Acrivastine

Oral
Allergic rhinitis, Chronic idiopathic urticaria

Severe: Contraindicated.

May be taken with or without food.

Severe renal impairment.

Patient with porphyria. Mild to moderate renal impairment. Children and elderly. Pregnancy and lactation.

Significant: CNS depression (e.g. drowsiness, dizziness).
Gastrointestinal disorders: Dry mouth.
Nervous system disorders: Headache.
Skin and subcutaneous tissue disorders: Rash.

PO: Z (Adverse pregnancy outcomes (e.g. spontaneous abortions, intrauterine death) have been reported. Should not be used unless benefits outweigh risks.)

This drug may cause drowsiness and dizziness, if affected, do not drive or operate machinery.

Symptoms: Drowsiness, restlessness, hyperactivity, tachycardia. Management: Supportive treatment. May administer activated charcoal if needed.

Additive CNS depression with other CNS depressants, including sedatives and tranquilisers. Erythromycin and ketoconazole may increase the plasma concentration or adverse effects of acrivastine, respectively.

May enhance the CNS depressant effect of alcohol.

Description:
Mechanism of Action: Acrivastine, a non-sedating antihistamine, is structurally related to triprolidine. It is a competitive antagonist of H₁-receptors but lacks significant anticholinergic effects. Additionally, it also has a low potential to penetrate the CNS.
Onset: Inhibition of wheals/flares: 15 minutes. Symptom relief of allergic rhinitis: Within 1 hour.
Duration: ≥8 hours (inhibition of wheals/flares).
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1.5 hours.
Distribution: Plasma protein binding: 50%, mainly to albumin.
Metabolism: Metabolised via reduction of acrylic acid side chain into propionic acid analogue.
Excretion: Via urine (59% as unchanged drug, 15-17% as active metabolite); faeces. Elimination half-life: 1.5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5284514, Acrivastine. https://pubchem.ncbi.nlm.nih.gov/compound/Acrivastine. Accessed Nov. 21, 2023.

Store below 30°C.

Antihistamines & Antiallergics

R06AX18 - acrivastine ; Belongs to the class of other antihistamines for systemic use.

Anon. Acrivastine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/06/2023.

Benadryl Allergy Relief (McNeil Products Limited). MHRA. https://products.mhra.gov.uk. Accessed 20/06/2023.

Brown & Burk Allergy Relief 8 mg Capsules, Hard (Brown & Burk UK Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 20/06/2023.

Buckingham R (ed). Acrivastine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/06/2023.

Joint Formulary Committee. Acrivastine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 20/06/2023.

Preston CL (ed). Acrivastine + Erythromycin. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/09/2023.

Preston CL (ed). Acrivastine + Ketoconazole. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/09/2023.