Broncaire Expectorant

Salbutamol sulfate: (C₁₃H₂₁NO₃)₂ H₂SO₄.
Di[(RS)-2-(1,1-dimethyl)ethylamino-1-[4-hydroxy-3- (hydroxymethyl)phenyl]ethanol] sulfate.
Characteristics: a white or almost white, crystalline powder, freely soluble in water, slightly soluble in alcohol and in ether, very slightly soluble in methylene chloride.
Guaifenesin: C₁₀H₁₄O₄.
1,2 Propanediol,3, (2-methoxyphenoxy).
Characteristics: white to slightly gray crystalline powder with a bitter taste; may have a slight characteristic odor; stable in light and heat and is non-hygroscopic; melts in range of 3° between 78° and 82°; pH (1 in 100 solution) between 5 and 7.
Solubility: 1 g in 60 to 70 mL water; soluble in alcohol, chloroform, glycerin and propylene glycol. Insoluble in petroleum ether.
Excipients/Inactive Ingredients: Sodium citrate dihydrate, purified water, citric acid monohydrate, sucrose, saccharin sodium, sorbitol solution 70%, menthol, propylparaben, glycerin, methylparaben, propylene glycol.

Pharmacology: Pharmacodynamics: Salbutamol: Salbutamol is a beta 2 adrenergic stimulant which has highly selective action on the receptors in the bronchial muscles, leading to bronchodilation. It has little or no action on the cardiac receptors.
Guaifenesin: Oral administration of guaifenesin facilitates expectoration by reducing mucus viscosity.
Pharmacokinetics: Salbutamol: Salbutamol is readily absorbed from the gastrointestinal tract. It is subject to first pass metabolism in the liver and possibly in the gut wall: The main metabolism is an inactive sulfate conjugate. It is rapidly excreted in the urine as metabolized and unchanged drug; there is some excretion in the faeces. It does not appear to be metabolized in the lung, therefore its ultimate metabolism and excretion following inhalation depends upon the delivery method used, which determines the proportion of inhaled salbutamol relative to the proportion inadvertently swallowed. It has been suggested that the majority of an inhaled dose is swallowed and absorbed from the gut.
The plasma half-life of salbutamol has been estimated to range from 4 to 6 hours.
Guaifenesin: Guaifenesin is absorbed from the gastrointestinal tract. It is metabolized then excreted in the urine.

Expectoration and the relief of bronchospasm in bronchitis, pneumonia, influenza and other acute respiratory tract infections. It is also useful in relieving cough and for treating bronchospasm in patients with coexisting cardiac disease or hypertension.

Adults and children over 12 years: 2-3 teaspoonful 2 to 3 times daily.
Children (6 to 12 years): 1-2 teaspoonful 2 to 3 times daily.
Children (up to 12 years): 1 teaspoonful 2 to 3 times daily.

The preferred antidote for overdosage with salbutamol is a cardioselective betablocking agent, but beta blocking drugs should be used with caution in patients with a history of bronchospasm.

It is contraindicated in patients with a history of hypersensitivity to any of its components. Although salbutamol is used in the management of uncomplicated premature labor, salbutamol preparations should not be used for threatened abortion during the first and second trimesters of pregnancy.

As with any other drug, avoid its use during the 1^st trimester of pregnancy. Salbutamol and other beta agonist should be given with caution in hyperthyroidism, myocardial insufficiency, arrhythmias, susceptible to QT-interval prolongation, hypertension and diabetes mellitus.

As with any other drug, avoid its use during the 1^st trimester of pregnancy.

The only side effect of significance with oral salbutamol is a fine tremor of skeletal muscle which occurs in some patients; usually the hands are most obviously affected. This effect is dose related and is common to all beta-adrenergic stimulants.
A few patients feel tense; this is also due to the effects on skeletal muscle and not to direct CNS stimulation.
With doses higher than those recommended or in patients who are usually sensitive to beta-adrenergic stimulants, peripheral vasodilation and a compensatory small increase in heart rate may occur.
Occasional headaches have been reported.
Salbutamol does not cause difficulty in micturition because unlike sympathomimetic drugs e.g. ephedrine, it does not stimulate alpha adrenoreceptors. Adverse effects associated with guaifenesin are rare.

Store at temperatures not exceeding 25°C.
Shelf-life: 30 months.

Antiasthmatic & COPD Preparations

R05CA10 - combinations ; Belongs to the class of expectorants. Used in the treatment of wet cough.

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