2 mg salbutamol, as sulfate, and 100 mg guaifenesin in each 10 mL of syrup.
Excipients/Inactive Ingredients: Lactic acid, Hydroxypropylmethyl cellulose, Sodium benzoate, Orange flavour liquid, Saccharine sodium dehydrate, Sodium hydroxide, Purified water.
Pharmacology: Pharmacodynamics: Mechanism of Action: Salbutamol is a selective beta2-adrenoceptor agonist. At therapeutic doses it acts on the beta2-adrenoceptors of bronchial muscle.
Guaifenesin can make the viscous mucus of the respiratory pathway more fluid and therefore facilitates expectoration and reduces cough.
Pharmacodynamic Effects: Salbutamol is a selective beta2-adrenoceptor agonist. At therapeutic doses it acts on the beta2-adrenoceptors of bronchial muscle providing short-acting (4 to 6 hour) bronchodilation in reversible airways obstruction.
Pharmacokinetics: Absorption: After oral administration, salbutamol is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism to the phenolic sulfate. Both unchanged drug and conjugate are excreted primarily in the urine.
Guaifenesin is well-absorbed after oral administration. After the administration of 600 mg guaifenesin in healthy adult volunteers the Cmax was approx 1.4 micrograms/mL with Tmax about 15 minutes after drug administration.
Distribution: The bioavailability of orally administered salbutamol is about 50%. Salbutamol is bound to plasma proteins to the extent of 10%.
Metabolism: Salbutamol administered intravenously has a half-life of 4 to 6 hours and is cleared partly renally and partly by metabolism to the inactive 4'-O-sulfate (phenolic sulfate) which is also excreted primarily in the urine.
Guaifenesin has a plasma half-life of approx 1 hour and was not detectable in the blood after 8 hours. Guaifenesin appears to undergo both oxidation and demethylation.
Elimination: The majority of a dose of salbutamol given intravenously, orally or by inhalation is excreted within 72 hours. The faeces are a minor route of excretion.
Guaifenesin is excreted in urine.
Toxicology: Non-clinical Information: In common with other potent selective beta2-receptor agonists, salbutamol has been shown to be teratogenic in mice when given subcutaneously. In a reproductive study, 9.3% of foetuses were found to have cleft palate, at 2.5 mg/kg, 4 times the maximum human oral dose. In rats, treatment at the levels of 0.5, 2.32, 10.75 and 50 mg/kg/day orally throughout pregnancy resulted in no significant foetal abnormalities. The only toxic effect was an increase in neonatal mortality at the highest dose level as the result of lack of maternal care. A reproductive study in rabbits revealed cranial malformations in 37% of foetuses at 50 mg/kg/day, 78 times the maximum human oral dose.
In an oral fertility and general reproductive performance study in rats at doses of 2 and 50 mg/kg/day, with the exception of a reduction in number of weanlings surviving to day 21 post partum at 50 mg/kg/day, there were no adverse effects on fertility, embryofetal development, litter size, birth weight or growth rate.
Animal studies on guaifenesin to assess carcinogenicity, genotoxicity, or effects on fertility or embryo-fetal development have not been performed.
Salbutamol is a selective beta2-adrenoceptor agonist. At therapeutic doses it acts on the beta2-adrenoceptors of bronchial muscle, with little or no action on the beta1-adrenoceptors of the heart. The combination of salbutamol with guaifenesin is designed to relieve respiratory obstruction and improve pulmonary ventilation.
Bronchodilators should not be the only or main treatment in patients with severe or unstable asthma. Severe asthma requires regular medical assessment as death may occur. Patients with severe asthma have constant symptoms and frequent exacerbations, with limited physical capacity, and PEF values below 60% predicted at baseline with greater than 30% variability, usually not returning entirely to normal after a bronchodilator. These patients will require high dose inhaled (e.g. greater than 1 mg/day beclometasone dipropionate) or oral corticosteroid therapy. Sudden worsening of symptoms may require increased corticosteroid dosage which should be administered under urgent medical supervision.
Respiratory disorders where bronchospasm and excessive secretion of tenacious mucus are complicating factors, e.g. bronchial asthma, chronic bronchitis and emphysema.
Salbutamol has a duration of action of 4 to 6 hours in most patients.
Increasing use of beta2-agonist may be a sign of worsening asthma. Under these conditions a reassessment of the patient's therapy plan may be required and concomitant glucocorticosteroid therapy should be considered.
As there may be adverse effects associated with excessive dosing, the dosage or frequency of administration should only be increased on medical advice.
Populations: The volumes of syrup quoted are based on a formulation strength of 2 mg salbutamol per 10 mL of syrup.
Adults: 10 to 20 mL of expectorant syrup (2 to 4 mg salbutamol) 2 or 3 times a day.
Children: 2 to 6 years: 5 to 10 mL of expectorant syrup (1 to 2 mg salbutamol) 2 or 3 times daily.
6 to 12 years: 10 mL of expectorant syrup (2 mg salbutamol) 2 or 3 times daily.
Over 12 years: 10 to 20 mL of expectorant syrup (2 to 4 mg salbutamol) 2 or 3 times daily.
The most common signs and symptoms of overdose with salbutamol are transient beta-agonist pharmacologically mediated events (see Precautions and Adverse Reactions).
Hypokalaemia may occur following overdose with salbutamol. Serum potassium levels should be monitored.
Lactic acidosis has been reported in association with high therapeutic doses as well as overdoses of short-acting beta-agonist therapy, therefore monitoring for elevated serum lactate and consequent metabolic acidosis (particularly if there is persistence or worsening of tachypnea despite resolution of other signs of bronchospasm such as wheezing) may be indicated in the setting of overdose.
