Usage
Levocetirizine + Paracetamol is prescribed for the relief of symptoms associated with allergic conditions like allergic rhinitis (hay fever) and urticaria (hives), along with the reduction of fever and mild to moderate pain.
It is classified pharmacologically as an antihistamine and analgesic combination.
Levocetirizine works by blocking the action of histamine, a chemical mediator responsible for allergic symptoms. Paracetamol reduces fever and provides pain relief by inhibiting the production of prostaglandins, chemical messengers involved in pain and inflammation.
Alternate Names
This combination medication may sometimes be referred to as Levocetirizine/Paracetamol. Brand names vary depending on the manufacturer and region.
How It Works
Pharmacodynamics:
Levocetirizine: Selectively blocks peripheral histamine H1 receptors, reducing vascular permeability, itching, and other allergy symptoms. It demonstrates high affinity for the H1 receptor and minimal anticholinergic or serotonergic activity.
Paracetamol: Inhibits cyclooxygenase (COX) enzymes in the central nervous system, primarily COX-3, thereby decreasing prostaglandin synthesis. This action results in antipyretic and analgesic effects.
Pharmacokinetics:
Levocetirizine: Rapidly absorbed after oral administration. Peak plasma concentration is achieved in approximately 0.9 hours. Food intake does not significantly affect absorption. Metabolized to a minor extent and eliminated mainly through renal excretion, with a half-life of approximately 7-10 hours.
Paracetamol: Well-absorbed after oral administration, reaching peak plasma concentration in 10-60 minutes. It undergoes extensive hepatic metabolism, primarily via glucuronidation and sulfation, with a small fraction metabolized by cytochrome P450 enzymes to a potentially hepatotoxic metabolite. Primarily eliminated renally, with a half-life of about 2-4 hours.
Elimination Pathways:
Levocetirizine: Primarily renal excretion.
Paracetamol: Primarily renal excretion of metabolites.
Dosage
Standard Dosage
Adults:
A typical adult dose is one tablet containing 5 mg Levocetirizine and 500 mg or 650 mg Paracetamol, taken twice daily. The maximum daily dose of Paracetamol should not exceed 4000 mg.
Children:
Dosage in children is based on age and weight and should be determined by a healthcare professional.
Special Cases:
- Elderly Patients: Dose adjustments may be necessary due to age-related decline in renal function.
- Patients with Renal Impairment: Dosage reduction is required based on the degree of impairment.
- Patients with Hepatic Dysfunction: Caution is advised, and dose adjustment may be necessary for Paracetamol.
- Patients with Comorbid Conditions: Individualized dosing should be considered for patients with conditions such as cardiovascular disease, diabetes, glaucoma, or prostatic hypertrophy.
Clinical Use Cases
The combination of Levocetirizine and Paracetamol is not typically used in settings like intubation, surgery, mechanical ventilation, or emergency situations. In such cases, individual medications are preferred for more precise control of therapeutic effects.
Dosage Adjustments
Dosage adjustments are essential for patients with renal or hepatic impairment based on their specific condition and should be guided by clinical judgment and laboratory values.
Side Effects
Common Side Effects
- Drowsiness
- Dry mouth
- Headache
- Fatigue
- Nausea
Rare but Serious Side Effects
- Severe allergic reactions (anaphylaxis, angioedema)
- Hepatotoxicity (with Paracetamol overdose)
- Stevens-Johnson syndrome (SJS)
- Toxic epidermal necrolysis (TEN)
Long-Term Effects
Chronic use of high doses of Paracetamol can cause liver damage. Regular monitoring of liver function is recommended with prolonged use.
Adverse Drug Reactions (ADR)
Clinically significant ADRs like anaphylaxis and hepatotoxicity require immediate medical intervention.
Contraindications
- Hypersensitivity to Levocetirizine, Paracetamol, or any component of the formulation.
- Severe hepatic impairment or active liver disease.
- End-stage renal disease.
- Concurrent use of MAO inhibitors.
Drug Interactions
- Alcohol: Increases the risk of hepatotoxicity with Paracetamol and may enhance the sedative effects of Levocetirizine.
- Other CNS depressants: May potentiate the sedative effects of Levocetirizine.
- Hepatotoxic drugs: Increase the risk of liver damage when used with Paracetamol.
- Medications that affect liver enzymes: May alter the metabolism of Paracetamol.
Pregnancy and Breastfeeding
Levocetirizine: Pregnancy Category B. Use only if clearly needed.
Paracetamol: Generally considered safe for use during pregnancy and breastfeeding at recommended doses. However, consult a physician before use.
Drug Profile Summary
- Mechanism of Action: Levocetirizine: H1 receptor antagonist. Paracetamol: COX inhibitor, primarily COX-3.
- Side Effects: Drowsiness, dry mouth, headache, fatigue, nausea, hepatotoxicity (Paracetamol overdose).
- Contraindications: Hypersensitivity, severe liver disease, end-stage renal disease.
- Drug Interactions: Alcohol, CNS depressants, hepatotoxic drugs.
- Pregnancy & Breastfeeding: Use with caution. Consult a physician.
- Dosage: Adults: Levocetirizine 5 mg + Paracetamol 500/650 mg twice daily. Pediatric and renal/hepatic impairment: Dose adjustments required.
- Monitoring Parameters: Liver function tests (with prolonged Paracetamol use).
Popular Combinations
Levocetirizine is sometimes combined with other medications like Ambroxol and Phenylephrine for the treatment of cold and flu symptoms.
Precautions
- Evaluate renal and hepatic function before initiating therapy, especially in elderly patients.
- Caution patients about potential drowsiness and advise against operating machinery or driving.
- Advise patients not to exceed the recommended dose of Paracetamol.
- Avoid alcohol during treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Levocetirizine + Paracetamol?
A: The usual adult dose is one tablet containing Levocetirizine 5 mg and Paracetamol 500 or 650 mg, taken twice daily. Pediatric doses are determined by the child’s weight and age.
Q2: Can this medication be taken during pregnancy or while breastfeeding?
A: Consult a physician before using this medication during pregnancy or breastfeeding. While Paracetamol is generally considered safe, Levocetirizine should be used cautiously.
Q3: What are the common side effects?
A: Common side effects include drowsiness, dry mouth, headache, fatigue, and nausea.
Q4: Are there any serious side effects?
A: Serious side effects are rare but can include severe allergic reactions and liver damage (Paracetamol overdose).
Q5: Can I take this with alcohol?
A: Alcohol should be avoided as it increases the risk of liver damage with Paracetamol and may worsen the drowsiness caused by Levocetirizine.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it’s close to the time for your next dose. Do not double the dose.
Q7: How does this medication interact with other drugs?
A: It can interact with medications like other CNS depressants and hepatotoxic drugs. Consult your doctor about potential interactions.
Q8: Is this combination available over-the-counter?
A: Availability varies by region. It may be available over-the-counter or require a prescription.
Q9: How should this medication be stored?
A: Store at room temperature away from moisture and heat.
