Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.

@article{Beresford1986BetaxololAR,
  title={Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.},
  author={Rosemary Beresford and Rennie C. Heel},
  journal={Drugs},
  year={1986},
  volume={31 1},
  pages={
          6-28
        }
}
Betaxolol is a relatively cardioselective beta-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilising (local anaesthetic) activity. Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life. It has a narrow dose-response range, which obviates the need for dose titration, with 10 to 20 mg once daily being the usual dosage. This dose reduces systolic and… 
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References

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TLDR
Betaxolol proved to be a potent and long-lasting beta-adrenoceptor blocking drug, devoid of intrinsic beta-sympathomimetic activity and perfectly consistent with the long duration of the pharmacological effects of betaxolOL in man.
Cardiovascular effects of single oral doses of the new beta-adrenoceptor blocking agents betaxolol (SL 75212) in healthy volunteers.
1 The effects of betaxolol (SL 75212), a new beta-adrenoceptor blocking agent, on the cardiovascular response to exercise have been studied in six normal subjects after placebo and single oral doses…
Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta-adrenoceptor blocking drug.
TLDR
It is shown that betaxolol is a potent beta-adrenoceptor antagonist with a long duration of effect on an exercise tachycardia and a long plasma elimination half-life.
Comparative effects of adimolol, labetalol and propranolol on heart rate and blood pressure in man.
TLDR
These studies show that adimolol is a potent, long acting beta-adrenoceptor blocking drug without evidence of alpha-adRenoceptor blockade in man.
Dose related efficacy of betaxolol in combination with nitroglycerin in patients with angina pectoris: a double blind cross-over study.
TLDR
BTX was well tolerated in all patients and exerted its effect also in the presence of nitroglycerin, making BTX an attractive choice as antianginal agent for chronic use.
Pharmacokinetics of the new beta-adrenoceptor blocking agent betaxolol (SL 75212) in man after repeated oral administration.
TLDR
The pharmacokinetic characteristics were unchanged after repeated doses, T/2 16-22 h, Vd 7-8.8 l/kg; clearance 0.28-0.33 l/h/kg.
Betaxolol kinetics in hypertensive children with normal and abnormal renal function
TLDR
The results indicate that betaxolol disposition in children aged 5 to 13 yr with different degrees of renal failure is of the same order as that in young healthy adults, implying that there may be a higher rate of non‐renal clearance.
Effect of betaxolol on heart rate at rest and during exercise.
TLDR
Betaxolol appears to be more effective than a single oral dose of 160 mg of long-acting propranolol and during exercise as well after administration.
Effects of topical betaxolol, timolol, and placebo on pulmonary function in asthmatic bronchitis.
The haemoglobin-oxygen dissociation curve: in vivo and in vitro effects of five beta-adrenoceptor antagonists and lignocaine.
TLDR
It is suggested that to increase P50 with propranolol requires plasma proPRanolol concentrations far in excess of concentrations normally achieved, and that the therapeutic effect of propr ethanol in patients with ischaemic heart disease cannot be attributed to an increase in P50.
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