Actif Cap 20 mg 14’s (Ebastine)-Potential overview

Pharmaceutical Class

• Class: Antihistamine (Second-generation H1-antagonist)
• Type: Non-sedating antihistamine

Indications for Use

• Seasonal Allergic Rhinitis: Provides relief from symptoms such as sneezing, itching, and runny nose due to seasonal allergies.
• Perennial Allergic Rhinitis: Relief from year-round allergic rhinitis symptoms, including nasal congestion and watery eyes.
• Chronic Urticaria: Reduces itching and hives associated with chronic urticaria (chronic hives).
• Other Allergic Conditions: Provides symptom relief in various allergic conditions, especially those involving histamine release.

Common Side Effects

• Headache
• Dry mouth
• Drowsiness (although less frequent compared to first-generation antihistamines)
• Fatigue
• Nausea

Serious Side Effects (Less Common)

• Severe allergic reactions: Rash, swelling of the face, lips, or tongue, difficulty breathing.
• Cardiovascular effects: Arrhythmia, tachycardia, and other heart rhythm disturbances.
• Dizziness or fainting: In rare cases, dizziness and fainting episodes may occur.
• Liver dysfunction: Uncommon, but could include jaundice or abnormal liver function tests.

Dosage

• Adults and Children over 12 years: 10 mg once daily.
• Pediatric Use: Generally not recommended for children under 12 years of age unless otherwise prescribed by a healthcare provider.
• Hepatic Impairment: Dose adjustment may be required for individuals with hepatic dysfunction.

Usage Instructions

• Take Actif Cap 20 mg once daily, preferably at the same time each day.
• The capsule may be taken with or without food, but should be swallowed whole. Do not chew or break the capsule.
• Missed Dose: If a dose is missed, take it as soon as remembered, unless it is almost time for the next dose. Do not take two doses at once.

Drug Interactions

• With Food: Food does not significantly affect the bioavailability of ebastine but may delay the onset of action when taken with a high-fat meal.
• With Other Medications:
  • CYP3A4 Inhibitors: Medications like ketoconazole, itraconazole, or erythromycin may increase the plasma concentration of ebastine, increasing the risk of side effects.
  • CNS Depressants: Caution with alcohol and other central nervous system depressants, as they may amplify drowsiness effects.
  • Other Antihistamines: Combining with other antihistamines may increase the risk of side effects such as drowsiness and dry mouth.
  • Antiarrhythmic Drugs: Caution is advised if taking drugs that affect heart rhythm due to the risk of arrhythmias.

Regulatory Approval and Manufacturer

• Regulatory Approval: Ebastine has been approved by regulatory authorities for use in the treatment of allergic rhinitis and urticaria.
• Manufacturer: Produced and marketed by various pharmaceutical companies that specialize in allergy and antihistamine products.

Pharmacist-Related Data

Drug Name and Chemical Details

• Generic Name: Ebastine
• Chemical Formula: C22H26ClN1O2
• Molecular Weight: 365.91 g/mol
• CAS Number: 97791-29-8

Pharmacodynamics

• Mechanism of Action: Ebastine works by selectively blocking H1 histamine receptors. Histamine is a chemical released during allergic reactions, and it plays a key role in symptoms such as itching, swelling, and fluid secretion. By blocking these receptors, ebastine reduces the severity of allergic symptoms. Unlike first-generation antihistamines, ebastine has minimal sedative effects as it does not cross the blood-brain barrier in significant amounts.
• Therapeutic Effects:
  • Reduces symptoms of allergic rhinitis such as sneezing, itching, and nasal discharge.
  • Alleviates itching and swelling from chronic urticaria.
  • Non-sedating, making it suitable for daytime use without causing drowsiness.

Pharmacokinetics

• Absorption: Ebastine is rapidly absorbed from the gastrointestinal tract with a peak plasma concentration occurring approximately 2–3 hours after oral administration.
• Distribution: It is widely distributed throughout the body and is highly bound to plasma proteins (approximately 96%).
• Metabolism: Ebastine is metabolized in the liver primarily by the cytochrome P450 enzyme system, particularly CYP3A4, to an active metabolite, carebastine.
• Excretion: The drug and its metabolites are mainly excreted in the urine, with a small portion excreted unchanged.
• Half-Life: Approximately 15–19 hours, which supports once-daily dosing.

Drug Interactions

• With Food:
  Food does not significantly alter the bioavailability of ebastine, but taking it with a high-fat meal may slightly delay its absorption.
• With Other Medications:
  • CYP3A4 Inhibitors: Drugs such as ketoconazole, itraconazole, or erythromycin may increase blood levels of ebastine.
  • CNS Depressants: Combining ebastine with alcohol or other CNS depressants could enhance sedative effects, although ebastine is generally considered non-sedating.
  • Antiarrhythmic Drugs: Caution is advised when taken with drugs affecting heart rhythm (e.g., quinidine, amiodarone) due to potential arrhythmia risk.
  • Other Antihistamines: Increased risk of anticholinergic effects like dry mouth and drowsiness if combined with other antihistamines.

Clinical Considerations

• Pregnancy Category: Category C (Use with caution during pregnancy and only if the potential benefit justifies the potential risk to the fetus).
• Lactation: It is unknown whether ebastine is excreted in human milk. Therefore, use with caution while breastfeeding or consider alternative treatments.
• Pediatric Use: Not recommended for children under 12 years of age unless otherwise directed by a healthcare provider.
• Geriatric Use: Generally well tolerated, but caution is recommended for patients with hepatic or renal impairment. Dose adjustment may be needed for those with liver dysfunction.
• Other Considerations:
  • Use caution in patients with severe liver impairment.
  • Monitor for side effects in patients with cardiovascular issues due to the potential for arrhythmias.