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Calcium channel blockers for hypertension: old, but still useful

Calcium channel blockers (CCBs) constitute a heterogeneous class of drugs that can be divided into dihydropyridines (DHPs) and non-DHPs. DHP-CCBs are subcategorized into four generations based on the duration of activity and pharmacokinetics, while non-DHP-CCBs are subcategorized into phenylethylamine and benzodiazepine derivatives. DHP-CCBs are vascular-selective and function as potent vasodilators, whereas non-DHP-CCBs are cardiac-selective and are useful for treating tachyarrhythmia, but reduce cardiac contractility and heart rate.

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 Calcium Channel Blockers: Key Medicine to Drive Global Hypertension Control

In summary, CCBs are among the three preferred antihypertensive medicine classes recommended by the WHO. For many LMIC settings, CCBs have the added advantages over other classes in LMIC settings based on their equivalent effectiveness and safety, and lack of need for laboratory monitoring, availability, affordability, and role in patient-centered HTN care. The advantages of CCBs naturally led to their primary role in HEARTS simple HTN treatment protocols around the world. As the most prescribed HTN medicine in Global Hearts programs, CCBs have the potential to transform the market for antihypertensive medicines in LMICs. The ubiquity of CCBs as part of first-step therapy across countries and regions could lead to an “economy of scale,” ushering in low medicine prices needed to accelerate the scale-up of HTN control programs in LMICs.

 The Evolving Role of Calcium Channel Blockers in Hypertension Management: Pharmacological and Clinical Considerations

While many studies demonstrate how CCBs should be included as first-line therapy for hypertensive patients, some research has demonstrated different effects of this class of medication amongst different ethnicities. For example, African Americans may have an improved response to CCB therapy alone when compared to combination therapy with diuretics. However, there is still a lack of significant data to conclude that CCB monotherapy is superior to combination therapy in African Americans.

Articles of Interest

Calcium channel blockers and cancer: a risk analysis using the UK Clinical Practice Research Datalink (CPRD)

This large population-based study provides strong evidence that CCB use is not associated with an increased risk of cancer. The analyses yielded robust results across all types of cancer and different durations of exposure to CCBs.

Calcium channel blockers caught in the act at atomic level

Atomic level analysis has revealed how two classes of calcium channel blockers, widely prescribed for heart disease patients, produce separate therapeutic effects by acting at different sites on the calcium channel molecule. The study looked at the anti-arrhythmia drug verapamil, and the hypertension and angina drug amlodipine.

Calcium channel blockers for stable SVT: A first line agent over adenosine?

CCBs by IV bolus or slow infusion are equally efficacious to adenosine in hemodynamically stable patients with SVT.

Calcium-Channel Blockers (CCBs)

Currently, approved calcium-channel blockers (CCBs) bind to L-type calcium channels on vascular smooth muscle, cardiac myocytes, and cardiac nodal tissue (sinoatrial and atrioventricular nodes).

Deja Vu All Over Again: Study Links Calcium-Channel Blockers To Breast Cancer

A new observational study raises the possibility that calcium-channel blockers (CCBs) may be associated with a higher risk for breast cancer. Although previous studies examining this relationship have failed to turn up convincing evidence of a link, the authors of a paper published in JAMA Internal Medicine state that their study is the first to look at long-term use of CCBs in a contemporary population.

Long-Term Safety and Effectiveness of Calcium Channel Blockers in Hypertension: A Systematic Review

Overall, CCBs are safe for long-term use and show sustained effectiveness in stroke and angina, although evidence for heart failure, myocardial infarction, and transient ischemic attack remains inconsistent.

Magnificent Magnesium

Magnesium operates as a natural calcium channel blocker and is responsible for relaxation—counter to calcium’s contraction. Thus magnesium is pivotally important to the healthy functioning of our parasympathetic nervous system. It may be hard to believe, but our bodies were actually designed to operate for the most part in a calm, relaxed parasympathetic state, rather than in the heart-pounding, stress- and adrenaline-driven mode of sympathetic nervous system dominance that is nearly constant for many of us today, and which uses up great quantities of magnesium.

