RSPT 1213 – Basic RC Pharmacology
Corticosteroids
Lecture Notes
Reference & Reading: Egan’s p. 179, 478-485, 640-641
I. Inflammation in the Airway
a. Several Causes
 Direct trauma
 Indirect trauma
 Inhaling noxious/toxic substances
 Respiratory/Systemic infections
 Septic shock
 Allergenic/nonallergenic stimulation in asthma
b. Two most common
 Chronic Bronchitis
 Asthma
II. Airway Inflammation in Asthma
a. Chronic inflammation of the airway wall; causing airflow limitation &
hyperresoponsiveness due to stimuli
b. Inflammation is mediated by inflammatory cells
 Mast cell*
 Eosinophil*
 T lymphocytes – coordinate the inflammatory response by releasing
proinflammatory cytokines which then act on basophils, epithelial
cells & endothelial cells furthering inflammatory process.
 Macrophages
*Major effector cells in airway inflammatory response Mediators released
by these cells during a reaction can cause:
1. Bronchospasm
2. Increased microvascular leakage
3. Mucus production
4. Remodeling of the airway (over long term)
III. Asthma attacks are Biphasic
a. After initial insult (allergen, cold air, viral infection, noxious gas inhalation)
b. Early Phase Response
 Caused by immunoglobulin E (IgE) – antibody activates mast cell
 Mast cell releases inflammatory mediators
1. Histamine – immediate response is bronchospasm
2. Eosinophils
 Response peaks @ approx 15 minutes & declines over an hour
 With mast cell degranulation mediators recruit other inflammatory
cells (eosinophils, basophils, etc.) to cause late-phase reaction
c. Late Phase Response
 Inflammatory cells have infiltrated airway & release inflammatory
mediators
1. Prostaglandin D2 (PGD2)
2. Leukotriene C4
 Occurs 6 to 8 hours after insult
 May last up to 24 hours
IV. Corticosteroids –
a. Three types of natural hormones:
 Glucocorticoids – cortisol
 Mineralocorticoids - aldosterone
 Sex hormones – androgens & estrogens
b. Corticosteroids used for pulmonary disease are a derivative of the naturally
occurring cortisol aka hydrocortisone
 Glucocorticoid agents are referred to as glucocorticosteroids,
generally corticosteroids, or simply steroids.
V. Indications & Purposes – Because of the large amount of systemic side effects involved
with systemic administration of steroids.
a. Can reduce or block the inflammatory process
b. In asthma & other inflammatory diseases steroids have the ability to inhibit
activity of inflammatory cells & mediators of inflammation
c. There are two preparations for respiratory delivery of steroids:
 Inhaled Corticosteroids:
1. Anti-inflammatory Maintenance therapy for:
a. Asthma – according to National Asthma Education and
Prevention Program Expert Panel Report 2; in
conjunction with systemic corticosteroids in severe
asthma; allows systemic dose reduction or elimination
in asthma control
b. COPD – recommended by American Thoracic Society &
Global Initiative for Chronic Lung Disease (GOLD)
 Intranasal aerosol:
1. Management of :
a. Seasonal & perennial allergic
b. Non-allergic rhinitis
d. Mode of Action – Lipid-soluble drugs that act on intracellular receptors (Figure
29-6, p. 642)
e. Suppress a local or systemic inflammatory response through several actions.
 Upregulation (induces) transcription of anti-inflammatory substances
that decrease airway responsiveness
 Suppress factors within the cell that cause the transcription of
inflammatory substances
 Upregulate inhibitor proteins which help to further suppress gene
expression for inflammatory proteins such as cytokines.
f. General result is to induce gene expression for anti-inflammatory proteins &
receptors as well as suppress gene expression for proinflammatory proteins
g. Inhibit cytokine production responsible for recruitment and migration of
inflammatory cells (eosinophils & lymphocytes in the airway)
VI. Aerosolized Corticosteroid Agents: high topical-to-systemic potency ratio  suitable for
maintenance with minimal systemic side effects.
a. Metered Dose Inhalers
Name
Brand
Name(s)
Indications
Contraindications
Maintenance
Maintenance drug; not
therapy for
to be used as rescue
asthma in children
drug
Dosing Schedule
Available in 44 μg 110 μg and 220 μg per puff
2 puffs BID
over 6 and adults
Wean over several
Fluticasone
Flovent®
Weaning off
weeks; do not stop
oral/systemic
abruptly
steroids
May not affect adrenal
Not studied in
glands, wean oral
children under 12
steroids when drug is
years of age.
