(L10) Autacoid Drugs

Question 1

Histamine’s only clinical use is….

Answer 1

as an aerosol, its used for a provacative test of nonspecific bronchial hypersensitivity

Question 2

Epinephrine is a (1) type drug when it is used to oppose Histamine during (2)

Answer 2

1- physiological antagonist (adrenergic agonist)

2- anaphylactic shock

Question 3

Cromolyn and Nedocromil are (1) type drugs with a (2) MOA and are used to treat (3)

Answer 3

1- histamine antagonists, release inhibitors
2- reduces mast cell degranulation
3- asthma

Question 4

_______ antagonizes Histamine by reducing mast cell degranulation

Answer 4

cromolyn, nedocromil

Question 5

list the 1st generation H1 receptor antagonists

Answer 5

(inverse agonist)

• chlorpheniramine
• cyclizine
• diphenhydramine (benadryl)
• dimenhydrate
• hydroxyzine
• meclizine
• promethazine

Question 6

list the 2nd generation H1 receptor antagonists

Answer 6

(inverse agonist)

• fexofenadine (allergra)
• loratadine (claritin)
• cetirizine (zyrtec)

Question 7

compare the uses of 1st and 2nd generation H1 receptor antagonists

Answer 7

(inverse agonists)
1st: allergic rhinitis, urticaria + CNS effects: motion sickness, nausea, somnifacients

2nd: allergic rhinitis, urticaria (no CNS effects)

Question 8

compare H1 receptor antagonist mechanism to H2 receptor antagonist mechanism

Answer 8

H1- inverse agonist

H2- competitive antagonist

Question 9

list the H2 receptor antagonists

Answer 9

• cimetidine
• ranitidine
• famotidine
• nizatidine

Question 10

H2 receptor antagonists are used for…..

Answer 10

• GERD
• peptic ulcers
• acute stress ulcers

Question 11

for allergies use H(1/2) blocker

for GERD use H(1/2) blocker

Answer 11

1- H1

2- H2

Question 12

serotonin has the following therapeutic uses…..

Answer 12

none- half life is too short

Question 13

Sumatriptan (triptans) is (are) (1) type drugs with a (2) MOA and are used for (3)

Answer 13

1- serotonin agonists
2- 5-HT-1b/1d receptor agonist
3- migraines

Question 14

______ are the first line drugs used for acute migraine management

Answer 14

triptans / sumatriptan (5-HT-1b/1d agonists)

Question 15

Metoclopramide and Cisapride are (1) type drugs with a (2) MOA and are used for (3)

Answer 15

1- serotonin agonists
2- 5-HT-4 receptor agonists
3- GERD- enhances GI motility / stomach emptying

Question 16

______ is used to treat GERD by enhancing GI motility which will speed up gastric emptying

Answer 16

metoclopramide, cisapride (5-HT-4 agonists)

Question 17

Cyproheptadine is a (1) type drug with a (2) MOA and is used for (3)

Answer 17

1- serotonin antagonist
2- 5-HT-2 receptor antagonist
3- allergic rhinitis, vasomotor rhinitis, management of serotonin syndrome (too much 5-HT)

Question 18

______ is used to treat serotonin syndrome, and allergic / vasomotor rhinitis

Answer 18

cyproheptadine (5-HT-2 antagonist)

Question 19

Ondansetron is a (1) type drug with a (2) MOA and is used for (3)

Answer 19

(zofran)
1- serotonin antagonist
2- 5-HT-3 receptor antagonist
3- anti-emetic for severe n/v in chemotherapy

Question 20

_______ is the anti-emetic used to treat the severe nausea and vomiting from chemotherapy

Answer 20

ondansetron / zofran (5-HT-3 antagonist)

Question 21

list the Ergot Alkaloids (from mushrooms)

Answer 21

• ergotamine, dihydroergotamine
• bromocriptine, cabergoline
• ergonovine, methylergonovine

Question 22

list the general mechanisms of action Ergot Alkaloids have

Answer 22

• agonist, partial agonist, antagonist for α-adrenergic and 5-HT receptors
• agonist, partial agonist for CNS DA receptors

Question 23

______ ergot alkaloids treat migraines

Answer 23

ergotamine, dihydroergotamine

Question 24

______ ergot alkaloids treat hyperprolactinemia

Answer 24

bromocriptine, cabergoline

Question 25

______ ergot alkaloids treat postpartum hemorrhage (include the preferred agent)

Answer 25

ergonovine, methylergonovine

oxytocin is the preferred agent

Question 26

______ can be used to diagnose variant angina

Answer 26

ergonovine (ergot alkaloid)- causes coronary artery spasm

Question 27

Misoprostol is a (1) type drug used to treat (2)

Answer 27

1- PG-E1 analog

2- prevent peptic ulcers (Pts taking high NSAID doses), ripen cervix at or near term, postpartum hemorrhage management

Question 28

Dinoprostone is a (1) type drug used to treat (2)

Answer 28

1- PG-E2

2- ripen (dilate) cervix at or near term

Question 29

______ is used to ripen / dilate the cervix at or near term

Answer 29

• Misoprostol (PG-E1 analog, has other functions, also used in combination as abortion inducer)
• Dinoprostone (PG-E2, an abortifacient)

Question 30

Alprostadil is a (1) type drug used to treat (2)

Answer 30

1- PG-E1
2- maintain PDA, impotence
(NOTE- indomethacin is an NSAID used to close PDA)

Question 31

______ is used to maintain PDA and to treat impotence

Answer 31

alprostadil (PG-E1)

Question 32

Epoprostenol is a (1) type drug used to treat (2)

Answer 32

1- PG-I2

2- severe pulmonary HTN, prevent platelet aggregation in dialysis

Question 33

______ is used to treat severe pulmonary HTN and to prevent platelet aggregation in dialysis

Answer 33

epoprostenol (PG-I2)

Question 34

Latanoprost is a (1) type drug used to treat (2)

Answer 34

1- PG-F2α derivative

2- glaucoma (enhances aqueous humor drainage)

Question 35

______ is an eicosanoid used to treat glaucoma

Answer 35

latanoprost (PG-F2α derivative)- enhances aqueous humor drainage

Question 36

zileuton functions to…..

Answer 36

inhibit LT pathway as 5-lypooxygenase inhibitor

Question 37

zafirlukast and montelukast functions to…..

Answer 37

inhibit LT pathway as LT-D4 antagonists

Question 38

glucocorticoids, in terms of eicosanoids, function to…..

Answer 38

• inhibits PLA2 –> blocking arachidonic acid release

- inhibits COX-2

Question 39

NSAIDs are inhibitors of (1) and have (2) effects

Answer 39

1- COX-1, COX-2, or both

2- anti-pyretic (fever reducer), analgesic, anti-inflammatory