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Drug intelligence / Profile preview
dimenhydrinate
- Development stage
- Approved
- Lead developer
- Wanbang Biopharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular, Intravenous, Rectal
01
Overview
Dimenhydrinate is a first-generation antihistamine and a salt consisting of diphenhydramine and 8-chlorotheophylline. It is primarily used for the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. The drug exerts its therapeutic effect through the diphenhydramine component, which acts as a competitive antagonist at H1 receptors in the vestibular system and the chemoreceptor trigger zone, thereby inhibiting the transmission of nauseogenic stimuli. Additionally, it exhibits anticholinergic properties by antagonizing muscarinic receptors. The 8-chlorotheophylline component was originally included to mitigate the sedative effects of diphenhydramine, though its clinical impact on alertness is minimal. Dimenhydrinate is widely available as an over-the-counter medication in various oral, rectal, and parenteral formulations.
- Brand names
- DramamineGravolDriminateVomex ATravelmin
- Other names
- diphenhydramine 8-chlorotheophyllinatediphenhydramine8-chlorotheophyllinatediphenhydramine-8-chlorotheophyllinate
02
Targets
HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)
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