Pharmacokinetic studies on the selectiveβ 1-receptor antagonist metoprolol in man

Regårdh, C G; Borg, K. O.; Johansson, Rustan; Johnsson, G.; Palmer, Lars

doi:10.1007/bf01061407

Cited by 186 publications

(122 citation statements)

References 12 publications

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“…Albumin concentrations were significantly lower in the Creatinine clearance (ml min 1) Figure 1 The relationship between atenolol renal clearance and creatinine clearance in young (v) and elderly (0) subjects. (Paterson et al, 1970;Reiss et al, 1970;Regardh et al, 1974). Atenolol is incompletely absorbed but a comparison of atenolol apparent oral clearance with atenolol renal clearance indicated that 31 + 3% and 41 + 6% of the dose was absorbed in the young and elderly groups respectively.…”

Section: Resultsmentioning

confidence: 99%

A comparison of the pharmacokinetics of atenolol, metoprolol, oxprenolol and propranolol in elderly hypertensive and young healthy subjects.

Rigby¹,

Scott²,

Hawksworth³

et al. 1985

Brit J Clinical Pharma

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1 Six elderly patients with established hypertension and six young healthy subjects were studied after 8 days of treatment with atenolol 50 mg day-1, metoprolol 50 mg day-', oxprenolol 80 mg day-' and propranolol 80 mg day-1. 2 The area under the blood concentration-time curve was increased in the elderly group for each drug, but the difference was statistically significant only for atenolol. 3 The lower serum albumin concentrations in the elderly group did not result in a decrease in the percentage of propranolol or oxprenolol bound to serum proteins.

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Section: Resultsmentioning

confidence: 99%

A comparison of the pharmacokinetics of atenolol, metoprolol, oxprenolol and propranolol in elderly hypertensive and young healthy subjects.

Rigby¹,

Scott²,

Hawksworth³

et al. 1985

Brit J Clinical Pharma

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“…This increase must be,due to a change in the fraction (F) of the dose (XO) Borg, Johansson, Johnsson & Palmer, 1974) and hepatic metabolism is the main route of elimination of the fraction which reaches the systemic circulation. The contribution of renal excretion is small.…”

Section: Discussionmentioning

confidence: 99%

The effect of age on the pharmacokinetics of metoprolol and its metabolites.

Quarterman¹,

Kendall²,

DeRuiter³

1981

Brit J Clinical Pharma

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1Plasma concentrations of metoprolol and a pharmacologically active metabolite, H119/66, have been measured in young and elderly volunteers after a single dose of 100 mg metoprolol tartrate and after repeated administration over a period of 1 week. Whilst concentrations of metoprolol are similar in each group, concentrations of H119/66 are approximately twice as high in the elderly. 2 Concentrations of unchanged metoprolol and of the major, but pharmacologically inactive, metabolite, H117/04, together with the two active metabolites of metoprolol have been determined in urine. Only the excretion of metoprolol was diminished in the elderly. 3 Areas under the plasma concentration curve for metoprolol after repeated administration are greater than would be predicted from single dose data, and possible explanations for this are discussed. Concentrations of the pharmacologically active metabolite, H119/66, remain unaltered during chronic dosing of metoprolol. 4 This study has shown that the effect of age on the pharmacokinetics of metoprolol and its metabolites is less pronounced than that observed for other drugs.

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“…Pharmacokinetic studies on metoprolol have shown that the drug is extensively distributed to various tissues and that only 1 to 2 % of the total amount of the drug in the body is localized in the blood (Regardh, Borg, Johansson, Johnsson & Palmer, 1974). Metoprolol must therefore readily cross different kinds of biological membranes including the placenta; it was recently shown that the concentration of metroprolol in maternal and umbilical cord blood is about the same (Sandstrom, 1978).…”

Section: Metoprolol Excretion Into Breast Milkmentioning

confidence: 99%