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

A

Dopamine

25
Q

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

A

Epinephrine

26
Q

Epinephrine is used to treat

A
Cardiac arrest
Severe hypotension
Bronchospasm in asthma
Anaphylaxis
Wide-angle glaucoma as an opthalmic solution
27
Q

Epinephrine side effects

A

HTN, Arrhythmias, MI,
pulmonary edema
headache,
anxiety

28
Q

When acting as an alpha 1 agonist, epinephrine causes

A

vasoconstriction, thereby leading to increased systolic and diastolic blood pressure.

29
Q

When acting as beta 1 agonist, epinephrine

A

increases heart rate and contractility –> increased CO and systolic BP.

30
Q

When acting as a beta 2 agonist, epinephrine

A

relaxes vascular and respiratory smooth muscle –> bronchodilation & mild decrease in diastolic BP

31
Q

Potent alpha 1, alpha 1, and beta 1 receptor agonist

A

Norepinephrine

32
Q

Net effect of NE administration

A

increased systolic & diastolic BP,
increased contractility,
no change in heart rate

33
Q

Clinical use of NE

A

Used as a pressor in the emergency treatment of severe hypotension and shock

34
Q

Side effects of NE

A

Angina; MI; arrhythmias; decrease in renal blood flow

35
Q

Increases CO without decreasing blood flow to vital organs, such as the kidneys

A

Dopamine (used as a pressor in the emergency treatment of severe hypotension and shock)

36
Q

Acts as an agonist at alpha 1 receptors at high doses and as an agonist at beta and D1 receptors at lower doses

A

Dopamine

37
Q

Dopamine effects

A

Vasoconstriction –> increased BP (alpha)
Increases HR & contractility –> inc. CO (beta1)
Promotes renal perfusion (D1)

38
Q

Dopamine side effects

A

Cardiac arrhythmias;
angina;
HTN
nausea

39
Q

Beta1 receptor agonist that increases CO in decompensated CHF or cardiogenic shock

A

Dobutamine

40
Q

Dobutamine side effects

A

Tachyarrhythmias

Peripheral vasodilation

41
Q

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)

A

Ephedrine

42
Q

Used as a nasal decongestant and in the treatment of stress incontinence in women

A

Ephedrine, pseudoephedrine

43
Q

SE of ephedrine

A

HTN, tremor, anxiety, arrhythmia

44
Q

Drug that enters the CNS and stimulates the release of NE, epi, and dopamine from neurons –> arousal state (insomnia, decreased appetite)p

A

Amphetamine

45
Q

Amphetamine overdose

A

Psychosis, arrhythmia, seizure, death

46
Q

Derivative of amphetamine that is used to treat narcolepsy and ADHD in kids

A

Methylphenidate

47
Q

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

A

Cocaine (can also be used as a local anesthetic for ENT surgery)

48
Q

SE of cocaine

A

HTN; drug of abuse; cardiac ischemia; arrhythmias

49
Q

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)

A

Reserpine

50
Q

Inhibits NE release from sympathetic neurons; previously used to treat HTN but has bad side effects (orthostatic hypotension –> shock)

A

Guanethidine

51
Q

Alpha1-agonist –> systemic vasoconstriction and pupil dilation. Topical application to nasal mucosa decreases mucosal secretions.

A

Phenylephrine

52
Q

Phenylephrine clinical uses

A

severe hypotension and shock,
nasal congestion
produce mydriasis for retinal examination

53
Q

Side effects of phenylephrine

A

cardiac arrhythmias (reflex bradycardia); headache

54
Q

Alpha 1 agonist that is used to treat hepatorenal syndrome and orthostatic hypotension due to ANS dysfunction; SE include supine HTN

A

Midodrine

55
Q

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

A

Clonidine

56
Q

Clinical use of clonidine

A

Hypertension, esp hypertension with comorbid renal disease

57
Q

Side effects of clonidine

A

Rebound HTN; bradycardia; sedation