Respiratory Pharmacology Flashcards
In asthma, inflammatory cells release what
mast cells
eosinophils
T helper 2 cells
what bronchospastic mediators are released in asthma
histamine
leukotriene D4
Prostaglandin D2
what test/challenge is used to diagnose asthma
Methacholine
what inflammatory cells are increased in COPD
neutrophils
macrophages
cytotoxic T-lymphocytes
COPD can cause
progressive fibrosis
emphysema
ariway narrowing
excessive mucus
what is a risk factor for COPD
- smoking
- deficiency in alpha1-proteinase inhibitor
what is allergic rhinitis and what does it activate
nasal epithelium inflammation
- IgE mediated activation of mast cells, basophils
what are important mediators of inflammation that induce symptoms characteristic of allergic rhinitis
histamine
prostaglandins
leukotrienes
where do most of the drugs go if they are inhaled
80-90% swallowed
Name the drugs that are given orally
Corticosteroids
Adrenergic Agonists
Methylxanthine (theophylline)
MOA for adrenergic agnoists
stimulates B2-adrenergic receptors
- increases cAMP
- activates PKA
- induces bronchial smooth muscle cell relaxation
when do short-acting B2-adrenergic receptor agonists work
quick relief during asthma attack
- onset 1-5 minutes
- duration of action 4-6 hrs
Name3 long acting B2-adrenergic receptor agonists LABA
Salmeterol
Formoterol
Indacaterol
which B2-adrenergic receptor agonist for long acting, acts the longest and is it usually used for
Indacaterol
COPD
Why does Salmeterol have a longer duration of action than albuterol
Salmeterol has lipophilic side chain
Name B2- selective SABA
Albuterol
Terburtaline
Pirbuterol
Metaproterenol
what are B2-selective agonists SABA used for
all types of asthma attakcs
- not as effective in COPD
How often is B2- receptor selective agonists SABA used
- not to be used several times a day
when one overdoses on B2- receptor selective agonist SABA, what more is needed?
need for more anti-inflammatory therapy
corticosteroids and Leukotriene inhibitor
What can account for the diminshed activity (tolerance) of B2-receptor selective agnoist SABA
B2-recetpor downregulation
what are adverse effects of B2-receptor selective agonist SABA
Tremor restlessness tachycardia hypokalemia - more with oral dose than inhalation
Name 2 non-selective SABA
Isoproterenol and Epinephrine
MOA for Isoproterenol
nonselective B-agonist and potent bronchodilator
MOA for epinephrine
non-selective alpha, beta agonist and potent bronchodilator
How is Isoproterenol administered and how is it given to
acute asthma attack
-inhaled and oral
What is the law in the US for Isoproterenol
inhalation or sublingual administration is no longer marketed in the US
when is epinephrine used and how is it administered
acute asthma attack
- inhaled or subcutaneously - emergency circumstances
Name B2- selective agonists LABA
Salmeterol
Formoterol
Indacaterol
what is B2- selective agonists LABA used for
control (prophylaxis therapy) persistent asthma
- effective for asthma and COPD
when should one not take Salmeterol, Formoterol and Indacaterol
for acute asthma attack
what do B2- selective agonists LABA need to be taken with
anti-infammatory therapy ( corticosteroids, leukotriene, inhibitors )
Indacaterol can be specifically be used for what
COPD
Adverse effects of Salmeterol, Formoterol, and Indacaterol? how can this be helped
- airway tolerance to B2 agonists: potential problem
- Corticosteroids may prevent tolerance by increasing B2 receptor numbers within airway
Name 2 muscarinic antagonists
Ipratropium and Tiotropium
MOA of Ipratropium and Tiotropium
- reduces ACH -stimulated cyclic GMP
- inhibits mucus secretion
what is a popular combination inhaler
Ipratropium and Albuterol
Ipratroprium can specially be used for what
nasal discharge from rhinorrhea
What are adverse effects of Muscarinic antagonists
unpleasant bitter taste
dryness of mouth
cause glaucoma if sprayed in eye