Biopharmaceutical evaluation of oral tablet Atenolol (100 and 50 mg) on local population.
An open-label, randomized study was designed to determine the bioavailability (BA); pharmacokinetic (PK) and pharmacodynamic (PD) behaviour of Atenolol 50 mg (two pills) and 100 mg (one pill) tablet manufactured by a national pharmaceutical industry. Peak plasma concentration (Cmax): 1.33 +/- 0.31 microg/ml, time to peak plasma concentration (Tmax): 2.2 +/- 0.27 hours, AUC (area under the plasma concentration-time curve) 6.34 +/- 2.1 microg-hr/ml for 100 mg tab and Cmax: 1.07 +/- 0.23 microg/ml, Tmax: 2.5 +/- 0.35 hours, AUC 4.97 +/- 1.09 microg-hr/ml for 50 mg (two pills) tab were observed. The BA and PK parameters such as Cmax, Tmax, are comparable to previous studies, although significant decrease in diastolic and systolic blood pressure (mmHg) upto a certain limit for a considerable duration was observed. However, relation between PK and PD may not be established due to regulatory biochemical feedback mechanism.
Ali
Obaid
O
Government of Pakistan, Ministry of Health, Central Drugs Laboratory, Karachi, Pakistan. mobaidali@yahoo.com
Obaid
Roohi
R
Saify
Zafar Saied
ZS
Ahmed
Syed Waseemuddin
SW
D000284:Administration, Oral; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D000328:Adult; D019540:Area Under Curve; D001262:Atenolol / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D001794:Blood Pressure / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008297:Male; D010154:Pakistan
D000319:Adrenergic beta-Antagonists; D001262:Atenolol