Dimenhydrinate

Source: Wikipedia, the free encyclopedia.
Not to be confused with diphenhydramine.
"Dramamine" redirects here. For other uses, see Dramamine (disambiguation).

Dimenhydrinate
8-chlorotheophylline
Stimulant
Clinical data
Trade namesDramamine, Draminate, Gravol, others
AHFS/Drugs.comMonograph
MedlinePlusa607046
License data
Pregnancy
category
  • AU: A
intramuscular
ATC code
Legal status
Legal status
  • AU: S2 (Pharmacy medicine)
  • CA: OTC
  • US: OTC
ECHA InfoCard
100.007.593 Edit this at Wikidata
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Dimenhydrinate, sold under the brand name Dramamine, among others, is an

8-chlorotheophylline (a chlorinated theophylline derivative) in a 1:1 ratio.[2]

Dimenhydrinate was introduced to the market by

G.D. Searle in 1949.[3][4]

Medical uses

Pills sold in Phonm Penh over the counter

Dimenhydrinate is an over-the-counter (OTC) antihistamine indicated for the prevention and relief of nausea and vomiting from a number of causes, including motion-sickness and post-operative nausea.[2]

Side effects

Common side effects may include:[5]

  • Drowsiness
  • Dry mouth, nose, or throat
  • Constipation
  • Blurred vision
  • Feeling restless or excited (especially in children)

Continuous and/or cumulative use of anticholinergic medications, including first-generation antihistamines, is associated with higher risk of cognitive decline and dementia in older people.[6][7]

Pharmacology

Diphenhydramine is the primary constituent of dimen­hydrinate and dictates the primary effect. The main differences relative to pure diphen­hydramine are a lower potency due to being combined with 8-chloro­theo­phylline (by weight, dimen­hydrinate is between 53% and 55.5% diphen­hydramine)[8] and the fact that the stimulant properties of 8-chloro­theo­phylline help reduce the side effect of drowsiness brought on by diphen­hydramine. Diphen­hydramine is itself an H1 receptor antagonist that demonstrates anticholinergic activity.[9]

Pharmacokinetics

The diphenhydramine component requires about 2 hours to reach peak concentration after either oral or sublingual administration of diphen­hydrinate, and has a half-life of 5 – 6 hours in healthy adults.[1]

Recreational use

Dimenhydrinate is recreationally used as a deliriant.[10][11][12] Slang terms for Dramamine used this way include "drama", "dime", "dime tabs", "D-Q", "substance D", "d-house", and "drams".[13] 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.[14]

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.[11]

Other CNS effects occur within the

ventricular arrhythmias, coma, and death.[15] Such a side effect profile is thought to give ethanolamine-class antihistamines a relatively low abuse liability.[citation needed] An antidote that can be used for dimenhydrinate poisoning is physostigmine.[16]

History

Dimenhydrinate (then known as Compound 1694) was being tested as a potential treatment for

Baltimore Sun, and other national newspapers covered the discovery, and Dramamine was made available in drugstores later that year.[3][4][17]

Brand names

Dimenhydrinate is marketed under many brand names: in the U.S., Mexico, Turkey and Thailand as Dramamine; in Serbia as Dimigal; 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 Indonesia as Antimo; in Italy as Xamamina or Valontan; in Peru as Gravicoll; in Poland and Slovakia as Aviomarin;[18] in Portugal as Viabom, Vomidrine, and Enjomin; in Spain as Biodramina; in Israel as Travamin; and in Pakistan as Gravinate.[19]

Popular culture

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.[20]

References

  1. ^
    PMID 2328304
    .
  2. ^
    S2CID 81387334
    .
  3. ^ a b Newman A (21 June 2012). "New Dramamine Ads Take Aim at Summer Vacationers". The New York Times. Retrieved 26 June 2023.
  4. ^ a b Grauer N (12 February 2019). "Hopkins History Moments: Neil A. Grauer explains how Hopkins expertise helped prevent seasickness". Johns Hopkins Medicine. Retrieved 27 June 2023.
  5. ^ "Dimenhydrinate". Drugs.com. Archived from the original on 28 May 2004. Retrieved 28 May 2004.
  6. PMID 25621434
    .
  7. PMID 19636034
    .
  8. ^ "Dimenhydrinate injection, solution". Daily Med. U.S. National Library of Medicine. Archived from the original on 13 October 2014. Retrieved 19 July 2014.}}
  9. PMID 26985532
    .
  10. ^ "The Health Risks of Abusing Motion sickness pills". Narconon International. Retrieved 13 September 2016.
  11. ^
    PMID 18178702
    .
  12. S2CID 30190588
    .
  13. ^ "The Dangers of Dimenhydrinate Abuse". Bright Hub. 6 October 2009. Retrieved 13 September 2016.
  14. ^ "Dramamine". Budderbongs forums. Retrieved 13 September 2016.
  15. ^ "Are Teens Abusing Motion Sickness Pills? - Muir Wood Adolescent and Family Services". Archived from the original on 18 September 2016. Retrieved 13 September 2016.
  16. S2CID 702353
    .
  17. PMID 30233361
    .
  18. ^ "Aviomarin, tabletki, 50 mg, 5 szt". Dox.pl (in Polish).
  19. ^ "Gravinate [Dimenhydrinate]". Karachi Pakistan: The Searle Company. Archived from the original on 5 May 2013.
  20. ^ "Modest Mouse: 'This is a long drive...'". Portland: Glacial Pace Recordings. Archived from the original on 27 March 2019. Retrieved 26 March 2019.

External links