Salbutarnol
Guaiphenesin
1. TRADE NAME OF THE MEDICAL PRODUCT
Ventolin Expectorant
2. QUALITATIVE AND QUANTITATIVE COMPOSITlON
1 mg Salbutamol, as sulphate and 50 mg guaiphenesin in each 5 ml syrup.
3. PHARMACEUTICAL FORM
Syrup (Sugar Free)
4. CLINICAL PARTICULARS
4.1 Therapeutic Indentations
Salbutamol is a selective β2-adrenoceptor agonist. At therapeutic doses it acts on the β2-adrenoceptors of bronchial muscle with little or no action on the β1-adrenoceptors of the heart. The combination of salbutamol with guaiphenesin 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 exacerbation's, 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. ›1 mg/day beclomethasone 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.
4.2 Posology and Method of Administration
Salbutamol has a duration of action of 4 to 6 hours in most patients. Increasing use of β2-agonists may be a sign of worsening asthma. Under these conditions a reassessment of the patients 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.
Adults:
10-20 ml (2-4 teaspoonfuls) of expectorant syrup (2-4 milligram salbutamol) two or three times a day.
Children:
2 - 6 years: 5 - 10 ml (1 - 2 teaspoonfuls) of expectorant syrup (1 - 2 milligram salbutamol) two or three times daily.
6 - 12 years: 10 ml (2 teaspoonfuls) of expectorant syrup (2 milligram salbutamol) two or three times daily.
Over 12 years: 10 - 20 ml (2 - 4 teaspoonfuls) of expectorant syrup (2 - 4 milligram salbutamol) two or three times daily.
The volumes of syrup quoted are based on a formulation strength of 2 milligram salbutamol per 10 ml of syrup.
4.3 Contra Indications
Ventolin Expectorant Syrup is contra-indicated in patients with a history of hypersensitivity to any of its components.
Although intravenous salbutamol and occasionally salbutamol tablets are used in the management of premature labour uncomplicated by conditions such as placenta praevia, ante-partum haemorrhage or toxaemia of pregnancy, salbutamol presentations should not be used for threatened abortion.
4.4 Special Warnings and Special Precautions for Use
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 β2-agonists to control symptoms indicates deterioration of asthma control. Under these conditions, the patients therapy plan should be reassessed. Sudden and progressive deterioration in asthma control is potentially life-threatening and consideration should be given to starling 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 should seek medical advice.
Salbutamol should be administered cautiously to patients with thyrotoxicosis. Potentially serious hypokalaemia may result from β2-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 β-adrenoceptor agonists, Ventolin 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 ketacidosis has been reported. Concurrent administration of corticosteroids can exaggerate this effect.
Long term treatment with Ventolin Expectorant Syrup (Sugar-containing formulation) increases the risk of dental caries. It is important that adequate dental hygiene is maintained. Safety and effectiveness have not been established in children below 2 years of age.
4.5 Interaction with Other Medicinal Products and Other Forms of Interaction
Salbutamol and non-selective β-blocking drugs, such as propranolol should not usually be prescribed together. Salbutamol is not contraindicated in patients under treatment with monoamine oxidase inhibitors (MAOIs).
4.6 Use during Pregnancy and Lactation
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 2-3%, a relationship with salbutamol use cannot be established.
As salbutamol is probably secreted in breast milk its use in nursing mothers 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.
4.7 Effects on Ability to Drive and Use Machines
None reported.
4.8 Undesirable Effects
Ventolin Expectorant Syrup may cause is a fine tremor of skeletal muscle, usually the hands are most obviously affected. This effect is dose related and is common to all β-adrenergic stimulants.
A few patients experience a feeling of tension; this is also due to the effects on skeletal muscle and not to direct CNS stimulation. Occasionally headaches have been reported.
Peripheral vasodilatation and a compensatory small increase in heart rate may occur in some patients.
Hypersensitivity reactions including angioedema, urticaria, bronchospasm, hypotension and collapse have been reported very rarely. There have been very rare reports of muscle cramps.
Potentially serious hypokalaemia may result from β2-agonist therapy.
As with other β2-agonists hyperactivity has been reported rarely in children.
Side effects associated with guaiphenesin are rare.
Tachycardia may occur in some patients.
Cardiac arrhythmias (including atrial fibrillation, supraventricular tachycardia and extrasystoles) have been reported, usually in suspectible patients.
4.9 Overdose
The preferred antidote for overdosage with salbutamol is a cardio-selective β-blocking agent. However, β-blocking drugs should be used with caution in patients with a history of bronchospasm.
Hypokalaemia may Occur following overdose with salbutamol. Serum potassium, levels should be monitored.
5. PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamics Properties
Salbutamol is a selective β2-adrenoceptor agonist. At therapeutic doses it acts on the β2-adrenoceptors of bronchial muscle with little or no action on the β1-adrenoceptors of cardiac muscle.
Guaiphenesin can make the viscous mucus of the respiratory pathway more fluid and therefore facilitates expectoration and reduces cough.
5.2 Pharmacokinetic Properties
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-sulphate (phenolic sulphate) which is also excreted primarily in the urine. The faeces are a minor route of excretion. The majority of a dose of salbutamol given intravenously, orally or by inhalation is excreted with in 72 hours. Salbutamol is bound to plasma proteins to the extent of 10%. After oral administration, salbutamol is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism to the phenolic sulphate. Both unchanged drug and conjugate are excreted primarily in the urine. The bioavailability of orally administered salbutamol is about 50%.
5.3 Preclinical Safety Data
In common with other potent selective β2-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 2.5mg/kg, 4 times the maximum human oral dose. In rats, treatment at the levels of 0.5, 2.32, 10.75 and 50mg/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 levels as the result of lack of maternal care. A reproductive study in rabbits revealed cranial malformations in 37% of foetuses at 50mg/kg/day, 78 times the maximum human oral dose.
6 PHARMACEUTICAL PARTICULARS
6.1 Incompatibilities
Dilution of Ventolin Expectorant Syrup with Syrup BP or Sorbitol solution is not recommended as this may result in precipitation of the cellulose thickening agent. Admixture of Ventolin Expectorant Syrup with other liquid preparations is not recommended.
6.2 Shelf Life
18 Months
6.3 Special Precautions for Storage
Store at a temperature not exceeding 30°C
Protect from light.
6.4 Instructions for Use/ Handling
Dilution; -
Ventolin Expectorant Syrup may be diluted with unpreserved syrup BP. The resulting mixture should be protected from light and used within 28 days. A 50 % v/v dilution of Ventolin Expectorant syrup has bean shown to be adequately preserved against microbial contamination. However to avoid the possibility of introducing excessive contamination, the purified water used for dilution should be recently prepared or alternatively it should be boiled and cooled immediately before use.
HARUS DENGAN RESEP DOKTER
Ventolin Expectorant Syrup is supplied in :
| Bottles of 60 ml | Reg. No. DKL9332002437A1 |
| Bottles of 100 ml | Reg. No. DKL9332002437A1 |
| Bottles of 60 ml | Reg. No. DKE9532002437A1 |
| Bottles of 150 ml | Reg. No. DKE9532002437A1 |
| Bottles of 1000 ml | Reg. No. DKE9532002437A1 |
Manufactured by
PT. Glaxo Wellcome Indonesia
Jakarta, Indonesia
™ Ventolin is a trademark of the GlaxoSmithKline group of companies
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