Ambroxol + Guaifenesin + Levosalbutamol

Usage

• This combination drug is primarily prescribed for the symptomatic relief of productive cough (cough with mucus) associated with respiratory conditions like bronchitis, asthma, chronic obstructive pulmonary disease (COPD), and lower respiratory tract infections (LRTIs) such as acute bronchitis, pneumonia, and tuberculosis. It helps loosen and clear mucus from the airways, making breathing easier.

• Pharmacological Classification: This is a combination of a bronchodilator (Levosalbutamol), a mucolytic agent (Ambroxol), and an expectorant (Guaifenesin).

• Mechanism of Action: Levosalbutamol relaxes the airway muscles, widening the airways. Ambroxol breaks down mucus, making it less viscous. Guaifenesin increases fluid secretion in the airways, thinning the mucus and aiding its expulsion.

Alternate Names

• No widely recognized alternate generic names exist. The combination is often referred to by its constituent drugs.
• Brand Names: Numerous brand names exist depending on the manufacturer and region. Examples include Ascoril LS, Eascof LS, Kofarest PD, Twigkof-LS, IFCOF-L, and TUSQ-LS.

How It Works

• Pharmacodynamics: Levosalbutamol, a beta-2 adrenergic agonist, relaxes bronchial smooth muscle, leading to bronchodilation. Ambroxol, a mucolytic, breaks down mucopolysaccharides in mucus, reducing its viscosity. Guaifenesin, an expectorant, increases respiratory tract fluid secretions, making mucus less sticky and easier to expectorate.

• Pharmacokinetics:

  • Absorption: Levosalbutamol is readily absorbed orally. Ambroxol and Guaifenesin are also well-absorbed from the gastrointestinal tract.
  • Metabolism: Levosalbutamol is minimally metabolized. Ambroxol undergoes hepatic metabolism. Guaifenesin is also metabolized in the liver.
  • Elimination: Levosalbutamol is primarily excreted renally. Ambroxol and Guaifenesin are excreted mainly in the urine.

• Mode of Action: Levosalbutamol acts by stimulating beta-2 adrenergic receptors in the lungs, leading to smooth muscle relaxation and bronchodilation. Ambroxol alters the structure and composition of mucus, reducing its viscosity. Guaifenesin enhances the production of thinner, less viscous secretions in the airways.

• Receptor binding, enzyme inhibition, or neurotransmitter modulation: Levosalbutamol binds to beta-2 adrenergic receptors. Ambroxol’s mechanism is related to altering mucus properties, not specific enzyme inhibition. Guaifenesin doesn’t involve specific receptor binding or neurotransmitter modulation; it works by increasing respiratory secretions.

• Elimination pathways: Levosalbutamol, Ambroxol, and Guaifenesin are primarily excreted renally, with some hepatic metabolism for Ambroxol and Guaifenesin.

Dosage

Standard Dosage

Adults:

• Syrup: 5-10 mL three times daily. Dosage depends on the specific formulation and the individual patient’s condition.

Children:

• 2-6 years: 2.5 mL three times a day.
• 6-11 years: 5 mL three times a day.
• Below 2 years: Use with caution and only as directed by a physician. Kofarest-PD drops may be an appropriate formulation for younger children.

Special Cases:

• Elderly Patients: Start with the lower end of the adult dose and increase cautiously as needed, based on clinical response and monitoring.
• Patients with Renal Impairment: Use with caution. Dose adjustment may be necessary.
• Patients with Hepatic Dysfunction: Use with caution. Dose adjustment may be necessary.
• Patients with Comorbid Conditions: Use with caution in patients with diabetes, hypertension, hyperthyroidism, cardiovascular disease, or peptic ulcers. Monitor accordingly.

Clinical Use Cases

Dosing in specific clinical situations should be individualized based on the patient’s needs and under the guidance of a physician. The combination is generally not indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations requiring immediate bronchodilation.

Dosage Adjustments

Adjustments should be made based on patient response and tolerability. Renal and hepatic impairment may necessitate lower doses.

