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Pharmacology > Adrenergics > Flashcards

Adrenergics Flashcards

1
Q

Phenylephrine: Brand Name

A

Neosynephrine

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2
Q

Phenylephrine: Description

A

Synthetic alpha-receptor agonist, alpha1»alpha2

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3
Q

Phenylephrine: Actions

A

Produce vasoconstriction and venoconstriction by stimulating contraction of vascular smooth muscle cells

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4
Q

Phenylephrine: Indications (3)

A

Nasal decongestant
Mydriatic (dilate pupil for eye exam)
Increase BP in vasodilated state

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5
Q

Phenylephrine: Other facts (3)

A

Less potent vasoconstrictor than NE
Not inactivated by COMT
Topical (eye, nose), IV (increase BP)

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6
Q

Clonidine: Brand name

A

Catapres

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7
Q

Clonidine: Description

A

Synthetic and selective alpha-2 receptor agonist

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8
Q

Clonidine: Actions

A

Stimulate alpha-2 receptors in brainstem -> down-regulation of SNS

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9
Q

Clonidine: Indications (2)

A

Treat HTN

Treat/prevent migraine

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10
Q

Clonidine: Other Facts (3)

A

May be given orally or patch
Causes sedation and dry mouth
If given IV or OD can cause increased BP

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11
Q

Isoproterenol: Brand Name

A

Isuprel

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12
Q

Isoproterenol: Description

A

Synthetic beta-1 and beta-2 receptor agonist

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13
Q

Isoproterenol: Action

A

Potent agonist at both beta receptors

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14
Q

Isoproterenol: Indications (3)

A

Increase cardiac contractility
Increase HR
Increase cardiac conduction

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15
Q

Isoproterenol: Other facts (3)

A

Given intravenously
No longer used as much in CCU
Also causes vasodilatation, tachyarrhythmias

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16
Q

Dobutamine: Brand name

A

Dobutrex

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17
Q

Dobutamine: Description

A

Synthetic beta-1 receptor agonist, with very little alpha stimulation at high doses

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18
Q

Dobutamine: Actions

A

Potent agonist at beta-1 receptors in heart (increase contractility) and blood vessels (dilates renal and mesenteric vessels

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19
Q

Dobutamine: Indications (2)

A

Increases cardiac contractility more than HR

Useful in CCU for pts in cardiogenic shock, where you do not want to produce tachycardia (eg post MI)

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20
Q

Dobutamine: Other facts (2)

A

Given as IV infusion

Side effects: unwanted tachycardia, HTN, ectopy

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21
Q

Albuterol: Brand name

A

Ventolin

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22
Q

Albuterol: Description

A

Synthetic selective beta-2 (»beta-1, esp at low doses) receptor agonist

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23
Q

Albuterol: Action

A

Potent agonist at beta-2 receptors on smooth muscle cells in airways

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24
Q

Albuterol: Indications (2)

A

Prompt-acting rescue inhaler for asthma, COPD (bronchodilator)
Inhibit premature labor (relaxes smooth muscle cells in uterus)

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25
Q

Albuterol: Other facts (4)

A

Most often given as MDI
Can be given via nebulizer
Rarely given as IV infusion
Side effects: anxiety, tachycardia, tremor

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26
Q

Mirabegron: Brand name

A

Myrbetriq

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27
Q

Mirabegron: Description

A

Synthetic selective beta-3 receptor agonist (»beta-1 and -2)

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28
Q

Mirabegron: Actions (2)

A

Stimulation of beta-3 receptors in smooth muscle of bladder

Reduces detrusor muscle tone

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29
Q

Mirabegron: Indications (3)

A

Treatment of pts with overactive bladder with features of urinary urgency or frequency
Increases bladder capacity
No anticholinergic symptoms

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30
Q

Mirabegron: Other facts (2)

A

Approved by FDA in June 2012

Administered orally as extended release tablets

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31
Q

Dopamine: Description

A

Endogenous/synthetic agonist at DA, beta-1, and alpha-1 receptors

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32
Q

Dopamine: Actions (3)

