Buy Dimenhydrinate (diphenhydramine) Cas 523-87-5

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.^[3]

Dimenhydrinate was introduced to the market by G.D. Searle in 1949.^[4][5]

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.^[3]

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.^[6][7][8] 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.^[9][10]

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)^[11] 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.^[12]

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

Dimenhydrinate is recreationally used as a deliriant.^[13][14][15] Slang terms for Dramamine used this way include “drama”, “dime”, “dime tabs”, “D-Q”, “substance D”, “d-house”, and “drams”.^[16] Abusing Dramamine is sometimes referred to as Dramatizing or “going a dime a dozen”, a reference to the number of Dramamine tablets generally necessary for a recreational dose. ^[17]

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.^[14]

Other CNS effects occur within the limbic system and hippocampus, causing confusion and temporary amnesia due to decreased acetylcholine signaling. Toxicity 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.^[18] 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.^[19]