N-Kast-L Dispersible Tablets

Description

N-Kast-L Dispersible Tablets (Montelukast 5mg & Levocetirizine 2.5mg) – Complete Reference

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1. Pharmacokinetics

Montelukast (5mg):

Absorption: Rapidly absorbed after oral administration. Peak plasma concentrations are typically reached within 3–4 hours.

Distribution: Widely distributed in plasma, highly protein-bound (approximately 99%).

Metabolism: Metabolized in the liver, primarily via cytochrome P450 enzymes, particularly CYP3A4.

Excretion: Excreted mainly through the feces (~86%), with a small amount excreted via the urine (~6%).

Half-life: Approximately 2.7 to 5.5 hours.

Levocetirizine (2.5mg):

Absorption: Levocetirizine is rapidly absorbed after oral administration, with peak plasma concentrations occurring in about 0.9 hours.

Distribution: Levocetirizine is moderately protein-bound (~90%) and is distributed widely throughout the body.

Metabolism: Minimal metabolism; it is primarily excreted unchanged in the urine.

Excretion: Excreted mainly unchanged via the urine.

Half-life: Approximately 8 hours in healthy adults.

 

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2. Pharmacodynamics

Montelukast (5mg):

Class: Leukotriene receptor antagonist.

Action: Montelukast selectively inhibits cysteinyl leukotriene receptors (CysLT1), preventing the effects of leukotrienes that play a key role in inflammation and bronchoconstriction in asthma and allergic rhinitis.

Effect: Reduces airway inflammation, alleviates bronchoconstriction, and improves respiratory symptoms.

Levocetirizine (2.5mg):

Class: Second-generation antihistamine.

Action: Levocetirizine is a selective H1-antagonist, meaning it blocks the action of histamine, a chemical that promotes allergic reactions.

Effect: Provides relief from allergy symptoms such as sneezing, itching, and runny nose by preventing histamine-mediated inflammation.

 

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3. Clinical Indications

Allergic Rhinitis: Relief from symptoms of seasonal and perennial allergic rhinitis, such as sneezing, itching, and nasal congestion.

Asthma: Management of asthma symptoms, especially for controlling exercise-induced bronchoconstriction and overall lung function.

Chronic Urticaria: Treatment of chronic hives, providing relief from itching and discomfort.

Other Allergic Conditions: Useful in managing symptoms of other allergic conditions like allergic conjunctivitis.

 

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4. Dosage Recommendations

Adults and Children (12 years and above):

Asthma & Allergic Rhinitis: 1 dispersible tablet (5mg Montelukast & 2.5mg Levocetirizine) once daily, preferably in the evening.

Children (6 to 12 years):

Asthma & Allergic Rhinitis: 1 dispersible tablet (5mg Montelukast & 2.5mg Levocetirizine) once daily, preferably in the evening.

Administration: The dispersible tablet should be dissolved in a small amount of water or taken directly. It should be taken once a day, preferably in the evening, to control allergic symptoms and improve breathing.

 

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5. Safety Precautions

Allergy: Contraindicated in patients with hypersensitivity to Montelukast, Levocetirizine, or any of the components of the formulation.

Renal Impairment: Use with caution in patients with severe renal impairment. Levocetirizine clearance may be reduced in such patients.

Hepatic Impairment: Use with caution in patients with liver disease; no dose adjustment is required for Montelukast but monitor carefully.

Pregnancy and Lactation: Montelukast is classified as Category B during pregnancy. Levocetirizine should be used cautiously during pregnancy and lactation. Consult a healthcare provider before use.

CNS Effects: Levocetirizine may cause drowsiness. Caution is advised when performing tasks requiring alertness, such as driving or operating machinery.

Neuropsychiatric Effects: Montelukast has been associated with mood changes, depression, anxiety, and aggressive behavior, especially in children. Close monitoring is recommended.

 

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6. Side Effects

Montelukast (5mg):

Common: Headache, abdominal pain, fatigue, dizziness, and sore throat.

Serious (rare): Neuropsychiatric symptoms such as aggression, agitation, hallucinations, depression, and suicidal thoughts.

Levocetirizine (2.5mg):

Common: Drowsiness, dry mouth, headache, dizziness, and fatigue.

Serious (rare): Tachycardia, difficulty urinating, allergic reactions (e.g., rash, swelling), and difficulty breathing.

 

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7. Storage and Stability

Storage: Store below 30°C in a dry place, away from direct sunlight.

Shelf-life: 2–3 years.

Reconstituted Solution: Use immediately after reconstitution. Can be stored at 2–8°C for up to 6 hours.

Note: Keep out of reach of children. Do not freeze.

 

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8. Overdose Management

Symptoms of Overdose: Overdose may cause excessive drowsiness, agitation, or restlessness.

Treatment: Symptomatic treatment is required. There is no specific antidote. Monitor vital signs, and provide supportive care as necessary.

 

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9. Additional Notes

Drug Interactions: Montelukast may interact with other medications metabolized by the cytochrome P450 system. Levocetirizine may increase the sedative effects of CNS depressants.

Monitoring: Monitor renal function in patients with renal impairment, and be vigilant for any neuropsychiatric symptoms in pediatric patients using Montelukast for long periods.

Patient Advice: Patients should report severe side effects such as unusual bruising, jaundice, severe diarrhea, or any signs of a serious allergic reaction (e.g., swelling, rash, difficulty breathing)