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Related Concept Videos

Antihypertensive Drugs: Action of Diuretics01:16

Antihypertensive Drugs: Action of Diuretics

Diuretics are antihypertensive drugs used to treat hypertension resulting from sodium and water retention. Sodium, vital for fluid balance and nerve or muscle function, is regulated by the kidneys through millions of nephrons. Blood enters nephrons via afferent arterioles, which branch into capillaries called glomeruli. These filter blood plasma, allowing water and solutes, like sodium ions, to pass through capillary walls into Bowman's capsule. The filtrate then flows through various tubules...
Antihypertensive Drugs: Thiazide-Class Diuretics01:15

Antihypertensive Drugs: Thiazide-Class Diuretics

Thiazide diuretics are sulfonamide derivatives featuring a benzothiadiazine ring system in their molecular structure. Based on this structure, thiazide diuretics can be categorized into two groups: thiazide-type and thiazide-like diuretics. Thiazide-type diuretics, including hydrochlorothiazide and chlorothiazide, consist of a benzothiadiazine backbone with an attached sulfonamide group. Thiazide-like diuretics, such as chlorthalidone and indapamide, lack the thiazide ring but demonstrate...
Antihypertensive Drugs: Action of β1 Blockers01:17

Antihypertensive Drugs: Action of β1 Blockers

β1-receptors are primarily located in the heart and kidneys. In cardiac myocytes, these receptors interact with neurotransmitters released by the sympathetic nervous system during heightened activity or danger. As a result, β1-receptors get activated, initiating a series of biochemical processes. Excessive activation of beta receptors due to chronic stress can abnormally increase heart rate and contractility, resulting in high blood pressure or hypertension. To counteract this, β1-blockers...
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:

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Related Experiment Video

Updated: Jul 14, 2026

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity
12:02

An Efficient Method for the Synthesis of Peptoids with Mixed Lysine-type/Arginine-type Monomers and Evaluation of Their Anti-leishmanial Activity

Published on: November 2, 2016

Chirality in antirheumatic drugs.

W F Kean1, C J Lock, H E Howard-Lock

  • 1Department of Medicine, McMaster University, Hamilton, Ontario, Canada.

Lancet (London, England)
|December 21, 1991
PubMed
Summary

Chiral drugs, existing as enantiomers, can have varying biological effects. Clinicians need greater awareness of these risks, advocating for single enantiomer use in research and clinical trials.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Clinical Practice

Background:

  • Chirality in drug molecules can lead to enantiomers with distinct biological activities.
  • Clinicians often lack awareness of the risks associated with chiral drug use.
  • Different enantiomers may exhibit varying efficacy and toxicity profiles.

Purpose of the Study:

  • To highlight the potential problems arising from the use of chiral molecules in clinical practice.
  • To discuss the influence of chirality on drug efficacy and toxicity.
  • To recommend the use of single enantiomers in research and clinical settings.

Main Methods:

  • Discussion of chemical conventions for describing chirality.
  • Presentation of examples illustrating chirality's impact on antirheumatic drugs.

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  • Review of biological activities and clinical implications of enantiomers.

    • Main Results:

    • Enantiomers of a drug can possess significantly different biological activities.
    • Chirality influences both the therapeutic efficacy and potential toxicity of drugs.
    • Lack of awareness among clinicians regarding chiral risks is a significant issue.

    Conclusions:

    • Single enantiomers should be preferentially used in biological experiments.
    • Clinical trials should focus on single enantiomer drugs to ensure predictable outcomes.
    • Increased awareness and education on drug chirality are crucial for patient safety.