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Pharmacology Approach to bronchial asthma treatment

Drug Sympathomimetic Route of Administration -Non selective epinephrine injection -Inhaled Short Acting B2 Agonist (SABA) -Inhaled Long Acting B2 Agonist (LABA) -Oral LABA Mechanisms Epinephrine -Relieve bronchospasm SABA (salbutamol, terbutaline, levalbuterol, pirbuterol) -Treat acute symptoms of bronchospasm -Prevent exercise-induced asthma (EIB) -Relax air way smooth muscle, increase air flow LABA (salmeterol, formoterol) -Bronchodilator at least 12hrs -Formoterol has an onset action similar to SABA (5mnts) due to lower lipophilicity than salmeterol (15mnts) -Used in combination with ICS for long term control and prevent moderate or severe persistent asthma symptoms due to synergistic anti inflammatory effects -Prevent EIB and nocturnal asthma Oral LABA (salbutamol, terbutaline, bambiterol) -Taken every 12hrs Atropine -Inhibit muscarinic cholinergic receptors -Reduce intrinsic vagal tone Adverse Effects Epinephrine -Systemic side effects (tachycardia, hypertension, hypergycemia, hypokalemia) SABA -Cardiac arrhythmia and MI especially elder or pre exesting CVS diseases patients or when combined with theophylline -Headache -Tremors -Hypokalemia -Tachyphylaxis Preferred/Not Epinephrine -Generally not preferred LABA -Not be used as monotherapy in long term control as may disguise poorly controlled persistent asthma -Treatment of acute and exacerbation is not preferred Oral LABA -Have no international guideline for management of bronchial asthma

Anti Muscarinic

-Injected atropine -Inhaled ipratropium bromide -Inhaled tiotropium bromide

Atropine -Dryness of secretion -Systemic side effects (tachycardia, blurring of vision, glaucoma, urine

Atropine -Not suitable Ipratropium bromide

Created by Qosru Iskandariah

retention Ipratropium bromide (short acting) -Low bioavailability decreases side effects -Provide additive effects to SABA in moderate-severe asthma exacerbation -Alternative bronchodilator for COPD patient who cannt tolerate SABA -Treatment of acute COPD Tiotropium bromide (long acting) -Treat COPD -Treat nocturnal asthma Aminophylline -Treat asthma exacerbation Oral theophylline -Alternative mild-moderate bronchodilator -Mild anti inflammatory effects -Produces a low plasma level over a prolonged period -Treat nocturnal asthma -Treat COPD

-Not approved effectiveness in long term management of asthma Tiotropium bromide -Not been studied in long term asthma management -Not approved in asthma treatment

Methylxanthine

-Injected short acting theophylline (aminophylline) -Oral sustained release theophylline

Oral theophylline -If plasma level above 20g/ml: 1) Headache 2)Insomnia 3) Convulsion 4) Tachycardia 5) Arrhythmia 6) Hypotension 7) Vomiting and nausea -If rapid injection, may cause CNS and cardiac effects -In case of liver disease, heart failure, concomitant use with erythromycin, ciprofloxacin or contraceptive pills, may increase its plasma level -In case of febrile illness, pregnancy or concomitant use with anti TB drugs may decrease its plasma level

-As alternative, not preferred

Created by Qosru Iskandariah

Magnesium Sulphate

-IV -Inhalation

IV -Add-on therapy with other anti asthmatic drug to decrease hospitalization rate in severe asthma Inhaled -Administrated with nobulized salbutamol as bronchodilator in asthma exacerbation Systemic steroids -Suppress, control and reverse airway -Treat severe asthma and poorly controlled asthma by other drugs -Prevent progression, speed up recovery, prevent relapses Inhaled steroids (beclomethasone dipropionate, fluticasone, budesonide, ciclesonide) -Most effective long term therapy of mild-severe persistent asthma -Do not have the same bioavailability as systemic steroids, so low side effects

-Cardiac arrest

Glucocorticoids

-Injected systemic steroids -Inhaled steroids

Systemic steroids -Adrenal suppression -Growth suppression -Dermal thinning -Hypertension -Cushings syndrome -Cataracts -Muscle weakness -Delayed type hypersensitivity loss -Reactivation of latent TB infection -Increase the risk of infection Inhaled steroids -Hoarseness voice -Oropharyngeal candidiasis -Dermal thinning -Increase ease in skin bruising -High doses have higher potential for linear growth suppression in children

-Most effective for long term therapy

Cromones

-Inhalation

-Block chloride channels -Modulate mast cells mediator release and eosinophil recruitment -Inhibit local axon reflex on bronchial tree -Treat mild persistent asthma -Prevent exercise-induced asthma or any allergen-induced -Protect against asthma

-Alternative, but not preferred for mild persistent asthma -Insufficient evidence to prove beneficial effect on maintenance treatment of childhood asthma

Created by Qosru Iskandariah

Anti leukotrienes (Leukotriene modifiers)

exacerbation leading to hospitalization -Less effective than ICS Zileuton -Inhibit lipooxygenase enzyme -Prevent bronchoconstriction during exercise and aspirinsensitive individu Leukotriene receptor antagonists (LTRA) -Same as zileuton Omalizumab -A recombinant DNA-derived humanized monoclonal antibody to Fc portion of IgE antibody to prevent binding of IgE to mast cells and basophils, leading to decreased release of mediator in response to allergen -Treat allergic and severe persistent asthma that inadequately controlled by combination of high dose of ICS and LABA -Treat allergic rhinitis

Zileuton -Hepatotoxicity -Cytochrome P450 enzyme inhibitor (inhibit metabolism of warfarin and theophylline, so less desirable than LTRA) LTRA -Same as zileuton -Urticaria -Anaphylaxis -Injected site pain and bruising -Malignancies

Immunomodulators

-Injection

Created by Qosru Iskandariah