started
Maintenance drug; not
Maintenance
to be used as rescue
therapy for
drug
Available in 42 μg or 84 μg per puff
2 puffs TID or BID
asthma for
Beclomethasone
dipropionate
Beclovent®
Vanceril®
teenager and
Wean over several
adults
weeks; do not stop
abruptly
May be used to
wean off
May not affect adrenal
oral/systemic
glands, wean oral
steroids
steroids when drug is
started
Maintenance drug; not
Maintenance
to be used as rescue
therapy for
drug
asthma in
Beclomethasone
dipropionate
QVAR®
HFA
Available in 40 μg or 80 μg per puff
teenagers and
Wean over several
adults
weeks; do not stop
2 puffs BID
abruptly
Weaning off
http://www.qvar.com/HCP/Dosing.aspx
oral/systemic
May not affect adrenal
steroids
glands, wean oral
steroids when drug is
started
Triamcinolone
acetonide
Maintenance
Maintenance drug; not
therapy for
to be used as rescue
asthma in
drug
2 puffs TID or QID
Wean over several
https://www.azmacort.com/downloads/Azmacort-
weeks; do not stop
PI.pdf
100 μg per puff
teenagers and
Azmacort®
adults
Weaning off
abruptly
High initial doses of 12-16 puffs may be used in
oral/systemic
steroids
May not affect adrenal
glands, wean oral
severe asthma
steroids when drug is
started
Maintenance drug; not
Maintenance
to be used as rescue
therapy for
drug
asthma in
Flunisolide
AeroBid®
teenagers and
Wean over several
adults
weeks; do not stop
abruptly
AeroBid-M®
Weaning off
oral/systemic
May not affect adrenal
steroids
glands, wean oral
250 μg per puff
2 puffs BID
http://www.frx.com/products/aerobid.aspx
steroids when drug is
started
Maintenance
Maintenance drug; not
therapy for
to be used as rescue
160 μg per inhalation
asthma for
drug
80 μg per inhalation
Wean over several
1 inhalation QD
teenager and
Ciclesonide
adults
Alvesco ®
weeks; do not stop
May be used to
abruptly
http://www.alvesco.com/en/Menu/About+alvesco/
wean off
oral/systemic
Very low systemic
steroids
effects
b. Dry powdered inhaler
Name
Brand
Name(s)
Indications
Contraindications
Maintenance
Maintenance drug; not to be
therapy for
used as rescue drug
asthma in children
over 6 and adults
Fluticasone
Flovent®
Diskus®
Dosing Schedule
Available in 44 μg 110 μg and 220 μg per puff
2 puffs BID
Wean over several weeks; do
not stop abruptly
Weaning off
http://www.gsk.com/products/prescription_medi
cines/us/flovent.htm
oral/systemic
May not affect adrenal glands,
steroids
wean oral steroids when drug is
started
Maintenance
Maintenance drug; not to be
therapy for
used as rescue drug
asthma in children
Budesonide
Pulmicort
Turbuhaler®
over 6 and adults
200 μg
DPI BID
Wean over several weeks; do
not stop abruptly
Weaning off
oral/systemic
May not affect adrenal glands,
steroids
wean oral steroids when drug is
started
http://www.twistclickinhale.com/
Maintenance
Maintenance drug; not to be
therapy for
used as rescue drug
asthma in children
Budesonide
over 6 and adults
Pulmicort
6 – 17 years 180 or 360 mcg BID
Wean over several weeks; do
not stop abruptly
Flexhaler ®
90 μg ; 180 μg
≥ 18 years: 360 or 720 BID
Weaning off
oral/systemic
http://www.pulmicortflexhaler.com/p/
steroids
Maintenance
Maintenance drug; not to be
therapy for
used as rescue drug
asthma 4years
and older
Mometasone
Asmanex
furoate
Twisthaler ®
110 μg, 220 μg
≥ 12 years 1 inhalation QD or 2 inhalations BID
Wean over several weeks; do
4 – 11 years 110 μg QD
not stop abruptly
Weaning off
http://www.spfiles.com/piasmanex.pdf
oral/systemic
May not affect adrenal glands,
steroids
wean oral steroids when drug is
started
c. Combination Steroids
Name
Brand
Indications
Name(s)
Contraindications
Dosing Schedule
Maintenance therapy for
Maintenance drug; not to
ADVAIR DISKUS
asthma in children 4-11
be used as rescue drug
100/50,
Wean over several weeks;
ADVAIR DISKUS
do not stop abruptly
250/50
May not affect adrenal
ADVAIR DISKUS
glands, wean oral steroids
500/50
years and adults 12 and
older
Weaning off oral/systemic
steroids
when drug is started
Fluticasone propionate
and Salmeterol
1 inhalation BID
Patients receiving ADVAIR
Advair Diskus®
DISKUS twice daily should
www.advair.com
not use additional
salmeterol or other inhaled,
long-acting beta2-agonists
(e.g., formoterol) for the
maintenance treatment of
COPD or for any other
reason.
Fluticasone propionate
and Salmeterol
Advair HFA®
Maintenance therapy for
Maintenance drug; not to
asthma in children 4-11
be used as rescue drug
45 μg fluticasone/
50 μg slameterol
years and adults 12 and
older
Wean over several weeks;
115 μg fluticasone/
do not stop abruptly
50 μg slameterol
Weaning off oral/systemic
steroids
May not affect adrenal
glands, wean oral steroids
230 μg fluticasone/
50 μg slameterol
when drug is started
Patients receiving ADVAIR
2 inhalations BID
DISKUS twice daily should
not use additional
salmeterol or other inhaled,
long-acting beta2-agonists
(e.g., formoterol) for the
maintenance treatment of
COPD or for any other
reason.
