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Pharmacology > S3 Catecholaminergic Drugs & Adrenergic Receptors > Flashcards

S3 Catecholaminergic Drugs & Adrenergic Receptors Flashcards

1
Q

Catecholaminergic drugs receptors
What is the signaling mechanism?
What stimulates all receptors?

A 
Alpha-adrenoceptors
Beta-adrenoceptors
Dopamine receptors 
ALL are coupled to G proteins
ALL are stimulated by Epi & NorEpi
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2
Q

Catecholaminergic molecules

A

Norepinephrine
Epinephrine
Dopamine

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3
Q

Alpha-adrenoceptors (A1 & A2)

Stimulator (effect) & blocker

A 
Stimulates all = Norepinephrine
Blocks all = Phentolamine
Stim. effect = smooth muscle CONTRACTION 
Alpha-1 = increases calcium
Alpha-2 = decreases cAMP
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4
Q

Beta-adrenoceptors (B1, B2 & B3)

Stimulator (effect) & blocker

A

Stimulates all = Isoproterenol
Blocks all = Propranolol
Stim. effect = smooth muscle RELAXATION
All increase cAMP

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5
Q

Dopamine stimulator (effect) & blocker

A

Stimulator = Apomorphine
Blocked = Chlorpromazine or Haloperidol
Stim. effect = Body wide vasoconstriction BUT vasodilation in kidney

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6
Q

Alpha1-adenoceptor locations

A

Smooth muscle

  • -Blood vessels
  • -Eye
  • -Bladder
  • -Heart
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7
Q

Alpha2-adenoceptor location

A 
*CNS neurons
Smooth muscle (some blood vessels)
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8
Q

Alpha-1 adenoceptor mechanism

A 
Increased Ca2+ --> activation of kinases
Location = smooth muscle
Effects 
1. Vasoconstriction
2. Mydriasis (dilation)
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9
Q

Alpha2-adenoceptor mechanism

A 
Dec. cAMP --> increased neuron K+
Location = CNS & smooth muscle
Effects
1. Vasoconstriction
2. Decreased release of NorEpi at nerve terminals
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10
Q

Beta1-adenoceptor mechanism

A 
Inc. cAMP & Beta-arrestin 
Location = heart, kidney, eye, nerves
Effects 
1. Increased HR and contractility
2. Increased Renin release
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11
Q

Beta2-adenoceptor mechanism

A 
Inc. cAMP & Beta-arrestin 
Location = smooth muscle
Effects
1. Smooth muscle relaxation
a. Vasodilation
b. Bronchodilation
c. Decreased GI motility
2. Increased blood glucose
3. Increased intracellular potassium
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12
Q

Beta3-adenoceptor mechanism

A

Inc. cAMP
NO clinical relevance
Location = adipocytes
Effect = increased lipolysis

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13
Q

Beta1-adenoceptor locations

A

*Heart
*Nerve terminals
Adipocytes
*Kidneys
*Eye

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14
Q

Beta2-adenoceptor locations

A
  • Smooth muscle
  • Airway
  • GI
  • Vasculature in skeletal muscle
  • Liver
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15
Q

Beta3-adenoceptor locations

A

*Adipocytes

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16
Q

Phenylephrine

A

Alpha1-adenoceptor selective agonist

Antagonist partner = Prazosin

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17
Q

Epinephrine

A

BOTH alpha- & beta-adenoceptor agonist

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18
Q

Isoproterenol

A

Beta-adenoceptor agonist

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19
Q

Dopamine

A

D1- & D2-receptors agonist
Low dose selective
High doses also bind to adenoceptrors

20
Q

Fenoldopam

A

D1-dopamine receptor selective agonist
NO effect on adenoceptors
Common crash cart drug

Effects

  1. Body wide = vasoconstriction
  2. Kidney = vasodilation
21
Q

Epinephrine (clinical use)

A

Alpha1,2- & Beta1,2,3- andenoceptor agonist

Effects
1. Vasoconstriction
a. Increased CO & systolic BP
2. Skeletal muscle vasodilation 
a. Decreased diastolic BP
= widens pulse range

Indications

  1. Anaphylactic shock
  2. Heaves
  3. Cardiac arrest
  4. Hypotension (shock)
  5. Hemostasis (applied locally)
  6. Added to Lidocaine to reduce diffusion

Risk of dysrhythmias

22
Q

Norepinephrine (clinical use)

A

Alpha1,2- & Beta1-adenoceptor agonist

Effects

  1. Vasoconstriction (Alpha1,2)
    a. Increased BP
  2. Reflex decreased HR

Indications

  1. Hypotension (shock)
  2. Cardiac arrest

Risk of dysrhythmias

23
Q

Phenylephrine

A

Alpha1-adenoceptor selective agonist

Effects (smooth muscle)

  1. Increased BP
  2. Reflex decreases HR
  3. Mydriasis (dilation)
24
Q

Medatomidine

A

Alpha2-adenoceptor selective agonist
Similar drug = Xylazine
(Antagonist partners = Atipamezole & Yohimnine)

Effects (CNS & blood vessels)

  • Decreases NT release = potassium
    1. Sedation
    2. Analgesia
    3. Hypotension
25
Q

