Usage
This combination medication is primarily prescribed for the treatment of respiratory conditions like asthma, chronic bronchitis, and emphysema (COPD). It helps manage symptoms such as wheezing, coughing, shortness of breath, and chest tightness. Pharmacologically, this is classified as a bronchodilator and works by relaxing and widening the airways in the lungs.
Alternate Names
While “Etofylline + Salbutamol + Theophylline” accurately represents the drug’s composition, no formally recognized alternate names exist. Brand names may vary depending on the manufacturer and region. One example is Deriphyllin S.
How It Works
Pharmacodynamics: This combination exerts its bronchodilatory effects through multiple mechanisms. Etofylline, a xanthine derivative, inhibits phosphodiesterase enzymes, increasing intracellular cyclic AMP levels, leading to bronchial smooth muscle relaxation. Theophylline, another xanthine derivative, acts similarly but also has anti-inflammatory properties and reduces airway responsiveness to allergens. Salbutamol, a beta-2 adrenergic receptor agonist, directly stimulates beta-2 receptors in the lungs, further relaxing bronchial smooth muscles and widening the airways.
Pharmacokinetics: Etofylline and theophylline are absorbed orally, while salbutamol can be administered orally or via inhalation. Metabolism primarily occurs in the liver, with theophylline being metabolized by CYP450 enzymes. Elimination pathways are primarily renal. Theophylline has a narrow therapeutic index, requiring careful dosage adjustments.
Dosage
Dosage guidelines are complex and should be individualized based on patient factors. Blood serum monitoring of Theophylline levels is crucial to avoid toxicity.
Standard Dosage
Adults: Standard dosage for adults has not been found in the provided sources for this combination. Dosage should be carefully titrated based on Theophylline serum level and patient response.
Special Cases:
- Elderly Patients: Reduced dosages are often necessary due to age-related decline in metabolic function and organ function.
- Patients with Renal Impairment: Dose adjustments based on creatinine clearance are essential to avoid accumulation and toxicity.
- Patients with Hepatic Dysfunction: Impaired metabolism necessitates careful dosing adjustments.
- Patients with Comorbid Conditions: Conditions like heart disease, hypertension, diabetes, hyperthyroidism, and seizure disorders require caution and individualized dosing strategies.
Clinical Use Cases
The provided sources do not offer specific dosage recommendations for clinical scenarios like intubation, surgery, mechanical ventilation, or ICU use. It can be used in emergency situations for acute bronchospasms as outlined below. The specific dosage must be individualized and titrated under medical supervision.
For Acute Bronchospasm, if the patient is not currently taking Theophylline, an intravenous or oral loading dose of 5-7 mg/kg is administered (not to exceed 25 mg/min IV). If the patient is taking Aminophylline, the loading dose is 6-7mg/kg IV infused over 20 minutes.
Dosage Adjustments
As stated before, dose modification is based on patient factors like renal or hepatic dysfunction. Smokers, patients with congestive heart failure, and those receiving drugs impacting theophylline clearance will also require dose adjustments.
Side Effects
Common Side Effects: Nausea, vomiting, headache, restlessness, dizziness, increased heart rate, insomnia, nervousness, tremors, gastrointestinal upset.
Rare but Serious Side Effects: Seizures, irregular heartbeats, fainting, confusion, severe allergic reactions (rash, itching/swelling, difficulty breathing), severe dizziness.
Long-Term Effects: Not explicitly documented for this particular combination, but chronic theophylline use can potentially lead to complications like cardiac arrhythmias.
Contraindications
Hypersensitivity to any component, severe liver or kidney disease, certain cardiac arrhythmias, coronary insufficiency, history of heart attack.
Drug Interactions
Multiple drug interactions are possible. Avoid concurrent use with other xanthines, beta-blockers, certain antidepressants (MAOIs, TCAs), diuretics, cardiac glycosides, corticosteroids, some antibiotics (quinolones, macrolides), and certain antifungals. Caffeine, alcohol, and smoking can also interact. Consult a comprehensive drug interaction checker for detailed information.
Pregnancy and Breastfeeding
Use with caution only if benefits outweigh risks. Fetal risks are not well-established, but animal studies suggest potential harm. Consult your doctor for alternative safer options.
Drug Profile Summary
- Mechanism of Action: Bronchodilation via phosphodiesterase inhibition (etofylline, theophylline) and beta-2 receptor stimulation (salbutamol).
- Side Effects: Nausea, vomiting, headache, dizziness, increased heart rate, insomnia, nervousness, tremors, rarely seizures or severe allergic reactions.
- Contraindications: Hypersensitivity, severe liver/kidney disease, certain cardiac conditions.
- Drug Interactions: Numerous, including other xanthines, beta-blockers, antidepressants, antibiotics.
- Pregnancy & Breastfeeding: Use with caution only if benefits outweigh risks.
- Dosage: Individualized based on patient factors and Theophylline serum levels; requires careful titration.
- Monitoring Parameters: Theophylline serum levels, heart rate, respiratory rate, electrolyte concentrations, blood gases (especially during prolonged IV therapy).
Popular Combinations
This combination itself is a popular choice for managing respiratory conditions.
Precautions
- General Precautions: Careful monitoring of Theophylline levels, cardiac and respiratory function.
- Specific Populations: Pregnant/breastfeeding women – use cautiously. Children and elderly – dosage adjustments needed.
- Lifestyle Considerations: Avoid alcohol, smoking, and excessive caffeine intake.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Etofylline + Salbutamol + Theophylline?
A: Dosage needs to be determined on a case-by-case basis considering patient specifics, underlying medical condition, and serum monitoring of Theophylline levels.
Q2: What are the primary uses of this combination?
A: It is primarily used to treat respiratory conditions, including asthma, chronic bronchitis, and COPD.
Q3: What are the most common side effects?
A: Nausea, vomiting, headache, tremor, insomnia, nervousness, dizziness, and increased heart rate are commonly reported.
Q4: Are there any serious side effects I should be aware of?
A: Yes, although rare, seizures, cardiac arrhythmias, and severe allergic reactions can occur. These warrant immediate medical attention.
Q5: Can this medication be taken during pregnancy?
A: It should be used with extreme caution during pregnancy and only if the potential benefits outweigh the risks to the fetus. Discuss alternatives with your physician.
Q6: What are the major contraindications for its use?
A: Hypersensitivity to any of the components, severe liver or kidney disease, and certain cardiac conditions are major contraindications.
Q7: Does it interact with other medications?
A: Yes, it interacts with numerous medications, including other xanthines, beta-blockers, some antibiotics, and certain antidepressants. Always provide a complete medication history to your physician.
Q8: Are there any dietary restrictions I should advise my patients to follow?
A: Limit caffeine intake from coffee, tea, or chocolate, as it can exacerbate side effects. Advise patients to maintain adequate hydration and a balanced diet.
Q9: What is the mechanism of action of the combination?
A: Etofylline and theophylline inhibit phosphodiesterase enzymes and relax the airway’s smooth muscles. Salbutamol directly stimulates beta-2 receptors in the lungs, leading to bronchodilation.
Q10: How is the drug metabolized and eliminated from the body?
A: Metabolism primarily occurs in the liver, with theophylline being metabolized by the CYP450 enzyme system. Elimination is mainly through the kidneys.
