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. 1987 Dec;24(6):705–711. doi: 10.1111/j.1365-2125.1987.tb03235.x

Ketanserin in essential hypertension: use as monotherapy and in combination with a diuretic or beta-adrenoceptor antagonist.

H A Cameron 1, P C Waller 1, L E Ramsay 1
PMCID: PMC1386393  PMID: 2894215

Abstract

1. The antihypertensive efficacy and tolerability of twice-daily treatment with the 5-hydroxytryptamine antagonist ketanserin were examined in a double-blind, placebo-controlled trial of 7 weeks duration in 56 hypertensive patients. Twenty were untreated, 20 were already taking bendrofluazide 5 mg daily, and 16 were already taking atenolol 100 mg daily. Randomisation was stratified to compare ketanserin with placebo as monotherapy (n = 20), when added to bendrofluazide (n = 20), and when added to atenolol (n = 16). 2. The antihypertensive effect of ketanserin in all patients completing the study (mean daily dose 71 mg) was 10/6 mm Hg supine (P less than 0.01/P less than 0.01) and 6/6 mm Hg standing (NS/P less than 0.01) when blood pressure was measured 2 h after the morning dose. Responses were similar in patients taking ketanserin as monotherapy, in addition to bendrofluazide, and in addition to atenolol, with reductions in mean arterial pressure of 4.6, 7.4 and 8.9 mm Hg respectively. 3. Ketanserin had no antihypertensive effect when measured 14 h after the last dose. The rise in blood pressure between 2 and 14 h after dosing was 11/4 mm Hg supine (P less than 0.01/NS) and 8/5 mm Hg standing (P less than 0.05/P less than 0.05). 4. The antihypertensive response to ketanserin was positively related to initial blood pressure and, independent of this, to age. It was not related to plasma concentrations of ketanserin or ketanserinol. 5. Five of 28 patients taking ketanserin discontinued treatment because of side-effects, compared with one of 28 patients taking placebo.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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  1. Andrén L., Svensson A., Dahlöf B., Eggertsen R., Hansson L. Ketanserin in hypertension. Early clinical evaluation and dose finding study of a new 5-HT2 receptor antagonist. Acta Med Scand. 1983;214(2):125–130. [PubMed] [Google Scholar]
  2. Cameron H. A., Ramsay L. E. Ketanserin in essential hypertension: a double-blind, placebo-controlled study. Postgrad Med J. 1985 Jul;61(717):583–586. doi: 10.1136/pgmj.61.717.583. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. De Crée J., Hoing M., De Ryck M., Symoens J. The acute antihypertensive effect of ketanserin increases with age. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S126–S127. doi: 10.1097/00005344-198500077-00037. [DOI] [PubMed] [Google Scholar]
  4. Fagard R., Fiocchi R., Lijnen P., Staessen J., Moerman E., de Schaepdryver A., Amery A. Haemodynamic and humoral responses to chronic ketanserin treatment in essential hypertension. Br Heart J. 1984 Feb;51(2):149–156. doi: 10.1136/hrt.51.2.149. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Freestone S., Silas J. H., Ramsay L. E. Sample size for short-term trials of antihypertensive drugs. Br J Clin Pharmacol. 1982 Aug;14(2):265–268. doi: 10.1111/j.1365-2125.1982.tb01971.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Hedner T., Persson B., Berglund G. A comparative and long-term evaluation of ketanserin in the treatment of essential hypertension. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S148–S153. doi: 10.1097/00005344-198500077-00042. [DOI] [PubMed] [Google Scholar]
  7. Hedner T., Persson B., Berglund G. Ketanserin, a novel 5-hydroxytryptamine antagonist: monotherapy in essential hypertension. Br J Clin Pharmacol. 1983 Aug;16(2):121–125. doi: 10.1111/j.1365-2125.1983.tb04974.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Hedner T., Persson B. Ketanserin in combination with beta-adrenergic receptor blocking agents in the treatment of essential hypertension. Br J Clin Pharmacol. 1984 Nov;18(5):765–771. doi: 10.1111/j.1365-2125.1984.tb02540.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Heykants J., Van Peer A., Woestenborghs R., Gould S., Mills J. Pharmacokinetics of ketanserin and its metabolite ketanserin-ol in man after intravenous, intramuscular and oral administration. Eur J Clin Pharmacol. 1986;31(3):343–350. doi: 10.1007/BF00981135. [DOI] [PubMed] [Google Scholar]
  10. Soffer J., Dreifus L. S., Michelson E. L. Polymorphous ventricular tachycardia associated with normal and long Q-T intervals. Am J Cardiol. 1982 Jun;49(8):2021–2029. doi: 10.1016/0002-9149(82)90224-7. [DOI] [PubMed] [Google Scholar]
  11. Staessen J., Fagard R., Fiocchi R., Lijnen P., Rorive G., Amery A. Double-blind comparison of ketanserin with propranolol in hypertensive patients: interim report. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S140–S147. doi: 10.1097/00005344-198500077-00041. [DOI] [PubMed] [Google Scholar]
  12. Waal-Manning H. J., Brown S. A., Spears G. F., Simpson F. O. Clinical studies with ketanserin in hypertension. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S154–S158. doi: 10.1097/00005344-198500077-00043. [DOI] [PubMed] [Google Scholar]
  13. Wenting G. J., Man in 't Veld A. J., Woittiez A. J., Boomsma F., Schalekamp M. A. Treatment of hypertension with ketanserin, a new selective 5-HT2 receptor antagonist. Br Med J (Clin Res Ed) 1982 Feb 20;284(6315):537–539. doi: 10.1136/bmj.284.6315.537. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Wing L. M., Chalmers J. P., West M. J., Bune A. J., Ayres B., Graham J. R. Effect of ketanserin on blood pressure and biochemical parameters in patients with essential hypertension. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S164–S167. doi: 10.1097/00005344-198500077-00046. [DOI] [PubMed] [Google Scholar]
  15. de Leeuw P. W., Birkenhäger W. H. Chronic effects of serotonin inhibition in hypertensive patients: hemodynamic and humoral findings. J Cardiovasc Pharmacol. 1985;7 (Suppl 7):S137–S139. doi: 10.1097/00005344-198500077-00040. [DOI] [PubMed] [Google Scholar]

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