(-)-Timolol is a more potent antagonist of the positive inotropic effects of (-)-adrenaline than of those of (-)-noradrenaline in human atrium

British Journal of Clinical Pharmacology

Volumn 42, Issue 2, 1996, Pages 217-223

  Wang, T ^a   Kaumann, A J ^b   Brown, M J ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b BABRAHAM INSTITUTE   (United Kingdom)

Author keywords

Adrenaline; Human atrium; Noradrenaline; Timolol; 1 and 2 adrenoceptors

Indexed keywords

ADRENALIN; ATENOLOL; BETA 1 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; METOPROLOL; NORADRENALIN; TIMOLOL;

ARTICLE; DRUG ANTAGONISM; DRUG HALF LIFE; DRUG RECEPTOR BINDING; ENANTIOMER; HEART ATRIUM; HUMAN; HUMAN TISSUE; INOTROPISM; PRIORITY JOURNAL;

EID: 0030035631     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1996.39412.x     Document Type: Article

References (48)

1. Zimmerman TJ, Kaufman HE. Timolol, a beta-adrenergic blocking agent for the treatment of glaucoma. Arch Ophthalmol 1977; 95: 601-604.
2. Obrien KP, Croxson RS. Timolol maleate (Blocadren) in the treatment of essential hypertension. NZ Med J 1975; 82: 293-296.
3. Lund-Johansen P. Hemodynamic long-term effects of timolol at rest and during exercise in essential hypertension. Acta Med Scand 1976; 199: 263-267.
4. The Norwegian Multicenter Study Group. Timolol-induced reduction in mortality and reinfarction in patients surviving acute myocardial infarction. N Engl J Med 1981; 304: 801-807.
5. Zimmerman TJ, Leader BJ, Golob DS. Potential side effects of timolol therapy in the treatment of glaucoma. Ann Opthalmol 1981; 13: 683-689.
6. Atkins JM, Pugh BR, Time RM. Cardiovascular effect of topical beta-blockers during exercise. Am J Ophthalmol 1985; 99: 173-175.
7. Guzman CA. Exacerbation of bronchorrhea induced by topical timolol, letter. Am Rev Respir Dis 1980; 121: 889.
8. Lawrsen SO, Bjerrum P. Timolol eyedrop-induced severe bronchospasm. Acta Med Scand 1982; 211: 505.
9. Noyes JH, Chervinsky P. Case report: exacerbation of asthma by timolol. Ann Allergy 1980; 45: 301.
10. Nelson WL, Fraunfelder FT, Sills JM, Arrowsmith JB, Kuritsky JN. Adverse respiratory and cardiovascular events attributed to timolol ophthalmic solution, 1978-1985. Am J Opthalmol 1986; 102: 606-611.
11. Van Buskirk EM. Adverse reaction from timolol administration. Ophthalmology 1980; 87: 447-450.
12. Williams T, Ginter WH. Hazard of ophthalmic timolol. N Engl J Med 1982; 306: 1485-1486.
13. Jones FL, Ekberg NL. Exacerbation of asthma by timolol. N Engl J Med 1979; 301:270.
14. Im Hof V. Beta blocker drugs and asthma. Schweizerische Rundschau fur Medizin/Praxis 1995; 84: 319-320.
15. Phan TMM, Nguyen KPV, Giacomini JC, Lee DA. Ophthalmic beta-blockers: determination of plasma and aqueous humor levels by a radioreceptor assay following multiple doses. J Ocular Pharmacol 1991; 7: 243-252.
16. Saari KM, Ali-Melkkila T, Vuori ML, Kaila T, Lisalo E. Absorption of ocular timolol drug concentrations and β-receptor binding activity in the aqueous humour of the treated and contralateral eye. Acta Ophthalmol 1993; 71: 671-676.
17. 2-antagonist activity of topically applied betaxolol and timolol in the systemic circulation. Acta Ophthalmol 1993; 71: 682-685.
18. 2-adrenoceptors in the stimulation of adenylate cyclase and concentractile force. Eur Heart J 1989; 10 (suppl B): 29-37.
19. 2-adrenoceptors in human atrial myocardium. Circ Res 1990; 66: 1610-1623.
20. 1-antagonist treatment. Circ Res 1991; 69: 959-964.
21. 2-adrenoceptor blockade. Br J Clin Pharmacol 1993; 35: 539P.
22. Hall JA, Ferro A, Dickerson JEC, Brown MJ. Beta adrenoceptor subtype cross regulation in the human heart. Br Heart J 1993; 69: 332-337.
23. Tocco DJ, Duncan AEW, Deluna FA, Hucker HB, Gruber VF, Vandenheuvel WJA. Physiological disposition and metabolism of timolol in man and laboratory animals. Drug Metab Dispos 1975; 3: 361-370.
24. Tocco DJ, Deluna FA, Duncan AEW. Electron-capture GLC determination of timolol in human plasma and urine. J Pharm Sci 1975; 64: 1879-1881.
25. Lancaster SG, Sorkin EM. Bisoprolol: a preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. Drugs 1988; 36: 256-285.
