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Dimenhydrinate
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Dimenhydrinate
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.
Dimenhydrinate was introduced to the market by G.D. Searle in 1949.
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.
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. 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.
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) 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.
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.
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 number of Dramamine tablets generally necessary for a recreational dose.
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.
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Dimenhydrinate
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.
Dimenhydrinate was introduced to the market by G.D. Searle in 1949.
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.
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. 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.
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) 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.
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.
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 number of Dramamine tablets generally necessary for a recreational dose.
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.
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