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FTCM Pharm > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Adrenergic drugs are useful in treating?

A

a LOT

  • hypertension
  • angina
  • HF
  • Asthma
    etc. ..
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2
Q

Response to adrenergic drugs depends on…

A

proportion of a and b receptors in a tissue

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3
Q

NE and E difference in regards to receptors

A

NE little effect on B2 so cannot cause bronchodilation

E is a great bronchodilator

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4
Q

What receptors do skin blood vessels have?

A

a1

= vasoconstriction

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5
Q

What receptors do smooth muscle of blood vessels in skeletal muscles?

A

a1 AND b2

so a1 = vasoconstriction and b2 = vasodilation

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6
Q

Epinephrine at low dose causes…

A

Vasodilation

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7
Q

Epinephrine at high dose causes…

A

Vasoconstriction

bc a1 predominates

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8
Q

Adrenergic agonists:

A
  1. Direct
    - Endogenous catecholamines
    - B agonists
    - A agonists
  2. Indirect
    - Releasing agents
    - Uptake inhibitors
  3. Mixed
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9
Q

Endogenous catecholamines

A
  • NE
  • E
  • Dopamine
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10
Q

Epinephrine effects on organs

A
  • agonist at both a and b receptors
    B1 effect:
  • increase in HR
  • increase in renin

A1 effect:
- vasoconstriction

B2 effect:

  • bronchodilation
  • glycogenolysis
  • lipolysis (b1 and b2)
  • dilation of skeletal muscle
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11
Q

E in IV large dose increases?

A

BP due to B1 and A1 effects

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12
Q

E in IV low dose?

A

no increase in mean BP

B2 dominates = diastolic pressure falls

B1= increase systolic pressure and HR

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13
Q

Epinephrine uses

A
  1. Anaphylactic shock
  2. Acute asthmatic attacks
  3. Cardiac arrest
  4. Local anesthetics
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14
Q

Norepinephrine

A

agonist at a1, a2, b1 receptors

  • increased HR (b1)
  • increased vasoconstriction (a1)

increase in BP
baroreceptor reflex = bradycardia

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15
Q

Norepinephrine uses

A
  • treat shock
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16
Q

Norepinephrine interesting fact:

A

If atropine is given before NE then NE will cause tachycardia

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17
Q

Dopamine

A

D1 > B1 > a1 receptors

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18
Q

Low rates of dopamine

A
  • vasodilation
  • increase in GFR
  • increase in renal blood flow
  • increase Na excretion
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19
Q

Moderate rates of dopamine

A
  • B1 activation = increase CO = increase in SBP
  • increase in MAP
  • release of NE
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20
Q

High rates of dopamine

A
  • a1 activation = vasoconstriction = increase BP

- PVR increase

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21
Q

Dopamine uses:

A

CHF

moderate to high rates for shock

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22
Q

B agonists:

A
  1. Non selective
    - Isoproterenol
  2. B1 selective
    - Dobutamine
  3. B2 selective
    - Albuterol
    - Salmeterol
    - Formoterol
  4. B3 selective
    - Mirabegron
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23
Q

Isoproterenol

A

B1 and B2

  • increases HR
  • dilation of skeletal muscle
  • DBP falls
  • MAP falls
  • bronchodilation
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24
Q

Isoproterenol use:

A

emergency to stimulate HR in pt with bradycardia

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25
Q

Dobutamine

A
  • potent inotrope with mild chronotropic effects
  • mild effects
  • increase O2 consumption = dobutamine stress echocardiogram
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26
Q

Dobutamine use:

A
  • acute HF

- cardiogenic shock

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27
Q

B2 agonist used mainly for?

A

bronchodilation (B2)

asthma

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28
Q

Short acting vs Long acting:

A

SA:
- Albuterol

LA:

  • Salmeterol
  • Formoterol
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29
Q

B2 AE:

A
  • tremor, restlessness, anxiety, tachycardia
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30
Q

Mirabegron

A

B3 in bladder = detrusor muscle relaxation and increased bladder capacity

used for overactive bladder

AE: increased BP, UTI, headache

CYP2D6 inhibitor

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31
Q

A agonists:

A
  1. A1 selective
    - phenylephrine
  2. A2 selective
    - clonidine
    - methyldopa
    - brimonidine
32
Q

Phenylephrine

A

vasoconstriction A1

used:
- nasal decongestant
- treat hypotension
- mydriatic

33
Q

Clonidine

A
  • partial a2
  • hypertensive

AE: lethargy, sedation

34
Q

Methyldopa

A
  • decrease BP
  • hypertension during pregnancy

AE: sedation, impaired mental concentration

35
Q

Brimonidine

A
  • lower pressure in glaucoma
36
Q

Indirect acting agonists:

A
  1. releasing agents
    - amphetamine
    - methylphenydate
    - tyramine
  2. uptake inhibitors
    - Cocaine
    - Atomoxetine
    - Modafinil
37
Q

Amphetamine mechanism

A
  • reverse action of monoamine transporters = inhibit VMAT = increase in monoamines
38
Q

Amphetamine action

A
  • increase BP

AE: nervousness, insomnia, hypertension, anorexia

USED:

