Substance
ID:862
Names and Identifiers
Brand Name
DramalenDramaminEldodramGravinolVomex ATroversinXamaminaDiamarinDimenestDramilinReise-EnglettenDramarinDromylHydrinateNovaminePermitalTravelminAmosytAnautineAnteminDimateDimentabsGravolMenhydrinateNeo-NaviganSupremalTeodraminTravelinAndramineAviomarinChloranautineDramyl
IUPAC name
8-chloro-1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-7-ide; [2-(diphenylmethoxy)ethyl]dimethylazanium
IUPAC Traditional name
8-chloro-1,3-dimethyl-2,6-dioxo-7H-purin-7-ide; [2-(diphenylmethoxy)ethyl]dimethylazanium
Synonyms
DiphenhydrinateDimenhydrinate
Properties
Physical Property
Solubility
3000 mg/L
Hydrophobicity(logP)
-0.39
Molecule Details
Drug Groups
approved
Description
Dimenhydrinate (Dramamine, Gravol and Vertirosan) is an over-the-counter drug used to prevent motion sickness. It is closely related to diphenhydramine HCl, or Benadryl. It is primarily a H1-antagonist, but also possesses an antimuscarinic effect.
Indication
Used for treating vertigo, motion sickness, and nausea associated with pregnancy.
Pharmacology
Dimenhydrinate is an antiemetics drug combination that contains diphenhydramine and theophylline. It is not effective in the treatment of nausea associated with cancer chemotherapy. Dimenhydrinate directly inhibits the stimulation of certain nerves in the brain and inner ear to suppress nausea, vomiting, dizziness, and vertigo. Diphenhydramine and dimenhydinate both reduce vestibular neuronal excitation due to angular or linear acceleration motions.
Toxicity
Symptoms of overdose include delerium, hallucinations, and excitment. Patients may be violent and confused.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic (cytochrome P-450 system).
Absorption
Well absorbed after oral administration.
Half Life
1 to 4 hours
Protein Binding
98 to 99%.
References
•
Takeda N, Morita M, Hasegawa S, Horii A, Kubo T, Matsunaga T: Neuropharmacology of motion sickness and emesis. A review. Acta Otolaryngol Suppl. 1993;501:10-5.
[Pubmed]
•
Halpert AG, Olmstead MC, Beninger RJ: Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7.
[Pubmed]
•
Jaju BP, Wang SC: Effects of diphenhydramine and dimenhydrinate on vestibular neuronal activity of cat: a search for the locus of their antimotion sickness action. J Pharmacol Exp Ther. 1971 Mar;176(3):718-24.
[Pubmed]
External Links
Molecular Spectra
No Data Available
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References
• Takeda N, Morita M, Hasegawa S, Horii A, Kubo T, Matsunaga T: Neuropharmacology of motion sickness and emesis. A review. Acta Otolaryngol Suppl. 1993;501:10-5. Pubmed
• Jaju BP, Wang SC: Effects of diphenhydramine and dimenhydrinate on vestibular neuronal activity of cat: a search for the locus of their antimotion sickness action. J Pharmacol Exp Ther. 1971 Mar;176(3):718-24. Pubmed
• Halpert AG, Olmstead MC, Beninger RJ: Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7. Pubmed