pharm drug list Flashcards
short acting beta agonist
SABAs albuterol (aka salbutamol) levalbuterol isoproterenol terbutaline epinephrine/ephedrine
SABA purpose
rescue meds
Long acting beta agonists
salmeterol formoterol indacaterol arformoterol olodaterol vilanterol
LABAs purpose
some have a relatively fast onset and can reduce symptoms quickly but NOT a rescue medications
oral albuterol
oral syrups and tablets are available, but rarely used
- slower onset <30 min peak effect 2-3 hours, duration 6-8 hours NOT a rescue med
- more pronounced systemic side effects than inhalation due to large dose and systemic distribution
albuterol inhalation
onset 5 min
both inhaler and nebulizer are rescue
peak action:
ventolin 25 min
nebulizer: 1-2 hrs
duration 4-6 hours
SABAs can be used alone
with mild intermittent asthma or in patients with exercise induced bronchoconstriction
-good for occasional symptoms
indications that asthma is not well controlled
needing rescue medication more than twice a week - means enhance the controller medications
frequent use of SABA or routine use of LABAs
can result in tolerance
frequent use and poor response to SABAs
can indicate poor adherence to controller or incorrect technique
rescue medications
rapid acting bronchodilators are appropriate for rescue and should be made available to all patients with asthma
LABA box warning
can be useful in asthma as add on therapy to inhaled corticosteroids but should not be used as only controller therapy
-monotherapy increases risk of asthma related death and hospitalization
SAMA lists
ipratropium bromide
ipratropium dosing
quick action but not a rescue medication: onset 15 min
half life 1.6 hours/duration 4 hours
continuous treatment requires minimum of q6h dosing
indications for inhaled muscarinic antagonists
primary use: important bronchodilators in COPD
-some are approved as bronchodilators in asthma but are less effective than beta 2 agoinists
side effects of muscarinic antagonists
due to quarternary ammonium structure if swallowed may cause constipation
Long acting muscarinic antagonists lists
tiotropium bromide
aclidinium bromide
umeclidinium bromide
glycopyrronium
tiotropium
LAMA onset 60 min duration 24-48 hrs peak 5-7 min half life 5-6 days
aclindinium
LAMA
longer acting than tiotropium
plasma half live of 5-8 hours
Phosphodiesterase inhibitor (non-specific) list
theophylline
theophylline side effects
non-specific PDE inhibitor is a methylxanthine side effects: CNS stimulation bronchodilation diuresis
compared with caffeine it causes less CNS stimulation and more bronchodilation
tobacco and theophyllines
theophylline is metabolized by CYP1A2
tobacco induces CYP1A2
the typical half-life of theophylline is 8 hours in smokers it is 4.5 hrs -problems of toxicity occur when patient quits smoking
theophylline toxicity reason
narrow therapeutic range (5-15 mg/L)
therapeutic index ED50/TD50 only 1 to 1.5 - toxic symptoms may occur at normal doses
theophylline toxic symptoms
Initial toxic symptoms: nausea/vomiting/abdominal pain, coarse muscle tremor.
Severe toxic symptoms: seizures, hypotension, and dysrhythmias.
If death occurs, usually due to intractable ventricular dysrhythmias.
MOA theophylline
inhibits phosphodiesterase isozymes and blocks the degradation of cAMP to 5’-AMP.
MOA ipratropium and tiotropium
block the stimulation of muscarinic receptors by acetylcholine (ACh) released from the vagus nerves and thereby attenuates reflex bronchoconstriction. The effect of ACh is mediated by IP3-induced calcium release and leads to smooth muscle contraction.