Very large doses of guaifenesin cause nausea and vomiting.
Treatment: Further management should be as clinically indicated or as recommended by the national poisons centre, where available.
Salbutamol and guaifenesin expectorant syrup is contraindicated in patients with a history of hypersensitivity to any ingredient of the preparation.
Non-i.v. formulations of salbutamol must not be used to arrest uncomplicated premature labour or threatened abortion.
The management of asthma should normally follow a stepwise programme, and patient response should be monitored clinically and by lung function tests.
Increasing use of short-acting inhaled beta2-agonist to control symptoms indicates deterioration of asthma control. Under these conditions, the patient's therapy plan should be reassessed.
Sudden and progressive deterioration in asthma control is potentially life-threatening and consideration should be given to starting or increasing corticosteroid therapy. In patients considered at risk, daily peak flow monitoring may be instituted.
Patients should be warned that if either the usual relief is diminished or the usual duration of action reduced, they should not increase the dose or its frequency of administration, but to seek medical advice.
Salbutamol should be administered cautiously to patients with thyrotoxicosis.
Potentially serious hypokalaemia may result from beta2-agonist therapy mainly from parenteral or nebulised administration. Particular caution is advised in acute severe asthma as this effect may be potentiated by concomitant treatment with xanthine derivatives, steroids, diuretics and by hypoxia. It is recommended that serum potassium levels are monitored in such situations.
In common with other beta-adrenoceptor agonists, salbutamol and guaifenesin can induce reversible metabolic changes, for example increased blood sugar levels. The diabetic patient may be unable to compensate for this and the development of ketoacidosis has been reported. Concurrent administration of corticosteroids can exaggerate this effect.
Long term treatment with salbutamol and guaifenesin expectorant syrup (sugar containing formulation) increases the risk of dental caries. It is important that adequate dental hygiene is maintained.
Ability to Perform Task that Require Judgement, Motor or Cognitive Skills: None reported.
Fertility: There is no information on the effects of salbutamol on human fertility. There were no adverse effects on fertility in animals (see Toxicology: Non-Clinical Information under Actions). There is no information on the effects of guaifenesin on human fertility.
Pregnancy: Administration of drugs during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus.
During worldwide marketing experience, rare cases of various congenital anomalies, including cleft palate and limb defects have been reported in the offspring of patients being treated with salbutamol. Some of the mothers were taking multiple medications during their pregnancies. Because no consistent pattern of defects can be discerned, and baseline rate for congenital anomalies is 2 to 3%, a relationship with salbutamol use cannot be established.
The safety of guaifenesin during pregnancy has not been established.
Lactation: As salbutamol is probably secreted in breast milk its use in nursing mother is not recommended unless the expected benefits outweigh any potential risk.
It is not known whether salbutamol in breast milk has a harmful effect on the neonate.
As the combination product contains salbutamol and guaifenesin, the type and severity of adverse reactions associated with each of the components may be expected. The adverse reaction profile is derived from the individual components since there are limited clinical and post marketing reports available for the combination product.
Adverse reactions are listed as follows by system organ class and frequency. Frequencies are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000) and very rare (<1/10,000) including isolated reports. Very common and common reactions were generally determined from clinical trial data. Rare and very rare reactions were generally determined from spontaneous data.
Salbutamol: Immune system disorders: Very rare: Hypersensitivity reactions including angioedema, urticaria, bronchospasm, hypotension and collapse.
Metabolism and nutrition disorders: Rare: Hypokalaemia.
Potentially serious hypokalaemia may result from beta
2-agonist therapy.
Nervous system disorders: Very common: Tremor. Common: Headache. Very rare: Hyperactivity.
Cardiac disorders: Common: Tachycardia, palpitations. Rare: Cardiac arrhythmias including atrial fibrillation, supraventricular tachycardia and extrasystoles.
Vascular disorders: Rare: Peripheral vasodilatation.
Musculoskeletal and connective tissue disorders: Common: Muscle cramps. Very rare: Feeling of muscle tension.
Guaifenesin: Immune system disorders: Unknown: Hypersensitivity and allergic reactions including anaphylactic reactions, angioedema, rash, urticaria and dyspnoea.
Gastrointestinal disorders: Unknown: Nausea, vomiting, abdominal discomfort.
Salbutamol and non-selective beta-blocking drugs, such as propranolol, should not usually be prescribed together.
Salbutamol is not contraindicated in patients under treatment with monoamine oxidase inhibitors (MAOIs).
Instructions for Use/Handling: Dilution: Salbutamol and guaifenesin expectorant syrup may be diluted with purified water BP. The resulting mixture should be protected from light and used within 28 days.
A 50% v/v dilution of salbutamol and guaifenesin expectorant syrup has been shown to be adequately preserved against microbial contamination. However, to avoid the possibility of introducing excessive microbial contamination, the purified water BP used for dilution should be recently prepared or alternatively it should be boiled and cooled immediately before use.
Incompatibilities: Dilution of salbutamol and guaifenesin expectorant syrup with syrup BP or sorbitol solution is not recommended as this may result in precipitation of the cellulose thickening agent.
A mixture of salbutamol and guaifenesin expectorant syrup with other liquid preparations is not recommended.
Store below 30°C.
Protect from light.
R05CA10 - combinations ; Belongs to the class of expectorants. Used in the treatment of wet cough.
Ventolin Expectorant syr
100 mL x 1's
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