Respiratory Flashcards
Beta 2 adrenoceptor agonist names?
Epinephrine
Salbutamol SABA fast-acting
Formoterol LABA fast-acting
Salmeterol LABA slow-acting
ADR of beta 2 adrenoceptor agonists?
“Sympathomimetic effects from systemic absorption:
Tremor and muscle cramps
Peripheral vasodilation - flushing
Palpitations, tachycardia (beta-1 effects)
Hypokalemia / Hyperglycaemia - usually transient
Beta-2 adrenoceptor tolerance - relievers may not work during attacks “
Muscarinic receptor agonist names?
Ipratropium bromide SAMA
Tiotropium bromide LAMA
Use of Ipratropium and Tiotropium?
Adjunct to inhaled B2 agonists and inhaled glucocorticoids
Patients intolerant of B2 agonists
ADR of Ipratropium and Tiotropium?
Typical parasympatholytic effects - dry mouth, urinary retention etc.
Limited systemic ADR
Bad taste
Methylxanthine names?
Theophylline
Aminophylline
MOA of methylxanthines?
Inhibit Phosphodiesterases (PDEs)
Block adenosine receptors, preventing bronchoconstriction
Increase adrenaline release from adrenal medulla
CNS stimulant effect on respiration
Anti-inflammatory effects on mast cells and T cells
Lower microvascular leakiness”
Uses of methylxanthines?
Less effective than B2 agonists
Used as Adjunct for severe COPD
Not used clinically as anti-inflammatory drug”
ADR of methylxanthines?
GI: Nausea, vomiting, anorexia, discomfort
CNS: Nervousness, tremor, seizures, insomnia, anxiety
CVS: Arrhythmias
Many DDRs
Narrow therapeutic window (5-20mg/L)
Seizures in children only slightly above therapeutic range
Cysteine-Leukotriene (CysLT) receptor Antagonist name?
Montelukast
MOA of montelukast?
Relax airways in mild asthma
Effective in aspirin-sensitive asthma
Effective in exercise-induced asthma”
Use of Montelukast?
Adjunct therapy for mild to moderate asthma
About 1/3 as effective as salbutamol
Additive effects with B2-adrenoceptor agonist
Magnesium sulphate uses?
Adjunct treatment of severe acute asthma
Inhaled corticosteroids names?
Budesonide
Fluticasone
Ciclesonide
MOA of inhaled corticosteroids?
“Reduce pro-inflammatory mediators in airways: e.g. T cells, mast cells, eosinophils, PLA2, pro-inflammatory cytokines, COX2, 5-LOX, Inducible NO synthase, Lower shedding of epithelial cells, lower mucus secretion
Increase Anti-inflammatory mediators:
1. Annexin A2
2. B2 adrenoceptors
- Do not relax smooth muscle directly
- Possibly prevent airway wall remodeling
Uses of inhaled corticosteroids?
First line prophylactic for asthma
For nocturnal asthma
For advanced COPD with acute exacerbation or high eosinophilic content
High receptor binding affinity (low dose needed)
High lipophilicity
Lower need for B2 agonist
Lower risk of death from asthma
Lower airway hyper-responsiveness in 4-6 weeks”
ADR of inhaled corticosteroids
“1. Oropharyngeal Candidiasis - opportunistic infection due to localized immunosuppression
2. Dysphonia - due to localized muscle wasting
3. Cough / throat irritation
4. Adrenal suppression - fluticasone
5. Easy bruising (elderly)
6. Posterior subcapsular cataracts
7. Osteoporosis
- ADR rare if inhaled, due to limited systemic absorption”
Leukotriene pathway inhibitors names?
Montelukast
Zileuton
Uses of leukotriene pathway inhibitors?
“1. Prophylaxis and chronic treatment of asthma
2. Aspirin-induced/NSAID exacerbated asthma
3. Exercise-induced asthma
- Less effective than glucocorticoids
- Less frequent asthma attacks
- Lower use of inhaled steroids
- Lower use of B2 agonist
- Lower peripheral blood eosinophil levels”
ADR of leukotriene pathway inhibitors
“Side effects few and mild
- Headache
- GI disturbances
- Associated with Churg-Straus Syndrome (systemic vasculitis + eosinophilia)
- Withdrawal or reduce glucocorticoid stepwise
- Suicidial thoughts and neuropsychiatric ADR (rare)”
Cromoglicic acid name?
Cromolyn
MOA of Cromolyn?
“1. Lower mast cell degranulation by IgE-mediated FceRI crosslinking
2. Lower secretion of inflammatory mediators from eosinophils, neutrophils and macrophages
3. Control Chloride channels to inhibit cellular activation
4. Raise Annexin A1 secretion - inhibit prostaglandin and Leukotriene production from mast cells”
Uses of Cromolyn?
“1. Prophylactic control of asthma (inhalation only)
2. Prophylactic control of allergic rhinitis, allergic conjunctivitis, vernal keratoconjunctivitis
- Prevent Ag, cold, dry air and exercise-induced bronchospasm
- Single-dose before Ag-challenge or exercise prevents bronchospasm
- Low bronchial hyper-reactivity in 4 weeks
- Less need for bronchodilator therapy
- Less effective than inhaled glucocorticoids”
ADR of Cromolyn?
Throat and nasal irritation, mouth dryness, cough
Bad taste
Can mucolytics like acetylcysteine and carbocisteine be used for respi?
Yes.
PDE-4 inhibitor name?
Roflumilast
MOA of Roflumilast?
- Prevent breakdown of cAMP
- Less inflammatory cell activity (main)
- Inhibit fibrosis (main)
- Relax smooth muscle
ADR of Roflumilast?
- Headaches, Dizziness, insomnia
- Weight loss, diarrhoea, nausea, decreased appetite
- Anxiety, suicidal thoughts (rare)
- Caution in hepatic impairment
Anti-IgE monoclonal Ab name?
Omalizumab
Use of omalizumab - Anti IgE mAb?
For severe asthmatics with allergies and high IgE level
Name of Anti-IL5 / IL4 mAb?
Reslizumab
