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DRUGS

FOR ASTHMA

Controllers
Drug Class Generic Mode of Action Pharmakokineti Indications Contraindica Adverse Effects Strength and Clinical
Name c & interactions tions Preparation Considerations
Inhaled Fluticasone Inhibits prostaglandin Duration: 1012 hrs Maintenance Hypersensitivity Headache Aerosol: 44mcg/inh, The most effective anti-
corticosteroids synthesis, inhibits treatment of to any Pharyngitis 110mcg/inh inflammatory medications
accumulation of asthma as ingredient, for persistent asthma. ICS
Epistaxis
macrophages prophylactic including lactose Nasal spray: 50mcg/inh reduce symptoms, increase
Nasal burning lung function, improve
therapy in Powder for inhalation:
Cough quality of life, and reduce
patients 4 years 50mcg/inh, 100mcg/inh, the risk of exacerbations
of age and Oropharyngeal 250mcg/inh and asthma-related
above candidiasis
hospitalizations or death
Dysphonia
Minimal systemic Oropharyngeal candidiasis:
steroid toxicity Use of spacer with pMDI,
(eg, adrenal and rinsing with water and
suppression) spitting out after inhalation.

High doses increase the


risk of systemic side-
effects.

Leukotriene Montelukast Binds with cysteinyl Oral Duration: 12 Prophylaxis Aspirin and Headache Tablets: 10 mg Used as an option for
antagonists leukotriene receptors thus 24 hrs and chronic NSAID Cough controller therapy,
preventing their action Zileuton: treatment of sensitivity particularly in children.
Oral Duration: 12 Abdominal pain
with their enzyme asthma in Lactation
hrs Influenza Used alone: less effective
adults and
Dyspepsia than low dose ICS; added
children 12
Elevated liver to ICS: less effective than
months of age ICS/LABA.
and older function tests
with zileuton
and zafirlukast

Long acting B2 Salmeterol Selective for B2 Inhalation (aerosol) Long-term Lactation Palpitations Powder for inhalation: 50 Use of LABA without ICS in
agonist adrenergic receptors Duration: 1224 hrs maintenance Tachycardia mcg/inh asthma is associated with
located in the bronchi and treatment of Tremor increased risk of adverse
heart asthma or in outcomes.
Dizziness
the prevention
Vertigo
of
bronchospasm Nervousness
in patients 4 Cramps
years and older
Asthma
prophylaxis
(not for acute
relief)
Indacaterol for
COPD

Methylxantine Theophylline Stimulates CNS, directly Oral slow-release Prophylaxis Hypersensitivity Nausea Capsules: 50 mg, 75 mg, 100
relaxes the smooth Duration: 12 hrs and treatment to xanthine Vomiting mg, 125 mg, 200 mg, 300 mg,
muscles of the bronchi of bronchial Peptic ulcer Headache 400 mg
and pulmonary blood asthma Seizure disorder
Arrhythmias
vessels Nocturnal Hypotension
attacks Insomnia
CAD
Angina pectoris
IgE antibody Omalizumab Inhibits binding of IgE to Parenteral Adjunct in the Hypersensitivity Induration Powder for injection: 129.6 mg, A treatment option for
the high affinity IgE Administered as treatment of to the drug Headache 202.5 mg patients with severe
receptor on the surface of several courses of asthma persistent allergic asthma
injections Sore throat
mast cells and basophils uncontrolled

Extremely expensive

long-term toxicity not yet


well documented

Mast cell stabilizers Cromolyn Acts locally to inhibit the Prophylactic Hypersensitivity Cough Nasal solution: 5.2mg/inh Very limited role in long-
degranulation of and adjunct in to the drug Nasal congestion term treatment of asthma.
sensitized mast cells that the Mastocytosis in Pharyngeal Aerosol spray:
occurs after exposure to management infants irritation 800mcg/actuation Weak anti-inflammatory
certain antigens of bronchial Solution for inhalation: effect, less effective than
Wheezing
asthma 20mg/2ml low-dose ICS.