Side Effects

Common Side Effects

• Nausea, vomiting, headache, dizziness, drowsiness, skin rash, tremor, stomach upset, diarrhea, dry mouth, throat irritation, palpitations, increased heart rate, sweating.

Rare but Serious Side Effects

• Allergic reactions (skin rash, itching, swelling), irregular heartbeat, seizures, angina, hypertension, tachycardia, nervousness, fatigue, insomnia.

Long-Term Effects

• Potential long-term effects are not well-established but may include worsening of underlying cardiovascular or metabolic conditions.

Adverse Drug Reactions (ADR)

• Clinically significant ADRs include severe allergic reactions, cardiac arrhythmias, and seizures.

Contraindications

• Hypersensitivity to any of the components.
• Severe coronary artery disease, certain cardiac arrhythmias.
• Hyperthyroidism, uncontrolled hypertension.
• Active peptic ulcer.
• Convulsive disorders.

Drug Interactions

• Beta-blockers (atenolol, metoprolol).
• MAO inhibitors (selegiline, linezolid).
• Digoxin, diuretics (furosemide, hydrochlorothiazide).
• Tricyclic antidepressants (amitriptyline).
• Other sympathomimetic bronchodilators (albuterol, formoterol).
• Antibiotics (erythromycin, doxycycline).
• Caffeine.

Pregnancy and Breastfeeding

• Safety during pregnancy and breastfeeding is not well-established. Use only if clearly needed and under the guidance of a physician.

Drug Profile Summary

• Mechanism of Action: Bronchodilation, mucolytic, expectorant.
• Side Effects: Nausea, vomiting, headache, dizziness, palpitations, allergic reactions.
• Contraindications: Hypersensitivity, severe heart disease, hyperthyroidism, peptic ulcer.
• Drug Interactions: Beta-blockers, MAO inhibitors, digoxin, diuretics, other sympathomimetics.
• Pregnancy & Breastfeeding: Use with caution if clearly needed.
• Dosage: Adults: 5-10 mL TID. Children: dose adjustments needed.
• Monitoring Parameters: Respiratory rate, oxygen saturation, heart rate, blood pressure, potassium levels.

Popular Combinations

This combination itself is a popular formulation. Sometimes, other medications might be added for specific conditions, such as corticosteroids for asthma exacerbations or antibiotics for bacterial infections.

Precautions

• Assess for allergies, cardiac, renal, or hepatic conditions before prescribing.
• Caution in pregnancy and breastfeeding.
• Avoid in children under 2 years without careful medical supervision.
• Monitor blood sugar in diabetic patients.
• Avoid alcohol and caffeine.
• May impair ability to drive or operate machinery.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Ambroxol + Guaifenesin + Levosalbutamol?

A: Adults: Typically 5-10 mL three times daily. Pediatric dosages vary by age and should be determined by a physician.

Q2: What are the common side effects?

A: Nausea, vomiting, headache, dizziness, dry mouth, palpitations.

Q3: Can this medication be used during pregnancy?

A: Use cautiously and only if clearly needed, as safety hasn’t been firmly established.

Q4: What are the contraindications for this drug?

A: Hypersensitivity, severe heart disease, hyperthyroidism, peptic ulcer.

Q5: What drug interactions are important to consider?

A: Beta-blockers, MAO inhibitors, digoxin, other sympathomimetics.

Q6: Can this combination be used for a dry cough?

A: It’s primarily indicated for productive cough. Consult a physician for a dry cough.

Q7: How long can this medication be used?

A: Generally for short-term symptom relief. Consult a physician for extended use.

Q8: Is it safe to drive while taking this medication?

A: It can cause dizziness or drowsiness, so caution is advised. Avoid driving if affected.

Q9: What should be done in case of an overdose?

A: Seek immediate medical attention. Symptoms may include dizziness, rapid heartbeat, and seizures.

Q10: Can this medicine be used in children under 2 years of age?

A: Use with extreme caution and only under strict medical supervision. Special formulations, like Kofarest-PD drops, may be more suitable. Consult a pediatrician.