Methylxanthines MOA
Bronchodilation to decrease the intensity and frequency of moderate to severe asthma
attacks and to control chronic obstructive pulmonary disease exacerbations
Methylxanthines Prototype Drug
Theophylline
Theophylline Toxicity Risk
can cause severe cardiac dysrhythmias and convulsions
Methylxanthines Contraindication
These drugs are contraindicated for patients with untreated seizure disorders or peptic
ulcer disease
Theophylline contraindication w/ Caffeine
can intensify the adverse effects of the drug on the heart and CNS; Can decrease drug
metabolism.
Theophylline contraindication w/ Smoking Tobacco or Marijuana
can increase clearance to 50% in adults and 80% in older adults; Can cause an
ineffective dosing.
Drugs that Reduce Theophylline Levels (CYP3A Inducers)
Phenobarbital, phenytoin, rifampin; May need to increase drug level if given in
conjunction; Increase metabolism rate of target drug;
Drugs that Increase Theophylline Levels (CYP3A Inhibitors)
Cimetidine, fluoroquinolone antibiotics; May need to reduce drug level if given in
conjunction; These drugs will increase AE associated w/ target drug due to prolonged
activity and decreased metabolism of target drug.
Theophylline Lifespan Concerns
Elderly patients: Use with extreme caution in elderly patients as these patients are at an
increased risk of serious toxicity.
Pediatric patients: Dose selection requires caution, and regular monitoring of
concentrations is necessary (especially if the child is younger than 1 year of age) as the
rate of clearance varies significantly in these patients.
, Pregnancy: Use cautiously only if risk outweighs benefit
Roflumilast (Daliresp)
phosphodiesterase-4 inhibitor (PDE) approved for the treatment of COPD (and not
asthma)
Roflumilast MOA
selective action that inactivates cyclic adenosine monophosphate (cAMP) which results
in decreased cytokine release and subsequent lower levels of pulmonary infiltration by
neutrophils and other white blood cells
Roflumilast (Daliresp) Indication
not a first-line drug treatment and is reserved for severe cases of COPD with a primary
component of chronic bronchitis.
Bronchodilators: Anticholinergic Drugs Prototype Drugs
Ipratropium (inhaled, short acting; SAMA)
Tiotropium (inhaled, long acting; LAMA)
ipratropium/Tiotropium are anticholinergics, it is also considered a muscarinic receptor
antagonist as it relates specifically to the lungs. Blocks acetylcholine receptors and
prevents broonchospasm/bronchoconstriction.
Anticholinergic Drugs MOA
blocks acetylcholine, preventing bronchial constriction and narrowing of the airways,
which indirectly facilitates bronchodilation.
improve lung function by blocking muscarinic receptors in the bronchi, reducing
bronchoconstriction.
Anticholinergic Drugs Contraindication
patients with acute narrow-angle glaucoma or an enlarged prostate.
Nicotine-Free Products Smoking Cessation Products
Bupropion SR (Zyban); Varenicline (Chantix)
Bupropion SR (Zyban) MOA
an atypical antidepressant; blocks uptake of norepinephrine and dopamine.