Pindolol‐a beta‐adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.

Aellig, W. H.

doi:10.1111/j.1365-2125.1982.tb01909.x

Cited by 53 publications

(18 citation statements)

References 63 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The aim of this study was to determine the effects of three different ,B-adrenoceptor drugs: epanolol (1l-selective with PAA (Pringle et al, 1986)), atenolol (31-selective with no PAA) and pindolol (non-selective with PAA) on heart rate and physiological tremor in diabetics with autonomic neuropathy. Their selectivity or otherwise has been established in man (Harry, 1977;Aellig, 1982;Norris et al, 1984;Pringle et al, 1986). In animals, atenolol has been shown to have no PAA, while epanolol and pindolol do (Harry et al, 1974;Bilski et al, 1979;Smith et al, 1983).…”

Section: Introductionmentioning

confidence: 98%

Effects of beta‐adrenoceptor blockade on heart rate and physiological tremor in diabetics with autonomic neuropathy. A comparative study of epanolol, atenolol and pindolol.

Reid

Ewing

Harry

et al. 1987

Brit J Clinical Pharma

View full text Add to dashboard Cite

Eight diabetics with autonomic neuropathy were given single oral doses of epanolol (200 mg), atenolol (50 mg), pindolol (5 mg) and placebo in a double‐blind randomised order at weekly intervals. Supine resting heart rate, physiological tremor and blood glucose were measured before, 2 and 4 h after dosing, and ambulatory heart rate monitored for 24 h. Supine resting heart rate was significantly lowered by atenolol both at 2 and 4 h, and increased on pindolol at 4 h. Heart rate was unaffected by epanolol compared with placebo. Heart rate during the ‘waking’ period (14.00‐23.00 h) was lower than placebo after epanolol and atenolol but unaffected by pindolol. During the ‘sleeping’ period (23.00 h‐08.00 h) heart rate was significantly increased by pindolol, lowered with atenolol and unaffected on epanolol. Pindolol significantly increased physiological tremor at 4 h. No differences were seen between epanolol, atenolol and placebo. Plasma glucose was significantly increased by pindolol 2 h after dosing. These results suggest that pindolol probably produces its partial agonist activity at both beta 1‐ and beta 2‐adrenoceptors, while the partial agonist activity of epanolol is beta 1‐selective. Despite abnormal cardiovascular reflex tests in these diabetics, the heart rate responses obtained in this study after beta‐adrenoceptor blockade were surprisingly normal, and suggest that the concept of ‘cardiac denervation’ in diabetes requires modification.

show abstract

Section: Introductionmentioning

confidence: 98%

Effects of beta‐adrenoceptor blockade on heart rate and physiological tremor in diabetics with autonomic neuropathy. A comparative study of epanolol, atenolol and pindolol.

Reid

Ewing

Harry

et al. 1987

Brit J Clinical Pharma

View full text Add to dashboard Cite

show abstract

“…This effect is inversely related to the background sympathetic activity [10,11]. Consequently, exercise at intensities producing an ele vated sympathetic activity reduces or eliminates the en hancement of cardiac function attributable to a sympatho mimetic effect [12], and other conditions or perturbations producing an elevated sympathetic activity also attenuate ISA effects [13].…”

Section: Discussionmentioning

confidence: 99%

Effects of Intrinsic Sympathomimetic Activity on Cardiac Function during Variations in Preload

