Acrivastine

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

Synonyms: Acrivastin; Acrivastina; Acrivastinum; Akrivastiini; BW-825C
BAN: Acrivastine
USAN: Acrivastine
INN: Acrivastine [rINN (en)]
INN: Acrivastina [rINN (es)]
INN: Acrivastine [rINN (fr)]
INN: Acrivastinum [rINN (la)]
INN: Акривастин [rINN (ru)]
Chemical name: (E)-3-{6-[(E)-3-Pyrrolidin-1-yl-1-p-tolylprop-1-enyl]-2-pyridyl}acrylic acid
Molecular formula: C22H24N2O2 =348.4
CAS: 87848-99-5
ATC code: R06AX18
Read code: y01uk

Adverse Effects and Precautions

As for the non-sedating antihistamines in general. Acrivastine should be given with care in renal impairment UK licensed product information recommends that it should not be given to patients with significant renal impairment, while product information in other countries, such as Switzerland for example, contra-indicates its use in those with a creatinine clearance of less than 50 mL/minute. Acrivastine should not be used in patients hypersensitive to triprolidine.

Sedation. For a discussion of the sedative effects of antihistamines.

Interactions

As for the non-sedating antihistamines in general.

Pharmacokinetics

Acrivastine is well absorbed from the gastrointestinal tract peak plasma concentrations are achieved in about 1.5 hours. The plasma half-life of acrivastine is about 1.5 hours and the drug does not appear to cross the blood-brain barrier to a significant extent. Acrivastine along with an active metabolite is excreted principally in the urine.

Uses and Administration

Acrivastine is anon-sedating antihistamine structurally related to triprolidine. It does not have any significant sedative or antimuscarinic actions. It is used for the symptomatic relief of allergic conditions such as rhinitis and various types of urticaria when it is given in oral doses of 8 mg three times daily. It is also used with a decongestant such as pseudoephedrine hydrochloride.

Preparations

Proprietary Preparations

Austria: Semprex

Czech Republic: Semprex

Denmark: Benadryl

Finland: Benadryl Semprex

Hong Kong: Semprex

Italy: Semprex

Malaysia: Semprex

The Netherlands: Semprex

Philippines: Semprex

Russia: Semprex

South Africa: Semprex

Singapore: Semprex

Sweden: Semprex

Switzerland: Semprex

Thailand: Semprex

Turkey: Semprex

United Kingdom: Benadryl Allergy Relief

Multi-ingredient

Austria: Duact

Denmark: Duact

Finland: Duact

Turkey: Duact

UK: Benadryl Plus

USA: Semprex-D


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