Exam 1 Adrenergic Drugs Flashcards

1
Q

Norephinephrine mech

A

-a1 agonist
-B1 agonist
-MAO and COMT sensitive

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2
Q

Norepinephrine structure

A

-catecholamine
-benzene with 2 OH + monoamine

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3
Q

Epinephrine mech

A

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

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4
Q

Epinephrine structure

A

NE with methyl group on N

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5
Q

Epinephrine use

A

-anaphylaxis
-cardiac arrest

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6
Q

Epinephrine problems

A

-not orally active bc MAO and COMT metabolism

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7
Q

Epinephrine counters hypoglycemia

A

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

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8
Q

Dipiveferin (epinephrine)

A

-infant glaucoma
-lipophilic
-activated by esterase

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9
Q

Dopamine (intropin) mech

A

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

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10
Q

Dopamine use

A

-shock
-acute congestive heart failure

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11
Q

selective D1 agonist problems

A

-severe HTN

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12
Q

a1 receptor agonists

A

-phenylephrine
-oxymetazoline

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13
Q

phenylephrine use

A

-nasal decongestant
-mydriasis
-pressor
-vasoCONSTRICTOR in anesthesia

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14
Q

Phenylephrine mech

A

-a1 agonist
-Gq pathway
-MAO substrate

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15
Q

Phenylephrine structure

A

-epinephrine without para -OH

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16
Q

Phenylephrine problems

A

-shit nasal decongestant
-first pass metabolism

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17
Q

oxymetazoline mech

A

-a1 PARTIAL agonist
-promote vasoCONSTRICTION
-tachyphylaxis/desenstization

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18
Q

oxymetazoline structure

A

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

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19
Q

Oxymetazoline use

A

-nasal and ophthalmic decongestants

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20
Q

non-selective B agonist

A

-Isoproterenol

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21
Q

Isoproterenol mech

A

-B1 and B2 agonist
-Gs
-COMT substrate

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22
Q

Isoproterenol effects

A

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

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23
Q

Isoproterenol uses

A

-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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24
Q

B1 agonist effects

A

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

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25
Q

B1 selective drugs

A

-Dopamine
-Dobutamine

26
Q

Dobutamine mech

A

-racemic
-B1 agonist (+)
-a1 agonist (-)
-COMT substrate

27
Q

Dobutamine use

A

-acute heart failure
-shock
-lab stress test

28
Q

B2 agonist effects

A

-bronchoDILATION
-vasoDILATION
-cardiac effects only at high doses

29
Q

B2 selective agonists

A

-Metaproterenol
-Terbutaline
-Albuterol
-Salmeterol
-Formoterol

30
Q

Metaproterenol and Terbutaline mech

A

-resorcinol derivatives
-B2 agonists
-not a substrate

31
Q

Metaproterenol and Terbutaline effects

A

-bronchoDILATION
-cardiac effects at high doses

32
Q

Terbutaline use

A

-prevent premature labor

33
Q

Metaproterenol and Terbutaline structure

A

-epinephrine with bottom left OH moved over to the right on the ring

34
Q

Albuterol and Salmeterol structure

A

-metahydroxymethyl derivatives
-CH2OH at bottom of ring
-no top left OH

35
Q

B2 agonist use

A

-asthma
-COPD

36
Q

Salmeterol and Formoterol mech

A

-short onset
-long acting

37
Q

Salmeterol and Formoterol problems

A

minor heart stimulation

38
Q

Formoterol structure

A

-ring
-OH
-NHCOH next to it on ring

39
Q

B3 agonist effects

A

-relax bladder
-prevent urination

40
Q

B3 agonist

A

-Mirabegron

41
Q

Mirabegron use

A

-treat overactive bladder

42
Q

Mirabegron problems

A

-slow onset
-HTN

43
Q

Mirabegron mech

A

-B3 agonist
-also M3 ANTAgonist

44
Q

a2 agonist effects

A

-Gi
-inhibit SNS output
-decrease transmitter release

45
Q

a2 agonist effects

A

-decrease HR
-decrease contractility
-dec BP
-dec renin release
-dec vasoconstriction

46
Q

selective a2 agonist drugs

A

-clonidine
-Guanabenz
-Guanfacine
-Methyldopa
-brimonidine
-Tizanidine

47
Q

Clonidine mech

A

-a2 agonist
-Gi

48
Q

Clonidine structure

A

-imidazoline
-pentagon nitrogen
-ring with 2 chlorine

49
Q

Clonidine use

A

-HTN
-neuropathic pain
-opiate withdrawal
-ADHD

50
Q

Clonidine problems

A

-hypotension
-sedation
-dry mouth
-withdrawal

51
Q

Guanabenz and Guanfacine structure

A

-open ring imidazolines
-nonionized at pH

52
Q

Guanabenz and Guanfacine uses

A

-HTN
-ADHD

53
Q

Methyldopa mech

A

-a2 agonist
-prodrug metabolized to active form

54
Q

Methyldopa use

A

-HTN esp in pregnancy

55
Q

Brimonidine mech

A

-a2 agonist
-inhibit aq humor production
-stimulate aq humor outflow

56
Q

Brimonidine use

A

-treat glaucoma

57
Q

Brimonidine structure

A

-imidazoline attached to rings with Br

58
Q

brimonidine problems

A

-allergic conjuctivitis

59
Q

Tizanidine use

A

-treat muscle spacisity

60
Q

Tizanidine mech

A

-a2 agonist

61
Q

Tizanidine problems

A

-sedation
-Na and water retention
-dry mouth
-withdrawal