BACKGROUND: Based on a series of clinical trials showing no difference in the effectiveness or tolerability of most major classes of antihypertensive medications, the Joint National Commission on High Blood Pressure Treatment recommends that physicians prescribe β -blockers or diuretics as initial hypertensive therapy unless there are compelling indications for another type of medication. Never...

Hundreds of thousands of patients around the world have been treated with drugs that antagonize the function of calcium channels. The development of these drugs was based on the remarkable scientific discovery of calcium channels, the identification of methods to antagonize their effects, and the development of compounds to block them.' As concepts of the pathophysiology and treatment of hypert...

Ten spinal-cord-injured males who exhibited autonomic dysreflexia during electroejaculation were given sublingual calcium channel blocker nifedipine pretreatment to prevent this complication. Nifedipine was successful in decreasing peak systolic, diastolic, and mean blood pressures during the procedure. The use of nifedipine resulted in fewer aborted trials and allowed higher energy delivery du...

About ten years ago, after fellowships and clinical experience in a community setting, I had my first experience as a ward attending in a university hospital. We were working with cardiac patients, and I was struck by the common treatment each patient received. No matter what the symptoms, patients received an exercise treadmill, an echocardiogram, and were put on a calcium channel blocker. Thi...

OBJECTIVE To assess the effects of calcium channel blockers on development of infarcts, reinfarction, and mortality. DESIGN A systematic overview of all randomised trials of calcium channel blockers in myocardial infarction and unstable angina. PATIENTS 19,000 Patients in 28 randomised trials. RESULTS In the trials of myocardial infarction 873 deaths occurred among 8870 patients randomise...

L-type calcium channels are present in most electrically excitable cells and are needed for proper brain, muscle, endocrine and sensory function. There is accumulating evidence for their involvement in brain diseases such as Parkinson disease, febrile seizures and neuropsychiatric disorders. Pharmacological inhibition of brain L-type channel isoforms, Cav1.2 and Cav1.3, may therefore be of ther...

The oomycete vegetable pathogen Phytophthora capsici causes significant losses of important vegetable crops worldwide. Calcium and other plant nutrients have been used in disease management of oomycete pathogens. Calcium homeostasis and signaling is essential for numerous biological processes, and Ca(2+) channel blockers prevent excessive Ca(2+) influx into the fungal cell. However, it is not k...

Aberrant activation of mast cells contributes to the development of numerous diseases including cancer, autoimmune disorders, as well as diabetes and its complications. The influx of extracellular calcium via the highly calcium selective calcium-release activated calcium (CRAC) channel controls mast cell functions. Intracellular calcium homeostasis in mast cells can be maintained via the modula...

The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium chann...