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Asthma Treatment

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Oscar Chak

on 11 December 2013

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Transcript of Asthma Treatment

Management of Asthma
Medications for asthma
Asthma Treatment
Metered dose Inhalers (MDIs)
Billy is currently on “Step 3”: Initial add-on therapy
Short acting β2 agonist
TWO puffs Use as directed
100 micrograms/metered inhalation

Seretide® 250 Inhaler
Indication: prophylaxis of asthma
Corticosteroid: fluticasone propionate
Long acting β2 agonist: salmeterol
ONE puff twice a day
fluticasone propionate 250 micrograms; salmeterol 25 micrograms/metered inhalation

UK/BTS guidance

Metered-dose inhaler
Drug Delivery

Shake canister vigorously for five seconds
Disperse the content evenly

Inhale when canister is pressed
Maximize the amount of drug inhaled

Take slow deep breath
Deeper penetration of drugs
Fast inhalation may lead to infections

Breath holding prior to exhalation
Increased sedimentation and diffusion of drugs

Failure to remove protective cap
Inhaler being used inverted
Failure to shake the canister
Failure to inhale slowly and deeply
Inadequate breath-holding
Poor inhalation/actuation synchronization
Problems in using inhalers

Self-management plan

Methylxanthine : bronchodilator
Narrow therapeutic range
Bronchodiation : 10-20mg/litre
Adverse effects : 10-20mg/litre
>20mg/litre -

Adverse effects include:
Nausea, vomitting, gastric irritation, convulsions, tachycardia
Metabolized by N-demethylation via CYP1A2

Medications for asthma

Comparison between the dose of a medication that causes the therapeutic effect and the dose that causes toxicity.
Therapeutic ratio = TD50/ED50.

Therapeutic Index

Theophylline has a very narrow therapeutic range.
Very small changes in doses can have drastic effects on the patient.
Theophylline has many interactions with other drugs.

Theophylline’s therapeutic index

Macrolide antibiotic
An alternative for penicillin-allergic patients
Metabolized by CYP 3A4


Naturally produced in the adrenal cortex of vertebrates
Involved in a wide range of physiological processes
Include immune response and regulation of inflammation

Used for treatment of reversible and irreversible airways disease

Medications for asthma

How do glucocorticoids
treat asthma?

Design of a glucocorticoid
Mechanism of glucocorticoid
treating asthma
Corticosteroid binds to
glucocorticoid receptors (GR)

Activated GR bind to coactivators and recruit histone deacetylases to the activated transcription complex

Switch off gene transcription

Inhaled corticosteroids (ICS) are the first line therapy for treatment of persistent asthma

Lipophilicity lung residence time
Slows dissolution in aqueous bronchial fluid
Longer duration of action

Pass through cell membrane more rapidly
Enhances a drug receptor’s binding affinity
Increase anti-inflammatory effect

Addition of lipophilic side chain to ICS increase lipophilicity
Example : Ciclesonide

Addition of an acetonide between C-16 and C-17 increases lipophilicity
Example : Triamcinolone acetonide

Lipid Conjugation
Allows ICS to retain longer in lung
Reversible via lipases
An ester bond is formed between the ICS and fatty acid in the pulmonary and airway tissues
Act as slow release reservoir

A hydroxyl group must be present at position 21 for lipid conjugation
Lipid conjugation
A hydroxyl group must be present at C-21 for lipid conjugation
Example : Desisobutyryl-ciclesonide (des – CIC)

Lipid Conjugation

On site activation
Activated in the lung tissue
Pulmonary esterase activate pro-drug

Reduce local side effects in the throat and oral cavity
Increase safety
Increase efficacy
On-site activation
Example : Ciclesonide

On-site Activation

Additional of double bond between C-1 and C-2 of cortisol in all synthetic corticosteroids
Example : Ciclesonide

Increase glucocorticoid activity

Additional fluorination at the C-9 position
Example : Fludrocortisone

Increase glucocorticoid activity

Involve in immune system to turn immune activity down
Anti-inflammation activity

Increase glucocorticoid activity

Increase glucocorticoid activities
Fluticasone propionate

Structurally altered
from cortisol
Synthetic trifluorinated glucocorticoid
Not an ester pro-drug
Log P=3.69

High affinity to the intracellular GC
Negligible side effects at normal therapeutic doses

Cytochrome P450 3A4 enzyme

Metabolite= inactive 17-beta-carboxlyic acid

5% of the oral dose is excreted in the urine

Renal clearance= less than 0.02% of the total clearance

Fluticasone Propionate Metabolism

Cardiovascular risk
Peptic ulcer
Adrenal insufficiency
Mood disorders

Adverse effects of corticosteroids.

Know when does asthma is in control and when it may become worse
What actions to take when their symptoms get worse
Recognise and know what to do in an asthma attack
Action plans improve health outcomes in adults with asthma
Group H3
British National Formulary 65 (2013)
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