Exam 1 Adrenergic Drugs Flashcards
Norephinephrine mech
-a1 agonist
-B1 agonist
-MAO and COMT sensitive
Norepinephrine structure
-catecholamine
-benzene with 2 OH + monoamine
Epinephrine mech
-a1 agonist (high concentrations)
-B1 agonist
-B2 agonist
-MAO and COMT sensitive
Epinephrine structure
NE with methyl group on N
Epinephrine use
-anaphylaxis
-cardiac arrest
Epinephrine problems
-not orally active bc MAO and COMT metabolism
Epinephrine counters hypoglycemia
-a1 activation inhibits insulin secretion
-B2 activation increases glycogenolysis and gluconeogenesis
=increases glucose
Dipiveferin (epinephrine)
-infant glaucoma
-lipophilic
-activated by esterase
Dopamine (intropin) mech
-D1 agonist: renal dilation
-B1 agonist: cardioSTIMULATION and vasoCONSTRICTION
Dopamine use
-shock
-acute congestive heart failure
selective D1 agonist problems
-severe HTN
a1 receptor agonists
-phenylephrine
-oxymetazoline
phenylephrine use
-nasal decongestant
-mydriasis
-pressor
-vasoCONSTRICTOR in anesthesia
Phenylephrine mech
-a1 agonist
-Gq pathway
-MAO substrate
Phenylephrine structure
-epinephrine without para -OH
Phenylephrine problems
-shit nasal decongestant
-first pass metabolism
oxymetazoline mech
-a1 PARTIAL agonist
-promote vasoCONSTRICTION
-tachyphylaxis/desenstization
oxymetazoline structure
-2-aralkylimidazoline
-pentagon with 2 Nitrogen
-resonance stabled
Oxymetazoline use
-nasal and ophthalmic decongestants
non-selective B agonist
-Isoproterenol
Isoproterenol mech
-B1 and B2 agonist
-Gs
-COMT substrate
Isoproterenol effects
-bronchoDILATION
-increase CO
-may lower BP (B2 vasodilation and lower peripheral resistance)
Isoproterenol uses
-COPD
-asthma
-cardiostimulant in emergency
-heartblock before pacemaker implantation
-after cardiac surgery
-not rlly used bc epinephrine and dopamine are better
B1 agonist effects
-increase CO
-increase AV conduction
-increase renin release in kidney
B1 selective drugs
-Dopamine
-Dobutamine
Dobutamine mech
-racemic
-B1 agonist (+)
-a1 agonist (-)
-COMT substrate
Dobutamine use
-acute heart failure
-shock
-lab stress test
B2 agonist effects
-bronchoDILATION
-vasoDILATION
-cardiac effects only at high doses
B2 selective agonists
-Metaproterenol
-Terbutaline
-Albuterol
-Salmeterol
-Formoterol
Metaproterenol and Terbutaline mech
-resorcinol derivatives
-B2 agonists
-not a substrate
Metaproterenol and Terbutaline effects
-bronchoDILATION
-cardiac effects at high doses
Terbutaline use
-prevent premature labor
Metaproterenol and Terbutaline structure
-epinephrine with bottom left OH moved over to the right on the ring
Albuterol and Salmeterol structure
-metahydroxymethyl derivatives
-CH2OH at bottom of ring
-no top left OH
B2 agonist use
-asthma
-COPD
Salmeterol and Formoterol mech
-short onset
-long acting
Salmeterol and Formoterol problems
minor heart stimulation
Formoterol structure
-ring
-OH
-NHCOH next to it on ring
B3 agonist effects
-relax bladder
-prevent urination
B3 agonist
-Mirabegron
Mirabegron use
-treat overactive bladder
Mirabegron problems
-slow onset
-HTN
Mirabegron mech
-B3 agonist
-also M3 ANTAgonist
a2 agonist effects
-Gi
-inhibit SNS output
-decrease transmitter release
a2 agonist effects
-decrease HR
-decrease contractility
-dec BP
-dec renin release
-dec vasoconstriction
selective a2 agonist drugs
-clonidine
-Guanabenz
-Guanfacine
-Methyldopa
-brimonidine
-Tizanidine
Clonidine mech
-a2 agonist
-Gi
Clonidine structure
-imidazoline
-pentagon nitrogen
-ring with 2 chlorine
Clonidine use
-HTN
-neuropathic pain
-opiate withdrawal
-ADHD
Clonidine problems
-hypotension
-sedation
-dry mouth
-withdrawal
Guanabenz and Guanfacine structure
-open ring imidazolines
-nonionized at pH
Guanabenz and Guanfacine uses
-HTN
-ADHD
Methyldopa mech
-a2 agonist
-prodrug metabolized to active form
Methyldopa use
-HTN esp in pregnancy
Brimonidine mech
-a2 agonist
-inhibit aq humor production
-stimulate aq humor outflow
Brimonidine use
-treat glaucoma
Brimonidine structure
-imidazoline attached to rings with Br
brimonidine problems
-allergic conjuctivitis
Tizanidine use
-treat muscle spacisity
Tizanidine mech
-a2 agonist
Tizanidine problems
-sedation
-Na and water retention
-dry mouth
-withdrawal