Block 2 Drugs Flashcards
Beta-2 adrenergic agonist (short-acting)
Salbutamol (short-acting)
Terbutaline (short-acting)
Beta-2 adrenergic agonist (long-acting)
Salmeterol (long-acting)
Formoterol (long-acting)
Beta-2 adrenergic agonist MoA
Stimulation of airway bronchiolar smooth muscle relaxation via adrenergic activation!
- Increases action of adenylate cyclase, increasing cAMP within cytoplasm
- cAMP activates Protein Kinase A - drives Ca2+ into storage vesicles away from cytoplasm
- Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction = bronchodilation
- Inactivation of MLCK also reduces smooth muscle contraction, promoting dilation of airway.
Beta-2 adrenergic agonist: Side Effects
Tremor
Tachycardia
Cardiac arrhythmia
Anti-muscarinic (short-acting)
Ipratropium (short-acting)
Anti-muscarinic (long-acting)
Tiotropium (long-acting)
Glycopyrronium (long-acting)
Anti-muscarinics MoA
Block M3 muscarinic receptors of cholinergic activity in airway smooth muscle = muscle relaxation
- Reduces phospholipasde C enzyme (PLC)
- Reduces IP3 generation and Ca2+ release into cytoplasm
- Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction = bronchodilation
Anti-muscarinics: Side Effects
Dry mouth
Urinary retention
Methylxanthine’s
Theophylline
Aminophylline
Methylxanthine’s MoA
Inhibit phosphodiesterase, increasing cellular cAMP = bronchodilation
Emergency only - need to monitor serum levels!
Methylxanthine’s: Side Effects
Cardiac arrhythmias
Seizures (can be fatal)
Glucocorticoid/Corticosteroid
Beclomethasone (inhaled)
Fluticasone (inhaled)
Prednisolone (oral)
Hydrocortisone (IV)
Glucocorticoid/Corticosteroid MoA
Activate glucocorticoid receptors in immune cells, reducing airway inflammation
(Prevent late phase effects of asthma)
- Cellular Targets: immune cells of the lungs macrophages/T-lymphocytes/eosinophils
- Molecular Target: Intracellular Glucocorticoid Receptor (GR) is TRANSCRIPTION FACTOR
- Activated GR interacts with selected DNA sequences and influences expression of genes
- Suppression of pro-inflammatory mediators e.g. TH2 cytokines such as IL-3, IL-5
- Expression of anti-inflammatory products e.g. SLPI
Glucocorticoid/Corticosteroid: Side Effects
Moon face
Increased abdominal fat
Osteoporosis
Leukotriene receptor antagonist
Montelukast
Zafirlukast
Leukotriene receptor antagonist MoA
Block proinflammatory leukotriene signalling - CysLT1 leukotriene receptor.
(Used as a preventer - prevent late phase effects of asthma)
Leukotriene receptor antagonist: Side Effects
Abdominal pain
Headache