Dimenhydrinate

Dimenhydrinate
ATC Code A04AB02
Formula C24H28ClN5O3
Molar Mass (g·mol−1) 469,96
Physical State solid
Melting Point (°C) 102-107
CAS Number 523-87-5
PUB Number 10660
Drugbank ID DB00985
Solubility soluble in water

Basics

Dimenhydrinate is a drug from the group of antihistamines. The active substance is a salt of diphenhydramine and 8-chlorotheophylline. After ingestion, the salt is broken down by the body and the two substances are released. Dimenhydrinate is therefore a combination of 2 active substances. The actual antihistamine is diphenhydramine, while 8-chlorotheophylline is stimulant and counteracts the fatigue-producing effect of the drug. Dimenhydrinate is usually used to treat nausea and vomiting and as a sedative. Dimenhydrinate is mainly taken as a tablet or chewable tablet/gum and does not require a prescription.

Pharmacology

Pharmacodynamics

Diphenhydramine is CNS mobile and acts at histamine receptors in the brain. In doing so, it acts as an inverse agonist. This means that diphenhydramine binds to the H1 receptor and decreases its activity. It is therefore activated less often. Since histamine is involved in the H1-receptor development of nausea, this reduces the accompanying nausea. 8-Chlortheophylline binds to A receptors and prevents the development of fatigue.

Pharmacokinetics

The protein binding of the substance is about 98% and the half-life is about 1-4 hours. The substance is degraded in the liver by enzymes of the CYP450 system and excreted in the urine.

Toxicity

Side effects

Chewing dimenhydrinate medicines may cause numbness in the mouth. Other possible side effects are dry mouth, increase in heart rate, stuffy nose, blurred vision, and increase in intraocular pressure.

Signs of overdose include hallucinations, delirium, confusion, and increased violent tendencies.

Toxicological data

1320 mg-kg-1 (LD50, Rat, Oral)

Editorial principles

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Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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