Usage
- This combination medication is primarily prescribed for the symptomatic relief of dry cough. It is also sometimes used to alleviate cough associated with allergies.
- Pharmacological Classification: Antitussive (Levocloperastine) and Antihistamine (Chlorpheniramine Maleate)
- Mechanism of Action: Levocloperastine suppresses cough by acting on the cough center in the brain. Chlorpheniramine maleate provides relief from allergy symptoms, which may contribute to cough, by blocking the action of histamine.
Alternate Names
- No widely recognized alternate names for this specific combination exist.
- Brand Names: Lupituss CPM, Asvitus-LC, Dropolev (with Levodropropizine, a similar antitussive)
How It Works
- Pharmacodynamics: Levocloperastine acts centrally on the cough center in the medulla oblongata, reducing the urge to cough. Chlorpheniramine maleate antagonizes the H1 histamine receptor, reducing the effects of histamine release, such as sneezing, runny nose, and watery eyes.
- Pharmacokinetics: Both drugs are absorbed orally. Levocloperastine’s metabolism and elimination pathways are not fully elucidated. Chlorpheniramine is metabolized in the liver and primarily excreted renally.
- Mode of Action: Levocloperastine peripherally blocks cough receptors while acting centrally on the cough center in the brain. Chlorpheniramine maleate competes with histamine for H1-receptor sites on effector cells, thus preventing the effects of histamine.
- Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Levocloperastine affects peripheral cough receptors and central cough centers, without significant respiratory depression. Chlorpheniramine competitively binds to H1 receptors.
- Elimination Pathways: Levocloperastine’s elimination is not fully characterized. Chlorpheniramine is metabolized in the liver, likely involving CYP450 enzymes, and primarily excreted in the urine.
Dosage
Standard Dosage
Adults:
- The typical adult dosage is 20 mg levocloperastine and 4 mg chlorpheniramine maleate, administered orally, two to three times daily. Do not exceed 60 mg of levocloperastine per day.
Children:
- The dosage should be adjusted based on the child’s age and weight and is typically 1 mg of levocloperastine per kg of body weight, thrice daily. Its use is generally not recommended for children under 8 years old, and caution should be used in children under 12 years of age.
Special Cases:
- Elderly Patients: Start with lower doses due to potential increased sensitivity to side effects like drowsiness and confusion.
- Patients with Renal Impairment: Caution is advised, and dose adjustment might be needed.
- Patients with Hepatic Dysfunction: Caution and dose adjustments are necessary.
- Patients with Comorbid Conditions: Close monitoring is warranted, especially for patients with cardiovascular disease, hypertension, diabetes, or hyperthyroidism.
Clinical Use Cases
- The combination is not typically indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use is primarily for symptomatic relief of dry cough.
Dosage Adjustments
- Adjust based on patient response and tolerance, considering renal and hepatic function, comorbid conditions, and drug interactions.
Side Effects
Common Side Effects
- Drowsiness, dizziness, headache, nausea, dry mouth, blurred vision, constipation.
Rare but Serious Side Effects
- Allergic reactions (rash, itching, swelling), difficulty breathing, irregular heartbeat, seizures.
Long-Term Effects
- Not well established, but potential for dependence with prolonged use of certain antitussives should be considered.
Adverse Drug Reactions (ADR)
- Severe allergic reactions, cardiac arrhythmias, seizures.
Contraindications
- Hypersensitivity to levocloperastine or chlorpheniramine, pregnancy, concurrent use of MAO inhibitors, severe respiratory compromise, narrow-angle glaucoma, urinary retention, prostatic hypertrophy.
Drug Interactions
- Alcohol, other CNS depressants (e.g., sedatives, hypnotics, opioids), antihistamines, MAO inhibitors, medications metabolized by CYP450 enzymes.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not established for levocloperastine. Chlorpheniramine is generally considered Category B but should be used cautiously.
- Fetal Risks: Potential for adverse effects, though limited data are available.
- Drug excretion in breast milk: Both drugs can be excreted in breast milk, potentially causing drowsiness or other effects in infants.
- Safer alternatives: Dextromethorphan or guaifenesin might be considered as alternatives.
Drug Profile Summary
- Mechanism of Action: Levocloperastine: Central and peripheral antitussive. Chlorpheniramine: H1-receptor antagonist.
- Side Effects: Drowsiness, dizziness, dry mouth, nausea, blurred vision.
- Contraindications: Hypersensitivity, pregnancy, MAOI use.
- Drug Interactions: CNS depressants, alcohol, antihistamines.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: Adults: 20 mg/4mg two to three times daily. Children: Weight-based dosing, not generally recommended for younger children.
- Monitoring Parameters: Respiratory status, heart rate, blood pressure, mental status.
Popular Combinations
- While this is a combination product, it is not commonly combined with other drugs for cough.
Precautions
- Evaluate renal and hepatic function, assess for concomitant medications, monitor for side effects. Advise against driving or operating machinery if drowsiness occurs. Caution in patients with cardiovascular or respiratory conditions. Avoid alcohol.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Chlorpheniramine Maleate + Levocloperastine?
A: Adults: 20 mg levocloperastine/4 mg chlorpheniramine maleate two to three times per day. Children: Weight-based dosing (1 mg/kg of levocloperastine thrice daily), use with caution, especially in younger children.
Q2: What are the common side effects?
A: Drowsiness, dizziness, dry mouth, nausea, blurred vision, constipation.
Q3: Is it safe to use during pregnancy or breastfeeding?
A: Caution is advised. Consult a doctor to weigh the benefits against potential risks. Safer alternatives may be considered.
Q4: Can I drink alcohol while taking this medication?
A: No, alcohol can exacerbate side effects such as drowsiness and dizziness.
Q5: What should I do if I experience severe side effects?
A: Seek immediate medical attention.
Q6: Can this medication be used for a productive cough?
A: It is primarily indicated for dry cough. It might not be appropriate for productive cough.
Q7: Are there any drug interactions I should be aware of?
A: Yes. Inform your physician about all other medications you are taking, including over-the-counter drugs and supplements. Significant interactions can occur with CNS depressants, alcohol, antihistamines, and MAOIs.
Q8: How long should I take this medication?
A: Use it for the duration prescribed by your physician. Generally, for short-term symptomatic relief. Consult your doctor if symptoms persist beyond seven days.
Q9: What are the contraindications for using this medicine?
A: Contraindications include hypersensitivity to either component, pregnancy, concurrent use of MAOIs, and certain medical conditions such as narrow-angle glaucoma, urinary retention, and prostatic hypertrophy.
Q10: Can children take this medicine?
A: It’s generally not recommended for children under 8 years of age. For older children, the dosage needs careful adjustment based on weight and age. Consult a pediatrician.
