Adrenergic drugs Flashcards

1
Q

Effects of Epi on vascular tone

A

Increase systolic BP

May decrease disatolic BP and total PVR

Vascular constriction in skin vessels and mucous membranes

Vascular dilation or constriction in skeletal muscle

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2
Q

What are the non-selective α-adrenoreceptor antagonists?

(direct acting antiadrenergic drugs)

A

Phentolamine

Phenoxybenzamine

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3
Q

Effects of beta-blockers on blood vessels

A

Initial rise in PVR

Chronic use leads to a decrease in PVR which lowers BP in hypertensive individuals

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4
Q

What direct acting adrenomimetics are mixed alpha and beta agonists?

A

Norephinephrine (Levophed**)

Epinephrine (Adrenalin)

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5
Q

Effects of isoproterenol

A

Positive inotropic and chronotropic action, increases CO (β1)

Vasodilator, decreases arterial pressure (β2)

Bronchodilation (β2)

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6
Q

Effects of Clonidine

A

Decreases sympathetic outflow, reduces BP, bradycardia by acting on the lower brainstem area

Regulates release of NE by binding to presynaptic α2 receptors

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7
Q

Effects of beta-blockers on the respiratory system

A

increase airway resistance

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8
Q

α2 receptor type activation utilizes what type of GPCR?

A

Gi

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9
Q

Effects of Epinephrine on cardiac function

A

Increase force of contraction

Increase HR

Increase conduction velocity of AV node

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10
Q

What direct acting adrenomimetics are beta agonists?

A

Dobutamine β1 > β2

Isoproterenol β1 = β2

Albuterol (Ventolin) β2 > β1

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11
Q

Locations of α1 adrenoreceptors

What is the outcome of receptor activation?

A

Most vascular smooth m.
Pupillary dilator m.
Prostate
Heart

Contraction

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12
Q

Effects of Dopamine

A

D1 receptors lead to vasodilation

D2 receptors suppress NE release

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13
Q

What dopamine receptors utilize Gi GPCRs?

A

D2, D3 and D4

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14
Q

What drug is an inhibitor of norephinephrine release?(indirect acting antiadrenergic drugs)

A

Guanethidine

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15
Q

What are the non-selective β-blockers? (direct acting antiadrenergic drugs)

A

Propranolol

Pindolol

Nadolol

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16
Q

What are the α1 selective α-adrenoreceptor antagonists?

A

Prazosin

Tamsulosin

Doxazosin

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17
Q

Locations of α2 adrenoreceptors (action)

A

Postsynaptic CNS neurons

Platelets (aggregation)

Adrenergic OR cholinergic nerve terminals (inhibits NT release)

Some vascular smooth m.

Fat cells (inhibits lipolysis)

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18
Q

Location of β2 adrenoreceptors

A

Respiratory, uterine and vascular smooth m. (relaxation)

Skeletal m. (K+ uptake)

Human liver (activate gluconeogenesis and glycogenolysis)

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19
Q

Effects of phenylephrine

A

mydriatic and decongestant

severe vasoconstriction and subsequent increase in BP

severe bradycardia

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20
Q

Location of β1 adrenoreceptors (action)

A

Heart ( + inotropy, + chronotropy)

Juxtaglomerular cells (increase renin release)

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21
Q

Indirect adrenomimetic that is a releasing agent and a direct adrenergic receptor agonist

A

Ephedrine

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22
Q

What are the mixed blockers?

(direct acting antiadrenergic drugs)

A

Labetalol (β and α1 antagonist)

Carvedilol (β and α1 antagonist)

23
Q

Adverse effects of adrenergic agonists

A

Elevated BP

Increased cardiac work leading to MI or HF

Sudden death d/t arrhythmias

Insomnia

Lack of appetite

Anxiety

Psychoses, convulsions

Hemorrhagic stroke

24
Q

Effects of Epi on respiratory system

A

Relaxes bronchial smooth m. (β2)

Decreases bronchial secretion and congestion within bronchial mucosa (α1)

25
Q

Effects of Phenelzine and Selegiline

A

Inhibit MAO and increase NE stores in CNS

Antidepressant action

26
Q

Effects of Epi on skeletal m.

