The antihypertensive and hypouricemic effects of eight-weeks administration of a uricosuric diuretic, tienilic acid (FR 3068), were examined in 18 hypertensive patients with hyperuricemia aged 38-78years. The antihypertensive effect of FR 3068 was compared with the effect of trichlormethiazide (TCMZ) in 10 paired studies, and its hypouricemic effect was also compared with the effect of xanthine oxidase inhibitor, allopurinol, co-administered with TCMZ in 10 patients. All values of blood pressure and the results of clinical examinations including serum uric acid levels were evaluated statistically using the paired t-test.
The blood pressures, both systolic and diastolic, in hypertensives were significantly decreased during the daily administration of 250mg FR 3068. The mean blood pressure 157.3 ± 9.7/90.0 ± 5.1 mmHg (mean ± S. E. ) under the control with 4 mg TCMZ was decreased to 147.0 ± 5.9/84.8 ± 3.4 mmHg during the administration of 250 mg FR 3068, but the difference was not significant. Consequently, the antihypertensive effect of FR 3068 was estimated to be almost equivalent or slightly superior to the effect of TCMZ.
The mean serum uric acid level in untreated hypertensives was significantly decreased from 8.43 ± 0.38 mg/dl to 5.59 ± 0.43 mg/dl during the treatment by 250 mg FR 3068. The mean uric acid level in those treated by 100 mg allopurinol with TCMZ was 6.91± 0.59 mg/dl,but it was decreased to 5.42±0.24 mg/dl when the regimen was changed to a single administration of 250 mg FR 3068.
The mean levels of serum sodium, potassium, chloride, total cholesterol, triglyceride, urea N, creatinine, sGOT, sGPT and alkalinephosphatase were not significantly changed during the 8-weeks administration of FR 3068, but fasting blood sugar was slightly but significantly elevated (101.4± 10.3 mg/dl before FR 3068 vs.115.0 ±8.3 mg/dl during FR 3068) in 5 paired studies.
In a patient who received 500 mg FR 3068 for 3 weeks complained of general malaise when his serum potassium level was 2.7 mEq/l, and in another patient who received 250 mg FR 3068 for 8 weeks serum potassium was decreased to 3.2 mEq/l. No other side-effects were detected throughout this study.
FR 3068 appears to be a useful agent because of its unique combined action of both antihypertensive and hypouricemic effects in the treatment of essential hypertension with hyperuricemia.
