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DIPRODIN ELIXIR

Product Information

Registration Status: Active

SIN07830P

DIPRODIN ELIXIR is approved to be sold in Singapore with effective from 1994-01-09. It is marketed by KOTRA PHARMA MARKETING, with the registration number of SIN07830P.

This product contains Diphenhydramine 12.5mg/5ml, and Ephedrine 6mg/5ml in the form of ELIXIR. It is approved for ORAL use.

This product is manufactured by KOTRA PHARMA (M) SDN BHD in MALAYSIA.

It is a Pharmacy Only Medicine that can be obtained from a pharmacist at a retail pharmacy.

Product Reference
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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.


Description

An alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.

Indication

Ephedrine commonly used as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia.

Mechanism of Action

Ephedrine is a sympathomimetic amine - that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system. Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine. The ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell. Ephedrine's action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent, serotonin by the same mechanism is presumed to have a major role in its mechanism of action.

Pharmacokinetics

Absorption
85%
Distribution
Metabolism
Elimination

Toxicity

Cardiovascular: tachycardia, cardiac arrhythmias, angina pectoris, vasoconstriction with hypertension

Active Ingredient/Synonyms

(-)-Ephedrine | (1R,2S)-1-Phenyl-1-hydroxy-2-methylaminopropane | L-Ephedrine | L-erythro-2-(Methylamino)-1-phenylpropan-1-ol | L(−)-ephedrine | Ephedrine |


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.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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