A

Tremor (β2)

Increase K+ uptake (β2)

27
Q

Indirect acting adrenomimetics that reverse NE and DA uptake mechanisms and increase their release

A

Amphetamines

Methylphenidate (Ritalin)

Tyramine (a byproduct of tyrosine metabolism, not a drug)

28
Q

β receptor type activation utilizes what type of GPCR?

A

Gs

29
Q

Location of D1 receptors

A

Smooth m. (dilates renal blood vessels)

30
Q

Adverse effects of alpha antagonists

A

Postural HoTN
Tachycardia
Retention of fluid and salt
Impaird ejaculation
Nasal stuffiness

31
Q

Clinical use of beta blockers

A

HTN
Angina pectoris
MI
Cardiac arrhythmias
HF
Glaucoma
Hyperthyroidism

32
Q

What is the receptor preference for phenylephrine?

A

α1 > α2 >>>> β

33
Q

Effects of Dobutamine

A

Potent inotropic action

Has α1 receptor activity (can act as an agonist or antagonist)

34
Q

Effects of Tyramine

A

Releases stored NE from presynaptic terminals

May increase BP in patients taking MAO inhibitors

35
Q

Adverse effects of beta-blockers

A

Sedation
Sleep disturbances
Depression
Increase airway resistance
Bronchospasms
Decrease HR and contractility
Hypoglycemic episodes

36
Q

Clinical use of alpha antagonists

A

Pheochromocytoma
Chronic (essential) HTN
ED
BPH

37
Q

Effects on beta-blockers on the heart

A

Negative inotropic effect

Negative chronotropic effect

Slow AV node conduction

38
Q

What dopamine receptors utilize Gs GPCRs?

A

D1 and D5

39
Q

What are the β1 selective β-adrenoreceptor blockers?(direct acting antiadrenergic drugs)

A

Metoprolol

Betaxolol

Acebutolol

Atenolol

40
Q

What direct acting adrenomimetics are dopamine agonists?

A

Dopamine

41
Q

What drug is an inhibitor of tyrosine hydroxylase? (indirect acting antiadrenergic drugs)

A

Metyrosine

42
Q

What drug is an indirect acting adrenomimetic that inhibits re-uptake of dopamine and norepinephrine?

A

Cocaine

43
Q

Effects of NE

A

Reduces HR

Potent vasoconstrictor

NO bronchodilation and vasodilation

Increases PVR and BP

44
Q

Location of D2 receptors

A

Nerve endings (modulate NT release)

45
Q

What is the receptor preference of NE?

A

α1 = α2

β1 >> β2

46
Q

What drugs are indirect acting adrenomimetics that inhibit MAO (monoamine oxidase)?

A

Selegiline

Phenelzine

47
Q

Effects of Albuterol

A

Bronchodilation

Relaxation of uterus

48
Q

α1 receptor type activation utilizes what type of GPCR?

A

Gq

49
Q

What direct acting adrenomimetics are alpha agonists?

A

Phenylephrine (α1 > α2)

Clonidine (α2 > α1)

50
Q

Location of β3 adrenoreceptors

A

Bladder (relaxes detrusor m.)

Fat cells (activation of lipolysis)

51
Q

What is the receptor preference for Clonidine?

A

α2 > α1 >>>> β

52
Q

Effects of beta-blockers on the eye

A

Reduced intraocular pressure through reduced production of aqueous humor

53
Q

Clinical use of Ephedrine

A

Nasal decongestant

Increase BP

Stress incontinence in women

54
Q

Clinical use of adrenergic agonists

A

Hypotensive emergencies
Chronic hypotension
Cardiogenic shock
HF
HTN
Cardiac arrest or complete AV block
Narcolepsy
ADHD
Obesity
Asthma
Decongestion
Anaphylaxis