Restrictive lung dz and PH

Question 1

This drug is a surfactant purified from bovine creatures

Answer 1

Beractant

Question 2

What does Beractant treat?

Answer 2

NRDS

Question 3

This is Dr. Sweatman’s favorite drug

Answer 3

Methotrexate

Question 4

Along with being an anticancer agent, what else can methotrexate treat?

Answer 4

Inflammatory disease that can effect the lung such as RA and sarcoidosis

Question 5

What is methotrexate’s MOA for treating cancer?

Answer 5

It inhibits the dihydrofolatereductase enzyme thus decreasing tetrahydrofolate synthesis –> inhibits formation of thymadine –> inhibits DNA synthesis

Question 6

What is methotrexate’s MOA for treating inflammatory diseases like RA and sarcoidosis?

Answer 6

Inhibits enzymes involved in purine metabolism –> increased levels of adenosine –> decreased inflammation

Question 7

This drug is the DOC for treating Wegener’s granulomatosis

Answer 7

Rituximab

Question 8

What is Rituximab’s MOA?

Answer 8

It is a B cell (CD20) antibody

Question 9

What is another treatment for Wegener’s

Answer 9

Cyclophosphamide

Question 10

What is cyclophosphamide’s MOA?

Answer 10

It is an alkylating agent that suppresses B cell activity

Question 11

What is yet another treatment of Wegener’s?

Answer 11

Azathioprine

Question 12

Acronym for Wegener’s drugs?

Answer 12

CAR: cyclophosphamide, azathioprine, rituximab

Question 13

What is the MOA for Azathioprine?

Answer 13

It is a purine analogue that inhibits purine synthesis.. It depresses the immune system

Question 14

What are the 4 classes of drugs that treat PH?

Answer 14

Prostanoids, Endothelin-1 receptor antagonists, Phosphodiesterase type 5 inhibitors, and Calcium channel blockers

Question 15

What are the 3 prostanoids?

Answer 15

EIT: Epoprosterenol, Iloprost, Treprostinil (all have “prost” in the name)

Question 16

What is the general side affect that you must watch for in all the prostenoids?

Answer 16

Bleeding (be careful giving these drugs in combination with antithrombic drugs like warfarin, aspirin)

Question 17

Which prostanoid is especially known for hemoptysis?

Answer 17

Iloprost

Question 18

Which prostanoid is a pain in the ass cuz you have to take 6-9 inhaled doses/day?

Answer 18

Iloprost

Question 19

Which prostanoid has the longest half life (4hr) and can be given SC or IV?

Answer 19

Treprostinil

Question 20

Which prostanoid has a weird side effect of jaw pain?

Answer 20

Treprostinil

Question 21

Which prostanoid is metabolized by CYP2C8 and thus has decreased clearance with gemfibrozil and increased clearance with rifampin?

Answer 21

Treprostinil

Question 22

What is the MOA of the prostanoids? 3 things

Answer 22

1. Induce vasodilation
2. Retard smooth muscle growth
3. Disrupt platelet aggregation

Question 23

What are the 2 endothelia-1 receptor antagonists?

Answer 23

BA: Bosentan, Ambrisentan (“sentan”)

Question 24

What is the MOA of the endothelia-1 antagonsits?

Answer 24

Endothelin-1 is a potent vasoconstrictor so these drugs antagonize the vasoconstriction –> vasodilation

Question 25

How are these drugs different/better than prostacyclins?

Answer 25

They are orally active

Question 26

What is a contraindication in both the endothelia-1 antagonists?

Answer 26

Pregnancy

Question 27

Which endothelia-1 receptor antagonist has ADE's including blood and liver toxicities and you need to check LFT's?

Answer 27

Bosentan

Question 28

Both the endothelia-1 antagonists are metabolized by what enzymes in the liver?

Answer 28

CYP3A4 and CYP2C9 (the most common ones)

Question 29

What is the only drug on the condensed drug list that is a Phosphodiesterase type 5 inhibitor?

Answer 29

Tadalafil

Question 30

What is Tadalafil's MOA?

Answer 30

Prepetuate endogenous cGMP --> vasodilation and decreased cell proliferation

Question 31

What is the weird and highly Sweatmany ADE of Tadalafil?

Answer 31

Change in color vision

Question 32

What are the 3 calcium channel blockers that treat PH?

Answer 32

DAV: Deltiazem, Amlodipine, Verapamil

Question 33

What is the MOA of the calcium channel blockers?

Answer 33

Block Calcium channels.. calcium is the key mediator of smooth muscle contraction

Question 34

What is the test you must do before giving someone a calcium channel blocker for PH?

Answer 34

Vasodilator challenge!!!

Question 35

Describe the vasodilator challenge

Answer 35

Give the patient IV epoprosterenol, IV adenosine, and inhaled NO. Monitor their PAP and CO. "Passing" the test means that they had a decrease in PAP and no change in CO

Question 36

What are some "in general" ADE's of calcium channel blockers?

Answer 36

Hypotension, bradycardia, flushing, edema

Question 37

Which calcium channel blocker is very favorable because of its long half life and thus easier dosing schedule?

Answer 37

Amlodipine (half life: 35-50 hr)

Question 38

This calcium channel blocker is contraindicated in PH

Answer 38

Verapamil