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Related Concept Videos

Principles of Drug Action01:24

Principles of Drug Action

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Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
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Targets for Drug Action: Overview01:26

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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

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Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
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Cholinergic Antagonists: Pharmacokinetics01:24

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Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
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Cholinergic Antagonists: Pharmacological Actions01:28

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Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
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Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
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Why medicines work.

David C Swinney1

  • 1DCSwinney Consulting, Belmont, CA 94002, USA.

Pharmacology & Therapeutics
|March 30, 2022
PubMed
Summary
This summary is machine-generated.

Analyzing first-in-class drugs approved by the FDA reveals key therapeutic actions. Most successful drugs modulate systems via sensors/controllers, while others repair or disrupt functions, offering insights into drug efficacy.

Keywords:
Drug actionDrug discoveryMechanismMedicinesPharmacologyPhysiologic context

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Area of Science:

  • Pharmacology and Therapeutics
  • Drug Discovery and Development
  • Molecular Biology

Background:

  • A small fraction of drug-target interactions lead to effective therapeutics.
  • Understanding the molecular mechanisms connecting drug action to phenotypic changes is limited.
  • Identifying successful drug action modalities is crucial for future drug development.

Purpose of the Study:

  • To analyze the actions of first-in-class drugs approved by the U.S. FDA between 1999 and 2020.
  • To identify characteristics of successful drug actions and their underlying molecular mechanisms.
  • To elucidate the relationship between drug modality, physiological processes, and therapeutic outcomes.

Main Methods:

  • Analysis of 233 first-in-class drugs approved by the U.S. FDA (1999-2020).
  • Classification of drugs based on their primary mechanism of action.
  • Examination of how drug actions interact with physiological processes to achieve therapeutic effects.

Main Results:

  • Drug actions were categorized into three main groups: system modulation via sensors/receptors and controllers (51%), disruption of essential functions (12%), and molecular repair/removal/silencing (33%).
  • Antimicrobials were grouped with function disruptors, while antivirals fell into the molecular action category.
  • Successful drug actions often leverage physiological processes, including committed transitions, to enhance specificity and therapeutic impact.

Conclusions:

  • Drug actions can be broadly classified, with system modulation being the most common successful strategy.
  • Understanding the molecular basis of drug action, particularly how they interface with physiological regulatory nodes, is key to therapeutic success.
  • Future drug development can benefit from insights into these successful action modalities and their reliance on physiological processes for specificity.