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Cardiopulm Exam 1 > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

What is the G protein and effect of alpha-1 type receptor?

A

G protein: Gq

Effect: Increased IP3, DAG common to all

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2
Q

What is the G protein and effect of alpha-2 type receptor?

A

G protein: Gi

Effect: Decreased cAMP common to all

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3
Q

What is the G protein and effect of Beta-type receptor?

A

G protein: Gs

Effect: Increased cAMP common to all

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4
Q

What is the G protein and effect of Dopamine-type receptor D1-D5?

A
  • D1: Gs; Increased cAMP
  • D2: Gi; Decreased cAMP
  • D3: Gi; Decreased cAMP
  • D4: Gi; Decreased cAMP
  • D5: Gs; Increased cAMP
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5
Q

What is the location and effects of activation of alpha-1 type receptor?

A
  • Most vascular smooth muscle (innervated): Contraction
  • Pupillary dilator muscle: Contraction (dilates muscle)
  • Prostate: Contraction
  • Heart: Increases force of contraction
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6
Q

What is the location and effects of activation of alpha-2 type receptor?

A
  • Postsynaptic CNS neurons: Probably multiple actions
  • Platelets: Aggregation
  • Adrenergic and cholinergic nerve terminals: Inhibits transmitter release
  • Some vascular smooth muscle: Contraction
  • Fat cells: Inhibits lipolysis
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7
Q

What is the location and effects of activation of Beta-1 type receptor?

A

• Heart, juxtaglomerular cells: Increases force and rate of contraction; increases renin release

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8
Q

What is the location and effects of activation of Beta-2 type receptor?

A
  • Respiratory, uterine and vascular smooth muscle: Promotes smooth muscle relaxation
  • Skeletal muscle: Promotes potassium uptake
  • Human liver: Activates glycogenolysis and gluconeogenesis
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9
Q

What is the location and effects of activation of Beta-3 type receptor?

A
  • Bladder: Relaxes detrusor muscle

* Fat cells: Activates lipolysis

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10
Q

What is the location and effects of activation of D1 type receptor?

A

• Smooth muscle: Dilates renal blood vessels

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11
Q

What is the location and effects of activation of D2 type receptor?

A

• Nerve endings: Modulates transmitter release

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12
Q

Direct Adrenomimetics: Alpha Agonists

A

• Phenylephrine (Neo-Synephrine)
- a1 > a2&raquo_space;»> B

• Clonidine (Catapres)
- a2> a1&raquo_space;»> B

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13
Q

Direct Adrenomimetics: Mixed alpha and beta agonists

A

• Norepinephrine (Levophed)
- a1 = a2; B1&raquo_space; B2

• Epinephrine (Adrenalin)
- a1 = a2; B1 = B2

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14
Q

Direct Adrenomimetics: Beta agonists

A

• Dobutamine (Dobutrex)
- B1 > B2&raquo_space;» a

• Isoproterenol (Isuprel)
- B1 = B2&raquo_space;» a

• Albuterol (Ventolin)
- B2&raquo_space; B1&raquo_space;» a

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15
Q

Direct Adrenomimetics: Dopamine agonists

A

• Dopamine (Intropin)

- D1 =D2&raquo_space; B&raquo_space; a

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16
Q

Indirect Adrenomimetics:

  • Inhibits re-uptake of DA and NE
A

Cocaine

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17
Q

Indirect Adrenomimetics:

  • Inhibitors of MAO
A
  • Selegiline (Eldepryl)

* Phenelzine (Nardil)

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18
Q

Indirect Adrenomimetics:

  • Reverse NE and DA uptake mechanisms and increase their release
A
  • Amphetamines
  • Methylphenidate (Ritalin)
  • Tyramine (a byproduct of tyrosine metabolism, not a drug)
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19
Q

Indirect Adrenomimetics:

  • Releasing agent AND a direct adrenergic receptor agonist
A

Ephedrine

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20
Q

Direct acting antiadrenergic drugs: alpha adrenoceptor antagonists

  • Non-selective (a 1 and a 2) receptor antagonists
  • alpha-1 receptor selective (all end in -osin)
A

• Non-selective (a1 and a2) receptor antagonists

  • Phentolamine (OraVerse)
  • Phenoxybenzamine (Dibenzyline)

• Alpha- 1 receptor selective

  • Prazosin (Minipress)
  • Tamsulosin (Flomax)
  • Doxazosin (Cardura)
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21
Q

Direct acting antiadrenergic drugs: Mixed Blockers

A
  • Labetalol (Trandate) (B- and alpha-1 antagonist)

* Carvedilol (Coreg) (B- and alpha-1 antagonist)

22
Q

Direct acting antiadrenergic drugs: Beta Adrenoceptor Blockers

  • B1 and B2 blockers
  • B1 selective
A

• B1 and B2 blockers

  • Propranolol (Inderal)
  • Pindolol (Visken)
  • Nadolol (Corgard)

• B1 selective

  • Metoprolol (Toprol)
  • Betaxolol (Kerlone)
  • Acebutolol (Sectral)
  • Atenolol (Tenormin)
23
Q

Indirect acting antiadrenergic drugs:

  • Norepinephrine release inhibitor
  • Inhibitor of tyrosine hydroxylase
A

• Norepinephrine release inhibitor
- Guanethidine (Ismelin)

• Inhibitor of tyrosine hydroxylase
- Metyrosine (Demser)

24
Q

Intrinsic activities of beta-blockers at the receptors:

Which ones are antagonists?

