PRELIM 07 - Adrenergic Agonists and Antagonists Flashcards

1
Q

Parent compound found in sympathomimetics

A

β-phenylethylamine

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2
Q

Bind to and activate alpha and/or beta receptors (Types of sympathomimetics)

A

Direct-acting sympathomimetics

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3
Q

3 examples of endogenous catecholamines (END)

A

Epinephrine, Norepinephrine, Dopamine

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4
Q

A nonselective α1α2 and β1β2 agonist; is a major hormone secreted by the adrenal medulla (Examples of endogenous catecholamines)

A

Epinephrine

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5
Q

Serves as the DOC for anaphylactic shock (Examples of endogenous catecholamines)

A

Epinephrine

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6
Q

2 other names of norepinephrine (LN)

A

Levarterenol, Noradrenaline

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7
Q

A nonselective α1α2 and β1 agonist; is the major neurotransmitter in postganglionic sympathetic nerves (Examples of endogenous catecholamines)

A

Norepinephrine

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8
Q

A compensatory vagal reflex that slows down heart rate and blood pressure in response to increased blood pressure; involves norepinephrine

A

Baroreceptor reflex

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9
Q

Used to raise or support blood pressure under certain intensive care conditions and is the vasopressor of choice in cardiogenic and septic shock (Examples of endogenous catecholamines)

A

Norepinephrine

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10
Q

A nonselective D1 = D2 > β1 > α1 agonist; is the major neurotransmitter in the CNS and is involved in the reward stimulus relevant to addiction (Examples of endogenous catecholamines)

A

Dopamine

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11
Q

Is used for congestive heart failure, and cardiogenic and septic shock (Examples of endogenous catecholamines)

A

Dopamine

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12
Q

Dopamine overdose can lead to __________

A

Excessive sympathomimetic activity

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13
Q

Used as a topical nasal decongestant (Examples of nonselective α1α2 agonists) (ONX)

A

Oxymetazoline, Naphazoline, Xylometazoline

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14
Q

Used as a nasal decongestant and mydriatic (Examples of selective α1 agonists) (PM)

A

Phenylephrine, Methoxamine (discontinued)

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15
Q

Used for the treatment of hypotension (Examples of selective α1 agonists) (MM)

A

Metaraminol, Mephentermine

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16
Q

A prodrug of desglymidodrine; used for the treatment of postural (orthostatic) hypotension (Examples of selective α1 agonists)

A

Midodrine

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17
Q

A 2-imidazoline derivative used for the treatment of hypertension; its adverse effects include xerostomia, sedation, and withdrawal syndrome (Examples of selective α2 agonists)

A

Clonidine

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18
Q

A prodrug of α-methylnorepinephrine; used as an antihypertensive (Examples of selective α2 agonists)

A

Methyldopa

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19
Q

More selective for α2 than Clonidine; used as an antihypertensive; its SR form is used for ADHD (Examples of selective α2 agonists)

A

Guanfacine

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20
Q

Used as an antihypertensive (Examples of selective α2 agonists)

A

Guanabenz

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21
Q

Used as an antihypertensive and analgesic (Examples of selective α2 agonists)

A

Moxonidine

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22
Q

Used as a sedative before anesthesia (Examples of selective α2 agonists)

A

Dexmedetomidine

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23
Q

Used as a muscle relaxant (Examples of selective α2 agonists)

A

Tizanidine

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24
Q

Used for bradycardia or heart block (Examples of nonselective β1β2 agonists)

A

Isoproterenol (Isoprenaline)

