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Related Concept Videos

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles in drug...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
Drug-Receptor Bonds01:25

Drug-Receptor Bonds

Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...
Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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Combined Effects of Drugs: Antagonism

The combined effects of drugs can result in various interactions, of which an important type is antagonism. Antagonism is a mechanism where one drug inhibits or counteracts the effects of another drug. Antagonism can occur through various means, including receptor binding, allosteric modulation, functional interaction, chemical reactions, and pharmacokinetic processes.
The most common type is receptor antagonism, where one drug acts as an antagonist to block the effects of another drug by...

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Related Experiment Video

Updated: Jul 19, 2026

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions
12:18

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions

Published on: August 3, 2021

Interactions between oxicams and membrane bilayers: an explanation for their different COX selectivity.

M Lúcio1, H Ferreira, José L F C Lima

  • 1Departamento de química Física, Faculdade de Farmácia da Universidade do Porto. Rua Aníbal Cunha, 164, 4050-047 Porto, Portugal.

Medicinal Chemistry (Shariqah (United Arab Emirates))
|October 5, 2006
PubMed
Summary

Investigating oxicam interactions with biomembrane models revealed distinct behaviors. Meloxicam and lornoxicam, COX-2 inhibitors, showed lower membrane partitioning but altered fluidity, unlike COX-1 inhibitors piroxicam and tenoxicam.

Related Experiment Videos

Last Updated: Jul 19, 2026

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions
12:18

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions

Published on: August 3, 2021

Area of Science:

  • Pharmacology
  • Biochemistry
  • Physical Chemistry

Background:

  • Meloxicam, a COX-2 selective NSAID for arthritis, has a superior safety profile attributed to its chemical structure.
  • Other structurally similar oxicams lack COX-2 selectivity and exhibit reduced gastric tolerance.
  • Understanding oxicam-biomembrane interactions is crucial for explaining gastrointestinal resorption and mucosal tolerability.

Purpose of the Study:

  • To investigate the interactions between oxicams and biomembrane models.
  • To correlate these interactions with their resorption and gastromucosal tolerability.
  • To differentiate oxicam behavior based on their membrane interactions.

Main Methods:

  • Liposome-water partition coefficient calculation to determine oxicam partitioning.
  • Fluorescence quenching to ascertain oxicam location within lipid bilayers.
  • Zeta-potential and steady-state anisotropy measurements to assess binding behavior and membrane perturbation.

Main Results:

  • Oxicams exhibited differential interactions with biomembrane models despite structural similarities.
  • COX-1 inhibitors (piroxicam, tenoxicam) showed higher liposome partitioning and less membrane perturbation.
  • COX-2 inhibitors (meloxicam, lornoxicam) displayed lower partitioning but greater alteration of membrane fluidity and surface potential.

Conclusions:

  • Oxicams can be virtually divided into two groups based on their biomembrane interaction profiles.
  • Meloxicam and lornoxicam's distinct membrane interactions may contribute to their COX-2 selectivity and safety profile.
  • Membrane interaction studies provide insights into NSAID gastrointestinal tolerability and resorption.