Nasal spray shows potential for quickly treating arrhythmia

A calcium-channel blocker delivered as a nasal spray rapidly restored individuals with paroxysmal supraventricular tachycardia (SVT) to normal sinus rhythm in a phase 2 study, raising the possibility that the drug could be self-administered in a real-world setting and prevent trips to the emergency department.

No, Pharmascolds Are Not Worse Than The Pervasive Conflicts Of Interest They Criticize

CCBs, you will recall, were among the most successful drugs in the golden age of pharma in the 1980s and 1990s. An enormous controversy– one that served as a prototype for the more recent Vioxx and Avandia episodes– exploded when several prominent “pharmascolds” questioned the safety of CCBs and claimed that these safety concerns had been hidden by investigators with COIs with the CCB manufacturers.

The Magic of Magnesium: A Mighty Mineral Essential to Health

Did you know that this mighty mineral may be even more essential for health? Here’s what I recommend: Keep your calcium intake between 800-1,400 mg per day, adding enough magnesium to balance it. For example, if you take 1,000 mg of calcium per day, you need at least 500-800 mg of magnesium.

Resources

Amlodipine (Norvasc)

The usual initial antihypertensive oral dose of NORVASC is 5 mg once daily with a maximum dose of 10 mg once daily.

Clevidipine (Cleviprex)

Initiate the intravenous infusion of Cleviprex at 1-2 mg/hour.

Diltiazem (Cardizem)

Starting with 30 mg four times daily, before meals and at bedtime, dosage should be increased gradually (given in divided doses three or four times daily) at 1- to 2-day intervals until optimum response is obtained.

Nicardipine (Cardene)

Cardene I.V. 20 mg in 200 mL (0.1 mg/mL): Initiate therapy at 50 mL/hr (5 mg/hr). If desired blood pressure reduction is not achieved at this dose, the infusion rate may be increased by 25 mL/hr (2.5 mg/hr) every 5 minutes (for rapid titration) to 15 minutes (for gradual titration) up to a maximum of 150 mL/hr (15 mg/hr), until desired blood pressure reduction is achieved.

Nifedipine {Procardia)

Therapy should be initiated with the 10 mg capsule. The starting dose is one 10 mg capsule, swallowed whole, 3 times/day. The usual effective dose range is 10–20 mg three times daily.

Verapamil

Dose should be individualized by titration. The usual initial monotherapy dose in clinical trials was 80 mg three times a day (240 mg/ day).

AMBOSS

Calcium channel blockers (CCBs) are drugs that bind to and block the L-type calcium channel. The L-type channels are the predominant calcium channels in the myocardium and the vascular smooth muscles. By blocking these channels, CCBs cause peripheral arterial vasodilation and myocardial depression, which leads to a drop in blood pressure and negative chronotropic, inotropic, and dromotropic effects on the myocardium.

FP Notebook

Extensive resource...

Heart Matters

There are two distinct chemical classes of CCBs: the dihydropyridines (such as nifedipine and amlodipine) and the nondihydropyridines (diltiazem and verapamil). The two classes both help to relax and widen arteries but non-dihydropyridines have an additional effect on the heart’s conduction system and can help to control certain fast heart rhythms (such as atrial fibrillation).

Patient

Calcium-channel blockers (CCBs) were developed in the 1970s and are now widely used. CCBs all inhibit inward movement of calcium ions through the slow channels of active membranes

StatPearls

Calcium channel blockers (CCBs), also known as calcium channel antagonists, have been approved by the US Food and Drug Administration (FDA) and are widely used to treat various conditions such as hypertension, coronary heart disease, and chronic stable angina. However, despite their widespread use, this class of cardiovascular drugs is one of the primary contributors to drug-related fatalities.