Clinical pharmacokinetics of atenolol--a review.
Atenolol is a hydrophilic betareceptor blocking drug, which is predominantly eliminated via the kidneys, only about 5% of the atenolol is metabolised by the liver. After oral administration atenolol is incompletely absorbed from the intestine, so about 50% of the beta blocker are finally biovailable. In plasma only 3% of atenolol are protein-bound. There exists a linear relationship between the atenolol plasma levels and the degree of beta blocking effect measured by inhibition of the exercise-induced tachycardia. No correlation was found between plasma levels of atenolol and blood pressure lowering activity of the drug. After oral administration elimination half life of atenolol is calculated from 6 to 9 h by different authors. In patients with impaired renal function elimination half life of atenolol gradually increases to values of 36 h in uraemic patients (glomerular filtration rate (GFR) less than 10 ml/min). Between GFR and atenolol plasma clearance as well as renal clearance a close significant correlation is described. Prolongation of elimination half life requires a dosage adjustment of atenolol in patients with renal failure. A marked interaction of atenolol is found when calcium or aluminium hydroxide are concurrently administered with the beta blocker whereas cimetidine does not influence atenolol kinetics.
D000284:Administration, Oral; D001262:Atenolol / Q000378:metabolism* / Q000627:therapeutic use; D001682:Biological Availability; D004347:Drug Interactions; D006801:Humans; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D007668:Kidney / Q000378:metabolism; D007674:Kidney Diseases / Q000378:metabolism; D007700:Kinetics; D008107:Liver Diseases / Q000378:metabolism; D011412:Propanolamines / Q000378:metabolism*; D006435:Renal Dialysis
D011412:Propanolamines; D001262:Atenolol