26. Kaumann AJ, Lemoine H, Schwederski-Menke U, Ehle B. Relations between β-adrenoceptor occupancy and increases of contractile force and adenylate cyclase activity induced by catecholamines in human ventricular myocardium - acute desensitization and comparison with feline ventricle. Naunyn-Schmiedeberg's Arch Pharmacol 1989; 339: 99-112.
27. 2-adrenoceptors of human atrium and ventricle to the effects noradrenaline and adrenaline as assessed with (-)-atenolol. Br J Pharmacol 1988; 95: 55-66.
28. 2-adrenoceptors of human heart. Differential antagonism of the positive inotropic effects and adenylate cyclase stimulation by (-)-noradrenaline and (-)-adrenaline. Naunyn-Schmiedeberg's Arch Pharmacol 1985; 331: 60-70.
29. Kaumann AJ, Lobnig BM. Mode of action of (-)-pindolol on feline and human myocardium. Br. J Pharmacol 1986; 89: 207-218.
30. Ablad B, Carlsson B, Carsson E, Danlof C, Ek L, Hultberg E. Cardiac effects of β-adrenergic receptor antagonists. Adv Cardiol 1974; 12: 290-302.
31. Kaumann AJ, Mcinerny TK, Gilmour DP, Blinks JR. Comparative assessment of β-adrenoceptor blocking agents as simple competitive antagonist in isolated heart muscle: similarity of inotropic and chronotropic blocking potencies against isoproterenol. Naunyn-Schmiedeberg's Arch Pharmacol. 1980; 311: 219-236.
32. Arunlakshana O, Schild HO. Some quantitative uses of drug antagonists. Br J Pharmacol 1959; 14: 48-58.
33. 125I]iodocyanopindolol binding. Circ Res 1983; 53: 752-758.
34. Clifton GD, Chandler MHH, Pennell MR, McCoy RA Harrison MR. Differential response of β-adrenregic receptor-mediated heart rate and aortic blood flow acceleration to timolol. Clin Pharmacol Ther 1992; 51: 296-301.
35. Molenaar P, Russell FD, Shimada T, Summers RJ. Function, characterization and autoradiographic location and quantitation β-adrenoceptors in cardiac tissues. Clin Exp Pharmacol Physiol 1989; 16: 529-533.
36. Motomura S, Zerkowski HR, Brodde OE. On the physiologic role of beta-2 adrenoceptors in the human heart: in vitro and in vivo studies. Am Heart J 1990; 119: 608-619.
37. Brodde OE. Cardiac beta-adrenergic receptors. ISI Atlas Sci Pharmacol 1987; 1: 107-112.
38. Dunn TL, Gerber MJ, Shen AS, Fernandez E, Iseman MD, Cherniack RM. The effect of topical ophthalmic instillation of timolol and betaxolol on lung function in asthmatic subjects. Am Rev Respir Dis 1986; 133: 264-268.
39. Ward RL, Beasley H. Effects of topical betaxolol, timolol, and placebo on pulmonary function in asthmatic bronchitis. Am J Ophthalmol 1984; 97: 86-92.
40. Zimmerman TJ, Kaufman HE. Timolol, dose response and duration of action. Arch Ophthalmol 1977; 95: 605-607.
41. McMahon CD, Shaffer RN, Hoskins HD, Hetherington J. Adverse effects experienced by patients taking timolol. Am J Ophthalmol 1979; 88: 736-738.
42. Prince DS, Carliner NH. Respiratory arrest following first dose of timolol ophthalmic solution. Chest 1983; 608: 640.
43. Diggory P, Heyworth P, Chau G, Mckenzie S, Sharma A. Unsuspected bronchospasm in association with topical timolol- a common problem in elderly people: can we easily identify those affected and do cardioselective agents lead to improvement? Age and Ageing 1994; 23: 17-21.
44. Diggory P, Casselsbrown A, Vall A, Abbey LM, Hillman JS. Avoiding unsuspected respiratory side-effects of topical timolol with cardioselective or sympathomimetic agents. Lancet 1995; 345: 1604-1606.
45. Diggory P, Heyworth P, Chau G, Mckenzie S, Sharma A, Luke I. Improved lung function tests on changing from topical timolol: Non-selective betablockade impairs lung function tests in elderly patients. Eye 1993; 7: 661-663.
46. Levy NS, Boone L, Ellis E. A control comparison of betaxolol and timolol with long-term evalution of safety and efficacy. Glaucoma 1985; 7: 54-62.
47. Schoene RB, Abulan T, Ward RL, Beasley H. Effects of topical betaxolol, timolol and placebo on pulmonary function in asthmatic bronchitis. Am J Ophthalmol 1984; 97: 86-92.
48. Chiou GCY. Development of D-timolol for the treatment of glaucoma and ocular hypertension. J Ocular Pharmacol 1990; 6: 67-74.