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Pharmacology > Adrenergics > Flashcards

Adrenergics Flashcards

1
Q

Direct acting adrenergic agonists:endogenous catecholamines (and D1 agonist) Drugs

A

Epinephrine
Norepinephrine
Dopamine
Fenoldopam

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2
Q

Epinephrine receptors

A

Alpha and beta2
Low dose: beta effects (vasodilation)
High dose: alpha effects (vasoconstriction)

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3
Q

Epinephrine effect

A

High dose-> potent vasopressor : increases BP (systolic > diastolic) -> +ve chronotropic and inotropic effects (beta 1) and vasoconstriction (alpha 1) -> increases CO (and O2 demand from heart)

Bronchodilation (beta 2)
Relaxed GI smooth muscle with contracted sphincters
Relaxed detrusor (beta 2) and contracted sphincter (alpha 1)
Prostatic smooth mm. contraction

Metabolic: hyperglycemia due to increased glycogenolysis and glucagon release (beta 2); net inhibition of insulin secretion (alpha 2 inhibits while beta 2 enhances secretion)
Increased lipolysis through beta 3 activation (increased cAMP and HSL)

DOC for pts in anaphylactic shock; cardiac arrest, asthma attacks combined with local anesthetics to increase duration; glaucoma (decreased production of aqueous humor)

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4
Q

Epinephrine PK

A

Rapid onset
Brief duration

Administered through IV in emergencies

Other routes include SC, ET tube, inhalation, topically in the eye

Do not give orally due to inactivation by intestinal enzymes

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5
Q

Epinephrine Adverse

A

CNS disturbances: Restlessness, fear, apprehension, headache, tremor (may be secondary to effects outside of CNS)

ICH due to increased BP

Cardiac arrhythmias-especially in patients on digitalis

Pulmonary edema

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6
Q

Epinephrine “other”

A

Synthesized from tyrosine in the adrenal medulla

Polar molecule: does not enter CNS in therapeutic doses

Metabolized by COMT and MAO -> VMA and metanephrine

Hyperthyroid may enhance CV actions likely due to upregulation of receptors

Cocaine prevents reuptake

Beta blockers cause predominate alpha effects such as increased TPR and BP

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7
Q

Norepinephrine receptor

A

alpha and beta 1 >beta 2

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8
Q

Norepinephrine effect

A 
Vasoconstriction (alpha 1) -> increased PVR -> increased SBP/DBP and MAP
Bradycardia due to decreased sympathetic outflow following the baroreceptor response (indirect effect through M2)
Induces hyperglycemia (less potent than epi)
Limited therapy value: *can treat shock*, but dopamine is better due to preservation of renal blood flow
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9
Q

Norepinephrine adverse

A

NE may cause kidney shutdown

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10
Q

Norepinephrine Other

A

Baroreceptor reflex coutneracts local action which can be blocked by pretreatment with atropine -> reveals direct effect of tachycardia

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11
Q

Dopamine receptor

A

D, alpha, beta

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12
Q

Dopamine effect

A

Central regulator of movement

CVS: low doses vasodilate (D1 receptors, cAMP) especially at renal, mesenteric and coronary
DOC for cardiogenic and hypovolemic shock : increase GFR, renal blood flow and sodium excretion -> preservation of renal function

Inotropic effect at intermediate concentration (beta 1) and increasing release of NE

Increase in systolic BP

High concentration -> alpha 1 mediated vasoconstriction

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13
Q

Dopamine PK

A

Ineffective orally (metabolism by MAO and COMT)

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14
Q

Dopamine adverse

A

Overdose-> sympathomimetic symptoms

Can cause nausea, HTN, arrhythmia but is short lived due to rapid metabolism to HVA

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15
Q

Dopamine other

A

Dopamine does not cross BBB

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16
Q

Fenoldopam receptor

A

D1

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17
Q

Fenoldopam effect

A

Peripheral vasodilation -> used in short term management of inpatient HTN

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18
Q

Fenoldopam PK

A

give continuously via IV, not bolus

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19
Q

Direct acting adrenergic beta agonists

A 
Isoproterenol
Dobutamine
Terbutaline
Alburterol
Salmeterol
Formoterol
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20
Q

