Description

Simple

A medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness.

Clinical

A medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness.

Overview

Dimenhydrinate, also known as Dramamine or Gravol, is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate is a combination drug composed of [DB01075] and [DB14132] in a salt form, with 53%-55.5% of diphenhydramine, and not less than 44%-47% of 8-chlorotheophylline, calculated on the dried basis.

The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system [3] while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade [4]. The addition of 8-chlorotheophylline was initially intended to counteract the sedative effects of diphenhydramine.

When used in large doses, dimenhydrinate has been shown to cause a "high" characterized by hallucinations, excitement, incoordination, and disorientation [Read more

Pharmacology

Indication

Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.

Pharmacodynamic

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, vomi... Read more

Mechanism of action

The mechanism by which some antihistamines exert their antiemetic, anti-motion sickness, and anti-vertigo effects is not precisely known but may be related to their central anticholinergic actions. They diminish vestibular stimulation and depress labyrinthine function. An action on the medullary che... Read more

Absorption

Well absorbed after oral administration.

Protein binding

98 to 99%.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

1 to 4 hours

Route of elimination

Information currently not available.

Toxicity

Symptoms of overdose include delerium, hallucinations, and excitment. Patients may be violent and confused.

Adverse Effects

Contraindications

  • Route:
    • Intramuscular
    • Intravenous
  • Dose Form:
    • Injection
  • Regions: US
  • Age Groups:
    • neonatal
    • premature infants

Food Interactions

  • Avoid alcohol.
  • Take with food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Dimenhydrinate.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Dimenhydrinate.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Dimenhydrinate.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abexinostat
The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Abexinostat.
Acebutolol
The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Acebutolol.
Acepromazine
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Aceprometazine.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Dimenhydrinate.
Acetophenazine
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Acetophenazine.
Acetyldigoxin
The risk or severity of QTc prolongation can be increased when Acetyldigoxin is combined with Dimenhydrinate.
Acetylglycinamide chloral hydrate
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Acetylglycinamide chloral hydrate.
Aclidinium
Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
Acrivastine
The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Dimenhydrinate.
Adenosine
The risk or severity of QTc prolongation can be increased when Adenosine is combined with Dimenhydrinate.
Adinazolam
The risk or severity of adverse effects can be increased when Adinazolam is combined with Dimenhydrinate.
Adipiplon
The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Adipiplon.
4 References
  1. 1 . 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: 8447218
  2. 2 . 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: 11835984
  3. 3 . 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: 4329456
  4. 4 . Spealman RD: Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism. Psychopharmacology (Berl). 1988;95(1):19-24.PubMed: 3133696