26- Serotonin Flashcards
1
Q
rizetriptan
A
5-HT1 agnoist
- drug of choice for acute migraines, cluster headaches
- block trigeminovascular system which inhibits release of inflammatory peptides (CGRP)
- secondary vasoconstriction in cranial blood vessels (1D)
- side effects- recurrent migraine, risk of coronary spasm
- metabolized via liver– contraindicated in hepatic failure
2
Q
sumatriptan
A
5-HT1 agnoist
- drug of choice for acute migraines, cluster headaches
- block trigeminovascular system which inhibits release of inflammatory peptides (CGRP)
- secondary vasoconstriction in cranial blood vessels (1D)
- side effects- recurrent migraine, risk of coronary spasm
- metabolized via liver– contraindicated in hepatic failure
3
Q
zolmitriptan
A
5-HT1 agnoist
- drug of choice for acute migraines, cluster headaches
- block trigeminovascular system which inhibits release of inflammatory peptides (CGRP)
- secondary vasoconstriction in cranial blood vessels (1D)
- side effects- recurrent migraine, risk of coronary spasm
- metabolized via liver– contraindicated in hepatic failure
- more lipophilic and rapidily absorbed, longer half-life
4
Q
cyproheptadine
A
nonselective 5-HT1/2 antagonist
- used for treatment of carcinoid tumor symptoms
- also H1 receptor antagonist
- adverse effects: drowsiness, GI distrubances
5
Q
ketanserin
A
5-HT2 receptor selective antagonist
- blocks 5-HT2 receptors on VSM
- blocks alpha-1 receptors on VSM
- used to lower BP, but not in US
6
Q
ergonovine
A
5-HT2 receptor partial agonist
- weak antagonist activity
- used to control postpartum and postabortal hemorrhage
- diagnostic tool vasospastic angia
7
Q
ergotamine
A
5-HT1/2 receptor partial agonist
- treatment for acute migraines- most likely due to 5HT-1 effects
- used to control postpartum bleeding (not as effective as ergonovine) via 5HT-2
- side effects- prolonged vasospasm, GI disturbances
8
Q
methysergide
A
5-HT2 receptor antagonist
- 5-HT1 receptor partial agonist
- used for treatment of carcinoid tumor symptoms
- side effects- CNS disturbances (hallucination)
9
Q
Bezold-Jarisch Reflex
A
5-HT3 receptor mediated reflex bradycardia due to stimulation of sensory nerve endings resulting in:
- inhibition of SNS
- increased activity of cardiac vagus nerve
10
Q
5HT-1 Receptor
A
A, B, D, E, F subtypes– dec. adenyl cyclase, Gi coupled (5HT-1a inc. adenyl cyclase in heart only)
- 5HT-1c inc. PLC, inc. NO, Gq coupled
- 5HT-1d also causes vasoconstriction
- normally 5HT-1 receptors inhibit release of NOR and stimulate release of NO and prostacyclin
11
Q
5HT-2 Receptor
A
- inc. PLC which inc. Ca (contraction, platelet aggregation), Gq coupled
- direct vasoconstriction of VSM
12
Q
5HT-3 Receptor
A
ligand gated cation channel
13
Q
carcinoid tumor
A
-tumor that hypersecretes serotonin
