Respiratory Drugs Flashcards
Tiotropium
Class: Synthetic, inhaled muscarinic receptor blocker
MOA: blocks the ability of acetylcholine to bind to and stimulate muscarinic receptors in the respiratory tract, thus leading to bronchodilatation
Indications: bronchospasm in chronic bronchitis and emphysema; bronchospasm in asthma; rhinorrhea in allergic rhinitis or with common cold
PK: much of an inhaled dose is actually swallowed (only 10% gets to lungs); not well absorbed from the resp tract; drug is metabolized in liver, or excreted unchanged in feces
Duration: 6-8 hours
Contraindications and ADRs: avoid in patients with problems with atropine or similar drugs; use cautiously in patients with angle-closure glaucoma, BPH, bladder neck obstruction;
ADRs include bitter taste, blurred vision, dry moiuth, nausea, bronchospasm (perhaps from propellant)
Other facts: close relative is tiotropium (Spiriva™)
Dose: for bronchospasm, usual dose is 2 puffs (36 mcg per puff) qid not to exceed 12 puffs per 24h
Salmeterol
Description: synthetic selective β2 (β2>>β1) receptor agonist (with relatively little β1 stimulation at normal doses) •
Actions: Potent agonist at β2 receptors on smooth muscle cells in airways (e.g. bronchioles) • increased mucociliary clearance, decrease vascular permeability, decrease mediator release
Metabolism: COMT/MAO,
Pharmacokinetics: F 15-75, 1/2 life is 6-8 hours. only 8-15% reaches systemic circulation
Pharmacodynamics: duration is 12 hours
Indications: • Prompt-acting rescue inhaler for asthma, COPD (bronchodilator) • Inhibit premature labor (relaxes smooth muscle cells in uterus as well) •
Other facts: • Most often given as MDI (metered dose inhaler) • Can be given via nebulizer • Rarely given any more as iv infusion • Side effects include CVS: tachycardia, palpitations, tremor, angina, arrhythmias, vasodilate pulm arterioles CNS: anxiety, headache and tremor. Metabolic- hypokalemia, hyperglycemia can develop tolerance.
diphenhydramine
H1 inhibitor
mechanism: competitive inhibtor of H1 receptor (histamine release)
indications: allergic rhintis
PK- oral, hepatic metabolism, gets to CNS
ADRs: sedation, headache, constipation, prolonged QT interval
disodium cromoglycate
unknown MOA- decreases chloride channels and Ca flux, decreases eosinophil cytokine release
indications: allergic rihintis
ADRS. nasal stinging, headache, nausea
Albuterol
Description: synthetic selective β2 (β2>>β1) receptor agonist (with relatively little β1 stimulation at normal doses) •
Actions: Potent agonist at β2 receptors on smooth muscle cells in airways (e.g. bronchioles) • increased mucociliary clearance, decrease vascular permeability, decrease mediator release
Metabolism: COMT/MAO,
Pharmacokinetics: F 15-75, 1/2 life is 6-8 hours. only 8-15% reaches systemic circulation
Pharmacodynamics: ORAL; 1 hr onset/ peak 3 hours/duration 6-8 hrs INHALED; 1 minute onset/ 30 min peak/ 4-6 hour duration
Indications: • Prompt-acting rescue inhaler for asthma, COPD (bronchodilator) • Inhibit premature labor (relaxes smooth muscle cells in uterus as well) •
Other facts: • Most often given as MDI (metered dose inhaler) • Can be given via nebulizer • Rarely given any more as iv infusion • Side effects include CVS: tachycardia, palpitations, tremor, angina, arrhythmias, vasodilate pulm arterioles CNS: anxiety, headache and tremor. Metabolic- hypokalemia, hyperglycemia can develop tolerance.
omalizumab
anti-IgE antibody
indication: severe asthma maintenance
mechanism- binds and inhibits IgE receptors on mast cells
ADRs:N/V, rashes, malignancy, anaphylaxis
PK- sub q administration
Ipratropium (Atrovent™)
Class: Synthetic, inhaled muscarinic receptor blocker
MOA: blocks the ability of acetylcholine to bind to and stimulate muscarinic receptors in the respiratory tract, thus leading to bronchodilatation Indications: bronchospasm in chronic bronchitis and emphysema; bronchospasm in asthma; rhinorrhea in allergic rhinitis or with common cold
PK: much of an inhaled dose is actually swallowed (only 10% gets to lungs); not well absorbed from the resp tract; drug is metabolized in liver, or excreted unchanged in feces
Duration: 6-8 hours
Contraindications and ADRs: avoid in patients with problems with atropine or similar drugs; use cautiously in patients with angle-closure glaucoma, BPH, bladder neck obstruction;
ADRs include bitter taste, blurred vision, dry moiuth, nausea, bronchospasm (perhaps from propellant)
Other facts: close relative is tiotropium (Spiriva™)
Dose: for bronchospasm, usual dose is 2 puffs (36 mcg per puff) qid not to exceed 12 puffs per 24h
montelukast
leukotriene inhibitor
indications: asthma maintenance therapy
mechanism: competitive inhibitor at CysLT receptor.
effects: block airway hyperresponsiveness, decrease permeability, decrease mucous secretion, increase mucociliary clearance, decrease PGs and TXs
PK tmax- 3-4 hours, F- 40%, T 1/2- 3/6 hours. hepatic metabolism- CYP3A.
ADRs- GI- N/V, headache, hepatitis, churg-strauss
other: good for aspirin, kids,
fluticasone
glucocorticoids
indications: chronic maintenance of asthma, severe acute asthma, inhaled: prophylaxis to reduce systemic steroids, COPD
mechanism: binds glucocorticoid response elements in nucleus
effects: decreased, PG, LT, and TX, decreased transcription of proinflammatory cytokines, degrades brady and tachykinins, increases b2 receptors, decreases TNF, increases eosinophil apoptosis
ADRs:
locally: thrush, hoarse voice- only 10% in lungs
systemically: HPA axis suppressoin, bruising, cataracts, decreased growth, behavioral disturbances, cushingoid appearances, hypertension, infection, osteoporosis, aseptic necrosis, acutely: insomnia/psychosis, hyperglycemia, hypernatremia, myopathy
hydrocortisone, prednisone, methylprednisone
glucocorticoids
indications: chronic maintenance of asthma, severe acute asthma, inhaled: prophylaxis to reduce systemic steroids, COPD
mechanism: binds glucocorticoid response elements in nucleus
metabolically: liver, CY3PA
effects: decreased, PG, LT, and TX, decreased transcription of proinflammatory cytokines, degrades brady and tachykinins, increases b2 receptors, decreases TNF, increases eosinophil apoptosis
ADRs: HPA axis suppressoin, bruising, cataracts, decreased growth, behavioral disturbances, cushingoid appearances, hypertension, infection, osteoporosis, aseptic necrosis, acutely: insomnia/psychosis, hyperglycemia, hypernatremia, myopathy
