Journal ArticleDOI
Interaction of Metoprolol, Propranolol and Atenolol With Concurrent Administration of Cimetidine
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TLDR
Application of cimetidine did not lead to any interaction with atenolol, whereas mean peak plasma levels of metoprolol were increased by 70%, and those of propranolol by 95% due to concurrent administration of cimentidine (P<0.05).Abstract:
Pharmacokinetics of metoprolol, propranolol, and atenolol were investigated in six healthy volunteers following 7 days of oral monotherapy with these drugs, and after 7 days concurrent administration of each of these betareceptor antagonists with cimetidine. Application of cimetidine did not lead to any interaction with atenolol, whereas mean peak plasma levels of metoprolol were increased by 70%, and those of propranolol by 95% due to concurrent administration of cimetidine (P<0.05). The plasma level time curve (AUC) of the two above-mentioned beta blockers behaved similarly (P<0.05). Other kinetic parameters of these two drugs were not influenced to a statistically significant extent by cimetidine, despite the tendency for the elimination half-life of metoprolol and propranolol to be prolonged when cimetidine is added. Measurement of exercise-induced tachycardia on the sixth day of administration showed no differences between monotherapy with the beta blockers and combined treatment with each of them together with cimetidine. Apart from one volunteer who complained of anxiety, weakness, and sweating on the sixth day of cimetidine/metoprolol administration, no adverse effects could be observed during the combination therapy with cimetidine and the beta blockers, nor during monotherapy with beta blockers.read more
Citations
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Histamine2-receptor antagonists-standard therapy for acid-peptic diseases
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Pharmacokinetic interactions of cimetidine 1987.
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Which concentration of the inhibitor should be used to predict in vivo drug interactions from in vitro data
Kiyomi Ito,Koji Chiba,Masato Horikawa,Michi Ishigami,Naomi Mizuno,Jun Aoki,Yasumasa Gotoh,Takafumi Iwatsubo,Shin-ichi Kanamitsu,Motohiro Kato,Iichiro Kawahara,Kayoko Niinuma,Akiko Nishino,Norihito Sato,Yuko Tsukamoto,Kaoru Ueda,Tomoo Itoh,Yuichi Sugiyama +17 more
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Clinical Pharmacokinetics of Drugs Used in the Treatment of Gastrointestinal Diseases (Part II)
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References
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Journal ArticleDOI
Reduction of Liver Blood Flow and Propranolol Metabolism by Cimetidine
TL;DR: The reduction in liverBlood flow produced by cimetidine has important therapeutic implications for patients with alterations in liver and gastrointestinal blood flow and when drugs are used whose hepatic elimination depends on liver blood flow.
Journal ArticleDOI
Disposition of propranolol. V. Drug accumulation and steady-state concentrations during chronic oral administration in man.
Gwyn H. Evans,David G. Shand +1 more
TL;DR: It is suggested that saturable hepatic tissue binding, as well as safurable metabolism, can result in nonlinear kinetics of drug disposition, and first‐order drug elimination in the presence of a saturated high affinity binding site in the liver is suggested.
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Clinical pharmacologic observations on atenolol, a beta-adrenoceptor blocker.
H. Colin Brown,S. George Carruthers,G. Dennis Johnston,J G Kelly,James McAinsh,D. G. McDevitt,Robin G. Shanks +6 more
TL;DR: Repeated oral administration of atenolol 200 mg daily either as a single dose or in divided 12 hourly doses for 8 days maintained reduction of an exercise tachycardia of at least 24% during the period of drug administration.
Journal ArticleDOI
Kinetics and absolute bioavailability of atenolol
TL;DR: Kinetic analysis of the intravenous data indicates a three‐compartment model with elimination from the central compartment, and the mean renal plasma clearance after oral doses is in the same range as renal clearance after intravenous doses.