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By Michael Bosse, PharmD
TCOYD Newsletter, Vol. 27, 2008
We all know there is no such
thing as a “natural” miracle
cure for any type of illness. There
are, however, a multitude of natural
products that have been, or are being
used to treat diabetes, obesity, and
many other conditions. Some people
swear by them while others swear
them off. Regardless of your philosophy
on the use of natural medicines
and supplements, it is important to
understand from a pharmacy standpoint
how your body processes them.
ADME: It’s Not Peer Pressure,
Every “Body” is Doing It
ADME stands for Absorption,
Distribution, Metabolism and
Excretion and it represents how
your body processes everything you
put into it: food, prescription drugs,
over the counter (OTC) products,
supplements and natural remedies.
Whether you had it prescribed,
purchased it over the counter at a
health food store, grew it or bought
it online, anything and everything
you ingest, inject, apply or inhale
MUST go through ADME. There
are no exceptions.
Whether you believe it or not, you
have been exposed to ADME before.
It is the baritone voice barking out
warnings near the end of a prescription
drug TV commercial while the
happy couple on screen frolic
gleefully on the beach “Take on a
empty stomach (Absorption); Talk to
your doctor if you have circulatory
disease (Distribution); Do not take if
you have active liver disease
(Metabolism); Talk to your doctor if
you have kidney disease (Excretion).”
Modern Day Medicinal Heirogyphics
Can you tell which of the figures pictured is
a natural product? These are the
chemical structures of some very
common prescription and natural
products. Your body interprets these
structures on a chemical level and
applies the ADME principles accordingly.
Figure 1 is metformin, which
works primarily in the liver where
sugar is made. Figure 2 and Figure 3
lower cholesterol, with Figure 2 being
the natural product red yeast rice and
Figure 3 being the prescription drug
Zocor (simvastatin). Can you see the
similarities in the ring structures?
Figure 4 is the anti-depressant Celexa
(citalopram). It needs to get into the
brain to exert it effects. The point
being that your body does not differentiate,
it goes to work on whatever
you put into it, regardless of whether
it is natural or prescription in origin.
A: Absorption
Pills, injections, creams, syrups,
elixirs, inhalers, and suppositories
all have one thing in common; they
want to get into your body and exert
an effect. How they get to intended
site of action depends on how your
body absorbs them. Oral pills need
to be broken down into their active
ingredients, like the chemical structures
above, and properly absorbed
into the blood stream. Most medications
found in inhalers are designed
to be absorbed in the lungs, appropriate
because this is their primary site
of action. Ever wonder why there is no insulin pill? Because insulin is a
protein, it would be broken down by
the high acid content of the stomach
and would never be absorbed into the
blood. When given by injection into
the subcutaneous tissue of the
abdomen, insulin bypasses the acidic
stomach and is absorbed into the
blood via the layers of fat just below
the skin.
D: Distribution
Now that the drug made its
way in and has been properly
absorbed, where does it go from
there? It is distributed into your
body according to its
chemical make-up.
Actos (pioglitazone)
needs to be distributed
to cells of the
body that utilize
sugar, specifically
into the nucleus and
DNA of these cells
where it exerts its
blood glucose lowering effects.
Anti-depressants work by crossing
the blood brain barrier (BBB) and
increase chemicals in the brain to
improve depressive symptoms. An
anti-itch cream such as 1% hydrocortisone
is mostly distributed right
where it is applied, on the skin, and
does not enter the blood stream. ALL
medications are distributed according
to their chemical properties as illustrated
by the ring structures above.
M: Metabolism
When a drug or natural product
enters the body, the process of metabolism
begins as your body attempts
to break it down into usable pieces.
Much the same way food is broken
down into sugar, fats and proteins,
medications suffer a similar fate
generally at the hands of the liver
and the enzymes of the cytochrome
P450 system. Think of this complex
system as lanes on the freeway, with
every drug, nutraceutical and supplement
having a preference for one
particular lane. Based on their
chemical make-up, many drugs
and natural
products like
to use the same
lane to be
metabolized.
Some natural
products such
as St. Johns
Wort “block”
many of these lanes used for metabolism
of prescription drugs, increasing
the chance for toxicity or unwanted
side effects. When this delicate
balance of metabolism is altered by
disease or other drugs, prescription
or otherwise, the result is often times
not pleasant and sometimes scary.
When a new medication is started
and throughout the course of
treatment, your doctor may order
blood tests to check on the health
of your liver.
E: Excretion
Once drugs have exerted their
effects, the body decides it is time
to get rid of them. The major routes
of elimination are the urine via the
kidneys and the feces via the liver.
“Half life” refers to the time it takes
for your body to excrete or
eliminate 50% of any given drug.
Generally, medication with a long
half life is given once a day and
drugs with shorter half life are given
two or three times a day. Disease or
damage to either the kidneys or
liver can impair the way drugs are
removed. Often times medication
dosing regimens are changed based
on the degree of kidney damage or
liver disease as assessed by a
physician.
The take-away from this is
to speak with your physician or
pharmacist about ALL medications
you take to manage your health—
natural, OTC, prescription or
otherwise. These all work off of
ADME principles and therefore the
potential for pharmacological issues
exists, drug interactions, decreasing
effectiveness, toxicities, etc. Natural
does not always equal a better
outcome any more than prescription
always means a better way to treat
your health.
Michael Bosse, PharmD, is owner of A1c Rx
Pharmacy in California
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