Dimenhydrinate

Dimenhydrinate
Combination of
DiphenhydramineAntiemetic
8-chlorotheophyllineStimulant
Names
Pronunciationdye" men hye' dri nate[1]
Trade namesDraminate, Gravol, Dramamine, others
Clinical data
Drug classFirst generation antihistamine[1]
Main usesMotion sickness, nausea, vertigo[2]
Side effectsSleepiness, blurry vision, dry mouth, confusion, dizziness[2][1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
    Routes of
    use    		By mouth, rectal, intravenous, intramuscular[2]
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa607046
    Legal
    Legal status
    • AU: S2 (Pharmacy medicine)
    • US: OTC

    Dimenhydrinate, marketed as Dramamine and Gravol among others, is a medication used to treat motion sickness, nausea, and vertigo.[2] While it maybe useful for allergies it has not been studied for this condition.[2] It is a combination of diphenhydramine and 8-chlorotheophylline.[1][4]

    Common side effects include sleepiness, blurry vision, dry mouth, headache, confusion, and dizziness.[2][1] Children may become hyperactive.[2] Other side effects may include urinary retention and glaucoma.[1] It has been taken by many pregnant women without any evidence of harm to the baby.[3] Low doses when breastfeeding appear safe.[3] Dimenhydrinate is a first generation antihistamine.[1] It works mostly via the effects of diphenhydramine which blocks acetylcholine.[2] The 8-chlorotheophylline is present to try to decrease the side effect of sleepiness.[1]

    Dimenhydrinate has been used medically since at least 1947 after being developed by G. D. Searle & Company.[5][6] It is avaliable over-the-counter drug and as a generic medication.[2] In the United States 120 tablets of 50 mg strength can be purchased for less than 10 USD as of 2020.[7] It may be used recreationally for the high that large doses can cause.[8][9]

    Medical uses

    Nausea

    Dimenhydrinate is used to prevent and treat nausea, vomiting, and motion sickness.[1] However, scopolamine, promethazine, or meclizine appears to work better for this indication.[2] Dimenhydrinate works better when taken preventatively rather than after the onset of symptoms.[2]

    Dosage

    The typical dose is 50 to 100 mg by mouth or by injection every four to six hours to a maximum of 400 mg by day.[2] In children doses of 1.25 mg/kg may be used, though use under the age of two is generally not recommended.[2]

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

    Side effects

    Common side effects include sleepiness, blurry vision, dry mouth, headache, confusion, and dizziness.[2][1] Children may become hyperactive.[2] Other side effects may include urinary retention and glaucoma.[1]

    It should not be used in newborns due to the injectable formulation containing benzyl alcohol which may result in "gasping syndrome".[10]

    Pregnancy and breastfeeding

    It has been taken by many pregnant women without any evidence of harm to the baby.[3] Low doses well breastfeeding appear safe.[3]

    Mechanism of action

    It is an H1 receptor antagonist that demonstrates anticholinergic activity.[11]

    Chemistry

    Diphenhydramine is the primary constituent of dimenhydrinate and dictates the primary effect. The main difference relative to pure diphenhydramine is a lower strength due to being combined with 8-chlorotheophylline. By weight, dimenhydrinate is between 53% to 56% diphenhydramine and 44% to 47% 8-chlorotheophylline.[12][13] 8-chlorotheophylline is derived from caffeine.[13]

    Society and culture

    Names

    Dimenhydrinate is marketed under many brand names: in the US, Mexico, and Serbia as Dramamine; in Ukraine as Driminate; in Canada, Costa Rica, and India 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 Colombia as Mareol; in Ecuador as Anautin; in Hungary as Daedalon; in Sweden as Calma or Arlevert;[14] in Indonesia as Antimo; in Italy as Xamamina or Valontan; in Peru as Gravicoll; in Poland and Slovakia as Aviomarin;[15] in Portugal as Viabom, Vomidrine, and Enjomin; in Spain as Biodramina; in Thailand as Daimenin; in Israel as Travamin; in Pakistan as Gravinate; and in Ethiopia as dimenhydrinate.[16]

    Recreational use

    Dimenhydrinate is recreationally used as a deliriant.[17][18][19] Slang terms for Dramamine used this way include "drama", "dime", "dime tabs", "D-Q", "substance D", "d-house", and "drams".[20] 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.[21]

    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.[18] 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.[22] 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.

