MUCORESP Drug Review (Ref. Drug Today, 0ct - Dec 2004)

INTRODUCTION :
Azine H. Care has introduced a unique combination of Ambroxol, Salbutamol and Theophylline combination, which is very
effective for the treatment of bronchial asthma and other forms of bronchospasams-eg. Chronic bronchitis, bronchiectasis and lung infections etc. Tolerance dose not develops even after regular long term use if given therapeutic doses.

COMPOSTION:

Each tablet contains:

Ambroxol 30 mg
Salbutamol 2 mg
Theophylline l00 mg

CLINICAL PHARMACOLOGY:

Ambroxol : It is an active metabolite of bromhexine. It facilitates expectoration of excessive secretions by virtue of its mucolytic mucokinetic actions. Ambroxol also acts as tissue protective (due to its inhibitory effect on release of destructive mediators and free oxygen radicals/species by phagocytes, due to its scavenging effect against free radical, due to its antiinflammatory effect by decreasing interleukins and due to its action of inactivating alpha anti-proteinase). Although it is completely absorbed from the GI tract following oral administration, its bioavailability is 60%. The therapeutic effective level of Ambroxol is 3mg/ ml. The average l/2 life is 9-10 hours. It is changed into various inactive metabolites, which are mainly eliminated as water-soluble conju­ gates; less than 10% of Ambroxol is eliminated unchanged in urine.

Salbutamol: Salbutamol is beta-adrenergic stimulant, which is chemically related to isoprenaline. It has no prominent bronchodilator due its Beta-2 receptor action. It has poor cardiac stimulant action as compared to isoprenaline and in therapeutic doses it may not produce palpitation or rise of blood pressure. The action of single oral dose lasts for about 4- 6 hours.

Theophylline: It acts as a potent bronchodilator by direct relaxation of the bronchial smooth muscle. The actions of theophylline may be mediated through inhibition of phosphodiesterase. It also cause relaxation of pulmonary blood vessels, coronary vasodilatation, cardiac and cerebral stimulation and diuresis. It has been shown that it reacts synergistically with beta agonists. No development of tolerance occurs with chronic use of theophylline. It is very well absorbed from the GI tract. The average half-life in non­ smoking adults is around 8-hours. Half-life in smokers is shorter than in non-smokers, therefore, smokers may require larger doses of theophylline.

INDICATIONS

• Acute and chronic diseases of the respiratory tract-eg. Acute and chronic bronchitis, COPD, asthmatic bronchitis, smokers cough.

• For the treatment of bronchial asthma and other forms of bronchospasms-eg. Chronic bronchitis, bronchiectasis and lung infections.

• For the prophylaxis and relief of reversible bronchospasm associated with asthma, bronchitis and emphysema and other obstructive airway disease where reversible airway narrowing occur.

CONTRAINDICATIONS: Hypersensitivity to any of its components. Severe kidney and liver diseases. In certain rare diseases of the bronchi, which are accompanied by excessive accumulation of the secretions- eg. In malignant ciliary syndrome. Acute myo- cardial infarction.

SPECIAL PRECAUTIONS: History of prptic ulcer, Gastric ulceration. Thyrotoxicosis. Tachycardia in large doses. Severe cardiac disease, Severe hypoxemia. Hypertention. Cor-pulmonale. Liver diseases. Pregnancy and lactation.

ADVERSE EFFECTS:

Ambroxol: Gastrointestinal disorders. Allergic reactions- swelling, redness and itching on the skin and mucous membrane, shortness of breath, raised temperature accompanied by shivering. The concomitant ingestion of Ambroxol and antibiotics- amoxicillin, cefuroxime, erythromycin, doxycycline; can lead to improved passage of the antibiotics into the pulmonary tissue.

Salbutamol : In large doses peripheral vasodilatation. Salbutamol can cause fine tremors of skeletal muscles, particularly of the hands. A small increase of heart rate may occur due to large doses, but is not usually accompanied by any change in the ECG.

Theophylline : Adverse effects are usually due to overdose—eg, nausea, vomiting, epigastric pain, hematemesis and diarrhea, headache, irritability, restlessness, insomnia,hyperexcitability, muscle twitching and convulsions, palpitation, tachycardia, extrasystoles,flushing, hypotension, ventricular arrhythmias, tachypnea, alhuminuria, increased of renaltubular casts and red blood cells, hypcrglycemia and syndrome of inappropriate ADH secretion, hyponatremia, seizures.

SAFETY PROFILE : Tolerance dose not develops even after prolonged use if administered in therapeutic doses.

DRUG INTERACTIONS : With antitussives congestion of the secretions can occur due to the reduced coughing reflex. Ephedring of sympathomimetic preparations.

DOSAGE & ADMINISTRATION:

Adult: One tablet three to four times a day orally.
Children: Not recommended below 12-years of age.
Pregnancy: Use with caution.
Lactation: Use with caution.

STORAGE: Store in cool and dry place and protect from direct exposure to sunlight.