-
serotonin function in cardiovascular system
- vasoconstriction (except skeletal muscle and heart)
- platelet aggregation
- subendocardial fibroplasia
-
serotonin function in GI tract
- contraction of smooth muscle
- prokinetic effect
- sever diarrhea in carcinoid syndrome
-
serotonin function in airway
bronchoconstriction
-
serotonin function in skeletal muscle
malignant hyperthermia
-
serotonin function in behavior
- control of sleep-wake cycle
- aggression and impulsivity
- anxiety and depression
-
serotonin function in nervous system
- neurotransmitter (itch & pain)
- activates
- vomiting center in medulla
- enteric nerves
- chemoreceptor reflex (bezold-jarisch reflex)
-
5-HT1 receptors
Gi - inhibits adenylyl cyclase, decrease cAMP
-
5-HT 2 receptors
Gq - increases IP3 & DAC
-
5-HT 3 receptors
activates ligand-operated ion channels
-
5-HT 4 receptors
Gs - activates adenylyl cyclase
-
4 serotonin agonist
- triptans 1D,1B
- buspirone 1A
- cisapride - propulsid 4
- SSRIs
-
MOA of triptans
- constricts intracranial blood vessels
- blocks the release of calcitonin gene related peptide (CGRP) in trigeminal nerves
-
4 AE of triptans
- chest discomfort
- altered sensation (paresthesis, warmth)
- rebound migraine
- SC inj - stinging, burning,
- nasal spray - bitter taste
-
5 CI of triptans
- ischemic heart disease and angina
- peripheral vascular disease
- concurrent (24hrs) of ergot or triptan
- renal or hepatic impairment
- wolff-parkinson-white syndrome
-
4 drug interactions of triptans
- ergot alkaloids
- MAOIs
- SSRI or SNRI - serotonin syndrome
- eletriptan should not be used w/i 72hrs of strong CYP3A4 inhibitor
-
serotonin agonist
indicated for chronic weight management in conjunction with dietary intervention
lorcaserin - belviq
-
serotonin antagonist
blocks (2) and histamine
ind - carcinoid tumor
post-gastrectomy dumping syndrome
cyproheptadine - periactin
-
serotonin antagonist
blocks (1c&2)
inhibits platelet aggregation
blocks a1-adrenergic receptors
hypotensive
-
serotonin antagonist
blocks (3)
ind - N/V associated with surgery and cancer chemo-therapy
setron's
-
formed from serotonin in pineal gland
maintains circadian rhythm
ind - insomnia, jet lag
MOA - Gi
melatonin
-
ergot acting on the CNS & Pituitary
- LSD
- bromocriptine
- pergolide
-
-
ergot working on the vessels
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