Adrenergic Drugs Flashcards

1
Q

Where do adrenergic drugs work?

A
  • sympathetics alpha, beta, and D receptors
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2
Q

What G protein do the following receptors use?

a. alpha 1
b. alpha 2
c. beta
d. D

A

a. q
b. i
c. s
d. s (D1, 5); I (D2-4)

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3
Q

Where does alpha 1 act? role?

A

a. smooth muscle of BVs, pupillary dilator m., prostate, heart
b. contraction, vasoconstriction, dilates pupil, increase force of heart contraction

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4
Q

Where does alpha 2 act? role?

A

a. Postsynaptic CNS neurons, Platelets,
Adrenergic and cholinergic nerve terminals, Some vascular smooth muscle, Fat cells
b. Probably multiple, Aggregation, Inhibits transmitter release, Contraction, Inhibits lipolysis

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5
Q

Where does beta 1 act? role?

A

a. heart, JG cells

b. increase force/rate of contraction, increase renin release

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6
Q

Where does beta 2 act? role?

A

a. Respiratory, uterine and vascular smooth muscle,
Skeletal muscle, Human liver
b. Promotes smooth muscle relaxation, Promotes potassium uptake, Activates glycogenolysis and gluconeogenesis

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7
Q

Where does beta 3 act? role?

A

a. bladder, fat cells

b. relax detractor muscle, activates lipolysis

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8
Q

Where does D1 act? role?

A

a. smooth muscle

b. dilate renal BVs

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9
Q

Where does D2 act? role?

A

a. nerve endings

b. modules transmitter release

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10
Q

What is the role of Monoamine Oxidase (MAO)?

A
  • leads to degradation of NE

- MAO inhibitors block the enzyme, and leave more NE available

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11
Q

Phenylephrine

a. receptors
b. function
c. adverse effects
d. treatment for…

A

a. a1 > a2
b. mydriatic, VC, increase BP
c. leads to severe bradycardia (baro R)
d. decongestant

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12
Q

Clonidine

a. receptors
b. function
c. treatment for…

A

a. a2 > a1 (esp. a 2 in lower brain stem)
b. decrease sympathetic outflow and BP, VC (with local application)
c. HTN

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13
Q

Epinephrine

a. receptors
b. function
c. treatment for…

A

a. a1 = a2; b1 = b2
b. increase glucose/FFA levels, increase HR/force of contraction/conduction velocity of AV node, increase K+ uptake in skeletal m/muscle tremor, bronchodilator/decrease secretions, increase renin release
c. emergency therapy for complete AV block and cardiac arrest

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14
Q

Norepinephrine

a. receptors
b. function
c. adverse effects

A

a. a1 =a 2; b1&raquo_space; b2
b. VC, increased PVR/BP, but reduces HR (baro)
c. lacks b2 agonist effects

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15
Q

Isoproterenol

a. receptors
b. function

A

a. b1 = b2
b. increase CO (+ inotropic/chronotropic), VD, bronchodilator; emergency therapy for complete AV block and cardiac arrest

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16
Q

Dobutamine

a. receptors
b. function
c. treatment for…

A

a. b1 > b2
b. inotropic action
c. cariogenic shock; acute HF

*less prominent chronotropic action as compared to isoproterenol

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17
Q

Albuterol

a. receptors
b. function
c. treatment for…

A

a. b2 > b1
b. bronchodilator, relaxation of uterus
c. asthma

18
Q

Dopamine

a. receptors
b. function
c. treatment for…

A

a. D1 = D2&raquo_space; b1&raquo_space; a1
b. D1 stimulates VD; D2 surpasses NE release
c. at higher doses, b1 activates in heart, and extremely high doses a1 causes VC; cariogenic shock, congetive, severe HF

