Usage
- This fixed-dose combination medication is primarily prescribed for the management of respiratory conditions like asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm (including exercise-induced bronchospasm).
- Pharmacological Classification: Bronchodilator (combining a xanthine derivative and a β2-adrenergic agonist).
- Mechanism of Action: Choline theophyllinate inhibits phosphodiesterase, increasing intracellular cyclic AMP (cAMP), leading to bronchodilation and some anti-inflammatory effects. Salbutamol, a β2-agonist, stimulates β2-adrenergic receptors in the lungs, also causing bronchodilation. The combination provides synergistic bronchodilation.
Alternate Names
- While no standard international non-proprietary name (INN) exists for this specific combination, the components are individually recognized as Choline Theophyllinate (or Cholinophylline) and Salbutamol (or Albuterol in the US).
- Brand Names: Brand names vary regionally and may include Durasalyn, Airomol, and others. (Please note: Brand names are numerous and vary by region; this list is not exhaustive).
How It Works
- Pharmacodynamics: The combination exerts a synergistic bronchodilatory effect by relaxing the airway smooth muscle. Choline theophyllinate, by inhibiting phosphodiesterase, increases cAMP, which in turn relaxes bronchial smooth muscle and exerts some anti-inflammatory action. Salbutamol directly stimulates β2 receptors in the lungs, further promoting bronchodilation.
- Pharmacokinetics: Both drugs are absorbed from the gastrointestinal tract. Choline theophyllinate is metabolized in the liver and primarily excreted by the kidneys. Salbutamol is also metabolized in the liver and eliminated through the kidneys.
- Mode of Action: Choline theophyllinate inhibits phosphodiesterase enzymes. Salbutamol activates β2-adrenergic receptors.
- Receptor Binding/Enzyme Inhibition: Choline theophyllinate inhibits phosphodiesterase enzymes. Salbutamol binds to and activates β2-adrenergic receptors.
- Elimination Pathways: Both drugs are primarily eliminated through renal excretion after hepatic metabolism.
Dosage
Standard Dosage
Adults:
- Oral: Choline theophyllinate (as theophylline) 400-800 mg, with salbutamol 2-4 mg, 3-4 times daily. Dosage may be adjusted based on clinical response and theophylline levels.
Children:
- Dosing is weight/age-based and must be individualized. Theophylline levels should be monitored closely. Consult pediatric dosing guidelines.
Special Cases:
- Elderly Patients: Dose reduction may be needed due to reduced renal and hepatic function. Theophylline level monitoring is especially crucial.
- Patients with Renal Impairment: Dose adjustments according to renal clearance are required.
- Patients with Hepatic Dysfunction: Dose reduction and careful monitoring of theophylline levels are necessary.
- Patients with Comorbid Conditions: Caution is advised in patients with cardiovascular diseases, hyperthyroidism, diabetes, peptic ulcers, seizures, and other conditions.
Clinical Use Cases
- Dosage in specific clinical settings (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations) must be individualized based on the patient’s condition and response. No fixed guidelines exist. Theophylline levels should be monitored when possible.
Dosage Adjustments
- Dose modifications are crucial for patients with renal/hepatic impairment, and in those with other comorbidities affecting drug metabolism or clearance. Individualized therapy guided by clinical response and theophylline levels is essential.
Side Effects
Common Side Effects
- Nausea, vomiting, headache, tremors, nervousness, insomnia, palpitations, tachycardia.
Rare but Serious Side Effects
- Seizures, cardiac arrhythmias, severe hypokalaemia, paradoxical bronchospasm.
Long-Term Effects
- Potential for theophylline toxicity with chronic use, necessitating regular monitoring of serum theophylline levels.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (angioedema, urticaria), paradoxical bronchospasm, severe hypokalaemia.
Contraindications
- Hypersensitivity to theophylline, salbutamol, or any component of the formulation.
- Active peptic ulcer.
- Uncontrolled hyperthyroidism, severe hypertension, tachyarrhythmias.
Drug Interactions
- Xanthines (additive effects), β-blockers (antagonistic effects), certain antidepressants, cimetidine, fluvoxamine, macrolide antibiotics, quinolones, some antiarrhythmics. Consult a comprehensive drug interaction database for a full list.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Information is limited, generally use only if clearly needed and under careful supervision.
- Fetal Risks/Teratogenicity: Potential risks exist but not fully elucidated.
- Breastfeeding: Both drugs are excreted in breast milk; caution advised. Monitor infant for potential side effects.
- Discuss risks and benefits with the patient and consider safer alternatives if possible.
Drug Profile Summary
(See previous sections for details)
Popular Combinations
- While this is already a combination product, it might be prescribed concomitantly with inhaled corticosteroids, especially for persistent asthma or COPD.
Precautions
(See previous sections for details)
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Choline Theophyllinate + Salbutamol?
A: See dosage section.
Q2: What are the common side effects?
A: Common side effects include nausea, vomiting, headache, tremors, insomnia, palpitations, tachycardia, nervousness.
Q3: What are the contraindications?
A: Key contraindications include hypersensitivity, active peptic ulcer, uncontrolled hyperthyroidism, and certain cardiac arrhythmias.
Q4: Can this medication be used during pregnancy?
A: Use with caution during pregnancy; weigh the benefits against potential risks. Consult with the patient.
Q5: Is it safe during breastfeeding?
A: Both drugs are excreted in breast milk; use cautiously and monitor the infant.
Q6: What are the potential drug interactions?
A: Consult a comprehensive drug interaction database for a full list. Notable interactions include xanthines, β-blockers, certain antidepressants, and some antibiotics.
Q7: How should dosage be adjusted in patients with renal impairment?
A: Dosage must be adjusted based on renal clearance. Monitor theophylline levels when possible.
Q8: What monitoring is required during long-term therapy?
A: Regular monitoring of serum theophylline levels is important to avoid toxicity.
Q9: How should this medication be administered?
A: Administer orally, usually 3-4 times a day.
Q10: Is this combination more effective than its individual components?
A: Yes, the combination produces synergistic bronchodilation, offering potentially superior efficacy compared to monotherapy with either drug.
