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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
Dobutamine effect
**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
26
Dobutamine PK
can build up tolerance with long term use
27
Dobutamine other
Racemic mixture: -ve alpha one and beat beta one agonist; +ve alpha 1 antagonist and potent beta 1 agonist Net effect: selective Beta 1
28
Terbutaline receptor
Beta 2
29
Terbutaline effect
Bronchodilator Emergency treatment of **status asthmaticus** Reduces uterine contraction in premature labor
30
Terbutaline PK
Resorcinol ring -> not metabolized by COMT giving it a longer duration Oral, Inhalation or SC
31
Terbutaline other
Selectivity is lost at high concentrations | Used in treatment of asthma without having effects on heart
32
Albuterol other
Selectivity is lost at high concentrations | Used in treatment of asthma without having effects on heart
33
Salmeterol and Formoterol other
Selectivity is lost at high concentrations | Used in treatment of asthma without having effects on heart
34
Albuterol Receptor
Beta 2
35
Salmeterol and Formoterol receptor
Beta 2
36
Albuterol effect
Inhalant bronchodilator; relief of symptoms in asthma
37
Salmeterol and Formoterol effect
Bronchodilator | Long acting-> not used for prompt relief of bronchospasm
38
Salmeterol and Formoterol PK
Slow onset, but prolonged action (12 hrs) after inhalation
39
Direct acting alpha agonist drugs
Phenylephrine Clonidine Methyldopa Brimonidine
40
Phenylephrine receptor
alpha 1
41
Phenylephrine mechanism
Peripheral vasoconstriction
42
Phenylephrine effects
Vasoconstrictor: increase SBP and DBP Nasal decongestant Mydriasis Tx of supraventricular tachycardia
43
Phenylephrine Other
NO direct effect on heart, but does cause reflex bradycardia after parenteral administration
44
Clonidine receptor
Alpha 2
45
Clonidine Mechanism
Partial agonist** : activation of *central alpha 2 receptors* suppresses sympathetic outflow
46
Clonidine effect
Antihypertensive
47
Clonidine PK
Acute rise in BP due to transient vasoconstriction when given IV, but not orally
48
Clonidine adverse
Centrally acting antiadrenergic drugs: sedation, mental lassitude, impaired concentration
49
Methyldopa adverse
Centrally acting antiadrenergic drugs: sedation, mental lassitude, impaired concentration
50
Methyldopa receptor
alpha 2
51
Methyldopa mechanism
Central acting anti HTN
52
Methyldopa effect
Metabolized to alpharmethylnorepinephrine which causes effects similar to clonidine: decrease TPR and BP *DOC in pregnant patients with HTN*
53
Methyldopa adverse
Can cause +ve Coombs test or hemolytic anemia or hepatitis
54
Brimonidine receptor
alpha 2
55
Brimonidine mechanism
Decrease aqueous humor production along with increased outflow
56
Brimonidine effect
Decrease intraocular pressure in glaucoma
57
Indirect acting Adrenergic agonist drugs
Amphetamine Methylphenidate Tyramine
58
Amphetamine mechanism
Displaces catecholamines from storage vesicle Weak inhibitor of MAO Blocks catecholamine reuptake
59
Amphetamine Effect
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)
60
Amphetamine adverse
Fatigue and depression follow stimulation
61
Amphetamine other
releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles
62
Methyphenidate other
releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles
63
Tyramine other
releasing agents potentiate actions of endogenous NE by causing release from presynaptic vesicles
64
Methyphenidate Mechanism
Structural analog of amphetamine
65
Methyphenidate indication
Tx of ADHD in children
66
Tyramine Indication
Not clinically useful, found in fermented foods (cheese and wine)
67
Tyramine PK
Byproduct of tyrosine metabolism, normally oxidized by MAO
68
Tyramine Adverse
******Serious vasopressor episodes in patients on MAO-I's after release of NE*******
69
Cocaine Receptor
DAT SERT NET
70
Cocaine mechanism
Blocks dopamine (major effect), serotonin, and NE transporters -> potentiation and prolonged effects
71
Cocaine effect
Sympathomimetic | Therpeutic use: blockage of voltage gated sodium channels -> local anesthetic
72
Cocaine Adverse
