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Drug Supplement Interactions
Drug Supplement Interactions
Drug-Supplement, Drug-Nutrient
Leo Galland, M.D.
Applied Nutrition, Inc.
www.nutritionworkshop.com
Overview
Of almost 900 drugs and fixed-drug
combinations used in the U.S.:
• Almost 400 may deplete specific nutrients.
• Over 400 may interact with food or food
components.
• Over 300 have been shown to interact with
dietary supplements, with adverse and
beneficial interactions equally common.
Types of Interactions
• Pharmacodynamic: two substances exhibit
pharmacologic actions that reinforce or
interfere with each other’s actions.
• Pharmacokinetic: the absorption,
distribution, excretion or enzymatic
transformation of one substance is altered
by another. Most adverse interactions are of
this type.
Pharmacokinetic Mechanisms
• Alteration of gastrointestinal or urinary pH.
• Stimulation, induction or inhibition of
enzymes involved in biotransformation or
transport of drugs or nutrients .
• Displacement of a drug from binding to
plasma proteins.
• Alteration of solubility.
Effects of Interactions
• Nutrient depletion: Individual nutrients may have
their dietary requirement increased by specific
drugs (or supplements).
• Adverse: A specific supplement may undesirably
decrease or increase the effect of a drug or
supplement being taken.
• Beneficial: Drugs (or supplements) may have their
actions enhanced or side effects diminished by
specific supplements.
Drug-Induced Nutrient Depletion
• About half the drugs used in clinical
practice have documented nutrient
depleting effects.
• Co-enzyme Q10, folic acid, B2, B6, Mg, Zn
are nutrients most likely to be depleted.
• Mechanisms include impaired absorption or
bioactivation; increased excretion.
Co-enzyme Q10 Depletion
• Statin-induced co-Q depletion impairs
mitochondrial function, raising the serum
lactate/pyruvate ratio. Simvastatin but not
atorvastatin depletes myofibrillar co-Q.
• Supplemental co-Q, 100 mg/day, prevents the
decline in serum co-Q levels without impairment
of the lipid-lowering effect of statins and may
reverse symptoms of statin myopathy.
Co-enzyme Q10 Depletion
(cont’d)
• Statin-induced Co-Q depletion is increased by
vitamin E (700 IU/day).
• Co-Q is consumed in recycling tocopheryl
quinones back to tocopherols.
• Thiazides, some beta-blockers and many older
psychotropic drugs have been shown to interfere
with co-Q dependent enzymes, creating a possible
need for co-Q supplementation in patients
receiving them.
Are reported adverse
cardiovascular effects of vitamin
E supplements related to co-Q
depletion in patients taking drugs
that interfere with co-Q
synthesis or co-Q dependent
enzymes?
Vitamin E and Statins
• a-Tocopherol prevents statin benefits in
people with low HDL-C and normal TC.
• Related to tocopherol inhibition of statin-
induced elevation of HDL2-C.
• Selenium (100 mcg/day) and fish oil have
the opposite effect.
• a-Tocopherol depletes gamma-tocopherol
by competitive binding to transport protein.
Clinically Significant Depletions-1
• Adriamycin depletes co-enzyme Q10.
Cardiotoxicity is reduced by co-Q and
proprionyl-L-carnitine.
• Cisplatin depletes Mg. Nephtrotoxicity is
reduced by i.v. and oral Mg (160 mg tid).
• Thiazides and 5-ASA derivatives deplete
folate, raising homocysteine concentration.
Clinically Significant Depletions-2