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Selective α1-adrenoreceptor blockers in the treatment of hypertension: Should we be using them more?

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Abstract

It has become apparent in recent years that in the treatment of essential hypertension, reduction of blood pressure alone is not sufficient to reduce significantly the morbidity and mortality from ischaemic heart disease. Since the emergence of a multifactorial approach to the prevention of cardiovascular disease, the potential interaction between antihypertensive therapy and metabolic factors, such as control of blood glucose and lipid levels, has become an important consideration. Abnormal function of the sympathetic nervous system may contribute to both the initiation, or maintenance, of hypertension and the associated metabolic disturbances. The new generation of selective α1-adrenoreceptor blockers, besides lowering blood pressure, appear to have favourable effects on lipid and glucose metabolism. The use of these drugs and their place in the treatment of hypertension are discussed.

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References

  1. Pollare T, Lithell H, Selinus I, Berne C. Application of prazosin is associated with an increase of insulin sensitivity in obese patients with hypertension.Diabetologia 1988;31: 415–420.

    PubMed  Google Scholar 

  2. Julius S. Changing the role of the autonomic nervous system in human hypertension.J Hypertension 1990;8: S59-S65.

    Google Scholar 

  3. Goldstein DS. Plasma catecholamines and essential hypertension: an analytical review.Hypertension 1983;5: 86–99.

    PubMed  Google Scholar 

  4. Julius S. The emerging field of borderline hypertension.J Cardiovasc Pharmacol 1986;8(suppl): 54–57.

    Google Scholar 

  5. Lunds-Johansen P. Haemodynamics in early essential hypertension.Acta Med Scand 1967;482(suppl): 1–105.

    Google Scholar 

  6. Safar ME, Weiss YA, Levenson JA. Haemodynamic study of 85 patients with borderline hypertension.Am J Cardiol 1973;31: 315–319.

    PubMed  Google Scholar 

  7. Frohlich ED, Kozu VJ, Tarazi RC. Physiologic comparison of labile and essential hypertension.Circ Res 1970;26 (suppl 1): 155–169.

    Google Scholar 

  8. Julius S, Conway J. Haemodynamic studies in patients with borderline blood pressure elevation.Circulation 1960;38: 282–288.

    Google Scholar 

  9. Julius S, Esler M. Autonomic nervous cardiovascular regulation in borderline hypertension.Am J Cardiol 1975;36: 685–696.

    PubMed  Google Scholar 

  10. Julius S, Pascual AV, London R. Role of parasympathetic inhibition in the hyperkinetic type of borderline hypertension.Circulation 1971;44: 413–418.

    PubMed  Google Scholar 

  11. Esler M, Jennings G, Biviano B. Mechanism of elevated plasma noradrenaline in the course of essential hypertension.J Cardiovasc Pharmacol 1986;8 (suppl 5): S39-S43.

    Google Scholar 

  12. Guzzetti S, Piccaluga E, Casati R. Sympathetic predominance in essential hypertension: a study employing spectral analysis of heart rate variability.J Hypertens 1988;6: 711–717.

    PubMed  Google Scholar 

  13. Anderson EA, Sinkery CA, Rawton WJ. Elevated sympathetic nerve activity in borderline hypertensive humans: evidence from direct intraneural recordings.Hypertension 1989;14: 177–183.

    PubMed  Google Scholar 

  14. Frohlich ED, Tarazi RC, Dustan HP. Hyperdynamic beta-adrenergic circulatory state: increased beta-receptor responsiveness.Arch Intern Med 1969;123: 1–7.

    PubMed  Google Scholar 

  15. Julius S, Randall OS, Esler MD. Altered cardiac responsiveness and regulation in the normal cardiac output type of borderline hypertension.Circ Res 1975;36–37 (suppl 1): I 191 1-I 191 207.

    Google Scholar 

  16. Trimarco B, Volpe M, Ricciardelli B. Studies of the mechanisms underlying impairment of beta-adrenoreceptor mediated effects in human hypertension.Hypertension 1983;5: 584–590.

