Respiratory pharmacology Flashcards
What are the different types of bronchodilators?
- Adrenergic Agonists
- Beta-2 agonists (Salbutamol, Salmeterol, formoterol)
- Muscarinic antagonists/Anticholinergics (Tiotropium= long acting anti muscarinic (LAMA),
- Ipratropium-short acting anti muscarinic (SAMA)
- Methylxanthines (Aminophylline)
What are the different types of anti-inflammatory drugs for the airways?
Steroids (Prednisolone=oral, Beclomethasone= an inhaled corticosteroid ICS)
Leukotriene receptor antagonist
What are the different types of inhaled drug devices?
•Pressurised Metered Dose Inhalers (pMDIs)
- Use spacer/aerochamber
- HCFC-carbon footprint
•Dry-Powder Inhalers
How do you use pressurised Metered Dose Inhalers (pMDIs)?
Deep exhale /Inhale and puff/Hold breath for slow ten count/Exhale slowly/Wait one minute before second puff
How do you use Dry-Powder Inhalers?
Usually one inhalation, not a puff
What is the duration of salbutamol?
Short acting (begin immediately, 3-5 hour duration)
What are the possible routes of salbutamol?
- Inhaled or nebuliser (higher dose)
- Intravenous (IV)-very rarely used
What is the mechanism of action for salbutamol?
- Binding to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP
- Short acting beta agonist (SABA)
What is salbutamol used for?
Asthma and COPD
What is the duration of salmeterol?
Long acting (begin 2-30 min, 10-12 hour dur)
What is the route of salmeterol?
Inhaled
What is the mechanism of action for salmeterol?
Long-acting beta-adrenoceptor agonist (LABA)
What is salmeterol used for?
Asthma: in patients requiring long-term regular bronchodilator therapy on ICS
NOT PRN (not as needed) and always used with ICS in asthma
COPD: persistent symptoms despite SABA
(either LABA/LAMA combination or
ICS/LABA combination
FEV1 < 50%)
What is the duration of formoterol?
Long acting (with short onset similar to salbutamol but with prolonged duration 10-12 hours)
What is the route of formoterol?
Inhaled
What is the mechanism of action for formoterol?
•Long-acting beta-adrenoceptor agonist
What is formoterol used for?
- Asthma and COPD
- Combined with ICS (always) for asthma
What is the duration of tiotropium?
•Long acting (24 hour). Once daily.
What is the route for tiotropium?
Inhaled (Dry powder Handihaler/Mist respimat)
What is the mechanism of action for tiotropium?
- Tiotropium is a long-acting, muscarinic antagonist (LAMA)
- It has similar affinity to the subtypes of muscarinic receptors, M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3-receptors at the smooth muscle leading to bronchodilatation
What is tiotropium used for?
- Stable COPD: Symptoms despite SABA (any severity and with LABA)
- Asthma: in not improving despite ICS/LABA-specialist advice from hospital
What is ipatropium?
Mechanism of action
Duration
Route
Use
- Short acting antimuscarinic agent
- Onset 30 minutes; lasts 6 hours
- Nebulised
- Nebulised for acute presentations of COPD and sometimes asthma
What is the duration of theophylline?
•Duration :Half life around 5 hours healthy adults
What is the route of theophylline?
•Routes: Oral/Intravenous
What is the mechanism of action of theophylline?
- Phosphodiesterase inhibitor
- Requires monitoring of level (blood test)
What is theophylline used for?
- Oral: COPD and asthma –persistent symptoms
- Intravenous: COPD and asthma-medical emergencies
What adverse effects can bronchodilators cause?
- Tachycardia
- Nervousness, Irritability, Tremor
- Inhaled preparations: less common
- Oral preparations (hardly used) and intravenous: More side effects common
- Tachyarrhythmias/Angina
- Usually dose related
What are the effects of glucocorticoids on the airway?
