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28 Cards in this Set

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What happens when an asthmatic inhales an antigen?

histamine, prosaglandins, leukotienes and cytokines are released


This causes broncho constriction, oedema, mucus secretion and inflammation

what drugs are used in the treatment of asthma?

Bronchodilators and antinflammatory agents

What drugs are used as bronchodilators?

Beta 2 agonists and muscarinic antagonists

What are some examples of anti-inflamatory agents?

Glucocorticosteriods


Xanthies


Cromones


Leukotriene antagonists


Anti IgE

Current drugs used for treatment of symptoms?

Short acting beta 2 agonists (SABA)


Long acting beta 2 agonists (LABA)


Thephylline



What are some examples of SABA and LABA drugs?

SABA= salbutamol, terbutalin enad fenoteral


LABA= salmeterol, formoterol and indacaterol

Mechanism of action of beta agonists

1)binds to receptor which activates adenyl cyclase to create cAMP from ATP


2) cAMP causes PKA to phosphorylate MICK which causes relaxation of smooth muscle of airways


3) cAMP is converted to AMP by phosphodiesterase (PDE)

Beta 2 agonists summary

Causes smooth muscle relaxation and mast cell degranulation


Administered via inhaled route


Side effects= tremor, increased HR and hypokalemia

What do muscarinic antagonists do?

Prevents smooth muscle contraction and mucus secretion induced by activation of PNS

Examples of muscarinic antagonists

ipratropium bromide


titotropium bromide

What are muscarinic anragonists mainly used to treat?

COPD

Side effects of muscarinic antagonists

dry mouth, urinary retention, constipation and acute angle glaucoma

What is the current anti inflamatory therapy?

glucocorticosteriods

Examples of glucocorticosteriods and method of administration

theophylline (oral)


Leukotriene receptor antagonists (oral)


Anti-IgE: Omalizumab (subcutanous)


Cromones: Sodium cromoglycate (inhaled)

How do glucocorticosteriods work in asthma?

1) enters cytosol via plasma mem and binds to heat shock protein 90 (HSP90)


2) HSP90 transports steriod into nucleus and binds to gene where it either activates or inhibits transcription which causes:


-inhibits leukotriene and cytokine synthesis/release


-inhibit recruit of inflammatory cells


-antioedema


-increased beta 2 adrenoreceptor function

Role of inhaled corticosteroids in asthma therapy

Prevents infiltration adn activation of inflammatory cells


Reduces mucosal oedema


improves airflow and hence lung function


decreases airway hyper-responsiveness


reduces symptoms


reduce frequency and severity of exacerbations


improve quality of life



side effects of inhaled glucocorticosteriods

oral candidasis


hoarseness, cough and voice problems

Side effects of oral or prolonged high dose of glucocorticosteroids

growth retardation


suppression of hypothalmic pituatory axis


osteoperosis, water retention, diabeties


hypertension, weight gain and occular hypertension

What does leukotriene cause?

bronchoconstriction


oedema


cellular infiltration


mucus production

Example of leukotriene antagonist

moteolukast

Use of leukotriene antagonist

greatest benefit in severe asthma


once per day


useful for aspirin sensitive and exercise inuced asthma



Side effects of leukotriene antagonists

headache and GI disturbance

What do xanthines do?

Inhibit PDE so cAMP is not broken down

Examples of xanthines

theophyline and aminophyline

side effects of xanthines

nausea


vommitting


arrythmias


hypokalemia

Examples of cromones

sodium cromoglicate


nedocrimil sodium

What do cromones do?

stabilize mast cells


reduce inflammatory cell activation and recruitment


less effective than glucocorticosteriods

Use of Omalizumbs

binds to free IgE


only used in moderate to severe asthma where glucocorticosteriods dont work


must be given as subcutaneous injection