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Dimenhydrinate

From Wikipedia, the free encyclopedia

Dimenhydrinate
Dimenhydrinate.svg
Combination of
diphenhydramine antiemetic
8-chlorotheophylline stimulant
Clinical data
Trade names Gravol, Dramamine
AHFS/Drugs.com Monograph
MedlinePlus a607046
Pregnancy
category
  • AU: A
  • US: B (No risk in non-human studies)
Routes of
administration
Oral, Rectal, Intravascular, Intramuscular
ATC code
Legal status
Legal status
  • AU: S2 (Pharmacy only)
  • US: OTC
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.007.593 Edit this at Wikidata
 ☒N☑Y (what is this?)  (verify)

Dimenhydrinate, marketed as Dramamine and Gravol among others, is an over-the-counter medication used to treat motion sickness and nausea. Dimenhydrinate is a combination, or a salt[1] of two drugs: diphenhydramine and 8-chlorotheophylline.

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

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Transcription

Diphenhydramine is an antihistamine and anticholinergic that's commonly used to combat allergies, insomnia, and cold symptoms. With doses beyond the recommend amount, it can have strong sedating and eventually deliriant effects. The experiences it provides are usually unpleasant. The effects of a drug will vary for each user, especially with a hallucinogen like Diphenhydramine. So, the most I can do is provide a general overview of the effects. Among the positive effects are music enhancement, muscle relaxation, and vivid hallucinations (though, the hallucinations can be negative.) The negative effects include delirium, confusion, fear, paranoia, nausea, muscle cramps, dry mouth, increased heart rate, itching, tremors, stomach pain, an inability to communicate, memory loss, impaired coordination, and urinary retention. The dose you use greatly determines Diphenhydramine's effects. At lower doses, such as under 300 mg, delirium doesn't occur. Instead, it's common to enter a somewhat uncomfortable, sedated, and restless state. Then, generally over 500 or 600 mg, delirium can take over. In between those doses, the experience may have some deliriant effects and is largely just uncomfortable both physically and mentally. The delirium it produces can result in fully realistic hallucinations, which are often nightmarish and can feature spiders, bugs, phantom people, and other disconcerting things. It's very important to understand that unlike with psychedelics, the mental effects of Diphenhydramine are almost always negative. Some users report feelings of impending doom and a general paranoia about everything that's taking place. Often, you will feel very heavy, which makes movement difficult. At lower doses, the drug does work for allergy-related issues, insomnia, motion sickness, and common cold symptoms. At sub-deliriant doses, it can also potentiate other depressants. When used orally, the experience usually lasts for 6 to 8 hours. The onset is 60 to 120 minutes. Depending on the dose, noticeable after effects could persist for up to 24 hours. Diphenhydramine is a member of the anticholinergic and antihistaminergic classes. Its allergy alleviating effects come from inverse agonism of histamine H1 receptors. Also, it affects central H1 receptors, contributing to drowsiness. It's been shown to inhibit serotonin reuptake, but it's not clear how important that effect is. Much of its effects come from antagonism at muscarinic acetylcholine receptors. This action provides delirium and contributes to sedation. Since the drug isn't selective, it binds to muscarinic receptors around the CNS and elsewhere. The drug was discovered in 1943. It was made by Dr. George Rieveschl, who was working on a project that hoped to find a substance to counter muscle spasms. By 1946, it had become the first prescription antihistamine on the market in the US. Then, we learned more about its pharmacology in the 1960s when its serotonin reuptake inhibition was discovered. In the 1980s, it was approved for over the counter sale, with people largely buying it as an anti-allergy drug and sleep aid. In 2002, the FDA began requiring a new label on Diphenhydramine products that warns people not to combine multiple Diphenhydramine products. The FDA was concerned about accidental deliriant doses being obtained, particularly in children. Diphenhydramine is usually found in capsules, tablets, liquids, and you can also order it as a powder. Among its brand names are Benadryl, Nytol, and Sominex. When using the drug, make sure you're taking a product that only contains Diphenhydramine as an active ingredient. Some products contain other drugs, like acetaminophen, which can be dangerous at high doses. A normal dose with common products is 25 to 50 mg per unit. When you're only using it for insomnia, around 50 mg is a normal amount. For recreational effects, a light dose is 150 to 250 mg. A common dose is 250 to 500 mg, and a strong dose is 500 to 650 mg or more. As noted earlier, the drug changes from mainly being a sedative to being a deliriant once you reach a high common or strong dose. You should always check your local laws before ordering or using Diphenhydramine. It's legal in the United States. And, it's usually legal elsewhere, though there may be age restrictions on the drug. In New Zealand, sales are restricted. The substance is controlled in Zambia and if you happen to be traveling there, you could end up in trouble with it. According to the State Department, US travelers have been detained and even jailed for products like Benadryl. One of the main issues with Diphenhydramine is that deliriants are inherently dangerous due to their mental effects. You cannot reliably make good decisions when in a delirious state. If you were to use the drug at high doses, a monitor would be needed. Psychotic states could be triggered by the drug and psychosis, which can go hand in hand with delirium, may result in dangerous behavior and hospitalizations. At lower doses, it can enhance the effects of other depressants. But, once a large amount is used, it should not be combined with other depressants. High doses have caused death before. We don't know what the lethal dose may be. Based on animal studies, the LD50 could be around 4,500 mg for the average adult. However, anything over 1 gram may be very troublesome and over 2 grams could conceivably be fatal. Large doses can also acutely damage the kidneys, particularly in susceptible people. When it's used regularly at recreational doses, it seems capable of causing kidney and bladder problems. Cardiac arrhythmias and other cardiac problems are possible, with the concern increasing as the dose rises. Regular use, which almost no one engages in, is likely to have negative cognitive effects and other issues. Again, make sure to avoid products that contain other active substances like acetaminophen. Tolerance to Diphenhydramine develops quickly. Even with a normal sedative dose, tolerance can develop within a few days and will dissipate in around a week. If you have any questions about Diphenhydramine, feel free to leave them in the comments section. You can also leave them in the Reddit thread for this video, which is linked in the description. Support on Patreon is greatly appreciated, since it allows me to provide more drug education. If you want to help out, head to patreon.com/thedrugclassroom. You can also contribute via PayPal, Bitcoin, or directly through YouTube on the channel page. You can connect with me on Twitter @ SethAFitzgerald and via email at thedrugclassroom@ gmail.com.

