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Pharm Serotonin
KYCOM Block 13
65
Pharmacology
Graduate
01/20/2014

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Cards

Term
how is serotonin made and broken down
Definition
L tryptophan ingested >
facillitated transport into brain (concentration in blood relation to other AA)>
RATE LIMITING: tryptophan hydroxylase + O2 + pteridine >
serotonin >
MAO >
5-hydroxyindole acetic acid >
transport out of brain (inhibited by probenecid) >
small amt in urine (unless malignant carcinoid)
Term
what are the 4 serotonin receptors how do they work, where are they located
Definition
all 16 in brain, not all in body

1: Gi: inc K, hyperpolarize, inhibit
2: Gq: dec K, depolarize, excite
3: ion: dec K, inc Na, depolarize (fast)
4: dec K, hyperpolarize, excite
Term
functions of serotnin in blood and vessels 2
Definition
platelets contact endothelium which releases 5HT which goes to 5HT2 on platelets causing aggregation and vasoconstriction

vasoconstriction in eplanchnic, renal, pulmonary, cerebral)
Term
functions of serotonin in lungs 2
Definition
pulmonary vessel constriction

constriction of bronchioles
Term
functions of serotonin in GI
Definition
enterochromaffin cells make it, store it, and use it.
released bia vagal stimulation to cause emesis
Term
functions of serotonin in CNS 9
Definition
sleep, cognotion, sensory, motor, temp, pain, appetite, sex, hormone secetion
Term
is serotonin hydrophillic or phobic what does this mean about its distribution and function
Definition
phillic
cannot cross BBB, must be made in brain

not all cells that use it make it so they need transporter
Term
why can serotonin be hallucinogenic
Definition
N and O methylated properities
Term
what is the chemical class of serotonin
Definition
indolealkyamines
Term
what compound is relative to serotonin, how is it foemed
Definition
melatonin
N acetylation
O methylation
in pineal gland controlled by light
Term
ergot: where does it come from, what does it to (biochem and physio)
Definition
fungus on rye and grain

interacts with 5HT, D, and a receptors different interaction in different systems

vasoconstriction, cerebral constriction, supress sensory neuropeptides
Term
complication of all ergots
Definition
vasoconstriction can cause gangrene and misscarriage
Term
migraine: family hx, sex, onset, location, character, duration, associated symptoms
Definition
hx: yes
sex: females
onset: variable
location: usually unilateral
character: pulse, throb
duration; 2-72h
symp: aura (15%), photosensitive, sound sensitive, pale, nausea, vomiting. aggrevated by physical activity
Term
cluster headache: family hx, sex, onset, location, character, duration, associated symptoms
Definition
hx: no
sex: males
onset: in sleep
location: behind/around eye
character: sharp, steady
duration: 15-90min
symp: uni/bilateral sweating, flushing, congestion, ptosis, lacrimation, pupillary changes
Term
tension headahce: family hx, sex, onset, location, character, duration, associated symptoms
Definition
hx: yes
sex: females
onset: stress
location: bilateral around head
character: dull, persistant, tight
duration: 30 mim - 7d
symp: mild photophobia, noise phobia, anorexia
Term
mild migraine: definition, tx
Definition
occasional throbbing, no major impairment

mild analegesics combo analegesics, amiemetics
Term
moderate migraine: definition, tx
Definition
some impairment in function, nausea

combination anaglesics, ergots, sumatriptan, amiemetics
Term
severe migraine: definition, tx
Definition
>3/mo, functional impairment, nausea, vomiting

ergot, sumatriptan, animetics, prophylaxis
Term
what drugs are used in migraine prophylaxis 5, what is #1
Definition
#1 B blocker
Ca channel blocker
TCA
serotonergic agonist
MAOI
Term
what B blocker are used in migraine prophylaxis 5
Definition
propranolol
timolol
atenolol
nadolol
metoprolol
Term
what TCA are used in migraine prophylaxis 2
Definition
amitriptyline
nortryptyline
Term
what serotonergic agonist are used in migraine prophylaxis 2
Definition
methylserglide
cyproheptadine
Term
what MAOI are used in migraine prophylaxis 2
Definition
phenlzine
isocarboxazide
Term
what are triggers someone can avoid for migraine
Definition
alcohol, foods, irregular sleep, stress, time zone shift, altitude, barometric pressure, menstural cycle
Term
SSRIs (6), uses (5)
Definition
citalopram
paroxetine
sertaline
fluoxetine
fluboxamine
escitalopram

