Adrenergic Drugs Flashcards

1
Q

Where do adrenergic drugs work?

A
  • sympathetics alpha, beta, and D receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Where does beta 1 act? role?

A

a. heart, JG cells

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Where does beta 3 act? role?

A

a. bladder, fat cells

b. relax detractor muscle, activates lipolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Where does D1 act? role?

A

a. smooth muscle

b. dilate renal BVs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Where does D2 act? role?

A

a. nerve endings

b. modules transmitter release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
Phenoxybenzamine a. action b. treatment for... c. fun fact
a. alpha 1 + 2 adrenoceptor antagonist b. Pheochromocytoma c. irreversible, non competitive antagonist
26
Prazosin a. action b. treatment for...
a. alpha 1 R selective antagonist | b. LUTS, HTN
27
Tamsulosin a. action b. treatment for...
a. alpha 1 R selective antagonist b. BPH *1A is the most important receptor subtype mediating prostate smooth muscle contraction
28
Doxazosin a. action b. treatment for...
a. alpha 1 R selective antagonist | b. LUTS, HTN
29
Labetalol a. action b. treatment for... c. fun fact
a. b and a antagonist b. c. partial agonist
30
Carvedilol a. action b. treatment for... c. fun fact
a. b and a antagonist b. c. inverse agonist
31
Propranolol a. action b. treatment for...
a. b 1 and 2 blocker | b. Long-term use in post-infarction period – prolong the survival; hyperthyroidism
32
Pindolol a. action b. treatment for... c. fun fact
a. b 1 and 2 blocker b. c. partial agonist
33
Nadolol a. action b. treatment for...
a. b 1 and 2 blockers
34
Metoprolol a. action b. treatment for... c. fun fact
a. b1 blocker b. Long-term use in post-infarction period – prolong the survival c. inverse agonist
35
Betaxolol a. action b. treatment for...
a. b1 blocker | b. glaucoma
36
Acebutolol a. action b. treatment for... c. fun fact
a. b1 blocker b. c. partial agonist
37
Atenolol a. action b. treatment for..
a. b1 blocker
38
What is the benefit of a beta blocker with an ISA?
* 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
What is an ISA?
- Intrinsic Sympathomimetic Activity | - partial agonists at beta adrenergic receptors
40
How do beta blockers affect renin release?
inhibit it
41
Why do you have to taper off beta blockers?
- 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
What are the true beta antagonist? what do they block?
- propanolol, betaxolol, nadolol, atenolol | - endogenous agonists; only work when those are present