ACRIVASTINE – Drug Information

Generic Name: Acrivastine

Therapeutic Classification: Antihistamines

Descriptions:

Acrivastine is an anti-allergy drug, indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia.

Mechanism of Action:

It is a Histamine-1 Receptor Antagonist. The mechanism of action of acrivastine is as a Histamine H1 Receptor Antagonist. It exhibits H1-antihistaminic receptor activity, which prevents histamine from binding to its receptor in target cells.

Pharmacokinetics:

  • Half-Life 1.9-3.5 hr
  • Absorption Rapid and complete
  • Peak Plasma Time 1.1 hr
  • Peak Plasma Concentration 227 ng/ml
  • Metabolism – Acrivastine 11% to propionic acid metabolite
  • Excretion – Feces (13%) urine (84%)

Contraindications:

  • It is contraindicated in patients with severe hypertension or severe coronary artery disease or other alkylamine antihistamines.
  • Hypersentivity to Acrivastine.
  • Hypersensitivity to pseudoephedrine or other sympathomimetic amines and in patients taking monoamine oxidase (MAO) inhibitors.
  • Moderate to Severe Kidney Impairment.
  • Severe coronary artery disease.

Pregnancy Category:

Category B

May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

Warnings and Precautions:

  • Concurrent use with alcohol or other CNS depressants may cause additional reductions in alertness and impairment of CNS performance and should be avoided.
  • Due to potential for sedation, driving a motor vehicle or operating machinery should be avoided.
  • It Should not be used in Kidney disease patients.
  • It Should not be used in children under 12 years old.

Adverse Reactions / Side Effects:

  • Headache and dizziness
  • Pharyngitis and increased cough
  • Palpitations and tachycardia
  • Menstrual cramps
  • Nervousness
  • Insomnia
  • Dry mouth

Other Drug Interaction with Acrivastine:

  • Acrivastine interacts with:
  • Ketoconazole
  • Erythromycin
  • Sedatives or tranquillizers
  • MAO inhibitors

Dose:

Seasonal Allergic Rhinitis or Nasal Congestion

8 mg/60 mg (1 capsule) PO q4-6h >14 days continuous treatment efficacy not adequately investigated

Trade Names / Brand Names:

India:

Nasorest Plus (8mg/325mg/25mg/5mg) | Nasorest | Benadry

International:

Semprex

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