A

Relative potency depends somewhat on dose being delivered
DA agonist = low dose
Beta-1 agonist = medium dose
Alpha-1 agonist = high dose

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33
Q

Dopamine: Indications (2)

A

Shock of various etiologies in ICU

Can -> increased contractility (b1), vasoconstriction (a1), and improved mesenteric and renal perfusion (DA)

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34
Q

Dopamine: Other facts

A

Given IV, preferably for short duration

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35
Q

Ephedrine: Description

A

Alkaloid obtained from plant

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36
Q

Ephedrine: Actions (2)

A

Acts indirectly to release NE from adrenergic nerve endings

Also some direct agonism at receptors

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37
Q

Ephedrine: Indications (2)

A

Mild to moderate hypotension during surgery

Nasal congestion

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38
Q

Ephedrine: Other facts (4)

A

Prolonged duration of action
Potent CNS stimulant
Side effects: HTN, insomnia
Banned OTC

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39
Q

Pseudoephedrine: Brand name

A

Sudafed

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40
Q

Pseudoephedrine: Description

A

Synthetic derivative of ephedrine

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41
Q

Pseudoephedrine: Actions (2)

A

Acts indirectly to release NE from adrenergic nerve endings

Some direct agonism at alpha and beta receptors

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42
Q

Pseudoephedrine: Indications (2)

A

Nasal and sinus decongestant

Less ability to dilate bronchioles than ephedrine

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43
Q

Pseudoephedrine: Other facts (3)

A

Need to report bulk sales
Locked behind counter, need ID to purchase
Risk of death for kids <2

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44
Q

Amphetamine: Description

A

Synthetic compound similar to ephedrine

45
Q

Amphetamine: Actions

A

Acts indirectly to release NE from adrenergic nerve endings

46
Q

Amphetamine: Indications (3)

A

Obesity
Narcolepsy
ADHD
(none FDA approved)

47
Q

Amphetamine: Other facts (2)

A

V. high risk of dependence

Insomnia, restlessness, tremor

48
Q

Tyramine: Description (2)

A

Naturally occurring byproduct of tyrosine metabolism

Present in many aged or fermented foods - red wine, smelly cheeses, pickled herring

49
Q

Tyramine: Actions

A

Acts indirectly to release NE from adrenergic nerve endings

50
Q

Tyramine: Indications (3)

A

Obesity
Narcolepsy
ADHD
(none FDA approved)

51
Q

Tyramine: Other facts (3)

A

Metabolized in liver by MAO
Caution in pts on MAOIs
Chance of food/drug interaction

52
Q

Cocaine: Description

A

Naturally occurring but purified alkaloid extracted from coca plant

53
Q

Cocaine: Actions (3)

A

Acts indirectly to block reuptake of NE (also epi, DA) at synapse
Can stimulate release of NE, epi, and DA from neuron
Also acts as local anesthetic and CNS stimulant

54
Q

Cocaine: Indications (2)

A 
Nose bleeds (anesthesia + vasoconstriction)
Anesthesia for corneal surgery
55
Q

Cocaine: Other facts (4)

A

CNS stimulation more intense, shorter lasting than amphetamine
Can be smoked, snorted, or injected
Side effects: HTN, tachycardia, arrhythmias, seizures, MI
Controlled substance

56
Q

Prazosin: Brand name

A

Minipress

57
Q

Prazosin: Drug class (3)

A

Pharmacologic: selective alpha-1 adrenoceptor blocker
Therapeutic: antihypertensive, treatment of BPH (not as good as tamsulosin)

58
Q

Prazosin: Pharmacodynamics (1)

A

Blocks alpha-1 receptors on arterioles and veins -> inhibits NE-mediated vasoconstriction and venoconstriction

59
Q

Prazosin: Pharmacokinetics (4)

A

Available po or transdermal
Variable oral bioavailability (60%)
Onset 2h, duration 12-24h
Extensively metabolized in liver

60
Q

Prazosin: Toxicity

A

Excessive hypotension with passing out, esp. orthostatic and in pts on diuretics (this is why it’s not first line therapy)

61
Q

Prazosin: Interactions

A

Additive effects with most other antiHTVs, esp. diuretics

62
Q

Prazosin: Special considerations (2)

A

Start gradually, at bedtime, to avoid first-time passing out

Male pts with BPH?

