Asthma and COPD Management Flashcards
Where are B2 adrenergic receptors generally located in the lungs?
- smooth muscle
- trachea down to terminal bronchioles
- ⬆️ noraadrenalin and adrenaline
What are the 5 different methods drugs can be given for asthma and COPD?
1 - inhaled (inhaler and nebuliser)
2 - oral
3 - intravenous
4 - intramuscular
5 - subcutaneous
What is the main benefit of use inhalers and nebulisers to deliver drugs to the lungs?
- direct deposition into the lungs
What is the main disadvantage of use inhalers and nebulisers to deliver drugs to the lungs?
- technique dependent
- disease can reduce drug accessing lungs
- 8-15% of drugs reaches lungs
What is the main benefit of taking asthma and COPD drugs orally?
- not technique dependent
What is the main disadvantage of taking asthma and COPD drugs orally?
- dependent on absorption in GIT
What are the 2 main benefits of taking asthma and COPD drugs intravenously?
1 - systemic effects
2 - not technique dependent
What are the main disadvantage of taking asthma and COPD drugs intravenously?
- ⬆️ risk of side effects
Are inhales and nebulisers fast acting?
- yes
- directly into lungs
Why are inhalers and nebulisers associated with low risk of side effects?
- majority of drugs remains in lungs
- small amount may enter circulation
Does the whole drug dose of the inhaler reach the lungs, even with the best technique?
- no
- aprox 8-15% reaches lungs
Do all inhalers have the same size particles in the aerosol?
- no
- small, medium and large particles
Why is it important to know the particle size of drugs delivered as inhalers or nebulisers?
- particle size affects where in the lungs drug reaches
How can we identify where in the lungs an inhaler or nebuliser reaches?
- lung specific radio-labelling
- radio-label appears on gamma camera
In addition to particle size, how does flow rate affect drug delivery in inhalers and nebbulisers?
- ⬇️ flow rate = poor drug delivery
- ⬆️ flow rate = good drug delivery
Do B2 agonists target adrenoreceptors or muscarinic receptors?
- adrenergic receptors
- Gas specifically
What is the basic pathway once an inhaler has bound to the Gas adrenergic receptor?
- adenylyl cyclase converts ATP to cAMP
- cyclic adenosine monophosphate (cAMP)
- cAMP activates protein kinase A (pKA)
- pKA activates intracellular phosphorylation
How does protein kinase A cause vasodilation and bronchodilation?
- ⬇️ intracellular Ca2+
In addition to bronchodilation, what are the other 2 things that inhalers are able to induce in the lungs that can cause problems in obstructive lung disease?
1 - ⬆️ mucous clearance
2 - ⬇️ vascular permeability
Why is ⬇️ permeability following the use of an inhaler a good thing?
- ⬇️ acute inflammation
What is the core drug used as a short term B2 agonist (SABA) for the treatment of asthma?
- salbutamol
- also known as ventolin
Salbutamol (ventolin) (SABA) is the core drug used as a short term B2 agonist for the treatment of asthma. What is another drug that can often be used?
- terbutaline - also known as terbutaline
What is the core drug used as a long term B2 agonist (LABA) for the treatment of asthma?
- salmeterol
Salmeterol is the core drug used as a long term B2 agonist (LABA) for the treatment of asthma. what is another drug that can often be used?
- formoterol
How quickly can the short acting Salbutamol (ventolin) (SABA) take its affects?
- generally <10 minutes
How long can the effects of the short acting Salbutamol (ventolin) (SABA) last?
- 3-5 hours - max dose several times/day
What are the 3 most common side effects from B2 adrenergic agonists (SABA)?
- tachycardia (B1 receptors in heart)
- termor (B2 in skeletal muscle)
- agitation
Would B2 adrenergic agonists used to treat asthma cause potential side effects on the sympathetic or para sympathetic nervous system?
- sympathetic - adrenergic are only in sympathetics system
Are there likely to be more side effects in inhalers or when B2 adrenergic agonist are given intravenously?
- intravenously - systemic distribution of drug
How quickly can the long acting Salmeterol (LABA) take its affects?
