Product Information
Registration Status: ActivePAXIDORM TABLET 25mg is approved to be sold in Singapore with effective from 1999-01-04. It is marketed by POLYMEDIC TRADING ENTERPRISE PTE LTD, with the registration number of SIN10851P.
This product contains Diphenhydramine 25mg in the form of TABLET, SUGAR-COATED. It is approved for ORAL use.
This product is manufactured by PHARMASERVE LTD in UNITED KINGDOM.
It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.
Description
Dimenhydrinate, also known as Dramamine or Gravol, is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness. Dimenhydrinate is a combination drug composed of [DB01075] and [DB14132] in a salt form, with 53%-55.5% of diphenhydramine, and not less than 44%-47% of 8-chlorotheophylline, calculated on the dried basis. The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular system [A1540] while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade [A33889]. The addition of 8-chlorotheophylline was initially intended to counteract the sedative effects of diphenhydramine. When used in large doses, dimenhydrinate has been shown to cause a "high" characterized by hallucinations, excitement, incoordination, and disorientation [A1539].
Indication
Dimenhydrinate is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.
Mechanism of Action
The mechanism by which some antihistamines exert their antiemetic, anti-motion sickness, and anti-vertigo effects is not precisely known but may be related to their central anticholinergic actions. They diminish vestibular stimulation and depress labyrinthine function. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Dimenhydrinate is a competitive antagonist at the histamine H1 receptor, which is widely distributed in the human brain. Dimenhydrinate's anti-emetic effect is probably due to H1 antagonism in the vestibular system in the brain.
Pharmacokinetics
- Absorption
- Well absorbed after oral administration.
- Distribution
- Metabolism
- Hepatic (cytochrome P-450 system).
- Elimination
Toxicity
Symptoms of overdose include delerium, hallucinations, and excitment. Patients may be violent and confused.
Active Ingredient/Synonyms
(O-Benzhydryl(dimethylamino)ethanol) 8-chlorotheophyllinate | 8-chloro-1,3-Dimethyl-3,7-dihydro-1H-purine-2,6-dione - 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1) | Benzhydryl-beta-dimethylaminoethylether 8-chlorotheophylline | beta-Dimethylaminoethyl benzhydryl ether 1,3-dimethyl-8-chloroxanthine | Dimenhidrinato | Dimenhydrinatum | Diphenhydramine 8-chlorotheophyllinate | Diphenhydramine 8-chlorotheophylline | Diphenhydramine theoclate | Diphenhydrinate | N,N-Dimethyl-2-diphenylmethoxyethylamine 8-chlorotheophyllinate | O-Benzhydryldimethylaminoethanol 8-chlorotheophyllinate | Dimenhydrinate |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.