Adrenergics Flashcards

1
Q

What drugs are direct acting adrenomimetics- alpha agonists?

A

Phenylephrine (Neo-synephrine) and Clonidine (Catapres)

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

What drugs are direct acting adrenomimetics- mixed alpha and beta agonists?

A

Norepinephrine (Levophed) and Epinephrine (Adrenalin)

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

What drugs are direct acting adrenomimetics- beta agonists?

A

Dobutamine (Dobutrex), Isoproterenol (Isuprel), and Albuterol (Ventolin)

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

What drugs are direct acting adrenomimetics- Dopamine agonists?

A

Dopamine (intropin)

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

What drugs are indirect acting adrenomimetics- inhibiting the re-uptake of DA and NE?

A

Cocaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What drugs are indirect acting adrenomimetics- inhibitors of MAO?

A

Selegiline (Eldepryl) and Phenelzine (Nardil)

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

What drugs are indirect acting adrenomimetics- reverse NE and DA uptake mechanisms and increase their release?

A

Amphetamines, Methylphenidate (Ritalin), Tyramine (byproduct, not a drug)

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

What drugs are indirect acting adrenomimetics- releasing agent AND a direct adrenergic receptor agonist?

A

Ephedrine

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

What drugs are direct acting antiadrenergic- alpha adrenoreceptor antagonists (NONSELECTIVE)?

A

Phentolamine (OraVerse) and Phenoxybenzamine (Dibenzyline)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What drugs are direct acting antiadrenergic- alpha adrenoceptor antagonists (A1 RECEPTOR SELECTIVE)?

A

Prazosin (Minipress), Tamsulosin (Flomax), and Doxazosin (Cardura)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What drugs are direct acting antiadrenergic- mixed blockers?

A

Labetalol (Trandate) and Carvedilol (Coreg)

Both are Beta and a1 antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What drugs are direct acting antiadrenergic- Beta adrenoceptor blockers (B1 AND B2)?

A

Propranolol (Inderal), Pindolol (Visken), and Nadolol (Corgard)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What drugs are direct acting antiadrenergic- Beta adrenoceptor blockers (B1 SELECTIVE)?

A

Metoprolol (Toprol), Betaxolol (kerlone), Acebutolol (Sectral), and Atenolol (Tenormin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What drugs are indirect acting antiadrenergic - NE release inhibitor?

A

Guanethidine (Ismelin)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What drugs are indirect acting antiadrenergic- inhibitor of tyrosine hydroxylase?

A

Metyrosine (Demser)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What receptor types are Gq?

A

Alpha 1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What receptor types are Gi?

A

Alpha 2

Also D2, D3, D4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What receptor types are Gs?

A

B1, B2, and B3

Also, D1 and D5

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Where are alpha 1 receptors most prevalent?

A

Most vascular smooth muscle, pupillary dilator m., prostate, heart

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What actions do alpha 1 receptors induce?

A

Contraction in vascular smooth muscle, dilates the pupil, contracts the prostate, and increases FORCE of contraction in heart (inotropy)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Where are alpha 2 receptors most prevalent?

A

Postsynaptic CNS neurons, platelets, adrenergic and cholinergic nerve terminals, some vascular smooth muscle, and fat cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What action do alpha 2 receptors induce?

A

Platelet aggregation, inhibits transmitter release in adrenergic and cholinergic nerve terminals, contracts vascular smooth muscle, and inhibits lipolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What tissues are beta 1 receptors most prevalent?

A

The heart and juxtaglomerular cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What actions do beta 1 receptors induce?

