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Time‐dependent antihypertensive effect of carteolol—A beta‐adrenoceptor antagonist with partial agonist activity
Author(s) -
Giles Thomas D,
Sander Gary E,
Kaneish Ahmed,
Quiroz Antonio C
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.34
Subject(s) - partial agonist , antagonist , pharmacology , agonist , adrenergic beta antagonists , chemistry , medicine , receptor , propranolol
The antihypertensive effect of Carteolol (0.5 to 60 mg daily), a β‐adrenoceptor antagonist with partial agonist activity, was studied in a double‐blind parallel protocol. A 3‐wk placebo period was followed by an 8‐wk treatment period during which patients received 0.5, 2.5, 20, and 60 mg in an increasing (group 1) or decreasing (group 2) manner for successive 2‐wk intervals, followed by a 2‐ to 6‐wk withdrawal period. Resting supine and standing blood pressures (BP) and heart rates (HR) were measured at each visit. Isometric handgrip exercise and treadmill exercise were used to evaluate β‐blockade. Plasma Carteolol concentration was measured by radioimmunoassay. Recumbent BP fell from 154 ± 101100 ±2 to 143 ± 10184 ± 11 mm Hg for group 1 and from 153 ± 101100 ±3 to 138 ± 14178 ±8 mm Hg for group 2 after 8 wk of treatment. HR was unchanged. The greater reduction in BP for each dose was observed with the later administrations, but was not related to serum concentration. β‐Blockade was evident at all doses of Carteolol. Carteolol is an effective antihypertensive. Duration of Carteolol therapy, independent of dosage, is important in its effectiveness. Clinical Pharmacology and Therapeutics (1984) 35, 301–306; doi: 10.1038/clpt.1984.34