Pharmacological Treatment Options for ___ASTHMA (Anti-inflammatory Agents) ___
Sareh Seyedkazemi, PharmD Candidate 2007
Corticosteroids
Product
Availability
Generic (Brand)
Mechanism
of Action
EFFICACY
(Indication/Use,
Clinical Data
Support)
Mast Cell Mediators
Inhaled:
Beclomethasone (QVAR)- 40 & 80
mcg/ACT
Budesonide (Pulmicort)- 200 mcg/
ACT
Flunisolide (Aerobid)-250 mcg/ACT
Fluticasone (Flovent)-44, 110, 220
mcg
triamcinolone acetonide (Azmacort)100 mcg/ACT
 ↓ mucous production &
hypersecretion.
 Prevent & reverse remodeling
 Reduces airway
hyperresponsiveness
 ↑ # of receptors & response
 ↓ microvascular leakage ↓
edematous airway.
cromolyn (Intal)- 1 mg/ ACT
nedocromil (Tiladel)- 1.75mg/ ACT
Severe:
 Inadequate response to B2-agonists
Chronic:
 Most potent and consistently
effective
 ↓ in severity of symptoms
 ↑ in PEF and spirometry
 ↓ airway hyper-responsiveness
 ↓ # of exacerbations
 Potential prevention of airway
remodeling
 Broad anti-inflammatory action
Chronic
 Agent of choice: most effective
 Low-med dose: ↓BHR, ↑PFT, ↓
ER/hospitalizations
 Reduce the risk of dying

Sareh Seyedkazemi, PharmD Candidate 2007
University of Maryland School of Pharmacy
Leukotriene Modifiers
Anti-IgE Antibodies
zafirlukast (Accolate)- 10,20 mg
Omalizumab (Xolair)- 150 mg
powder for reconstitution
montelukast (Singulair)- granules
4mg/packet. Tablets: 4 (chewable), 5
(chewable), and 10 mg
zileuton (Zyflo)-300, 600 mg tablets







modulation of mast cell release
and recruitment of eosiophils.
Inhibit early and late phase and
exercise induced bronchospasm
Inhibit bronchoconstriction but
does not cause
bronchodilatation.
Both are equally effective
against allergens
nedocromil > potent than
cromolyn.
No change in BHR with longterm use.
Dose dependent efficacy
Equiefficacious to LT
antagonists and methylxanthines
for persistent asthma
zafirlukast/ montelukast- antagonists
of the LTD4 receptor antagonists
preventing bronchospasm, mucous
secretion, microvascular
permeability, % airway edema.
zileuton: inhibition of the synthesis
of leukotrienes by blocking 5lipoxygenase.
 Alternative for chronic persistent
asthma
 ↑ PFT, ↓ nocturnal awakenings
and B2-agonist use, & improve
asthma symptoms.
 Aspirin-sensitive asthma
 Allergic rhinitis-modest efficacy
Antibody against IgE that becomes
part of the receptor complex and
does not induce anaphylaxis but
reduces activation of immunologic
response.

FDA approved for corticosteroid
dependent severe asthma.
o Atopy and elevated IgE
concentrations
o Studied in patients 1274 years of age.
**Shown to increase efficacy when
combined with inhaled
corticosteroids versus increasing the
dose of corticosteroids along.
Pharmacotherapy Presentation – Pharmaceutical Care Rotation
Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
SAFETY
(Major Drug
Interactions,
Pre-cautions,
Contraindications,
Adverse Effects,
Pregnancy Risk
Category)
Adverse Effects:
Low-Med Dose- delayed growth; not
significant.
High Dose- osteoporosis/ glaucoma/
cataracts in the elderly, adrenal
insufficiency
Local Effects: oropharyngeal
candidiasis, dysphonia
Contraindications- viral TB, bacterial
respiratory infection,
Drug Interactions- CYP 3A4
inhibitors, grapefruit juice,
salmeterol.
Pregnancy Category:
Beclomethasone- (C)
Budesonide- (C/B)
Flunisolide- (C)
Fluticasone- (C)
Triamcinolone- (C)
**See Dosing Chart**
Dosage &
Administration Severe:
(Include renal
and/or hepatic
adjustments)
 Oral or systemic indicated; no
therapeutic advantage of either
 Full course continued until PF
reaches 80% or predicted.
 Systemic multiple daily dosing
more effective than high doses or
very high pulse dosing.
 4-12 hours for effects to be seen
Chronic: delivery method alters
comparable dose
 Mild- QD
 Most controlled with BID, less
toxicity
 Severe- multiple daily dosing, start
high then taper down
Sareh Seyedkazemi, PharmD Candidate 2007
University of Maryland School of Pharmacy
Adverse Effects: Cough and
wheezing
 Nedocromil only: bad taste
and headache
Contraindications: hypersensitivity;
acute asthma attack
Precautions: children <6 yo,
breastfeeding, cardiac arrythmias
Pregnancy Category:
cromolyn (B)
nedocromil (B)


