Exam 1 Adrenergic Drugs Flashcards by Brooke Thornburg

Norephinephrine mech

-a1 agonist
-B1 agonist
-MAO and COMT sensitive

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Norepinephrine structure

-catecholamine
-benzene with 2 OH + monoamine

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Epinephrine mech

-a1 agonist (high concentrations)
-B1 agonist
-B2 agonist
-MAO and COMT sensitive

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Epinephrine structure

NE with methyl group on N

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Epinephrine use

-anaphylaxis
-cardiac arrest

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Epinephrine problems

-not orally active bc MAO and COMT metabolism

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Epinephrine counters hypoglycemia

-a1 activation inhibits insulin secretion
-B2 activation increases glycogenolysis and gluconeogenesis
=increases glucose

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Dipiveferin (epinephrine)

-infant glaucoma
-lipophilic
-activated by esterase

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Dopamine (intropin) mech

-D1 agonist: renal dilation
-B1 agonist: cardioSTIMULATION and vasoCONSTRICTION

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Dopamine use

-shock
-acute congestive heart failure

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selective D1 agonist problems

-severe HTN

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a1 receptor agonists

-phenylephrine
-oxymetazoline

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phenylephrine use

-nasal decongestant
-mydriasis
-pressor
-vasoCONSTRICTOR in anesthesia

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Phenylephrine mech

-a1 agonist
-Gq pathway
-MAO substrate

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Phenylephrine structure

-epinephrine without para -OH

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Phenylephrine problems

-shit nasal decongestant
-first pass metabolism

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oxymetazoline mech

-a1 PARTIAL agonist
-promote vasoCONSTRICTION
-tachyphylaxis/desenstization

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oxymetazoline structure

-2-aralkylimidazoline
-pentagon with 2 Nitrogen
-resonance stabled

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Oxymetazoline use

-nasal and ophthalmic decongestants

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non-selective B agonist

-Isoproterenol

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Isoproterenol mech

-B1 and B2 agonist
-Gs
-COMT substrate

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Isoproterenol effects

-bronchoDILATION
-increase CO
-may lower BP (B2 vasodilation and lower peripheral resistance)

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Isoproterenol uses

-COPD
-asthma
-cardiostimulant in emergency
-heartblock before pacemaker implantation
-after cardiac surgery

-not rlly used bc epinephrine and dopamine are better

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B1 agonist effects

-increase CO
-increase AV conduction
-increase renin release in kidney

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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