asthma & COPD Flashcards
Short Acting Beta2 Agonists (SABA) Agents
Albuterol
Levalbuterol
SABA
- MOA: Stimulate adenylyl cyclase at beta2 receptor –> increase cAMP in bronchial smooth muscle –> bronchodilation
- Selective for beta2 receptor
- DOC for ACUTE ASTHMA ATTACKS and exercise induced asthma
- Onset: 5 min
- Duration: 3-4hr
- Given (almost) exclusively via inhalation
SABA ADE
- Well tolerated with PRN use: (as needed)
Mouth irritation, cough - ADE at high doses: Skeletal muscle tremor, atachycardia/palpitation, arrhythmia, tolerance with exercise use (decreased responsiveness and decrease in number of beta receptors)
Long Acting Beta2 Agonist (LABA) Agents
Long acting - Salmeterol - Formoterol Ultra-Long acting - Indacterol - Olodaterol - Vilanterol (in combo with ICS)
LABA
- MOA: Stimulate adenylyl cyclase at beta2 receptor –> increase cAMP in bronchial smooth muscle –> bronchodilation
- Slower onset of action (~30 min)
- Longer duration of action (12-24hrs)
- NOT for rescue therapy
- CANNOT be used as monotherapy in asthma
- OK in COPD
LABA ADE
- Well tolerated with PRN use: (as needed)
Mouth irritation, cough - ADE at high doses: Skeletal muscle tremor, atachycardia/palpitation, arrhythmia, tolerance with exercise use (decreased responsiveness and decrease in number of beta receptors)
Antimuscarinic Agents
Short Acting - Ipratropium Long Acting - Tiotropium - Aclidinium - Umeclidinium - Glycoprolate
Antimuscarinic
- MOA: competitively block muscarinic receptors (M1, M2, M3) and the effects of ACh in airway –> prevent vasoconstriction mediated by vagal discharge
- No effects on chronic inflammation
- bronchodilating effects last longer than Beta agonists
Antimuscarinic ADE
- Minimally absorbed, generally well tolerated
- Potential for: dry mouth, dry eyes, bitter/metallic taste, constipation, urinary retention
- NO Tremors or Arrhythmia
Methylxanthine derivative agents
theophylline - oral
Methylxanthine derivative
MOA: (1) non-selectively inhibits phosphodiesterase (PDE) –> Increases cAMP –> bronchodilatuon (2) Block adenosine receptors in CNS (inhibits bronchoconstriction)
- Available PO in IR and SR formulations
- Duration of action ~ 12hrs
- Requires high concentration to be effective
- Considered narrow therapeutic index drug
Theophylline
Metabolized via CYP450 1A2 enzyme system
- MANY drug-drug interactions – febuxostat, bupropion, carbamazepine, macrolide antibiotics, etc.
Clearance mediated by age, smoking status and other drugs
- Younger patients clear drug faster vs. elders
- Smokers clear the drug faster vs. non-smokers
Requires therapeutic monitoring
- Therapeutic range 10-20 mcg/mL
- Levels correlate with efficacy
Theophylline ADE:
- GI distress (enhanced gastric acid secretion)
- Tremor
- Insomnia
- In overdose, severe nausea and vomiting, hypotension, agitation, arrhythmia, cardiac arrest, seizures
PDE-4 Inhibitor Agents
Roflumilast - Oral
PDE-4 Inhibitor
MOA: not fully elucidated; electively inhibits PDE-4 –> increases cAMP –> bronchodilation
- Used for severe or very severe COPD (should be given in combo with at least one LAMA or LABA for COPD)
- Given by mouth once daily (duration of action >10-20 hrs)
Roflumilast
- Partially metabolized by CYP3A4 DDI with rifampin, phenobarbital, phenytoin, carbamazepine
- ADE: diarrhea, nausea, vomiting, abdominal pain, headache, dyspepsia, psychiatric events, weight loss