Asmalin

Syrup: Salbutamol (Asmalin) 2 mg/5 mL syrup is a pink to dark pink, clear syrup with fruity strawberry odor and sweet strawberry taste using the TasteRite Technology. TasteRite technology is a unique taste-masking system developed specifically for liquid dosage forms to improve the taste of the medicine.
Each 5 mL (1 teaspoonful) contains: Salbutamol sulfate 2 mg.
Pulmoneb: Salbutamol (Asmalin) 1 mg/mL Solution for Inhalation is a clear colorless to light yellow solution in a plastic ampoule. Each ampoule contains 2.5 mL of solution equivalent to 2.5 mg salbutamol.
Each mL solution for inhalation contains: Salbutamol (as sulfate), BP 1 mg.

Pharmacology: Pharmacodynamics: Salbutamol is a selective short-acting beta₂-adrenergic agonist with a preferential effect on beta₂-adrenergic receptors found in the respiratory tract. It stimulates adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cAMP). cAMP mediates cellular responses such as bronchial smooth muscle relaxation resulting in bronchodilation.
Pharmacokinetics: Syrup: Salbutamol is readily absorbed from the gastrointestinal tract after oral administration. When given by inhalation, 10% to 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. Plasma protein binding is around 10%.
Salbutamol undergoes first-pass metabolism in the liver, being converted to salbutamol 4'-O-sulfate. The plasma half-life of salbutamol has been estimated to range from 4 to 6 hours. Salbutamol is rapidly excreted, mainly in the urine, as metabolites and unchanged drug; a smaller proportion is excreted in the feces. Majority of a salbutamol dose given orally or by inhalation is excreted within 72 hours.
Bronchodilation begins within 30 minutes after oral administration of salbutamol, peaks in 2 to 3 hours, and persists 4 to 6 hours.
Pulmoneb: Onset of bronchodilation is within 5 minutes after nebulization with Salbutamol, peaks in 1 to 2 hours, and persists for 3 to 4 hours. Bronchodilation generally persists up to 6 hours or longer. After inhalation of nebulized Salbutamol, less than 20% of the drug is absorbed in the lungs. The remaining amount is retained in the nebulizer and recovered in expired air. Much of the Salbutamol dose delivered by oral inhalation is deposited on the buccal mucosa and subsequently swallowed and absorbed from the gastrointestinal tract.
Salbutamol is metabolized in the liver, being converted to Salbutamol 4'-O-sulfate. This is then excreted in the urine and feces. In patients with asthma, about 70% of the inhaled dose is excreted in urine as unchanged drug and metabolites within 24 hours, and 80 to 100% within 72 hours. About 30% of the inhaled dose is excreted unchanged in the urine in 24 hours. About 10% of the inhaled dose may be excreted in the feces.
Animal studies show that Salbutamol can cross the blood-brain barrier and the placenta. It may be secreted in breast milk but the concentrations are not known.

Syrup: For the relief of bronchospasm associated with reversible obstructive airway diseases such as bronchial asthma and chronic obstructive pulmonary disease.
Pulmoneb: For the prevention and relief of bronchospasm associated with reversible obstructive airway diseases such as bronchial asthma.
For the treatment of acute exacerbations of asthma.

Syrup: This medicine should be taken orally (by mouth). (See Table 1.)

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In elderly patients or in those known to be unusually sensitive to beta-adrenergic stimulant drugs, it is advisable to initiate treatment with 2 mg salbutamol every 6 to 8 hours.
Pulmoneb: To be administered via a nebulizer. (See Table 2.)

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Syrup: Overdosage with salbutamol produces symptoms that may be expected with beta₂-agonists such as tachycardia, central nervous system stimulation, tremor, hypokalemia, and hypoglycemia.
Nausea, vomiting and hyperglycemia have been reported, predominantly in children and when salbutamol overdose has been taken via the oral route.
Lactic acidosis has been reported in association with high therapeutic doses as well as overdoses of short-acting beta-agonist therapy.
Cardiac arrest and even death may occur following excessive use of salbutamol.
Discontinue salbutamol and institute appropriate symptomatic therapy in cases of salbutamol overdosage. Administration of a beta-adrenergic blocking agent may be appropriate, but use with caution in patients with a history of bronchospasm. There is no adequate evidence to support the use of dialysis in the treatment of salbutamol overdose.
Pulmoneb: Symptoms of nebulized Salbutamol overdose include extensions of the common undesirable effects (e.g., tremors, seizure, nervousness, dizziness, headache, sleeplessness/insomnia, hypertension or hypotension, palpitation, tachycardia, arrhythmia, angina, dry mouth, nausea, fatigue, and malaise).
Excessive use of oral sympathomimetic inhalations may result in cardiac arrest and even fatalities. Hypokalemia has also been reported. Thus, plasma potassium concentrations should be monitored. Discontinue Salbutamol and institute appropriate symptomatic therapy in cases of Salbutamol overdosage. Administration of a beta-adrenergic blocking agent may be appropriate, but use with caution if the patient is asthmatic. There is no adequate evidence to support the use of dialysis in the treatment of Salbutamol overdose.

