ATC Class:R06AX18
AHFS Class:
- Second Generation Antihistamines 4:08
Generic Name(s):
Chemical Name:
- 3-[6-[1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]-2-propenoic acid
Associated Monographs
Acrivastine, an alkylamine, is classified as a second generation antihistamine.1,2,3,11
Acrivastine, as the fixed-combination preparation containing pseudoephedrine hydrochloride, is used to provide symptomatic relief of seasonal allergic rhinitis (e.g., hay fever) in adults and children 12 years of age and older1,2,3,4,6 when symptoms amenable to each ingredient are present concurrently.1,2,3,12,13,14,15 Because antihistamines alone generally are not optimally effective in relieving symptoms of nasal congestion,1,2,3,12,15,16 combined use with a nasal decongestant such as pseudoephedrine can improve efficacy when such symptoms are present.1,2,3,6,15 For additional information, see Uses: Nasal Allergies and the Common Cold in the Antihistamines General Statement 4:00. Although acrivastine also has been used alone for the relief of symptoms associated with seasonal allergic rhinitis,2,4,6,7 the drug currently is commercially available in the US only in fixed combination with pseudoephedrine hydrochloride.1,3 The manufacturer states that the fixed-combination preparation containing acrivastine and pseudoephedrine hydrochloride has not been studied adequately to establish efficacy in relieving symptoms of the common cold†.1
Administration 
Acrivastine, as a fixed-combination preparation containing pseudoephedrine hydrochloride, is administered orally.1,2,3
Dosage
Acrivastine Combinations
The manufacturer states that safety and efficacy of the fixed-combination preparation containing acrivastine and pseudoephedrine hydrochloride in children younger than 12 years of age have not been established.1,3 Adjustment of dosage of the combination in geriatric patients with normal renal function is not necessary.1,18,19
For symptomatic relief of seasonal allergic rhinitis, the usual dosage of acrivastine in fixed combination with pseudoephedrine hydrochloride in adults and children 12 years of age and older is 8 mg every 4-6 hours 4 times daily.1,2,3,6 However, because acrivastine currently is commercially available in the US only in fixed combination with pseudoephedrine, it may be difficult to titrate dosage optimally.3 In addition, some patients with insomnia may benefit from administration of an antihistamine alone at bedtime.3,15 The manufacturer states that efficacy of acrivastine combined with pseudoephedrine for seasonal allergic rhinitis has not been established by adequate clinical studies for periods exceeding 14 days of continuous therapy.1
Dosage in Renal Impairment
Both acrivastine and pseudoephedrine hydrochloride are eliminated via renal mechanisms and accumulate to differing degrees in patients with diminished renal function.1,20 Therefore, the manufacturer states that use of the fixed-combination preparation containing the drugs is not recommended in patients with renal impairment (creatinine clearance of 48 mL/minute or less).1
Description
Acrivastine is an alkylamine antihistamine structurally related to triprolidine,1,2,3,11 differing only in the addition of a polar acrylic chain to the pyridine ring.2 Because of this structural difference, acrivastine is relatively less lipophilic and distributes poorly into the CNS,2,11 with a resultant decreased potential for adverse CNS effects compared with many other antihistamines.2,3,8,9,10,11 While acrivastine, like astemizole (no longer commercially available in the US), loratadine, and terfenadine (no longer commercially available in the US), has been referred to as a relatively “nonsedating” or second generation antihistamine, acrivastine is not devoid of adverse CNS effects (e.g., drowsiness), particularly when administered concomitantly with CNS depressants (e.g., alcohol).1,2,3,8,9,10,11 In addition, the relative risk of adverse CNS effects with acrivastine compared with other second generation antihistamines (e.g., astemizole, loratadine, terfenadine) remains to be established further.2,3,11,15 Acrivastine did not exhibit appreciable anticholinergic activity in pharmacologic studies2,3,11,15,17,18 and does not prolong the QT interval.3,15,17,18
Acrivastine currently is commercially available in the US only as the fixed-combination preparation containing pseudoephedrine hydrochloride.1,3
Additional Information
SumMon® (see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the labeling be consulted for detailed information on the usual cautions, precautions, and contraindications.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Acrivastine Combinations
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
Oral | Capsules | 8 mg with Pseudoephedrine Hydrochloride 60 mg | Semprex®-D | Celltech |
AHFS® Drug Information. © Copyright, 1959-2022, Selected Revisions November 1, 2008. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