- usually within 30 minutes
How long can the long acting Salmeterol (LABA) affects last?
- 10-12 hours - max dose twice a day
How can the long acting Salmeterol (LABA) be administered?
- inhaler only
Can the long acting Salmeterol (LABA) be administered in isolation like Salbutamol (Ventolin)?
- no - ALWAYS administered with inhaled corticosteroids (ICS) and or LAMA
In addition to treating asthma, what can the combination of long acting Salmeterol (LABA) and inhaled corticosteroids (ICS) be used to treat?
- COPD - common treatment
What is the common core drug used as a short term muscarinic antagonist (SAMA) in the treatment of asthma and COPD?
- Ipratropium Bromide (SAMA) - also known as Atrovent
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA), which GPCR does it act on?
- M3 muscarinic receptors - Gaq (M1, M3 and M5 are Gaq)
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA), acting on the Gaq GPCR receptors, how does it cause bronchodilation?
- inhibits Ca2+ release - ⬇️ Ca2+ = brochodilation
What is the basic pathway for Gaq, which muscarinic antagonist act on?
- phospholipase C cleavea PiP2
- PiP2 cleaved into IP3 and DAG
- IP3 binds to sarcoplasmic retculum and ⬆️ Ca2+
- Ca2+ and DAG activate protein kinase C (pKC)
- pKC activates phosphorylation
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA), how long does it take to have an effect on the patient?
- 30 minutes
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA), how long do the effects last for?
- 6 hours - can be used up to 4/day
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA) generally used to treat asthma, but what other obstructive lung disease can it be used to treat?
- COPD - 20-40ug quantum dots (qds) nano carriers for drugs
If a patient has an acute exacerbation of asthma or COPD, why is Ipratropium Bromide (Atrovent), a short acting muscarinic antagonist (SAMA) given via a nebuliser?
- higher dosage of the drug delivered - 250-500ug quantum dots (qds) nano carriers for drugs
Do short term B2 adrenoreceptor agonist (SABA) or short term muscarinic antagonists (SAMA) have a larger bronchodilator effect?
- SABA - SABA and SAMA together are best
Ipratropium Bromide (Atrovent) is a short acting muscarinic antagonist (SAMA), in addition to bronchodilation, what else do they help with in obstructive lung diseases such as asthma and COPD?
- ⬇️ mucus production
Does Ipratropium Bromide (Atrovent), a short acting muscarinic antagonist (SAMA) influence the parasympathetic nervous system?
- minimal effects - muscarinic only in parasympathetic system
What is the common core drug used as a long term muscarinic antagonist (LAMA) in the treatment of asthma and COPD?
- Tiotropium
Tiotropium is a long acting muscarinic antagonist (LAMA), in addition to bronchodilation, what else do they help with in obstructive lung diseases such as asthma and COPD?
- ⬇️ bronchospasm - ⬇️ mucus production
Tiotropium is a long acting muscarinic antagonist (LAMA), how long does it generally last for?
- 12-24 hours - max 2/day
Tiotropium is a long acting muscarinic antagonist (LAMA), how is it administered?
- inhaler
What are some common side effects of long and short acting muscarinic antagomists?
- dry mouth - blurred vision - urinary retention - cardiac arrhythmia’s - dizziness - epistaxis (nose bleeds) - closed angle glaucoma (iris bulges forward)
What are corticosteroids?
- class of steroid hormones
Other than antibiotics, what is the most commonly prescribed drug for lung disease?
- corticosteroids
What is the main purpose for the use of corticosteroids in lung disease?
- anti-inflammation - they do have systemic effects
Where are corticosteroids receptors located in the body?
- on most cells in the body
How do corticosteroids induce their effects in the body?
- hormone so can cross plasma membrane
- binds to glucocorticoid receptor in cytoplasm
- receptor binds to nucleus and enters
- specifically binds to nucleotides
- ⬇️ inflammatory translation and transcription occur
- ⬇️ inflammatory protein translation
What is the most common corticosteroids prescribed orally to patients with lung disease?
- prednisolone