Isoproterenol receptor

A

Beta 1 and 2

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21
Q

Isoproterenol effect

A

CVS: increase CO through rate and force of contraction (AV block or C arrest)

Major Decrease in TPR through vasodilation (beta 2) because there is no alpha 1 opposing it
Slight increase in SBP, decrease in MAP and DBP, tachycardia

Bronchodilation and GI smooth muscle relaxation mediated by beta 2
Use stimulate heart in emergency

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22
Q

Isoproterenol PK

A

most reliable when given parenterally or inhaled

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23
Q

Isoproterenol adverse

A

similar adverse effects compared to epi:
CNS disturbances: Restlessness, fear, apprehension, headache, tremor (may be secondary to effects outside of CNS)

ICH due to increased BP

Cardiac arrhythmias-especially in patients on digitalis

Pulmonary edema

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24
Q

Dobutamine receptor

A

beta 1

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25
Q

Dobutamine effect

A

Acute management of congestive heart failure: increases contractility
Increases CO with little change in heart rate -> O2 demands of the myocardium are not significantly affected gives it an advantage over other sympathomimetics

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26
Q

Dobutamine PK

A

can build up tolerance with long term use

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27
Q

Dobutamine other

A

Racemic mixture: -ve alpha one and beat beta one agonist; +ve alpha 1 antagonist and potent beta 1 agonist
Net effect: selective Beta 1

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28
Q

Terbutaline receptor

A

Beta 2

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29
Q

Terbutaline effect

A

Bronchodilator
Emergency treatment of status asthmaticus
Reduces uterine contraction in premature labor

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30
Q

Terbutaline PK

A

Resorcinol ring -> not metabolized by COMT giving it a longer duration
Oral, Inhalation or SC

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31
Q

Terbutaline other

A

Selectivity is lost at high concentrations

Used in treatment of asthma without having effects on heart

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32
Q

Albuterol other

A

Selectivity is lost at high concentrations

Used in treatment of asthma without having effects on heart

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33
Q

Salmeterol and Formoterol other

A

Selectivity is lost at high concentrations

Used in treatment of asthma without having effects on heart

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34
Q

Albuterol Receptor

A

Beta 2

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35
Q

Salmeterol and Formoterol receptor

A

Beta 2

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36
Q

Albuterol effect

A

Inhalant bronchodilator; relief of symptoms in asthma

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37
Q

Salmeterol and Formoterol effect

A

Bronchodilator

Long acting-> not used for prompt relief of bronchospasm

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38
Q

Salmeterol and Formoterol PK

A

Slow onset, but prolonged action (12 hrs) after inhalation

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39
Q

Direct acting alpha agonist drugs

A

Phenylephrine
Clonidine
Methyldopa
Brimonidine

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40
Q

Phenylephrine receptor

A

alpha 1

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41
Q

Phenylephrine mechanism

A

Peripheral vasoconstriction

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42
Q

Phenylephrine effects

A

Vasoconstrictor: increase SBP and DBP
Nasal decongestant
Mydriasis
Tx of supraventricular tachycardia

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43
Q

Phenylephrine Other

A

NO direct effect on heart, but does cause reflex bradycardia after parenteral administration

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44
Q

Clonidine receptor

A

Alpha 2

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45
Q

Clonidine Mechanism

A

Partial agonist** : activation of central alpha 2 receptors suppresses sympathetic outflow

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46
Q

Clonidine effect

A

Antihypertensive

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47
Q

Clonidine PK

A

Acute rise in BP due to transient vasoconstriction when given IV, but not orally

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48
Q

Clonidine adverse

A

Centrally acting antiadrenergic drugs: sedation, mental lassitude, impaired concentration

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49
Q

Methyldopa adverse

A

Centrally acting antiadrenergic drugs: sedation, mental lassitude, impaired concentration

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50
Q

Methyldopa receptor

A

alpha 2

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51
Q

Methyldopa mechanism

A

Central acting anti HTN

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52
Q

Methyldopa effect

A

Metabolized to alpharmethylnorepinephrine which causes effects similar to clonidine: decrease TPR and BP
DOC in pregnant patients with HTN