depression, PMDD, OCD, anxiety, migrane prophylaxis
Term
serotoniin agonists and their receptors (3)
Definition
sumatriptan: 5HT-1D
LSD: 5HT-2A, 2C
buspirone: 5HT-1A
Term
serotonin antagonist and their receptors:
Definition
odansteron: 5HT-3
risperidone: 5HT- 2A, 2C, D
cyproheptadine: 5HT-2A
methysergide: 5HT-2A, 2C
Term
ergots 6
Definition
ergoloid methylate
ergonovine
ergotamine
bromocryptine
methysergide
dihydroergotamine
Term
MOA sumatriptan 2
Definition
constrict vessels
supress release of neuropeptides
Term
MOA LSD
Definition
non selective
ergot derivative
Term
MOA buspirone
Definition
K channel open, hyperpolarization, inhibitory
Term
MOA cyproheptadine
Definition
inhibit 5HT-2A on smooth muscle
Term
MOA methysergide 2
Definition
LSD and methylergovine relative

inhibits vasoconstriction and vasopressin
inhibits 5HT-2A, 2C on smooth muscle
Term
SE sumatriptan
Definition
IV causes coronary spasm
Term
SE LSD
Definition
psychic alterations
hallucinations
Term
SE buspirone
Definition
headache, dizzy
Term
SE risperidone
Definition
gynecomastia: D receptor inhibition allows activity of prolactin
Term
MOA methysergide
Definition
inflammatory fibrosis (esp heart) in prolonged tx
Term
administration sumatriptan 3
Definition
IV - NO causes coronary vasospasm
oral - poor absorption
SC
nasal
Term
administration odansteron 2
Definition
IV, oral
Term
administration methysergide
Definition
stop for 3 wk every 6 mo
Term
use sumatryptan
Definition
acute migraine attacks
Term
use LSD
Definition
fun
Term
use buspirone
Definition
chronic anxiety
Term
use odansetron (MOA too)
Definition
nausea and vomiting (esp from chemo due to enterochromaffin release of 5HT in SI stimulation emesis

vagal afferents through 5HT-3 receptors initiate vomiting, this is stopped
Term
use of cyproheptadine 2
Definition
migraine prophylaxis
counteract sex SE of SSRI
Term
use methysergide 5
Definition
migraine prophylaxis
vascular headache prophylaxis
depression
schizophrenia
Term
use risperdone 3
Definition
migraine
depression
schizophrenia
Term
MOA ergoloid methylate
Definition
increase brain metabolism
Term
MOA ergonobine
Definition
increase strength, duration, and frequency of uterine contraction to decrease uterine bleeding
Term
use ergoloid methylate
Definition
early onset alzheimers
Term
use ergonovine
Definition
post partum hemorrhage
abortion bleeding control
Term
MOA ergotamine
Definition
caffiene + belladonna + phenobarbitol
Term
MOA bromocryptine
Definition
D2 agonist
Term
MOA methysergide 2
Definition
ergot derivative
inhibit vasoconstriction and vasopressin
inhibit 5HT action on smooth muscle
Term
MOA dihydroergotamine
Definition
caffiene + belladonna + phenobarbitol
Term
administration ergotamine
Definition
PO, SL, retro rocks

should not exceede 6mg/d or 10mg/wk
take 1-2mh/0,5h until relief
Term
administration of dihydroergotamine
Definition
IM, nasal
Term
SE ergotamine
Definition
CP, coronary vasoconstriction, tachy, brady

numbness, tingling of fingers and toes

nausea, vomiting
Term
contraindications of ergotamine 4
Definition
pregnancy, peripherial vascular disease, hepatic/renal impairment
Term
contraindications of dihydroergotamine 4
Definition
pregnancy, peripherial vascular disease, hepatic/renal impairment
Term
interactions of ergotamine 4
Definition
azithro, dirithro, clathro, erythromycin causes ergotism (HTN, ischemia)
Term
interactions of dihydroergotamine 4
Definition
azithro, dirithro, clathro, erythromycin causes ergotism (HTN, ischemia)
Term
use ergotamine 2
Definition
acute migraine or cluser headache
Term
use dihydroergotamine 2
Definition
migraine or cluster headache
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