Usage
- This drug is prescribed for respiratory conditions like asthma, chronic bronchitis, and emphysema (COPD). It helps manage symptoms such as wheezing, coughing, chest tightness, and shortness of breath.
- Pharmacological Classification: Bronchodilator and Expectorant. It combines a bronchodilator (Salbutamol) and an expectorant (Guaifenesin).
- Mechanism of Action: Etofylline is a xanthine derivative that acts as a weak bronchodilator and anti-inflammatory agent. Salbutamol is a beta-2 adrenergic agonist, relaxing the airways’ muscles. Guaifenesin reduces mucus viscosity, facilitating expectoration.
Alternate Names
- No widely recognized alternate names exist for this specific combination.
- Brand Names: Derivent E, Deriphylline-G
How It Works
- Pharmacodynamics: Salbutamol relaxes bronchial smooth muscle by stimulating beta-2 adrenergic receptors. Etofylline inhibits phosphodiesterase, increasing intracellular cAMP, which also leads to bronchodilation. Guaifenesin increases respiratory tract fluid secretions, making the mucus less viscous and easier to expectorate.
- Pharmacokinetics: All three drugs are absorbed orally. Salbutamol and Etofylline are metabolized in the liver. Guaifenesin is excreted unchanged in the urine.
- Mode of Action: Salbutamol acts on beta-2 receptors in the lungs, activating adenylate cyclase and increasing cAMP, resulting in bronchodilation. Etofylline inhibits phosphodiesterase, also leading to increased cAMP. Guaifenesin’s mechanism is not fully understood but involves altering the properties and production of mucus.
- Elimination Pathways: Salbutamol is primarily eliminated renally. Etofylline is metabolized and excreted in the urine. Guaifenesin is excreted largely unchanged in the urine.
Dosage
Standard Dosage
Adults:
- The usual dose is one tablet/5-10ml syrup two to three times daily. Dosages may differ based on the brand.
- The maximum dose is usually up to four times a day, under medical supervision.
Children:
- Dosage is typically weight-based and requires careful calculation by a healthcare professional. The general recommendation is 1 to 2 mg salbutamol per dose.
- It is crucial to consider the strength of the medication based on the child’s weight and age.
- Safety must be carefully assessed for pediatric usage, considering potential side effects such as tremors and hyperactivity.
Special Cases:
- Elderly Patients: Start with lower doses and adjust based on the patient’s response and renal function.
- Patients with Renal Impairment: Dose adjustment is necessary; consult a nephrologist for tailored recommendations based on the level of renal impairment.
- Patients with Hepatic Dysfunction: Reduce the dose based on the severity of dysfunction, with close monitoring of liver function tests.
- Patients with Comorbid Conditions: Patients with hypertension, diabetes, thyroid issues, glaucoma, or heart disease should be monitored closely.
Clinical Use Cases
- Typically not used for intubation, surgical procedures, mechanical ventilation, or in the ICU or emergency settings in this combined form. Salbutamol may be used independently via nebulizer or injection in these settings.
Dosage Adjustments
- Adjust doses based on individual patient factors such as age, weight, renal function, and comorbid conditions.
- Genetic polymorphisms impacting drug metabolism may necessitate further dose individualization.
Side Effects
Common Side Effects:
- Nausea, vomiting, diarrhea, restlessness, headache, rash, tremor, muscle cramps, palpitations, increased heart rate, dizziness, and trouble sleeping.
Rare but Serious Side Effects:
- Allergic reactions (swelling, difficulty breathing, skin rash), irregular heartbeat.
Long-Term Effects:
- Potential for tolerance with prolonged use of salbutamol.
Adverse Drug Reactions (ADR):
- Severe allergic reactions, paradoxical bronchospasm, hypokalemia, hyperglycemia, and cardiac arrhythmias.
Contraindications
- Hypersensitivity to any component of the medication.
- Severe heart disease, uncontrolled hypertension, hyperthyroidism, and certain types of glaucoma.
Drug Interactions
- Beta-blockers (propranolol, atenolol), MAO inhibitors (phenelzine), tricyclic antidepressants (amitriptyline), diuretics, digoxin, corticosteroids, and some antibiotics.
- Caffeine can exacerbate side effects.
Pregnancy and Breastfeeding
- Consult a doctor before using during pregnancy or breastfeeding. Limited data suggest potential risks; use only if benefits clearly outweigh risks.
- Animal studies indicate potential fetal risks.
- Salbutamol is excreted in breast milk; consider potential neonatal effects.
Drug Profile Summary
- Mechanism of Action: Bronchodilation (Salbutamol, Etofylline), Expectorant (Guaifenesin).
- Side Effects: Nausea, vomiting, tremor, headache, palpitations.
- Contraindications: Hypersensitivity, severe heart disease, uncontrolled hypertension.
- Drug Interactions: Beta-blockers, MAO inhibitors, caffeine.
- Pregnancy & Breastfeeding: Consult doctor, potential risks.
- Dosage: Adult: 1 tablet or 5ml-10ml syrup, 2-3 times/day, as directed by the physician. Pediatric: weight-based.
- Monitoring Parameters: Respiratory function, heart rate, blood pressure, potassium levels, and blood glucose (in diabetics).
Popular Combinations
- Not typically combined with other drugs due to the fixed combination nature of this product.
Precautions
- Pre-existing heart, liver, or kidney conditions should be evaluated before starting the medication.
- Monitor for potential adverse effects, especially in elderly and pediatric patients.
- Advise against driving or operating machinery until the effects are known.
- Caution patients about caffeine intake and its potential interaction.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Etofylline + Guaifenesin + Salbutamol?
A: Adults: One tablet/5-10ml syrup two to three times daily. Children: weight-based. Elderly and patients with comorbidities: Start with lower doses.
Q2: What are the common side effects?
A: Nausea, vomiting, tremors, headache, and palpitations are common side effects.
Q3: Can this drug be taken during pregnancy?
A: Consult a doctor before use during pregnancy.
Q4: What are the contraindications for this medication?
A: Hypersensitivity, severe heart disease, and uncontrolled hypertension are contraindications.
Q5: How does this medication interact with other drugs?
A: It interacts with beta-blockers, MAO inhibitors, and caffeine.
Q6: Can I take this medicine with food?
A: It can be taken with or without food but preferably at the same time each day.
Q7: Is it safe to drive after taking this medicine?
A: Caution is advised as it may cause dizziness. Avoid driving if such side effects are experienced.
Q8: Is it addictive?
A: It is generally not considered addictive but always follow the doctor’s prescription.
Q9: What should I do if I miss a dose?
A: Take the missed dose as soon as remembered, unless it’s close to the next dose. Don’t double the dose.
