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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
Q

Intrinsic activities of beta-blockers at the receptors:

Which ones are partial agonists?

A

– Acebutolol
– Labetalol
– Pindolol

26
Q

Intrinsic activities of beta-blockers at the receptors:

Which ones are inverse agonists?

A

– Carvedilol

– Metoprolol

27
Q

Epinephrine effects on Cardiac Function (B1)

A

– Increases the force of contraction (positive inotropic effect)
– Increases heart rate
– Increases conduction velocity at AV node

28
Q

Epinephrine effects on Vascular Tone (B2 and a1)

A

• 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
Q

Epinephrine effects on respiratory system

A
  • Relaxes bronchial muscle (B2)

* Decreases bronchial secretion and congestion within bronchial mucosa (a1)

30
Q

Epinephrine: Other Effects

  • Skeletal muscle?
  • Glucose?
  • Free fatty levels?
  • Renin?
A

• 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
Q

Norepinephrine Effects

A
  • Potent cardiac stimulant but reduces heart rate
  • Potent vasoconstrictor
  • Lacks vasodilation
  • Increases peripheral vascular resistance and blood pressure
  • Role of baroreflex
32
Q

Alpha Agonist (a1>a2) : Phenylephrine Effects

A

– Effective mydriatic and decongestant

– Causes severe vasoconstriction, blood pressure elevation, and severe bradycardia

– Role of baroreflex in the response to
phenylephrine

33
Q

Alpha Agonist: Clonidine (selective a2)

A 
• Central effect on presynaptic  a2 receptors in the lower
brainstem area
- Decreasing sympathetic outflow 
- Reduction in blood pressure 
- Bradycardia

•Local application
produces
vasoconstriction

34
Q

Beta Agonist (B1=B2): Isoproterenol Effects

A

– Non-selective beta agonist

– Positive inotropic and chronotropic action, increases cardiac output ( B1)

– Vasodilator, decreases arterial pressure ( B2)

– Causes bronchodilation ( B2)

35
Q

Beta Agonist (B1>B2): Dobutamine

A

• 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
Q

Beta Agonist (B2>B1): Albuterol

A
  • Selective B2 agonists

* Cause bronchodilation and relaxation of uterus

37
Q

Dopamine (D1=D2) Effects

A

•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
Q

Drug used to increase BP:

For hypotensive emergencies - hemorrhagic shock, overdose of antihypertensives, CNS depressants

A
  • Norepinephrine

* Phenylephrine

39
Q

Drug used to increase BP:

For chronic hypotension

A

Ephedrine

40
Q

Drug used to increase BP:

For cardiogenic shock – due to massive acute myocardial infarction

A
  • Dopamine

* Dobutamine

41
Q

Drugs used for heart failure:

  • Acute HF
  • Congestive severe HF
A

– Short-term use of dobutamine in acute HF

– Dopamine in congestive severe HF with reduced renal perfusion

42
Q

What drug is used for hypertension?

A

Alpha-2 agonists for the long-term treatment

43
Q

What drug is used for emergency therapy for complete AV block and cardiac arrest

A

– Epinephrine

– Isoproterenol

44
Q

What drug is used for Narcolepsy – sudden brief sleep attacks

A

– Amphetamines

– Methylphenidate

45
Q

What drug is used for ADHD – short attention span, learning problems, and hyperkinetic physical behavior

A

Methylphenidate

46
Q

What drug is used for Obesity – central inhibition of appetite and increased energy expenditure

A

– Ephedrine

– Amphetamines

47
Q

What drug is used for Bronchial asthma

A

– Beta-2 selective agonist

• Albuterol

48
Q

What drug is used for decongestion of mucous membranes

A

– Phenylephrine – Ephedrine

49
Q

What drug is used for Anaphylaxis – immediate (type 1) allergic reaction characterized by respiratory and cardiovascular components

A

– Respiratory component - bronchospasm and upper airway congestion

– Cardiovascular component- severe hypotension, cardiac depression

– Epinephrine - effective at both components

50
Q

What drug is used for Ophthalmic applications:

– Examination of retina – induction of mydriasis

A

Phenylephrine

51
Q

What drug is used for Ophthalmic applications:

– Glaucoma

A

Alpha-2 selective agonists

52
Q

What drug is used for Genitourinary applications:

Stress urinary incontinence

A

Ephedrine

Cardiopulm Exam 1 (13 decks)

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