PHARM

Question 1

What is the MOA of first generation antihistamines?

Answer 1

They DOWNREGULATE constitutive H1 receptor activity, not antagonists but INVERSE AGONISTS

Question 2

What are the adverse effects of first generation antihistamines in adults?

Answer 2

They have a sedative effect b/c lipophilic and cross the BBB

Question 3

What paradoxical effect may first generation antihistamines have in children?

Answer 3

Paradoxical agitation

Question 4

Below what age is it the use of first generation antihistamines contraindicated? Why?

Answer 4

Below the age of 2 because there have been a small number of deaths associated

Question 5

Why were second generation antihistamines developed? When is the onset of action? Peak serum level?

Answer 5

Developed LIPOPHOBICALLY to avoid the sedative effects of Gen1. Onset is in one hour and peaks at 2-3 hours.

Question 6

How are third generation antihistamines similar to second generation?

Answer 6

3rd generations are METABOLITES of second generation

Question 7

What are the antiinflammatory properties of 3rd generation antihistamines?

Answer 7

1) They decrease release of mast cell mediators 2) they downregulate adhesion molecules and 3) they inhibit the production of IL-4 and IL-13

Question 8

What receptor do beta agonists for asthma act on? What is the route of administration?

Answer 8

Relative affinity for beta 2 (though they can cause tachycardia and tremors) and they are inhaled

Question 9

What is an MDI?

Answer 9

Metered Dose inhaler

Question 10

What is the problem with chronic use of a beta agonist for asthma?

Answer 10

It may 1) Increase mortality and 2) It may lead to tolerance

Question 11

Is it best to use a beta agonist daily or PRN? Why?

Answer 11

PRN because daily use is associated with increased death and tolerance

Question 12

Why was salmeterol better than other beta-agonists? What was the problem and how is it circumvented?

Answer 12

Because it was long-acting but it was associated with INCREASED DEATH; however, co-administration with an inhaled steroid was not associated with increased death

Question 13

Why might the fact that corticosteroids reverse B-2 downregulation be important?

Answer 13

Because they improve mortality in ppl who use Beta-agonists chronically; probably because they decrease tolerance

Question 14

Why do people get a first pass effect from inhaled corticosteroids? What pathology in GI is associated?

Answer 14

Because they swallow their inhalations! Candida esophagitis

Question 15

A pregnant asthmatic in need of an inhaled corticosteroid should be given:

Answer 15

Budenoside

Question 16

Why would a person on inhaled steroids have a scratchy throat? What other oral pathology may present?

Answer 16

Because the steroid can deposit on the oropharynx and larynx; they can get oral thrush

Question 17

Which types of inhaled steroid devices have reduced risk of dysphonia?

Answer 17

Those with dry powder

Question 18

How can a person asthma medications reduce the risk for thrush?

Answer 18

Rinsing of the mouth after administration

Question 19

What are 4 systemic side effects of corticosteroids?

Answer 19

Osteoporosis, adrenal suppression, and ocular effects. In children it can cause short-term growth deceleration.

Question 20

What are the two types of leukotriene modifying drugs?

Answer 20

1) 5-lipooxygenase enzyme inhibitor 2) Leukotriene receptor antagonist

Question 21

Name a 5-lipoxygenase inhibitor

Answer 21

Zileuton

Question 22

Name 2 LTD4 receptor antagonists:

Answer 22

Zafirlukast and Montelukast

Question 23

What is the MOA of theophylline? Safe for pregnancy?

Answer 23

It is similar to caffeine and prevents the breakdown of cAMP which allows for increased calcium and bronchodilation; YES it is safe in pregnancy

Question 24

Why would coffee help ameliorate Sx of asthma?

Answer 24

It would act like theophylline by decreasing breakdown of cAMP

Question 25

Name 4 1st Gen antihistamines:

Answer 25

Diphenhydramine, Hydroxyzine, Chlorpheniramine, and Brompheniramine

Question 26

Which drugs for allergic rhinitis may affect intellectual and motor function?

Answer 26

First generation antihistamines

Question 27

Name 4 2nd generation antihistamines (COAL):

Answer 27

Ceterizine, Olopatadine, Azelelastine, and Loratidine

Question 28

What is better for nasal congestion: a second gen antihistamine or a nasal steroid?

Answer 28

Nasal steroid

Question 29

Name 3 3rd generation antihistamines:

Answer 29

Fexofenadine, Desloratidine, and Levocetirizine

Question 30

Which interleukins are inhibited by 3rd gen antihistamines?

Answer 30

IL-4 and IL-13

Question 31

The MOA of a drug that will treat an asthma attack acutely is:

Answer 31

Beta-2 agonist

Question 32

What are 2 effects of local deposition of inhaled corticosteroids?

Answer 32

Dysphonia and thrush

Question 33

Why do inhaled corticosteroids cause osteoporosis?

Answer 33

They inhibit osteoblast activity and decrease absorption by gut and kidney

Question 34

How do inhaled corticosteroids cause adrenal suppression?

Answer 34

They reduce ACTH secretion by the pituitary which secondarily leads to decreased cortisol from the adrenals

Question 35

What are 3 systemic side effects of inhaled steroids in adults?

Answer 35

Osteoporosis, adrenal suppression, and ocular effects

Question 36

What is the major effect of an inhaled corticosteroid in a child?

Answer 36

Can lead to short-term growth retardation

Question 37

What is the MOA of zileuton?

Answer 37

It is a 5-lipoxygenase inhibitor

Question 38

Montelukast and Zafirlukast inhibit the action of which molecule?

Answer 38

Leukotriene D4

Question 39

What drug has an MOA similar to that of caffeine?

Answer 39

Theophylline

Question 40

What 6 general classes of drugs where discussed in the pharm lecture?

Answer 40

1) Antihistamines (3 generations) 2)Nasal steroids 3) Beta agonists 4) Inhaled steroids 5) Leukotriene-modifying drugs and 6) Theophylline

Question 41

Drugs ending in “pheneramine” belong to which class?

Answer 41

First generation antihistamine