Amosulalol, a combined alpha and beta adrenoceptor antagonist: Kinetics after intravenous and oral doses

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Abstract
Amosulalol kinetic studies were conducted in seven subjects who received 0.16 mg/kg iv and in 18 subjects who received 12.5, 25, 50, 100, or 150 mg by mouth. Plasma levels of amosulalol after intravenous dosing declined biphasically and fitted a two‐compartment model. Kinetics were as follows: coefficients A = 0.85 ± 0.09 μg/ml and B = 0.22 ± 0.01 μg/ml; rate constants α = 2.78 ± 0.24 hr−1 and β = 0.25 ± 0.01 hr−1; elimination rate constants, kl2 = 1.36 ± 0.17 hr−1, k21 = 0.78 ± 0.06 hr−1, and kel = 0.88 ± 0.06 hr−1; terminal phase volume of distribution = 0.75 ± 0.06 l/kg; clearance = 8.09 ± 0.54 l/hr; AUC = 1.22 ± 0.09 μg · hr/ml; and t½α = 0.26 ± 0.02 hr and t½β = 2.8 ± 0.1 hr. After single oral doses, amosulalol peak plasma levels were generally reached within 2 to 4 hr. Maximum plasma concentrations and AUC increased in a dose‐dependent manner, whereas t½s were about 5 hr (range 4.4 to 5.7 hr) at each dose. Systemic availability of amosulalol was about 100% as determined by the ratio of AUC after oral and intravenous dosing. These results suggest that amosulalol is well absorbed and is little affected by first‐pass metabolism. Clinical Pharmacology and Therapeutics (1984) 36, 436–443; doi:10.1038/clpt.1984.201

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