Medicinal Chemistry and Pharmacology of Pulmonary Disease Flashcards
Main Treatment Strategies in Asthma
Bronchodilation
(3 drug classes)
- B2 adrenergic agonists
- methylxanthines
- anticholinergics
Main Treatment Strategies in Asthma
Anti-inflammation
(2 drug classes)
- glucocorticoids
- antileukotriene agents
Main Treatment Strategies in Asthma
inhibition of mast cell degranulation
(2 drug classes)
- Cromolyn
- Omalizumab
Main Treatment Strategies in Asthma
LABA
long acting beta agonists
Main Treatment Strategies in Asthma
ICS
inhaled corticosteroid
Main Treatment Strategies in Asthma
LTRA
leukotriene receptor antagonist
Main Treatment Strategies in Asthma
LAMA
long acting muscarinic agents
B2 adrenergic receptor agonists - sympathomimetic amines
primary activity - ___ bronchial smooth muscle
secondary activities - inhibit release of mediators from ___ cells, inhibit ___ leakage, increase microciliary ___ of mucus
- relax
- mast
- microvascular
- transport
B2 adrenergic receptor agonists
LTC4 and LTD4 or histamine activate ___ pathway which causes contraction.
B2-agonists activate the ___ pathway which causes relaxation
- Gq
- Gs
Selective B2- Adrenergic Agonists
SABA examples
albuterol (Ventolin)
levalbutoral (Xopenex)
terbutaline (Brethine)
SABA
short acting beta agonist
Selective B2- Adrenergic Agonists
T or F: albuterol has optimal B2 selectivity wheras terbutaline is more potent
True; terbutaline causes increased palpitations
Selective B2- Adrenergic Agonists
LABA examples
formoterol
salmeterol
SABA examples
albuterol
terbutaline
SABAs are resistant to ___
COMT
LABAs are resistant to ___ and ___
COMT and MAO
Selective B2 - Adrenergic Agonists
T or F: salmeterol/formoterol are for acute attacks
False
Selective B2- Adrenergic Agonists
- Inhaled drugs have ___ systemic adverse effects compared to oral B2 agonists
- inhaled drugs provide a ___ action on brochial smooth muscle
- fewer
- local
Selective B2- Adrenergic Agonists
Regular vs. PRN dosing
* ___ for acute or anticipated attack
* __ dosing confined to oral drugs or salmeterol and formoterol (in combination with ___ only). Used morning/evening.
- PRN
- regular
- ICS
Selective B2- Adrenergic Agonists
skeletal muscle ___ , palpitations, ___
* occurs less with B2 selective agents
* high doses of B2 selective agents may stimulate B1 receptors in the heart
* reflex tachycardia may occur due to vasodilation caused by B2 activation
vasodilation → decreased blood pressure → increased heart rate
- tremors
- tachycardia
LABA
what 2 drugs are contraindicated as monotherapy for prevention of asthma attacks?
salmeterol and formoterol
monotherapy LABA increases risk of asthma related death; need ICS + LABA
Glucocorticoids: Mechanism of Action
alter gene expression of proteins important in the ___ process
* Eosinophils, macrophages, and mast cells in the ___ epithelium and submucosa are decreased.
* Inhibit synthesis of ___ and ___.
* Decrease the ___ of bronchial smooth muscle cells that occurs in ___ asthma.
inflammatory
* bronchial
* prostaglandins and leukotrienes
* hyperresponsiveness, chronic
Glucocorticoids: Clinical Use in Asthma
___ dosing reduces the frequency and severity of acute attacks in patients with chronic bronchial asthma.
* ___ weeks to experience full effects of the medication
daily, 4-8 weeks
albuterol and terbutaline
- SABA inhalation onset ___ and duration ___
- SABA oral onset ___ and duration ___
- 5 min, 3-4 h
- 30 min, 3-8 h
salmeterol and formoterol -LABA
- salmeterol inhalation onset ___ and duration ___
- fomoterol inhalation onset __ and duration ___
- > 20 min, 12 h
- 10 min, >12 h
Advair
fluticasone + salmeterol combo