Pharmacology of OLDs Flashcards
which immune cells are in asthma
- mast cells
- eosinophils
- Th2 lymphocytes
which immune cells are in COPD
- neutrophils
- macrophages
- CTLs
what is the parasympathetic receptor in the lung
what happens when we activate it
- M3
- bronchoconstriction
what is the sympathetic receptor in the lung
what happens when we activate it
- B2
- bronchodilation
drugs that are beta 2 agonists
- albuterol
- epineprhine
- salmeterol
- formoterol
- indacaterol
ISAFE
drugs that are M3 antagonists
- Ipatropium (nonselective)
- Tiotropium
- Glycopyrrolate (nonselective)
- Aclidinium
- Umeclidium
ITAGU
drug that is M3 agonist
- methacholine
SABA (short acting beta agonist) drugs
- albuterol
- epinephrine
LABA (long acting beta agonist drugs)
- salmeterol (A/COPD BID)
- formoterol (A/COPD BID)
- indacaterol (COPD QD)
short acting M3 antagonists
- ipatropium
long acting M3 antagonists
- tiotropium
- aclidinium
- umeclidinium
- glycoprrolate
TAGU
rescue therapy used for
duration of effect
- treatment of acute symptoms
< 12 hours
maintenance therapy used for
duration of effect
- prevention of acute asthma symptoms
- > 12 hours or <12 with multiple dosing
can you use ipatropium for maintenance therapy?
how?
- yes
- you take multiple doses per day (4 to be exact)
epinephrine selectivity
- alpha 1, 2
- beta 1, 2
epinephrine indications
- anaphlyaxis (allergy)
epinephrine dosing (how we put it in the patient)
- subQ
albuterol indications
albuterol dosing (how we put it in the patient)
- asthma (acute)
- inhalation, prn
what happens if you chronically use short acting beta agonists
- beta 2 receptors will desensitize to it
chronic use of short term beta agonists how they become desensitized within minutes
- phosphorylation by PKA and GPCR
chronic use of short term beta agonists and how they become down regulated within hours
- receptor degradation
important toxicities of beta two agonists are because of
some toxicities
are these effects major concerns?
- cross agonism of beta 1 in the heart
- they are only partial agonists
- tachycardia
- chest pain
- a-fib
- angina
- vasoconstriction
- hypertension
- not generally major concerns
what is the full beta 2 agonist
- epinephrine
what happens with the majority of drugs that you inhale
- swallow vast majority
important toxicities of M3 antagonists are primarily based on which system
examples of some toxicities
- parasympathetic
- inhibit rest and digest responses
- dry mouth
- urinary retention
- constipation
corticosteroid drugs
- beclomethasone
- triamcinolone
- flunisolide
- fluticasone
- budesonide
- mometasone
- solumedrol
- predinosone
BFFB TMSP
which corticosteroid drug do you give via IV
- solumedrol
which corticosteroid drug do you give via oral
- prednisone
in which way do you give most corticosteroid drugs?
- inhaled
inhaled corticosteroid toxicities:
- immunosuppression
- thrush
- pneumonia
most inhaled steroids in pregnancy are which category
except which drug (what category)
- C
- prednisone (D)
why do we use corticosteroids with long acting beta 2 agonists
- they increase bronchiole smooth muscle responsiveness to beta 2 agonists because they
- increase the synthesis of the beta 2 receptor
MOA of Zileuton
- inhibit synthesis of leukotrienes by inhibiting 5-lipoxygenase
MOA of Montelukast and Zafirlukast
- competitive antagonists for leukotriene binding to receptors in bronchiole smooth muscle
what inhibits leukotriene synthesis by also inhibiting phospholipase A2 activity
how?
- corticosteroids
- increase expression of lipocortin
leukotriene inhibitors treat what kind of asthma
- allergic asthma
side effects of montelukast
- vasculitis (Churg-Strauss syndrome also known as eosinophilic granulomatosis with polyangiitis
- suicide tendencies?
can we use montelukast during pregnancy
- yes
mepolizumab target
used in which kind of asthma
- IL-5
- severe eosinophilic asthma
omalizumab target
used in which kind of asthma
- IgE - inhibits mast cell activation
- IgE-mediated allergic asthma
omalizumab and mepolizumab are given how
- SubQ
can you use omalizumab and mepolizumab in pregnancy
- yes
theophylline bronchodilator effects
- inhibits phosphodiesterase in bronchiole smooth muscle
- competitive antagonist of adenosine (which induces smooth muscle contraction in bronchioles)
theophylline toxicities
- seizures
- arrhythmias
why is theophylline use declining
- difficulties in safe dosing
- low therapeutic index
Moa of cromolyn
- stabilizes mast cells
- prevents degranulation of mast cells
- prevents release of inflammatory mediators
roflumilast MOA
- inhibits phosphodiesterase-4 (very selective) in bronchiole smooth muscle
- less toxicities
only with COPD drugs do you see what
- anti-cholinergic
why don’t we use LABAs alone
- they may increase risk of death from asthma
what do we use roflumilast for (what condition)
- COPD
