The chemist and druggist, 18/25. December 2010 (issue 6778)
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Practical Approach
Effect of exercise on drug activity
Lauren Olsen, a GP trainee at a
practice to which David Spencer
provides prescribing advice, contacts
David to discuss an issue that has
been concerning her.
"David," she says, "these days
we're always encouraging our
patients to take lifestyle measures to
improve or maintain their general
health, and I've been quite impressed
by how many are taking the advice
seriously and implementing it.
"A lot of them have taken up
regular exercise, like running,
swimming or using a gym, and that's
great because it obviously brings
physiological benefits. But,
particularly in the case of people on
long-term medication, I wonder
whether exercise might affect the
effectiveness of their drugs?"
"I think I can give you some
pointers there," replies David.
1. What are the four processes
involved in the pharmacokinetics
of a drug's activity?
2. What is the additional factor
connected with exercise?
3. What is the effect of exercise
on drug pharmacokinetics, and
for which drugs has an effect
been shown?
Answers
1. Absorption, distribution,
metabolism, excretion.
2. Blood flow: At rest, the liver and
kidneys - where much of drug
metabolism and excretion take place
- receive about 50 per cent of the
body's blood flow. During moderate-
to-intense physical activity, blood is
redirected from central organs
(except the heart) to working
muscles and, as a result, only 3 per
cent of the body's blood is
distributed to the liver and kidneys.
In addition, exercise decreases
glomerular filtration rates in the
kidneys by as much as 30 per cent
and can take more than an hour to
return to normal afterwards. It is
therefore advisable not to take
medication immediately before
moderate-to-intense exercise.
3. Drug absorption can occur in
subcutaneous and transdermal
tissues; redistribution of blood flow
to these sites during exercise can
affect drug absorption. The rate of
absorption of insulin increases
significantly after subcutaneous
injections into working muscles, and
low plasma glucose levels have been
reported as a result of the rapid
absorption of insulin when injected
into a muscle that is about to be
actively worked. Exercising with a
transdermal patch such as
nitroglycerin or nicotine has also
produced increased plasma drug
concentrations.
Exercise has been shown to change
drug binding to plasma proteins and
other tissues, increasing during
exercise, and this in turn may
influence drug binding to plasma
proteins and tissues. In addition,
alterations in drug distribution may
occur because of redistribution of
blood to active muscles. Drugs
shown to be affected in this way
include theophylline and acebutolol
Digoxin binding has also been shown
to be altered during exercise.
Improved fitness can alter
metabolic enzyme activity and
therefore affect drugs whose
metabolism depends on this
mechanism, although to date there is
little evidence of clinical effect.
LenzTL. Pharmacokinetic Drug
Interactions with Physical Activity.
Am J Lifestyle Med. 2010;4:226-229
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