Relievers
Drug Class Generic Name Brand Mode of Action Pharmakokinetic Indications Contraind Adverse Strength and Clinical
Name & Interactions ications Effects Preparation Considerations
Short acting Salbutamol Ventolin Stimulates beta-2 Inhalation (aerosol) Prophylaxis and Children <12 Headache Inhalation aerosol: Excess use, or poor
beta 2 agonists receptors of the Duration: 24 h treatment of years old Nausea 90mcg/inh response indicate poor
bronchi leading to bronchospasm due to Lactation Vomiting asthma control.
bronchodilation reversible obstructive Inhalation
Palpitations
airway disease solution: 0.042%,
Tachycardia
0.083%, 0.5%,
Asthma acute attack Tremor 0.63mg/3ml,
relief drug of choice 1.25mg/3ml
Syrup: 2mg/5ml

Tablets: 2 mg, 4
mg

Terbuteline Brethine Specific beta-2 Prophylaxis and Lactation Palpitations Metered dose
receptor stimulant, treatment of Tremor inhaler: 0.2mg/inh
resulting in bronchospasm in Dizziness
bronchodilation and patients 12 years and Injection: 1mg/ml
Vertigo
relaxation of older Tablets: 2.5 mg, 5
Nervousness
peripheral vasculature mg
Tension
Nausea
Vomiting

Epinephrine Epinephrine EpiPen Causes marked Inhalation (aerosol, Temporary relief of Narrow angle Palpitation Aerosol: Asthma (obsolete)
stimulation of alpha, nebulizer) Duration: shortness of breath, glaucoma Tachycardia 0.2mg/inh
beta-1 and beta-2 12 hrs tightness of chest, and Aphakia PVCs
receptors, causing wheezing due to Lactation Autoinjector: 0.15
Dizziness
sympathomimetic bronchial asthma mg (0.15 ml), 0.3
Vertigo
stimulation, pressor mg (0.3 ml)
effects, cardiac Nervousness
stimulation, Headaches Injection: 1:200
bronchodilation, and Insomnia (5mg/ml), 1:1,000
decongestion Nausea (1mg/ml), 1:2,000
Vomiting (0.5mg/ml),
Sweating 1:10,000
Anorexia (0.1mg/ml)

Anticholinergic Ipratropium bromide Atrovent Antagonizes the Inhalation (aerosol) As a bronchodilator Narrow angle Dryness of Inhalation aerosol: Long-term use:
drugs action of Duration: several for maintenance glaucoma the mouth 17mcg/inh, ipratropium is a less
acetylcholine, prevents hours treatment of Prostatic or a bitter 18mcg/inh effective reliever
increase in bronchospasm hypertrophy taste. medication than
intracellular levels of associated with Bladder neck Headache Nasal spray: 0.03% SABAs.
cGMP COPD obstruction Dizziness (21mcg/spray),
Lactation Chest pain 0.06% Short-term use in
(42mcg/spray) acute asthma: inhaled
URTI
ipratropium added to
Nausea
Solution for SABA reduces the risk
Bronchitis inhalation: 0.02% of hospital admission
Coughing (500mcg/vial)
Dyspnea
Pharyngitis

Methylxanthine Theophylline Asmasolon Stimulates the CNS, Oral slow-release Prophylaxis and Hypersensiti Nausea Capsules: 50 mg,
directly relaxes the Duration: 12 hrs treatment of bronchial vity to any Vomiting 75 mg, 100 mg,
smooth muscles of the asthma xanthine Headache 125 mg, 200 mg,
bronchi and Peptic ulcer 300 mg, 400 mg
Arrhythmias
pulmonary blood Seizure
Insomnia
vessels disorder
Hypotension
CAD
Angina
pectoris

References:

Katzung & Trevors Pharmacology Examination and Board Review, 10th Edition

Katzung & Trevors Basic & Clinical Pharmacology, 11th Edition

GINA ASTHMA MANAGEMENT AND PREVENTION 2015

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