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Brand Name, Dosage Format and Strength
Solmux Broncho 2 mg / 500 mg Capsule
Therapeutic Category
Respiratory System
Class
Corticosteroid, Anticholinergic, Beta2-Agonist, Leukotriene Inhibitor, Beta2-Agonist, Beta2-Agonist, Expectorant, Antiasthma-Beta2- Agonist, Mucolytic, Beta2-Agonist, Mucolytic, Antitussive, Nasal Decongestant, Analgesic-Antipyretic, Antitussive, Nasal Decongestant, Analgesic-Antipyretic, Nasal Decongestant, Antihistamine, Nasal Decongestant, Antihistamine, Analgesic-Antipyretic, Nasal Decongestant, Analgesic-Antipyretic, Alpha Adrenergic Agonist, Nasal Decongestant, Antihistamine, Analgesic-Antipyretic
CLINICAL PHARMACOLOGY
Pharmacodynamics
Salbutamol
Salbutamol stimulates adenyl cyclase, the enzyme which catalyzes the formation of cAMP from ATP. The cAMP thus formed mediates the cellular responses, such as bronchial smooth muscle relaxation. In vitro and in vivo pharmacologic studies have demonstrated that compared with isoproterenol, salbutamol has a preferential effect on beta2-adrenergic receptors found in the respiratory tract. Salbutamol has been shown in most controlled studies to have more effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, than isoproterenol at comparable doses while producing fewer cardiovascular effects.
Carbocisteine
Carbocisteine, a derivative of acetylcysteine, is a mucoregulating agent. Its major action is thought to be on the metabolism of mucus-producing cells. The mucus produced under the influence of carbocisteine has an increased content of the less viscous sialomucin and a reduced content of the highly viscous fucomucin. Sialomucins influence the rheological properties of mucus and may also, through the inhibition of kinins, reduce or prevent bronchial inflammation and bronchospasm.
Pharmacokinetics
Salbutamol
Salbutamol is rapidly and well absorbed from the gastrointestinal tract. After oral administration, salbutamol’s onset of action is within 30 min, with peak effect 2 to 3 hrs after the dose, and duration of action of up to 6 hrs. The plasma half-life of salbutamol is from 4 to 6 hrs. It is extensively metabolized in the liver, mainly to salbutamol 4’-O-sulfate which has no beta-adrenergic blocking effect. Salbutamol is rapidly excreted in the urine as metabolites and unchanged drug; a small fraction is excreted in the feces.
Results of animal studies indicate that salbutamol does not cross the blood-brain barrier, but the drug apparently crosses the placenta. It is not known if the drug is distributed into milk.
Carbocisteine
Carbocisteine is rapidly and well absorbed after oral administration. Following oral administration of 1.5 g carbocisteine, Cmax of 13 to 16 mg/L were reached in 1 to 2 hrs; t½ was 1.5 to 2 hrs. Carbocisteine penetrates well into lung tissues and respiratory mucus, suggesting local action. Carbocisteine undergoes acetylation, decarboxylation, and sulfoxidation. Majority of the drug is excreted unchanged in the urine.