    PubMed  Google Scholar 

  17. Bertel O, Buhler FR, Kiowski W. Decreased beta-adrenoreceptor responsiveness as related to age, blood pressure and plasma catecholamines in patients with essential hypertension.Hypertension 1980;2: 130–138.

    Google Scholar 

  18. Sivertsson R. The haemodynamic importance of structural vascular changes in essential hypertension.Acta Physiol Scand 1970;79 (suppl 343): 3–56.

    Google Scholar 

  19. Folkow B. Physiological aspects of primary hypertension.Physiol Rev 1982;62: 347–503.

    PubMed  Google Scholar 

  20. Philipp TH, Distler A, Cordes V. Sympathetic nervous system on blood pressure control in essential hypertension.Lancet 1978;ii: 959–963.

    Google Scholar 

  21. Ostman-Smith J. Cardiac sympathetic nerves as the final common pathway in the induction of adaptive cardiac hypertrophy.Clin Sci 1981;61: 265–272.

    PubMed  Google Scholar 

  22. Meggs LG, Ben-Ari J, Gammon D, Goodman AI. Myocardial hypertrophy: the effect of sodium and the role of sympathetic nervous system activity.Am J Hypertens 1988;1: 11–15.

    PubMed  Google Scholar 

  23. Verrier RL, Lown B. Behavioral stress and cardiac arrhythmias.Annu Rev Physiol 1984;46: 155–176.

    PubMed  Google Scholar 

  24. Borhani NO. Left ventricular hypertrophy arrhythmias and sudden death in systemic hypertension.Am J Cardiol 1987;60: 131–181.

    Google Scholar 

  25. Izzo JLJ. Sympathoadrenal activity, catecholamines and the pathogenesis of vasculopathic hypertensive target-organ damage.Am J Hypertens 1989;2: 305 S-312 S.

    Google Scholar 

  26. Kalley MC, Smith RJ, Izzo JLJ. The contribution of plasma norepinephrine, renin and age to compliance (abstract).Chest 1986;89: 495.

    Google Scholar 

  27. Bonaduce D, Ferrara N, Petretta M, Cononico V, Romango E, Rengo F. Comparison of the antihypertensive activities of xipamide and chlorthalidone: a double-blind randomized, crossover trial.Curr Med Res Opinion 1981;7: 247–252.

    Google Scholar 

  28. Egan B, Julius S. Vascular hypertrophy in borderline hypertension: relationship to blood pressure and sympathetic drive.Clin Exp Hypertens 1985;A7: 243–255.

    Google Scholar 

  29. Clayton S, Cross MJ. The aggregation of blood platelets by catecholamines and by thrombin.J Physiol (Lond) 1963;169: 81.

    Google Scholar 

  30. Mathias CJ. Role of the central nervous system in human secondary hypertension.J Cardiovasc Pharmacol 1987;10 (suppl 12): 593–599.

    PubMed  Google Scholar 

  31. Lucci MS, Pucacco LR, Dubose TD, Kokko JP, Carter NW. Direct evaluation of acidification by rat proximal tubule: role of carbonic anhydrase.Am J Physiol 1980;238: F372-F379.

    PubMed  Google Scholar 

  32. Brown JJ, Cuesta V, Davis Dlet AL. Mechanisms of renal hypertension.Lancet 1976; 1219–1221.

  33. Severs WB, Daniels-Severs AE. Effects of angiotensin on the central nervous system.Pharmacol Rev 1973;25: 415–449.

    PubMed  Google Scholar 

  34. Izzo JLJ, Licht MR, Smith RJ. Chronic effects of direct vasodilation (pinacidil), alpha-adrenergic blockade (prazosin) and angiotensinconverting enzyme inhibition (captopril).Am J Cardiol 1987;60: 303–308.

    PubMed  Google Scholar 

  35. Mathias CJ, Wilkinson AH, Lewis Pset AL. Clonidine lowers blood pressure independently of renin supression in patients with unilateral renal artery stenosis.Chest 1983;83: 357–359.

    PubMed  Google Scholar 

  36. Akpogomeh BA, Johns EJ. The characteristics of alpha-adrenoceptors mediating the renal nerve induced antinatriuresis and antidiuresis in hypertensive rats.J Hypertension 1991;9: 373–384.

