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Related Experiment Videos

Photosensitization by drugs

D E Moore

    Journal of Pharmaceutical Sciences
    |September 1, 1977
    PubMed
    Summary
    This summary is machine-generated.

    UV light exposure triggers oxygen consumption in 20 drugs, revealing photosensitizing potential via free radical or single molecular oxygen pathways. Some drugs show dual mechanisms, correlating with in vivo photosensitivity.

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    Area of Science:

    • Photochemistry
    • Medicinal Chemistry
    • Biochemistry

    Background:

    • Many drugs absorb ultraviolet (UV) light, potentially leading to photochemical reactions.
    • Photosensitivity is a known adverse effect of certain medications.
    • Understanding drug photosensitization mechanisms is crucial for drug safety and development.

    Purpose of the Study:

    • To investigate the photosensitizing capabilities of 20 UV-absorbing drugs.
    • To differentiate between Type I (free radical) and Type II (singlet molecular oxygen) photosensitization mechanisms.
    • To correlate in vitro photosensitization findings with known in vivo photosensitivity reactions.

    Main Methods:

    • UV irradiation (365 nm) of air-saturated methanol solutions containing drugs.
    • Monitoring oxygen uptake using a polarographic oxygen electrode.

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  • Assessing Type I mechanism via acrylamide polymerization.
  • Assessing Type II mechanism via 2,5-dimethylfuran oxidation.

    • Main Results:

    • Oxygen uptake was observed for all tested drugs, indicating photosensitization.
    • Phenothiazine and thiazide derivatives exhibited both Type I and Type II mechanisms.
    • Promethazine, trifluoperazine, and furosemide demonstrated high reactivity.
    • Several drugs, including diazepam, tetracycline, and quinine, primarily reacted via the Type II mechanism.
    • A correlation was found between in vitro results and reported in vivo photosensitivity.

    Conclusions:

    • The study elucidates the photosensitization mechanisms of various drugs under UV irradiation.
    • Drug photosensitization can occur through free radical or singlet molecular oxygen pathways.
    • Findings suggest a link between drug structure, photochemical reactivity, and clinical photosensitivity.