Adrenoreceptor Agonists And Antagonists Flashcards

1
Q

Drugs that mimic epinephrine and norepinephrine

A

Sympathomimetic drugs

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2
Q

Adrenergic agonists

A

Direct-acting (selective, non-selective), mixed-acting, indirect-acting (releasing agents, uptake inhibitor, MAO/COMT inhibitors)

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3
Q

Direct-acting selective agonists (alpha OR beta)

A

a1-phenylephrine, midorine
a2-clonidine, methyldopa
b1-dobutamine
b2-terbutaline

PCDT

PMCMDTl

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4
Q

Direct-acting non-selective agonists (alpha AND beta)

A

a1 a2-oxymetazoline
b1 b2-isoproterenol
a1 a2 b1 b2-epinephrine
a1 a2 b1-norepinephrine

OIEN

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5
Q

Mixed-acting agonist

A

Ephedrine

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6
Q

Indirect-acting releasing agonists

A

Amphetamine
Tyramine

-amine

Methylphenidate
Modafinil

Ms

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7
Q

Indirect-acting uptake inhibitor agonist

A

Cocaine

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8
Q

Indirect-acting MAO/COMT inhibitor agonists

A

Pargyline
Entacapone

PE

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9
Q

Drug of choice for anaphylaxis

A

Epinephrine

b1 - vasoconstriction and cardiac stimulant; increase in SBP due to inotropism, chronotropism

b2 - vasodilation in skeletal muscles to increase blood flow

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10
Q

Deficient in Parkinson’s disease

A

Dopamine

Regulates Na excretion, renal function
Reward stimulus relevant to addiction
Target for antipsychotic drugs

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11
Q

Norepinephrine drug

A

Levarterenol

Increase in peripheral resistance, SBP, DBP
Inotropism, chronotropism

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12
Q

Direct-acting selective alpha 1 agonist for mydriasis and decongestion

A

Phenylephrine

Increase BP

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13
Q

Direct-acting selective alpha 1 agonist for orthostatic hypotension

A

Midorine

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14
Q

Direct-acting selective alpha 2 agonist/s for hypertension

A

Clonidine
Methyldopa

Lowers BP through CNS effects which decrease sympathetic tone

A/E: sedation

*Remember PCDT

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15
Q

Direct-acting non-selective agonist for decongestion (topical)

A

Oxymetazoline (a1 a2)

Newer drug for sedation in the ICU

A/E: hypotension (central clonidine-like effect)

*Remember OIEN

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16
Q

Direct-acting non-selective agonist for vasodilation

A

Isoproterenol (b1 b2)

Inotropism, chronotropism

*Remember OIEN

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17
Q

Direct-acting selective beta 1 agonist of choice for cardiogenic shock

A

Dobutamine

Resembles dopamine
Inotropism

*Remember PCDT

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18
Q

Direct-acting selective beta 2 agonist for asthma and suppression of premature labor

A

Terbutaline

*Remember PCDT

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19
Q

Mixed-acting agonist that can cross the BBB and is centrally-acting

A

Ephedrine

Increased bioavailability and longer duration

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20
Q

Indirect-acting releasing agonist for mood stimulation, alertness, and appetite suppression

A

Amphetamine (I’m wide awake and not hungry)

Mediated through release of NE

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21
Q

Indirect-acting releasing agonist for ADHD

A

Methylphenidate

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22
Q

Indirect-acting releasing agonist for increased wakefulness in narcolepsy

A

Modafinil

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23
Q

Indirect-acting releasing agonist that is metabolized by MAO

A

Tyramine

Increased hepatic first pass = decreased bioavailability

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24
Q

Indirect-acting catecholamine-reuptake inhibitor agonist for ADHD

A

Atomoxetine

Selective inhibition of NE receptor transporter

AA

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25
Q

Indirect-acting catecholamine-reuptake inhibitor agonist for depression

A

Duloxetine

DD

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26
Q

Dopamine agonist for Parkinson’s disease and prolactinemia

A

Levodopa

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27
Q

Dopamine agonist for hypertension (IV)

A

Fenoldopam (d1)

Selective peripheral vasodilation

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28
Q

Chronic orthostatic hypotension - agonist

A

Midorine (a1)

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29
Q

Cardia arrest - agonist

A

Epinephrine (a1 a2 b1 b2)

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30
Q

Cardiac stress test - agonist

A

Dobutamine (b1)

31
Q

Local vasoconstriction - agonist

A

Epinephrine (a1 a2 b1 b2)

32
Q

Asthma - agonist

A

Terbutaline (b2)
Albuterol
Metaproterenol

33
Q

COPD - agonist

A

Long-acting b2 agonists or LABAs
Formoterol
Salmeterol
Bambuterol

-terols

34
Q

Mydriasis - agonist

A

Phenylephrine (a1)

35
Q

Glaucoma - agonist

A

Apraclonidine (has clonidine in its name so it’s a2)

Brimonidine

36
Q

Suppresses premature labor - agonist

A

Terbutaline (b2)

Ritodrine

37
Q

Narcolepsy - agonist

A

Modafinil (indirect releasing)

38
Q

ADHD - agonist

A

Methylphenidate (indirect releasing)
Clonidine (a2)
Guanfacine

39
Q

Sedation - agonist

A

Dexmedetomidine (a2, like Clonidine, Methyldopa)

