dimenhydrinate

ジメンヒドリナート 　

WordNet

1. antihistamine and antiemetic (trade name Dramamine) used to treat motion sickness (同)Dramamine

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/04/09 18:30:38」(JST)

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"Dramamine" redirects here. For other uses, see Dramamine (disambiguation).

Dimenhydrinate

Combination of
diphenhydramine	antiemetic
8-chlorotheophylline	stimulant
Clinical data
Trade names	Gravol, Dramamine
AHFS/Drugs.com	Monograph
MedlinePlus	a607046
Pregnancy category	AU: A US: B (No risk in non-human studies)
Routes of administration	Oral, Rectal, I.V.
ATC code	R06AA52 (WHO)
Legal status
Legal status	AU: S2 (Pharmacy only) US: OTC
Identifiers
CAS Number	523-87-5 Y
PubChem CID	10660
DrugBank	DB00985 Y
ChemSpider	10210 Y
UNII	JB937PER5C
KEGG	D00520 Y
ChEMBL	CHEMBL1200406 N
ECHA InfoCard	100.007.593
NY (what is this?)  (verify)

Dimenhydrinate, marketed as Dramamine and Gravol among others, is an over-the-counter medication used to treat motion sickness and nausea. Dimenhydrinate is a combination of two drugs: diphenhydramine and 8-chlorotheophylline.

It is most commonly prepared as tablets, although it is also available in liquid form and in suppositories.

Medical uses

Dimenhydrinate is primarily used to treat nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate has also been found to aid in the treatment of ear congestion.

Diphenhydramine is the primary constituent of dimenhydrinate and dictates the primary effect. The main difference relative to pure diphenhydramine is a lower potency due to being combined with 8-chlorotheophylline. By weight, dimenhydrinate is between 53% to 55.5% diphenhydramine.

8-Chlorotheophylline, a chlorinated derivative of theophylline, was added in order to counteract drowsiness. Theophylline is very closely related to caffeine and theobromine, mild central nervous system stimulants. It was thought by scientists that by combining the antiemetic effects of diphenhydramine with a stimulant, the extreme drowsiness induced by the former could be mitigated somewhat by the latter. The sedation caused by diphenhydramine, however, is substantially stronger than the stimulation caused by 8-chlorotheophylline, so the overall effect is still mostly sedating.

Recreational use

Dimenhydrinate is recreationally used as a deliriant. Slang terms for Dramamine used this way include "drama", "dime", "dime tabs", "D-Q", "substance D", "d-house", and "drams". Abusing Dramamine is sometimes referred to as Dramatizing or "going a dime a dozen", a reference to the amount of Dramamine tablets generally necessary for a trip.

Many users report a side effect profile consistent with tropane alkaloid (e.g. atropine) poisoning as both show antagonism of muscarinic acetylcholine receptors in both the central and autonomic nervous system, which inhibits various signal transduction pathways. In the CNS, diphenhydramine readily crosses the blood-brain barrier, exerting effects within the visual and auditory cortex.

Other CNS effects occur within the limbic system and hippocampus, causing confusion and temporary amnesia due to decreased acetylcholine signaling. Toxicology also manifests in the autonomic nervous system, primarily at the neuromuscular junction, resulting in ataxia and extrapyramidal side-effects and the feeling of heaviness in the legs, and at sympathetic post-ganglionic junctions, causing urinary retention, pupil dilation, tachycardia, irregular urination, and dry red skin caused by decreased exocrine gland secretions, and mucous membranes. Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death. Such a side-effect profile is thought to give ethanolamine-class antihistamines a relatively low abuse liability. The specific antidote for dimenhydrinate poisoning is physostigmine, usually given by IV in a hospital.

Veterinary use

Dimenhydrinate has successfully been used as an antiemetic and sedative in housepets. It is commonly used to reduce the effects of idiopathic vestibular syndrome.