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53
Q

Methyldopa adverse

A

Can cause +ve Coombs test or hemolytic anemia or hepatitis

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54
Q

Brimonidine receptor

A

alpha 2

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55
Q

Brimonidine mechanism

A

Decrease aqueous humor production along with increased outflow

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56
Q

Brimonidine effect

A

Decrease intraocular pressure in glaucoma

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57
Q

Indirect acting Adrenergic agonist drugs

A

Amphetamine
Methylphenidate
Tyramine

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58
Q

Amphetamine mechanism

A

Displaces catecholamines from storage vesicle
Weak inhibitor of MAO
Blocks catecholamine reuptake

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59
Q

Amphetamine Effect

A

Increase BP through alpha 1 and Beta effects
Central stimulatory action: alertness, decrease fatigue and appetite, insomnia
Tx of depression, narcolepsy, and appetite suppression (in the past)

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60
Q

Amphetamine adverse

A

Fatigue and depression follow stimulation

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61
Q

Amphetamine other

A

releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles

62
Q

Methyphenidate other

A

releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles

63
Q

Tyramine other

A

releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles

64
Q

Methyphenidate Mechanism

A

Structural analog of amphetamine

65
Q

Methyphenidate indication

A

Tx of ADHD in children

66
Q

Tyramine Indication

A

Not clinically useful, found in fermented foods (cheese and wine)

67
Q

Tyramine PK

A

Byproduct of tyrosine metabolism, normally oxidized by MAO

68
Q

Tyramine Adverse

A

**Serious vasopressor episodes in patients on MAO-I’s after release of NE***

69
Q

Cocaine Receptor

A

DAT
SERT
NET

70
Q

Cocaine mechanism

A

Blocks dopamine (major effect), serotonin, and NE transporters -> potentiation and prolonged effects

71
Q

Cocaine effect

A

Sympathomimetic

Therpeutic use: blockage of voltage gated sodium channels -> local anesthetic

72
Q

Cocaine Adverse

A

Intense euphoria from blockage of dopamine reuptake in limbic system

73
Q

Cocaine other

A

Monoamine reuptake inhibitor

74
Q

Atomoxetine receptor

A

NET

75
Q

Atomoxetine Mechanism

A

Selective NET inhibitor

76
Q

Atomoxetine Indication

A

Tx of ADHD

77
Q

Atomoxetine other

A

Monoamine reuptake inhibitor

78
Q

Ephedrine receptor

A

alpha and beta

79
Q

Ephedrine effect

A

Vasoconstriction and cardiac stimulation -> increase BP
Bronchodilation (prophylactic tx of asthma because it is slower onset and less potent than epi or isoproterenol)
Synergistic effect with Anti-AChE in treatment of myasthenia gravis
Mild CNS stimulation (alertness) and increased athletic performance

Pressor in spinal anesthetisa, works for MG; asthma

80
Q

Ephedrine PK

A

NOT a catecholamine -> poor substrate for COMT and MAO -> longer duration of action
Excellent oral absorption, enters CNS

Eliminated unchanged in urine

81
Q

Ephedrine Adverse

A

Herbal supplements banned in 2004 due to life threatening cardiovascular reactions

82
Q

Ephedrine other

A

Induces release of NE* and activates adrenergic receptors*

Use declining due to better drugs with fewer side effects

83
Q

Pseudoephedrine mechanism

A

ephedrine enantiomer

84
Q

Pseudoephedrine receptor

A

alpha and beta

85
Q

Pseudoephedrine effect

A

Nasal decongestant with an H1 histamine antagonist

86
Q

Alpha antagonist drugs

A 
Phenoxybenzamine
Phentolamine
Prazosin
Terzosin
Doxazosin
Tamsulosin
Yohimbine
87
Q

alpha 1 blockers

A

-osins

88
Q

Phenoxybenzamine receptor

A

non selective alpha

89
Q

Phenoxybenzamine mechanism

A

alkylation irreversibly blocks receptor

slightly alpha one selective
Also blocks H1, M and 5-HT receptors; inhibits NET

90
Q

Phenoxybenzamine effect

A

CVS: prevents vasoconstriction of peripheral blood vessels -> reflex tachycardia

Presynaptic alpha 2 block -> increase CO

91
Q

Phenoxybenzamine indications

A

DOC Pheochromocytoma blocks effects of excess catecholamines (may require a beta blocker to control tachycardia after alpha blockade is established)

