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Acrivastine

A Review of its Pharmacological Properties and Therapeutic Efficacy in Allergic Rhinitis, Urticaria and Related Disorders

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An Erratum to this article was published on 01 October 1991

Summary

Synopsis

Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine was more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine was superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine caused less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine.

Thus, acrivastine is an effective addition to drugs currently available for the treatment of patients with allergic diseases in whom a histamine H1-receptor antagonist is indicated. Because of its rapid onset of action acrivastine will be particularly useful for ‘on demand’ therapy in patients with intermittent symptoms.

Pharmacodynamic Properties

Acrivastine is a histamine H1-receptor antagonist with a rapid (within about 30 minutes) onset of action and a low sedative potential due to poor penetration into the CNS. The lack of anticholinergic effects in animals has been confirmed by the low incidence of such effects in clinical trials. In healthy volunteers, acrivastine 2 to 8mg inhibits the flare and weal response to intradermally injected histamine and the increase in nasal airway resistance, bronchial airway resistance and conjunctival inflammatory response to direct challenge with histamine. The onset of action of acrivastine was more rapid than that of terfenadine as demonstrated by inhibition of bronchial challenge with histamine.

Acrivastine 4 to 16mg administered to small numbers of healthy volunteers did not impair psychomotor performance as assessed by adaptive tracking, reaction time, auditory vigilance, tapping tests or eye movement tests, unlike triprolidine 2.5 and 5mg or diphenhydramine 50mg. Acrivastine 4mg did not cause sedation relative to placebo when assessed subjectively or by multiple sleep latency test. The enhancement of the effect of alcohol on psychomotor function appears to be small.

Pharmacokinetic Properties

Mean peak plasma concentrations (Cmax) of acrivastine (parent drug plus metabolites) of 73 and 179 μg/L were attained 1.4 and 0.85 hours after single doses of 4mg capsules and 12mg oral solution, respectively. Repeated administration of acrivastine 2 to 32mg three times daily for 7 days resulted in dose-related linear increases in Cmax and area under the plasma concentration-time curve. There are no data on tissue distribution of acrivastine in humans, but animal studies indicate a low brain: plasma ratio. The metabolic transformation of acrivastine has not been fully characterised. The principal metabolite formed by reduction of the acrylic side chain accounts for about 10% of total plasma drug concentrations and 15 to 17% of a dose recovered in urine, and is 2 to 3 times more active than acrivastine in inhibiting histamine-induced bronchospasm in guinea-pigs.

Apparent total body clearance is around 0.26 L/h/kg and elimination half-life is between 1.4 and 2.1 hours in healthy young volunteers; The slightly prolonged half-life in older volunteers is probably related to their inherently lower creatinine clearance rate.

Therapeutic Efficacy

Acrivastine has been evaluated in clinical trials involving small numbers of patients with chronic idiopathic urticaria, symptomatic dermographism, cholinergic urticaria or idiopathic acquired cold urticaria and in larger numbers of patients with seasonal allergic rhinitis. Short term double-blind studies of acrivastine 4 or 8mg administered 2 or 3 times daily have shown its superiority to placebo in patients with seasonal allergic rhinitis. Acrivastine 16 or 24mg daily in 2 or 3 divided doses was of comparable efficacy to clemastine 2 or 3mg daily or terfenadine 120mg daily, when assessed by reduction in severity of symptoms. Acrivastine, like other antihistamines, relieves nasal congestion less consistently than other symptoms. In the various dermatoses, acrivastine 8mg 3 times daily was similar in efficacy to clemastine 1mg, hydroxyzine 20mg, chlorpheniramine 4mg, cyproheptadine 4mg or terfenadine 60mg, also administered 3 times daily. Preliminary studies in patients with atopic eczema suggest that 3 daily doses of acrivastine 8mg or terfenadine 60mg can equally enhance the benefits of standard treatment of itching in this condition.

Preliminary published data indicate that a combination of acrivastine and pseudoephedrine is more effective than either of its individual components in relieving nasal congestion, sneezing and rhinorrhoea in patients, with seasonal allergic rhinitis.

Tolerability

Short term studies of acrivastine 12 to 24mg daily have shown it to be well tolerated. In the small numbers of patients studied in each published trial, acrivastine appeared to cause less drowsiness than clemastine or hydroxyzine. In an analysis of about 2600 patients treated with acrivastine alone or placebo the incidence of adverse effects with acrivastine was not statistically significantly different from those with placebo.

Dosage and Administration

The recommended dosage of acrivastine in adults and children over 12 years is 8mg 3 times daily in Europe and the UK and 4 times daily in the US. A combination of acrivastine and pseudoephedrine is available as a conventional (8mg/60mg 3 times daily) or sustained release (12mg/90mg twice daily) formulation.

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Various sections of the manuscript reviewed by: M.L. Brandon, Diplomatic American Board of Allergy, San Diego, California, USA; G. Bruno, Universita Degli Studi Di Roma, First Department of Clinical Medicine, Rome, Italy; A.E. Gale, Winterbourne House, Hindmarsh, South Australia, Australia; S.T. Holgate, University of Southampton Faculty of Medicine, Southampton General Hospital, Southampton, England; F. Horak, Lazarettg, Vienna, Austria; J.F. Kemp, Allergy and Asthma Medical Group and Research Center, San Diego, California, USA; A. Kobza Black, Institute of Dermatology, Guy’s and St Thomas’s Hospitals, University of London, London, England; D.Wm. Moote, University of Western Ontario, London, Ontario, Canada; N.W. Todd, Division of Otolaryngology, Emory University School of Medicine, Atlanta, Georgia, USA; J.S. Turner, The Emory Clinic, Atlanta, Georgia, USA; Th. van Joost, Dermatologie en Venerologie, Academisch Ziekenhuis, Rotterdam, The Netherlands.

An erratum to this article is available at http://dx.doi.org/10.1007/BF03259139.

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Brogden, R.N., McTavish, D. Acrivastine. Drugs 41, 927–940 (1991). https://doi.org/10.2165/00003495-199141060-00008

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