Brand names

Dimenhydrinate is marketed under many brand names: in the USA, Mexico and Serbia as Dramamine, in Ukraine as Driminate, in India and Canada as Gravol, in Iceland as Gravamin, in Russia and Croatia as Dramina, in South Africa and Germany as Vomex, in Australia and Austria as Vertirosan, in Brazil as Dramin, in Ecuador as Anautin, in Hungary as Daedalon, in Sweden as Calma or Arlevert, in Indonesia as Antimo, in Italy as Xamamina or Valontan, in Peru as Gravicoll, in Poland and Slovakia as Aviomarin, in Portugal as Viabom, in Spain as Biodramina, in Thailand as ไดเมนนีน (Daimenin), and in Pakistan as Gravinate.

References

UpToDate Contents

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• 1. 乗物酔い motion sickness
• 2. 回転性めまいの治療 treatment of vertigo
• 3. 妊娠の悪心および嘔吐の治療および転帰 treatment and outcome of nausea and vomiting of pregnancy
• 4. 制吐剤の特性 characteristics of antiemetic drugs
• 5. 前庭神経炎および内耳炎 vestibular neuritis and labyrinthitis

English Journal

• Selective determination of dimenhydrinate in presence of six of its related substances and potential impurities using a direct GC/MS method.

• Belal TS1, Abdel-Hay KM2, Clark CR3.
• Journal of advanced research.J Adv Res.2016 Jan;7(1):53-8. doi: 10.1016/j.jare.2015.01.010. Epub 2015 Feb 7.
• A novel simple, direct and selective gas chromatography-mass spectrometry (GC/MS) procedure was developed for the determination of the antihistamine drug dimenhydrinate (DMH) in presence of six of its related substances and potential impurities, namely, diphenylmethane, diphenylmethanol, benzophenon
• PMID 26843970

• Simultaneous Determination of Cinnarizine and Dimenhydrinate in Binary Mixture Using Chromatographic Methods.

• Lamie NT1, Monir HH2.
• Journal of chromatographic science.J Chromatogr Sci.2016 Jan;54(1):36-42. doi: 10.1093/chromsci/bmv103. Epub 2015 Sep 8.
• Two accurate and sensitive chromatographic methods have been developed and validated for simultaneous determination of cinnarizine (CIN) and dimenhydrinate (DIM). The first method uses simultaneous quantitative thin layer chromatography (TLC) spectrodensitometric evaluation of them, using ethyl acet
• PMID 26354946

• Effect of Oral Dimenhydrinate in Children with Acute Gastroenteritis: A Clinical Trial.

• Gheini S1, Ameli S1, Hoseini J2.
• Oman medical journal.Oman Med J.2016 Jan;31(1):18-21. doi: 10.5001/omj.2016.04.
• OBJECTIVES: One of the major causes of mortality in children is acute gastroenteritis. Vomiting is common in early stages of the disease. The aim of this study was to determine the effect of oral dimenhydrinate (DH) in the control of vomiting in cases of acute gastroenteritis in children.METHODS: Th
• PMID 26813018

Japanese Journal

• Determination of dimenhydrinate in human plasma by liquid chromatography-electrospray tandem mass spectrometry : Application to a relative bioavailability study

• Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 853(1), 127-132, 2007-06-15
• NAID 10025803752

• Intramuscular droperidol versus intramuscular dimenhydrinate for the treatment of acute peripheral vertigo in the emergency department : A randomized clinical trial

• Acad Emerg Med 9, 650-653, 2002
• NAID 30022441567

• Intravenous Lorazepam versus dimenhydrinate for treatment of vertigo in the emergency department : a randomized clinical trial

• Ann Emerg Med 36, 310-319, 2000
• NAID 30016777101

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★リンクテーブル★

リンク元	「ジメンヒドリナート」「triptone」

「ジメンヒドリナート」

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英

dimenhydrinate

ラ

dimenhydrinatum

商

ドラマミン Dramamine

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トリプトン

「triptone」

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トリプトン

関

dimenhydrinate