[5] Adrenergic Receptors Flashcards

1
Q

Rate Limiting Step of Norepinephrine

A

Tyrosine Hydroxylase

Tyrosine -> DOPA

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2
Q

Receptors prolific in smooth muscles and blood vessels

A

Alpha-1

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3
Q

Postsynaptic effector mostly found in the heart

A

Beta-1

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4
Q

Postsynaptic effector cells especially in smooth muscles

A

Beta-2

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5
Q

Postsynaptic effector cells especially in lipocytes

A

Beta-3

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6
Q

Which has a methyl group? Epinephrine or Norepinephrine?

A

Epinephrine

because

NO-repinephrine

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7
Q

Subtypes of Beta-1 Receptors

A

Heart

Juxtaglomerular cell

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8
Q

Subtypes of Beta-2Receptors

A

Respiratory, uterine, and vascular smooth muscle
Skeletal Muscle
Human Liver

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9
Q

Function: Activation of Beta-2 in Respiratory Tissue

A

Smooth muscle relaxation

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10
Q

Function: Activation of Beta-2 in Skeletal Muscle

A

Potassium Uptake

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11
Q

Function: Activation of Beta-2 in the Liver

A

Activates glycogenolysis

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12
Q

Function: Activation of Beta-3 Receptors

A

Increased lipolysis

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13
Q

Receptor Specificity is ____ but not _____?

A

Relative, but not absolute

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14
Q

Parent Compound of Adrenergic Agents

A

Phenylethylamine

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15
Q

Effect: Increased size of alkyl substituents on Amino Group

A

Increased beta-receptor activity

Decreased alpha-receptor activity

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16
Q

A lower Kd value would mean?

A

Higher potency

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17
Q

Effect: Decreased substitution of benzene ring

A

Increased bioavailability and prolongs duration of action

Since they are not catecholamines, they are spared from COMT Inactivation in the Gut and Liver

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18
Q

Effect: Substitution on the Alpha Carbon

A

Prolonged action of drugs especially in noncatecholamines

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19
Q

Effect: Substitution on the Beta-Carbon

A

Important for storage

20
Q

Relative Selectivity of Adrenoceptor Agonists

Alpha Agonists
Phenylephrine, Midodrine

A

Alpha 1 > Alpha 2&raquo_space;»> Beta

Me-dodrine, me is 1

21
Q

Relative Selectivity of Adrenoceptor Agonists

Alpha Agonists
Clonidine, Methylnorepinephrine

A

Alpha 2 > Alpha 1&raquo_space;»> Beta

Clone ni Din, so they are 2

22
Q

Beta-1 Receptor Agonist Effect as a:

Chronotrope
Intrope

A

C: +
I: +

23
Q

What receptor agonists do you use for Congestive Heart Failure and Cardiogenic Shock

A

Beta-1 Receptor

24
Q

Classification of Dobutamine

A

Complex

( + ) Isomer: Alpha 1 Antagonist ; Beta-1 Agonist

( - ) Potent Alpha 1 Agonist

25
Q

Function: Alpha-1 Receptor Agonists

A

Constriction smooth muscles causing increased peripheral resistance and venous return

26
Q

Are there Alpha-1 receptors in the heart?

A

Yes

27
Q

How come if you give a lot of epinephrine it actually causes decreased heart rate instead of increased?

A

Reflex Baroreceptor Vagal Discharge

28
Q

Function: Alpha-2 Receptor Agonist

A

Reduce blood pressure

29
Q

Classification of Clonidine

A

Alpha-2

30
Q

Classification of Methyldopa

A

Alpha-2

Me-thoo

31
Q

Classification of Phenylephrine

A

Alpha-1

32
Q

Function: Alpha and Beta receptor agonists in GI Tract

A

Relax gastrointestinal smooth muscle

33
Q

Function: Alpha-2 Selective Agonists in GI Tract

A

Enhanced salt and water reabsorption

Treatment of diarrhea, Clonidine

34
Q

Function: Beta-2 Receptor Agonist in Genitourinary Tract

A

Relax smooth muscle

Relaxation of bladder wall

35
Q

Function: Alpha-1 Agonist in Genitourinary Tract

A

Constriction of bladder base, urethral sphincter

36
Q

Which receptor causes increased lipolysis in fat cells?

A

Beta-3

3 layers of fat

37
Q

Which receptor causes increased insulin uptake?

A

Beta-2

In-THWOO-Lin, pretend may lithp ka

38
Q

Effect: Amphetamine

A

Non-exocytotic release of Norepinephrine

It is taken up by NET and blocks MAO

39
Q

Examples of Alpha-1 Receptor Antagonists

A

Prazosin
Terzosin
Doxazosin

(They are SIN-ners, antagonists to Alpha-1)

40
Q

What is Tamsulosin used for?

A

Benign Prostatic Hypertrophy

Binds better to A and D better than B so it is used for this instead of for hypertension

41
Q

Is Epinephrine selective or non-selective?

A

Non-Selective

42
Q

Prototypic non-selective beta blocker

A

Propranolol

43
Q

Prototypic selective beta blocker

A

Metoprolol

44
Q

What are the selective B-Agonists?

A

A BEAM of B1-Blocker

Acebutolol
Betaxolol
Esmolol
Atenolol
Metoprolol
45
Q

Examples of Partial Agonists

A

Pindolol
Acebutulol

(Eh, why not Atenolol? Dahil hindi raw partial si Ate.)