Hypersensitivity to salbutamol or other ingredients in the product.
Syrup: Certain maternal or fetal conditions may contraindicate tocolytic therapy (e.g., eclampsia or severe preeclampsia, intrauterine infection, intrauterine fetal death, antepartum hemorrhage, placenta previa, cord compression, or toxemia of pregnancy); salbutamol should not be used for threatened abortion.

Syrup: Seek medical advice if either the usual relief is diminished or the usual duration of action is reduced. Do not increase the dose or frequency of administration.
Pulmoneb: If a previously effective dose fails to provide the usual relief or the usual duration of action is reduced, consult a physician for medical advice as this is a sign of worsening of asthma that would require reassessment of therapy.
Excessive use of sympathomimetic oral inhalations has been associated with fatalities in asthmatic patients. The exact cause of death is unknown but cardiac arrest following severe, acute asthmatic crisis and hypoxia is suspected.
Paradoxical bronchospasm, a potentially life-threatening event, may occur with the first use of a new ampoule. If it occurs, discontinue Salbutamol immediately and institute alternative therapy.
Immediate hypersensitivity reactions including urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema may occur rarely after administration of the product.

Syrup: Paradoxical bronchospasm: Paradoxical bronchospasm, a potentially life-threatening event, has been observed with salbutamol. If it occurs, discontinue use of the product immediately.
Deterioration of asthma: Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. Increased use of beta₂-agonists, especially daily use, is a sign of deterioration of asthma control and indicates the need to reassess treatment. Possible need for anti-inflammatory treatment (e.g., corticosteroids) should be considered.
Hypokalemia: Therapy with salbutamol and other beta₂-agonists may produce decrease in plasma potassium concentration possibly through intracellular shunting resulting in cardiovascular undesirable effects. Use with caution in acute severe asthma where concomitant therapy with steroid, xanthine derivatives, or diuretics, and by hypoxia may result in hypokalemia; potassium concentrations should be monitored in severe asthma.
Metabolic Effects: As with other beta₂-agonists, salbutamol can induce reversible metabolic changes (e.g., increased blood sugar levels). The diabetic patient may be unable to compensate for this; and thus, result in the development of ketoacidosis. Concomitant administration of corticosteroids can exaggerate this effect.
Coexisting Conditions: Use with caution in patients with the following conditions: Cardiovascular disorders including coronary insufficiency, cardiac arrhythmias, or hypertension: Salbutamol, like all other beta₂-agonists, can produce clinically significant cardiovascular effects such as changes in pulse rate or blood pressure; Convulsive disorders; Hyperthyroidism; Diabetes mellitus; In patients who are unusually responsive to sympathomimetic amines.
Pulmoneb: Patients should be advised that increased blood glucose has occurred after inhalation of Salbutamol via nebulization of higher than recommended doses of the drug. Use with caution in patients with the following conditions: Cardiovascular disorders including coronary insufficiency, cardiac arrhythmias or hypertension; Convulsive disorders; Hyperthyroidism; Diabetes mellitus; In patients who are unusually responsive to sympathomimetic amines.
Use with caution in acute severe asthma where concomitant therapy with steroid, xanthine derivatives, or diuretics, and by hypoxia may result in hypokalemia. Potassium concentrations should be monitored in severe asthma.
Therapy with Salbutamol and other beta₂-agonists may decrease plasma potassium concentration possibly through intracellular shunting resulting in cardiovascular adverse effects such as palpitation.

Pregnancy: Pregnancy Category C. There have been reports of congenital anomalies (e.g., cleft palate and limb defects) in children of patients treated with salbutamol. Some of the mothers, however, were receiving various medications in the course of their pregnancies. Since there is no consistent pattern of congenital abnormality development, a relationship between the use of salbutamol and the development of congenital anomalies cannot be established. Therefore, salbutamol should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
Labor and Delivery: Syrup: Since beta₂-agonists may interfere with uterine contraction, salbutamol should be used in labor only if the potential benefit justifies the potential risk.
Lactation: Salbutamol may be secreted in breast milk. Therefore, do not administer to breastfeeding women unless, in the opinion of a physician, the potential benefit of the drug justifies the potential risk.

