Drugs For Asthma

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Treatment / Management for Asthma:

β-agonists β-agonists Methylxanthines Anticholinergics Corticosteroids Mast cell stabilizers Leukotriene pathway inhibitors Anti-IgE
(short-acting) (long-acting) monoclonal
highly selective antibodies
Example Salbutamol, Salmeterol, fomoterol Theophyline (oral) IpratropiumIV: Hydrocortisone Sodium Leukotriene Leukotrien Omalizumab
terbutaline, fenoterol Aminophyline (IV) bromide, Oral: Prednisolone cromoglycate, receptor synthesis
tiotropium Inhaler:Budenoside, nedocromil antagonist: inhibitor:
Beclomethasone, Montelukast Zileuton
Mode of ~ Act at ß2 receptor on bronchial smooth ~ block adenosine receptor ~ competitively ~ anti-inflammatory (inhibit ~Inhibit mast cell ~ ↓ broncho- ~inhibit 5- ~Inhibit IgE
Action muscle (via cAMP) ~ inhibit phosphodiesterase (↑ inhibit Ach production of inflam degranulation constriction lipoxygenase binding to mast
~ prevent edema camp & cGMP-bronchodilation) muscarinic mediators (release of ~ ↓ inflammatory reversibly cell & other
~ prevent release of mediators from mast ~ prevent release of mediators receptor ~ contraction of engorged mediators) in the cell infiltration inflammatory
cells from mast cells ~ combine with ß- vessel in bronchial mucosa lungs cell
~↑mucociliary clearance agonist for better ~Inhibit IgE
~prevent edema efficacy synthesis
Main ~bronchodilation ~chronic treatment ~ bronchodilation ~bronchodilation ~prophylactic only ~for moderate ~for
function / ~prophylaxis before ~improve lung f(x) for acute ~ ↓ risk of death or mearly ~no effect on asthma prophylaxis &
Advantage exercise ~↓ asthma sx exacerbation pt death from asthma bronchospasm ~for prophylaxis maintanance
~treat nocturnal cough ~↓ use of short- ~for pt cant ~ ↓ hyper-responsiveness ~more in children & maintanance
Oral: acting drugs tolerate with ß- ~ inhaler: avoid adverse
~prevent premature ~↓ nocturnal cough agonist systemic effect
birth
~child X manipulates
inhaler
Method of Inhaler, nebulizer, oral inhaler Oral, IV Aerosol, IV, oral, inhaler (1 week to 10 inhaler Oral (1 or 2 hrs oral Subcutaneous
delivery nebulizer days) before meal) injection 2-4
weekly
Onset ~ Secs - 5mins delayed Fast (rapidly absorbed by GIT) Immediate
~ 30mins (oral)
Duration 2 – 6 hrs >12 hrs (high lipid prolong
solubility-slowly de-
tach from receptor)
Toxicity Convulsion
(narrow therapeutic window)
Side-effect Small dose: nausea, diarrhoea, ~Orophayngeal candidiasis ~GIT upset ~dyspepsia
tarchycardia ~impaired CHO metabolism ~headache ~liver toxicity
Big dose: hypotension, ~growth retardation ~↑Warfarin level ~ inhibit
~ inhibit cytochrome
hypokalaemia, seizures, cardiac ~suppress immunity
cytochrome P450 P450
dysrhythias ~psychiatric illness
~peptic ulcer ~cataract

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