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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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Related Experiment Video

Updated: Jan 4, 2026

Assessing the Autonomic and Behavioral Effects of Passive Motion in Rats using Elevator Vertical Motion and Ferris-Wheel Rotation
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Intranasal Scopolamine for Motion Sickness.

Aleksandra S Stankovic, Donna L Alvarenga, Vernie R Coleman Daniels

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    Intranasal scopolamine (IN SCOP) shows potential for rapid motion sickness relief. However, its time to maximum concentration was longer than expected, indicating a need for formulation improvements.

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    Area of Science:

    • Pharmacology
    • Neuroscience
    • Emergency Medicine

    Background:

    • Motion sickness (MS) requires rapid, non-injection therapies for
    • Intranasal scopolamine (IN SCOP) offers a potential fast-acting route, bypassing slowed gastric motility during MS.

    Purpose of the Study:

    • To evaluate the efficacy, pharmacodynamics, and pharmacokinetics of IN SCOP.
    • To compare IN SCOP pharmacokinetic outcomes with existing literature.

    Main Methods:

    • A placebo-controlled, randomized, double-blind, dose-ranging study.
    • 18 healthy adults received placebo, 0.2 mg, or 0.4 mg IN SCOP via a nasal pump with gel formulation.
    • Participants underwent motion challenge in an OVAR chair 1.25 hours post-dose; PK/PD assessed in 8 subjects.

    Main Results:

    • Both low and high doses of IN SCOP significantly increased motion sickness tolerance (chair time) versus placebo.
    • No significant adverse effects like sleepiness or cognitive impairment were observed.
    • Time to maximal concentration (Tmax) was prolonged (61.9-75.0 min), not superior to oral scopolamine.

    Conclusions:

    • IN SCOP demonstrates potential as a rapid administration route for motion sickness.
    • Further research is needed to optimize intranasal formulations and delivery methods for improved pharmacokinetics.