A

Increases FORCE and RATE of contraction (inotropic and chronotropic) in the heart and increases renin release

25
What tissues are Beta 2 receptors most prevalent?
Respiratory, uterine, and vascular smooth muscle; skeletal muscle; human liver
26
What actions do beta 2 receptors induce?
Promotes smooth muscle relaxation in the lungs, uterus, and vascular smooth muscle; promotes potassium uptake in skeletal muscle; activates glycogenolysis and gluconeogenesis in the liver
27
What tissues are beta 3 receptors most prevalent?
Bladder and fat cells
28
What action do beta 3 receptors induce?
Relaxes the detrusor muscle and activates lipolysis
29
Where are D1 receptors and what do they do?
Present in smooth muscle and lead to dilation of renal blood vessels
30
Where are D2 receptors and what do they do?
Nerve endings and they modulate transmitter release
31
What adrenergic receptor affinity does phenylephrine have?
A1> a2 >>>> B
32
What adrenergic receptor affinity does Clonidine have?
A2 > a1 >>>> B
33
What adrenergic receptor affinity does NE have?
A1 = A2; B1 >> B2
34
What adrenergic receptor affinity does Epi have?
A1= A2; B1 = B2
35
What adrenergic receptor affinity does Dobutamine have?
B1 > B2 >>>> A
36
What adrenergic receptor affinity does Isoproterenol have?
B1 = B2 >>>> a
37
What adrenergic receptor affinity does Albuterol have?
B2 >> B1 >>>> a
38
What adrenergic receptor affinity does Dopamine have?
D1 = D2 >> B >> a
39
What effect does epinephrine have on cardiac function? What receptor is it mainly affecting?
Increases the force of contraction, heart rate, and conduction velocity at AV node B1 receptor
40
What effect does Epi have on vascular tone? What receptors is it affecting?
Increases sBP, may decrease dBP and total peripheral vascular resistance, MAP unchanged B2 and a1
41
What effect does epi have on the respiratory system and what receptors does it affect?
Relaxes bronchial muscle and decreases secretion (B2) congestion within bronchial mucosa (a1)
42
What are the effects of NE?
Potent cardiac stimulant but reduces HR Vasoconstriction NO BRONCHODILATION AND VASODILATION Increases peripheral vascular resistance and blood pressure
43
What effect does phenylephrine have?
Effective mydriatic and decongestant Vasconstriction BP elevation Severe bradycardia
44
What effect does clonidine have?
Central effect on a2 receptors in lower brain stem Decreasing sympathetic outflow Reduction in BP Bradycardia
45
What effect does Isoproterenol have?
Positive inotropic and chronotropic action, so increases Cardiac output (B1) Vasodilation and decreases arterial pressure (B2) Bronchodilation (B2)
46
What effect does Dobutamine have?
Potent inotropic action Selective B1 agonist Note: the negative isomer is an agonist for a1 but the positive isomer is an antagonist
47
What effect does albuterol have?
Selective B2 agonist Bronchodilation Relaxation of uterus
48
What effect does dopamine have?
Vasodilation But activates B1 in heart at higher doses At even HIGHER doses, stimulates vascular a1 to cause vasoconstriction
49
What is the MOA and selectivity of Ephedrine?
Releases stored catecholamines Nonselective
50
What is the clinical use for ephedrine?
Nasal decongestant, increases BP, stress incontinence in women
51
What is the MOA of Phenelzine, selegiline?
They inhibit MAO so they increase NE stores in the CNS Antidepressants
52
What does tyramine do?
Product of tyrosine metabolism and releases stored NE from presynaptic adrenergic terminals
53
What are cardiovascular adverse side effects of adrenergic agonists?
Elevation in BP, increased cardiac work, sinus tach
54
What are some adverse effects in the CNS of adrenergic agonists?
Insomnia, lack of appetite, anxiety/restlessness, psychoses, convulsions and hemorrhagic stroke (cocaine)
55
What are adverse effects of ALPHA antagonists?
Postural hypotension, tachycardia, retention of fluid and salt, impaired ejaculation, nasal stuffiness
56
Which beta blockers are antagonists?
Atenolol, nadolol, propranolol, betaxolol
57
What beta blockers are partial agonists?
Acebutolol, labetalol, pindolol
58
What beta blockers are inverse agonists?
Carvedilol and metoprolol
59
What are some adverse effects of beta blockers?
Depression; sedation; increased airway resistance; decreased HR, contractility, excitability; hypoglycemic episodes