PDE-4 inhibitors
roflumilast
roflumilast MOA
phosphodiesterase (PDE) enzymes degrades cAMP
PDE-4 is a major isoform of PDE found in the lung tissue
this is a PDE-4 inhibitor
roflumilast clinical role
prevent COPD exacerbation
used after LAMA and LABA and ICS
Very expensive
roflumilast adverse effects
like the leukotrene antagonists may be associated with neuropsychiatric effects
-may decrease appetite/weight may cause nasuea and vomiting
oral/systemic corticosteroids ie glucocorticoids list
prednisone
prednislone
methylprednisolone
dexamethasone
risk of long term system glucocorticodids
- infection risk
- risk for developing diabetes, osteoporosis, weight gain, abnormal fat distribution
- adrenal suppression (crisis)
- hypertension
- glaucoma, cataracts
- restlessness/anxiety, insomnia/euphoria/psychosis
- GI upset
- hyperglycemia
use of systemic oral glucocorticoids
acceptable and often required for SHORT term use in asthma or COPD exacerbation
-limit long term use
Inhaled corticosteroids list
beclomethasone, Triamcinolone, budesonide, fluticasone
inhaled corticosteroids are
the most effective controllers
-because with proper technique 20-30% of dose is deposited at the site of action
inhaled corticosteroids and the need for a rescue medication
inhaled corticosteroids exert a delayed onset of action. Acute exacerbations require “rescue” medication, and may require systemic glucocorticoids
ICS adverse effects
-thrush; candidias of the mouth/esophagus
rinse mouth with water after use
-dysphonia
-throat irritation
-URI
-osteoporosisrare but serious side effects of ICS
hypercortisolism, anaphylaxis, hypersensitvity reaction, raised intraocular pressure, penumonia
fluticasone
one of the most potent and most commonly ICS used ‘flovent -when alone
‘advair when in combination with salmeterol LABA
budesonide
the only FDA ICS for pregnancy
lowest oral bioavalibilty
triamcinolone
ICS lower potency than others, may requires more puffs to achieve moderate to high dose (3-4 per day)
properties of ICS
full response can take 8 weeks
-not started during exacerbation (systemic are helpful not inhaled during exacerbation)
regular use of ICS
Asthma symptoms nearly —absent, and prevent progression.
- Reduce bronchial hyper-reactivity.
- Decrease airway mucus production.
- Increase the number of bronchial beta2 receptors as well as their responsiveness to beta2 agonists.- this reverses the tolerance and maintain B2 effect
Degranulation inhibitors drug list
cromolyn
mast cell stabilizer
antibody therapy drug list
omalizumab
leukotriene inhibitor drug list
zileutin (a 5-lipoxygenase inhibitor)
montelukast (leukotriene receptor antagonists)
zafirlukast
cromolyn MOA
inhibits mast cell degranulation
- prevents histamine release
- reduce the release of inflammatory leukotrienes
cromolyn onset and use
onset may take 1-2 weeks
full benefit 3-4 weeks
for asthma, now only used by nebulizer (usually not used at all)
omalizumab MOA
IgE binders
binds IgE and prevents activation of mast cells and basophils
omalizumab limitations
only for refractory “allergic” asthma -eosinophilia
EXPENSIVE
and only administered in healthcare setting 3 injections in office for two hours
omalizumab only in health care settings reason
Should only be administered in a healthcare setting by providers who are prepared to identify and treat anaphylaxis
-delayed hypersensitivity can occur (should dispense an epinephrine auto injector)
omalizumab dose and frequency
based on serum IgE levels
300 mg injected SC every 2-4 weeks
omalizumab pharmacokinetics
degraded in liver - excreted in bile
half life in 25 days
peak time after single SC injection 8 days
montelukast MOA
cysLT1 receptor antagonists
cysLT1 creates sustained bronchoconstriction, mucus secretion and edema.
montelukast in asthma
Prophylaxis and chronic treatment of asthma in patients 12 months of age and older.
Once daily in the evening.
montelukast for EIB
Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 6 years of age and older.
Dose = once daily PRN, 2 hours before exercise.
montelukast for AR
Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 6 months of age and older.
Once daily.
clinical role of leukoriene
Less effective than inhaled corticosteroids for asthma.
An accepted asthma-controller medication alternative to ICS (or adjunct) in mild, persistent asthma. (people or parents that don’t want to or don’t want their kids to take a inhaled corticosteroid)
receptor
montelukast clinical role
For allergic rhinitis usually combined with an antihistamine and/or intranasal glucocorticoid…
- A “compelling indication” for patients with allergic asthma?
- Leukotrienes are released from nasal mucosa in response to allergen exposure symptoms: sneezing, nasal itching, & congestion
zileuton MOA
inhibits 5-lipxygenase
only approved for asthma
drugs for TB
rifampin, isoniazid, ethambutol, pyrazinamide, and bedaquiline
Parameters to monitor when taking fluticasone
- Bone mineral density (at baseline and periodically thereafter)
- Ocular changes (IOP, catatracts)
- Signs/symptoms of oral/systemic infection
- Hypercotrisolism for adrenal suppression
Parameters to monitor when taking a beta agonist (umeclidinium)
BP, HR, serum K+, glucose
