Pulmonary Flashcards
Beta 2 agonist
Bronchodilator
Mechanism
- stimulation of B2 receptors
- increase cAMP
- smooth muscle relaxation, mast cell stabilization and skeletal muscle stimulation
Drugs
- SABA: albuterol, levalbuterol, terbuatline
- LABA: formoterol, salmeterol, indacaterol, vilanterol
Use:
- SABA: acute asthma exacerbation, exercise induced asthma, acute COPD exacerbation
- LABA: maintenance therapy for prevention of bronchospasm in asthma in conjunction with inhaled corticosteroids, maintenance therapy for prevention of bronchospasm in COPD
Side effects:
- tachycardia/palpitations
- decrease in serum K
- tremors
- lactic acidosis
Leukotriene modifiers
Anti-inflammatory
Mechanism:
- LT antagonists: bind to leukotriene receptor
- 5-lipoxygenase inhibitors: arachidonic acid not converted to leukotrienes
Use:
- long term control and prevention of symptoms in mild/persistent asthma
- allergic rhinitis
Drugs:
- leukotriene receptor antagonist: zafirlukast, montelukast
- 5-lipoxygenase inhibitor: zileuton
Side effects:
- LT antagonist: headache, nausea, abdominal pain
- 5-LO inhibitor: liver toxicity, hyperbilirubinemia
Anticholinergic
Bronchodilator
Mechanism:
- inhibit muscarinic receptors in bronchial smooth muscles M1 and M3
- block acetylcholine, decrease cGMP, lead to bronchodilation
Drugs:
- short acting: ipratropium
- long acting: tiotropium, aclidinium, umeclidinium
Use:
- short acting: acute asthma exacerbation, acute COPD exacerbation, maintenance tx of bronchospasm associated with COPD
- long acting: maintenance tx of bronchospasm associated with COPD
Side effects:
- blurred vision
- dry mouth
- urinary retention
- nausea
- CNS
- tachycardia
- increased cardiovascular events
Methylxanthines
Bronchodilator Mechanism: - non-selective inhibition of phosphodiesterase, increase cAMP, bronchodilation - inflammatory cell regulation - anti-inflammatory effects Use: - acute exacerbatio of asthma - tx of symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung disease (COPD) Drugs: - theophylline, aminophylline Side effects: - nausea, vomit - gastric upset - tachyarrhythmias - seizures - jitteriness, insomnia, headache
Corticosteroids
Anti-inflammatory Mechanism: - binds glucocorticoid receptor in cell, translocates to nucleus, activates transcription of anti-inflammatory genes and other genes Effects: - reduce inflammatory cell activation, recruitment and infiltration - decrease vascular permeability Use: - inflammatory conditions, acute exacerbation of asthma and COPD, maintenance therapy to prevent bronchospasms and symptoms of asthma, maintenance to prevent bronchospasms of COPD, allergic rhinitis Drugs: - hydrocortisone - prednisone - methylprednisolone - dexamethasone Side effects: - HPA suppression, impaired wound healing, growth retardation in kids, osteoporosis, pancreatitis, psychiatric disturbances, glaucoma - hyperglycemia, HTN, hypoK - oral thrush, hoarseness
Cromolyn/nedocromil
Anti-inflammatory
Mechanism:
- mast cell stabilizers, inhibit mast cell degranulation
- inhibit activation and release of mediators from eosinophils and epithelial cells
- inhibit neurally mediated bronchoconstriction
Use:
- long term for prevention of symptoms of asthma
- preventative tx prior to exposure to exercise or known allergen
Side effects:
- cough and wheeze
- bad taste with nedocromil
Mepolizumab
Mechanism: - target IL-5, eosinophils not recruited Use: - add on maintenance therapy for pts with eosinophilic asthma not well controlled with other therapies Precautions: - herpes zoster - parasitic infxn Side effects: - hypersensitivity rxn/anaphylaxis - injection site rxn - headache - myalgias
Omalizumab
Mechanism: - binds to Fc of IgE - prevents activation of mast cells Use: - Tx of allergic asthma not well controlled with use of corticosteroids - dosage depnds on pts baseline IgE Side effects: - anaphylaxis
Anti-histamines
Mechanism
- competitive antagonist to H1 receptors
- first gen: lipophilic and non-selective; anticholinergic and CNS effects
- second gen: less CNS effects; specific to peripheral histamine receptor
Use:
- allergic rxns, allergic rhinitis
- first gen: anti-emetic
Drugs:
- first gen: diphenhydramine, chlorpheneramine, hydroxyzine
- second gen: cetirizine, levocitirizine, loratidine, fexofenadine, desloratidine
Opioids
Anti-tussive Mechanism: - acts centrally on respiratory center in medulla and nucleus tractus solitaris to increase cough threshold Use: - supression of cough caused by chemical or mechanical respiratory tract irritation Drugs: - codeine, hydrocodone, hydromorphone Side effects: - nausea, vomit - sedation - constipation
Dextromethorphan
Anti-tussive
Mechanism:
- acts centrally on respiratory center in medulla and nucleus tractus solitaris to increase cough threshold
Use:
- suppress cough associated with common cold or allergy
Side effects
- CNS at high doses - confusion, excitation, nervousness, irritability
- respiratory depression at high doses
- can’t take with MAO-I
Benzonatate
Anti-tussive
Mechanism:
- anesthetic effect on the stretch receptors of the vagal afferent fibers in the bronchi, alveoli and pleura
- blocks cough reflex
Use:
- suppress cough associated with common cold, bronchitis
Side effects:
- nausea
- mucosal numbness associated with breaking capsule
Guaifenesin
Expectorant Mechanism: - loosens and thins lower respiratory secretions Use: - symptomatic relief of ineffective productive coughs Side effects: - nausea, vomit - dizziness - diarrhea - due to formulation
Pirefenidone
Antifibrotic Mechanism: - inhibits growth factors and inflammatory factors like TNFa and IL-IB - reduces fibrosis through TGF- B Use: - idiopathic pulmonary fibrosis Side effects: - skin rash - photosensitivity - nausea/vomit - liver toxicity - drug interactions: cyp1A2
Nintedanib
Antifibrotic Mechanism: - tyrosine kinase inhibitor - inhibits PDGF and FGF - slows fibrosis Use: - idiopathic pulmonary fibrosis Side effects: - GI - diarrhea, nausea/vomit, abdominal pain - increased liver enzymes - MI - increased bleeding - drug interactions: cyp3A4, P-glycoprotein
