Current status of safety and efficacy of calcium channel blockers in cardiovascular diseases: A critical analysis based on 100 studies

2000 ◽  
Vol 43 (2) ◽  
pp. 171-196 ◽  
Author(s):  
Lionel H Opie ◽  
Salim Yusuf ◽  
Wolfgang Kübler
Keyword(s):  
Cardiovascular Diseases ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Critical Analysis ◽  
Current Status ◽  
Channel Blockers ◽  
Safety And Efficacy

scholarly journals Synthesis of Pseudellone Analogs and Characterization as Novel T-type Calcium Channel Blockers

Marine Drugs ◽  
2018 ◽  
Vol 16 (12) ◽  
pp. 475 ◽  
Author(s):  
Dan Wang ◽  
Pratik Neupane ◽  
Lotten Ragnarsson ◽  
Robert Capon ◽  
Richard Lewis
Keyword(s):  
Cardiovascular Diseases ◽  
Patch Clamp ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Absence Epilepsy ◽  
Channel Blockers ◽  
Synthetic Route ◽  
State Dependent ◽  
Whole Cell Patch Clamp ◽  
Potential Therapeutics

T-type calcium channel (CaV3.x) blockers are receiving increasing attention as potential therapeutics for the treatment of pathophysiological disorders and diseases, including absence epilepsy, Parkinson’s disease (PD), hypertension, cardiovascular diseases, cancers, and pain. However, few clinically approved CaV3.x blockers are available, and selective pharmacological tools are needed to further unravel the roles of individual CaV3.x subtypes. In this work, through an efficient synthetic route to the marine fungal product pseudellone C, we obtained bisindole alkaloid analogs of pseudellone C with a modified tryptophan moiety and identified two CaV3.2 (2, IC50 = 18.24 µM; 3, IC50 = 6.59 µM) and CaV3.3 (2, IC50 = 7.71 µM; 3, IC50 = 3.81 µM) selective blockers using a FLIPR cell-based assay measuring CaV3.x window currents. Further characterization by whole-cell patch-clamp revealed a preferential block of CaV3.1 activated current (2, IC50 = 5.60 µM; 3, IC50 = 9.91 µM), suggesting their state-dependent block is subtype specific.

Safety and Efficacy of Tocolytics for the Treatment of Spontaneous Preterm Labour

2019 ◽  
Vol 25 (5) ◽  
pp. 577-592 ◽  
Author(s):  
Ronald F. Lamont ◽  
Jan S. Jørgensen
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Preterm Labour ◽  
Oxytocin Receptor ◽  
Channel Blockers ◽  
Prostaglandin Synthetase ◽  
Receptor Antagonists ◽  
Safety And Efficacy ◽  
Line Therapy ◽  
Β2 Agonists

Background: Preterm birth is the major cause of perinatal mortality and morbidity worldwide. Attempts to reduce the burden may be proactive using biochemical or biophysical prediction and preventative measures. If these efforts fail, then the approach may have to be reactive using tocolytics to inhibit spontaneous preterm labour. Objective: We have reviewed the evidence concerning the safety and efficacy of various classes of tocolytic agents. Results: The evidence to support the use of magnesium sulfate or nitric oxide donors as a tocolytic is poor. Compared to placebo or no treatment, there is evidence to support the efficacy of calcium channel blockers (mainly nifedipine), prostaglandin synthetase inhibitors (mainly indomethacin and sulindac), oxytocin receptor antagonists (mainly atosiban) and β2-agonists (mainly ritodrine, terbutaline, salbutamol and fenoterol). Maternal safety concerns have reduced the use of β2-agonists. Fetal safety and gestational age restrictions have largely condemned prostaglandin synthetase inhibitors to second-line therapy. First-line therapy in Europe and other parts of the world outside the USA and Australia is limited to calcium channel blockers and oxytocin receptor antagonists. With respect to efficacy, atosiban and nifedipine are similar, but the robustness of the evidence favours atosiban. With respect to safety, atosiban is clearly the safest tocolytic as there are fetomaternal concerns with nifedipine, particularly in high daily doses. Conclusion: The perfect tocolytic that is uniformly effective and safe does not exist. Cost, licensing and informed consent are considerations involved in the choice. Efforts continue to develop and introduce other or better agents, including novel compounds such as progesterone, PGF2α antagonists and statins.

Current status of calcium channel blockers in patients with cardiovascular disease

1999 ◽  
Vol 24 (5) ◽  
pp. 229-340 ◽  
Author(s):  
Mark Freher ◽  
Sridevi Challapalli ◽  
Jack V. Pinto ◽  
Janice Schwartz ◽  
Robert O. Bonow ◽  
...  
Keyword(s):  
Cardiovascular Disease ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Current Status ◽  
Channel Blockers
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