Changes in valvular function and blood pressure level during long-term pharmacological anti-hypertensive therapy were investigated in patients with mild to moderate essential hypertension. Sixty-seven patients with hypertension (mean [+/-SD] 60 +/- 10 years) were followed up for 5.4 +/- 1.6 years with antihypertensive medication. During the follow-up period, valvular dysfunction was assessed by color Doppler echocardiography. Increased mitral valve regurgitation > or = grade II and/or aortic valve regurgitation > or = grade II were aggravated in 17 patients, whereas the other 50 patients did not reveal any significant changes in valvular functions. Systolic blood pressure and end-systolic wall stress at the end of the follow-up period were higher in the aggravated group (156 +/- 30 mmHg and 79 +/- 23 dyne/cm2) than in the unchanged group (143 +/- 17 mmHg and 63 +/- 18 dyne/cm2). Dimensions of the left atrium and left ventricle at both systole and diastole were enlarged in the aggravated group (37 +/- 4 to 40 +/- 4, 31 +/- 4 to 33 +/- 4 and 48 +/- 3 to 51 +/- 3 mm, respectively), but not in the unchanged group. Nine patients in the aggravated group received additional treatment with imidapril hydrochloride over 6 months in an attempt to further reduce blood pressure levels, resulting in significant improvements in systolic blood pressure (151 +/- 12 to 129 +/- 7 mmHg), diastolic blood pressure (91 +/- 4 to 79 +/- 8 mmHg), left atrial dimension (41 +/- 3 to 39 +/- 3 mm) and left ventricular end-diastolic dimension (49 +/- 4 to 48 +/- 3 mm). Adequate pharmacological intervention can ameliorate valvular dysfunction, left ventricular enlargement and increased ventricular wall stress.