Salbutamol Injection B.P.

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0.500 mg/ml, 5 mg/5 ml

For the use of a Registered Medical Practitioner or a Hospital or a Institution only.

BRONCHODILATOR

Reversible bronchospasm associated with asthma

Adjunctive treatment of hyperkalaemia in patients undergoing dialysis

DESCRIPTION:

SALBUTAMOL INJECTION (Salbutamol) is used as bronchodilator in the management of asthma and chronic obstructive pulmonary disease. Chemically, Salbutamol sulphate is bis [(1RS-2-[1,1-dimethylethyl)amino]-1-4-hydroxy-3-ydroxymethyl)phenyl]ethanol]sulphate.The
molecular formula is (C₁₃H₂₁NO₃)2H₂SO₄ and molecular weight is 576.7.

STRUCTURAL FORMULA :
Its structural formula is :

Salbutamol Injection B.P.

DESCRIPTION OF INJECTION:

SALBUTAMOL INJECTION is a colourless or very pale yellow solution filled in amber ampoule of suitable size.

COMPOSITION :
Each ml contains :
Salbutamol Sulphate B.P.
equivalent to Salbutamol 0.500 mg
Water for Injections B.P. q.s.

ACTIONS :
Salbutamol is a bronchodilator act by stimulating Beta2 – adrenergic receptors in the lungs to relax bronchial smooth muscle, thereby relieving bronchospasm. This action is believed to result from increased production of cyclic adenosine 3,5-monophosphate (cyclic 3,5 –AMP ; cAMP and ensuing reduction in intracellular calcium concentration caused by activation of the enzyme adenylate cyclase that catalyzes the conversion of adenosine triphosphate (ATP) to cAMP. Increased cAMP concentrations, in addition to relaxing bronchial smooth muscle, inhibit release of mediators of immediate hypersensitivity from cells, especially from mast cells.

PHARMACOKINETICS :
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 within 72 hours. Salbutamol is bound to plasma protein to the extent of 10 %

INDICATIONS :
SALBUTAMOL INJECTION is used for the prevention and treatment of reversible bronchospasm associated with asthma and other obstructive pulmonary diseases. Adjunctive treatment of hyperkalaemia in patients undergoing dialysis.

DOSAGE AND ADMINISTRATION:

Administration :

SALBUTAMOL INJECTION administered by the subcutaneous, intramuscular or intravenous route, under the direction of physician.

INSTRUCTION FOR USE OF AMPOULE :

The ampoule used in this product is equipped with O.P.C (One Point Cut) opening system. No ampoule file is needed to open the ampoule. The neck of the ampoule is prescored at the point of constriction. A coloured dot on the ampoule head helps to orientate the ampoule. Take the ampoule and face the coloured dot. Let the solution at the head of the ampoule to flow down by shaking or a gentle stroke. The ampoule opens easily by placing the thumb on the coloured dot and gently pressing downwards as shown.

Ampoules equipped with One Point Cut (OPC) technology

Dosage :

Adults :

Subcutaneous route : 500 micrograms (8 micrograms/kg body weight) and repeated every four hours has required. Intramuscular route : 500 micrograms (8 micrograms/kg body weight) and repeated every four hours has required.

Slow Intravenous injection :

250 micrograms (4 micrograms/kg body weight) injected slowly. If necessary the dose may be repeated. The use of SALBUTAMOL INJECTION 500 micrograms in 1 ml (500 micrograms/ml) for intravenous administration may be facilitated by dilution to 10 ml with Water for Injections B.P. (final concentration of 50 micrograms/ml) and 5 ml of the diluted preparation (250 micrograms/5 ml) administered by slow intravenous injection.

Children :

At present there are insufficient data to recommend a dosage regimen for routine use.

CONTRAINDICATIONS :

Although intravenous Salbutamol, and occasionally Salbutamol tablets, are used in the management of premature labour uncomplicated by conditions such as placenta praevia, antepartum haemorrhage or toxaemia of pregnancy, Salbutamol preparations should not be

used for threatened abortion. LBUTAMOL INJECTION is contraindicated in patients with a history of hypersensitivity to any of the components.

WARNINGS AND PRECAUTIONS :

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 agonists 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. The use of SALBUTAMOL INJECTION parenteral preparations in the treatment of severe bronchospasm or status asthmaticus does not obviate the requirement for glucocorticoid steroid therapy as appropriate. When practicable, administration of oxygen concurrently with parenteral SALBUTAMOL INJECTION is recommended, particularly when it is given by patients. In common with other Beta2 adrenoceptor agonists, SALBUTAMOL INJECTION can induce reversible metabolic

changes such as reversible hypocalcaemia and increased blood glucose 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.

Potentially serious hypocalcaemia may result from Beta2 agonist therapy mainly from parenteral and 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. Diabetic patients and those concurrently receivingcorticosteroids should be monitored frequently during intravenous infusion of SALBUTAMOL INJECTION so that remedial steps (e.g. an increase in insulin dosage) can be taken to counter any metabolic change occurring. For these patients SALBUTAMOL INJECTION for Intravenous Infusion should be diluted with Sodium Chloride Injection B.P. rather than Sodium Chloride and Dextrose Injection B.P. Lactic acidosis has been reported very rarely in association with high therapeutic doses of intravenous and nebulised short-acting beta-agonist therapy, mainly in patients being treated for an acute asthma exacerbation. Increase in lactate levels may lead to dyspnoea and compensatory hyperventilation, which could be misinterpreted as a sign of asthma treatment failure and lead to inappropriate intensification of short-acting beta-agonist treatment. The population at risk primarily includes patients with an acute exacerbation of the underlying respiratory disease undergoing high dose treatment regimens, particularly with intravenous and nebulised salbutamol. It is therefore recommended that patients are monitored for the development of elevated serum lactate and consequent metabolic acidosis in this setting. Salbutamol should be administered cautiously to patients with thyrotoxicosis.