    Google Scholar 

  37. Himanen P. Serum lipid changes in a one-year, multicentre, double-blind comparison of doxazosin and atenolol for mild to moderate essential hypertension.Am J Cardiol 1987;59: 616–676.

    Google Scholar 

  38. Van Zwieten PA, Timmermans P. Cardiovascular alpha2-adrenoceptors.J Mol Cell Cardiol 1983;15: 717–733.

    PubMed  Google Scholar 

  39. Van Zwieten PA. Role of alpha-adrenoceptors in hypertension and antihypertensive drug treatment.Am J Med 1984;77: 17–25.

    Google Scholar 

  40. Langer SZ, Masingham R, Shepperson NB. Presence of postsynaptic alpha2-adrenoceptors of predominantly extrasynaptic location in the vascular smooth muscle of the dog hind limb.Clin Sci 1980;59: 225S-228S.

    PubMed  Google Scholar 

  41. Van Zwieten PA. In:Alpha-adrenoceptor-blocking Agents in the Treatment of Hypertension. New York, B. M. Brenner Raven Press, 1990; 2233.

    Google Scholar 

  42. Michel MC, Insel PA. Are there multiple imidazoline binding sites?Trends Pharmacol Sci 1989;10: 342–344.

    PubMed  Google Scholar 

  43. McMahon FG.Management of Essential Hypertension. Mount Kisco, 1978.

  44. Langer SZ. Presynaptic regulation of catecholamine release.Biochem Pharmacol 1974;23: 1793–1800.

    PubMed  Google Scholar 

  45. Lowerstein J, Steele JM. Prazosin.Am Heart J 1978;95: 262–265.

    PubMed  Google Scholar 

  46. Veterans Administration Cooperative Study Group on Antihypertensive Agents. Effects of treatment on morbidity in hypertension: II. Results of patients with diastolic blood pressure averaging 90 through 114 mmHg.J Am Med Assoc 1970;213: 1143–1151.

    Google Scholar 

  47. Langer SZ, Cavero I, Massingham R. Recent developments in noradrenergic neurotransmission and its relevance to the mechanism of action of certain antihypertensive drugs.Hypertension 1980;2: 372–382.

    PubMed  Google Scholar 

  48. Graham RM, Pettinger WA. Effects of prazosin and phentolamine on arterial pressure, heart rate and renin activity. Evidence in the conscious rat for the functional significance of the presynaptic alpha-blockade.J Cardiovasc Pharmacol 1982;4: 44–52.

    PubMed  Google Scholar 

  49. Cox DA, Leader JP, Milson JA. The antihypertensive effects of doxazosin: a clinical overview.Br J Clin Pharmacol 1991.

  50. Reid J, Davies HC. Alpha1 -adrenoceptor blockade in hypertension: pharmacological and clinical profile of doxazosin.Br J Clin Pharmacol 1986;21 (suppl 1).

  51. Elliott HL, Meredith PA, Reid JL. Pharmacokinetic overview of doxazosin.Am J Cardiol 1987;59: 786–816.

    Google Scholar 

  52. Lund-Johansen P, Omvik P, Hangland H. Acute and chronic haemodynamic effects of doxazosin in hypertension at rest and during exercise.Br J Clin Pharmacol 1986;21: 45S-54S.

    PubMed  Google Scholar 

  53. Gillin A, Fletcher P, Horvath J. Comparison of doxazosin and atenolol in mild hypertension and effects on exercise capacity, hemodynamics and left ventricular function.Am J Cardiol 1989;63: 950–954.

    PubMed  Google Scholar 

  54. Leenen FHH, Smith DL, Farkas RM. Vasodilators and regression of left ventricular hypertrophy: hydralazine versus prazosin in hypertensive humans.Am J Med 1987;82: 969–978.

    PubMed  Google Scholar 

  55. Graham RM, Pettinger WA. Prazosin.N Engl J Med 1979;300: 232–236.

    PubMed  Google Scholar 

  56. Graham RM, Mulvihill-Wilson J. Clinical pharmacology of prazosin used alone or in combination in the therapy of hypertension.J Cardiovasc Pharmacol 1980;2 (suppl 13): 5387–5398.

