PubMed · 35277
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S M McLeod. 1979-03-03. Evolution of antihypertensive therapy.. https://pubmed.ncbi.nlm.nih.gov/35277/
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Three groups of patients with different premedications were examined for changes of blood pressure, heart rate, ECG and plasma free fatty acid levels during esophago-gastro-duodenoscopy: Group A was premedicated with Bunitrolol, group B was premedicated with Hyoscin-N-butyl-bromide and diazepam, group C was endoscopied without premedication. The pulse rate rose significantly less in group A than in groups A and C; the same phenomenon was observed with regard to the systolic blood pressure. Premature beats occurred in all 3 groups: 32 per cent of the patients in group A, 43 per cent in group B and 60 per cent in group C had at least occasional premature beats; an accumulation of premature beats however occurred significantly less frequently in group A than in groups B or C. A drop of the ST-part of the ECG occurred with about the same frequency in each group. An increase of the plasma free fatty acids, which was noted in groups B and C, could be observed in Group A. A pre-endoscopic medication of beta blocking agents could be a useful measure in patients with labile arterial hypertension, vegatative dysregulation and a hyperkinetic heart syndrome.
Two new beta-adrenoceptor blocking drugs with acute antihypertensive and positive inotropic effects are described: Compound A (2-[4-(3-tert.butylamino-2-hydroxypropoxy)phenyl]-4-trifluoromethylimidazole) and MK-761 (2-(3-tert.butylamine-2-hydroxypropoxy)-3-cyanopyridine hydrochloride). In SH rats both compounds, given orally, lowered arterial pressure and were more potent than hydralazine. The antihypertensive effect of compound A but not of MK-761 was antagonized by timolol. Both compounds had positive inotropic activity on cat heart papillary muscles; these effects were antagonized by timolol. The pretreatment of animals with reserpine greatly reduced the positive inotropic effect of MK-761 but not of compound A. The acute antihypertensive and positive inotropic effects of compound A are like to be at least partially due to stimulation of beta-adrenoceptors, e.g. intrinsic sympathomimetic activity. The effects of MK-761 on the same parameters appear to be mediated by different mechanisms.