathways including bile, sweat, saliva, and milk. Volatile drugs such as anesthetic gases are excreted via the...

Drug Elimination: Non-Renal Routes

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2023

The liver plays a pivotal role in eliminating drugs and their metabolites, primarily through a process known as biliary excretion. This process involves the hepatocytes, the primary cells in the liver that generate bile. A range of transporters actively expels polar drugs or hydrophilic drug metabolites into the bile, which transports the drugs and metabolites into the small intestine. From here, they are eventually expelled from the body through feces. In some instances, the original drug or a...

Drug Elimination: The Concept of Clearance

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2023

Drug elimination refers to removing drugs from the body, either through urine by the kidneys or through bile by the liver. Drug clearance is a pharmacokinetic parameter that measures the efficiency of drug removal from the bloodstream within a specific time frame. It is calculated as the rate at which a drug is eliminated from plasma divided by the plasma concentration of the drug. Drug clearance is not limited to renal excretion but encompasses all organs involved in drug elimination,...

Drug Elimination by Renal Route: Tubular Reabsorption

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2023

During the process of renal excretion, as the glomerular filtrate progresses to the distal convoluted tubule (DCT), drugs that are highly permeable, lipophilic, and nonionized undergo passive reabsorption from the tubular fluid into the surrounding peritubular capillaries. This reabsorption process restricts their elimination through the kidneys. However, the majority of drugs are either weak acids or weak bases, and their ionization level is dependent on pH. By altering the pH of urine, the...

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