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Welcome. My name is Paul Boylan,
I am an Associate Professor
in the department of Pharmacy,
at the University of Oklahoma,
Health Sciences
College of Pharmacy
in Oklahoma City, Oklahoma.
Today we'll be discussing
the topics of "Theophylline,
and Anti-Leukotrienes
for the Treatment
of Airway Allergic Disorders".
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Welcome to Part 2 of this
presentation on theophylline,
anti-leukotrienes
for the treatment
of airway allergic diseases.
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In Part 2, we will cover
the methylxanthine,
theophylline.
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Theophylline is a
medication that possesses
many various
mechanisms of action
to reduce inflammation and
cause bronchodilation.
I've listed the most
common mechanisms
for you on this
slide in this table.
Starting at the top,
theophylline is
known as a phosphodiesterase
inhibitor,
specifically a non-selective
phosphodiesterase inhibitor.
Clinically, that leads to
relaxation or bronchodilation of
lung tissues that helps to
open up the airways to help
patients living
with inflammation
in the airways to
breathe better.
Its second mechanism is to
inhibit adenosine receptors.
By inhibition of those
adenosine receptors,
it will ultimately inhibit
the histamine molecule
as well as leukotrienes.
This also serves to help
relieve bronchoconstriction by
inhibiting histamine
and leukotrienes.
This doesn't necessarily
increase bronchodilation
but instead
inhibits compounds
that are responsible
for causing
bronchoconstrictive actions.
As you will recall from
Part 1 of our presentation,
interleukin-10 is involved
in the inflammatory pathway.
Theophylline may
increase concentrations
of this interleukin compound,
and by increasing concentrations
of interleukin-10,
it would increase the production
of anti-inflammatory cytokines.
Theophylline also works
in the nucleus of
the cell by inhibiting
something called NF Kappa B,
or nuclear factor
kappa-light-chain B
and by inhibiting this,
it works on transcription and
translation to help
reduce the production
of pro-inflammatory
genes to help down
regulate the production of
pro-inflammatory molecules.
Theophylline may also work
directly on circulating
granulocytes
such as eosinophils
and neutrophils.
By acting on those cells,
it may cause them to apostatize.
When it does that, it helps
to decrease levels of
innate inflammation by working
on the innate immune response.
Theophylline's last
major mechanism is
to activate histone deacetylase.
By activating this
particular enzyme,
it works in synergy with
the corticosteroids.
Common corticosteroids include
prednisone, triamcinolone,
budesonide,
fluticasone, so theophylline
may help to have
a synergistic effect with
those compounds which
also reduce inflammation.
