Dimenhydrinate

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Dimenhydrinate, also known as diphenhydramine/8-chlorotheophylline salt and sold under the brand names Dramamine and Gravol, among others, is an over-the-counter medication used to treat motion sickness and nausea. Dimenhydrinate is a theoclate salt composed of diphenhydramine and 8-chlorotheophylline (a theophylline relative) in a 1:1 ratio.<ref name = "Hemmings_2019">Template:Cite book</ref>

Dimenhydrinate was introduced to the market by G.D. Searle in 1949.<ref name="Newman 2012">{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref name="Grauer 2019">{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>

Medical uses

File:Dimenhydrinate .jpg

Pills sold in Phonm Penh over the counter

Dimenhydrinate is an over-the-counter (OTC) first-generation antihistamine indicated for the prevention and relief of nausea and vomiting from a number of causes, including motion-sickness and post-operative nausea.<ref name = "Hemmings_2019" />

Side effects

Common side effects of dimenhydrinate may include drowsiness, dry mouth, nose, or throat, constipation, and blurred vision. Some individuals, particularly children, may experience feelings of restlessness or excitement. In certain cases, more severe symptoms may arise, such as delirium, weakness, and a tendency to be easily startled. Hallucinations, psychosis, and an unusual sensitivity to sudden sounds have also been reported.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref>Template:Cite journal</ref><ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> 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. However, in younger people this is not relevant. <ref>Template:Cite journal</ref><ref>Template:Cite journal</ref>

Pharmacology

Pharmacodynamics

Diphenhydramine is the primary constituent of dimenTemplate:Shyhydrinate and dictates the primary effect. The main differences relative to pure diphenTemplate:Shyhydramine are a lower potency due to being combined with 8-chloroTemplate:ShytheoTemplate:Shyphylline (by weight, dimenTemplate:Shyhydrinate is between 53% and 55.5% diphenTemplate:Shyhydramine)<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}}}</ref> and the fact that the stimulant properties of 8-chloroTemplate:ShytheoTemplate:Shyphylline help reduce the side effect of drowsiness brought on by diphenTemplate:Shyhydramine. DiphenTemplate:Shyhydramine is itself an H1 receptor antagonist that demonstrates anticholinergic activity.<ref name="review">Template:Cite journal</ref>

Pharmacokinetics

The diphenhydramine component requires about 2Template:Spaceshours to reach peak concentration after either oral or sublingual administration of dimenTemplate:Shyhydrinate, and has a half-life of Template:Nowrap6Template:Spaceshours in healthy adults.<ref name="oral_sublingual2328304"/>

Recreational use

Dimenhydrinate is recreationally used as a deliriant.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref><ref name=":0">Template:Cite journal</ref><ref>Template:Cite journal</ref> Slang terms for Dramamine used this way include "drama", "dime", "dime tabs", "D-Q", "substance D", "d-house", and "drams".<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> 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 recreational dose.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>

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.<ref name=":0" />

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 arrhythmias, coma, and death.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref> Such a side effect profile is thought to give ethanolamine-class antihistamines a relatively low abuse liability.Template:Citation needed An antidote that can be used for dimenhydrinate poisoning is physostigmine.<ref>Template:Cite journal</ref>

History

Dimenhydrinate (then known as Compound 1694) was being tested as a potential treatment for hay fever and hives at Johns Hopkins Hospital in 1947 by allergists Dr. Leslie Gay and Dr. Paul Carliner. Among those who received the drug was a pregnant woman who had suffered from motion sickness her entire life. She remained symptom-free if she took dimenhydrinate a few minutes before boarding a trolley, whereas the placebo was ineffective. To confirm these findings, the following year, G.D. Searle & Co. conducted a trial in which dimenhydrinate or placebo was given to U.S. troops crossing the Atlantic during "a rough passage" in a converted freight ship, the General Ballou, for 10 days as a rescue therapy for sea sickness. The findings were positive, as were the findings of a second trial of mostly women on the ship's return voyage. Gay and Carliner announced their discovery at a meeting of the Johns Hopkins Medical Society on February 14, 1949, as well as in the Bulletin of The Johns Hopkins Hospital. The New York Times, the Baltimore Sun, and other national newspapers covered the discovery, and Dramamine was made available in drugstores later that year.<ref name="Newman 2012"/><ref name="Grauer 2019"/><ref name="pmid30233361">Template:Cite journal</ref>

Brand names

Dimenhydrinate is marketed under many brand names:

Brand name	Countries
Dramamine	U.S, Mexico, Turkey, Thailand
Dimigal	Serbia
Driminate	Ukraine
Gravol	Canada, Costa Rica, India
Gravamin	Iceland
Dramina	Russia, Croatia
Vomex	South Africa, Germany
Travacalm	Australia
Vertirosan	Austria
Dramin	Brazil
Mareol	Colombia
Anautin	Ecuador
Daedalon	Hungary
Antimo	Indonesia
Xamamina	Italy
Valontan	Italy
Gravicoll	Peru
Aviomarin	citation	CitationClass=web }}</ref> Slovakia
Viabom	Portugal
Vomidrine	Portugal
Enjomin	Portugal
Biodramina	Spain
Travamin	Israel
Gravinate	citation	CitationClass=web }}</ref>
Cinfamar	citation	CitationClass=web }}</ref>

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.<ref>{{#invoke:citation/CS1|citation |CitationClass=web }}</ref>

"The Ending Of Dramamine" is the opening track of the album How To Leave Town by Car Seat Headrest.

External links

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