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Related Experiment Videos

Safety by design.

D Jack1

  • 1The Slype, Wheathampstead, Hertfordshire, United Kingdom.

Drug Safety
|January 1, 1990
PubMed
Summary
This summary is machine-generated.

Designing safer drugs involves modifying physiological mediators for selective action. This approach led to improved asthma, chemotherapy, and migraine treatments, resulting in more effective and safer medications.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Medicinal Chemistry

Background:

  • Drug safety relies on selective action at target cells, minimizing off-target effects.
  • Physiological mediators like epinephrine, hydrocortisone, and histamine have been modified to create safer, more effective drugs.
  • Past 20 years saw significant improvements in treating conditions like bronchial asthma through targeted drug development.

Purpose of the Study:

  • To outline the principles of "safety by design" in drug development.
  • To illustrate how modifying physiological mediators can lead to safer and more efficacious drugs.
  • To introduce the concepts of type 1 and type 2 agonism in drug action.

Main Methods:

  • Analysis of existing drug development pathways, including beta-2 adrenoceptor stimulants, anti-inflammatory steroids, and antihistamines.

Related Experiment Videos

  • Identification and definition of type 1 and type 2 agonism based on drug-mediator interactions.
  • Modification of existing drugs like salbutamol and serotonin to create novel therapeutic agents.

    • Main Results:

    • Development of salmeterol, a long-acting beta-2 adrenergic bronchodilator, through salbutamol modification.
    • Creation of ondansetron, an antiemetic for chemotherapy, by modifying serotonin (5-hydroxytryptamine).
    • Development of sumatriptan, a novel migraine treatment, also through serotonin modification.

    Conclusions:

    • Modifying physiological mediators is a successful strategy for developing safer and more effective drugs.
    • The principles of "safety by design" and understanding agonism types are crucial for rational drug discovery.
    • Newer drugs like salmeterol, ondansetron, and sumatriptan demonstrate superior efficacy and safety profiles compared to predecessors.