Xylazine

A

Alpha2-adenoceptor selective agonist
Rompun brand
Similar drug = Medatomide
(Antagonist partners = Atipamezole & Yohimnine)

Effects (CNS & blood vessels)

  • Decreases NT release = potassium
    1. Sedation
    2. Analgesia
    3. Hypotension
    4. Vomiting at low doses
26
Q

Isoproterenol

A

BOTH Beta1- & beta2-adenoceptor agonist

Effects
1. Increased HR & CO 
a. Increased systolic BP
2. Huge skeletal muscle vasodilation
a. Big decrease in diastolic BP
3. Bronchodilator 
*Similar effect to Epinephrine 
Risk for arrhythmias
27
Q

Dobutamine

A

Beta1-adenoceptor selective agonist
(Antagonist partners = Atenolol, Betaxolol & Esmolol)

Effects (heart, kidney, nerves, eye)

  1. Increases cardiac contractility = inc. CO
  2. Increases HR
    * Stereoselectivity is important
28
Q

Albuterol

A

Beta2-adenoceptor selective agonist
Similar drug = Clenbuterol
NO antagonists

29
Q

Clenbuterol

A

Beta2-adenoceptor selective agonist
Similar drug = Albuterol
NO antagonists

Effects (heart, kidney, nerves, eye)

  1. Relaxes smooth muscle
    a. Bronchodilator
    b. Uterine relaxation = slows down labor
    c. Vasodilation
30
Q

Ractopamine

A

BOTH Beta1- & beta2-adenoceptor agonist
Paylean brand
Controversial feed additive
Turkeys, pigs and cattle

Effects
1. Increases blood flow to skeletal muscle

31
Q

Phentolamine

A

BOTH Alpha1- & alpha2-adenoceptor antagonist

Effects (smooth muscle)
1. Orthostatic hypotension (stand up = faint)

32
Q

Prazosin

A

Alpha1-adenoceptor selective antagonist
(Agonist partner = Phenylephrine)

Effects (smooth muscle)

  1. Decreases pre- & after-load = CHF
  2. Decreases BP
  3. Decreases SM contractions
33
Q

Yohimbine

A

Alpha2-adenoceptor selective antagonist
Shares effects with Atipamezole

Effects (CNS & blood vessels)
1. Reversal agent of Alpha2-agonists
Ex. Xylazine & Medetomidine

34
Q

Propranolol

A

BOTH Beta1- & beta2-adenoceptor antagonist

Effects

  1. Decreases HR & contractility
    a. Dec. CO
  2. Blocks effects of NorEpi at AV node
    a. Decreases activity of ectopic pacemakers

Indications

  1. Hypertension
  2. Class II anti-arrhythmia drug
35
Q

Atenolol

A

Beta1-adenoceptor selective antagonist
Shares effects with Betaxolol, Esmolol & Carvedilol

Effects (heart, nerve, kidney, eye)

  1. Decreases HR and contractility
    a. Reduces CO
  2. Decreases AV node conduction
    b. Anti-arythmia class II drug
36
Q

Betaxolol

A

Beta1-adenoceptor selective antagonist
Shares effects with Atenolol, Esmolol & Carvedilol

Effects (heart, nerve, kidney, eye)

  1. Decreases HR and contractility
    a. Reduces CO
  2. Decreases AV node conduction
    b. Anti-arythmia class II drug
    * Treatment of glaucoma!
37
Q

Esmolol

A

Beta1-adenoceptor selective antagonist
Shares effects with Atenolol, Betaxolol & Carvedilol
Very short acting

Effects (heart, nerve, kidney, eye)

  1. Decreases HR and contractility
    a. Reduces CO
  2. Decreases AV node conduction
    b. Anti-arythmia class II drug
38
Q

Carvedilol

A

Beta1-adenoceptor selective antagonist
Shares effects with Atenolol, Betaxolol & Esmolol

Effects (heart, nerve, kidney, eye)

  1. Decreases HR and contractility
    a. Reduces CO
  2. Decreases AV node conduction
    b. Anti-arythmia class II drug
39
Q

Antipamezole

A

Alpha2-adenoceptor selective antagonist

Shares effects with Yohimbine

40
Q

Crash cart drugs

A
  1. Atropine
  2. Epinephrine & norepinephrine
  3. Isoproterenol
  4. Dobutamine
  5. Dopamine & fenoldopam
  6. Yohimbine
41
Q

Two drugs that both dilate pupils

A
  1. mAChR blocker
    = Atropine, Scopolamine
  2. Alpha1-andenoceptor agonist
    = Phenylephrine
42
Q

Alpha-adenoceptor agonists

A

Norpeinephrine (both)
Phenylephrine (A1)
Medatomidine (A2)
Xylazine (A2)

43
Q

Alpha-andeoceptor antagonists

A

Phentolamine (both)
Prazosin (A1)
Yohimbine (A2)
Antipamezole (A2)

44
Q

Beta-adenoceptor agonists

A 
Isoproterenol (both)
Ractopamine (both)
Dobutamine (B1)
Albuterol (B2)
Clenbuterol (B2)
45
Q

Beta-adenoceptor antagonists

A 
Propranolol (both)
Atenolol (B1)
Betaxolol (B1)
Esmolol (B1)
Carvedilol (B1)

Pharmacology (9 decks)

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