What is CBD? How does it work? Why is it so important?

by Harry Lattanzio, RPh; and Tim Gregorius, RPh, as seen in America's Pharmacist Magazine's February 2020 Issue

To begin to answer those questions above, you must first understand the endocannabinoid system, or ECS. 

“The ECS is an essential regulator of bodily functions. There is hardly any physiological process that is not affected by it to some degree,” says Ethan Russo, MD. Russo is the world’s foremost researcher of the endocannabinoid system, who coined the phrase that the ECS “regulates regulation.”

Just because medical science only discovered its existence in the 1990s doesn’t mean the ECS is any less important to the human body than the cardiovascular system, the endocrine system, or the central nervous system. As a matter of fact, homeostasis itself wouldn’t be possible without the ECS. It is an essential regulatory mechanism of the body’s biochemistry and involved in the basic machinery of cell and organ physiology.

But, because its fundamental functions have only begun to be studied over the past 20 years, a small percentage of pharmacy and medical schools even address the ECS in the curriculums. Thus, there exists a knowledge deficit among practicing health care practitioners. We believe it is critical to address this deficit, especially considering that millions of Americans are already using CBD with little or no idea of side effects or drug interactions. And isn’t that one of our major roles as pharmacists, to be the drug expert for our patients? They aren’t going to get that information from the convenience store or beauty salon, and certainly not online.

As a starting point, the pharmacist, at least needs to understand how and why CBD works in the body by grasping the importance of its role in the ECS. Let’s briefly glance at the components of the ECS and CBD’s interaction with them.

The ECS comprises three essential parts:

  1. Two primary G protein-coupled receptors, CB1 and CB2;
  2. Their endogenous arachidonyl ligands (anandamide and 2-AG)
  3. Enzymes which synthesize and degrade these endogenous cannabinoids (endocannabinoids)


The ECS receptors (CB1 and CB2) are the most abundant receptors in the body – actually more numerous than all other receptors combined (58% of ALL receptors in the body)! That’s an incredible statistic considering how pervasive just the dopamine, serotonin, GABA, and opioid receptors are. The two main endogenous cannabinoids that interact with these receptors are referred to as anandamide and 2-AG, which are produced and broken down by regulatory enzymes embedded in cell walls.

The first thing to note is that there are no “CBD receptors.” CBD interacts via a unique and indirect method of inhibiting the breakdown of the endocannabinoids, while at the same time slightly inhibiting the CB1 and CB2 receptors via a different binding location than the endocannabinoids. This leads to a counter-intuitive increase in the number of the receptors. This gentle chemical tug of war has the net effect of an overall increase in ECS activity leading to modulated and improved regulation of millions of cellular processes every second! You can think of this system as a sort of biological buffer.

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