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Basic Pharmacology > 3. Histamine, Serotonin, and Ergot Alkaloids- Eicosanoids > Flashcards

3. Histamine, Serotonin, and Ergot Alkaloids- Eicosanoids Flashcards

1
Q

endogenous molecules with powerful pharmacologic effects that do not fall into traditional autonomic groups

A

Autacoids

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2
Q

Histamine precursor

A

histidine

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3
Q

histamine is metabolized by enzyme

A

Monoamine oxidase

diamine oxidase

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4
Q

how to detect excess production by histamine

A

imidazole acetic acid in urine

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5
Q

important pathophysiologic roles of histamine

A

seasonal rhinitis (hay fever )
urticaria
angioedema
control of acid secretion in the stomach

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6
Q

triple response of Lewis

A

wheal
flush
flare

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7
Q

triple response of Lewis

mediated by these receptors

A

H1 and H2

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8
Q

Histamine receptors

smooth muscle

A

H1

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9
Q

stomach
heart
mast cells

histamine receptor

A

H2

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10
Q

nerve endings
CNS

histamine receptor

A

H3

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11
Q

Leukocytes

Histamine receptor

A

H4

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12
Q

postreceptor mechanism of each histamine receptor subtype

A

H1 - Gq, Inc IP3, DAG
H2 - Gs, Inc cAMP
H3 - Gi, dec cAMP
H4 - Gi, dec cAMP

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13
Q

Prototype antagonist

H1

A

Diphenhydramine

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14
Q

Prototype antagonist

H2

A

cimetidine

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15
Q

Prototype antagonist

H3

A

clobenpropit

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16
Q

H1 effects

A

pain and itching
bronchoconstriction
vasodilation
local edema

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17
Q

H2

effects

A

gastric acid secretion

cardiac stimulation

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18
Q

H3 effects

A

modulation of other neurotransmitters

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19
Q

H4 effects

A

leukocyte chemotaxis

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20
Q

why are H1 receptor antagonists not given to neonates

A

susceptible to antimuscarinic effects

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21
Q

H1 receptor antagonists SE

A 
sedation
drowsness
blurred vision
dry mouth 
urinary retention
anorexia 
orthostatic hypotension
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22
Q

H1 receptor antagonists first -generation

A 
Diphenhydramine
brompheniramine
chlorpheniramine
cyclizine 
meclizne
buclizine
carbonoxamine
dimenhydrinare
hydroxyzine
promethazine
cyproheptadine
clemastine
tripelennamine
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23
Q

MOA diphenhydramine

A

competitive block of peripheral and CNS H1 receptors
alpha and M receptor block
antimotion sickness effect

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24
Q

uses of diphenhydramine

A 
hay fever
angioedema 
motion sickness (cyclizine - more antimotion sickness action, less sedative and less autonomic)
insomnia 
dystonia 
anti-emetic (promethazine)
for serotonin syndrome (cyproheptadine)
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25
Q

H1 receptor agonists (second - generation)

A 
cetirizine
loratadine 
fexofenadine 
desloratadine
levocetirizine
terfenadine
astemizole
ebastine
azelastine
bilastine
rupatadine
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26
Q

MOA cetirizine

A

block of peripheral H1 receptors

no autonomic or anti-motion sickness effects

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27
Q

Uses of cetirizine

A

hay fever
angioedema
urticaria

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28
Q

H2 receptor antagonist

A

cimetidine
ranitidine
famotidine
nizatidine

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29
Q

uses of cimeditine

A

peptic ulcer disease
zollinger ellison syndrome
gastroesophageal reflux

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30
Q

cimetidine only SE

A

CYP450 inhibitor and antiandrogen effects like gynecomastia

dec hepatic flow

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31
Q

used in ICU setting o prevent gastric erosion and hemorrhage

A

cimeditine

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32
Q

serotonin (5 hydroxytryptamine)

produced from

A

tryptophan

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33
Q

serotoni metabolized by

A

monoamine oxidase

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34
Q

excess production of serotonin in the body is detected by

A

5-hydroxyindole acetic acid in the urine

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35
Q

neurotransmitter in CNS and enteric nervous system

local hormone that modulates gastroinestinal activity

A

serotonin

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36
Q

serotonin receptor

brain

A

5HT 1D

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37
Q

serotonin receptor

smooth muscle
platelets

A

5HT2

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38
Q

serotonin receptor
smooth muscle
platelets

A

5HT2

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39
Q

serotonin receptor
area postrema (CNS)
sensory and enteric nerves

A

5 HT3

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40
Q

serotonin receptor

presynaptic nerve terminals in enteric nervous system

A

5-HT4

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41
Q

5-HT 1D receptor agonists

A 
sumatriptan
almotriptan
eletriptan
frovatriptan
naratriptan
rizatriptain
zolmitriptan
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42
Q

