• Document: Syrup (Levosalbutamol sulphate)
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Published on: 10 Jul 2014 LEVOLIN Tablets/Syrup (Levosalbutamol sulphate) Composition LEVOLIN-1 Tablets Each uncoated tablet contains: Levosalbutamol Sulphate equivalent to Levosalbutamol ……..1 mg LEVOLIN-2 Tablets Each uncoated tablet contains: Levosalbutamol Sulphate equivalent to Levosalbutamol……. 2 mg LEVOLIN Syrup Each 5 ml contains: Levosalbutamol Sulphate equivalent to Levosalbutamol……1 mg Dosage Form Oral tablet and syrup Pharmacology Pharmacodynamics Activation of beta2-adrenergic receptors on airway smooth muscle leads to the activation of adenyl cyclase and to an increase in the intracellular concentration of cyclic-3′, 5′-adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which, in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation. Levosalbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levosalbutamol acts as a functional antagonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges. While it is recognized that beta2-adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there are beta-receptors in the human heart, 10–50% of which are beta2-adrenergic receptors. The precise function of these receptors has not been established (see WARNINGS AND PRECAUTIONS). However, all beta- adrenergic agonist drugs can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic (ECG) changes. Pharmacokinetics Absorption Whether administered alone or as the racemate, salbutamol enantiomers are well absorbed from the gastrointestinal tract and have time to maximum drug concentration (tmax) values ranging from 45 to 360 minutes. (S)-Salbutamol has a longer tmax when administered orally as the pure enantiomer compared with when it is administered in the racemate. This phenomenon may be due to altered gastrointestinal motility subsequent to beta-adrenoceptor stimulation by (R)-salbutamol in the racemate. The bioavailability of (S)-salbutamol is approximately 70% at both steady state and following a single oral dose, whereas the bioavailability of (R)-salbutamol increases from 9% after a single oral dose to 30% at steady state. Distribution The blood to plasma ratio for total salbutamol appears to be near unity (0.96 ± 0.13) in healthy volunteers, suggesting that the total blood clearance of salbutamol is equal to the total plasma clearance once steady state has been reached. Values for binding to blood components, along with similar volumes of distribution for salbutamol enantiomers, suggest that protein binding plays a relatively minor role in the disposition of salbutamol enantiomers Metabolism (R)-Salbutamol was metabolized up to 12 times more efficiently than its antipode, with large, normally distributed inter-individual variation being observed in human tissue samples. It is clear from these studies that SULT1A3 expression is higher in intestine than in the other tissues studied, notably hepatic tissue. This supports clinical observations that the intestine is the main site of enantio-selective presystemic metabolism of salbutamol for drug absorbed in the gastrointestinal tract. Elimination Calculated renal clearance values for both enantiomers were significantly larger than creatinine clearance, indicating active renal excretion. This leads to relatively higher concentrations of the drug in urine than in plasma. (S)-Salbutamol is almost always found in higher amounts in urine than (R)-salbutamol, regardless of the route of administration. Indications LEVOLIN Tablets and Syrup are indicated for the treatment or prevention of bronchospasm in adults, adolescents, and children (6–11 years old) with reversible obstructive airway disease. Dosage And Administration LEVOLIN-1 and -2 Tablets/Syrup Adults and Adolescents (Above 12 Years of Age) 1–2 mg/5–10 ml three times daily. Children (Aged 6–11 Years) 1 mg/5 ml three times daily. Contraindications LEVOLIN Tablets and Syrup are contraindicated in patients with a history of hypersensitivity to any of their components. It should not be used for threatened abortion during the first or second trimester of pregnancy. Levosalbutamol and beta-blocking drugs such as propranolol should not usually be prescribed together. Warnings And Precautions General Paradoxical Bronchospasm Levosalbutamol can produce paradoxical bronchospasm, which may be life-threatening. If paradoxical bronchospasm occurs, levosalbutamol should be discontinued immediately and alternative therapy instituted. It should be recognized that paradoxical bronchospasm, when associated with inhaled formulations, frequ

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