Intense euphoria from blockage of dopamine reuptake in limbic system
73
Cocaine other
Monoamine reuptake inhibitor
74
Atomoxetine receptor
NET
75
Atomoxetine Mechanism
Selective NET inhibitor
76
Atomoxetine Indication
Tx of ADHD
77
Atomoxetine other
Monoamine reuptake inhibitor
78
Ephedrine receptor
alpha and beta
79
Ephedrine effect
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
Ephedrine PK
NOT a catecholamine -> poor substrate for COMT and MAO -> longer duration of action Excellent oral absorption, enters CNS Eliminated unchanged in urine
81
Ephedrine Adverse
Herbal supplements banned in 2004 due to life threatening cardiovascular reactions
82
Ephedrine other
Induces release of NE* and activates adrenergic receptors* | Use declining due to better drugs with fewer side effects
83
Pseudoephedrine mechanism
ephedrine enantiomer
84
Pseudoephedrine receptor
alpha and beta
85
Pseudoephedrine effect
Nasal decongestant with an H1 histamine antagonist
86
Alpha antagonist drugs
``` Phenoxybenzamine Phentolamine Prazosin Terzosin Doxazosin Tamsulosin Yohimbine ```
87
alpha 1 blockers
-osins
88
Phenoxybenzamine receptor
non selective alpha
89
Phenoxybenzamine mechanism
alkylation *irreversibly* blocks receptor slightly alpha one selective Also blocks H1, M and 5-HT receptors; inhibits NET
90
Phenoxybenzamine effect
CVS: prevents vasoconstriction of peripheral blood vessels -> reflex tachycardia Presynaptic alpha 2 block -> increase CO
91
Phenoxybenzamine indications
*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
Phenoxybenzamine adverse
``` Postural hypotension Nasal stiffness Nausea and vomiting Inhibit ejaculation Contraindicated in patients with decreased coronary perfusion due to reflex tachycardia ```
93
Phenoxybenzamine contraindication
Patients with decreased coronary perfusion
94
Phentolamine receptor
nonselective alpha
95
Phentolamine mechanism
*Reversible* alpha blocker Serotonin blocker Muscarinic, H1 and H2 agonist
96
Phentolamine indications
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
Phentolamine adverse
Postural hypotension-baroreceptor reflex and alpha 2 blockade on cardiac nerves Arrhythmia and angina Contraindicated in patients with decreased coronary perfusion
98
Prazosin receptor
Selective alpha 1 | Useful in treatment of HTN
99
Prazosin mechanism
decrease TPR through relaxation of arterial and venous smooth muscle
100
Prazosin effects
**decrease BP without reflex tachycardia (alpha2)** Decrease LDL/TAG, increase HDL Improves urinary blood flow
101
Prazosin Indications
Suppress sympathetic outflow from CNS Tx of HTN, BPH
102
Prazosin Adverse
Not the DOC for primary HTN First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)
103
Terazosin and Doxazosin receptor
Selective alpha 1 | Useful for treatment of HTN
104
Terazosin and Doxazosin mechanism
Structural analog of prazosin -> longer half life -> less frequent dosing Decrease TPR through relaxation of arterial and venous smooth muscle
105
Terazosin and Doxazosin effect
**decrease BP without reflex tachycardia (alpha2)** Decrease LDL/TAG, increase HDL Improves urinary blood flow
106
Tamsulosin effect
Relaxes genitourinary smooth muscle
107
Terazosin and Doxazosin indication
Suppress sympathetic outflow from CNS Tx of HTN, BPH
108
Tamsulosin indication
Used in treatment of BPH with little effect on BP | reduced orthostatic HTN
109
Terazosin and Doxazosin adverse
Not the DOC for primary HTN First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)
110
Tamsulosin adverse
Not the DOC for primary HTN First dose effect may cause exaggerated hypotensive response and syncope (adjust first dose 1/4 of normal)
111
Tamsulosin receptor
Selective alpha 1 | Treatment of HTN
112
Tamsulosin mechanism
Selective for alpha1A receptor found in genitourinary smooth muscle
113
Yohimbine receptor
alpha 2
114
Yohimbine mechanism
alpha 2 blocker -> indirect adrenergic agonist
115
Yohimbine effect
increase NE release -> increase BP
116
Yohimbine indication
treatment of *erectile dysfunction*, but has been replaced by PDE-5 inhibitors
117
Yohimbine contraindications
Can reverse effects of alpha 2 agonists (clonidine--bad!)