MOA of sumatriptan

A

5HT1D agonists
vasoconstriction
modulates neutrotransmitter release

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43
Q

DOC for acute migraine

cluster headache

A 
sumatriptan
almotriptan
eletriptan
frovatriptan
naratriptan
rizatriptain
zolmitriptan
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44
Q

SE of sumatriptan

A 
paresthesias 
dizziness
chest pain
coronary vasospasm
injection site reaction
45
Q

5HT1D agonists
route of administration
and DOA

A

all are PO except sumatriptain which can also be intranasally, transdermal and IV

All has 2-27 hours DOA
except sumatriptan DOA 2-4 hours

46
Q

5HT3 receptor antagonist

A 
ondansetron
granisetron
dolasetron
palonosetron
alosetron
47
Q

blocks chemoreceptor trigger zone and enteric nervous systm 5 HT3 receptors

A

ondansetron

48
Q 
uses of 
ondansetron
granisetron
dolasetron
palonosetron
alosetron
A

chemotherapy and postoperative vomiting

Irritable bowel syndrome (alostron only)

49
Q

SE of 5HT 3 antagonist

A 
diarrhea
headache
malaise
QRS and QT prolongation(dolasetron only)
constipation (alosetron only)
50
Q

St. Anthony’s fire

A

ergot alkaloid

51
Q

complex molecules produced by a fungus found in wet or spoiled grain

A

ergot aklaloids

52
Q

classification of ergot alkaloids

A

vasoselective

uteroselective

53
Q

5HT2 receptor antagonist

vasoselective

A

ergotamine
dihydroergotamine
methysergide

54
Q

5-HT2 antagonist

uteroselective

A

ergonovine

methyergonovine

55
Q

MOA ergot alkaloids

A

partial agonist a alpha and 5HT 2 receptors

some have potent agonist effect at dopamine receptors

56
Q

uses of ergotamine

A

migraine

cluster headache

57
Q

ergonovine uses

A

postpartum bleeding

migraine

58
Q

antidote for ergotamine

A

nitroprusside

59
Q

SE of vasoselective 5HT2 antagonist

A 
GI upset 
vasospasm
gangrene
uterine spasm 
abortion
60
Q

effect of ergotamine to epinephrine

A

epinephrine reversal as a partial agonist

61
Q

ergonovine SE

A

GI upset (n,v, diarrhea)
uterine spasm
abortion

62
Q

drugs used for vertigo

A

betahistine
cinnarizine
dimenhydrinate

63
Q

strong antagonist at H3 receptor (inc levels of NT histamine, acetylchoine, norepinephrine, serotonin and GABA )
weak agonist at H1 (vasodilation and inc permeability in the inner ear)

A

betahistine q

64
Q

an antihistamine and CCB

promotes cerebral blood flow

A

cinnarizine

65
Q

first gen antihistamine used for nausea , vomiting, and dizziness caused by motion sickness

A

dimenhydrinate

66
Q

betahistine used for

A

balance disorders

Meniere’s disease

67
Q

Cinnarizien used for

A

nausea
vomiting due to motion sickness
Meniere’s disease
vertigo

cerebral apoplexy
cerebral arteriosclerosis
post trauma cerebral symptoms

68
Q

selective calcium entry blocker with calmodulin binding propreties and H1 antagonist activity

A

flunarizine

69
Q

flunarizine uses

A

prophylaxis of migraine
occlusive peripheral vascular disease
vertigo
adjuvant for epilepsy

