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Cardiovascular Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: Pindolol is not a teratogen; however, its use during the 2nd and 3rd Trimesters is discouraged because its administration, during this period, has been linked with the incidence of reduced placental weight and IUGR.
Treatment of Anti-Phospholipid Antibody Mediated Fetal Loss: The Case for Corticosteroid Therapy
Published in E. Nigel Harris, Thomas Exner, Graham R. V. Hughes, Ronald A. Asherson, Phospholipid-Binding Antibodies, 2020
We believe that hypertension should be treated early and aggressively. Intervention with antihypertensive agents should be as soon as an upward trend in blood pressure is identified and the diastolic pressure approaches 90 mmHg. We have found the use of pindolol (starting with 2.5 mg tds, increasing to 10 mg tds) with or without prazosin (starting with 0.5 mg tds, increasing to 5 mg tds) effective and without adverse effects. Severe episodes of hypertension are treated with nifedipine. We have avoided the use of hydralazine in these patients because of its recognized propensity for inducing autoantibody production.
Pharmacological Treatment of Orthostatic Hypotension
Published in David Robertson, Italo Biaggioni, Disorders of the Autonomic Nervous System, 2019
Clinical studies have shown an increased peripheral resistance and attenuation of postural hypotension (Chobanian et al., 1977; Brevetti et al., 1981). Negative inotropic and chronotropic actions can limit their usefulness, and side effects of β-blockers are common in the elderly population. Pindolol, the partial agonist β-blocker has been used (Manin’t Veld and Schalekamp, 1981) and may have β-agonist effects in the setting of low basal sympathetic tone. Other studies have found this agent less useful (Davies et al., 1981). In general, as with non-steroidal anti-inflammatory drugs, the response is unpredictable in individual patients.
Pindolol potentiates the antidepressant effect of venlafaxine by inhibiting 5-HT1A receptor in DRN neurons of mice
Published in International Journal of Neuroscience, 2021
According to some extracellular electrophysiological animal studies [12,13] and clinical [14,15] studies, the delay of antidepressant response can be prevented with 5-HT1A receptor blockers like pindolol [13,16,17]. Actually, pindolol is a non-selective beta-blocker and used in the cure of hypertension. However, some studies demonstrated that pindolol also blocks the 5-HT1A receptors through a partial agonistic mechanism [12,18]. While pindolol blocks the somatodendtritic 5-HT1A receptors in the raphe nuclei, it does not block the postsynaptic 5-HT1A receptors [12]. Therefore, it can be useful when used in combination with antidepressants for a new MD treatment strategy. For that reason, we aimed to study the effect of pindolol on 5-HT1A receptor response in DRN neurons with patch clamp technique and potentiation capacity of pindolol on antidepressant effect of venlafaxine through behavior experiments.
Pharmacotherapeutic options for cancer cachexia: emerging drugs and recent approvals
Published in Expert Opinion on Pharmacotherapy, 2023
Lorena Garcia-Castillo, Giacomo Rubini, Paola Costelli
S-pindolol, a novel nonselective β blocker with central serotonin 1A receptor (5-HT1a) and partial β2 receptor agonist effect was reported to prevent body weight loss and depletion of both fat and lean mass in an experimental model of severe cachexia. The molecular mechanisms behind these effects involve a reduced expression of proteins contributing to proteolysis (FoxOs, NF-kB, myostatin, and LC3-I/LC3-II ratio) as well as to the activation of protein synthesis (via AKT/mTOR pathway) [59]. In this regard, S-pindolol can be included in a particular category of compounds, namely Anabolic/Catabolic Transforming Agents [60]. A few years ago, the phase IIa ACT-ONE study showed that S-pindolol administration significantly reversed body weight loss, maintained fat mass and enhanced handgrip strength in patients with advanced colorectal cancer and non-small cell lung cancer [44]. While these observations are encouraging, several issues still remain to be solved, mainly related to dosage and pharmacokinetics. In this regard, the company holding global rights on the exploitation of S-pindolol is designing a study dedicated to clarify the pharmacodynamic and pharmacokinetic properties and the most appropriate dosages of the drug. Subsequently, a phase 2b study in patients with non-small cell lung cancer or colorectal cancer is planned (https://www.nature.com/articles/d43747-020-01167-0). On the whole, while S-pindolol and similar compounds are suggested to be beneficial to improve cancer cachexia, acting both stimulating anabolism and inhibiting catabolism, their use in clinical practice is nowadays far from being accepted.
Diverse pharmacological properties, trial results, comorbidity prescribing and neural pathophysiology suggest European hypertension guideline downgrading of beta-blockers is not justified
Published in Blood Pressure, 2022
Murray Esler, Sverre E. Kjeldsen, Atul Pathak, Guido Grassi, Reinhold Kreutz, Giuseppe Mancia
The side effect profile of the various beta-blockers relates to individual drug properties. β-1 selective agents minimise risk of bronchospasm. Non-selective beta-blockers reduce skeletal muscle blood flow, increase insulin resistance and can have other adverse metabolic effects like lowering of HDL cholesterol and increasing triglycerides. Vasodilator beta-blockers minimise these adverse effects. Combined alpha-beta blockers can cause postural hypotension at higher dose. Risk of excessive heart rate slowing is limited with sympathomimetic beta-blockers; i.e. pindolol is frequently used in Australia if beta-blockade causes bradycardia or Raynaud’s phenomenon.