    Songs

    Modest Mouse produced a song titled "Dramamine" on their 1996 debut album This Is a Long Drive for Someone with Nothing to Think About. The song uses side effects of the drug as a metaphor for the deteriorating state of a personal relationship.[23]

    References

    1. 1 2 3 4 5 6 7 8 9 10 11 "Dimenhydrinate". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. January 16, 2017. Archived from the original on 28 August 2021. Retrieved 10 September 2020.
    2. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 "Dimenhydrinate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 18 October 2020. Retrieved 10 September 2020.
    3. 1 2 3 4 5 6 "Dimenhydrinate Use During Pregnancy". Drugs.com. Archived from the original on 19 October 2020. Retrieved 10 September 2020.
    4. ↑ Putra, Okky Dwichandra; Yoshida, Tomomi; Umeda, Daiki; Higashi, Kenjirou; Uekusa, Hidehiro; Yonemochi, Etsuo (29 July 2016). "Crystal Structure Determination of Dimenhydrinate after More than 60 Years: Solving Salt–Cocrystal Ambiguity via Solid-State Characterizations and Solubility Study". Crystal Growth & Design. 16 (9): 5223–5229. doi:10.1021/acs.cgd.6b00771.
    5. ↑ Sneader, Walter. Drug Discovery: A History. John Wiley & Sons. p. 405. ISBN 978-0-471-89979-2. Archived from the original on 2021-08-28. Retrieved 2020-09-10.
    6. ↑ Root, Walter S.; Hofmann, Frederick G. The Nervous System: Central Nervous System Drugs. Elsevier. p. 311. ISBN 978-1-4832-7583-3. Archived from the original on 2021-08-28. Retrieved 2020-09-10.
    7. ↑ "Compare Dimenhydrinate Prices". GoodRx. Retrieved 10 September 2020.
    8. ↑ Hoffman, Robert S.; Howland, Mary Ann; Lewin, Neal A.; Nelson, Lewis S.; Goldfrank, Lewis R. (2014). Goldfrank's Toxicologic Emergencies, Tenth Edition (ebook). McGraw Hill Professional. p. 667. ISBN 978-0-07-180185-0. Archived from the original on 2021-08-28. Retrieved 2020-10-31.
    9. ↑ Gold, Jennifer. "ConsumerMedSafety.org - Prevent Medication Errors - Consumer Med Safety". consumermedsafety.org. Archived from the original on 21 January 2021. Retrieved 10 September 2020.
    10. ↑ "Dimenhydrinate - FDA prescribing information, side effects and uses". Drugs.com. Archived from the original on 20 October 2020. Retrieved 10 September 2020.
    11. ↑ Canadian Agency for Drugs and Technologies in Health (2015). "Abuse and Misuse Potential of Dimenhydrinate: A Review of the Clinical Evidence [Internet]". CADTH Rapid Response Reports. PMID 26985532.{{cite journal}}: CS1 maint: uses authors parameter (link)
    12. ↑ "Dimenhydrinate injection, solution". Daily Med. U.S. National Library of Medicine. Archived from the original on 4 July 2013. Retrieved 19 July 2014.
    13. 1 2 Enarson, P; Gouin, S; Goldman, RD (April 2011). "Dimenhydrinate use for children with vomiting". Canadian family physician Medecin de famille canadien. 57 (4): 431–2. PMID 21490354.
    14. ↑ "Dimenhydrinat" (in Swedish). Fass-verksamheten. Archived from the original on 2019-08-05. Retrieved 2016-09-27.{{cite web}}: CS1 maint: unrecognized language (link)
    15. ↑ "Aviomarin, tabletki, 50 mg, 5 szt". Dox.pl (in Polish). Archived from the original on 2018-09-09. Retrieved 2014-02-08.{{cite web}}: CS1 maint: unrecognized language (link)
    16. ↑ "Gravinate [Dimenhydrinate]". Karachi Pakistan: The Searle Company Ltd. Archived from the original on 5 May 2013.
    17. ↑ "The Health Risks of Abusing Motion sickness pills". Narconon International. Archived from the original on 2016-09-18. Retrieved 2016-09-13.
    18. 1 2 Lessenger JE, Feinberg SD (2008). "Abuse of prescription and over-the-counter medications". Journal of the American Board of Family Medicine. 21 (1): 45–54. doi:10.3122/jabfm.2008.01.070071. PMID 18178702.
    19. ↑ Gardner DM, Kutcher S (March 1993). "Dimenhydrinate abuse among adolescents". Canadian Journal of Psychiatry. 38 (2): 113–6. doi:10.1177/070674379303800208. PMID 8467436.
    20. ↑ "The Dangers of Dimenhydrinate Abuse". Bright Hub. 2009-10-06. Archived from the original on 2016-09-03. Retrieved 2016-09-13.
    21. ↑ "Dramamine". Grasscity forums. Archived from the original on 2019-08-05. Retrieved 2016-09-13.
    22. ↑ "Are Teens Abusing Motion Sickness Pills? - Muir Wood Adolescent and Family Services". Archived from the original on 2016-09-18. Retrieved 2016-09-13.
    23. ↑ "Modest Mouse: 'This is a long drive...'". Portland. Retrieved 2019-03-26: Glacial Pace Recordings. Archived from the original on 2019-03-27. Retrieved 2019-03-26.{{cite web}}: CS1 maint: location (link)
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