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Ambroxol is a clinically proven systemically active mucolytic agent. When administered orally onset of action occurs after about 30 minutes. The breakdown of acid mucopolysaccharide fibers makes the sputum thinner and less viscous and therefore more easily removed by coughing. Although sputum volume eventually decreases, its viscosity remains low for as long as treatment is maintained.
Levosalbutamol or levalbuterol is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). It is marketed under the brand name Xopenex by Sunovion Pharmaceuticals Inc.
Ambroxol (group of benzilamides) belongs to secretolitical and secretomotoric medicinal products. It possesses expressed expectorant effect. Mechanism of action of the medicinal product is stipulated by stimulation of serous cells of tonsils of bronchial tubes' mucous membrane, increasing of mucous secretion content and changing of correlation of serous and mucous components of phlegm, breached under pathological processes in lungs. Under this hydrolyzing ferments activate and releasing of lizosoms from Clark's cells strengthens, that causes decreasing of viscosity of phlegm. Ambroxol increases content of surfactant in lungs, which is dealt with strengthening of synthesis of the last and secretion in alveolar pneumocytes, and also with breach of its disintegration. The medicinal product increases mucociliar transport of phlegm. It suppresses
coughing insignificantly. Ambroxol well penetrates through the placenta barrier, improving synthesis of surfactants during uterine life of foetus, and also it has an ability to warn syndrome of insufficient breathing in newborn. The medicinal product does not cause immense creating of secretion, reduces spastic hyperactivity of bronchial tubes- one of the main factors of developing of bronchial asthma under allergy. Ambroxol is more effective, than its predecessor
Guaiphenesin is thought to exert its pharmacological action by stimulating receptors in the gastric mucosa. This increases the output from secretory glands of the gastrointestinal system and reflexly increases the flow of fluids from glands lining the respiratory tract. The result is an increase in volume and decrease in viscosity of bronchial secretions. Other actions may include stimulating vagal nerve endings in bronchial secretory glands and stimulating certain centres in the brain, which in turn enhance respiratory fluid flow. Guaiphenesin produces its expectorant action within 24 hours.
Levosalbutamol is a single isomer beta2-agonist that differs from racemic salbutamol by elimination of (S)-salbutamol. Levosalbutamol is an effective bronchodilator whose primary mechanism of action is unimpeded by (S)-salbutamol. Therefore, when compared with racemic salbutamol, clinically comparable bronchodilation can be achieved with doses that substantially lessen beta-mediated side effects.
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.
Absorption: Ambroxol is rapidly absorbed (70-80%) after oral administration. The time to reach peak plasma concentration is approximately 2 hours.
Distribution:The distribution half-life of ambroxol is around 1.3 hours.
Metabolism: Metabolite is dibromoanthranilic acid (activity unspecified).
Excretion:Excretion is primarily via the kidneys. Renal clearance (rate) is approximately 53 ml/minute; approximately 5-6% of a dose is excreted unchanged in the urine. The elimination half-life of ambroxol is biphasic, with an alpha half-life of 1.3 hours and a beta half-life of 8.8 hours.
Absorption: Guaiphenesin is well absorbed from the gastro-intestinal tract following oral administration, although limited information regarding its pharmacokinetics is available. After the administration of 600 mg Guaiphenesin to healthy adult volunteers, the Cmax was approximately 1.4ug/ml, with tmax occurring approximately 15 minutes after drug administration.
Distribution: No information is available on the distribution of Guaiphenesin in humans. Metabolism and elimination: Guaiphenesin appears to undergo both oxidation and demethylation. Following an oral dose of 600 mg guaifenesin to 3 healthy male volunteers, the t½ was approximately 1 hour and the drug was not detectable in the blood after approximately 8 hours.
Pharmacokinetics in Renal/Hepatic Impairment: There have been no specific studies of Guaiphenesin in subjects with renal or hepatic impairment. Caution is therefore recommended when administering this product to subjects with severe renal or hepatic impairment.
Expectorant is indicated for clinical relief of cough associated with bronchitis, bronchial asthma, emphysema and other bronchopulmonary disorders where bronchospasm, mucous plugging and problems of expectoration co-exist, prevention of bronchospasm in adults, adolescents, and children.
Hypersensitivity to any of the components of the formulation. It should not be used in patients with pre-existing ischaemic heart disease or those patients with significant risk factors for ischaemic heart disease. It is also contraindicated in patients with gastric ulceration.
Terbutaline: As for all beta2-agonists caution should be observed in patients with thyrotoxicosis.
Cardiovascular effects may be seen with sympathomimetic drugs, including terbutaline. There is some evidence from post-marketing data and published literature of myocardial ischaemia associated with beta agonists.
Terbutaline: Beta-blocking agents (including eye drops); especially the non-selective ones such as propranolol, may partially or totally inhibit the effect of beta-stimulants. Therefore terbutaline preparations and non-selective beta-blockers should not normally be administered concurrently. Terbutaline should be used with caution in patients receiving other sympathomimetics. Hypokalaemia may result from beta2-agonist therapy and may be potentiated by concomitant treatment with xanthine derivatives, corticosteroids and diuretics.
