Pharmacology of Allergy and pulmonary drugs

Question 1

What are the 3 main symptoms of asthma or COPD

Answer 1

Bronchoconstruction, inflammation, mucus

Question 2

What is the MOA for beta-2 agonists

Answer 2

bind to beta2-adrenergic receptors causing smooth muscle relaxation resulting in dilation of bronchial passages

Question 3

What neurotransmitters bind to beta-2 agonists

Answer 3

epinephrine and norepinephrine

Question 4

T/F: Beta-2 agonists work on the sympathetic path of the nervous system while muscarinic antagonists work on the parasympathetic path of the nervous system

Answer 4

True

Question 5

T/F: S and R enatiomers of catecholamines are active Beta-adrenergic agents

Answer 5

False: Only R enatiomer is active

Question 6

What are the three interaction points that allow catecholamines to bind to the beta-2 receptor

Answer 6

1) para and meta hydroxy groups, 2) hydroxy group at the beta carbon, 3) the amine group (primary or secondary) that is seperated by two carbons

Question 7

What are the two enzymes that metabolize catecholamines, where do they attack

Answer 7

monoamine oxidase (MOA)- oxidizes the amine group, catechol o-methyltransferase (COMT)- attacks the hydroxy groups on the aromatic ring

Question 8

What changes to amine group leads to better beta selectivity

Answer 8

adding bulk to N-substituent

Question 9

What are the two amine groups that have the most beta-2 selectivity

Answer 9

N-tertiary butyl, and aromatic methylhydroxy substitution

Question 10

T/F: A larger amino substituent is correlated to protection from MAO

Answer 10

True

Question 11

What is the consequence of having an alpha carbon substitution in cathecholamines for beta-adrenergic agents

Answer 11

decreased alpha/beta activity but has MAO protection that increases the oral bioavailability

Question 12

What is another way to position the hydroxy groups in catecholamine instead of para/meta, what is the consequence

Answer 12

ortho/para (resorcinol), protection from COMT metabolism

Question 13

What are the short acting beta-2 agonists (SABAs)

Answer 13

albuterol, salbutamol, terbutaline, metaproterenol

Question 14

How doe salbutamol and albuterol protect themselves from oxidation reaction, protection from MAI

Answer 14

Add a carbon in between hydroxy group and aromatic ring, bulky N-subistiuent

Question 15

Which SABAs are based on para/meta hydroxy placement, which SABAs are based on ortho/para hydroxy placement

Answer 15

Albuterol and salbutamol/ terbutaline and metaproterenol

Question 16

What are the long acting beta-2 agonists (LABAs)

Answer 16

Salmeterol, Formoterol, Bamuterol

Question 17

What makes salmeterol, formoterol, and bambuter LABAs

Answer 17

long lipohillic side chain, pro drugs

Question 18

What is the amount of time needed to be considered long acting

Answer 18

12 or more hours

Question 19

What is MOA of muscarinic antagonists

Answer 19

bind the M3 receptor causing a decrease in forming of cGMP resulting in dilation of bronchonconstrictor muscles and decreased mucus secretion

Question 20

What are the muscarinic antagonists derivatives of

Answer 20

naturally occuring tropine alkaloids

Question 21

What is tropane, tropine

Answer 21

nitrogenous bicyclic compound, hydroxylated tropane

Question 22

What is the long acting LAMA, short acting LAMA

Answer 22

tiotropium, Ipatropium

Question 23

What is the key feature that makes muscarnic antagonists antagonists

Answer 23

chiral carbon connected to the aromatic ring points backwards

Question 24

Why do muscarinic antagonists not cause systemic side effects, do not cross the blood barrier, and do not have central side effects

Answer 24

The quaternary amines are charged

Question 25

T/F: Muscarinic antagonists are selective but only work in the lungs because that is where all the muscarinic receptors are

Answer 25

False: muscarinic antagonists are nonselective but they only block M3 receptors because those are only the receptors in the lungs and they are not systemic

Question 26

T/F: Corticosteroids do not act directly on the airway smooth muscle and do not provide immediate relief of symptoms

Answer 26

True

Question 27

What receptors do corticosteroids increase expression of

Answer 27

beta-2 receptors

Question 28

Why are corticosteroids inhaled

Answer 28

In order to avoid first pass metabolism

Question 29

What are the leukotrine modifiers

Answer 29

theopylline

Question 30

What is the MOA of mast cell stabilizers, what medications are they

Answer 30

block calcium channels essential for mast cell degranulation, nedocromil and chromolyn

Question 31

What is the human immunoglobulin antibody that binds to IgE for patients with severe asthma

Answer 31

Omalizumab (xolair)