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 antagonists) (PM)

A

Phenylephrine, Methoxamine (discontinued)

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15
Q

Used for the treatment of hypotension (Examples of selective α1 antagonists) (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 antagonists)

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 antagonists)

A

Clonidine

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18
Q

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

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 antagonists)

A

Guanfacine

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20
Q

Used as an antihypertensive (Examples of selective α2 antagonists)

A

Guanabenz

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21
Q

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

A

Moxonidine

22
Q

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

A

Dexmedetomidine

23
Q

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

A

Tizanidine

24
Q

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

A

Isoproterenol (Isoprenaline)

25
Q

Used for short-term treatment of cardiac decompensation and is the inotropic of choice in cardiogenic shock (Examples of selective β1 agonists)

A

Dobutamine

26
Q

Metaproterenol, albuterol, and levalbuterol are examples of __________ selective β2 agonists

A

Short-acting (SABA)

27
Q

Salmeterol, forrmoterol, and arformoterol are examples of __________ selective β2 agonists

A

Long-acting (LABA)

28
Q

Indacaterol, olodaterol, and vilanterol are examples of __________ selective β1 agonists

A

Very long-acting (VLABA)

29
Q

__________ agonists are used as the DOC for acute asthmatic bronchoconstriction, COPD, and used as a tocolytic

A

Selective β2

30
Q

Used for incontinence; induces detrusor muscle relaxation and increased bladder capacity (Examples of selective β3 agonists)

A

Mirabegron

31
Q

3 examples of mixed-acting sympathomimetics (EPP)

A

Ephedrine, Pseudoephedrine, Phenylpropanolamine

32
Q

Has been used in China; used for asthma, promote urinary incontinence, and hypotension in spinal anesthesia (Examples of mixed-acting sympathomimetics)

A

Ephedrine

33
Q

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)

A

Pseudoephedrine

34
Q

Used as a nasal decongestant and appetite suppressant; withdrawn in the US due to risk of hemorrhagic stroke (Examples of mixed-acting sympathomimetics)

A

Phenylpropanolamine

35
Q

A racemic mixture of β-phenylisopropylamine; used for narcolepsy and ADHD (Examples of indirect-acting sympathomimetics: releasing agents)

A

Amphetamine

36
Q

Widely abused as a cheap, accessible recreational drug (Examples of indirect-acting sympathomimetics: releasing agents)

A

Methamphetamine/N-methylamphetamine/Crystal meth/Shabu

37
Q

An amphetamine variant; used for narcolepsy and is a first-line drug for ADHD in children (Examples of indirect-acting sympathomimetics: releasing agents)

A

Methylphenidate

38
Q

A normal byproduct of tyrosine metabolism; produced in high concentrations in protein-rich foods (Examples of indirect-acting sympathomimetics: releasing agents)

A

Tyramine

39
Q

Inhibits norepinephrine transporter (NET) and dopamine transporter (DAT); used as a first-line agent for narcolepsy (Examples of indirect-acting sympathomimetics: reuptake inhibitors)

A

Modafinil

40
Q

Has a shorter but more intense effect than amphetamine; used as a local anesthetic (Examples of indirect-acting sympathomimetics: reuptake inhibitors)

A

Cocaine (coke)

41
Q

Used for pheochromocytoma and reversal of soft tissue anesthesia; its adverse effects include orthostatic hypotension and inhibition of ejaculation (Examples of α1α2 antagonists) (PP)

A

Phentolamine, Phenoxybenzamine

42
Q

Ergot alkaloids, which are examples of α1α2 antagonists, are sourced from the fungi __________ and __________ (CP, CP)

A

Claviceps purpurea, Claviceps paspali

43
Q

2 examples of ergot alkaloids (ED)

A

Ergotamine, Dyhydroergotamine

44
Q

__________ are the first adrenergic receptor antagonists to be discovered

A

Ergot alkaloids

45
Q

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)

A

Prazosin, Tamsulosin, Idoramin, Urapidil

46
Q

An indolealkylamine alkaloid from Pausinystalia yohimba bark and in Rauwolfia serpentina root; formerly used for erectile dysfunction (Examples of α2 antagonists)

A

Yohimbine

47
Q

Propanolol, nadolol, penbutolol, pindolol, and timolol are examples of __________ β antagonists

A

1st generation (Nonselective)

48
Q

Metoprolol, acebutolol, atenolol, bisoprolol, and esmolol are examples of __________ β antagonists

A

2nd generation (β1 selective)

49
Q

Carteolol, carvedilol, and labetalol are examples of __________ β antagonists

A

3rd generation (Nonselective w/ additional CV actions)

50
Q

Betaxolol, celiprolol and nebivolol are examples of __________ β antagonists

A

3rd generation (β1 selective with additional CV actions)