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Cholesterol-Lowering Bile Acid Blockers Increase Risk For Mental Decline

Shocking Study Finds A Class Of Widely-Prescribed Cholesterol-Lowering Medications That Bind To Bile Are Associated With An Increased Risk Of Dementia Among Males. The Antidote Is Vitamin C.

For the first time medical investigators have made a link between irregularities in the breakdown of cholesterol into bile and the development of dementia (forgetfulness, thinking, having an “adult moment).”

For over 40 years physicians have prescribed a class of cholesterol-lowering drugs that bind to bile, bile being composed of cholesterol.  Drugs that attempt to lower circulating levels of cholesterol are now associated with beta amyloid plaque in the brain.

These findings were primarily observed in males.  The pharmacological practice of lowering bile levels with the use of bile-binding drugs (bile acid sequestrants) may impair signaling in the brain which in turn may explain dementia among adult males.

Researchers also found higher blood serum concentrations of bile acid are associated with lower brain amyloid deposition, and slower brain atrophy (shrinkage) in males.

The use of bile sequestrant drugs was also correlated with low vitamin D blood levels.  Bile aids in the metabolism of vitamin D from dietary sources.  This ground-breaking report is published in PLOS MEDICINE, May 27, 2021.

Bile acid binders

Bile acid binders have been used since the 1970s to reduce circulating levels of cholesterol.

Bile acid sequestrant drugs bind to cholesterol in the gut, preventing reabsorption.  The drugs involved are: Cholestyramine {Questran, Prevalite}, Colestipol {Colestid}, Colesevelam {Welchol}).

Bile acids represent the primary pathway for cholesterol breakdown (catabolism) and account for ∼50% of the daily turnover and disposal of cholesterol.

Bile acids, produced in the liver, facilitate digestion and absorption of fats in the small intestine as well as regulate cholesterol homeostasis. Over the last decade, however, it has become clear that bile acids are not simply digestive detergents.  Bile has functions outside of the digestive tract.

Co-factors for bile

Nutrients play a role in the metabolism of cholesterol into bile.  Vitamin C, the amino acid taurine, oxygen, a niacin derivative (nicotinamide adenine dinucleotide phosphate (NADPH), choline, and betaine (trimethylglycine) are required to convert cholesterol to bile.

Bile, produced in the liver and stored in the gall bladder, is transported out of the liver by amino acids glycine and taurine.

Vitamin C, bile and gallstones

In the 1970s Slovakian researcher Emil Ginter demonstrated the transformation of cholesterol to bile is controlled by vitamin C.

High doses of ascorbic acid significantly stimulates cholesterol transformation to bile acids in guinea pigs and decreases plasma cholesterol concentration in humans.

Vitamin C therapy for elevated cholesterol has been shunned for over five decades.

Vitamin C is also a preventive against gallstones.  Ascorbic acid-deficient animals more frequently develop cholesterol gallstones.

Bile and estrogen

Women develop gallstones differently than men.  Pregnancy, oral contraceptives, and hormone replacement therapy all contribute to the formation of gallstones. Estrogen increases the risk for gall bladder disease or surgery.

This is because estrogen and progesterone increase the cholesterol to bile ratio conversion in the gall bladder, leading to supersaturation and thicker bile.

Bile is an important agent in the elimination of estrogen and its metabolites through the liver.  The less bile, the slower the elimination of estrogen at the end of a woman’s monthly cycle.  Women then experience symptoms like cramping, breast tenderness, water retention, and acne.

Other maladies associated with abnormal bile flow

Bile is also crucial for proper absorption of the fat-soluble vitamins A, D, E, and K and cholesterol. These bile-binding drugs may prevent absorption of folic acid and the fat-soluble vitamins A, D, E, and K.  Animal studies suggest calcium and zinc may also be depleted by taking one class of these drugs (cholestyramine).

The problem of poor bile flow is worsened by surgical removal of the gall bladder, which is a storehouse and “squirt gun” for bile.

There are hundreds of thousands of gall bladder removal surgeries annually due to stones or symptoms caused by thick sludgy bile.

There are other adverse consequences that emanate from chronic use of bile acid binders.

This is another example of doctors touting prescription drugs to the exclusion of vitamin therapy.