As maternal pulmonary oedema and myocardial ischaemia have been reported during or following treatment of premature labour with Beta2 agonists, careful attention should be given to fluid balance and cardio-respiratory function, including ECG, should be monitored. If signs of pulmonary oedema or myocardial ischaemia develop, discontinuation of treatment should be considered. In the treatment of premature labourby intravenous infusion of Salbutamol increases in maternal heart rate of the order 20 to 50 beats per minute usually

accompany the infusion. The maternal pulse rate should be monitored and not normally allowed to exceed a steady rate of 140 beats per minute. Maternal blood pressure may fall slightly during the infusion ; the effect being greater on diastolic than on systolic pressure. Falls in diastolic pressure are usually within the range of 10 to 20 mmHg. The effect of infusion on foetal rate is less marked but increases of up to 20 beats per minute may occur. In the treatment of premature labour, before SALBUTAMOL INJECTION parenteral preparations are given to any patient with known heart disease, an adequate assessment of the patient’s cardiovascular status should be made by a physician experienced in cardiology.

PREGNANCY AND LACTATION:

Pregnancy :
Although adequate and well-controlled studies in pregnant women have not been done with inhaled adrenergic bronchodilators, Salbutamol, is used in pregnancy when any potential risk that may be associated with treatment is preferable to the risk of placental hypoxaemia from uncontrolled pulmonary disease. Extensive use of adrenergic bronchodilators during pregnancy has provided no evidence that the sympathomimetic class effects seen in animal studies are relevant to human use.

Nursing Mothers :
As salbutamol is probably secreted in breast milk its use in nursing mothers is not recommended unless the expected benefits outweigh any potential risk. In such situations the use of the inhaled route may be preferable although it is not known whether salbutamol has a harmful effect on the neonate.

Paediatric Use :
Use of Salbutamol, in children has not demonstrated paediatrics – specific problems that would limit their usefulness.

INTERACTIONS AND INCOMPATIBILITES :

Beta – Blockers : Severe bronchospasms may be produced in asthmatic patients taking Salbutamol.

Digoxin : Salbutamol may decrease serum digoxin levels.

Diuretics : ECG changes and hypocalcaemia associated with these diuretics may worsen with Salbutamol co administration.

SIDE EFFECTS :
ide effects are listed below by system organ class and frequency. Frequencies are defined as : very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1000 and <1/100), rare (≥ 1/10,000 and <1/1000) and very rare (<1/10,000) Including isolated reports. Very common and common events were generally etermined from clinical trial data. Rare and very rare events were generally determined from spontaneous data.

Immune system disorders
Very rare : Hypersensitivity reactions including angioedema, urticaria, bronchospasm, hypotension and collapse.

Metabolism and nutrition disorders
Rare : Hypocalcaemia. Potentially serious hypocalcaemia may result from beta2 agonist therapy.
Very rare : Lactic acidosis Lactic acidosis has been reported very rarely in patients receiving intravenous and nebulised Salbutamol therapy for the treatment of acute asthma exacerbation.

Nervous system disorders
Very common : Tremor.
Common : Headache.
Very rare : Hyperactivity.
Cardiac disorders
Very common : Tachycardia, palpitations.
Uncommon : Myocardial ischaemia
In the management of pre – term labour
Rare : Cardiac arrhythmias including atrial fibrillation, supraventricular tachycardia and extrasystoles.

Vascular disorders
Rare : Peripheral vasodilatation.
Respiratory, thoracic and mediastinal disorders
Uncommon : Pulmonary oedema.

In the management of pre-term labour, salbutamol Injection/ solution for infusion have uncommonly been associated with pulmonary oedema. Patients with predisposing factors including multiple pregnancies, fluid overload, maternal infection and pre-eclampsia may have an increased risk of developing pulmonary oedema.

Gastrointestinal disorders
Very rare : Nausea, vomiting In the management of premature labour, intravenous infusion of Salbutamol Injection has very rarely been associated with nausea and vomiting. Musculoskeletal and connective tissue disorders Common : Muscle cramps. Injury, poisoning and procedural complications Very rare : Slight pain or stinging on I.M. use of undiluted injection.

OVERDOSAGES AND TREATMENT OF OVERDOSAGES:
The most common signs and symptoms of overdose with salbutamol are transient beta agonist pharmacologically mediated events, including tachycardia, tremor, hyperactivity and metabolic effects including hypocalcaemia and lactic acidosis. Hypocalcaemia may occur following overdose with salbutamol. Serum potassium levels should be monitored. Nausea, vomiting and hyperglycaemia have been reported, predominantly in children and when salbutamol overdose has been taken via the oral route. Consideration should be given to discontinuation of treatment and appropriate symptomatic therapy such as cardio-selective beta-blocking agents in patients presenting with cardiac symptoms (e.g. tachycardia, palpitations). Beta-blocking drugs should be used with caution in patients with a history of bronchospasm.

PHARMACEUTICAL PRECAUTIONS :
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

STORAGE :
Store below 30ºC, protected from light.
Do not refrigerate.

SHELF LIFE :
24 months from the date of manufacture.

PRESENTATION :
SALBUTAMOL INJECTION contains Salbutamol Sulphate B.P. equivalent to Salbutamol 0.500 mg in 1 ml aqueous solution.
Such 10 Ampoules are packed in box.

Disclaimer : For the use of a Registered Medical Practitioner or a Hospital or a Institution only. Also it is not intended to be used by healthcare professionals or patients for the purpose of prescribing or administering these products. Questions regarding the complete and current content of product labeling / specification / presentation should be directed to SGPharma.