Serotonin

Question 1

rizatriptan

Answer 1

serotonin agonist

Sumatriptan (zolmitriptan, rizatriptan and others)
are 5-HT1B,D,F agonists inactive at other
receptors.
b. Drug of choice for Rx acute migraines, cluster
headaches. Highly effective, rapidly reduce or
abort headache in over 70% of patients.
c. Mechanism
• activation of prejunctional 5-HT1B/D receptors
on sensory nerves resulting in blockade of
trigeminovascular system

Question 2

sumatriptan

Answer 2

serotonin agonist

Sumatriptan (zolmitriptan, rizatriptan and others)
are 5-HT1B,D,F agonists inactive at other
receptors.
b. Drug of choice for Rx acute migraines, cluster
headaches. Highly effective, rapidly reduce or
abort headache in over 70% of patients.
c. Mechanism
• activation of prejunctional 5-HT1B/D receptors
on sensory nerves resulting in blockade of
trigeminovascular system

Question 3

zolmitriptan

Answer 3

serotonin agonist

Sumatriptan (zolmitriptan, rizatriptan and others)
are 5-HT1B,D,F agonists inactive at other
receptors.
b. Drug of choice for Rx acute migraines, cluster
headaches. Highly effective, rapidly reduce or
abort headache in over 70% of patients.
c. Mechanism
• activation of prejunctional 5-HT1B/D receptors
on sensory nerves resulting in blockade of
trigeminovascular system

Question 4

cyproheptadine

Answer 4

serotonin antagonist

nonselective 5HT1, 5HT2 antagonist
• Rx of symptoms resulting from carcinoid tumors
• It also is an H1 histamine receptor
antagonist and is used for that purpose.
Adverse effects like other H1 antagonists
(drowsiness, GI disturbances)

Question 5

ketanserin

Answer 5

serotonin antagonist

5HT2 receptor selective (5HT2A > 5HT2C)
• lowers arterial pressure in hypertensives,
approved for use in some countries (Mexico,
Europe, S. America) but not U.S.
• mechanism
• blocking 5-HT2 receptors on vascular
smooth muscle
• blocking

Question 6

ergonovine

Answer 6

serotonin partial agonist

these drugs have both agonist and antagonist actions

5HT2 receptor partial agonist, weak
antagonist activity
• diagnostic tool vasospastic angina
• used to control postpartum and
postabortal hemorrhage

Question 7

ergotamine

Answer 7

serotonin partial agonist (combined with caffeine)

ergotamine partial agonist at 5-HT1/2 receptors
• VSM constrictor

Ergotamine effective for Rx acute migraines
(probably via 5-HT1 receptors given effectiveness
of triptans for migraine relief) and is still
prescribed for that purpose.
• Ergotamine is used also to control postpartum
bleeding (via 5-HT2 receptors), however
ergonovine is more active and less toxic.
• Adverse effects of 5-HT2 receptor agonists include
prolonged vasospasm, GI disturbances.
Methysergide can produce CNS disturbances
including hallucination.

Question 8

methysergide

Answer 8

serotonin partial agonist

these drugs have both agonist and antagonist actions

methysergide is an antagonist at 5-HT2
(5-HT2A/C) receptor and also a partial agonist
at 5-HT1 receptor
• methysergide effective for Rx symptoms of
carcinoid tumors