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Pharmacology > S3 Catecholaminergic Drugs & Adrenergic Receptors > Flashcards

S3 Catecholaminergic Drugs & Adrenergic Receptors Flashcards

(45 cards)

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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

Study These Flashcards
A

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

20
Q

Fenoldopam

Study These Flashcards
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)

Study These Flashcards
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)

Study These Flashcards
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

Study These Flashcards
A

Alpha1-adenoceptor selective agonist

Effects (smooth muscle)

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

Medatomidine

Study These Flashcards
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
Xylazine
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
Isoproterenol
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
Dobutamine
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
Albuterol
Beta2-adenoceptor selective agonist Similar drug = Clenbuterol NO antagonists
29
Clenbuterol
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
Ractopamine
BOTH Beta1- & beta2-adenoceptor agonist Paylean brand Controversial feed additive Turkeys, pigs and cattle Effects 1. Increases blood flow to skeletal muscle
31
Phentolamine
BOTH Alpha1- & alpha2-adenoceptor antagonist Effects (smooth muscle) 1. Orthostatic hypotension (stand up = faint)
32
Prazosin
Alpha1-adenoceptor selective antagonist (Agonist partner = Phenylephrine) Effects (smooth muscle) 1. Decreases pre- & after-load = CHF 2. Decreases BP 3. Decreases SM contractions
33
Yohimbine
Alpha2-adenoceptor selective antagonist Shares effects with Atipamezole Effects (CNS & blood vessels) 1. Reversal agent of Alpha2-agonists Ex. Xylazine & Medetomidine
34
Propranolol
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
Atenolol
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
Betaxolol
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
Esmolol
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
Carvedilol
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
Antipamezole
Alpha2-adenoceptor selective antagonist | Shares effects with Yohimbine
40
Crash cart drugs
1. Atropine 2. Epinephrine & norepinephrine 3. Isoproterenol 4. Dobutamine 5. Dopamine & fenoldopam 6. Yohimbine
41
Two drugs that both dilate pupils
1. mAChR blocker = Atropine, Scopolamine 2. Alpha1-andenoceptor agonist = Phenylephrine
42
Alpha-adenoceptor agonists
Norpeinephrine (both) Phenylephrine (A1) Medatomidine (A2) Xylazine (A2)
43
Alpha-andeoceptor antagonists
Phentolamine (both) Prazosin (A1) Yohimbine (A2) Antipamezole (A2)
44
Beta-adenoceptor agonists
``` Isoproterenol (both) Ractopamine (both) Dobutamine (B1) Albuterol (B2) Clenbuterol (B2) ```
45
Beta-adenoceptor antagonists
``` Propranolol (both) Atenolol (B1) Betaxolol (B1) Esmolol (B1) Carvedilol (B1) ```

Pharmacology (9 decks)

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