Smith¹,

Nixon²,

Raven³

1993

Am J Noninvas Cardiol

View full text Add to dashboard Cite

The effect of intrinsic sympathomimetic activity (ISA) on ventricular function during wide variations in preload was investigated in 10 healthy men. Hemodynamic and ventricular performance responses were measured during minute 90 of 5° head-down tilt (TILT) and -40 Torr lower body negative pressure (LBNP) after bolus injections of either saline, pindolol (0.01 mg/kg) or propranolol (0.1 mg/kg). Differences in response between drugs were attributed to ISA effects. Heart rate, chamber volumes, ejection fraction, mean velocity of circumferential fiber shortening (V(cf)) and diastolic and systolic wall stress were determined by M-mode échocardiographie and electrocardiographic measurements. Propranolol decreased V(cf) and heart rate (p < 0.05) relative to both saline and pindolol during all preload conditions, whereas the responses during pindolol treatment were not different from those during saline. Systolic and diastolic wall stress were increased (p < 0.05) by propranolol treatment regardless of preload. Both systolic and diastolic wall stress increased >12% during TILT with propranolol while no changes were observed with saline (-1%) or pindolol (+2%). These data indicate that the noncardiodepressive effects of β-blockade with ISA persist regardless of variations in preload. In addition, increases in wall stress by β-blockade (propranolol), particularly during increases in preload (TILT), are prevented by blockade with ISA (pindolol). Thus, under certain conditions, pindolol does not elicit the wall-stressrelated increases in myocardial oxygen demand that occur with propranolol treatment.

show abstract

“…cause any stimulation of these receptors (Aellig, 1982). Pindolol is also a non-specific /3-adrenoceptor antagonist, but with ISA, i.e.…”

Section: Introductionmentioning

confidence: 99%

“…it blocks fl-receptors but also acts as a partial agonist (Aellig, 1982). This partial agonist activity of pindolol is said to be about as high as the normal resting sympathetic activity, and consequently it has been shown to reduce only enhanced sympathetic tone, whereas fi-adrenoceptor antagonists without ISA reduce even normal sympathetic activity (Aellig, 1982).…”

Section: Introductionmentioning

confidence: 99%

Influence of two β‐adrenoceptor antagonists, propranolol and pindolol, on cold adaptation in the rat

Kortelainen

Huttunen

Lapinlampi

1990

British J Pharmacology

View full text Add to dashboard Cite

Adult male rats were treated with propranolol (2.0 mg kg−1 day−1 i.p.), pindolol (0.2 mg kg−1 May−1 i.p.) or 0.9% NaCl day−1 i.p. and exposed to +4°C for 42 days, or treated with 0.9% NaCl day−1 i.p. and kept at +23°C for 42 days. They were weighed once a week, when a 24 h urine sample was also collected and colon temperature measured. Urinary noradrenaline (NA), adrenaline (Ad) and dopamine were analysed by high‐performance liquid chromatography with an electrochemical detector. After the acclimatization period the interscapular brown adipose tissue was excised and weighed and the activity of the oxidative enzymes succinate dehydrogenase and cytochrome oxidase measured. The pindolol‐treated and propranolol‐treated rats gained weight during the cold‐acclimatization period. The amount of interscapular brown adipose tissue increased in the cold, but the increase was lowest in the pindolol‐treated group. No changes were seen in the other brown adipose tissue parameters in cold‐exposed animals. The excretion of catecholamines followed the same pattern in all three cold‐exposed groups, with an initial rise in noradrenaline and adrenaline excretion and a slight rise in dopamine excretion. The results suggest possible connections between β‐adrenoceptor antagonists, weight gain and cold acclimatization. Pindolol had a slight inhibitory effect on cold‐induced brown adipose tissue hypertrophy in rats.

show abstract

Pindolol‐a beta‐adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.

Cited by 53 publications

References 63 publications

Effects of beta‐adrenoceptor blockade on heart rate and physiological tremor in diabetics with autonomic neuropathy. A comparative study of epanolol, atenolol and pindolol.

Effects of beta‐adrenoceptor blockade on heart rate and physiological tremor in diabetics with autonomic neuropathy. A comparative study of epanolol, atenolol and pindolol.

Effects of Intrinsic Sympathomimetic Activity on Cardiac Function during Variations in Preload

Influence of two β‐adrenoceptor antagonists, propranolol and pindolol, on cold adaptation in the rat

Contact Info

Product

Resources

About