Historically used to lower BP, but was unsuccessful (block presynaptic alpha 2)

92
Q

Phenoxybenzamine adverse

A 
Postural hypotension
Nasal stiffness
Nausea and vomiting
Inhibit ejaculation
Contraindicated in patients with decreased coronary perfusion due to reflex tachycardia
93
Q

Phenoxybenzamine contraindication

A

Patients with decreased coronary perfusion

94
Q

Phentolamine receptor

A

nonselective alpha

95
Q

Phentolamine mechanism

A

Reversible alpha blocker

Serotonin blocker
Muscarinic, H1 and H2 agonist

96
Q

Phentolamine indications

A

Dx and control hypertensive episodes of pheochromocytoma
Prevents dermal necrosis when NE extravasates
**Antihypertensive in stimulant OD, sudden withdrawal of sympatholytics (clonidine), interaction between MAO-Is and tyramine*

97
Q

Phentolamine adverse

A

Postural hypotension-baroreceptor reflex and alpha 2 blockade on cardiac nerves
Arrhythmia and angina

Contraindicated in patients with decreased coronary perfusion

98
Q

Prazosin receptor

A

Selective alpha 1

Useful in treatment of HTN

99
Q

Prazosin mechanism

A

decrease TPR through relaxation of arterial and venous smooth muscle

100
Q

Prazosin effects

A

decrease BP without reflex tachycardia (alpha2)
Decrease LDL/TAG, increase HDL
Improves urinary blood flow

101
Q

Prazosin Indications

A

Suppress sympathetic outflow from CNS

Tx of HTN, BPH

102
Q

Prazosin Adverse

A

Not the DOC for primary HTN

First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)

103
Q

Terazosin and Doxazosin receptor

A

Selective alpha 1

Useful for treatment of HTN

104
Q

Terazosin and Doxazosin mechanism

A

Structural analog of prazosin -> longer half life -> less frequent dosing
Decrease TPR through relaxation of arterial and venous smooth muscle

105
Q

Terazosin and Doxazosin effect

A

decrease BP without reflex tachycardia (alpha2)
Decrease LDL/TAG, increase HDL
Improves urinary blood flow

106
Q

Tamsulosin effect

A

Relaxes genitourinary smooth muscle

107
Q

Terazosin and Doxazosin indication

A

Suppress sympathetic outflow from CNS

Tx of HTN, BPH

108
Q

Tamsulosin indication

A

Used in treatment of BPH with little effect on BP

reduced orthostatic HTN

109
Q

Terazosin and Doxazosin adverse

A

Not the DOC for primary HTN

First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)

110
Q

Tamsulosin adverse

A

Not the DOC for primary HTN

First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)

111
Q

Tamsulosin receptor

A

Selective alpha 1

Treatment of HTN

112
Q

Tamsulosin mechanism

A

Selective for alpha1A receptor found in genitourinary smooth muscle

113
Q

Yohimbine receptor

A

alpha 2

114
Q

Yohimbine mechanism

A

alpha 2 blocker -> indirect adrenergic agonist

115
Q

Yohimbine effect

A

increase NE release -> increase BP

116
Q

Yohimbine indication

A

treatment of erectile dysfunction, but has been replaced by PDE-5 inhibitors

117
Q

Yohimbine contraindications

A

Can reverse effects of alpha 2 agonists (clonidine–bad!)

