Statins Dysregulate the Endocannabinoid System

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Coronary heart illness is the main reason for loss of life globally. Hundreds of thousands of individuals deal with coronary heart illness by taking statins to manage their ldl cholesterol. Sadly, these medicine may cause muscle weak point and myopathy in some sufferers. Docs as soon as thought muscular ache was psychosomatic, however there’s extra to it. Statin medicines deplete cannabinoid receptor operate, in response to a current research by a workforce of distinguished Italian scientists.

The research, launched as a preprint on Analysis Sq. earlier than peer overview, means that simvastatin, a broadly used treatment, impacts enzymes within the endocannabinoidome, the expanded endocannabinoid system encompassing a number of endogenous fatty acid compounds along with anandamide and 2-AG (the 2 most distinguished endocannabinoids). Extra troublesome, although, is that simvastatin alters genes concerned in regulating cannabinoid receptors.

Mapping cannabimimetic pathways manipulated by statins and redesigning current medicines to respect the endocannabinoidome might result in therapeutic adjuvants which will restrict opposed reactions to statins. That is vital, contemplating that statins are essentially the most prescribed lipid-lowering brokers worldwide – not solely to decrease ldl cholesterol but additionally to inhibit irritation and stabilize atherosclerotic plaques.

Statins & Lipid-Reducing Medication

Statins cut back ldl cholesterol by inhibiting an enzyme within the liver known as HMG-CoA reductase. General, they decrease low-density lipoprotein (unhealthy ldl cholesterol) and triglycerides, whereas growing good levels of cholesterol.

Lipid regulation helps cut back the danger of heart problems. The lipidome, nonetheless, consists of endocannabinoids and endocannabinoid-like neurotransmitters. And this might be why statin medicines, similar to simvastatin, whereas typically nicely tolerated, may cause severe uncomfortable side effects, together with ache and poisonous myopathies, in some folks.

HMG-CoA liberates a pathway that, in crops, is liable for phytocannabinoid manufacturing. In animals, a novel enzyme household converts important dietary Omega-3 fats into endocannabinoids. Simvastatin dysregulates endocannabinoid tone by altering enzymes within the endocannabinoidome, in response to the current preprint. Simvastatin additionally reduces cannabinoid receptor expression.

Simvastatin Alters Endocannabinoid Gene Expression

The Italian scientists examined simvistatin on particular mouse cells and tissues. The cells utilized within the experiment had been a sort of myoblast, a stem cell that varieties muscle. The scientists additionally examined the lipid-lowering drug on skeletal muscle tissue, which they extracted from sacrificed mice, and on human myoblasts. Simvastatin diminished muscle energy in handled mice in comparison with their untreated littermates.

Extreme endocannabinoid exercise is related to pathological circumstances similar to sort 2 diabetes, liver and kidney dysfunctions.

The cholesterol-cutting drug altered genes liable for endocannabinoid creation and degradation. Publicity to the statin-based treatment in the end elevated mobile endocannabinoid expression, that means it boosted the degrees of anandamide and 2-AG. This may be problematic as a result of extreme endocannabinoid exercise “is related to a plethora of pathological circumstances affecting each the mind and peripheral organs and tissues,” the preprint authors clarify, citing examples similar to “sort 2 diabetes, liver and kidney dysfunctions.”

Simivastin Additionally Stunts a Cannabinoid Receptor

The endocannabinoid system is the last word homeostatic regulator. It fine-tunes a big selection of physiological processes that reply to “numerous intrinsic in addition to extrinsic stimulants via a fancy cascade of receptor activation, gene expression [and] enzymes reactions.” Thus, when endocannabinoid ranges are extreme, cannabinoid receptors will downregulate as a compensatory response. (Persistent hashish consumption downregulates cannabinoid receptor expression.) And, conversely, when endocannabinoid ranges are low or poor, cannabinoid receptors will compensate reply by upregulating.

Along with boosting endocannabinoid ranges, simvastatin repressed CB1 and CB2 receptors in addition to TRPV1 ion channels, which negatively impacted the endocannabinoid system. CB1 receptors in skeletal muscle cells regulate key metabolic pathways that have an effect on insulin sensitivity and glucose uptake. The administration of artificial cannabinoid receptor antagonists (rimonabant and AM251), which block the CB1 receptor, additionally elevated muscular ache and weak point induced by simvastatin.

To summarize: statins trigger toxicity by dysregulating anandamide and 2-AG and suppressing CB1 receptor expression, leading to impaired cannabinoid receptor signaling in myoblasts. However sooner or later cholesterol-regulating statins formulated with optimistic allosteric modulators, which improve CB1 receptor operate, could negate some poisonous uncomfortable side effects of statins. Additional analysis that explores how statins have an effect on the endocannabinoid system, inflicting muscular ache and weak point, must be a precedence on condition that 200 million sufferers across the globe take these lipid-lowering medicine.

Travis Cesarone is a contract author and communicator specializing in medical hashish sciences.. Copyright, Undertaking CBD. Is probably not reprinted with out permission.


Hilal Kalkan, Elisabetta Panza, Ester Pagano et al. MicroRNA-mediated repression of endocannabinoid CB1 receptor expression contributes to simvastatin-induced skeletal muscle toxicity, 20 December 2022, PREPRINT (Model 1)


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