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Each puff contains Salbutamol sulphate equivalent to Salbutamol 100 mcg.
Pharmacology: Pharmacodynamics: Mechanism of Action: Activation of beta 2-adrenergic receptors on airway smooth muscle leads to the activation of adenylcyclase and to an increase in the intracellular concentration of cyclic-3',5'-adenosine monophosphate (cyclic AMP). This increase of cyclic AMP leads to the activation of protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in relaxation. Salbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Salbutamol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor challenges. Increased cyclic AMP concentrations are also associated with the inhibition of release of mediators from mast cells in the airway.
Salbutamol is a selective beta2-adrenoceptor agonist. At therapeutic doses it acts on the beta 2-adrenoceptors of bronchial muscle providing short acting (4-6 hour) bronchodilatation with a fast onset (within 5 minutes) in reversible airways obstruction.
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.
After administration by the inhaled route between 10 and 20% of the dose reaches the lower airways. The remainder is retained in the delivery system or is deposited in the oropharynx from where it is swallowed. The fraction deposited in the airways is absorbed into the pulmonary tissues and circulation, but is not metabolised by the lung. On reaching the systemic circulation it becomes accessible to hepatic metabolism and is excreted, primarily in the urine, as unchanged drug and as the phenolic sulphate.
The swallowed portion of an inhaled dose 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. Most of a dose of salbutamol given intravenously, orally or by inhalation is excreted within 72 hours. Salbutamol is bound to plasma proteins to the extent of 10%.
Toxicology: Preclinical Safety Data: In common with other potent selective beta 2-agonists, salbutamol has been shown to be teratogenic in mice when given subcutaneously. In a reproductive study, 9.3% of fetuses were found to have cleft palate at 2.5mg/kg 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 fetal abnormalities. The only toxic effect was an increase in neonatal mortality at the highest dose level as the result of lack of maternal care. Reproductive studies in the rabbit at doses of 50mg/kg/day orally (i.e. much higher than the normal human dose) have shown fetuses with treatment related changes; these included open eyelids (ablepharia), secondary palate clefts (palatoschisis), changes in ossification of the frontal bones of the cranium (cranioschisis) and limb flexure. Reformulation of the Salbumol inhaler has not altered the known toxicological profile of salbutamol.
The non-CFC propellant, HFA 134a, has been shown to have no toxic effect at very high vapour concentrations, far in excess of those likely to be experienced by patients, in a wide range of animal species exposed daily for periods of two years.
For the relief and prevention of asthma symptoms in mild, moderate or severe asthma.
It should be used to relieve symptoms when they occur, and to prevent them in those circumstances recognised by the patient to precipitate an asthma attack (e.g. before exercise or unavoidable allergen exposure).
It provides short-acting (4 to 6 hours) bronchodilatation with fast onset (within 5 minutes) in reversible airways obstruction.
Aerotamol inhaler is for oral inhalation use only.
Adults (including the elderly): For the relief of acute asthma symptoms including bronchospasm, one inhalation (100 micrograms) may be administered as a single minimum starting dose. This may be increased to two inhalations if necessary. To prevent allergen- or exercise-induced symptoms, two inhalations should be taken 10-15 minutes before challenge. For chronic therapy, two inhalations up to four times a day.
Children: For the relief of acute asthma symptoms including bronchospasm, or before allergen exposure or exercise, one inhalation, or two if necessary. For chronic therapy, two inhalations up to four times a day.
On-demand use, it should not exceed 8 inhalations in any 24 hours. Reliance on such frequent supplementary use, or a sudden increase in dose, indicates poorly controlled or deteriorating asthma.
Symptom: 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 hypokalaemia. Hypokalaemia may occur following overdose with salbutamol. Serum potassium levels should be monitored.
Treatment: 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.
It is contraindicated in patients with a history of hypersensitivity to salbutamol, sympathomimetic amines, aerosol propellants or any other components. Rare cases of hypersensitivity reactions, including urticaria, angioedema, and rash have been reported after the use of salbutamol sulfate; hyperthyroidism; tachyarrhythmia.