Only effective by Inhalation!!!
Cromolyn- available MDI &
nebulizer
 Nedocromil- MDI only
Cromolyn:
 Nebulizer: >2 & adults
o Initial- 20 mg QID
 MDI: >5 -12 yo
o Initial: 2 inhalations QID
o Usual: 1-2 Inhalations 34 times per day
MDI: >12 yo
o Initial: 2 inhalations QID
o Usual:2-4 inhalations 3-4
times per day
Nedocromil:
>6 yo: 2 inhalations QID; ↓ when
stable (BID-TID)
Adverse Effects:
zileuton: elevated liver enzymes,
headache, pain, dyspepsia, nausea,
abdominal pain.
zafirlukast/montelukast:
Churg Strauss Syndrome; dizziness,
fatigue, fever, rash
Drug Interactions:
Zileuton- inhibitor of 1A2, warfarin,
theophylline, and propanolol.
Zafirlukast/montelukast- substrate of
2C19 and inhibitor of 2C9 mod, ASA
Pregnancy Category:
zafirlukast (B)
montelukast (B)
zileuton (C)
Contraindications: hypersensitivity.
Zileuton- LFT ≥3 x’s ULN
Precautions: safety and efficacy
unknown in children <5 yo,
chewable form of Singulair contains
phenylalanine. Females >65 yo at
greater risk of liver AE with
zileuton- caution with hx of liver
disease and/or alcohol abuse.
zileuton:
 ≥12 yo: 600mg QID
zafirlukast:
 5-11 yo: 10 mg BID
 >12 yo: 20 mg BID
 Hepatic: 50-60%↓
 1 hr before 2 hr after meals
montelukast:
 12-23 mo: 4 mg QHS
(granules)
 2-5 yo: 4mg QHS (granules
or chewable)
 6-14 yo: chew 5 mg/d QHS
 >15 yo: 10mg/d QHS
 No hepatic/renal
adjustments, severe hepatic
cases where not studied.
 Unlabeled use in acute
Adverse Effects: headache, injectionsite reaction, URI, sinusitis,
pharyngitis, viral infection,
Drug Interactions:
Pregnancy Category: (B)
Contraindications: hypersensitivity,
acute bronchospasm, status
asthmaticus.
Precautions: risk for parasitic
infections (helminth), Safety and
efficacy in children <12 yo not
established.

Administered SubQ

Dose determined by baseline
total serum IgE levels and body
weight

Range (150-375 mg)

2-4 week intervals

Consistent dose for duration of
therapy.
Pharmacotherapy Presentation – Pharmaceutical Care Rotation
Happy Harry’s Pharmacy Patient Care Center, Perryville, MD
Corticosteroids
Mast Cell Mediators
Leukotriene Modifiers
Monitoring
Efficacy: PFT, coughing, wheezing,
dyspnea, beta agonist use
Efficacy: PFT, coughing, wheezing,
dyspnea, beta agonist use
Efficacy: PFT, coughing, wheezing,
dyspnea, beta agonist use
(Efficacy and
Toxicity
Parameters)
Toxicity: difficulty/ change in voice
quality,
Toxicity: c/o change in taste, c/o
wheezing, cough.
Patient
Education
Use dose as directed. Do not stop
use abruptly.
Prime pump (if applicable)
Proper Use of inhalers
Rinse mouth with water after use
Wipe off mouth piece with dry tissue
Use as instructed. Do not
discontinue. Proper use.
Toxicity: symptoms of hepatic
injury (right upper quadrant pain,
nausea, fatigue, lethargy, pruritus,
jaundice, flu-like symptoms), LFT
(ALT/AST)
Take on empty stomach and do not
discontinue despite improvement.
Montelukast granules can be mixed
with food. Must be administered 15
min after opening package.
Cost
beclomethasone:
40 mcg (7.3gm) $60.84
80 mcg (7.3gm) $73.57
budesonide:
1 inhaler (104 gm) $148.12
flunisolide:
(7gm) $74.57
fluticasone:
triamcinolone
Pharmacotherapy, Dipiro 2005
Lexicomp-Online
cromolyn- 8.1gm $65.39 – 112 ACT
14.2gm $90.47- 200 ACT
(1-month)
References
nedocromil- 16.2 gm $71.62
zileuton- 600 mg (120)$92.99
Anti-IgE Antibodies
Efficacy: FEV1, Peak Flow, cough,
wheezing, dyspnea, NOT IgE
levels!!
Toxicity: # of headaches, signs and
symptoms of infection,
Proper use. Potential Adverse
Reaction response and reporting.
Reconstitution: SWFI 1.4 ml to
upright vial and swirl gently for 5-10
seconds every 5 minutes until
dissolved.
Storage: after reconstitution, lasts 8
hrs if refrigerated and 4 hrs if not
refrigerated.
Range $541- $2,706 depending on
the dosage.
zafirlukast- 10 mg (60) $80.50
20 mg (60) $74.99
montelukast- 4 mg (30) $91.14
5 mg (30) $89.99
10 mg (30) $89.99
See below
See below
See below**
(Guidelines,
Drug Info
Sources)
Kelly HW, Sorkness CA. Asthma. In: Dipiro JT, Talbert RL, Yee GC, Matzke GR, Wells BG, Posey LM, editors. Pharmacotherapy: A Pathophysiologic Approach 6 th Edition.
New York: McGraw-Hill Companies, Inc;2005. p. 503-35.
Lexi-Comp OnlineTM [database on the Internet]. Hudson (OH): Lexi-Comp. c1978-2006 [cited: 2006 July]. Lexi-Drugs. Available from: www.crlonline.com
** https://www.clevelandclinicmeded.com/medical_info/pharmacy/janfeb2004/omalizumab.htm
Sareh Seyedkazemi, PharmD Candidate 2007
University of Maryland School of Pharmacy
Pharmacotherapy Presentation – Pharmaceutical Care Rotation
Happy Harry’s Pharmacy Patient Care Center, Perryville, MD