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Pharmacology > Adrenergic Agonist and Antagonist > Flashcards

Adrenergic Agonist and Antagonist Flashcards

1
Q

Adrenoreceptor physiology

A

NE is released from postganglionic sympathetic fibers at the end organs
*Exocytosis => NE is terminated by reuptake into postganglionic nerve endings

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2
Q

Prolonged activation of adrenoreceptors

A

can lead to desensitization and hyporesponsiveness

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3
Q

Eye Innervation

A

Superior cervical plexus

  • Alpha: mydriasis
  • Beta - ciliary relaxation
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4
Q

Salivary Innervation

A

Superior cervical plexus

- Alpha 1 and Beta 2 : increased secretions

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5
Q

Heart Innervation

A

Superior Cervical Plexus

- beta 1: increased HR, conduction and contractility

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6
Q

Lung Innervation

A

Middle and Lower Cervical Plexus

  • Alpha 1 : bronchoconstriction
  • beta 2: bronchodilation
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7
Q

Pancreas Innervation

A

Celiac Ganglion

  • Alpha 1: decreased insulin
  • Beta 2: increased insulin
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8
Q

Upper GI Tract Innervation

A

Celiac Ganglion

  • alpha 1: sphincter relaxation
  • beta 2: decreased motility
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9
Q

Liver Innervation

A

Celiac Ganglion

  • alpha 1: glycogenolysis
  • beta 2 & 3: gluconeogenesis
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10
Q

Abdominal Vessels Innervation

A

Celiac Ganglion

  • alpha 1 : vasoconstriction
  • beta 2 : vasodilation
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11
Q

Bladder Innervation

A

Inferior Mesenteric Ganglion

  • alpha 1 : sphincter contraction
  • beta 2: detrusor relaxation
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12
Q

Alpha 1 Receptors

A

1) post-synaptic adrenoreceptors in smooth muscle
- activation –> increased Calcium –> contract smooth muscle –> vasoconstriction
2) inhibits insulin secretion
3) (+) inotropic effect on heart

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13
Q

Alpha 2 Receptors

A

1) Presynaptic nerve terminals –> inhibits adenylyl cyclase –> decreased Calcium –> limits amount of NE released
* stimulation of alpha 2 in CNS –> sedation and decreased sympathetic outflow

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14
Q

Beta 1 Receptors

A

1) Postsynaptic membranes of heart –> (+) adenylyl cyclase –> kinase phosphorylation –> (+) chronotropy and inotropy
* Equal potency for NE and Epi

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15
Q

Beta 2 Receptors

A

1) Postsynaptic receptors in smooth muscle –> (+) adenylyl cyclase –> smooth muscle relaxation
* bronchodilation, vasodilation*
* Epi > NE in potency

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16
Q

Beta 3 Receptors

A

found in gallbladder and brain adipose tissue

17
Q

Dopaminergic Receptors

A

activated by dopamine
D1 = vasodilation of heart, kidney, gut
D2 = antiemetic (droperidol)

18
Q

Phenylephrine

A 
DIRECT non-catecholamine
- pure alpha 1 agonist -> vasoconstriction
- SHORT acting (10-15 minutes)
- reflex bradycardia
Dose: 50-100 mcg bolus
19
Q

Clonidine

A

Alpha 2 agonist

  • anti-hypertensive and (-) chronotropy
  • sedative and anxiolytic
  • circulatory stability by decreasing catecholamine levels
20
Q

Dexmedetomidine

A

PURE alpha 2 agonist –> acts centrally on locus cereleus –> sedative, analgesic, sympatholytic effect
*can reduce other anesthetic needs intraop
*good in the ICU for sedation/extubation
**short t1/2 = 2-3 hrs
**prolonged duration = upregulation of receptors
Hypotension and Bradycardia

21
Q

Milrinone

A

PDE-3 inhibitor (vasodilator) –> needs loading dose
(+) inotropy, chronotropy, lusitropy => vasodilation
*GREAT for R heart failure and pulm HTN

22
Q

Epinephrine

A

endogenous catecholamine from the adrenal medulla
- direct beta1 stimulation -> increased BP, CO, HR, contractility
- alpha 1 stimulation -> vasoconstriction
*decreased splanchnic and renal blood flow
*increased coronary perfusion pressure (ADP - LVEDP)
Dose: 0.05-0.1 mg boluses
100-500 mcg for anaphylaxis

23
Q

Effects of Epi with differing doses

A

Lower dose = beta > alpha

Higher dose = alpha > beta

24
Q

Ephedrine

A

indirect noncatecholamine sympathomimetic - plant derived
- alpha 1 stimulation : vasoconstriction
- beta 1 stimulation : increased HR
Dose: 2.5-10 mg boluses
*have to increase subsequent doses to avoid tachyphylaxis

25
Q

Norepinephrine

A 
DIRECT alpha 1 stimulation -> intense vasoconstriction or arterial and venous systems
- beta 2 activity
* mild reflexive bradycardia 
Dose: 0.1 mcg/kg bolus
    2-20 mcg/min for infusions
26
Q

Dopamine

A

endogenous nonselective direct and indirect adrenergic and dopaminergic agonist
- promotes the release of NE from presynaptic membranes
Dose: 1-20 mcg/kg/min for infusion

27
Q

Doses of Dopamine

A

Low dose: dopaminergic (vasodilation and diuresis)
Moderate: beta 1 stim (increased HR, CO)
High : alpha 1 effects (increased SVR)

28
Q

Isoproterenol

A

PURE beta agonist

  • beta 1 = increased HR, contractility and CO
  • beta 2 = decreased PVR
  • drops myocardial oxygen supply while increasing demand
29
Q

Dobutamine

A

racemic mixture of 2 isomers w/ affinity for beta 1 and 2 receptors
- increased CO and contractility
- drops LV filling pressure = increases coronary blood flow
DOSE: 2-20 mcg/kg/min

30
Q

Phentolamine

A

competitive blocker of alpha 1 and 2 receptors

  • alpha 1: peripheral vasodilation -> decreased MAP
    • reflexive tachycardia
  • alpha 2: augments tachycardia by promoting NE release
31
Q

Labetalol

A 
blocks alpha 1, beta 1, beta 2 receptors
- decreased PVR and BP
- HR and CO are unchanged/decreased 
- peaks in 5 minutes, lasts 5 hours
DOSE: 2.5-10 mg
32
Q

Esmolol

A

ULTRA short acting selective beta 1 blocker
- drops HR w/ some BP effect
- shortest duration due to rapid redistribution and hydrolysis by RBCesterase (10 minutes)
Dose: anywhere from 10-60 mg

33
Q

Metoprolol

A

selective beta 1 antagonist w/ no intrinsic sympathomimetic activity
- every 2-5 minutes as needed
DOSE: 2.5-5 mg boluses

34
Q

Propranolol

A

nonselective beta 1+2 blocker
- lowers BP by:
- decreasing contractility, HR, renin release
- slows AV nodal conduction
*Great for thyrotoxicosis, pheochromocytoma
SE: bronchospasm, CHF, bradycardia, heart block

35
Q

Nebivolol

A

newer beta-blocker w/ beta 1 selectivity

- direct vasodilation by stimulating endothelial NO synthetase

36
Q

Carvedilol

A

Mixed alpha and beta blocker

- GREAT for CHF

Pharmacology (11 decks)

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