Pharm - Asthma and COPD Flashcards
Structure vs. function of sweat glands
Anatomically SNS (long postganglionic fiber) Functionally PNS (releases ACh)
Non-specific beta agonists
Epi, ephedrine, isoproterenol
Fast acting, short lived beta 2 agonists
Albuterol, levalbuterol, terbutaline
LABAs
Salmeterol, formoterol
used with steroid
Antiinflammatory meds
Steroids
Cromolyn
Leukotriene inhibitors
Leukotriene receptor blockers
Montelukast, zafirlukast
Leukotriene synthesis blocker
Zileuton
IgE mab
Omalizumab
What has highest density of B2R?
Bronchial smooth muscle cells
Bronchial SMCs don’t have ___ innv, while blood vessels don’t have ___ innv
Symp
Parasymp
What is unique about the adrenergic receptors in bronchial SMCs?
Epinephrine is their endogenous ligand rather than NE like other adrenergic receptors
What type of cholinergic receptors are present on bronchial SMCs?
M2 and M3
M2R responsible for ___ using what G protein?
Decreased ACh release (M2R is autoreceptor)
Gi
M3R responsible for ___ using what G protein?
Bronchoconstriction
Gq –> increased Ca2+
Relationship between eosinophils and asthma/COPD
Major basic protein of eo’s causes bronchoconstriction by inhibiting M2R (so increasing ACh)
When would an M2R AGONIST cause bronchoconstriction?
In presence of a B2R agonist which would increase levels of cAMP and cause relaxation; by working through Gi, an M2R agonist would inhibit this effect and cause constriction.
How do B2 agonists cause bronchial SMC relaxation?
Increase cAMP –> PKA –> phosphorylation of MLCK –> relaxation
Which nerve is stimulated in asthma pts? Effect?
Vagal afferents –> sends messages to vagal afferents –> release ACh (parasymp) –> constriction of bronchial SMC
Affinity of epi vs. ephedrine vs. isproterenol
Epi - B1, B2, alpha
Ephedrine - B1, B2, some alpha
Isoproterenol - B1, B2
4 MOA beta agonists
- Increase cAMP –> relaxation
- Increase mucociliary transport
- Decrease mast cell release of mediators
- Decrease microvascular permeability
How do LABAs cause increased mortality?
Through Gq –> PLC –> inflammation
(beta2 agonists do NOT treat inflammation of asthma/COPD; they might exacerbate it