5-Ht Receptor Agonists And Antagonists

Front 1

subtypes of 5-HT receptors for which centrally acting drugs have been developed?

Back 1

1, 2, 3 families

Front 2

5-HT1 receptor:
-effector mechanism
-effect
-location

Back 2

5-HT1 receptor:
-GPCR;
-hyperpolarize by increasing K+ conductance;
-brainstem and basal ganglia

Front 3

5-HT2 receptor:
-effector mechanism
-effect
-location

Back 3

5-HT2 receptor:
-GPCR;
-slow depolarization;
-prefrontal cortex

Front 4

5-HT3 receptor:
-effector mechanism
-effect
-location

Back 4

5-HT3 receptor:
-ligand-gated receptors;
-rapid depolarization due to Na+ gating;
-emetic centers in brainstem and GI

Front 5

enterochromaffin cell location and clinical significance?

Back 5

GI tract;
carcinoid syndrome (appendix) resulting in increased GI motility and coagulopathy

Front 6

5-HT and platelets?

Back 6

5-HT is stored in platelets and released in response to tissue injury inducing smooth muscle contraction and intense local vasospasm

Front 7

heart response to 5-HT?

Back 7

positive inotropic and chronotropic effects

Front 8

Bezold-Jarisch reflex?

Back 8

augmented vagal tone to heart caused by 5-HT, can result in 3rd degree heart block

Front 9

CNS and 5-HT?

Back 9

diffuse projections, thought to be important in pathogenesis of psychosis and behavioral disorders

Front 10

how many 5-HT subtypes are there?

Back 10

14

Front 11

buspirone:
-mechanism
-therapeutic uses
-toxicity

Back 11

buspirone:
-5-HT1 agonist
-anxiolytic, smoking cessation
-little or no habituation or tolerance

Front 12

triptans:
-prototype
-mechanism
-therapeutic uses
-toxicity

Back 12

triptans:
-sumatryptan (imitrex)
-5-HT1 agonists
-emergency treatment of migraine and migraine variants;
-heart block and spasm of coronary arteries

Front 13

sumatryptan (imitrex)?

Back 13

antimigraine agent
5-HT1 agonist

Front 14

ergot alkaloids:
-prototype
-mechanism
-therapeutic uses
-toxicity

Back 14

ergot alkaloid:
-ergotamine
-agonist activity at 5-HT and α receptors with presumed vasoconstriction of meningeal and cerebral vessels;
-antimigraine (mostly replaced);
-cardiac valvular lesions, retroperitoneal fibroplasias

Front 15

ergotamine?

Back 15

antimigraine agent
ergot alkaloid
agonist activity at 5-HT and α receptors

Front 16

which drugs can cause cardiac valvular lesions and retroperitoneal fibroplasias?

Back 16

ergot alkaloids

Front 17

lysergic acid diethylamide (LSD):
-mechanism
-therapeutic uses
-toxicity

Back 17

LSD:
-high affinity agonist at several 5-HT subtypes;
-none, recreational
-hallucinations

Front 18

ketanserin:
-mechanism
-therapeutic uses
-toxicity

Back 18

ketanserin:
-antagonist of 5-HT1 and 5-HT2 receptors;
-anti-HTN
-sedation

Front 19

ondansetron:
-mechanism
-therapeutic uses

Back 19

ondansetron:
-selective 5-HT3 antagonists
-control cnacer chemotherapy-induced emesis, also reduces cravings in alcoholics

Front 20

drugs related to ondansetron?

Back 20

dolasetron
granisetron

Front 21

cyproheptadine:
-mechanism
-therapeutic use

Back 21

cyproheptadine:
-5-HT2 and H2 receptor antagonist
-control post-gastrectomy dumping syndrome

Front 22

ritanserin:
-mechanism
-therapeutic use

Back 22

ritanserin:
-selective 5-HT2 antagonist
-prevent thromboembolism (phase III trials)

Front 23

antithrombotic agent?

Back 23

ritanserin

Front 24

antiemetics?

Back 24

ondansetron
dolasetron
granisetron
cyproheptadine

Front 25

anti-HTN agent?

Back 25

ketanserin

Front 26

antimigraine agents?

Back 26

triptans
ergot alkaloids

Front 27

antianxiety agent?

Back 27

buspirone