63
Q

Prazosin: Indications/dose/route

A

Monotherapy: 1mg tid -> 20mg divided tid

64
Q

Prazosin: Monitor (3)

A

BP, weight, edema

65
Q

Tamsulosin: Brand name

A

Flomax

66
Q

Tamsulosin: Drug class (2)

A

Pharmacologic: selective alpha-1 adrenoceptor blocker
Therapeutic: treatment of obstructive symptoms of BPH

67
Q

Tamsulosin: Pharmacodynamics

A

Selectively blocks alpha-1 receptors, but preferentially in the prostate -> relaxation of smooth muscles in bladder neck and prostate -> improved urine flow, reduced symptoms

68
Q

Tamsulosin: Pharmacokinetics (3)

A

Completely absorbed after oral ingestion
>90% metabolized by CYP450 enzymes
Half life about 6 hours, duration of action up to 15 hrs (slow absorption)

69
Q

Tamsulosin: Toxicity (3)

A

Excessive hypotension with syncope, esp. orthostatic and in pts on diuretics
Allergic reactions
Decreased libido

70
Q

Tamsulosin: Interactions

A

Additive effects with most other antihypertensives, esp. diuretics

71
Q

Tamsulosin: Special considerations (3)

A

Rule out carcinoma of prostate before beginning treatment
Do not crush or chew (will speed absorption)
Can also be used to treat spasm of ureter in pts with kidney stones

72
Q

Tamsulosin: Indications/dose/route

A

For symptoms of BPH, 0.4mg po qd or bid; similar for renal colic from kidney stones

73
Q

Tamsulosin: Monitor

A

BP

74
Q

Phentolamine: Brand name

A

Regitine

75
Q

Phentolamine: Drug class (2)

A

Pharmacologic: non-selective competitive alpha-adrenoceptor blocker
Therapeutic: antihypertensive drug for pts with pheochromocytoma

76
Q

Phentolamine: Pharmacodynamics

A

Blocks ***alpha-1 and alpha-2 receptors at presynaptic and postsynaptic alpha receptors, decreasing preload and afterload

77
Q

Phentolamine: Pharmacokinetics (2)

A

**Only via IV (F=100%)

Plasma half life ~20min

78
Q

Phentolamine: Toxicity (3)

A

Excessive hypotension with syncope, esp. orthostatic and in pts on diuretics
Allergic reactions
Decreased libido

79
Q

Phentolamine: Interactions

A

Additive effects with most other antihypertensives, esp. diuretics

80
Q

Phentolamine: Special considerations (2)

A

Rule out carcinoma of prostate before beginning treatment

Can also be used to treat spasm of ureter in pts with kidney stones

81
Q

Phentolamine: Indications/dose/route (5)

A

Aid in Dx of pheo
***Treatment of intra-op HTN during pheo removal surgery
Prevention of dermal sloughing after extravasation of NE infusion
**Hypertensive crisis from sympathomimetic amines (tyramine - MAOI interaction) or overdose of cocaine

82
Q

Phentolamine: Monitor

A

BP

83
Q

Atenolol: Brand name, others in class

A 
Tenormin
Metoprolol (Toprol XL) - has most studies done
84
Q

Atenolol: Drug class (5)

A

Pharmacologic: specific beta-1 blocker
Therapeutic: antihypertensive, anti-arrhythmic, primary and secondary prevention of MI, antianginal

85
Q

Atenolol: Pharmacodynamics (2)

A

Binds directly to beta-1 receptors (beta-1»beta-2) -> lower BP via decreased CO and decreased RAAS activation
Less effective in preventing strokes than other drugs

