Abstract
1 Twenty-two patients with moderately severe essential hypertension were treated for a period of 12 months with guanfacine (BS 100-141), a new centrally-acting antihypertensive agent. A twice daily schedule was followed and the dose range of guanfacine was 1-8 mg daily.
2 In twenty patients satisfactory blood pressure responses (diastolic pressure below 95 mmHg) were achieved in both the supine and the standing position. Pulse rate decreased slightly, though not significantly.
3 Tolerance to the pressure-lowering effect of the drug developed during the third or fourth month of therapy. This could be overcome by either increasing dosage or adding a diuretic.
4 All patients reported side-effects, mainly dryness of the mouth and fatigue. These side-effects became less or disappeared at the end of 3 months. Rebound hypertension on discontinuation of therapy occurred in two patients.
5 Plasma concentrations of noradrenaline and adrenaline as well as plasma renin activity were decreased after 1 week of treatment with the drug.
6 Guanfacine in conjunction with a diuretic is a useful drug in the long-term treatment of hypertension. Reduced central sympathetic outflow may be the major mechanism underlying the antihypertensive effect of the drug.
Full text
PDF



Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Bream J. B., Lauener H., Picard C. W., Scholtysik G., White T. G. Substituted phenylacetylguanidines: a new class of antihypertensive agents. Arzneimittelforschung. 1975 Oct;25(10):1477–1482. [PubMed] [Google Scholar]
- Da Prada M., Zürcher Simultaneous radioenzymatic determination of plasma and tissue adrenaline, noradrenaline and dopamine within the femtomole range. Life Sci. 1976 Oct 15;19(8):1161–1174. doi: 10.1016/0024-3205(76)90251-4. [DOI] [PubMed] [Google Scholar]
- Haber E., Koerner T., Page L. B., Kliman B., Purnode A. Application of a radioimmunoassay for angiotensin I to the physiologic measurements of plasma renin activity in normal human subjects. J Clin Endocrinol Metab. 1969 Oct;29(10):1349–1355. doi: 10.1210/jcem-29-10-1349. [DOI] [PubMed] [Google Scholar]
- Kirch W., Distler A. Antihypertensive effect of N-amidino-2-(2,6-dichlorophenyl) acetamide hydrochloride. A double-blind cross-over trial versus clonidine. Int J Clin Pharmacol Biopharm. 1978 Mar;16(3):132–135. [PubMed] [Google Scholar]
- Scholtysik G., Lauener H., Eichenberger E., Bürki H., Salzmann R., Müller-Schweinitzer E., Waite R. Pharmacological actions of the antihypertensive agent N-amidino-2-(2,6-dichlorophenyl)acetamide hydrochloride (BS 100-141). Arzneimittelforschung. 1975 Oct;25(10):1483–1491. [PubMed] [Google Scholar]
- Stumpe K. O., Kolloch R., Vetter H., Gramann W., Krück F., Ressel C., Higuchi M. Acute and long-term studies of the mechanisms of action of beta-blocking drugs in lowering blood pressure. Am J Med. 1976 May 31;60(6):853–865. doi: 10.1016/0002-9343(76)90905-0. [DOI] [PubMed] [Google Scholar]
