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ACTIFED EXPECTORANT

Product Information

Registration Status: Active

SIN03436P

ACTIFED EXPECTORANT is approved to be sold in Singapore with effective from 1989-06-17. It is marketed by GSK CONSUMER HEALTHCARE SINGAPORE PTE LTD, with the registration number of SIN03436P.

This product contains Guaiphenesin 100mg/5ml,Pseudoephedrine 30mg/5ml, and Triprolidine 1.25mg/5ml in the form of SYRUP. It is approved for ORAL use.

This product is manufactured by Aspen Bad Oldesloe GmbH in GERMANY.

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

Product Reference
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Description

An expectorant that also has some muscle relaxing action. It is used in many cough preparations. [PubChem]

Indication

Used to assist the expectoration of phlegm from the airways in acute respiratory tract infections.

Mechanism of Action

Guaifenesin may act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that cause glandular exocytosis of a less viscous mucus mixture. Cough may be provoked. This combination may flush tenacious, congealed mucopurulent material from obstructed small airways and lead to a temporary improvement in dyspnea or the work of breathing.

Pharmacokinetics

Absorption
Rapidly absorbed from the GI tract
Distribution
Metabolism
Rapidly hydrolyzed (60% within seven hours) and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary metabolite.
Elimination

Toxicity

LD50 1510 mg/kg (rat, oral)

Active Ingredient/Synonyms

Glyceryl guaiacolate | guaiphenesin | Hustosil | Guaifenesin |


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

For the treatment of nasal congestion, sinus congestion, Eustachian tube congestion, and vasomotor rhinitis, and as an adjunct to other agents in the optimum treatment of allergic rhinitis, croup, sinusitis, otitis media, and tracheobronchitis. Also used as first-line therapy of priapism.

Mechanism of Action

Pseudoephedrine acts directly on both alpha- and, to a lesser degree, beta-adrenergic receptors. Through direct action on alpha-adrenergic receptors in the mucosa of the respiratory tract, pseudoephedrine produces vasoconstriction. Pseudoephedrine relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors. Like ephedrine, pseudoephedrine releasing norepinephrine from its storage sites, an indirect effect. This is its main and direct mechanism of action. The displaced noradrenaline is released into the neuronal synapse where it is free to activate the postsynaptic adrenergic receptors.

Pharmacokinetics

Absorption
Pseudoephedrine is readily and almost completely absorbed from the GI tract and there is no evidence of first-pass metabolism.
Distribution
Metabolism
Hepatic.
Elimination

Toxicity

Common adverse reactions include nervousness, restlessness, and insomnia. Rare adverse reactions include difficult/painful urination, dizziness/lightheadedness, heart palpitations, headache, increased sweating, nausea/vomiting, trembling, troubled breathing, unusual paleness, and weakness.

Active Ingredient/Synonyms

(+) threo-2-(methylamino)-1-phenyl-1-propanol | (+)-(1S,2S)-Pseudoephedrine | (+)-Pseudoephedrine | (+)-psi-Ephedrine | (+)-threo-Ephedrine | d-Isoephedrine | d-Pseudoephedrine | d-psi-2-Methylamino-1-phenyl-1-propanol | d-psi-Ephedrine | Isoephedrine | L-(+)-Pseudoephedrine | L(+)-psi-Ephedrine | Pseudoefedrina | pseudoéphédrine | Pseudoephedrine D-form | Pseudoephedrinum | Psi-ephedrin | Psi-ephedrine | trans-Ephedrine | ψ-ephedrine | Pseudoephedrine |


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

First generation histamine H1 antagonist used in allergic rhinitis; asthma; and urticaria. It is a component of cough and cold medicines. It may cause drowsiness.

Indication

For the symptomatic relief of seasonal or perennial allergic rhinitis or nonallergic rhinitis; allergic conjunctivitis; and mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Also used in combination with other agents for the symptomatic relief of symptoms associated with the common cold.

Mechanism of Action

Triprolidine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.

Pharmacokinetics

Absorption
Rapidly absorbed in the intestinal tract.
Distribution
Metabolism
Elimination

Toxicity

Symptoms of overdose include drowsiness, weakness, inco-ordination, difficulty with micturition, respiratory depression, hypotension, agitation, irritability, convulsions, hypertension, palpitation and tachycardia.

Active Ingredient/Synonyms

Tripolidina | Triprolidin | Triprolidine | Triprolidinum | Triprolidine |


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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