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106 Cards in this Set

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Histamie
144
H1-R mech
Gq
H1-R located on
SM
H2-R mech
Gs
H2R located on 3
stomach, heart, mast cells
H3-R mech
Gi
H3R located on 2
nerve endings, CNS
H4-R mech
Gi
H4R located on
WBC
Prototype H1x
diphenhydramine
Second-generation H1x 5
chlorpheniramine, cyclizine, fexofenadine, loratadine, cetirizine
Difference b/t 1st & 2nd generation H1x
less lipid soluble -> less CNS fx -> less sedation
Anti-motion sickness H1x 2
diphenhydramine, dimenhydrinate, cyclizine, meclizine, promethazine
CNS fx of H1x
sedation, antimuscarinic, ortho hypotension
H2x 4
cimetidine, ranitidine, famotidine, nizatidine
main purpose of H2x
block gastric acid secretion (dec Sx, healing time, recurrences)
main tox of H2x
dec hepatic drug metabolism
Serotonin
146
5HT 1D-R mech
Gi
5HT 1D-R located on
Brain
5HT 2-R mech
Gq
5HT 2-R located on 2
SM, plt
5HT 3-R mech
ligand-gated cation channel
5HT 3-R located on
CNS area postrema, sensory & enteric nerves
5HT 4-R mech
Gs
5HT 4-R located on
Presynaptic nerve terminals in ENS
5HT 1D agonists 2
sumatriptan, naratriptan
triptans are used for
acute migraine & cluster HA
5HT 4 partial agonist
tegaserod
5HT 2x 4
ketanserin, phenoxybenzamine, cyproheptadine
5HT3x end in
setron
which 5HT 2x is an irreversible inh
phenoxybenzamine
5HT 2x also having block fx on which R? 2
alpha, H1
Setrons are used for
vomitting assoc w/ chemo, post-op
Alosetron is also used for
diarrhea in women with IBS
Dolasetron is contraindicated in pt w/
heart dz (QRS & QT prolongation)
Ergot alkaloids
147
Common name for ergotism (severe vasoconstriction)
St. Anthony's fire
ergot that stimulates D2 but inh alpha 1 and 5HT2
bromocriptine
ergot that stim D2 and uterine SM but inh alpha1 and 5HT2
ergonovine
ergot that stim 5HT2 and uterine SM but inh alpha1 and D2
ergotamine
ergot that stim D2 and uterine SM but inh and stim 5HT2
LSD
ergot used for migraines
ergotamine
ergot used for obstetric bleeding 2
ergonovine, ergotamine
ergot used for hyperPRL and parkinsonism
bromocriptine
Vasoactive peptides
152
AII-R mech
Gq (AT1)
Fx of AII 2
constrict arterioles, inc aldosterone
Bradykinin-R mech
Gq, Gs, NO (B1, B2)
Fx of bradykinin 3
dilates arterioles, inc cap perm, stim sensory nerve endings
BNP-R mech (think nesiritide)
cGMP (ANPA)
Fx of BNP 3
dilate vessels, inh aldo secretion, inc glomerular filtration
Endothelin-R mech
Gq (ETA, ETB)
Fx of endothelin 1
SM contractor (esp vessels)
Neuropeptide Y-R mech
Gq
Fx of NPY 2
Vasoconstriction; stim heart
Substance P-R mech
NK1-3
Fx of substance P 4
dilates arterioles, contracts veins, contract intestinal & bronchial SM, promote diuresis
VIP-R mech
Gs (VPAC1, VPAC 2)
Fx of VIP
dilate vessels, relax intestinal & bronchial SM
Eicosanoids
157
Dinoprostone is which PG?
PGE2
Purpose of dinoprostone?
ripen uterus before labor induction
Tox of dinoprostone
N/V/D
Misoprostol is
PGE1
Misoprostol use
Abortion, keep PDA OPEN, prevent ulcer in chronic NSAID use
Epoprostenol is
PGI2
Epoprostenol use
severe pulm HTN
Alprostadil is
PGE1
Alprostadil use
Injection/insert into urethra for impotence
Latanoprost is
PGF2 derivative
Latanoprost use
Glaucoma (inc aq humor outflow)
Zileuton is
selective LOX inh
Zafirlukast & montelukast are
LTD4-Rx
Steroid mech on eicosanoids 2
inh PLP, inh COX-2 synth
NSAID mech
COX-inh
COX-2 specific NSAIDs
celecoxib
Which NSAID irreversibly binds to COX
aspirin
mech for NSAID induce asthma
shunt AA to synth of LT
Why don't NSAIDs cancel out their fx on PGI2 and TXA2?
Permanent TXA2 synth inh v temporary PGI2 synth inh
NO FX
163
endogenous NO synth by
NO synthase (NOS)
mech of NO relaxing SM
NO -> guanylyl cyclase -> cGMP -> dephosphorylate MLC -> relaxation
NO fx on cell adhesion 2
dec plt aggregation, dec neutrophil adhesion to vasc endo
NO donor Rx 3
nitroprusside, nitrates, nitrites
Asthma Rx
166
Short acting beta2 agonists 3
albuterol, terbutaline, metaproterenol
long acting beta2 agonists 2
salmeterol, formoterol
Mech for beta agonists
stim adenylate cyclase -> inc cAMP
Which beta agonists are used for prophylaxis
long-acting only
which beta agonists are used for acute bronchospasm
short-acting only
most common tox of beta-2 agonist? 3
sk muscle tremor, tachyphylaxis, transient tachycardia
3 methylxanthines
caffeine, theophylline, theobromine
Sources of methylxanthine
caffeine from coffee, theophylline from tea, theobromine from cocoa
which is the only methylxanthine that is used to Tx asthma
theophylline
Mech of theophylline
blocks PDE -> inc cAMP
3 common tox of theophylline
tremor, GI, insomnia
short acting anti-muscarinic aerosol
ipratropium
long acting anti-muscarinic analog of ipratropium
tiotropium
2 uses for anti-muscarinics in lungs
asthma, COPD
Do anti-muscarinics run the risk of tremors or arrhythmias
no
cromolyn/nedcromil mech
stabilize membrane
cromolyn/nedcromil must be administered p.o. why?
cause irritation by aerosol
the anti-IgE Ab is
omalizumab
Rx that block the formation of LT?
steroids, zileuton
Rx that block LT from working?
LT-Rx: lukasts