Actif Cap 40 mg 14’s(Ebastine)-Potential overview

Pharmaceutical Class

• Class: Antihistamines
• Type: Non-sedating antihistamine

Indications for Use

• Allergic Rhinitis: Seasonal and perennial allergic rhinitis (hay fever) symptoms such as sneezing, itching, and nasal congestion.
• Chronic Urticaria: Treatment of chronic idiopathic urticaria (hives), reducing itching and skin reactions.

Common Side Effects

• Drowsiness (less common compared to first-generation antihistamines)
• Dry mouth
• Headache
• Dizziness
• Fatigue

Serious Side Effects (Less Common)

• Severe allergic reactions (anaphylaxis)
• Heart palpitations or irregular heartbeat
• Blurred vision or difficulty urinating
• Jaundice or liver problems (rare)
• Swelling in the throat or face

Dosage

• Standard Dose: 10–20 mg once daily.
• For Allergic Rhinitis: 10 mg daily.
• For Chronic Urticaria: 20 mg daily, typically for severe cases.
• Adjustment for Liver Dysfunction: Reduce the dose, typically 10 mg daily.

Usage Instructions

• Take orally with or without food.
• Swallow the tablet whole with water.
• Avoid taking more than the recommended dose to prevent the risk of side effects.

Drug Interactions

• With Food: Food does not significantly affect the absorption of ebastine.
• With Other Medications:
  • CYP3A4 Inhibitors: Drugs like ketoconazole or erythromycin may increase ebastine levels, increasing the risk of side effects.
  • Other Antihistamines: Avoid using with other antihistamines to prevent excessive sedation.
  • Alcohol: It may enhance sedative effects; use with caution.

Regulatory Approval and Manufacturer

• Approval: Approved for use by regulatory agencies like the FDA and EMA, under the brand name Actif and generics in many countries.
• Manufacturer: The manufacturer varies by region but typically includes companies like Macleods Pharmaceuticals, Dr. Reddy’s Laboratories, and others.

Pharmacist Related Data

Drug Name and Chemical Details

• Drug Name: Ebastine
• Chemical Name: 4-[4-(4-tert-butylphenyl)-1-piperazinyl]-2,3-dihydro-1H-pyrrolo[3,4-b]quinazolin-1-one
• Molecular Formula: C28H33N3O2

Pharmacodynamics

• Mechanism of Action: Ebastine is a selective antagonist of histamine H1 receptors. By binding to these receptors, it prevents histamine from exerting its allergic effects, reducing symptoms such as itching, swelling, and redness.
• Therapeutic Effects: It helps relieve symptoms of allergic rhinitis and chronic urticaria by blocking histamine, leading to less inflammation, reduced itching, and less congestion.

Pharmacokinetics

• Absorption: Ebastine is well absorbed from the gastrointestinal tract. Peak plasma concentrations are reached approximately 2 to 5 hours after oral administration.
• Distribution: It is widely distributed in the body, including the tissues and plasma. It has a high plasma protein binding rate (about 97%).
• Metabolism: Ebastine is metabolized in the liver by cytochrome P450 enzymes, mainly CYP3A4, to an active metabolite, carebastine.
• Excretion: Excreted primarily in the urine (less than 10% as unchanged drug), with the rest eliminated as metabolites.
• Half-Life: Approximately 15 to 19 hours.

Drug Interactions

• With Food: No significant food interactions, though absorption might be delayed slightly.
• With Other Medications:
  • CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole): May increase ebastine concentrations and risk of side effects.
  • CYP3A4 Inducers (e.g., rifampin): May decrease the effectiveness of ebastine.
  • Erythromycin: May increase blood levels of ebastine.
• Other Interactions: Avoid using with alcohol or other CNS depressants to prevent drowsiness.

Clinical Considerations

• Pregnancy Category: Category C (Risk cannot be ruled out; should only be used if clearly needed).
• Lactation: It is not known whether ebastine is excreted in breast milk. Use with caution during breastfeeding.
• Pediatric Use: Safety and effectiveness in children under 12 years have not been established.
• Geriatric Use: No specific dosage adjustments are required for elderly patients, but caution is advised due to the potential for increased sensitivity.
• Other Considerations: Patients with liver dysfunction may need dose adjustments.