Adrenergic Agents Flashcards

1
Q

Direct sympathomimetics

A

Epinephrine
Norepinephrine
Dopamine

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2
Q

Indirect sympathomimetics

A

Ephedrine

Cocaine

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3
Q

Adrenergic Agonists

A

Phenylephrine
Isoproterenol
Clonidine
Albuterol

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4
Q

Adrenergic Antagonists

A
Methyldopa
Phenoxybenzamine
Prazosin
Propranolol
Metoprolol
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5
Q

Alpha 1 receptor mechanism of action

A

PLC activated –> increased IP3 –> and DAG –> increased intracellular Ca2+

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6
Q

Alpha 1 receptor locations

A

vascular smooth muscle, prostate, heart, and pupillary dilator muscle (leads to pupil dilation)

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7
Q

Alpha 2 receptor MOA

A

AC inhibited –> decreased cAMP

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8
Q

Beta 1 receptor MOA

A

AC activated –> increased cAMP

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9
Q

Beta 2 receptor MOA

A

AC activated –> increased cAMP

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10
Q

D1 MOA

A

AC activated –> increased cAMP

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11
Q

D2 MOA

A

AC inhibited –> decreased cAMP

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12
Q

Alpha 2 receptor locations

A

Nerve terminals of adrenergic and cholinergic neurons;

Platelets

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13
Q

Alpha 2 receptor action in nerve terminals of adrenergic and cholinergic neurons

A

inhibit release of neurotransmitters

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14
Q

Alpha 2 receptor action in platelets

A

increase aggregation

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15
Q

Beta 1 action

A

increases rate and contractility of the heart

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16
Q

Beta 2 locations

A

smooth muscle of respiratory vascular and uterine tissue;

Liver

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17
Q

Beta 2 actions

A

Promotes relaxation, leading to bronchodilation, vasodilation, and uterine relaxation;
increases glycogenolysis

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18
Q

D1 receptor location

A

smooth muscle of splanchnic and renal vessels

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19
Q

D1 receptor action

A

vasodilation of renal blood vessels

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20
Q

D2 receptor location

A

Nerve terminals of CNS neurons

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21
Q

D2 action

A

regulates neurotransmitter release

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22
Q

Preferred substrate of alpha 1 & 2 receptors

A

Epi > NE&raquo_space; Isoproterenol

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23
Q

Preferred substrate of beta 1 & 2 receptors

A

Isoproterenol > Epi > NE

24
Q

Preferred substrate of D1 & D2 receptors

25
Acts as an alpha agonist when the drug is given at high doses and as a beta agonist if the drug is given at low doses
Epinephrine
26
Epinephrine is used to treat
``` Cardiac arrest Severe hypotension Bronchospasm in asthma Anaphylaxis Wide-angle glaucoma as an opthalmic solution ```
27
Epinephrine side effects
HTN, Arrhythmias, MI, pulmonary edema headache, anxiety
28
When acting as an alpha 1 agonist, epinephrine causes
vasoconstriction, thereby leading to increased systolic and diastolic blood pressure.
29
When acting as beta 1 agonist, epinephrine
increases heart rate and contractility --> increased CO and systolic BP.
30
When acting as a beta 2 agonist, epinephrine
relaxes vascular and respiratory smooth muscle --> bronchodilation & mild decrease in diastolic BP
31
Potent alpha 1, alpha 1, and beta 1 receptor agonist
Norepinephrine
32
Net effect of NE administration
increased systolic & diastolic BP, increased contractility, no change in heart rate
33
Clinical use of NE
Used as a pressor in the emergency treatment of severe hypotension and shock
34
Side effects of NE
Angina; MI; arrhythmias; decrease in renal blood flow
35
Increases CO without decreasing blood flow to vital organs, such as the kidneys
Dopamine (used as a pressor in the emergency treatment of severe hypotension and shock)
36
Acts as an agonist at alpha 1 receptors at high doses and as an agonist at beta and D1 receptors at lower doses
Dopamine
37
Dopamine effects
Vasoconstriction --> increased BP (alpha) Increases HR & contractility --> inc. CO (beta1) Promotes renal perfusion (D1)
38
Dopamine side effects
Cardiac arrhythmias; angina; HTN nausea
39
Beta1 receptor agonist that increases CO in decompensated CHF or cardiogenic shock
Dobutamine
40
Dobutamine side effects
Tachyarrhythmias | Peripheral vasodilation
41
Stimulates the release of NE and Epi from neurons, directly stimulates alpha and beta receptors --> increased BP & CO, bronchodilation, CNS stimulation (insomnia, decreased appetite, improved athletic performance)
Ephedrine
42
Used as a nasal decongestant and in the treatment of stress incontinence in women
Ephedrine, pseudoephedrine
43
SE of ephedrine
HTN, tremor, anxiety, arrhythmia
44
Drug that enters the CNS and stimulates the release of NE, epi, and dopamine from neurons --> arousal state (insomnia, decreased appetite)p
Amphetamine
45
Amphetamine overdose
Psychosis, arrhythmia, seizure, death
46
Derivative of amphetamine that is used to treat narcolepsy and ADHD in kids
Methylphenidate
47
Blocks the Na+/K+ ATPase that is responsible for the reuptake of NE, serotonin, and dopamine into synaptic terminals, potentiating their effects; also blocks voltage-gated Na+ channels
Cocaine (can also be used as a local anesthetic for ENT surgery)
48
SE of cocaine
HTN; drug of abuse; cardiac ischemia; arrhythmias
49
Inhibits the neuron's ability to store NE, dopamine, and serotonin --> depletion of these neurotransmitters throughout body --> serious psych depression + parkinsonism (previously used to treat HTN)
Reserpine
50
Inhibits NE release from sympathetic neurons; previously used to treat HTN but has bad side effects (orthostatic hypotension --> shock)
Guanethidine
51
Alpha1-agonist --> systemic vasoconstriction and pupil dilation. Topical application to nasal mucosa decreases mucosal secretions.
Phenylephrine
52
Phenylephrine clinical uses
severe hypotension and shock, nasal congestion produce mydriasis for retinal examination
53
Side effects of phenylephrine
cardiac arrhythmias (reflex bradycardia); headache
54
Alpha 1 agonist that is used to treat hepatorenal syndrome and orthostatic hypotension due to ANS dysfunction; SE include supine HTN
Midodrine
55
Alpha 2 agonist that acts primarily the vasomotor centers of the medulla --> reduced NE release --> decreased central adrenergic activity --> decrease in vasoconstriction, CO, and HR; does not decrease RBF
Clonidine
56
Clinical use of clonidine
Hypertension, esp hypertension with comorbid renal disease
57
Side effects of clonidine
Rebound HTN; bradycardia; sedation