Pharmacology of Allergy and pulmonary drugs Flashcards Preview

504 (Immunology) > Pharmacology of Allergy and pulmonary drugs > Flashcards

Flashcards in Pharmacology of Allergy and pulmonary drugs Deck (31)
Loading flashcards...
1
Q

What are the 3 main symptoms of asthma or COPD

A

Bronchoconstruction, inflammation, mucus

2
Q

What is the MOA for beta-2 agonists

A

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

3
Q

What neurotransmitters bind to beta-2 agonists

A

epinephrine and norepinephrine

4
Q

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

A

True

5
Q

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

A

False: Only R enatiomer is active

6
Q

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

A

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

7
Q

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

A

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

8
Q

What changes to amine group leads to better beta selectivity

A

adding bulk to N-substituent

9
Q

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

A

N-tertiary butyl, and aromatic methylhydroxy substitution

10
Q

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

A

True

11
Q

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

A

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

12
Q

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

A

ortho/para (resorcinol), protection from COMT metabolism

13
Q

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

A

albuterol, salbutamol, terbutaline, metaproterenol

14
Q

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

A

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

15
Q

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

A

Albuterol and salbutamol/ terbutaline and metaproterenol

16
Q

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

A

Salmeterol, Formoterol, Bamuterol

17
Q

What makes salmeterol, formoterol, and bambuter LABAs

A

long lipohillic side chain, pro drugs

18
Q

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

A

12 or more hours

19
Q

What is MOA of muscarinic antagonists

A

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

20
Q

What are the muscarinic antagonists derivatives of

A

naturally occuring tropine alkaloids

21
Q

What is tropane, tropine

A

nitrogenous bicyclic compound, hydroxylated tropane

22
Q

What is the long acting LAMA, short acting LAMA

A

tiotropium, Ipatropium

23
Q

What is the key feature that makes muscarnic antagonists antagonists

A

chiral carbon connected to the aromatic ring points backwards

24
Q

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

A

The quaternary amines are charged

25
Q

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

A

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

26
Q

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

A

True

27
Q

What receptors do corticosteroids increase expression of

A

beta-2 receptors

28
Q

Why are corticosteroids inhaled

A

In order to avoid first pass metabolism

29
Q

What are the leukotrine modifiers

A

theopylline

30
Q

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

A

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

31
Q

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

A

Omalizumab (xolair)