Antihypertensive and metabolic effects of nifedipine and labetalol alone and in combination in primary hypertension. 1985

K P Ohman, and L Weiner, and H von Schenck, and B E Karlberg

In a randomised, double-blind, cross over trial, 25 patients with mild to moderate primary hypertension were given nifedipine 20-40 mg twice daily and labetalol 200-400 mg twice daily after a 4 week period on placebo, followed by the two drugs in combination. The BP during placebo therapy was 164/108 mmHg supine and 159/110 mmHg standing. After monotherapy with nifedipine for 6 weeks the supine BP was reduced by 18/13 mmHg and the standing BP by 20/12 mmHg; with labetalol the corresponding figures were 26/15 mmHg and 28/21 mmHg, respectively. The combined therapy induced a larger fall in BP, by 36/22 mmHg supine and by 39/24 mmHg standing; in 21 of 23 patients the BP became normal. The heart rate (HR) decreased during labetalol treatment alone and on the combined therapy. With nifedipine alone, the HR was unchanged in the supine position and increased on standing. Nifedipine increased plasma renin activity (PRA) and urinary aldosterone excretion (uA), whereas labetalol reduced both. During combination therapy, PRA and uA remained unchanged. There was a slight fall in HDL-cholesterol during treatment with labetalol alone and in combination with nifedipine. The fasting blood glucose increased slightly during treatment with each of the drugs, but neither caused a change in the concentrations of glycosylated haemoglobin A1, serum insulin, C-peptide, or plasma glucagon. Adverse effects as a rule were well tolerated and were related to the pharmacological effects of the drugs. Only 2 patients left the trial, both during labetalol treatment.

UI MeSH Term Description Entries
D006973 Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more. Blood Pressure, High,Blood Pressures, High,High Blood Pressure,High Blood Pressures
D007741 Labetalol A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS. AH-5158,Albetol,Apo-Labetalol,Dilevalol,Labetalol Hydrochloride,Labetalol, (R,R)-Isomer,Labetolol,Normodyne,Presolol,R,R-Labetalol,SCH-19927,Trandate,AH 5158,AH5158,Apo Labetalol,ApoLabetalol,Hydrochloride, Labetalol,R,R Labetalol,SCH 19927,SCH19927
D008055 Lipids A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed) Lipid
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D009543 Nifedipine A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. Adalat,BAY-a-1040,Bay-1040,Cordipin,Cordipine,Corinfar,Fenigidin,Korinfar,Nifangin,Nifedipine Monohydrochloride,Nifedipine-GTIS,Procardia,Procardia XL,Vascard,BAY a 1040,BAYa1040,Bay 1040,Bay1040,Monohydrochloride, Nifedipine,Nifedipine GTIS
D011897 Random Allocation A process involving chance used in therapeutic trials or other research endeavor for allocating experimental subjects, human or animal, between treatment and control groups, or among treatment groups. It may also apply to experiments on inanimate objects. Randomization,Allocation, Random
D012083 Renin A highly specific (Leu-Leu) endopeptidase that generates ANGIOTENSIN I from its precursor ANGIOTENSINOGEN, leading to a cascade of reactions which elevate BLOOD PRESSURE and increase sodium retention by the kidney in the RENIN-ANGIOTENSIN SYSTEM. The enzyme was formerly listed as EC 3.4.99.19. Angiotensin-Forming Enzyme,Angiotensinogenase,Big Renin,Cryorenin,Inactive Renin,Pre-Prorenin,Preprorenin,Prorenin,Angiotensin Forming Enzyme,Pre Prorenin,Renin, Big,Renin, Inactive
D012084 Renin-Angiotensin System A BLOOD PRESSURE regulating system of interacting components that include RENIN; ANGIOTENSINOGEN; ANGIOTENSIN CONVERTING ENZYME; ANGIOTENSIN I; ANGIOTENSIN II; and angiotensinase. Renin, an enzyme produced in the kidney, acts on angiotensinogen, an alpha-2 globulin produced by the liver, forming ANGIOTENSIN I. Angiotensin-converting enzyme, contained in the lung, acts on angiotensin I in the plasma converting it to ANGIOTENSIN II, an extremely powerful vasoconstrictor. Angiotensin II causes contraction of the arteriolar and renal VASCULAR SMOOTH MUSCLE, leading to retention of salt and water in the KIDNEY and increased arterial blood pressure. In addition, angiotensin II stimulates the release of ALDOSTERONE from the ADRENAL CORTEX, which in turn also increases salt and water retention in the kidney. Angiotensin-converting enzyme also breaks down BRADYKININ, a powerful vasodilator and component of the KALLIKREIN-KININ SYSTEM. Renin-Angiotensin-Aldosterone System,Renin Angiotensin Aldosterone System,Renin Angiotensin System,System, Renin-Angiotensin,System, Renin-Angiotensin-Aldosterone
D001786 Blood Glucose Glucose in blood. Blood Sugar,Glucose, Blood,Sugar, Blood

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