Dramamine

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1. ドラマミン(乗物酔い予防の抗ヒスタミン剤の商標名)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/26 13:30:44」(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	Dramamine
AHFS/Drugs.com	monograph
MedlinePlus	a607046
Pregnancy category	AU: A US: B (No risk in non-human studies)
Legal status	AU: Pharmacy Only (S2) US: OTC
Routes of administration	Oral, Rectal, I.V.
Identifiers
CAS Registry Number	523-87-5 Y
ATC code	R06AA52
PubChem	CID: 10660
DrugBank	DB00985 Y
ChemSpider	10210 Y
UNII	JB937PER5C Y
KEGG	D00520 Y
ChEMBL	CHEMBL1200406 N
N (what is this?)  (verify)

Dimenhydrinate (marketed as Dramamine, Gravol and many other brand names) is an over-the-counter antiemetic used for the treatment of the symptoms of motion sickness. It is most commonly prepared as tablets, although it is also available in liquid form and in suppositories. Dimenhydrinate is a combination of two drugs: diphenhydramine and 8-chlorotheophylline.

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 used as a deliriant at doses of 50mgs to 700mgs although body weight plays a significant part in dosing of this drug. Slang terms for Dramamine used this way include "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 tabs 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. The suggested dosage is 50 mg for dogs and 10 mg for cats; duration of effect is 8 hours. This dosage is not a proper measure for all pets and should be adjusted by weight.

Brand names

Dimenhydrinate is marketed under many brand names: in the USA and Serbia as Dramamine, in Ukraine as Driminate, in India and Canada as Gravol, in Iceland and Russia as Gravamin, in South Africa and Germany as Vomex, in Australia as Vertirosan, in Brazil as Dramin, in Ecuador as Anautin, in Hungary as Daedalon, in Sweden as Amosyt, in Indonesia as Antimo, in Italy as Xamamina, in Peru as Gravicoll, in Poland 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. Postoperative nausea and vomiting
• 2. 乗物酔い motion sickness
• 3. 回転性めまいの治療 treatment of vertigo
• 4. 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
• 5. 小児における片頭痛の急性期治療 acute treatment of migraine in children

English Journal

• Transcutaneous aortic valve replacement with the Edwards SAPIEN XT and Medtronic CoreValve prosthesis under fluoroscopic guidance and local anaesthesia only.

• Greif M, Lange P, Näbauer M, Schwarz F, Becker C, Schmitz C, Pohl T, D'Anastasi M, Boekstegers P, Massberg S, Kupatt C.Author information Medizinische Klinik und Poliklinik I, Klinikum Grosshadern, University Hospital of Munich, , Munich, Germany.AbstractOBJECTIVE: To assess the feasibility of transcatheter aortic valve implantation (TAVI; Medtronic CoreValve and Edwards SAPIEN XT) under local anaesthesia with only mild analgesic medication and fluoroscopic guidance.
• Heart (British Cardiac Society).Heart.2014 Jan 23. doi: 10.1136/heartjnl-2013-304918. [Epub ahead of print]
• OBJECTIVE: To assess the feasibility of transcatheter aortic valve implantation (TAVI; Medtronic CoreValve and Edwards SAPIEN XT) under local anaesthesia with only mild analgesic medication and fluoroscopic guidance.METHODS: 461 patients underwent TAVI under local anaesthesia with lidocaine. The pro
• PMID 24459291

• Erythema Multiforme Secondary to Dimenhydrinate in a Patient With Previous Similar Reactions to Pamabrom.

• Tan DS, Sklar GE.Author information Khoo Teck Puat Hospital, Singapore.AbstractOBJECTIVE: To report a case of erythema multiforme secondary to dimenhydrinate and pamabrom cross-sensitivity.
• The Annals of pharmacotherapy.Ann Pharmacother.2014 Jan 6. [Epub ahead of print]
• OBJECTIVE: To report a case of erythema multiforme secondary to dimenhydrinate and pamabrom cross-sensitivity.CASE SUMMARY: A 22-year-old Chinese female presented with a complaint of lip mucosal ulceration with necrosis and stomatitis, worsening over the past 24 hours and associated with reduced ora
• PMID 24396093

• Evaluation of the effects of anti-motion sickness drugs on subjective sleepiness and cognitive performance of healthy males.