Long-term maintenance
therapy of asthma for
patients ≥12 years old
Budesonide/formoterol
fumarate HFA
Patients who are receiving
SYMBICORT should not use
additional formoterol or other
long-acting beta2-agonists for
any reason
Symbicort ®
80/4.5 (80 mcg
budesonide, 4.5 mcg
formoterol)
160/4.5 (160 mcg
budesonide, 4.5 mcg
formoterol
2 inhalations BID
www.symbicort.com
d. Nebulized Steroids
Name
Brand
Name(s)
Indications
Contraindications
Maintenance
Maintenance drug; not to be used
treatment of
as rescue drug
asthma and as
Budesonide
Pulmicort
Respules®
Dosing Schedule
Available in 0.25mg or 0.5 mg
Initiate with 0.5 mg daily (0.25 BID) if
prophylactic
Wean over several weeks; do not
previously on inhaled steroids or 1 mg daily
therapy in
stop abruptly
(0.5 mg BID) if previously on oral steroids
children 12
2 puffs BID; Continue 0.25-0.5 mg QD or
months to 8
May not affect adrenal glands, wean
years of age.
oral steroids when drug is started
BID after evaluation
http://www.pulmicortrespules.com/professional
/benefitprt/intro.asp
e. Nasal Solutions
Name
Budesonide
Brand Name(s)
Rhinocort®
Indications
Relieve symptoms of
Allergy Rhinitis
Dosage
32μg per spray
Initial dose 4 sprays QAM
Wean to 2 sprays
Fluticasone
propionate
50μg per spray
Flonase®
Relieve symptoms of
Allergy Rhinitis
2 sprays QD
For use in children ≥ 4
years
27.5 μg per spray
Fluticasone furoate
Veramyst ®
Relieve symptoms of
1-2 sprays/nostril QD
Allergy Rhinitis
For use in children ≥2
years
Flunisolide
Triamcinolone
acetonide
Nasalide®, Nasarel®
Nasacort®
Relieve symptoms of
Allergy Rhinitis
Relieve symptoms of
Allergy Rhinitis
58μg per spray
Adults: 2 sprays BID
Children: 1 spray TID
50μg per spray
2 sprays QD
42μg or 84μg per spray
1 spray 42μg 2-4 time a
day
Bechlomethasone
Beconase®,
Relieve symptoms of
Vancenase®
Allergy Rhinitis
Adults & Children older
than 12: 1-2 sprays of
84μg BID
Children 6-12 years: 1
spray 84μg BID
Mometasone furoate
monohydrate
Nasonex®
Relieve symptoms of
Allergy Rhinitis
50μg per spray
2 sprays QD
VII. Adverse Effects of Corticosteroids (Box 29-3; p. 642)
a. Systemic – typically oral administration
 Hypothalamic-Pituitary-Adrenal (HPA) Axis
1. Pathway for release a& control of endogenous corticosteroids
2. Hypothalamus sends impulses via median eminence to pituitary
gland that releases adrenocorticotropic hormone (ATCH) into
bloodstream stimulate adrenal cortex to secrete
glucocorticoids such as cortisol.
 HPA suppression/Adrenal insufficiency – occurs with
administration of steroids.
1. In the body endogenous steroids are regulated by feedback
within HPA axis to limit production
2. the body can’t tell between exogenous & endogenous steroids
3. With exogenous administration; drugs raise body level of
hormones, inhibits hypothalamus & pituitary gland which 
adrenal production
 To help the body regulate:
1. Wean to inhaled steroid – when aerosol started & oral tapered
off at the same time
2. Every other day administration – administering like this mimics
the body’s natural pattern
3. Tapered dose therapy: allows time for recovery of the body’s
own adrenal secretion
 Cushing’s syndrome: characterized by elevated plasma ACTH levels
and enlargement of the adrenal cortex and hyperactivity of the gland
1. http://csrf.net/smTwins2.jpg
2. Some signs and symptoms include: rounded face, reddened
cheeks, acne, headache, excess hair growth (fine downy hair on
cheeks, arms, and legs), purplish-pink stretch marks (more
common in older children and adults), darkened skin around
neck and armpit areas, easy bruising, development of pubic hair
at a younger age than usual, irregular or absent menstrual
periods, and high blood pressure.
 Obesity with fat distribution to the face, upper back and belly
resulting in the classic “Moon face” & “buffalo hump” appearance of
the long-time steroid patient.
1. http://www.virusmyth.net/aids/pics/buffalo.jpg
2. http://www.passarella.com/matt/matt-moonface.jpg
 Muscle weakness & myopathy
 Mood swings
 Growth retardation
b. Local side effects
 Two most common:
1. Oropharyngeal fungal infections
http://pathmicro.med.sc.edu/lecture/images/thrush.jpg
2. Dysphonia – hoarseness & changes in voice quality
 Use of MDI spacer & gargling recommended