Nitrendipine is a new nifedipine-like calcium antagonist antihypertensive agent. In this study, nitrendipine 5-40 mg orally bid was administered for up to three months to 16 patients with severe essential hypertension (untreated supine diastolic blood pressure greater than or equal to 115 mm Hg). Hydrochlorothiazide or propranolol or both were also given to patients who did not achieve goal blood pressure with nitrendipine alone. Five patients achieved goal blood pressure (supine less than or equal to 90 mm Hg) with nitrendipine alone and six more after the addition of a second drug, and only four required triple-drug therapy. One patient was terminated from the study because of headaches, a common nitrendipine side effect. This study demonstrates that nitrendipine is an effective and well-tolerated agent in the treatment of severe hypertension.

Adult↗

PubMedDate not supplied

Transdermal administration of clonidine: a new approach to antihypertensive therapy.

This study assessed the antihypertensive efficacy and side effects of clonidine administered transdermally. Twenty-five patients with mild to moderate essential hypertension (seated diastolic blood pressure 95-120 mm Hg with diuretic therapy alone) controlled with oral diuretic plus oral clonidine were enrolled. Transdermal clonidine was substituted for oral clonidine and titrated until adequate blood pressure control (seated diastolic blood pressure less than 90 mm Hg) was attained. At the end of titration, seated morning blood pressure averaged 129/90 +/- 15/5 mm Hg (mean +/- standard deviation) compared to 136/96 +/- 13/7 mm Hg (p less than 0.01/0.001) during oral clonidine administration. Standing morning blood pressure was also lower during transdermal than oral therapy (131/94 +/- 16/5 vs 136/99 +/- 14/7, p less than 0.05/0.001). Afternoon blood pressures (at peak effect of oral dose) were virtually identical during oral and transdermal therapy in both seated and standing positions. Typical side effects of oral clonidine, including dry mouth, drowsiness, and sexual dysfunction, were reduced during transdermal therapy. There was less morning-to-afternoon variability of blood pressure control and plasma clonidine concentrations during transdermal than during oral therapy. One patient left the study because of drowsiness and two because of skin reactions to the transdermal skin patch. Mild transient local skin irritation occurred frequently. Transdermal clonidine plus a diuretic is an effective treatment for mild to moderate essential hypertension, improves compliance and reduces side effects of therapy.

Administration, Topical↗

PubMedDate not supplied

Indapamide: clinical pharmacology, therapeutic efficacy in hypertension, and adverse effects.

Indapamide will soon be marketed in the United States as an oral antihypertensive agent and diuretic. Its molecular structure includes both a polar sulfamoyl chlorobenzamide moiety and a lipid-soluble methylindoline moiety. It differs chemically from the thiazides in that it does not possess the thiazide ring system and it contains only one sulfonamide group. Indapamide is rapidly and well absorbed after oral ingestion, and it has a long terminal half-life in whole blood which permits once daily administration. Indapamide is extensively metabolized by the liver with excretion of unchanged drug accounting for approximately 5% of the total dose. Although indapamide is thought to exert its antihypertensive effect by its diuretic action, several investigations employing laboratory animal preparations have documented a direct vascular action. It has been categorized as a calcium channel blocking agent and this may account for a portion of its antihypertensive effectiveness. In both the treatment of edema and as an antihypertensive agent, indapamide appears to be comparable to hydrochlorothiazide, chlorthalidone and furosemide and seems to have no clinically important advantage over these agents. Side effects associated with indapamide are minimal and appear to be comparable to those observed with other antihypertensive diuretics. Based on few published studies, indapamide appears to be a useful long acting antihypertensive and diuretic agent that is well tolerated and associated with minimal biochemical abnormalities or side effects.

Blood Proteins↗

PubMedDate not supplied

Comparison of ramipril and enalapril in patients with essential hypertension.

STUDY OBJECTIVE: To compare the clinical safety and efficacy of ramipril, a new long-acting nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE), with enalapril. DESIGN: A randomized, double-blind trial. SETTING: Multicenter trial involving 4 large teaching hospitals and 12 community medical centers. PATIENTS: One hundred fifty-nine patients with mild to moderate essential hypertension were enrolled. Two patients were excluded from the efficacy analysis because they failed to return for follow-up. INTERVENTIONS: Patients were randomized to receive ramipril 2.5, 5, or 10 mg, or enalapril 5, 10, or 20 mg once/day for 3 or 4 weeks. MEASUREMENTS AND MAIN RESULTS: At baseline, supine diastolic blood pressures ranged from 98-116 mm Hg. Supine and standing systolic blood pressures were reduced by 11.8 and 10.2 mm Hg with ramipril 10 mg (p < or = 0.001) and 9.3 and 10.7 mm Hg with enalapril 20 mg (p < or = 0.001). At the end of the 4-week trial, patients in all six dosage groups had clinically and statistically significant reductions in supine diastolic blood pressure compared with baseline values. The agents did not differ significantly with respect to their blood pressure-lowering effects. Both lowered plasma ACE activity; after 4 weeks, changes from baseline were highly significant for all dosage groups (p < or = 0.001). CONCLUSION: Ramipril was as effective in reducing blood pressure and was as well tolerated as enalapril. A larger average decrease in plasma ACE activity was achieved with ramipril over all dosages (71%) compared with that for enalapril (48%), suggesting that ramipril has greater ACE inhibition in the circulation.

Adult↗