Summary
The kinetics and short-term (10 weeks) effects of trimazosin, an alpha1-adrenoreceptor antagonist, on renal function and blood pressure in patients with moderate chronic renal insufficiency and hypertension, have been studied for the first time. Eight patients in whom the blood pressure was not normalized with a diuretic alone underwent pharmacokinetic studies and assessment of the renal function during a 10-week period of trimazosin therapy. Trimazosin significantly lowered blood pressure (recumbent and upright) without significantly altering renal function. Renal vascular resistance was decreased by 14%. Fractional sodium excretion, proteinuria and laboratory serum tests remained unchanged. Neither body weight nor pulse rate were affected. Moderate renal insufficiency did not modify the pharmacokinetics of the drug. Thus, trimazosin, as second-step antihypertensive agent, appeared to be safe and effective in patients with moderate renal insufficiency and hypertension, without exerting favourable or adverse renal effects during short-term therapy.
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References
Reid JL, Meredith PA, Eliott HL (1983) Pharmacokinetics and pharmacodynamics of trimazosin in man. Am Heart J 106: 1222–1227
Koshy MC, Mickley D, Boorgoignie J, Blaufox MD (1977) Physiologic evaluation of a new antihypertensive agent: Prazosin HCL. Circulation 55: 533–537
Cambridge D, Davey MJ, Massingham R (1977) Prazosin, a selective antagonist of postsynaptic alpha1-adrenoreceptors. Br J Pharmacol 59: 514–515
Chrysant SG (1983) Autonomic, systemic and renal haemodynamic actions of trimazosin in hypertensive patients. Am Heart J 106: 1243–1250
Constantine JW, Hess HJ (1981) The cardiovascular effects of trimazosin. Eur J Pharmacol 74: 227–238
Chrysant SG, Miller RF, Brown JL, Danisa K (1981) Long-term haemodynamic and metabolic effects of trimazosin in essential hypertension. Clin Pharmacol Ther 30: 600–612
DeGuia D, Mendlowitz M, Russo C, Vlachakis N, Antram S (1973) The effect of trimazosin in essential hypertension. Curr Ther Res 15: 339–348
Vlachakis N, Mendlowitz M, Deguzman D (1975) Treatment of essential hypertension with trimazosin, a new vasodilator agent. Curr Ther Res 17: 564–569
Pool PE, Seagren SC, Salel AF (1983) Clinical haemodynamic profile of trimazosin in hypertension. Am Heart J 106: 1237–1242
Aronow WS, Tobis J, Hughes D, Siegel J, Easthope J (1977) Comparison of trimazosin and methyldopa in hypertension. Clin Pharmacol Ther 22: 425–429
Taylor CR, Leader JP, Singleton W, Munster EW, Falkner FC, O'Neil JA (1983) Profile of trimazosin: An effective and safe antihypertensive agent. Am Heart J 106: 1269–1283
Chrysant SG, Luu TM, Danisa K, Kem DC, Manion CV (1980) Systemic and renal haemodynamic effects of trimazosin: a new vasodilator. J Cardiovasc Pharmacol 2: 205–214
Hughes MA, Meredith PA, Eliott HL (1986) The determination of trimazosin and its metabolite (CP 23445) in whole blood by high performance liquid chromatography using fluorescence detection. J Chromatogr (in press)
Donker AJM, van der Hem GK, Sluiter WJ, Beekhuis H (1977) A radioisothope method for simultaneous determination of the glomerular filtration rate and the effective renal plasma flow. Neth J Med 20: 97–102
Gomez DM (1951) Evaluations of renal resistance with special reference to changes in essential hypertension. J Clin Invest 30: 1143–1155
Starke K, Docherty JR (1980) Recent developments in alpha-adrenoreceptor research. J Cardiovasc Pharmacol 2: 269–286
O'Connor DT, Preston RA, Sasso EH (1979) Renal perfusion changes during treatment of essential hypertension: prazosin versus propranolol. J Cardiovasc Pharmacol 1: 38–42
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van Kalken, C.K., van der Meulen, J., Oe, P.L. et al. Pharmacokinetics of trimazosin and its effects on blood pressure, renal function and proteinuria during short-term therapy of patients with impaired renal function and hypertension. Eur J Clin Pharmacol 31, 63–68 (1986). https://doi.org/10.1007/BF00870988
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DOI: https://doi.org/10.1007/BF00870988