70
Q

major families of eicosanoids include

A

straight chain: leukotrienes

cyclic: prostacyclin, prostaglandings, thromboxane

71
Q

cyclooxygenase isoform

A

COX-1

  • many tissue
  • normal physio processes

COX-2

  • inflammatory cells
  • synthesis of prostacycln in vascoular endothelium
  • synthesis of prostaglandins for renal fx
72
Q

drug the inhibts phospholipase A2

A

corticosteroids

73
Q

inhibits COX-2 COX-2

A

NSAIDS

74
Q

inhibits lipoxygenase

A

zileuton

75
Q

inhibits leukotrienes

A

zafirlukast

76
Q

this eicosanoid promotes

leukocyte chemotaxis

A

LTB4

77
Q

this eicosanoid promotes
bronchoconstriction
, slow reacting substance of anaphylaxis

A

LTC4

LTD2

78
Q

this eicosanoid promotes
vascular smooth muscle relaxation
protective effects on gastric mucosa
maintains PDA

A

PGE1

79
Q

this eicosanoid promotes
vascular smooth muscle relaxation
maintains PDA
inc uterine tone

A

PGE2

80
Q

this eicosanoid promotes
vascular smooth muscle relaxation
(peripheral, pulmonary, coronary)

A

PGI2

81
Q

this eicosanoid promotes
inc uterine tone
dec IOP

A

PGF 2alpha

82
Q

this eicosanoid promotes

platelet aggregation

A

TXA2

83
Q

prostaglandin E1 analog

A

misoprostol
gemeprost
alprostadil

84
Q

MOA of misoprostol

A

activates EP receptors
inc HCO3 and mucus secretion in stomach
uterine contraction

85
Q

indications of misoprostol

A

peptic ulcer disease
prevention of NSAID induced gastric mucosa injury
abortifacient

86
Q

SE of misoprostol

A 
abdominal pain
diarrhea
uterine cramping
misacarriage 
teratogen - moebius sequence
87
Q

misoprostol is used together with ___ as safe abortifacient

A

mifepristone

methotrexate

88
Q

MOA of alprostadil

A

prostaglandin E1 analog
activates EP receptors
causes vascular smooth muscle relaxation and vasodilation

89
Q

uses of alprostadil

A 
maintenance of PDA for infants with right ventricular outflow obstruction 
erectile dysfunction (injected into cavornosa)
90
Q

SE of alprostadil

A 
apnea
hypotension 
arrythmia 
priapism
lightheadedness
91
Q

Prostaglandine E2 analog

A

Dinoprostone

Sulprostone

92
Q

MOA low conc contract
higher conc relax uterine and cervical smooth muscle
soften cervix at term before induction with oxytocn

A

Dinoprostone

93
Q

Uses of dinoprostone

A

induction of labor

abortifacient (2nd trimester)

94
Q

Dinoprostone SE

A

cramping

fetal trauma

95
Q

Prostaglanding F2 alpha analog

A

carboprost
bimatoprost
Travoprost
Unoprostone

96
Q

MOA activates FP receptors

A

carboprost
bimatoprost
Travoprost
Unoprostone

97
Q

uses of carboprost
bimatoprost
Travoprost
Unoprostone

A

control of postpartum hemorrhage
for refractory postpartum bleeding
abortifacient

98
Q

carboprost SE

A

vomiting
diarrhea
transient bronchoconstriction

99
Q

prostaglandin I2 analog

A

epoprostenol
beraprost
iloprost
treprostinil

100
Q

MOA activates IP receptors
causes vasodilation
reduces platelet aggregation

A

epoprostenol
beraprost
iloprost
treprostinil

101
Q

latanoprost

MOA

A

prostaglandin F2 alpha analog

102
Q

Latanoprost MOA

A

activates FP receptors
inc outflow of aq humour
reduces IOP

103
Q

Uses latanoprost

A

Glaucoma

104
Q

SE latanoprost

A

alters color of iris causing permanent eye color change

105
Q

Sildenafil
Tadalafil Vadernafil
MOA

A

Phosphodiesterase 5 inhibitor -> degrades cGMP to inactive GMP -> vasodilation

106
Q

Uses of Sildenafil

A

erectile dysfunction
pulmonary arterial hypertension
raynaud’s phenomenon

107
Q

Sildernafil SE

A 
headache
flushing
priapism
hearing loss
optic neuropathy
108
Q

Sildefil should not be taken with ___ it may lead to fatal hypotension

A

ISDN
ISMN
NTG

Basic Pharmacology (15 decks)

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