1. Medeva. Semprex®-D (acrivastine and pseudoephedrine HCl) capsules prescribing information. Rochester, NY; 1998 March.
2. Brogden RN, McTavish D. Acrivastine: a review of its pharmacological properties and therapeutic efficacy in allergic rhinitis, urticaria and related disorders. Drugs . 1991; 41(6):927-40. [PubMed 1715267]
3. Anon. Acrivastine/pseudoephedrine (Semprex-D) for seasonal allergic rhinitis. Med Lett Drugs Ther . 1994; 36:78-80. [PubMed 7914667]
4. Meran A, Morse J, Gibbs TG. A cross-over comparison of acrivastine, pseudoephedrine and their combination in seasonal allergic rhinitis. Rhinology . 1990; 28(1):33-40. [PubMed 1970907]
5. Gibbs TG, McDonnell KA, Stokes T et al. Acrivastine in two doses compared with placebo in a multicentre, parallel group study for the treatment of seasonal allergic rhinitis. Br J Clin Pract . 1989; 43(1):11-4. [PubMed 2574054]
6. Boijkowski CJ, Gibbs TG, Hellstern KH et al. Acrivastine in allergic rhinitis: a review of clinical experience. J Int Med Res . 1989; 17(Suppl 2):54B-68B. [PubMed 2570003]
7. Bruno G, D'Amato G, Del Giacco GS et al. Prolonged treatment with acrivastine for seasonal allergic rhinitis. J Int Med Res . 1989; 17(Suppl 2):40B-46B. [PubMed 2570001]
8. Cohen AF, Hamilton MJ, Peck AW. The effects of acrivastine (BW825C), diphenhydramine and terfenadine in combination with alcohol on human CNS performance. Eur J Clin Pharmacol . 1987; 32(3):279-88. [PubMed 2885203]
9. Cohen AF, Hamilton M, Philipson R et al. The acute effects of acrivastine (BW825C), a new antihistamine, compared with triprolidine on measures of central nervous system performance and subjective effects. Clin Pharmacol Ther . 1985; 38(4):381-6. [PubMed 3840066]
10. Cohen AF, Hamilton MJ, Liao SH et al. Pharmacodynamic and pharmacokinetics of BW 825C: a new antihistamine. Eur J Clin Pharmacol . 1985; 28(2):197-204. [PubMed 2859204]
11. Aaronson DW. Comparative efficacy of H(IF)1(OK) antihistamines. Ann Allergy . 1991; 67:541-7. [PubMed 1683523]
12. Food and Drug Administration. Over-the-counter drugs: establishment of a monograph for OTC cold, cough, allergy, bronchodilator, and antiasthmatic products. [21 CFR Part 341] Fed Regist . 1976; 41:38312-424.
13. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; tentative final monograph for combination drug products. [21 CFR Part 341] Fed Regist . 1988; 53:30522-64.
14. Bryant BG, Cormier JF. Cold and allergy products. In: American Pharmaceutical Association. Handbook of nonprescription drugs. 8th ed. Washington, DC: American Pharmaceutical Association; 1986;127-74.
15. Simons FER, Simons KJ. The pharmacology and use of H1-receptor-antagonist drugs. N Engl J Med . 1994; 330: 1663-70. [PubMed 7909915]
16. Anon. Treatment of seasonal and perennial rhinitis. BMJ . 1981; 283:808-10. [PubMed 6117350][PubMedCentral]
17. Sanders RL, Dockhorn RJ, Alderman JL et al. Cardiac effects of acrivastine compared to terfenadine. J Allergy Clin Immunol . 1992; 89:183.
18. Medeva Inc, Fort Worth, TX: Personal communication.
19. Liao SHT, Fleck RJ, Blum MR et al. Clinical pharmacokinetics and safety of acrivastine with pseudoephedrine in geriatric volunteers. J Pharm Sci . 1987; 76:S113.
20. Baumelou A, Deray G, Bidault R et al. Pharmacokinetics of Duact, a combination of acrivastine and pseudoephedrine in chronic renal failure. J Am Soc Nephrol . 1993; 4:245. [PubMed 8400089]