118
Q

Beta antagonist drugs

A 
Propranolol
Nadolol
Timolol
Atenolol
Metoprolol
Esmolol
119
Q

Propranolol receptor

A

Beta 1 and 2

120
Q

Propranolol mechanism

A 
CVS: decrease HR and contractility
Increase TPR (beta 2)

Metabolic: decrease glycogenolysis and glucagon secretion -> severe hypoglycemia in patients on insulin

121
Q

Propranolol indication/effect

A 
Used in treatment of:
HTN (through decreased CO, no the DOC)
Migraine (blocks vasodilation)
Hyperthyroidism
Chronic angina (decrease O2 requirements)
A-fib, MI (protective)
Performance anxiety/stage fright (DOC)*
Essential tremor
122
Q

Propranolol Adverse

A

Bronchoconstriction->contraindicated in patients with COPD or asthma; variant angina

Impair recovery from hypoglycemia in insulin dependent patients -> syncope. Mask signs (ex. tachycardia seen in such episodes)

CNS: sedation, dizziness, lethargy, fatigue, depression

123
Q

Propranolol other

A

Does not induce postural hypotension because alpha 1 receptors remain active

Reduce HDL, and increase LDL and TAGs (block activation of HSL) -beta 1 selectively actually improve the lipid profile

Abrupt withdrawal -> HTN

124
Q

Nadolol indication/effect

A

long term treatment of angina and HTN

125
Q

Timolol indication/effect

A

HTN, prophylaxis for migraines

Glaucoma (open angle)

126
Q

Atenolol and Metoprolol indication/effect

A

Management of HTN in patients with impaired pulmonary function or IDDM

127
Q

Atenolol and Metoprolol receptor

A

B1 cardioselective

128
Q

Timolol receptor

A

Beta 1 and 2

129
Q

Nadolol receptor

A

beta 1 and 2

130
Q

Esmolol receptor

A

beta 1 cardioselective

131
Q

Atenolol and Metoprolol other

A

less likely to produce bronchospasm

long term management of angina; s/p MI reduces mortality

132
Q

Esmolol indication/effect

A

Useful in controlling arrhythmia (supraventricular or thyrotoxicosis), perioperative HTN, and MI in acutely ill patients

133
Q

Esmolol other

A

Safer in critically ill patients

PK: ultra short acting, administer IV

134
Q

Alpha 1 and Beta antagonists

A

Labetalol

Caverdilol

135
Q

Labetalol receptor

A

alpha 1 and beta

136
Q

Labetalol mechanism

A

Decrease in BP:
alpha 1 ->relaxation of arterial smooth muscle
beta 1 ->blocks sympathetic reflex
beta 2 -> sympathomimetic action contributes to vasodilation

137
Q

Labetalol PK

A

more potent beta antagonist
Oral: chronic HTN
IV: emergencies

138
Q

Labetalol Adverse

A

Orthostatic hypotension and dizziness (alpha 1)

139
Q

Carvedilol indication/effect

A

used on patients with CHF and HTN

140
Q

Carvedilol other

A

antioxidant properties

141
Q

Pindolol receptor

A

partial beta agonist

142
Q

Pindolol mechanism

A

Beta blocker with intrinsic sympathomimetic activity helps manage HTN

143
Q

Pindolol indication / effect

A

causes a smaller reduction in resting HR and BP

Preferred in patients with diminished cardiac reserve or propensity to bradycardia

HTN in pregnant women

144
Q

Alpha methyltyrosine
aka metyrosine
mechanism

A

Blocks NE and E synthesis through competitive inhibition of tyrosine hydroxylase

145
Q

Alpha methytyrosine/ metyrosine indication/effect

A

used in adjuvant therapy with phenoxybenzamine in treatment of malignant pheochromocytoma (when surgery is not possible)

146
Q

Reserpine (obsolete) mechanism

A

Irreversible damage to VMAT ->decrease NE and dopamine availability -> sympatholytic response

147
Q

Reserpine indication/effect

A

Unable to concentrate and store NE and dopamine in the vesicle -> continuous breakdown by MAO
Decrease BP and HR

148
Q

Reserpine other

A

historical treatment of HTN

149
Q

Guanethidine mechanism

A

Uptake into nerve terminal via NET -> storage in vesicle and displacement of NE -> NE depletion

150
Q

Guanethidine indication/effect

A

anti-hypertensive that was used in the early 1970s

151
Q

Guanethidine adverse

A

orthostatic HTN and male sexual dysfunction

152
Q

Guanethidine other

A

also disrupts the release of NE from the nerve terminal

Pharmacology (24 decks)

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