Bisolpent

Uses

Bromhexineis used for the treatment of respiratory disorders associated with productive cough. These include; tracheobronchitis, bronchitis with emphysema, bronchiectasis, bronchitis with bronchospasm, chronic inflammatory pulmonary conditions and pneumoconiosis.

Orciprenaline is a beta-2 adrenergic agonist used to treat bronchospasm, asthma, and COPD.

For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.

Bisolpent is also used to associated treatment for these conditions: Bronchiectasis, Common Cold, Cough, Cough caused by Common Cold, Nasal Congestion, Whooping Cough, Airway secretion clearance therapyAsthma, Bronchospasm, Chronic Bronchitis, Pulmonary Emphysema

How Bisolpent works

Inflammation of the airways, increased mucus secretion, and altered mucociliary clearance are the hallmarks of various diseases of the respiratory tract. Mucus clearance is necessary for lung health; bromhexine aids in mucus clearance by reducing the viscosity of mucus and activating the ciliary epithelium, allowing secretions to be expelled from the respiratory tract.

Recent have studies have demonstrated that bromhexine inhibits the transmembrane serine protease 2 receptor (TMPRSS2) in humans. Activation of TMPRSS2 plays an important role in viral respiratory diseases such as influenza A and Middle East Respiratory Syndrome (MERS). Inhibition of receptor activation and viral entry by bromhexine may be effective in preventing or treating various respiratory illnesses, including COVID-19. In vitro studies have suggested the action of ambroxol (a metabolite of bromhexine) on the angiogensin-converting enzyme receptor 2 (ACE2), prevents entry of the viral envelope-anchored spike glycoprotein of SARS-Cov-2 into alveolar cells or increases the secretion of surfactant, preventing viral entry.

Orciprenaline stimulates the β2-adrenergic receptor expressed in the lungs, uterus, and vasculature supplying skeletal muscles by acting as a moderately selective agonist. It exerts minimal or no effect on alpha-adrenergic receptors. Intracellularly, the actions of orciprenaline are mediated by cAMP, the production of which is augmented by beta stimulation. The drug is believed to work by activating adenylate cyclase, the enzyme responsible for producing the cellular mediator cAMP.

Dosage

Bisolpent dosage

BromhexineTablet:

Adults and children over 10 years: 8-16 mg 3 times daily. Children 5-10 years: 4 mg 3 times daily.

BromhexineSyrup:

Adults: The recommended daily dose is 2 to 4 teaspoonful 3 times. Initially 4 teaspoonful 3 times daily and then as required.

Children: Suggested dosage for children under 2 years is 1/4 teaspoonful 3 times daily, for 2-5 years 1/2 teaspoonful 3 times daily and for children aged 5-10 years 1 teaspoonful 3 times daily.

Side Effects

Gastrointestinal side-effects may occur occasionally with Bromhexine and a transient rise in serum aminotransferase values has been reported. Other reported adverse effects include headache, dizziness, sweating and skin rash.

Toxicity

The oral LD50 of bromhexine in rats is 6 g/kg. The observed symptoms of accidental overdose with bromhexine are consistent with the known adverse effects of bromhexine, including headache, nausea, and vomiting, among other symptoms. Provide symptomatic treatment and contact poison control services if an overdose is confirmed or suspected.

Symptoms of overdose include angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. LD₅₀=42 mg/kg (orally in rat).

Precaution

Since mucolytics may disrupt the gastric mucosa so Bromhexine should be used with care in patients with a history of peptic ulceration.

Volume of Distribution

After intravenous administration in a pharmacokinetic study, bromhexine was found to be widely distributed. Bromhexine is known to cross the blood-brain barrier; small concentrations may cross the placenta. The average volume of distribution of bromhexine was 1209 ± 206 L (19 L/kg). Lung tissue concentrations of bromhexine two hours after a dose were 1.5 to 3.2 times higher in bronchial tissues than plasma concentrations. Pulmonary parynchema concentrations were 3.4 to 5.9 times higher when compared to plasma concentrations.

Elimination Route

After oral administration, bromhexine demonstrates linear pharmacokinetics when given in doses of 8-32 mg. Bromhexine is readily absorbed in the gastrointestinal tract at a rapid rate. This drug undergoes extensive first-pass effect in the range of 75-80%. The bioavailability is therefore reduced to approximately 22-27%.

3% (oral bioavailability of 40%)

Half Life

Following single oral doses ranging from 8 and 32 mg, the terminal half-life of bromhexine has been measured between 6.6 and 31.4 hours.

6 hours

Clearance

The clearance of bromhexine ranges from 843-1073 mL/min, within the range of the hepatic circulation.

Elimination Route

After a dose of bromhexine was administered during a pharmacokinetic study, approximately 97% of the radiolabeled dose was detected in the urine; under 1% was detected as the parent drug.

Pregnancy & Breastfeeding use

Pregnancy Category B. Bromhexine has been taken by a large number of pregnant women and women of child bearing age without any proven increase in the frequency of malformations or other direct or indirect harmful effects on the fetus having been observed.

It is not known whether bromhexine is excreted in breast milk or whether it has a harmful effect on the breastfeeding infant. Therefore it is not recommended for breast feeding mothers unless the potential benefits to the patient are weighed against the possible risk to the infant.

Contraindication

Contraindicated to those who are hypersensitive to Bromhexine Hydrochloride.

Storage Condition

Store below 25° C. Protect from light. Keep the container tightly closed.

Innovators Monograph

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