86
Q

Atenolol: Pharmacokinetics (5)

A 
Available PO or iv
Variable oral F
Onset 1-2h, duration 12-24h
Can be given once per day
Renally excreted (longer half life)
Metoprolol has hepatic metabolism (shorter half life)
87
Q

Atenolol: Toxicity (4)

A

Excessive hypotension
Bradycardia
Heart block can worsen severe CHF (but indicated for mild to moderate CHF)
***Worsen bronchospasm in severe asthmatics

88
Q

Atenolol: Interactions (2)

A

Additive effects with most other antihypertensives

Additive AV block with CEBs

89
Q

Atenolol: Special considerations (4)

A

May be especially useful in HTN pts with exertional angina, MI, a fib
Watch out for abrupt withdrawal
No longer first line drug for essential HTN
Metoprolol needs to be taken several times per day

90
Q

Atenolol: Indications/dose/route

A

For treatment of hypertension, 25-100mg/day in one or two doses

91
Q

Atenolol: Monitor (3)

A

BP, HR, exercise tolerance

92
Q

Propranolol: Brand name

A

Inderal

93
Q

Propranolol: Drug class (5)

A

Pharmacologic: **non-specific beta-receptor blocker
Therapeutic: antihypertensive, antiarrhythmic, primary and secondary prevention of MI, anti-anginal

94
Q

Propranolol: Pharmacodynamics (2)

A

Binds directly to beta-1 and beta-2 receptors -> lower BP via decreased CO and decreased RAAS activation
Less effective in preventing strokes than other drugs

95
Q

Propranolol: Pharmacokinetics (4)

A

Available po or IV
Variable oral F
Onset 1-2h, duration 12-24h
Can be given once per day

96
Q

Propranolol: Toxicity (4)

A

Excessive hypotension
Bradycardia
Heart block can worsen severe CHF (but indicated for mild to moderate CHF)
***Worsen bronchospasm in severe asthmatics

97
Q

Propranolol: Interactions (2)

A

Additive effects with most other antihypertensives

Additive AV block with CEBs

98
Q

Propranolol: Special considerations (3)

A

May be especially useful in HTN pts with exertional angina, MI, a fib
Watch out for abrupt withdrawal
No longer first line drug for essential HTN

99
Q

Propranolol: Indications/dose/route

A

For treatment of hypertension, 25-100mg/day in one or two doses

100
Q

Propranolol: Monitor (3)

A

BP, HR, exercise tolerance

101
Q

Labetalol: Brand name, others in class

A

Trandate

Carvedilol/Coreg (know)

102
Q

Labetalol: Drug class (3)

A

Pharmacologic: mixed alpha and beta-receptor blocker
Therapeutic: antihypertensive, treatment of CHF (coreg)

103
Q

Labetalol: Pharmacodynamics (2)

A

Reduces BP by blocking access of NE to beta- and alpha-1 receptors
Pts differ in degree of beta-blockade vs alpha blockade

104
Q

Labetalol: Pharmacokinetics (3)

A

Excellent absorption but high first-pass effects -> F~25%
Onset 1-2h po, 2-5 min iv
Extensively metabolized in liver by IID6

105
Q

Labetalol: Toxicity (3)

A 
Avoid in pt with bradycardia, heart block, CHF, asthma, shock
Use with caution in pts with cardiomyopathy, pheo
Pregnancy class D
106
Q

Labetalol: Interactions

A

Additive effects with most other antihypertensives

107
Q

Labetalol: Special considerations (3)

A

Use reduced doses in pts with impaired liver function
Dizziness most troubling early side effect
Most often used for hypertensive crises

108
Q

Labetalol: Indications/dose/route

A

Most commonly given iv with initial small boluses of 20mg, followed by continuous infusion at 2mg/min
Not usually given po for chronic treatment

109
Q

Labetalol: Monitor (2)

A

BP, HR

Pharmacology (10 decks)

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