[Use of carvedilol compared to nifedipine in the treatment of mild and moderate essential arterial hypertension]. / O uso do carvedilol comparado à nifedipina no tratamento da hipertensão arterial essencial leve e moderada.

PURPOSE: To compare the efficacy of carvedilol, a new antihypertensive drug that combines vasodilatory and beta-blocker properties, with nifedipine. METHODS: In a multicenter double-blind trial, 106 mild to moderate essential hypertensive patients were treated with either carvedilol (n = 51), or nifedipine (n = 55) as monotherapy. Following 4 weeks of wash-out/run-in period, patients from the carvedilol group received this drug once a day at a dosage of 25 mg/day for 8 consecutive weeks. In order to maintain the double-blind character of the study, a placebo was administered in the carvedilol group at identical dosage intervals as used in the nifedipine s.r. group. Nifedipine was also administered for 8 weeks at a dosage of 40 mg/day given b.i.d. RESULTS: Both treatments were equally efficient in reducing blood pressure in the seated and upright positions. Blood pressure response to treatment was obtained in 79% and 78% of patients treated with carvedilol and nifedipine, respectively. The carvedilol group did not develop reflex tachycardia which is usually seen when prescribing vasodilators. Blood biochemistry remained unchanged with both treatments. Besides similar blood pressure efficacy, side effects by patients taking carvedilol were less frequent than nifedipine group. CONCLUSION: Carvedilol is a safe, efficient, once/day choice as monotherapy for mild to moderate essential hypertensive patients.

[Reversal of left ventricular hypertrophy after the use of benazepril]. / Reversão de hipertrofia ventricular esquerda após o uso de benazepril.

PURPOSE: To assess the effects of benazepril (ACE inhibitor) on arterial blood pressure (ABP) and left ventricular mass index (LVMI). METHODS: Nineteen patients (7 men, 12 women) with mean age 38.2 +/- 10.2 years, with mild to moderate hypertension were evaluated. Besides raised blood pressure, the necessary inclusion criterion was the presence of left ventricular hypertrophy detected by echocardiogram. After a wash-out period, all patients were given placebo followed by the active drug benazepril at a dose of 10 mg once a day. For those patients who did not achieve a satisfactory control of the blood pressure (BP) 25 mg of chlorthalidone was added. All patients underwent 180 days of benazepril treatment. RESULTS: The ABP was gradually controlled as follow: at seated position the systolic BP changed from 156.05 +/- 5.07 mmHg to 129 +/- 3.74 mmHg (p < 0.001) and the diastolic BP from 99.74 +/- 1.59 mmHg to 81.8 +/- 2.27 mmHg (p < 0.001). At orthostatic position the systolic BP changed from 156.9 +/- 5.35 mmHg to 124.28 +/- 5.33 mmHg (p < 0.001) and the diastolic BP from 101.7 +/- 1.34 to 81.36 +/- 2.81 (p < 0.001). The heart rate did not change significantly during the study. The LVMI decreased significantly from 182.4 +/- 9.2g/m2 to 122.6 +/- 4.2g/m2 (p < 0.001). CONCLUSION: Our data revealed that 100% of the patients achieved satisfactory degrees of LVMI regression and in 34% there was a normalization of it.

[Treatment of hypertensive crisis in outpatients with sublingual isradipine]. / Tratamento da crise hipertensiva em pacientes ambulatoriais com isradipina sublingual.

PURPOSE: Evaluate the efficacy and tolerability of isradipine, a new dihydropyridine calcium antagonist in the therapy of outpatients hypertensive crisis. PATIENTS AND METHODS: Twenty seven patients with mean age of 37.2 +/- 2.5 years (ages ranging from 18 to 59 years old) of different races (14 white, 13 not white); 15 men and 12 women, with diastolic blood pressure over 130 mmHg and without signs of recent target organ damage were studied. The patients were divided in three groups according to the used dosage of Isradipine tablets by sublingual route. Group I (n = 10): 1.25 mg; Group II (n = 10): 2.5 mg and Group III (n = 7): 5.0 mg. Arterial blood pressure levels and heart rate were determined before the drug administration and every 30 minutes until 120 minutes after dosing. RESULTS: Mean arterial blood pressure (MABP) decrease significantly in all patients from 153.43 +/- 4.3 to 124.0 +/- 2.3 mmHg after 60 minutes and to 118.0 +/- 2.1 mmHg after 120 minutes (p < 0.001). Heart rate did not show significant changes with the drug. Clinical significant side effects were not observed. The comparative analysis of MABP curves did not show significant differences among the groups I, II and III. However, a tendency of a greater decrease in MABP was observed in the patients of group III. CONCLUSION: Isradipine tablets in the dosages of 1.25, 2.5 and 5.0 mg by sublingual route is effective and well tolerated in the treatment of ambulatorial patients with hypertensive crisis.