118
Beta antagonist drugs
``` Propranolol Nadolol Timolol Atenolol Metoprolol Esmolol ```
119
Propranolol receptor
Beta 1 and 2
120
Propranolol mechanism
``` CVS: decrease HR and contractility Increase TPR (beta 2) ``` Metabolic: decrease glycogenolysis and glucagon secretion -> severe hypoglycemia in patients on insulin
121
Propranolol indication/effect
``` 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
Propranolol Adverse
**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
Propranolol other
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
Nadolol indication/effect
long term treatment of angina and HTN
125
Timolol indication/effect
HTN, prophylaxis for migraines | Glaucoma (open angle)
126
Atenolol and Metoprolol indication/effect
Management of HTN in patients with impaired pulmonary function or IDDM
127
Atenolol and Metoprolol receptor
B1 cardioselective
128
Timolol receptor
Beta 1 and 2
129
Nadolol receptor
beta 1 and 2
130
Esmolol receptor
beta 1 cardioselective
131
Atenolol and Metoprolol other
less likely to produce bronchospasm long term management of angina; s/p MI reduces mortality
132
Esmolol indication/effect
Useful in controlling arrhythmia (supraventricular or thyrotoxicosis), perioperative HTN, and MI in acutely ill patients
133
Esmolol other
Safer in critically ill patients | PK: ultra short acting, administer IV
134
Alpha 1 and Beta antagonists
Labetalol | Caverdilol
135
Labetalol receptor
alpha 1 and beta
136
Labetalol mechanism
Decrease in BP: alpha 1 ->relaxation of arterial smooth muscle beta 1 ->blocks sympathetic reflex beta 2 -> sympathomimetic action contributes to vasodilation
137
Labetalol PK
more potent beta antagonist Oral: chronic HTN IV: emergencies
138
Labetalol Adverse
Orthostatic hypotension and dizziness (alpha 1)
139
Carvedilol indication/effect
used on patients with CHF and HTN
140
Carvedilol other
antioxidant properties
141
Pindolol receptor
partial beta agonist
142
Pindolol mechanism
Beta blocker with intrinsic sympathomimetic activity helps manage HTN
143
Pindolol indication / effect
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
Alpha methyltyrosine aka metyrosine mechanism
Blocks NE and E synthesis through competitive *inhibition of tyrosine hydroxylase*
145
Alpha methytyrosine/ metyrosine indication/effect
used in adjuvant therapy with phenoxybenzamine in treatment of malignant pheochromocytoma (when surgery is not possible)
146
Reserpine (obsolete) mechanism
*Irreversible damage to VMAT* ->decrease NE and dopamine availability -> sympatholytic response
147
Reserpine indication/effect
Unable to concentrate and store NE and dopamine in the vesicle -> continuous breakdown by MAO Decrease BP and HR
148
Reserpine other
historical treatment of HTN
149
Guanethidine mechanism
Uptake into nerve terminal via NET -> storage in vesicle and displacement of NE -> NE depletion
150
Guanethidine indication/effect
anti-hypertensive that was used in the early 1970s
151
Guanethidine adverse
orthostatic HTN and male sexual dysfunction
152
Guanethidine other
also disrupts the release of NE from the nerve terminal

Pharmacology (24 decks)

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