Dimenhydrinate
Dimenhydrinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Dimehydrinate was first described in the literature in 1949, and patented in 1950. Early research into dimenhydrinate focused on its role as an antihistamine for urticaria; the treatment of motion sickness was an accidental discovery.
Dimenhydrinate, also known as B-dimethylaminoethyl benzohydrol ether 8-chlorotheophyllinate, is indicated to prevent nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate is a combination of Diphenhydramine and 8-chlorotheophylline in a salt form, with 53%-55.5% dried diphenhydramine, and 44%-47% died 8-chlorotheophylline.
The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade.
| Trade Name | Dimenhydrinate |
| Availability | Rx and/or OTC |
| Generic | Dimenhydrinate |
| Dimenhydrinate Other Names | Dimenhidrinato, Dimenhydrinate, Dimenhydrinatum, Diphenhydramine theoclate |
| Related Drugs | hydroxyzine, lorazepam, ondansetron, Zofran, meclizine, promethazine, diphenhydramine, Benadryl, Phenergan, scopolamine |
| Type | |
| Formula | C24H28ClN5O3 |
| Weight | Average: 469.97 Monoisotopic: 469.1880675 |
| Protein binding | Dimenhydrinate is 70-85% protein bound in plasma. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Canada |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Dimenhydrinate is a medication used to prevent and treat nausea, vomiting, vertigo, and motion sickness.
Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.
Dimenhydrinate is also used to associated treatment for these conditions: Dizziness, Labyrinthine disorder, Menière's Disease, Morning Sickness, Motion Sickness, Nausea, Nausea and vomiting, Post Operative Nausea and Vomiting (PONV), Vomiting, Radiation therapy induced nausea and vomiting
How Dimenhydrinate works
Dimenhydrinate is a theoclate salt that separates into diphenhydramine and 8-chlorotheophylline. While the exact mechanism of action is unknown, diphenhydramine is theorized to reduce disturbances to equilibrium through antimuscarinic effects or histamine H1 antagonism. 8-chlorotheophylline may produce excitation through blocking adenosine receptors, reducing the drowsiness produced by diphenhydramine.
Toxicity
Infants and children experiencing an overdose may lead to hallucinations, convulsions, or death. Adults experiencing an overdose may present with drowsiness, convulsions, coma, or respiratory depression. Treat overdoses with symptomatic and supportive measures including mechanically assisted ventilation.
In mice the oral LD50 is 203 mg/kg, while in rats it is 1320 mg/kg. The intraperitoneal LD50 in mice is 149 mg/kg.
Food Interaction
- Avoid alcohol.
Dimenhydrinate Alcohol interaction
[Moderate] GENERALLY AVOID:
Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.
In addition, the potential for abuse may be increased with the combination.
The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.
No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.
However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.
Alcohol should generally be avoided during therapy with anticholinergic agents.
Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.
Dimenhydrinate Drug Interaction
Moderate: lorazepam, lorazepam, diphenhydramine, diphenhydramine, pregabalin, pregabalin, acetaminophen / codeine, acetaminophen / codeineUnknown: aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Dimenhydrinate Disease Interaction
Major: prematurityModerate: anticholinergic effects, asthma/COPD, cardiovascular, renal/liver disease
Volume of Distribution
The volume of distribution of dimenhydrinate is 3-4 L/kg.
Elimination Route
A 50 mg oral film coated tablet reaches a Cmax of 72.6 ng/mL with a Tmax of 2.7 hours. A 100 mg suppository reaches a Cmax of 112.2 ng/mL with a Tmax of 5.3 hours.
Half Life
The plasma elimination half life of dimenhydrinate is 5-8 hours.
Elimination Route
Dimenhydrinate is predominantly eliminated in the urine. 1-3% of the dissociated diphenhydramine is eliminated in the urine unchanged, while 64% of diphenhydramine is eliminated in the urine as metabolites. The elimination of dimenhydrinate has not been fully studied.
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