    Google Scholar 

  57. Okun R, Kraut J. Prazosin versus captopril as initial therapy: effect on hypertension and lipid levels.Am J Med 1987;82: (suppl 4A): 29–34.

    Google Scholar 

  58. Dauer AD. Terazosin: an effective once-daily monotherapy for the treatment of hypertension.Am J Med 1986;80 (suppl 5B): 29–34.

    Google Scholar 

  59. Deger G, Cutler RE, Dietz AJJ. Comparison of the safety and efficacy of once-daily terazosin versus twice-daily prazosin for the treatment of mild to moderate hypertension.Am J Med 1986;80 (suppl 5B): 62–67.

    Google Scholar 

  60. Mersey JH. Long-term experience with terazosin for the treatment of mild to moderate hypertension.Am J Med 1985;80 (suppl 5B): 68–72.

    Google Scholar 

  61. Pool JL, Nelson EB, Taylor AA. Terazosin (Hytrin): cumulative experience of clinical trials in the USA for the treatment of mild to moderate essential hypertension.Br J Clin Pract 1987;41 (suppl 54): 9–14.

    Google Scholar 

  62. Hayduk K, Schneider HT. Antihypertensive effects of doxazosin in systemic hypertension and comparison with terazosin.Am J Cardiol 1987;59: 956–986.

    PubMed  Google Scholar 

  63. Taylor SH. Pharmacotherapeutic stature of doxazosin and its role in coronary risk reduction.Am Heart J 1988;116: 1735–1747.

    PubMed  Google Scholar 

  64. Smythe P, Pringle S, Jackson G, Lorimer AR. Twenty-four hour control of blood pressure by once daily doxazosin: a multicentre double-blind comparison with placebo.Eur J Clin Pharmacol 1988;34: 613–618.

    PubMed  Google Scholar 

  65. Rosenthal J. Clinical experience with doxazosin in general medical practice.Am Heart J 1988;116: 1748–1757.

    PubMed  Google Scholar 

  66. Stamler R, Stamler J, Gosch FG. Initial anti-hypertensive drug therapy: alpha blocker or diuretic.Am J Med 1986;80 (suppl 2A): 90–93.

    PubMed  Google Scholar 

  67. Trost BN, Weidmann P, Riesen W. Comparative effects of doxazosin and hydrochlorothiazide on serum lipids and blood pressure in essential hypertension.Am J Cardiol 1987;59: 996–1046.

    PubMed  Google Scholar 

  68. Kirkendall WM. Comparative assessment of first-line agents for treatment of hypertension.Am J Med 1988;84 (suppl 3B): 32–41.

    PubMed  Google Scholar 

  69. Nechwatal W, Berger J, Blumrich W. A double-blind comparative study of doxazosin and nitrendipine in patients with mild to moderate essential hypertension.Am Heart J 1988;116: 1806–1814.

    PubMed  Google Scholar 

  70. Taylor SH, Lee PS, Sharma SK. A comparison of doxazosin and enalapril in the treatment of mild and moderate essential hypertension.Am Heart J 1988;116: 1820–1825.

    PubMed  Google Scholar 

  71. Rudd P, Berenson G, Brown M. Comparative trials of terazosin with other antihypertensive agents.Am J Med 1986;80 (suppl 5B): 49–54.

    PubMed  Google Scholar 

  72. Chrysant SG. Experience with terazosin administered in combination with other antihypertensive agents.Am J Med 1986;80 (suppl 5B): 55–61.

    Google Scholar 

  73. Davies RO, Irvin JD, Kramach DK. Enalapril worldwide experience.Am J Med 1984;77 (suppl 2A): 23–35.

    Google Scholar 

  74. Honna M, Ui M. Plasma cyclic GMP: response to cholinergic agents.Eur J Pharmacol 1978;47: 1–10.

    PubMed  Google Scholar 

  75. Weth VG, Schneider J, Rodatz H, Haubitz I. Effect of B-blocker nadolol on the second messenger cyclic adenosine monophosphate in serum and on blood pressure and heart rate.Arzneimittelforschung 1985;35: 1711–1713.

