Composition Each 5ml contains
Ambroxol Hydrochloride 15mg
Terbutaline Sulphate 1.25mg
Guiephenesin 50mg
Mango Syrup Base q.s.

 

DOSAGE FORM 

Oral Syrup (Alphonso Mango Flavoured)

DESCRIPTION

Bronkolyte-PD ™ SYRUP is a combination of Terbutaline Sulphate, Ambroxol Hydrochloride and Guaiphenesin. Terbutaline is a selective beta2  -adrenergic agonist which predominantly  stimulates beta2-receptors, thus producing relaxation of bronchial smooth  muscle.  Ambroxol possesses mucokinetic (improvement in mucus transport) and  secretolytic (liquifies secretions) properties. It promotes the removal of tenacious  secretions in the respiratory tract and reduces mucus stasis (arresting the  secretion of mucus). Besides that, Ambroxol also exhibits anti-oxidant activity.  Guaiphenesin, by increasing respiratory tract fluid, reduces the viscosity of  tenacious secretions and acts as an expectorant. Another possible mechanism  by which it acts is by increasing the water bonding in the sputum, thereby  decreasing its viscosity and leading to an increase in mucokinesis. Guaiphenesin  is effective in both productive and nonproductive coughs.

PHARMACOLOGY/ PHARMACOKINETICS

Terbutaline:

Terbutaline is a selective beta2  – adrenergic causing bronchodilation; increase in  mucociliary clearance; suppression of oedema and anti-allergic effects.   The pharmacologic effects of beta-adrenergic agonist drugs, including  terbutaline, are at least in part, attributable to stimulation through beta-adrenergic  receptors on intracellular adenyl cyclase, the enzyme that catalyses the  conversion of adenosine triphosphate (ATP) to cyclic-3?,5?-adenosine  monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of  immediate hypersensitivity from cells, especially from mast cells.

Basic parameters have been  evaluated in man after oral administration of  therapeutic doses, e.g.  Renal clearance (CLR): 1.925/ml/min (males)   Renal clearance (CLR): 2.32ml/min (females). Terminal half-life T½ has been determined after single and multiple dosing (mean  values varied between 16-20 h)

Food reduces bioavailability following oral dosing (10% on average).   Fasting values of 14-15% have been obtained.  Metabolism:   The main metabolite after oral dosing is the sulphate conjugate and also some  glucoronide conjugate can be found in the urine.

Ambroxol:

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  – Bromhexine; it is non-toxic one and well endured by patients. Action of retard  form of Ambroxol is kept in 9-10 hours after administration inside.

Ambroxol is rapidly absorbed (70-80%) after oral administration. The time to  reach peak plasma concentration is approximately 2 hours. The distribution half-life of ambroxol is around 1.3 hours. Metabolite is dibromoanthranilic acid (activity unspecified). 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.

Guaiphenesin:

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.

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. 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.

INDICATIONS

Bronkolyte-PD ™ SYRUP  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.

DOSAGE AND ADMINISTRATION

Adults

10-20 ml thrice daily

Children (6-12 years):

10 ml thrice daily

Children (under 6 years):

5-10 ml thrice daily

CONTRAINDICATIONS

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.

WARNINGS AND PRECAUTIONS

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.   Due to the positive inotropic effect of beta2-agonists, these drugs should not be  used in patients with hypertrophic cardiomyopathy.

Tocolysis:

Terbutaline should be used with caution in tocolysis and supervision of cardiorespiratory function, including  ECG monitoring, should be considered.  Treatment should be discontinued if signs of myocardial ischaemia (such as  chest pain or ECG changes) develop. Terbutaline should not be used as a  tocolytic agent in patients with significant  risk factors for or pre-existing heart  disease.   During infusion treatment  in pregnant women with beta2-stimulants in combination with corticosteroids a rare  complication with a  pathological picture  resembling pulmonary oedema, has been reported.  Increased tendency to uterine bleeding has been reported in connection with  Caesarean section. However, this can be effectively stopped by propranolol 1-2  mg injected intravenously.

Respiratory indications:

Patients with underlying severe heart disease (e.g. ischaemic heart disease,  arrhythmia or severe heart failure) who are receiving Terbutaline should be  warned to seek medical advice if they experience chest pain or other symptoms  of worsening heart disease.   Attention should be paid to assessment of symptoms such as dyspnoea and  chest pain, as they may be of either respiratory or cardiac origin.   Due to the hyperglycaemic effects of beta2-agonists, additional blood glucose  controls are recommended initially in diabetic patients.   Potentially serious hypokalaemia may result from beta2-agonist therapy.

Particular caution is recommended in acute severe asthma as the associated risk  may be augmented by hypoxia. The hypokalaemic effect may be potentiated by  concomitant treatments. It is recommended that serum potassium levels are  monitored in such situations.   If a previously effective dosage regimen no longer gives the same symptomatic  relief, the patient should urgently seek further medical advice. Consideration  should be given to the requirements for additional therapy (including increased  dosages of anti-inflammatory medication). Severe exacerbations of asthma  should be treated as an emergency in the usual manner.

Ambroxol:

Care to be taken to avoid contact with eye, skin, serious ingestion or inhalation.

Guaiphenesin:

Guaiphenesin should be not used for persistent or chronic cough, such as occurs  with asthma, or where cough is accompanied by excessive secretions, unless  directed by a physician. Caution should be exercised in the presence of severe  renal or severe hepatic impairment. Patients with rare hereditary problems of  fructose intolerance should not take this medicine. Not more than 4 doses should  be given in any 24 hours. Avoid with any other cough and cold medicine. Consult  a pharmacist or other healthcare professional before use in children under 6  years.

Drug interactions

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.

Ambroxol:

No data available

Guaiphenesin:

If urine is collected within 24 hours of a dose of Guaiphenesin, its metabolite may  cause a colour interference with laboratory determinations of urinary 5- hydroxyindoleacetic acid (5-HIAA) and vanillylmandelic acid (VMA).   Others

Bronkolyte-PD ™ SYRUP should be used with caution in patients with diabetes  mellitus, serious cardiovascular disorders, hypertension, hyperthyroidism and  peptic ulcers.

Pregnancy

However, there are no adequate and well-controlled studies of this combination in pregnant women. Hence this combination should be administered with caution in pregnancy.

Lactation

It is not known whether this combination is secreted in breast milk. However terbutaline is secreted in breast milk, but effect on the infant is unlikely at therapeutic doses. Therefore this combination should be used with caution nursing mothers.

PACKAGING INFORMATION

Bronkolyte-PD ™ SYRUP Bottle of 60 ml

 

Disclaimer: The above product related information is intended for medical practitioners only