• Weerts A, Pattyn N, Van de Heyning P, Wuyts F.Author information 1Antwerp University Research Center for Equilibrium and Aerospace, University of Antwerp, Antwerp, Belgium.AbstractThis study aimed to investigate the clinical and cognitive side effects of baclofen (10 mg), meclizine (50 mg), dimenhydrinate (40 mg) plus cinnarizine (20 mg) and promethazine (25 mg) plus d-amphetamine (5 mg). The study had a double-blind, placebo controlled, repeated measures design and was conducted on healthy male volunteers. The psychomotor vigilance test, the Sternberg working memory task, the implicit memory test and the automated Operation Span (Ospan) task were performed. The Stanford, the Karolinska and the Epworth Sleepiness scale determined the degree of sleepiness. The Profile of Mood States (POMS) evaluated mood states and adverse effects were reported on a 22-item questionnaire. Letter recalls and time for solving mathematical problems, recorded during the Ospan task, were impaired by baclofen and dimenhydrinate-cinnarizine respectively, suggesting an influence of these drugs on the working memory. Significant side effects for baclofen were: sleepiness, tiredness, blurred vision, concentration problems and dizziness whereas for dimenhydrinate-cinnarizine only sleepiness and blurred vision were reported. Meclizine decreased the accuracy on the Sternberg working memory task and thus seemed to affect short-term memory. A reported side effect was increased sleepiness. Promethazine plus d-amphetamine did not affect any of the tested cognitive functions. However, many side effects such as sleepiness, dry mouth, dizziness, vertigo, confusion, insomnia and tremors were reported. The results show that meclizine and dimenhydrinate combined with cinnarizine were the two drugs with the most acceptable combination of side effects.
• Journal of psychopharmacology (Oxford, England).J Psychopharmacol.2013 Dec 17. [Epub ahead of print]
• This study aimed to investigate the clinical and cognitive side effects of baclofen (10 mg), meclizine (50 mg), dimenhydrinate (40 mg) plus cinnarizine (20 mg) and promethazine (25 mg) plus d-amphetamine (5 mg). The study had a double-blind, placebo controlled, repeated measures design and was condu
• PMID 24346808

Japanese Journal

• 手術後の嘔吐を抑えるためのDimenhydrinate(Dramamine)筋注

• Moore D.C. [他]
• The Journal of the American Medical Association 日本版 24(4), ????, 1956-10-00
• NAID 40017455231

• 抗-Histamine劑の嘔吐鎭靜作用に関する研究 第1報 β-Dimethylaminoethyl benzohydryl ether 8-chlorotheophyllinate (Dramamine) の二，三薬理作用，特にBenadrylとの比較研究

• 久本 一與
• 岡山医学会雑誌 65(1), 130-139, 1953-01-31
• NAID 120002789831

• 抗-Histamine劑の嘔吐鎭靜作用に関する研究 第2報 β-Dimethylaminoethyl benzohydryl ether 8-chlorotheophyllinate (Dramamine) のApomorphine-嘔吐に対する鎭静作用

• 久本 一與
• 岡山医学会雑誌 65(1), 139-145, 1953-01-31
• NAID 120002789830

Related Links

• Dramamine® Motion Sickness Relief

Dramamine® Motion Sickness Relief for prevention and treatment of nausea, vomiting and dizziness associated with motion sickness. CONTACT US WHERE TO BUY Login SignUp Forget your password? Motion Sickness Relief

• Dramamine® Motion Sickness Relief

Dramamine® Motion Sickness Relief for prevention and treatment of nausea, vomiting and dizziness associated with motion sickness. ... Product Information For the prevention and treatment of the symptoms associated with motion ...

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