|Pronunciation||dye" men hye' dri nate|
|Trade names||Draminate, Gravol, Dramamine, others|
|Drug class||First generation antihistamine|
|Main uses||Motion sickness, nausea, vertigo|
|Side effects||Sleepiness, blurry vision, dry mouth, confusion, dizziness|
|By mouth, rectal, intravenous, intramuscular|
|(what is this?)|
Dimenhydrinate, marketed as Dramamine and Gravol among others, is a medication used to treat motion sickness, nausea, and vertigo. While it maybe useful for allergies it has not been studied for this condition. It is a combination of diphenhydramine and 8-chlorotheophylline.
Common side effects include sleepiness, blurry vision, dry mouth, headache, confusion, and dizziness. Children may become hyperactive. Other side effects may include urinary retention and glaucoma. It has been taken by many pregnant women without any evidence of harm to the baby. Low doses when breastfeeding appear safe. Dimenhydrinate is a first generation antihistamine. It works mostly via the effects of diphenhydramine which blocks acetylcholine. The 8-chlorotheophylline is present to try to decrease the side effect of sleepiness.
Dimenhydrinate has been used medically since at least 1947 after being developed by G. D. Searle & Company. It is avaliable over-the-counter drug and as a generic medication. In the United States 120 tablets of 50 mg strength can be purchased for less than 10 USD as of 2020. It may be used recreationally for the high that large doses can cause.
Dimenhydrinate is used to prevent and treat nausea, vomiting, and motion sickness. However, scopolamine, promethazine, or meclizine appears to work better for this indication. Dimenhydrinate works better when taken preventatively rather than after the onset of symptoms.
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. In children doses of 1.25 mg/kg may be used, though use under the age of two is generally not recommended.
Common side effects include sleepiness, blurry vision, dry mouth, headache, confusion, and dizziness. Children may become hyperactive. Other side effects may include urinary retention and glaucoma.
Pregnancy and breastfeeding
Mechanism of action
It is an H1 receptor antagonist that demonstrates anticholinergic activity.
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. 8-chlorotheophylline is derived from caffeine.
Society and culture
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; in Indonesia as Antimo; in Italy as Xamamina or Valontan; in Peru as Gravicoll; in Poland and Slovakia as Aviomarin; 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.
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.
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.
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