Paradoxical Bronchospasm: Inhaled sulbutamol sulfate can produce paradoxical bronchospasm, which may be life threatening. If paradoxical bronchospasm occurs, it should be discontinued immediately and alternative therapy instituted. It should be recognized that paradoxical bronchospasm, when associated with inhaled formulations, frequently occurs with the first use of a new canister.
Deterioration of Asthma: Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. If the patient needs more doses than usual, this may be a marker of destabilization of asthma and requires reevaluation of the patient and treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids.
Use of Anti-Inflammatory Agents: The use of beta-adrenergic agonist bronchodilators alone may not be adequate to control asthma in many patients. Early consideration should be given to adding anti-inflammatory agents, e.g., corticosteroids, to the therapeutic regimen.
Cardiovascular Effects: Salbutamol, like all other beta 2-adrenergic agonists, can produce clinically significant cardiovascular effects in some patients such as changes in pulse rate or blood pressure. If such effects occur, it may need to be discontinued. In addition, beta-agonists have been reported to produce electrocardiogram (ECG) changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression. The clinical relevance of these findings is unknown. Therefore, it like all other sympathomimetic amines should be used with caution in patients with underlying cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.
Do Not Exceed Recommended Dose: Fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs in patients with asthma. The exact cause of death is unknown, but cardiac arrest following an unexpected development of a severe acute asthmatic crisis and subsequent hypoxia is suspected.
Immediate Hypersensitivity Reactions: Immediate hypersensitivity reactions may occur after administration of salbutamol sulfate inhalation aerosol, as demonstrated by cases of urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema. Discontinue if immediate hypersensitivity reactions occur.
Coexisting Conditions: Salbutamol, like other sympathomimetic amines, should be used with caution in patients with convulsive disorders, hyperthyroidism, or diabetes mellitus and in patients who are unusually responsive to sympathomimetic amines. Large doses of intravenous salbutamol have been reported to aggravate preexisting diabetes mellitus and ketoacidosis.
Hypokalemia: As with other beta-agonists, salbutamol may produce significant hypokalemia in some patients, possibly through intracellular shunting, this has the potential to produce adverse cardiovascular effects. The decrease is usually transient, not requiring supplementation.
Patients' inhaler technique should be checked to make sure that aerosol actuation is synchronized with inspiration of breath for optimum delivery of drug to the lungs. Patients should be warned that they may experience a different taste upon inhalation compared to their previous inhaler.
Bronchodilators should not be the only or main treatment in patients with severe or unstable asthma. Severe asthma requires regular medical assessment, including lung-function testing, as patients are at risk of severe attacks and even death. Physicians should consider using the maximum recommended dose of inhaled corticosteroid and/or oral corticosteroid therapy in these patients.
The dosage or frequency of administration should only be increased on medical advice. If a previously effective dose of inhaled salbutamol fails to give relief lasting at least three hours, the patient should be advised to seek medical advice.
Increasing use of bronchodilators, in particular short-acting inhaled beta 2-agonists, to relieve symptoms, indicates deterioration of asthma control. The patient should be instructed to seek medical advice if short-acting relief bronchodilator treatment becomes less effective, or more inhalations than usual are required. In this situation the patient should be assessed and consideration given to the need for increased anti-inflammatory therapy (e.g. higher doses of inhaled corticosteroid or a course of oral corticosteroid).
Severe exacerbations of asthma must be treated in the normal way.
Cardiovascular effects may be seen with sympathomimetic drugs, including salbutamol. There is some evidence from post-marketing data and published literature of rare occurrences of myocardial ischaemia associated with salbutamol. Patients with underlying severe heart disease (e.g. ischaemic heart disease, arrhythmia or severe heart failure) who are receiving salbutamol should be warned to seek medical advice if they experience chest pain or other symptoms of worsening heart disease. Attention should be paid to assessment of symptoms such as dyspnoea and chest pain, as they may be of either respiratory or cardiac origin.
Salbutamol should be administered cautiously to patients with thyrotoxicosis.
Potentially serious hypokalaemia may result from beta 2-agonist therapy, mainly from parenteral and nebulised administration. Particular caution is advised in acute severe asthma as this effect may be potentiated by hypoxia and by concomitant treatment with xanthine derivatives, steroids and diuretics. Serum potassium levels should be monitored in such situations.
