Tolerability profile of tasosartan, a long-acting angiotensin II AT1 receptor blocker, in the treatment of patients with essential hypertension

This paper summarizes tolerability data for 1420 patients with essential hypertension who were enrolled in eight double-masked, controlled clinical trials and who received tasosartan, a long-acting, nonpeptidic angiotensin II AT₁ receptor blocker. A total of 2084 patients were included in all treatment groups in these studies. Patients were treated with tasosartan at doses ranging from 10 to 600 mg, over periods of 3 to 16 weeks, except for one study with a 6-day treatment period. Tasosartan was administered once daily (seven studies) or twice daily (one study). No adverse events occurred at a significantly greater frequency in tasosartan-treated patients than in patients who received placebo. Headache, the most frequently reported adverse event, occurred significantly less frequently among tasosartan-treated patients than among those taking placebo (19% and 28%, respectively). The following adverse events (tasosartan and placebo groups) were reported by at least 3% of tasosartan-treated patients: asthenia (7% in each group), pharyngitis (7% in each group), dizziness (7% and 5%, respectively), infection (6% and 7%, respectively), rhinitis (4% and 6%, respectively), pain (4% in each group), diarrhea (4% in each group), nausea (3% in each group), and dyspepsia (3% and 2%, respectively). Cough occurred with a similar frequency in the tasosartan group and in the placebo group (2% and 3%, respectively). Peripheral edema occurred in 2.7% of tasosartan-treated patients and 3.4% of the patients who received placebo. Hyperglycemia occurred in <1% of patients in both groups. Potentially clinically significant laboratory values occurred with comparable frequency in the tasosartan and placebo groups. Discontinuation rates because of adverse events were similar in the tasosartan and placebo groups (2.8% and 2.6%, respectively). Discontinuations because of other medical events occurred less frequently in the tasosartan group than in the placebo group (2.5% vs 4.6%, respectively). Tasosartan had a smooth onset of action without clinical evidence of first-dose hypotension. Blood pressure gradually returned to baseline after tasosartan withdrawal. No safety concerns were identified in these studies. The excellent tolerability profile of tasosartan administered once daily makes it an attractive choice for the clinical management of essential hypertension.