Drug Classes used in Treatment of Asthma

Drug Class

Therapeutic effect
MAJOR DRUG CLASSES

β-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 β 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

The activated receptor regulates transcription of target genes. Termer.Blurred vision. which increases intracellular production of cyclic adenosine monophosphate cAMP. nervousness. 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. stomachache. Drowsiness. Paradoxical bronchospasm. palpitations. and nasal congestion. CHF. coughing. peptic ulcer. anticholinergics Trouble urination or not being able to urinate. 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. less commonly. wheezing. dizziness. Corticosteroids bind to glucocorticoid receptors on the cytoplasm of cells. blurred vision. tachycardia. dryness of throat Nausea. palpitation. Improved mucocillary clearance and reduced inflammatory cell mediator release. feeling nervous or excitable. careful monitoring is necessary in patients with diabetes hypertension. tired feeling. activating adenylyl cyclase. Anticholinergi cs Competitively inhibit binding of the neurotransmitter. and headache.Mechanism of Action and Adverse effects if anti-asthmatic Agents Drug Class Mechanism of Action Adverse Effects β-agonist Β2 agonists stimulate β2 receptors. 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 (FcεRI) Local side effects associated with inhaled corticosteroids include hoarseness and fungal infection (candidiasis) of mouth and throat. nasal congestion. headache. seizures Dry mouth. vomiting diarrhea. 1) Activation of cAMP results in bronchodilation. anorexia. depression & cataracts Flu-like symptoms. nervousness. joint or muscle pain. Headache. insomnia. Confusion. . acetylcholine. They are selective cyiestnyl leukotriene 1 receptor antagonist therefore they prevent leukotrienes from interacting with their receptors. nausea or vomiting. They target either muscarinic acetylcholine receptors or. Dizziness. Dry mouth.

Reduction in surface-bound IgE on FcεRI-bearing cells limits the degree of release of mediators of the allergic response. ear pain. . cold symptoms. hair loss. sore throat. injection site reactions (or leg or arm pain.on the surface of mast cells and basophils.

5 mg/dose q20min then prn DPI 12mg/cap for inhalation Nebulizer 0.r.30.025 mg/puff DPI 0. Maintenance: 40 mg orally every other day.i.d up to 1.100. 20 mg twice daily HFA 40 or 80 ug/puff DPI : 200ug/inhalation Oral tablet .i.220 ug/puff DPI: 50.i.25mg t.n 0.37 mg/puff SC (1ug/ml) 4-6 puffs every 20 min then prn 0.d p.2 mg/puff No recommendation MDI 0.Following table comprises drugs in each drug class used in treatment of asthma along with their dosage form and adult dose Drug class β 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.i. 110 .25mg MDI 0.63mg: 1.d q.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: 44.2mg/puff SC: 1ug/ml CFC 42 or 84 ug/puff 0.d 4-8 puffs q20 min upto 4 hour then prn No recommendation 2 puffs t.05 mg/inhalation MDI:0.63 mg t.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.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.

Tablet Omalizumab (XOLAIR®) SC injection 150 to 375 mg SC injection every 2 or 4 weeks.25 mcg/actuation) inhaled PO qDay 1 mg b.5 mcg) q12hr Inhaler 3-4 puffs t.4 mg/kg/hr.i.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. 2 ml ampule SR tablets 20 mg via nebulizer q.i. then PRN Tiotropium Inhaler Antihistaminic agents Anti IgE compounds Ketotifen (used as Syrup.i.5 mcg (2 actuations. 8 puffs q20min PRN for 3 doses 500 mcg q20min for 3 doses. 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.d q.d supportive therapy) (ZATOFEN®) . 1.d IV bolus IV maintenance Inhalation Nebulizer 10mg/kg/day Maximum to 800 mg/day 5mg/kg 0.d 2.i.d Nebulized Soln.