Effects on Ability to Drive and Use Machines: None reported.
Use in Children: The safety and effectiveness in children 4 years of age and older has been established based upon two 12-week clinical trials in patients 12 years of age and older with asthma and one 2-week clinical trial in patients 4 to 11 years of age with asthma.
Results from the 2-week pediatric clinical study in patients with asthma 4 to 11 years of age showed that this pediatric population had an adverse reaction profile similar to that of the adolescent and adult populations.
Use in Elderly: Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Pregnancy: There are no adequate and well-controlled studies of salbutamol sulfate in pregnant women. During worldwide marketing experience, 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. No consistent pattern of defects can be discerned, and a relationship between salbutamol use and congenital anomalies has not been established. Animal reproduction studies in mice and rabbits revealed evidence of teratogenicity. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Plasma levels of sulbutamol sulfate and HFA-134a after inhaled therapeutic doses are very low in humans, but it is not known whether the components of formula are excreted in human milk. Because of the potential for tumorigenicity shown for salbutamol in animal studies and lack of experience with the use by nursing mothers, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Caution should be exercised when it is administered to a nursing woman.
Adverse events 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 determined from clinical trial data. Rare, very rare and unknown 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: Hypokalaemia. Potentially serious hypokalaemia may result from beta2 agonist therapy.
Nervous system disorders: Common: Tremor, headache. Very rare: Hyperactivity.
Cardiac disorders: Common: Tachycardia. Uncommon: Palpitations. Very rare: Cardiac arrhythmias (including atrial fibrillation, supraventricular tachycardia and extrasystoles). Unknown: Myocardial ischaemia.
Vascular disorders: Rare: Peripheral vasodilatation.
Respiratory, thoracic and mediastinal disorders: Very rare: Paradoxical bronchospasm.
As with other inhalation therapy, paradoxical bronchospasm may occur with an immediate increase in wheezing after dosing. This should be treated immediately with an alternative presentation or a different fast-acting inhaled bronchodilator. It should be discontinued immediately, the patient assessed, and, if necessary, alternative therapy instituted.
Gastrointestinal disorders: Uncommon: Mouth and throat irritation.
Musculoskeletal and connective tissue disorders: Uncommon: Muscle cramps.
Beta-Blockers: Beta-adrenergic receptor blocking agents such as propranolol not only block the pulmonary effect of beta-agonists, such as salbutamol, but may produce severe bronchospasm in patients with asthma. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers should be considered, although they should be administered with caution.
Other short-acting sympathomimetic aerosol bronchodilators should not be used concomitantly with salbutamol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.
The effects of salbutamol may be enhanced by concomitant administration of aminophylline or other xanthines.
Diuretics: The ECG changes and/or hypokalemia that may result from the administration of nonpotassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical relevance of these effects is not known, caution is advised in the coadministration of beta-agonists with nonpotassium-sparing diuretics. Consider monitoring potassium levels.
Digoxin: Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of salbutamol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical relevance of these findings for patients with obstructive airway disease who are receiving inhaled salbutamol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully evaluate the serum digoxin levels in patients who are currently receiving digoxin and salbutamol.
Monoamine Oxidase Inhibitors or Tricyclic Antidepressants: Salbutamol should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, because the action of salbutamol on the vascular system may be potentiated. Consider alternative therapy in patients taking MAOs or tricyclic antidepressants.
Handling precaution: Avoid spraying in eyes.
Contents under pressure: Do not puncture. Do not use or store near heat or open flame. Exposure to temperatures above 50°C may cause bursting. Never throw container into fire or incinerator.
Store the inhaler with the mouthpiece down. For best results, the inhaler should be at room temperature before use. SHAKE WELL BEFORE EACH SPRAY.
It does not contain chlorofluorocarbons (CFCs) as the propellant.
Store below 30°C. Keep in tight containers, protected from light.
R03AC02 - salbutamol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Aerotamol 100 MDI 100 mcg/dose
(CFC-free) 200 dose x 1's
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