Disease relevance of Acrivastin

• Acrivastine. A review of its pharmacological properties and therapeutic efficacy in allergic rhinitis, urticaria and related disorders [1].
• A phase II study of vinblastine in combination with acrivastine in patients with advanced renal cell carcinoma [2].
• Therefore, in clinical settings when a fast onset of the H1-blocking action is mandatory (e.g., after insect stings or for short-term prophylaxis) we recommend acrivastine [3].
• One study on 31 patients found both 4 and 8 mg acrivastine given three times daily to be significantly better than placebo for alleviating hay fever [4].
• Both doses of BW 825C were found to be highly effective and significantly better than placebo in controlling signs and symptoms of urticaria [5].

Psychiatry related information on Acrivastin

• Triprolidine increased reaction times after 1.5 hours (2.5 and 5 mg) and 3 hours (5 mg), but acrivastine did not have any effect on reaction time at any dose [6].

High impact information on Acrivastin

• The acute effects of acrivastine (BW825C), a new antihistamine, compared with triprolidine on measures of central nervous system performance and subjective effects [6].
• There are several to choose from, including cetirizine, astemizole, loratadine, terfenadine and acrivastine, each with its own pharmacokinetics and antiallergic properties [7].
• Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action [1].
• Based on in vitro data, the plasma levels of acrivastine were within a range adequate to block P-glycoprotein activity [2].
• Effects of semprex-D and diphenhydramine on learning in young adults with seasonal allergic rhinitis [8].

Chemical compound and disease context of Acrivastin

• A comparison of acrivastine versus terfenadine and placebo in the treatment of chronic idiopathic urticaria [9].
• A comparison of acrivastine versus clemastine and placebo in the treatment of patients with chronic idiopathic urticaria [10].
• A comparison of acrivastine versus chlorpheniramine in the treatment of chronic idiopathic urticaria [11].
• A comparison of acrivastine versus hydroxyzine and placebo in the treatment of chronic idiopathic urticaria [12].

Biological context of Acrivastin

• The mean +/- SD relative bioavailability of acrivastine from colonic compared to oral dosing was 0.18 +/- 0.09 [13].
• Analysis of AUC values indicated that greater amounts of 270C81 than acrivastine circulated in plasma after both iv and po dosing, and that first-pass metabolism of acrivastine to 270C81 occurred [14].
• The IC50 (mean +/- SEM) value for the acrivastine-induced inhibition of dV/dt was estimated to be 8.0 +/- 3.7 x 10(-3) M [15].
• The onset of effect of acrivastine, a new H1-antagonist, has been assessed using antagonism of histamine-induced bronchoconstriction in sensitive volunteers [16].
• In addition, a trend was demonstrated for both active agents to improve peak expiratory flow rate (PEFR) following exercise, when compared with placebo, and this trend reached statistical significance in the case of acrivastine (p less than 0.05) [17].

Anatomical context of Acrivastin

• Terfenadine alters action potentials in isolated canine Purkinje fibers more than acrivastine [15].

Associations of Acrivastin with other chemical compounds

• OBJECTIVE: The efficacy of the antihistamine-decongestant combination product (Semprex-D capsules) containing acrivastine 8 mg plus pseudoephedrine HCl 60 mg was evaluated for the treatment of seasonal allergic rhinitis symptoms [18].
• In contrast, acrivastine and fexofenadine had low brain-to-plasma ratios of 0.072 +/- 0.014 and 0.018 + 0.002, consistent with low passive membrane permeability for both compounds (16.2 and 66 nm/s, respectively) and Pgp efflux [19].
• RESULTS: The odds ratios (adjusted for age and sex) for the incidence of sedation were 0.63 (95% confidence interval 0.36 to 1.11; P=0.1) for fexofenadine; 2.79 (1.69 to 4.58; P<0.0001) for acrivastine, and 3.53 (2.07 to 5.42; P<0.0001) for cetirizine compared with loratadine [20].
• These studies indicate that 8 mg acrivastine given three times daily is both well tolerated and of equal efficacy to clemastine for the treatment of seasonal allergic rhinitis [4].
• 32 cases in the control group were treated with antihistamines (such as Acrivastine, Cinnarizine or Ranitidine) [21].

Analytical, diagnostic and therapeutic context of Acrivastin

• 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 [1].
• The efficacy of the treatment was evaluated by a daily symptom score, six physical examinations, the requirement of rescue antihistamines (acrivastine) and an overall assessment by the patient andthe investigating physician [22].
• Quantification of antihistamine acrivastine in plasma by solid-phase extraction and high-performance liquid chromatography [23].
• Acrivastine was analyzed at the wavelength of 254nm using a reversed-phase HPLC assay [23].
• Drowsiness measured using visual analogue scales followed both triprolidine treatments, but not BW 825C [24].

References