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Drug Classes used in Treatment of Asthma

Drug Class

Therapeutic effect
MAJOR DRUG CLASSES

-agonist

These sympathomimetic agents relieve bronchoconstriction during


acute asthma exacerbations as well as during chronic therapy and
prevent exacerbations from occurring during exercise.
Corticosteroids suppress the inflammatory response and decrease
airway hyper responsiveness.
Newest agents with anti-inflammatory and bronchodilation activity.
They are categorized as 2nd line agents because less effective than
corticosteroids but useful in children for whom administration of
inhaled drugs is challenging. Useful in patients with concurrent allergic
rhinitis and asthma
Only available as nebulized solution. It is less effective in in its antiinflammatory properties than the inhaled steroids but is sometime still
used in children due to its excellent safety profile. when used
prophylactically it prevents early and late response of asthma and
when used as maintenance therapy of asthma, it suppresses
nonspecific airway reactivity
Theophylline compounds produce bronchodilation to a lesser extent
then agonist. Other effects include reduced mucus secretion,
enhanced mucocilliary transport, improved diaphragmatic
contractility, anti-inflammatory activity and possibly reduced
fatigability.
SUPPORTIVE THERAPEUTIC AGENTS
These drugs block postganglionic muscarinic receptors in the airways
resulting in bronchodilation.
They are useful for patients with coexisting allergic rhinitis
Useful in some patients because of its bronchodilation activity. It also
improves respiratory muscle strength
Used for severe asthma and concurrent allergies

Corticosteroids
Leukotriene
modifiers

Cromolyn

Theophylline
compounds
(methylxanthin
es)

Anti-cholinergic
Antihistamines
Magnesium
sulfate
Anti IgE
compounds
Immunotherapy

Improves asthma control in some patients by improving lung function,


reduce symptoms and decreased medication requirements in a
significant no. of patients while is renderd ineffective in others

Mechanism of Action and Adverse effects if anti-asthmatic Agents


Drug Class

Mechanism of Action

Adverse Effects

-agonist

2 agonists stimulate 2 receptors,


activating adenylyl cyclase, which
increases intracellular production of
cyclic adenosine monophosphate cAMP.
1) Activation of cAMP results in
bronchodilation. Improved mucocillary
clearance and reduced inflammatory
cell mediator release.
Corticosteroids bind to glucocorticoid
receptors on the cytoplasm of cells. The
activated receptor regulates
transcription of target genes. They
reduce inflammation via inhibition of
transcription and release of
inflammatory genes and increased
transcription of anti-inflammatory genes
that produce proteins that suppress the
inflammatory process.
They are selective cyiestnyl leukotriene
1 receptor antagonist therefore they
prevent leukotrienes from interacting
with their receptors.

Termer, palpitation,
tachycardia, nervousness,
and headache.

Corticosteroid
s

Leukotriene
modifier

Cromolyn

It acts locally by stabilizing mast cells


and thereby inhibiting mast cell
degranulation

Theophylline
compounds

Theophylline induced
phosphodiesterase inhibition results in
increased levels of cAMP.

Anticholinergi
cs

Competitively inhibit binding of the


neurotransmitter, acetylcholine. They
target either muscarinic acetylcholine
receptors or, less commonly, nicotinic
acetylcholine receptors
They compete with histamine for 1
receptor sites on effector cells and thus
help prevent the histamine mediated
responses that influence asthma

Antihistamine
s

Anti-IgE
compounds

Omalizumab inhibits the binding of IgE


to the high-affinity IgE receptor (FcRI)

Local side effects associated


with inhaled corticosteroids
include hoarseness and
fungal infection (candidiasis)
of mouth and throat, careful
monitoring is necessary in
patients with diabetes
hypertension, CHF, peptic
ulcer, depression &
cataracts
Flu-like symptoms, feeling
nervous or excitable,
headache, stomachache,
nausea or vomiting, and
nasal congestion.
Paradoxical bronchospasm,
wheezing, coughing, nasal
congestion, dryness of
throat
Nausea, vomiting diarrhea,
anorexia, palpitations,
insomnia, nervousness,
seizures
Dry mouth, blurred vision,
anticholinergics

Trouble urination or not


being able to urinate.Blurred
vision, Confusion, Dry
mouth, Drowsiness,
Dizziness.
Headache, tired feeling, joint
or muscle pain, dizziness,

on the surface of mast cells and


basophils. Reduction in surface-bound
IgE on FcRI-bearing cells limits the
degree of release of mediators of the
allergic response.

ear pain, hair loss, sore


throat, cold symptoms,
injection site reactions (or
leg or arm pain.

