Activent

Activent

salbutamol

Manufacturer:

Hizon

Distributor:

S V More
Full Prescribing Info
Contents
Salbutamol sulfate.
Description
Each 5 mL syrup contains salbutamol (as sulfate) 2 mg.
Action
Pharmacology: Pharmacodynamics and Pharmacokinetics: Salbutamol is used as bronchodilator in the management of reversible airway obstruction, as in asthma and in various forms of chronic obstructive pulmonary diseases.
Salbutamol is a direct-acting sympathomimetic amine with mainly beta-adrenergic activity. It acts selectively on beta-2 adrenergic receptors in the lungs to relax bronchial smooth muscle, thereby relieving bronchospasm and reducing airway resistance. It also relaxes the smooth muscle of the uterus and enhances vascular supply to the skeletal muscle. These are said to result from increased production of cyclic adenosine 3',5' - monophosphate (cyclic 3',5' - AMP) caused by activation of the enzyme adenyl cyclase.
Following oral administration, salbutamol is well absorbed from the gastrointestinal tract. It is metabolized in the liver and possibly in the gut wall. Estimated plasma half-life of salbutamol ranges from 4 to 6 hours.
Salbutamol is rapidly excreted mainly in the urine within 48-72 hours after oral administration, little portion is excreted via the feces.
Indications/Uses
For the relief of bronchospasm in bronchial asthma, chronic bronchitis and emphysema.
Dosage/Direction for Use
Adults (Syrup): 10 mL (2 teaspoonfuls) 3-4 times a day.
Or as prescribed by the physician.
Children (Syrup): 2-6 years: 2.5 mL-5 mL (½-1 teaspoonful) 3-4 times a day.
7-12 years: 5 mL (1 teaspoonful) 3-4 times a day.
Over 12 years: 5 mL-10 mL (1-2 teaspoonfuls) 3-4 times a day.
Or as prescribed by the physician.
Overdosage
Most common manifestations of overdose with salbutamol include nausea, vomiting, tachycardia, CNS stimulation, tremors, lactic acidosis, hypokalemia and hyperglycemia. Symptomatic management of these conditions has proved to be valuable.
In cases of oral overdose, activated charcoal may be considered. Appropriate medical management should be done or as recommended by the National Poison Center.
Contraindications
Salbutamol (Activent) should not be used in patients with history of hypersensitivity to salbutamol.
Salbutamol should not be administered concomitantly with other sympathomimetic agents as it may cause adverse effects on the cardiovascular system.
Caution should be exercised in administering salbutamol to patients with thyroid disorders, myocardial insufficiency, arrhythmias, hypertension, susceptibility to QT-interval prolongation and diabetes mellitus.
The bronchodilator effects of beta-agonist are opposed by non-cardioselective beta-blockers. Non-cardioselective beta blocker are contraindicated in asthmatic patients as they may cause serious bronchoconstriction. Normally, no adverse interaction occurs between beta-agonist bronchodilators and cardioselective beta blocker; however, bronchospasm can occur in asthmatic patients particularly if high doses are used.
As the use of salbutamol with corticosteroids, diuretics or xanthines increases the risk of hypokalemia, monitoring of potassium concentrations is recommended in severe asthma where such combination therapy is common.
Use In Pregnancy & Lactation
Most adverse effects of salbutamol in pregnancy relate to the cardiovascular and metabolic effects of the very high doses given by intravenous infusion to delay premature labor.
The use of salbutamol in lactating mothers is generally not recommended since it is not known whether salbutamol in breast milk has harmful effects on the neonate.
Pulmonary edema has been reported in pregnant women given with salbutamol for premature labor, although most cases are seen in patients given very high doses intravenously. Maternal effects include myocardial ischemia, unifocal ventricular ectopics associated with the hypoischemic response to intravenous salbutamol and heart failure in hypersensitive woman.
Adverse Reactions
Salbutamol like other beta-agonists, may cause fine tremors of the skeletal muscles specially the hands, nervous tension, hyperacidity, restlessness, headaches, increased heart rate, palpitations, tachycardia, hyperglycemia, peripheral vasodilation and rarely muscle cramps. The said effects which are common to all symphatomimetic drugs are dose-related.
Potentially serious hypokalemia and myocardial ischemia can occur in large doses. Hypersensitivity reactions including paradoxical bronchospasms, angioedema, urticaria, hypotension and collapse may also occur.
Drug Interactions
Salbutamol should not be prescribed together with non-selective beta-adrenergic agents like propranolol.
The use of salbutamol with corticosteroids, diuretics and xanthines may increase the risk of hypokalemia.
Storage
Store at temperatures not exceeding 30°C. Protect from light.
MIMS Class
Antiasthmatic & COPD Preparations
ATC Classification
R03CC02 - salbutamol ; Belongs to the class of adrenergics for systemic use, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
Presentation/Packing
Form
Activent syr 2 mg/5 mL
Packing/Price
60 mL x 1's (P86.91/bottle)
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