Print

Print


Camilla Flintermann <[log in to unmask]> wrote: <<<I have to
confess to some confusion about the Sinemet/food connection.  We have had
very persuasive
info from a number of people to the effect that Sinemet taken with food
loses much of its value by the time it gets out of the stomach. It sounds
so reasonable--then I notice that Peter's new RX bottle of Sin.CR 50/200
has a label shouting "TAKE WITH FOOD"!  So I called the pharmacist and
asked about it, telling him what I had learned here. His reply was that this
is the instruction from the manufacturer and the FDA requires them to so label
it.  He stated that the "package insert" is taken right from the PDR, which
is the info supplied by the manufacturer. He could not explain it further.
Now I wonder, are we correct in believing there's a problem, and that we need
to wait 30-60 min. after taking it before eating? Is there something about
the CR form that makes a difference in this way?  (He could not find ANY
info in the PDR about regular Sin. and food, only the CR form.) We would very
much appreciate clarification on this issue, which is something Peter and
others have to decide about many times a day! Thanks for any help you can
give.(We did discuss the need for food if one is nauseated.)... the
pharmacist quoted from the PDR that uptake (absorption) of Sin.CR is
25%-50% IMPROVED when taken with food.>>>
My understanding is that the residence time in the stomach is time during
which the metabolic "destruction" of the levodopa is occurring, but there
is no significant absorption of levodopa before it enters the small
intestine where the absorption of nutrients, et cetera is done via the
blood vessels very near the chyme absorbing molecules small enough to pass
through the thin membrane.

The levodopa will probably not be enough mass to get carried this far by
itself, so the dissolving is what is accomplished by waiting.  (The CR will
not dissolve completely for several hours.)  The pre-dissolving in water
with ascorbic acid (vitamin C) antioxidant to retard oxidation of the
levodopa eliminates the stomach wait and, IF the stomach is relatively
empty, the liquid carries the dissolved levodopa directly to the small
iintestine.  If that is empty, the liquid carries the medication quite far.

The "carrier" is labeled LNAA-carrier.  It is not likely to be very active
if there is no chyme, so my "prescription" is to use small food intake of
optimum sort with the medication(s).  Some Large Neutral Amino Acids
(LNAAs) will come from most foods.  There is also some benefit to have some
sugar and some bulk - but avoid: fat, animal protein (especially if you
tend to chew only enough to swallow since large chunks reside in the
stronger digestive juices and the levodopa is made useless).  Dairy fat is
not helpful, plant protein is usually not as much harm, but don't eat seeds
and nuts then.

The small intestine is small in diameter - this causes close proximity to
the blood vessels and nutrients, water excess, and many chemicals are
absorbed, some resorbed that go later back into the stomach to aid
digestion, etc.

If there is enough mass of food to carry much of the medication into the
small intestine before the main meal actually is put into the stomach, one
benefits by optimum absorption of levodopa into the bloodstream.  (There is
a saturation or concentration limit for LNAAs (levodopa is only one of ?
many).  More blood moves if digestion-absorption is continuing so that the
blood with the levodopa gets to the brain where transporting out of blood
into brain takes time also.

In short, eat a couple of crackers, a prune perhaps, after taking the meds
with water or some orange or other juice.  Sucking one peppermint or
butterscotch sugar-bomb or piece of ginger may help by chewing, swallowing
and saliva generation which aid digestion.  You might find less med
required following this advice.  Or, if you take less more often.  The
blood plasma concentration peaks rather quickly after the dose reaches the
intestine and then is rapidly dropping unless you are using the CR type
which apparently dissolves for several hours with decreasing surface area
providing decreasing amount as this occurs.

The Sinemet CR presentation to the recent meeting in Europe should soon be
available as a paper.  This may add much to the store of knowledge.  I feel
that this subject needs further discussion and probably could be aided by
those of us interested trying to prepare a monograph or some sort of
document that could have the distortions removed over the next few years
and yield some pertinent needed educational advice.

I did a little with graphical addition plots of concentration in plasma
following Bob Naylor's inputs and help, but have not finished what I
started.  Maybe I will get back to that...

ron      1936, dz PD 1984  Ridgecrest, California
Ronald F. Vetter <[log in to unmask]>
http://www1.ridgecrest.ca.us/~rfvetter