Following table comprises drugs in each drug class used in treatment of asthma
along with their dosage form and adult dose

Drug class
Agonist

Corticosteroi
ds

Drugs
Albuterol
(VENTOLIN)
Bitolterol
(TORNALATE)
Epinephrine
(Adrenalin
Chloride)
Formoterol
(ATIMOS)
Levalbuterol
(XOPENEX)
Pirbuterol
(MAXAIR)
Salmeterol
(SEREVENT)
Terbutaline
(BRITANYL)
Beclomethasone
(CLIPPER)
Budesonide
(PULMICORT)
Flunisolide
(NASALIDE)
Fluticasone
(FLIXOTIDE)
Mometasone
(NASONEX)
Triamcinolone
(ARISTOCORT)
Methylprednisolo
ne (SOLU
MEDROL)
Prednisone
(DELTASONE)

Leukotriene

Zafirlukast

Dosage Form

Dose

Nebulizer (5 ug/ml)
MDI 0.09m/puff
Oral 4mg SR
Nebulizer (2mg/ml)

10-15mg/hr continuously
4-8 puffs q20 mins then prn
No recommendation
10-15mg/hr

MDI 0.37 mg/puff


SC (1ug/ml)

4-6 puffs every 20 min then prn


0.30.5 mg/dose q20min then prn

DPI 12mg/cap for


inhalation
Nebulizer 0.63mg:
1.25mg
MDI 0.2 mg/puff

No recommendation

MDI 0.025 mg/puff


DPI 0.05 mg/inhalation
MDI:0.2mg/puff
SC: 1ug/ml
CFC 42 or 84 ug/puff

0.63 mg t.i.d up to 1.25mg t.i.d


4-8 puffs q20 min upto 4 hour then
prn
No recommendation
2 puffs t.i.d q.i.d p.r.n
0.25mg q20 min 3 doses
L: 168-504
ug
L: 80-240
ug
L:200-600
ug

M: 504-840
ug
M: 250-480
ug
M:600-1200
ug

H: >840
ug
H: >480
ug
H: >1200
ug

MDI 250 ug/puff

L: 5001000ug

M:10002000ug

H: >
2000ug

MDI: 44. 110 ,220


ug/puff
DPI: 50.100,250
ug/inhalation
DPI: 200 ug/inhalation

L: 88-264
ug
L: 100-300
ug
L: 200 ug

M: 264-660
ug
M: 300-600
ug
M: 400 ug

H: >660
ug
H: >760
ug
H: >400
ug

MDI 100 ug/puff

L: 400-1000
ug

M: 10002000ug

H: >2000
ug

Intravenous

60-80 mg in 3 or 4 divided doses for


48 hours

Oral tablet

Acute: 40 mg orally every 12


hours.
Maintenance: 40 mg orally every
other day.
20 mg twice daily

HFA 40 or 80 ug/puff
DPI : 200ug/inhalation

Oral tablet

Modifiers

Cromolyn
Methylxanth
ine
Anticholinergic
agents

(ZUKAST)
Montelukast
(MONTEGET)
Zileuton
(ZYFLO)
Cromolyn
(INTAL)
Theophylline
(RESPRO SR)
Ipratropium (used
with short acting
beta agonist)
(ATEM)

Oral tablet

10 mg once daily

Oral tablet

400 mg q.i.d

Nebulized Soln. 2 ml
ampule
SR tablets

20 mg via nebulizer q.i.d

IV bolus
IV maintenance
Inhalation
Nebulizer

10mg/kg/day Maximum to 800


mg/day
5mg/kg
0.4 mg/kg/hr.
8 puffs q20min PRN for 3 doses
500 mcg q20min for 3 doses, then
PRN

Tiotropium

Inhaler

Antihistaminic
agents
Anti IgE
compounds

Ketotifen (used as

Syrup, Tablet

Omalizumab
(XOLAIR)

SC injection

150 to 375 mg SC injection every 2


or 4 weeks.

Combinition
inhalers

salmeterol/flutica
sone (SERETIDE
)
budesonide/form
oterol
(COMBIVAIR)
Salbutamol/
Beclomethasone
(VENTIDE)

inhaled powder
Inhaled aerosol

1 puffs q12hr
2 puffs q12hr

Inhaler

160 mcg/9 mcg (2 puffs of 80


mcg/4.5 mcg) q12hr

Inhaler

3-4 puffs t.i.d q.i.d

2.5 mcg (2 actuations; 1.25


mcg/actuation) inhaled PO qDay
1 mg b.i.d

supportive therapy)
(ZATOFEN)

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