Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Meier, Jörg; Nüesch, E.

doi:10.1111/j.1365-2125.1977.tb00726.x

Cited by 20 publications

(10 citation statements)

References 11 publications

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“…The comparative effects of oral and intravenous pindolol indicate that the bioavailability of oral pindolol is at least 70%, a figure which is substantially above the 53% reported by Jennings and his colleagues (1979) but were in accordance with the 87% reported by Meier & Nuesch (1977). Preliminary plasma concentration data support this conclusion.…”

Section: Discussionsupporting

confidence: 68%

Cardiac dose‐response relationships of oral and intravenous pindolol.

Carruthers¹

1982

Brit J Clinical Pharma

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1 The dose-response curve of pindolol on exercise heart rate has been constructed from observations in healthy male subjects studied 2 h after oral doses of pindolol 0.25 mg, 0.5 mg, 1 mg, 2.5 mg, 5 mg, 10 mg and 20 mg. This dose-response curve has been compared with historical controls who received atenolol, oxprenolol, practolol, propranolol and sotalol. 2 The dose-response curves differ in the relative potency of the drug, the maximum reduction of heart rate and possibly in the slope of the curves. Pindolol is extremely potent. At doses which produce 15 % reduction of exercise heart rate, the relative potencies of the drugs were: pindolol ( 1), atenolol (1:21) oxprenolol (1:19), practolol (1:44), propranolol (1:25) and sotalolol (1:160). The maximum effects produced by pindolol, oxprenolol and practolol were less than those of the other P-adrenoceptor blocking drugs, an effect which is probably the result of their partial agonist activity.3 Following intravenous pindolol 0.005, 0.01, 0.02 and 0.045 mg/kg the reduction of exercise heart rate and duration of action were dose-dependent. 4 The effects of pindolol 0.045 mg/kg i.v. (mean total dose 3.5 mg), pindolol 5 mg p.o., propranolol 0.3 mg/kg i.v. (mean total dose 25.1 mg) and propranolol 80 mg p.o. were assessed on resting, standing and exercise heart rates. Neither drug reduced resting heart rate but propranolol reduced standing heart rate from 98.8 to 80.3 beats/min. The effects of all four preparations on exercise heart rate were similar. 5 Oral pindolol is approximately 16-20 times as potent as oral propranolol. 6 Intravenous pindolol is approximately 6-8 times as potent as intravenous propranolol.

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Section: Discussionsupporting

confidence: 68%

Cardiac dose‐response relationships of oral and intravenous pindolol.

Carruthers¹

1982

Brit J Clinical Pharma

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“…The mean bioavailability reported by Meier & Nuesch (1977) in eight different studies was quite close to our value of 79.5 ± 8.6%.…”

Section: Discussionsupporting

confidence: 63%

“…In healthy subjects its bioavailability is high due to an excellent digestive absorption and a slight first pass effect (Meier & Nuesch, 1977). In hypertensive patients with chronic renal failure its bioavailability is slightly diminished (Lavene et al, 1977).…”

Section: Introduction Methodsmentioning

confidence: 99%

Study of the bioavailability of pindolol in malabsorption syndromes.

Evard¹,

Aubry²,

Quintrec³

et al. 1984

Brit J Clinical Pharma

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Pindolol kinetics and bioavailability were studied after a single dose (oral 5 mg; intravenous 3 mg) in nine patients with malabsorption (two with villous atrophies, seven with short bowel syndromes) and in six healthy volunteers. After oral administration no significant differences were observed in bioavailability (59.4 ± 6.2% in patients vs 79.5 ± 8.6% in controls) and for most plasma and urinary pharmacokinetic parameters between the experimental and control groups as a whole. However, detailed analysis revealed decreased absorption for pindolol in two out of nine patients. After i.v. administration, apparent distribution volume was smaller (V: 2.10 ± 0.25 1 kg-' vs 3.05 + 0.31 1 kg-') and global elimination constant was larger (ke: 1.43 + 0.46 h-1 vs 0.56 + 0.10 h-1), in patients with malabsorption than in controls (P < 0.05). The smaller weight of patients and pharmacokinetic modifications due to the pathology could account for this.

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“…Their comparison after oral and intravenous administration indicated an 87% absolute bioavailability. Therefore, pindolol has a small first-pass effect of about 13% in man (7). Similar experiments in the rat and tire dog (8) yielded 40 and 45% first-pass effect.…”

Section: First-pass Effect and Bioavailabilitymentioning

confidence: 50%

“…2. Determination of the absorption, the absolute oral bioavailability and the first-pass effect of pindolol in man (7). After oral and intravenous administration of '*C-labeled pindolol the plasma levels and urinary excretions were determined.…”

Section: First-pass Effect and Bioavailabilitymentioning

confidence: 99%

<i>β</i>-Adrenoceptor-Blocking Agents: Pharmacokinetic Differences and Their Clinical Implications Illustrated on Pindolol

Meier¹

1979

Cardiology

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Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Cited by 20 publications

References 11 publications

Cardiac dose‐response relationships of oral and intravenous pindolol.

Cardiac dose‐response relationships of oral and intravenous pindolol.

Study of the bioavailability of pindolol in malabsorption syndromes.

<i>β</i>-Adrenoceptor-Blocking Agents: Pharmacokinetic Differences and Their Clinical Implications Illustrated on Pindolol

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Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Cited by 20 publications

References 11 publications

Cardiac dose‐response relationships of oral and intravenous pindolol.

Cardiac dose‐response relationships of oral and intravenous pindolol.

Study of the bioavailability of pindolol in malabsorption syndromes.

<i>&beta;</i>-Adrenoceptor-Blocking Agents: Pharmacokinetic Differences and Their Clinical Implications Illustrated on Pindolol

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<i>β</i>-Adrenoceptor-Blocking Agents: Pharmacokinetic Differences and Their Clinical Implications Illustrated on Pindolol