Syrup: Infections and infestations: Conjunctivitis.
Immune system disorders: Erythema multiforme, hypersensitivity (anaphylaxis, angioedema, bronchospasm, collapse, hypotension, oropharyngeal edema, rash, urticaria), Stevens-Johnson syndrome.
Metabolism and nutrition disorders: Hypokalemia, increased appetite.
Psychiatric disorders: Hoarseness, hyperactivity, nervousness.
Nervous system disorders: Central nervous stimulation, dizziness, headache, tremor, vertigo.
Eye disorders: Mydriasis.
Cardiac disorders: Angina, cardiac arrhythmias (including atrial fibrillation, supraventricular tachycardia, and extrasystoles), myocardial ischemia, palpitations, tachycardia.
Vascular disorders: Epistaxis, hypotension, pallor, peripheral vasodilatation.
Respiratory, thoracic and mediastinal disorders: Cough, paradoxical bronchospasm.
Gastrointestinal disorders: Epigastric pain, stomachache.
Musculoskeletal and connective tissue disorders: Feeling of muscle tension, muscle cramps.
General disorders and administration site conditions: Increased sweating.
Pulmoneb: Tremors (particularly the hands), nervousness, dizziness, headache, sleeplessness/insomnia, tachycardia, palpitations, chest pain, hypertension, peripheral vasodilation, increased coughing, wheezing, asthma exacerbation, bronchitis, nasal congestion, rhinitis, pharyngitis, sinusitis, viral infection, increased hemoptysis in patients with pre-existing hemoptysis, hoarseness, otitis media, nausea, vomiting, diarrhea, hypertonia, asthenia, back pain, fever, lymphadenopathy, and rarely, muscle cramps have been observed after administration of nebulized Salbutamol.
Potentially serious hypokalemia has also been reported.
Hypersensitivity reactions (such as urticaria, angioedema, rash, bronchospasm, anaphylaxis, oropharyngeal edema, hypotension, and collapse) and arrhythmias (such as atrial fibrillation, supraventricular tachycardia, and extrasystoles) have also been noted after the use of orally inhaled Salbutamol.
Salbutamol, like other sympathomimetic agents, can also cause angina, vertigo, central nervous system stimulation, paradoxical bronchospasm, and dry mouth.

Syrup: Sympathomimetic agents: Salbutamol should not be administered concomitantly with other sympathomimetic agents or epinephrine since serious adverse cardiovascular effects may occur.
Beta-adrenergic blocking agents (e.g., propranolol): Beta-adrenergic blocking agents may inhibit the effect of beta-agonists such as salbutamol. It may also produce severe bronchospasm in asthmatic patients.
Diuretics: Administration of nonpotassium-sparing diuretics (e.g., loop or thiazide diuretics) may result in electrocardiographic changes and/or hypokalemia and can be acutely worsened by administration of beta₂-agonists such as salbutamol, especially when the recommended dose of the beta₂-agonist is exceeded.
Digoxin: Following administration of single-dose intravenous or oral salbutamol to healthy individuals who had received digoxin for 10 days, a 16% to 22% decrease in serum digoxin concentration was observed. Although the clinical importance of these findings for patients who are receiving inhaled salbutamol and digoxin on a chronic basis is unclear, patients receiving such concomitant therapy should have their serum digoxin concentration carefully evaluated.
Monoamine oxidase inhibitors (MAOIs) or Tricyclic antidepressants (TCAs): Salbutamol should be used with caution in patients receiving MAOIs or TCAs, or within 2 weeks of discontinuation of such agents, because the effect of salbutamol on the vascular system may be potentiated. Alternative therapy should be considered in patients taking MAOIs or TCAs.
Pulmoneb: Do not use with other sympathomimetic aerosol bronchodilators or epinephrine. Administer with caution additional sympathomimetic agents by any route to patients using Salbutamol aerosol to avoid deleterious cardiovascular effects.
Concurrent administration with monoamine oxidase (MAO) inhibitors or tricyclic antidepressants may increase the risk for cardiac arrhythmia, tachycardia, and increased or decreased blood pressure.
Do not administer with beta-receptor blockers since these agents inhibit Salbutamol's effect.
The combination of nebulized Salbutamol and a nebulized anticholinergic drug has been reported to precipitate acute angle closure glaucoma and therefore should be used with caution in patients with actual or potential glaucoma.

Pulmoneb: Directions for Use: Salbutamol (Asmalin) must only be used in a nebulizer for inhalation.
1. Prepare the nebulizer for use.
2. Remove the ampoule from the strip by twisting and pulling.
3. Hold the ampoule upright and twist off the cap. Transfer the content to the reservoir of the nebulizer. If dilution is required, use only sterile normal saline as directed by the physician.
4. Use the nebulizer, as instructed by the manufacturer.
5. After use, discard any remaining solution. Thoroughly clean the nebulizer.
Patient Information: Administer in a well-ventilated area.
Do not mix the solution with other medicines, unless instructed to do so by the physician.
Do not allow the solution for nebulization or the mist to come into contact with the eyes.
If a dose was missed, do not take a double dose.

Syrup: Store at temperatures not exceeding 25°C.
Pulmoneb: Store at temperatures not exceeding 30°C.
Protect from light.

Antiasthmatic & COPD Preparations

R03AC02 - salbutamol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
R03CC02 - salbutamol ; Belongs to the class of adrenergics for systemic use, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.

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