25
Used for short-term treatment of cardiac decompensation and is the inotropic of choice in cardiogenic shock (Examples of selective β1 agonists)
Dobutamine
26
Metaproterenol, albuterol, and levalbuterol are examples of __________ selective β2 agonists
Short-acting (SABA)
27
Salmeterol, forrmoterol, and arformoterol are examples of __________ selective β2 agonists
Long-acting (LABA)
28
Indacaterol, olodaterol, and vilanterol are examples of __________ selective β2 agonists
Very long-acting (VLABA)
29
__________ agonists are used as the DOC for acute asthmatic bronchoconstriction, COPD, and used as a tocolytic
Selective β2
30
Used for incontinence; induces detrusor muscle relaxation and increased bladder capacity (Examples of selective β3 agonists)
Mirabegron
31
3 examples of mixed-acting sympathomimetics (EPP)
Ephedrine, Pseudoephedrine, Phenylpropanolamine
32
Has been used in China; used for asthma, promote urinary incontinence, and hypotension in spinal anesthesia (Examples of mixed-acting sympathomimetics)
Ephedrine
33
One of the 4 ephedrine enantiomers; used as a nasal decongestant (OTC); can be used as a precursor for meth (Examples of mixed-acting sympathomimetics)
Pseudoephedrine
34
Used as a nasal decongestant and appetite suppressant; withdrawn in the US due to risk of hemorrhagic stroke (Examples of mixed-acting sympathomimetics)
Phenylpropanolamine
35
A racemic mixture of β-phenylisopropylamine; used for narcolepsy and ADHD (Examples of indirect-acting sympathomimetics: releasing agents)
Amphetamine
36
Widely abused as a cheap, accessible recreational drug (Examples of indirect-acting sympathomimetics: releasing agents)
Methamphetamine/N-methylamphetamine/Crystal meth/Shabu
37
An amphetamine variant; used for narcolepsy and is a first-line drug for ADHD in children (Examples of indirect-acting sympathomimetics: releasing agents)
Methylphenidate
38
A normal byproduct of tyrosine metabolism; produced in high concentrations in protein-rich foods (Examples of indirect-acting sympathomimetics: releasing agents)
Tyramine
39
Inhibits norepinephrine transporter (NET) and dopamine transporter (DAT); used as a first-line agent for narcolepsy (Examples of indirect-acting sympathomimetics: reuptake inhibitors)
Modafinil
40
Has a shorter but more intense effect than amphetamine; used as a local anesthetic (Examples of indirect-acting sympathomimetics: reuptake inhibitors)
Cocaine (coke)
41
Used for pheochromocytoma and reversal of soft tissue anesthesia; its adverse effects include orthostatic hypotension and inhibition of ejaculation (Examples of α1α2 antagonists) (PP)
Phentolamine, Phenoxybenzamine
42
Ergot alkaloids, which are examples of α1α2 antagonists, are sourced from the fungi __________ and __________ (CP, CP)
Claviceps purpurea, Claviceps paspali
43
2 examples of ergot alkaloids (ED)
Ergotamine, Dyhydroergotamine
44
__________ are the first adrenergic receptor antagonists to be discovered
Ergot alkaloids
45
Used for hypertension, CHF, and for urinary retention in benign prostatic hyperplasia (BPH); its adverse effects include the first-dose effect (Examples of α1 antagonists) (PTIU)
Prazosin, Tamsulosin, Idoramin, Urapidil
46
An indolealkylamine alkaloid from Pausinystalia yohimba bark and in Rauwolfia serpentina root; formerly used for erectile dysfunction (Examples of α2 antagonists)
Yohimbine
47
Propanolol, nadolol, penbutolol, pindolol, and timolol are examples of __________ β antagonists
1st generation (Nonselective)
48
Metoprolol, acebutolol, atenolol, bisoprolol, and esmolol are examples of __________ β antagonists
2nd generation (β1 selective)
49
Carteolol, carvedilol, and labetalol are examples of __________ β antagonists
3rd generation (Nonselective w/ additional CV actions)
50
Betaxolol, celiprolol and nebivolol are examples of __________ β antagonists
3rd generation (β1 selective with additional CV actions)
51
Epinephrine results to positive inotropic and chronotropic effect via __________ receptor
β1
52
Epinephrine results to vasoconstriction in most blood vessels via __________ receptor
α1
53
Epinephrine results to vasodilation in some blood vessels (ex: skeletal muscle blood vessels) via __________ receptor
β2
54
Epinephrine results to inhibition of insulin secretion via __________ receptor
α2
55
Epinephrine results to promotion of insulin secretion via __________ receptor
β2
56
Epinephrine results to promotion of glucagon secretion via __________ receptor
β2
57
Epinephrine results to glycogenolysis via __________ and __________ receptor
α1, β2
58
Epinephrine results to lipolysis via __________ receptor (activates hormone-sensitive lipase)
β3
59
Epinephrine administered orally is inactivated by __________ and __________ (MC)
MAO, COMP