Angiotensin converting enzymes from urine of treated and untreated essential mild hypertensive patients (EHP) with diuretic: partial purification and characterization.

Urine of untreated EHP was eluted, on a ion-exchange chromatography, in two protein peaks with ACE activity, at 0.7 mS (BI) and 1.25 mS (BII), while urine of treated EHP, was eluted only in one peak with ACE activity (0.7 mS). BI (Mr, 88 kDa) and BII (Mr, 61 kDa) convert AI to AII, hydrolyze bradikinin, are inhibited by captopril, EDTA and metal ions.

Isradipine in the treatment of hypertensive crisis in ambulatory patients.

In order to investigate the efficacy of isradipine in the treatment of hypertensive crisis, we treated three groups of patients who had diastolic blood pressure (DBP) greater than 120 mm Hg, and who were without signs of acute target-organ damage. Isradipine was given sublingually in doses of 1.25 mg (group 1; n = 10), 2.5 mg (group 2; n = 10), and 5 mg (group 3; n = 7). Mean arterial pressure (MAP) was reduced in all patients [from 153.4 +/- 4.3 to 124.0 +/- 2.3 mm Hg at 60 min, and to 118.0 +/- 2.1 mm Hg at 2 h after administration (p less than 0.001)]. The heart rate (HR) did not change significantly (from 82.4 +/- 3.7 to 84.0 +/- 6 beats/min; NS). No significant differences were noted in the overall responses of the three groups; however, blood pressure reduction was more rapid in the group receiving 5 mg compared with the other two dosages. These results show that isradipine given sublingually is effective in reducing the elevated blood pressure of a hypertensive crisis and is not accompanied by limiting side effects. Isradipine's onset of action is early (approximately 30 min after dosing) and reaches its maximum blood pressure response within 2 h of administration. No dose-dependent reductions in blood pressure were observed with the dosage range employed in this study.

Regression of left ventricular hypertrophy in the short-term treatment of hypertension with isradipine.

This was a study of the effectiveness of isradipine, a calcium antagonist of the dihydropyridine group, in reversing left ventricular hypertrophy (LVH) in patients with mild-to-moderate hypertension. Mean arterial pressure was effectively reduced at 90 days of treatment (from 129.5 +/- 2.0 to 111.5 +/- 2.8 mm Hg; P less than .001). The electrocardiographic Romhilt-Estes score for LVH showed early reduction at 45 days of treatment (from 7.1 +/- 0.6 to 5.1 +/- 0.4 points; P less than .001), and further diminutions were observed at 90 days of treatment (3.8 +/- 0.4 points; P less than .01). The echocardiographically determined left ventricular mass indices confirmed these findings (from 175.0 +/- 8.9 to 141.7 +/- 5.5 and to 124.8 +/- 4.2 g/m2; P less than .001) for 45 and 90 days, respectively. The results indicate that isradipine is effective in reducing left ventricular mass and that these reductions are observed early in the course of treatment.

Reversal of left ventricular hypertrophy following treatment of hypertension with isradipine.

In order to complement earlier short-term observations, we studied the effects of isradipine (1.25 or 2.5 mg twice daily) on blood pressure as well as its action in reversing cardiac hypertrophy in 25 moderately hypertensive patients. We observed that the treatment produced short-term (3 month) and longer-term (9 month) control of blood pressure [decreases in mean arterial pressure (MAP) from 128 +/- 2.3 to 112 +/- 2.7 mm Hg and to 105.5 +/- 2.9 mm Hg; p less than 0.001] while heart rate remained constant throughout the study (from 76.6 +/- 2.3 to 74.7 +/- 2.4 beats/min; NS). Reversal of left ventricular hypertrophy (LVH) obtained after 3 months of treatment (LV mass index from 173.7 +/- 8.8 to 135.7 +/- 4.5 g/m2; p less than 0.001) was accentuated with continued therapy (to 131.0 +/- 4.0 and 124.4 +/- 3.1 g/m2 at 6 and 9 months, respectively; p less than 0.01). These results indicate that significant regression of LVH can be obtained with short-term treatment of hypertension with isradipine and that this effect will be fully obtained with longer-term (9 month) therapy.