40
Q

Alpha receptor reversible antagonists

A

Phentolamine
Prazosin

Do dissociate
Can be overcome with high concentrations

Decrease peripheral vascular resistance and BP
Prevent pressor effects
Cause orthostatic hypotension and reflex tachycardia
Miosis
Nasal stuffiness
Treatment of urinary retention (BPH)

41
Q

Alpha receptor irreversible antagonist

A

Phenoxybenzamine

Does not dissociate
Cannot be overcome with high concentrations

Decrease peripheral vascular resistance and BP
Prevent pressor effects
Cause orthostatic hypotension and reflex tachycardia
Miosis
Nasal stuffiness
Treatment of urinary retention (BPH)

42
Q

Treatment for hypertension, angina, chronic heart failure, after myocardial infarction - antagonist

A

Beta receptor antagonists

Lowers BP
Acute - increase in peripheral resistance
Chronic - decrease in peripheral resistance (works like an agonist)

43
Q

Treatment for glaucoma (reduce IOP due to decreased aqueous humor production) - antagonist

A

Beta receptor antagonists

44
Q

Selective alpha 1 antagonist

A

Prazosin - prototype?
Terazosin
Doxazosin
Tamsulosin

-osin

45
Q

Selective alpha 2 antagonist

A

Yohimbine - prototype

46
Q

Nonselective reversible alpha antagonist

A

Phentolamine

Phentolamine is shorter than Phenoxybenzamine
Reversible is shorter than irreversible

47
Q

Nonselective irreversible alpha antagonist

A

Phenoxybenzamine

Phenoxybenzamine is longer than Phentolamine
Irreversible is longer than reversible

48
Q

Pheochromocytoma (nonselective, irreversible antagonist)

A

Phenoxybenzamine

Inhibits reuptake of released NE
Blocks histamine, acetylcholine, serotonin, alpha receptors
Vasodilation

A/E: orthostatic hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation

PhePhe

49
Q

Pheochromocytoma (nonselective, reversible antagonist)

A

Phentolamine

Lowers peripheral resistance
Presynaptic a2 blockade -> cardiac stimulation

A/E: severe tachycardia, arrhythmias, myocardial ischemia

PhePhe

50
Q

Hypertension (selective alpha 1 antagonist)

A

Prazosin
Relative absence of tachycardia
Relaxes both arterial and venous smooth muscles and smooth muscles in the prostate
Half-life: 3 hours

Terazosin
Urinary retention symptom treatment (BPH)
Half-life: 9-12 hours

Doxazosin
BPH treatment
Half-life: 22 hours

51
Q

Greater potency in inhibiting contraction in prostate smooth muscles (relaxation) - antagonist

A

Tamsulosin

High bioavailability
Half-life: 9-15 hours
Increased risk for intraoperative floppy iris syndrome (IFIS)

52
Q

Male erectile dysfunction and orthostatic hypotension - antagonist

A

Yohimbine

Promotes increased NE release (CNS and periphery)
Reverses antihypertensive effect of Clonidine

53
Q

Hypertensive emergencies - antagonist

A

Labetalol

54
Q

Peripheral vascular disease - antagonist

A

Prazosin
Phenoxybenzamine

PP

55
Q

Urinary obstruction - antagonist

A

Prazosin
Doxazosin
Terazosin

PDT

56
Q

Erectile dysfunction - antagonist

A

Yohimbine

57
Q

Selective beta 2 antagonist

A

Butoxamine

58
Q

Selective beta 1 antagonists

A
Betaxolol, Bisoprolol
Esmolol
Atenolol*
Metoprolol
Nebivolol
Celliprolol

BEAM NC (nice)

59
Q

Nonselective beta antagonists

A

Nadolol
Sotalol
Timolol
Propanolol - prototype

NSTP

60
Q

Most highly selective beta 1 antagonist / most cardioselective

A

Nebivolol (third generation blocker)

Vasodilation
Increase insulin sensitivity

61
Q

Nonselective beta antagonist with ocular hypotensive effects

A

Timolol

62
Q

Selective beta 1 antagonist for glaucoma (topical)

A

Betaxolol

63
Q

Reversible beta antagonist

A

Labetolol

Induced hypotension with less tachycardia

64
Q

Nonselective beta antagonist for chronic heart failure

A

Carvidelol

Half-life: 6-8 hours

65
Q

Ultra short-acting selective beta 1 antagonist for supraventricular arrhythmias

A

Esmolol

Half-life: 10 minutes

66
Q

Ischemic heart disease - antagonist

A

Timolol
Metoprolol
Propanolol

TMP (timp)

67
Q

Cardiac arrhythmias - antagonist

A

Esmolol
Sotalol

ES

68
Q

Heart failure - antagonist

A

Carvidelol
Metoprolol
Bisoprolol

CMB (comb)

69
Q

Glaucoma - antagonist

A

Timolol
Metipranolol
Betaxolol
Levobunolol

TMBL (timble)

70
Q

Hyperthyroidism - antagonist

A

Propanolol

71
Q

Migraine - antagonist

A
Propanolol
Atenolol
Timolol
Metoprolol
Nadolol

PAT MN (pat men)

72
Q

Performance anxiety and alcohol withdrawal - antagonist

A

Propanolol

73
Q

Major common cardiac A/E for antagonists

A

Bradycardia