Food-induced reduction in bioavailability of atenolol

Melander, Arne; Stenberg, P.; Liedholm, Hans; Scherstén, Bengt; Wåhlin-Boll, E

doi:10.1007/bf00605630

Cited by 63 publications

(27 citation statements)

References 15 publications

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“…This is a genuine possibility as judged from studies on atenolol, a non-metabolised beta blocker with a pKa ( = 9) similar to that of propranolol; concomitant food intake may increase the absorption rate of atenolol, possibly by promoting absorption from the stomach [14].…”

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confidence: 96%

Mechanisms and variations in the food effect on propranolol bioavailability

Liedholm

Wåhlin-Boll

Melander

1990

Eur J Clin Pharmacol

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Mechanisms and variations in the food-induced increase in the bioavailability of propranolol were assessed by single-dose (80 mg) studies in healthy volunteers who took the drug on an empty stomach, immediately after a protein-rich breakfast, and together with a carbohydrate-rich, protein-poor breakfast. Concomitant intake of the protein-rich, but not the carbohydrate-rich, protein-poor breakfast, increased the bioavailability of propranolol in most, but not all, subjects. The food (protein) effect displayed much inter-individual variation, from a decrease to a 250% increase, which could be explained, at least in part, by a correlation between the oral clearance of propranolol and the food-induced increase in its bioavailability. The food effect was not associated with decreased total availability, but with delayed appearance, of the oxidative metabolites 4-OHP, NLA and PG. Hence the food (protein) effect does not seem to be caused by enzyme inhibition, but rather it is due to reduced hepatic extraction of propranolol, probably consequent to an increase hepatic entry rate. When taken together with the protein-rich breakfast, propranolol usually appeared in systemic blood at least as early as when taken on an empty stomach, implying that gastric absorption of propranolol may be possible in the presence of protein-rich food. Within the individual the food effect was reproducible, but its magnitude showed an intraindividual variation that may reflect its dependence upon the rates of gastrointestinal absorption and splanchnic-hepatic blood flow, and hence upon the rate of hepatic drug entry.

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confidence: 96%

Mechanisms and variations in the food effect on propranolol bioavailability

Liedholm

Wåhlin-Boll

Melander

1990

Eur J Clin Pharmacol

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“…administration of foods was reported to reduce the area under the plasma concentration-time curve (AUC) of atenolol by 20% as compared with the fasting state (Melander et al, 1979). Metabolsim of atenolol is limited in the liver (only 5%).…”

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Hydrophilic interaction liquid chromatographic tandem mass spectrometric determination of atenolol in human plasma

Francisco

et al. 2005

Biomedical Chromatography

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A hydrophilic interaction liquid chromatographic method with tandem mass spectrometry for the determination of atenolol, a beta-blocking agent, in human plasma has been developed and validated over the curve range of 10--2000 ng/mL. The assay was based on protein precipitation followed by evaporation of the extraction solvent, reconstitution with acetonitrile, and chromatography on an Hypersil silica column (50 x 4.6 mm) using a low aqueous--high organic mobile phase. The mobile phase consists of 85% acetonitrile, 15% water, 0.5% acetic acid and 0.04% trifluoroacetic acid and runs isocratically at a flow rate of 2.0 mL/min. The column ef fluent was split so that 50% of it was transferred into the LC-MS/MS interface operated in positive electrospray ionization mode. The chromatographic run time was 2.0 min per injection. Atenolol and the internal standard, atenolol-d(7), showed a retention time of 1.0 min. The inter-day and intra-day precision and accuracy of the quality control samples were <5.3% relative standard deviation and <8.0% relative error, respectively. To explore the application of the current method for the analysis of other beta-blocking agents, propranolol and metoprolol were tested under the same chromatographic conditions with retention times of 0.68 and 0.75 min, respectively. The present method could be used for therapeutic drug monitoring, pharmacokinetic and drug--drug interaction studies of beta-blocking agents.

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“…Decreased secretion of insulin and increased insulin resistance result in hyperglycemia and metabolic acidosis that are commonly observed with amlodipine overdose (Melander et al, 1979). Amlodipine overdose predominantly casues hypotension, conduction disturbances like sinus bradycardia and varying degrees of atrioventricular block and less commonly, non-cardiogenic pulmonary edema (Stanek et al, 1997;Sanaei-Zadeh, 2012).…”

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confidence: 99%

Amlodipine-Atenolol Overdose Management: A Physician's Nightmare

Rao¹,

Jayaprakash²,

Patil³

et al. 2016

J App Pharm Sci

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The author reports a case of a 22-year-old female, daughter of a known hypertensive patient, who happened to consume her mother's medicine. Her mother was on a fixed drug combination (FDC) of amlodipine and atenolol. The patient was brought to the emergency department with drowsiness following ingestion of 15 tablets of amlodipine-atenolol FDC (5+ 50 mg). On evaluation, she had refractory bradycardia and hypotension along with hyperkalemia. She was managed initially with gastric lavage with activated charcoal, and subsequently with supplementation of atropine, inotropes, anti-hyperkalaemic measures, pacemaker and levosimendan.

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Food-induced reduction in bioavailability of atenolol

Cited by 63 publications

References 15 publications

Mechanisms and variations in the food effect on propranolol bioavailability

Mechanisms and variations in the food effect on propranolol bioavailability

Hydrophilic interaction liquid chromatographic tandem mass spectrometric determination of atenolol in human plasma

Amlodipine-Atenolol Overdose Management: A Physician's Nightmare

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