19
Q

Cocaine

a. action
b. result

A

a. inhibits re-uptake of DA and NE by clocking transporter

b. Local anesthetic properties

20
Q

Phenelzine, Selegiline

a. action
b. result

A

a. inhibits MAO

b. Antidepressant action

21
Q

Amphetamines, methylphenidate

a. action
b. result

A

a. inhibit re-uptake of DA and NE, increases their release, may have weak direct effect
b. 1. Marked stimulant effect on mood and alertness, Decrease appetite
2. used to tx ADHD
= both tx narcolepsy

22
Q

Ephedrine

a. action
b. result
c. treatment for…

A

a. releasing agent and direct adrenergic receptor agonist
b. long duration of action, enters CNS as mild stimulant (similar to E in actions)
c. Nasal decongestant, Increases blood pressure, Stress incontinence in women; chronic hypotension, obesity

23
Q

Tyramine

a. action
b. result
c. source

A

a. Releases stored NE from presynaptic adrenergic terminals (if administered parenterally); metabolized by MAO in liver
b. increase BP in patients taking MAO inhibitors
c. found in cheese, cured meats, and smoked/pickled fish

24
Q

Phentolamine

a. action
b. treatment for…
c. fun fact

A

a. alpha 1 + 2 adrenoceptor antagonist
b. Pheochromocytoma
c. reversible, competitive antagonist

25
Q

Phenoxybenzamine

a. action
b. treatment for…
c. fun fact

A

a. alpha 1 + 2 adrenoceptor antagonist
b. Pheochromocytoma
c. irreversible, non competitive antagonist

26
Q

Prazosin

a. action
b. treatment for…

A

a. alpha 1 R selective antagonist

b. LUTS, HTN

27
Q

Tamsulosin

a. action
b. treatment for…

A

a. alpha 1 R selective antagonist
b. BPH

*1A is the most important receptor subtype mediating prostate smooth
muscle contraction

28
Q

Doxazosin

a. action
b. treatment for…

A

a. alpha 1 R selective antagonist

b. LUTS, HTN

29
Q

Labetalol

a. action
b. treatment for…
c. fun fact

A

a. b and a antagonist
b.
c. partial agonist

30
Q

Carvedilol

a. action
b. treatment for…
c. fun fact

A

a. b and a antagonist
b.
c. inverse agonist

31
Q

Propranolol

a. action
b. treatment for…

A

a. b 1 and 2 blocker

b. Long-term use in post-infarction period – prolong the survival; hyperthyroidism

32
Q

Pindolol

a. action
b. treatment for…
c. fun fact

A

a. b 1 and 2 blocker
b.
c. partial agonist

33
Q

Nadolol

a. action
b. treatment for…

A

a. b 1 and 2 blockers

34
Q

Metoprolol

a. action
b. treatment for…
c. fun fact

A

a. b1 blocker
b. Long-term use in post-infarction period – prolong the survival
c. inverse agonist

35
Q

Betaxolol

a. action
b. treatment for…

A

a. b1 blocker

b. glaucoma

36
Q

Acebutolol

a. action
b. treatment for…
c. fun fact

A

a. b1 blocker
b.
c. partial agonist

37
Q

Atenolol

a. action
b. treatment for..

A

a. b1 blocker

38
Q

What is the benefit of a beta blocker with an ISA?

A
  • Block sympathetic effects BUT have submaximal effects of their own = a blunted sympathetic response
  • Less risk for bradycardia, increase in VLDL/HDL, and other effects of beta receptor blockade
  • Example: atenolol drastically drops HR, but pindolol only partially drops HR, so it’s safer
39
Q

What is an ISA?

A
  • Intrinsic Sympathomimetic Activity

- partial agonists at beta adrenergic receptors

40
Q

How do beta blockers affect renin release?

A

inhibit it

41
Q

Why do you have to taper off beta blockers?

A
  • because while using them the body makes more beta receptors in an attempt to get a response, but these are all blocked by the drug
  • with removal of the drug, there are more available receptors, and they all get activated, and have an increase sympathetic response
42
Q

What are the true beta antagonist? what do they block?

A
  • propanolol, betaxolol, nadolol, atenolol

- endogenous agonists; only work when those are present