  • ADHD
  • Narcolepsy
39
Q

Methylphenidate

A

ADHD in kids

40
Q

Tyramine

A

found in fermented food

usually oxidized by MAO

41
Q

Cocaine

A
  • blocks DAT
  • high conc block SERT and NET
  • blocks voltage gated NA channels
    effects: tachycardia, hypertension, seizures
42
Q

Atomoxetine

A
  • inhibit NET

- ADHD

43
Q

Modafinil

A

MOA not known

  • psychostimulant
  • blocks NE and Dopamine transporters = increase in NE, dopamine, serotonin, glutamate
  • decrease GABA
  • narcolepsy
44
Q

Mixed agents:

A
  1. Ephedrine
  2. Pseudoephedrine
    - release of NE
    - activate adrenergic receptors
45
Q

Ephedrine

A

pressor agent used in spinal anesthesia

  • used in myasthenia gravis
46
Q

Pseudoephedrine

A
  • decongestant
47
Q

Adrenergic Antagonists:

A
  1. A antagonists
    - nonselective
    - a1
  2. B antagonists
    - non selective
    - b1
  3. A1 and B antagonists
  4. Partial agonists
  5. Presynaptic drugs
48
Q

Non selective A blockers:

A
  • phenoxybenzamine

- phentolamine

49
Q

phenoxybenzamine

A
  • irreversible

- pheochromocytoma

50
Q

phentolamine

A
  • reversible block of a1 and a2
    used in:
  • diagnosis of pheochromocytoma, hypertension
  • hypertensive crisis due to stimulant drug overdose
51
Q

ALL a blockers do what?

A

reverse epinephrine effects –> decrease in BP when given epinephrine and a blocker

52
Q

A1 selective blockers:

A

“sins”

  • prazosin (prototype)
  • terazosin
  • doxazosin
  • tamsulosin

used in hypertension and BPH

53
Q

A1 selective blockers CV effects

A
  • low BP

- first dose causes big response = fainting so first dose must be 1/3 or 1/4 normal dose

54
Q

Non selective B blockers:

A
  • Propranolol
  • Nadolol
  • Timolol
55
Q

B blocker effects:

A

CV: slow HR and decrease contractility

Resp: contraindicated in pt with asthma

Metabolic: decrease glycogenolysis and glucagon secretion

56
Q

B1 selective antagonists:

A

Atenolol
Metoprolol
Esmolol

57
Q

Atenolol & Metoprolol

A
  • hypersensitive pt with bad pulmonary function
58
Q

Esmolol

A

rapid control of ventricular rate in pt with atrial fibrillation or atrial flutter

59
Q

a1 and b blocker:

A

Labetalol

Carvedilol

60
Q

Labetalol

A

hypertension

61
Q

Carvedilol

A

hypertension and CHF

62
Q

Partial B agonist:

A

Pindolol

63
Q

Pindolol

A

diminished cardiac reserve or bradycardia

64
Q

B blocker use:

A
  • hypertension - decrease CO
  • glaucoma- esp timolol
  • migrane
  • hyperthyroidism
  • angina pectoris- chronic management*
  • atrial fibrillation
  • MI
  • bleeding from esophageal varices in cirrhosis
  • performance anxiety
  • essential tremor
65
Q

B blockers AE:

A
  • bronchoconstriction: especially non selective, B1 is better
  • hypoglycaemia: espeically non selective, B1 better
  • lipid metabolism: both non selective and B1 increase TG and reduce HDL–> unaffected by labetalol and pindolol
  • sedation, fatigue, dizziness
66
Q

Should B blockers be withdrawn fast or slow and why?

A

slowly to avoid tachycardia, hypertension, ischemia

67
Q

Presynaptic drugs:

A
  1. inhibit NE synthesis
    - a-methyltyrosine
  2. Inhibit NE storage
    - Reserpine
    - tetrabenazine
68
Q

a-methyltyrosine

A

inhibitor of tyrosine hydroxylase

- used to manage pheochromocytoma

69
Q

Reserpine

A

blocks VMAT
cannot store NE and D
MAO degrades NE in cytoplasm –> decrease BP and cardiac rate

  • past for hypertension
70
Q

tetrabenazine

A

inhibits VMAT

  • depletion of catecholamines
  • treats chorea in Huntington’s
71
Q

The eye has 2 muscles:

A
  1. Radial A1

2. Sphincter M3

72
Q

M agonist effect in eye

A

Contraction of sphincter M3= miosis

73
Q

Anti-M in eye:

A

relaxation of sphincter M3 = mydriasis

74
Q

a-adrenergic agonist in eye:

A

contraction of pupillary dilator in eye (radial muscle a1) = mydriasis

reduces aqueous humor production –> decrease pressure –> helps glaucoma

75
Q

b antagonists in eye

A

secretion of aqueous humour

blocking B2 –> reduces secretion –> helps glaucoma

76
Q

Prostaglandins in eye

A

found in ciliary body, muscle, wtc

increases uveoscleral outflow –> reduces pressure –> helps glaucoma

77
Q

Carbonic anhydrase inhibitors in eye

A

inhibit CA in ciliary body of epithelium–> reduces aqueous humor –> reduce pressure –> helps glaucoma

FTCM Pharm (4 decks)

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