Eicosanoids

Question 1

Prostaglandins are _________ (rapidly/slowly) metabolized to inactive products at their site of action.

Answer 1

rapidly

Question 2

_____________ is the primary precursor of prostaglandins

Answer 2

Arachidonic acid

Question 3

Free arachidonic acid is released from the tissue phospholipids by the action of ______________ enzyme

Answer 3

phospholipase A2

Question 4

All eicosanoids with ring structures are synthesized via the ______________ pathway.

Answer 4

cyclooxygenase

Question 5

Eicosanoids with _______ structures include prostaglandins, thromboxanes, and prostacyclins

Answer 5

ring

Question 6

_______ is responsible for the physiologic production of prostanoids

Answer 6

COX-1

Question 7

_______ causes elevation of prostanoids usually at the site of chronic diseases and inflammation.

Answer 7

COX-2

Question 8

Name some of the functions that are regulated by COX-1.

Answer 8

Gastric cytoprotection
Vascular homeostasis
Platelet aggregation
Reproductive and kidney function

Question 9

What is the location of COX-2 enzymes?

Answer 9

Brain
Kidney
Bone

Question 10

COX-2 is stimulated by ____________

Answer 10

IL-1 and TNF

Question 11

COX-2 is inhibited by ____________

Answer 11

Glucocorticoids

Question 12

Lipoxygenases act on arachidonic acid to form _____________

Answer 12

leukotrienes

Question 13

Name some anti leukotriene drugs?

Answer 13

Zileuton
Zafirleukast
Montelukast

Question 14

Antileukotriene drugs are used to treat _________

Answer 14

asthma

Question 15

Name some prostaglandin E1 analogs

Answer 15

Alprostadil
Luboprostone
Misoprostol

Question 16

Name some prostaglandin F2α analogs

Answer 16

Bimatoprost
Tafluprost
Travoprost
Latanoprost

Question 17

Name some prostacyclin (PGI2) analogs

Answer 17

Epoprostenol
Iloprost
Treprostinil

Question 18

Where is alprostadil naturally produced?

Answer 18

Seminal vesicles
Cavernous tissues
Placenta
Ductus arteriosus in the fetus

Question 19

Alprostadil is used to treat two conditions

Answer 19

Erectile dysfunction

To keep the ductus arteriosus patent

Question 20

Zileuton MOA?

Answer 20

Inhibits lipoxygenase so no leukotrienes

Question 21

Monteleukast and Zafirleukast MOA

Answer 21

Leukotriene Receptors blockers

Question 22

A 63-year-old man with glaucoma maintained on a regimen of topical medications with an exacerbation
of his symptoms. He complains of difficulty with his vision in both eyes and has headaches. Which of the following drugs is the most appropriate treatment for this patient?
(A) Bimatoprost
(B) Latanoprost
(C) Pilocarpine
(D) Tetracycline
(E) Travoprost

Answer 22

Pilocarpine

Question 23

__________ is used fro the treatment of opioid induced constipation, chronic idiopathic constipation and IBS-constipation.

Answer 23

Lubiprostone

Question 24

What is MOA of lubiprostone?

Answer 24

It stimulates chloride channels in the luminal cells of the intestinal epithelium, thereby increasing intestinal fluid secretion

Question 25

___________ and ________ are the most common adverse effects of lubiprostone

Answer 25

Nausea and diarrhea

Question 26

Nausea can be decreased if lubiprostone is taken __________ (with food/empty stomach)

Answer 26

with food

Question 27

Misoprostol is used for?

Answer 27

Prevent NSAIDs induced ulcer | Induction of labor (off-label)

Question 28

____________ is contraindicated in pregnancy

Answer 28

Misoprostol (bcz it causes abortion)

Question 29

PGF2 alpha analogs are used for?

Answer 29

Open angle glaucoma | Eyelash hypotrichosis

Question 30

Adverse effects of PGF2 alpha analogs?

Answer 30

``` Blurred vision Iris color change ↑ number and pigmentation of eyelashes Ocular irritation Foreign body sensation ```

Question 31

Prostacyclin analogs are used for?

Answer 31

Pulmonary arterial hypertension

Question 32

ROA of Prostacyclin analogs?

Answer 32

Epoprostenol → Continuous IV infusion Treprostinil → PO/Continuous IV/SC/Inhalation Iloprost → Inhalation

Question 33

Prostacyclin analogs have _________ (short/long) half lives

Answer 33

short

Question 34

What are the adverse effects of prostacyclin analogs?

Answer 34

Dizziness, headache, flushing, and fainting | Bronchospasm and cough with iloprost

Question 35

___________ used as abortifacient

Answer 35

Carboprost

Question 36

_______ and _________ are both ↑ in primary dysmenorrhea

Answer 36

PGE2 and PGF2

Question 37

Dinoprostone can be used for “___________” and as abortifacient

Answer 37

cervical ripening

Question 38

___________ is used to close a patent | ductus arteriosus

Answer 38

Indomethacin

Question 39

A 6-year-old boy presents to his doctor for followup of recurrent hay fever and asthma. He usually has two to three attacks per week. For symptom control, he uses an albuterol inhaler, but his parents would like to try something more. They would like him to take something that would lessen the amount of attacks he has. Although corticosteroids would probably work best for prophylaxis, they are contraindicated in children. Which of the following drugs would decrease the amount of asthma attacks by preventing an arachidonic acid derivative from binding to its receptor? (A) Aspirin (B) Celecoxib (C) Ipratropium (D) Montelukast (E) Zileuton

Answer 39

D (Montelukast)