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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
Indirect-acting catecholamine-reuptake inhibitor agonist for depression
Duloxetine DD
26
Dopamine agonist for Parkinson's disease and prolactinemia
Levodopa
27
Dopamine agonist for hypertension (IV)
Fenoldopam (d1) Selective peripheral vasodilation
28
Chronic orthostatic hypotension - agonist
Midorine (a1)
29
Cardia arrest - agonist
Epinephrine (a1 a2 b1 b2)
30
Cardiac stress test - agonist
Dobutamine (b1)
31
Local vasoconstriction - agonist
Epinephrine (a1 a2 b1 b2)
32
Asthma - agonist
Terbutaline (b2) Albuterol Metaproterenol
33
COPD - agonist
Long-acting b2 agonists or LABAs Formoterol Salmeterol Bambuterol -terols
34
Mydriasis - agonist
Phenylephrine (a1)
35
Glaucoma - agonist
Apraclonidine (has clonidine in its name so it's a2) | Brimonidine
36
Suppresses premature labor - agonist
Terbutaline (b2) | Ritodrine
37
Narcolepsy - agonist
Modafinil (indirect releasing)
38
ADHD - agonist
Methylphenidate (indirect releasing) Clonidine (a2) Guanfacine
39
Sedation - agonist
Dexmedetomidine (a2, like Clonidine, Methyldopa)
40
Alpha receptor reversible antagonists
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
Alpha receptor irreversible antagonist
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
Treatment for hypertension, angina, chronic heart failure, after myocardial infarction - antagonist
Beta receptor antagonists Lowers BP Acute - increase in peripheral resistance Chronic - decrease in peripheral resistance (works like an agonist)
43
Treatment for glaucoma (reduce IOP due to decreased aqueous humor production) - antagonist
Beta receptor antagonists
44
Selective alpha 1 antagonist
Prazosin - prototype? Terazosin Doxazosin Tamsulosin -osin
45
Selective alpha 2 antagonist
Yohimbine - prototype
46
Nonselective reversible alpha antagonist
Phentolamine Phentolamine is shorter than Phenoxybenzamine Reversible is shorter than irreversible
47
Nonselective irreversible alpha antagonist
Phenoxybenzamine Phenoxybenzamine is longer than Phentolamine Irreversible is longer than reversible
48
Pheochromocytoma (nonselective, irreversible antagonist)
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
Pheochromocytoma (nonselective, reversible antagonist)
Phentolamine Lowers peripheral resistance Presynaptic a2 blockade -> cardiac stimulation A/E: severe tachycardia, arrhythmias, myocardial ischemia PhePhe
50
Hypertension (selective alpha 1 antagonist)
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
Greater potency in inhibiting contraction in prostate smooth muscles (relaxation) - antagonist
Tamsulosin High bioavailability Half-life: 9-15 hours Increased risk for intraoperative floppy iris syndrome (IFIS)
52
Male erectile dysfunction and orthostatic hypotension - antagonist
Yohimbine Promotes increased NE release (CNS and periphery) Reverses antihypertensive effect of Clonidine
53
Hypertensive emergencies - antagonist
Labetalol
54
Peripheral vascular disease - antagonist
Prazosin Phenoxybenzamine PP
55
Urinary obstruction - antagonist
Prazosin Doxazosin Terazosin PDT
56
Erectile dysfunction - antagonist
Yohimbine
57
Selective beta 2 antagonist
Butoxamine
58
Selective beta 1 antagonists
``` Betaxolol, Bisoprolol Esmolol Atenolol* Metoprolol Nebivolol Celliprolol ``` BEAM NC (nice)
59
Nonselective beta antagonists
Nadolol Sotalol Timolol Propanolol - prototype NSTP
60
Most highly selective beta 1 antagonist / most cardioselective
Nebivolol (third generation blocker) Vasodilation Increase insulin sensitivity
61
Nonselective beta antagonist with ocular hypotensive effects
Timolol
62
Selective beta 1 antagonist for glaucoma (topical)
Betaxolol
63
Reversible beta antagonist
Labetolol Induced hypotension with less tachycardia
64
Nonselective beta antagonist for chronic heart failure
Carvidelol Half-life: 6-8 hours
65
Ultra short-acting selective beta 1 antagonist for supraventricular arrhythmias
Esmolol Half-life: 10 minutes
66
Ischemic heart disease - antagonist
Timolol Metoprolol Propanolol TMP (timp)
67
Cardiac arrhythmias - antagonist
Esmolol Sotalol ES
68
Heart failure - antagonist
Carvidelol Metoprolol Bisoprolol CMB (comb)
69
Glaucoma - antagonist
Timolol Metipranolol Betaxolol Levobunolol TMBL (timble)
70
Hyperthyroidism - antagonist
Propanolol
71
Migraine - antagonist
``` Propanolol Atenolol Timolol Metoprolol Nadolol ``` PAT MN (pat men)
72
Performance anxiety and alcohol withdrawal - antagonist
Propanolol
73
Major common cardiac A/E for antagonists
Bradycardia

Pharmacology (5 decks)

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