DESCRIPTION
Bromhexine – Bromhexine is an expectorant/mucolytic agent. Bromhexine is not available in the United States. It is marketed under the trade name Bisolvon® in Germany, England, Belgium, France, Italy, Netherlands, Norway, Sweden, Australia, and South Africa. Guaifenesin -An expectorant that also has some muscle relaxing action. It is used in many cough preparations. Terbutaline – A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.
CATEGORIES
Bromhexine – Cough & Cold Preparations,Guaifenesin – Expectorants ,Terbutaline – Sympathomimetics,Adrenergic beta-2 Receptor Agonists,Bronchodilator Agents,Tocolytic Agents.
CHEMICAL FORMULA
Bromhexine – C14H20Br2N2,Guaifenesin -C10H14O4,Terbutaline – C12H19NO3.
COMPOSITION
Terbutaline sulphate 1.25 mg + Guaiphenesin 50 mg + Bromhexine Hcl 2 mg +Menthol 0.5 mg
INDICATION
Guaifenesin -Used to assist the expectoration of phlegm from the airways in acute respiratory tract infections.Terbutaline – For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease, as well as symptomatic management of reversible bronchospasm associated with bronchitis and emphysema. Also used acute IV and sub-Q therapy in selected women to inhibit uterine contractions in preterm labor (tocolysis) and prolong gestation when beneficial.
PHARMACODYNAMICS
Guaifenesin -Guaifenesin is an expectorant which increases the output of phlegm (sputum) and bronchial secretions by reducing adhesiveness and surface tension. The increased flow of less viscous secretions promotes ciliary action and changes a dry, unproductive cough to one that is more productive and less frequent. By reducing the viscosity and adhesiveness of secretions, guaifenesin increases the efficacy of the mucociliary
MECHANISM
in removing accumulated secretions from the upper and lower airway. Terbutaline -Terbutaline is a relatively selective beta2-adrenergic bronchodilator that has little or no effect on alpha-adrenergic receptors. The drug has exerts a preferential effect on beta2-adrenergic receptors but stimulates beta-adrenergic receptors less selectively than relatively selective beta2-agonists. Terbutaline appears to have a greater stimulating effect on beta-receptors of the bronchial, vascular, and uterine smooth muscles (beta2 receptors) than on the beta-receptors of the heart (beta1 receptors). This drug relaxes smooth muscle and inhibits uterine contractions, but may also cause some cardiostimulatory effects and CNS stimulation.
No Information
ABSORPTION
Guaifenesin -Rapidly absorbed from the GI tract ,Terbutaline – Approximately 30-50% if administered orally and well absorbed subcutaneously.
METABOLISM
Guaifenesin -Rapidly hydrolyzed (60% within seven hours) and then excreted in the urine, with beta-(2-methoxyphenoxy)-lactic acid as its major urinary metabolite.
ELIMINATION
Terbutaline – About 90% of the drug was excreted in the urine at 96 hours after subcutaneous administration, with about 60% of this being unchanged drug. It appears that the sulfate conjugate is a major metabolite of terbutaline and urinary excretion is the primary route of elimination
HALF LIFE
Guaifenesin -1 hour,Terbutaline – 5.5-5.9 hours.
TOXICITY
Guaifenesin -LD50 1510 mg/kg (rat, oral),Terbutaline -Terbutaline Sulfate: Oral LD50(rat) = 8.7 g/kg; Oral LD50(mouse) = 205 mg/kg; Oral LD50(dog) = 1.5 g/kg; IP LD50(rat)= 220 mg/kg ; IP LD50(mouse) = 130 mg/kg; Oral LD50(rabbit) = >8 g/kg; IV LD50(mouse) = 36 mg/kg; IV LD50(dog) = 116 mg/kg; IV LD50(rabbit) = 110 mg/kg.
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Bromhexine – Rhinorrhoea, lacrimation, gastric irritation and hypersensitivity.Guaifenesin – Feeling dizzy. Rise slowly over a few minutes when sitting or lying down. Be careful climbing. Headache. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Terbutaline – Nervous and excitable. Headache. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Dry mouth. Good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. See a dentist often. Not able to sleep. – Shot: – Low blood pressure. Flushing. Wearing layers of clothes or summer clothes and staying in cool places may help. Low potassium levels. Signs include feeling tired, weak, numbness, or tingling; muscle cramps; hard stools (constipation); throwing up; or a fast heartbeat. High blood sugar may cause diabetes while on this drug. This most often goes back to normal when this drug is stopped.