PBL Drugs

Question 1

What is the MOA of Diphenhydramine and Chlorpheniramine?

Answer 1

H1 antagnoist (1st gen.)

Question 2

What are the pharmacokinetics of Diphenhydramine and Chlorpheniramine?

Answer 2

Crosses the blood-brain barrier

Question 3

What side effects are associated with first generation H1 antagonists?

Answer 3

Anti-muscarinic effects –> drying of secretions, GI disturbances, etc.

Question 4

What is the MOA of Fexofenadine, Cetirizine and Loratadine?

Answer 4

H1 antagnoist (2nd generation)

Question 5

What are the pharmacokinetics of Fexofenadine, Cetirizine and Loratadine?

Answer 5

Substrate for P-glycoprotein, actively pumped out of the blood-brain barrier (less drowsiness)

Question 6

What class is Theophylline in? What is also in this class?

Answer 6

• Methylxanthine

- Caffeine is also part of this class

Question 7

What is the MOA for Theophylline?

Answer 7

Controversial.
May be an adenosine antagonist.
In high doses, it’s a phosphodiesterase inhibitor, inhibits cAMP –> AMP. This may cause bronchodilation.

Question 8

What are the pharmacokinetics for Theophylline?

Answer 8

Very narrow therapeutic index

Question 9

What are the toxicities associated with Theophylline?

Answer 9

Arrhythmias, nervousness, GI bleeding

Question 10

What is the mechanism of action for Cromolyn sodium?

Answer 10

May block Ca2+ receptors in mast cells –> no Ca2+ release into cytoplasm –> no degranulation of histamine (Dynamed)
–> Dr. Trachte mentioned it might be stabilizing K+ channels

Question 11

What class is Epinephrine in?

Answer 11

Non-selective adrenoceptor agonist

Question 12

What is the mechanism of Epinephrine?

Answer 12

Beta1, Beta2, Alpha1 agonist

Question 13

What is the route of administration for epinephrine?

Answer 13

Inhalant or subcutaneous

Question 14

What is the toxicity associated with epinephrine?

Answer 14

Because of beta-1 action, cardiac effects include tachycardia, arrhythmias, angina exacerbation

Question 15

What class is Albuterol in?

Answer 15

Short acting beta-2 adrenoceptor agonist (SABA)

Question 16

What is the MOA of Albuterol?

Answer 16

Beta-2 agonist

Question 17

Why is it important to not overuse beta agonists?

Answer 17

Because tolerance can develop.

–> Overuse of beta agonist causes down regulation of the body’s beta receptors

Question 18

What toxicity is associated with albuterol?

Answer 18

Skeletal muscle tremor

Question 19

What class does Salmeterol belong to?

Answer 19

Long acting beta-2 adrenoreceptor agonist.

Question 20

What is the MOA of Salmeterol?

Answer 20

Beta-2 agonist, slower onset and longer duration than SABAs

Question 21

What toxicity is associated with Salmeterol?

Answer 21

Overuse can lead to tolerance, down regulation of systemic beta receptors. Skeletal muscle tremor

Question 22

What is the MOA of Zileuton?

Answer 22

5-lipoxygenase inhibitor, prevents leukotriene synthesis, less leukotriene B4

Question 23

What is the side effect of Zileuton?

Answer 23

Hepatotoxicity

Question 24

What is the MOA of Zafirlukast?

Answer 24

Leukotriene receptor antagonist.

Question 25

What is the MOA of Montelukast?

Answer 25

Leukotriene receptor antagonist

-Antiluekotrienes

Question 26

What is the MOA of Phenylephrine?

Answer 26

Alpha-1 agonist

Question 27

What is the MOA of Pseudoephedrine?

Answer 27

Alpha-1 agonist and Alpha-2 agonist

Question 28

What class does Betamethasone belong to?

Answer 28

Corticosteroid

Question 29

What class does Dexamethasone belong to?

Answer 29

Corticosteroid

Question 30

What class does methylprednisone belong to?

Answer 30

Corticosteroid

Question 31

What is the mechanism of Prednisone and other Corticosteroids?

Answer 31

Induces lipocortin to inhibit PLA2. Thus inhibiting the synthesis of cytokines, especially NF-kappaB.

Question 32

What are the most effective anti-inflammatory agents used in asthma therapy? How do they work?

Answer 32

ICS - Inhaled Corticosteroids.
They reduce inflammatory cell numbers and their activation in the airways. They reduce eosinophils in the airways and sputum and the numbers of activated T lymphocytes and surface mast cells in the airway mucosa.

Question 33

What is another mechanisms behind corticosteroids like prednisone?

Answer 33

Recruitment of HDAC2 to the inflammatory gene complex, which reverses the histone acetylation associated with increased gene transcription.

Question 34

What class is Triamcinolone in?

Answer 34

Corticosteroid

Question 35

What class is Beclamethasone in?

Answer 35

Corticosteroid

Question 36

What is the mechanism of action for Omalizumab?

Answer 36

Binds specifically to circulating IgE and blocks its binding with the high-affinity IgE receptor (FcERI) on the surface of mast cell and basophils. Reduces the number of FcERI receptors on basophils and submucosal cells in atopic patients.

Question 37

Why are first generation antihistamines sedative but second generation antihistamines are not?

Answer 37

Second generation antihistamines do NOT cross the blood brain barrier, thus they are NOT sedative.

Question 38

What is the MOA of Flunisolide?

Answer 38

Flunisolide is a glucocorticoid receptor agonist.

Question 39

How do Corticosteroids act as anti-inflammatory drugs?

Answer 39

They are thought to involve Lipocortins, Phospholipase A2 inhibitor proteins which through inhibition of arachidonic acid, control the synthesis of prostaglandins and leukotrienes

Question 40

How do Corticosteroids suppress the immune system?

Answer 40

Due to decrease function of the lymphatic system, a reduction in immunoglobulin and complement concentration, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Flu

Question 41

What does Flunisolide bind? When does it become acitive?

Answer 41

It binds to plasma transcortin. It becomes active when it is not bound to transcortin