Contents

Medical uses

Dimenhydrinate is primarily used to treat nausea, vomiting, and dizziness caused by motion sickness.[2] 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.[3]

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[who?] 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.[citation needed]

Recreational use

Dimenhydrinate is recreationally used as a deliriant.[4][5][6] Slang terms for Dramamine used this way include "drama", "dime", "dime tabs", "D-Q", "substance D", "d-house", and "drams".[7] 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.[8]

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.[5] 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.[9] 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.[citation needed]

Brand names

Dimenhydrinate is marketed under many brand names: in the USA, Mexico and Serbia as Dramamine, in Ukraine as Driminate, in India and Canada 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 Ecuador as Anautin, in Hungary as Daedalon, in Sweden as Calma or Arlevert,[10] in Indonesia as Antimo, in Italy as Xamamina or Valontan, in Peru as Gravicoll, in Poland and Slovakia as Aviomarin,[11] in Portugal as Viabom, in Spain as Biodramina, in Thailand as ไดเมนนีน (Daimenin), in Israel as Travamin,in Pakistan as Gravinate,and in Ethiopia as dimenhydrinate.[12]

References

  1. ^ Putra OD, Yoshida T, Umeda D, Higashi K, Uekusa H, Yonemochi E (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.
  2. ^ "Dimenhydrinate". MedlinePlus. National Institutes of Health. Retrieved 19 July 2014.
  3. ^ "Dimenhydrinate injection, solution". Daily Med. U.S. National Library of Medicine. Retrieved 19 July 2014.
  4. ^ "The Health Risks of Abusing Motion sickness pills". Narconon International. Retrieved 2016-09-13.
  5. ^ a b 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.
  6. ^ Gardner DM, Kutcher S (March 1993). "Dimenhydrinate abuse among adolescents". Canadian Journal of Psychiatry. Revue Canadienne De Psychiatrie. 38 (2): 113–6. PMID 8467436.
  7. ^ "The Dangers of Dimenhydrinate Abuse". Bright Hub. Retrieved 2016-09-13.
  8. ^ "Dramamine". Grasscity forums. Retrieved 2016-09-13.
  9. ^ "Are Teens Abusing Motion Sickness Pills? - Muir Wood Adolescent and Family Services". Retrieved 2016-09-13.
  10. ^ "Dimenhydrinat" (in Swedish). Fass-verksamheten.
  11. ^ "Aviomarin, tabletki, 50 mg, 5 szt". Dox.pl (in Polish).
  12. ^ "Gravinate [Dimenhydrinate]". Karachi Pakistan: The Searle Company Ltd. Archived from the original on 5 May 2013.

External links

This page was last edited on 4 November 2018, at 09:56
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