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Flashcards in Antihistamine Deck (20)
1

Histamine is released from what cells?

Basophil and mast cells

2

How is NO produced?

Arginine ---(NO synthase)--->citrulline + NO

3

H1 receptor is __ coupled receptor, and activation of it would cause?

Gq
Vasodilation via NO
Increase capillary permeability
Smooth muscle contraction
Pain and itch

4

Where are H2 receptor cells located and activation causes what?

H2 receptors are found in gastric parietal cells
Activation-->increase acid secretion

5

H1 antagonists are competitive or noncompetitive blockers? and what are the 1st and 2nd gen drugs?

Competitive
1st gen--->diphenhydramine/promethazine/chlorpheniramine/meclizine
2nd gen--->cetirizine/loratadine/fexofenadine

6

What are the benefits of 2nd gen H1 blockers comparing with 1st gen?

2nd gen do not cross BBB--->non sedating
2nd gen do not block M--->unlike 1st gen
1st gen--->sedating/anti M

7

What are the 2 commonly used antiemetic H1 blockers? and what about nausea and vomiting in pregnancy?

Meclizine and promethazine
Meclizine

8

H1 or H2?
Allergic reaction
Motion sickness
Preoperative sedation
Sleep aid
Parkinson
Acute EPS

Allergic--->both H1 and H2
All the rest are for H1

9

What is the end product of 5HT metabolism?

5-HIAA

10

Which 5HT receptor that is directly coupled to an ion channel? and what are the rest of the 5HT receptor coupled with?

5HT3
The rest are G-protein coupled receptors

11

What is the mechanism of buspirone?

5HT1a partial agonist for chronic anxiety

12

What is the mechanism of "triptans" and what are they used for?

5HT1d agonist--->vasocontrict--->acute migraine

13

Are 5HT2 receptor inhibitory or excitatory in the CNS

Excitatory

14

What group of drugs that block 5HT2a receptor?

Atypical antipsychotic like olanzapine

15

What is the mechanism of cyproheptadine?

5HT2 blocker for serotonin syndrome
H1 blocker--->seasonal allergy

16

What does 5HT3 receptor do? and what drugs act on them?

Mediate vomiting
"setrons" drugs block them--->antiemetic

17

What is the mechanism of ergotamine and what is it used for? side effect?

Alpha 1/5HT2 agonist--->vasoconstriction--->acute migraine
Prolonged vasoconstriction--->ischemia and gangrene/abortion

18

What other drugs can be used for acute migraine? and what drugs do we use for prophylaxis of migraine?

NSAIDs and acetaminophen
Propranolol (DOC)/verapamil/TCA/valproic acid

19

What is ergonovine used for?

Uterine smooth muscle contraction--->give IM after placental delivery

20

What are the drugs that cause gynecomastia?

Some Drugs Causes Awesome Knockers
Spironolactone
Digoxin
Cimetidine
Alcohol
Ketoconazole