A

– Atenolol
– Nadolol
– Propranolol
– Betaxolol

25
Intrinsic activities of beta-blockers at the receptors: Which ones are partial agonists?
– Acebutolol – Labetalol – Pindolol
26
Intrinsic activities of beta-blockers at the receptors: Which ones are inverse agonists?
– Carvedilol | – Metoprolol
27
Epinephrine effects on Cardiac Function (B1)
– Increases the force of contraction (positive inotropic effect) – Increases heart rate – Increases conduction velocity at AV node
28
Epinephrine effects on Vascular Tone (B2 and a1)
• Increases systolic BP • May decrease diastolic BP and total peripheral vascular resistance • Mean arterial pressure often remains unchanged •Significant differences in receptor types found in vascular beds - Skin vessels and mucous membranes = mostly a1 - skeletal muscle = a1 and B2 - Renal, cerebral = D1 and a1
29
Epinephrine effects on respiratory system
* Relaxes bronchial muscle (B2) | * Decreases bronchial secretion and congestion within bronchial mucosa (a1)
30
Epinephrine: Other Effects - Skeletal muscle? - Glucose? - Free fatty levels? - Renin?
• Effects on skeletal muscle: - Causes muscle tremor (B2) - Increases K+ uptake by skeletal muscle (B2) - Promotes hypokalemia and decreases K+ excretion by kidneys • Elevates blood glucose levels - Enhances liver glycogenolysis and gluconeogenesis (B2) * Increases free fatty levels in blood (B) * Increases renin release (B1)
31
Norepinephrine Effects
* Potent cardiac stimulant but reduces heart rate * Potent vasoconstrictor * Lacks vasodilation * Increases peripheral vascular resistance and blood pressure * Role of baroreflex
32
Alpha Agonist (a1>a2) : Phenylephrine Effects
– Effective mydriatic and decongestant – Causes severe vasoconstriction, blood pressure elevation, and severe bradycardia – Role of baroreflex in the response to phenylephrine
33
Alpha Agonist: Clonidine (selective a2)
``` • Central effect on presynaptic a2 receptors in the lower brainstem area - Decreasing sympathetic outflow - Reduction in blood pressure - Bradycardia ``` •Local application produces vasoconstriction
34
Beta Agonist (B1=B2): Isoproterenol Effects
– Non-selective beta agonist – Positive inotropic and chronotropic action, increases cardiac output ( B1) – Vasodilator, decreases arterial pressure ( B2) – Causes bronchodilation ( B2)
35
Beta Agonist (B1>B2): Dobutamine
• Selective B1 agonist • a1 receptor activity - (-) isomer is an agonist at the receptors while (+) isomer is an a1 antagonist * Potent inotropic action * Less prominent chronotropic action as compared to isoproterenol
36
Beta Agonist (B2>B1): Albuterol
* Selective B2 agonists | * Cause bronchodilation and relaxation of uterus
37
Dopamine (D1=D2) Effects
•D1 stimulation causes vasodilation - High density of D1 receptors in renal, cerebral, mesenteric and coronary vessels • Activation of presynaptic D2- suppresses norepinephrine release * Activation B1 in heart at higher doses * At still higher doses stimulates vascular a1 AR to cause vasoconstriction
38
Drug used to increase BP: For hypotensive emergencies - hemorrhagic shock, overdose of antihypertensives, CNS depressants
* Norepinephrine | * Phenylephrine
39
Drug used to increase BP: For chronic hypotension
Ephedrine
40
Drug used to increase BP: For cardiogenic shock – due to massive acute myocardial infarction
* Dopamine | * Dobutamine
41
Drugs used for heart failure: - Acute HF - Congestive severe HF
– Short-term use of dobutamine in acute HF – Dopamine in congestive severe HF with reduced renal perfusion
42
What drug is used for hypertension?
Alpha-2 agonists for the long-term treatment
43
What drug is used for emergency therapy for complete AV block and cardiac arrest
– Epinephrine | – Isoproterenol
44
What drug is used for Narcolepsy – sudden brief sleep attacks
– Amphetamines | – Methylphenidate
45
What drug is used for ADHD – short attention span, learning problems, and hyperkinetic physical behavior
Methylphenidate
46
What drug is used for Obesity – central inhibition of appetite and increased energy expenditure
– Ephedrine | – Amphetamines
47
What drug is used for Bronchial asthma
– Beta-2 selective agonist | • Albuterol
48
What drug is used for decongestion of mucous membranes
– Phenylephrine – Ephedrine
49
What drug is used for Anaphylaxis – immediate (type 1) allergic reaction characterized by respiratory and cardiovascular components
– Respiratory component - bronchospasm and upper airway congestion – Cardiovascular component- severe hypotension, cardiac depression – Epinephrine - effective at both components
50
What drug is used for Ophthalmic applications: – Examination of retina – induction of mydriasis
Phenylephrine
51
What drug is used for Ophthalmic applications: – Glaucoma
Alpha-2 selective agonists
52
What drug is used for Genitourinary applications: Stress urinary incontinence
Ephedrine

Cardiopulm Exam 1 (13 decks)

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