- Decrease release of inflammatory mediator
- Decrease infiltration and action of white blood cells
- Decrease airway oedema
- Decrease airway mucus production
- Increase number and sensitivity of beta-2 receptors
What are the differences between inhaled and systemic glucocorticoids
Systemic -
- IV or oral
- Stronger effects as higher doses
- Action unaffected by inspiratory effort/inhaler technique
- More side effects, especially with long term therapy
Inhaled -
- Localized action
- Fewer side effects: some absorption occurs
- Disease may prevent penetration of drug to affected areas
Name an examples of a systemic glucocorticoid
Prenisolone
Name 3 examples of inhaled glucocorticoids
•e.g. Beclometasone, fluticasone, budesonide
What are the adverse effects caused by inhaled glucocorticoids?
- Oral candidiasis-white plaques in mouth
- Dysphonia
To avoid - gargle and use spacer
What are the general adverse effects of glucocorticoids?
- Adrenal suppression
- Bone loss: exercise, Vit D, calcium
- Slow growth in children, but not ultimate height
- Increase risk of cataracts and glaucoma
- Increased risk of infection
- Gastric ulceration
- Hypertension
- Diabetes
Mood disturbance
What are the types of combination inhalers?
ICS/LABA
- Formoterol/Budesonide
- Formoterol/beclomethasone
- Salmeterol/fluticasone
LAMA/LABA
•E.g Tiotropium/Olodaterol
How does the asthma treatment ladder work?
•You move up and down the ladder depending on symptoms and success of current drugs
Complete the diagram
Complete the diagram
Which medications are used for allergic rhinitis?
•Antihistamines
- H1 antagonists
- Side effects: Drowsiness, Dry Mouth, Dry Eyes, Confusion
- Intranasal Glucocorticoids
- Montelukast (Singulair)
- •Inhibit leukotriene receptors
- •↓inflammation, bronchoconstriction, oedema, mucus, recruitment of eosinophils
•Sympathomimetics (Decongestants)
Bronchitis and pneumonia are treated differently.
True or false
True
Bronchitis ≠ Pneumonia - different treatments!
Which penicillins are used to treat respiratory infections?
•Amoxicillin
- •moderate-spectrum, bacteriolytic, B lactam antibiotic
- •Routes - IV/Oral
- •Use – CAP (typical)/COPD exacerbations/bronchitis
- •Active against gram negative and gram positive bacteria
•Co-amoxiclav
- Amoxicillin is susceptible to degradation by B lactamase -producing bacteria so can be combined with clavulinic acid – a beta lactamase inhibitor
What are tetracyclines?
- Tetracycline inhibits protein synthesis
- Broad spectrum action Gram positive and negative
- Useful for ‘atypical infections’ e.g. mycoplasma, legionella
Oral route only
Side effects - GI Upset/staining teeth/lupus/allergy/photosensitivity
Name a tetracycline
Doxycycline
What are quinolones?
- Mechanism of action - DNA fragmentation
- Gram negative and positive coverage (And Pseudomonas)
- Route - IV/Oral/Inhaled (CF)
- Side effects – GI upset/ C difficile/ Tendonitis/Liver upset/Prolonged QTc and arrthymia
Name 3 quinolones
Ciprofloxacin,Levofloxacin, moxifloxacin
What are macrolides?
- Commonly used in respiratory infection (including aytpical pneumonia)
- Mechanism of action - Protein synthesis inhibitors
- Route- IV/PO
- Gram positive /limited gram negative cover
- Side effects- GI/allergy/liver abnormality/prolonged QTc and interactions
Name 2 macrolides
erythromycin, clarithromycin
What is the treatment for interstistial lung disease?
Some idiopathic interstitial pneumonias e.g. hypersensitivity pneumonia
•Prednisolone/Azathioprine/MMF
Sarcoid
•prednisolone
Idiopathic pulmonary fibrosis
•Pirfenidone,
Anti inflammatory/ Anti Fibrotic
Reduces fibroblast proliferation, reduces collagen production
Which disease is a multi disciplinary meeting important for therapeutic decision making?
ILD