    PubMed  Google Scholar 

  76. Rouffy J, Jaillard J. Effects of two antihypertensive agents on lipids, lipoproteins and apoproteins A & B; comparison of prazosin and atenolol.Am J Med 1986;80 (suppl 2A): 100–103.

    Google Scholar 

  77. Talseth T, Westlie L, Daac L, Vatle S. Comparison of the effects of doxazosin and atenolol on blood pressure and blood lipids: a one year, double-blind study in 228 hypertensive patients.Am Heart J 1988;116: 1790–1796.

    PubMed  Google Scholar 

  78. Howenstein J, Neusy AJ. Effects of prazosin and propranolol on serum lipids in patients with essential hypertension.Am J Med 1984;76: 79–84.

    Google Scholar 

  79. Frick M, Halttunen P, Himanem P. A long term double-blind comparison of doxazosin and atenolol in patients with mild to moderate essential hypertension.Br J Clin Pharmacol 1986;21: 55S-62S.

    PubMed  Google Scholar 

  80. Chichester CO, Rodgers RL. Effects of doxazosin on vascular collagen synthesis, arterial pressure and serum lipids in the spontaneously hypertensive rat.J Cardiovasc Pharmacol 1987;10: S21-S26.

    PubMed  Google Scholar 

  81. Grimm RHJ. Alpha 1 antagonists in the treatment of hypertension.Hypertension 1989;13 (suppl I): I-131–I-136.

    Google Scholar 

  82. Sperzel WD, Glassman H, Jordan DC. Overall safety of terazosin as an antihypertensive agent.Am J Med 1986;80 (suppl 5B): 77–81.

    Google Scholar 

  83. Gifford RW, Borazanian RA. Traditional first-line therapy.Hypertension 1989;13 (suppl I): I-119–I-124.

    Google Scholar 

  84. Krane RJ, Goldstein I, Saenz de Tejada I. Impotence.N Engl J Med 1989;321: 1648–1659.

    PubMed  Google Scholar 

  85. Max B. This and that: an unsuitable eponym, leeches, and the transmutation of the disciplines.Trends in Pharmacol Sci 1990;11: 143–146.

    Google Scholar 

  86. Siegel S, Streem SB, Steinmuller DR. Prazosin-induced priapism. Pathogenic and therapeutic implications.Br J Urology 1988;61: 165.

    Google Scholar 

  87. Kirby RS, Coppinger SWC, Corcoran MO, Chapple CR, Flannigan M, Milroy EJ. Prazosin in the treatment of prostatic obstruction. A placebo controlled study.Br J Urol 1987;60: 136–142.

    PubMed  Google Scholar 

  88. Lepor H, Knapp-Maloney G, Wozniak-Petrofsky PJ. The safety and efficacy of terazosin for the treatment of benign prostatic hyperplasia.Int J Clin Pharmacol Ther Toxicol 1989;27: 392–397.

    PubMed  Google Scholar 

  89. Chapple CR, Christmas TJ, Milroy EJG. A twelve week placebo controlled study of prazosin in the treatment of prostatic obstruction.Urol Int 1990;45: 47–55.

    PubMed  Google Scholar 

  90. Cramer P, Nerveux E, Regnier F, Depassio J, Berard E. Bladder-neck opening test in spinal cord injury patients using a new i.v. alpha-blocking agent, alfuzosin.Paraplegia 1989;27: 119–124.

    PubMed  Google Scholar 

  91. Dollery CT, Warren JB. The usefulness of alpha-adrenoceptor blockade in the treatment of hypertension.J Hypertens 1988;6 (suppl 12): S43-S49.

    Google Scholar 

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Ligueros, M., Unwin, R. & Wilkins, M. Selective α1-adrenoreceptor blockers in the treatment of hypertension: Should we be using them more?. Clinical Autonomic Research 1, 251–258 (1991). https://doi.org/10.1007/BF01824996

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