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