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Pharmacology- Block 1 > (6) Autonomic Nervous System Drugs II (Norepinephrine & Epinephrine) > Flashcards

(6) Autonomic Nervous System Drugs II (Norepinephrine & Epinephrine) Flashcards

1
Q

Epinephrine (Class, Receptor Affinity, Dose-Dependent Effects, Uses, Adverse effects)

A
  1. Class: Non-selective, direct adrenergic agonist
  2. Receptor Affinity: Alpha 1 = Alpha 2; Beta 1 = Beta 2;
  3. Dose-Dep Effects:
    - Low dose = Beta effects; - High dose = Alpha 1 effects
  4. Uses: Anaphylactic shock, cardiac arrest, topical vasoconstriction
  5. Adverse effects: tremor, palpitations, headache & arrhythmias
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2
Q

Norepinephrine (Class, Receptor Affinity, Uses, Adverse effects)

A
  1. Class: Non-selective direct adrenergic agonist
  2. Receptor Affinity: Alpha 1 = Alpha 2; Beta 1 &raquo_space; Beta 2
  3. Uses: Hypotension
  4. Adverse effects: tremor, palpitations, headache & arrhythmias
  5. Greater peripheral vascular resistive effects than epinephrine (b/c less Beta 2 binding, which causes vasodilation)
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3
Q

Isoproterenol (Class, Receptor Affinity, Uses, Adverse effects)

A
  1. Class: Non-selective direct adrenergic BETA agonist
  2. Receptor Affinity: Beta 1 = Beta 2
  3. Uses: potent vasodilator (Beta 2 effects), inotropic agent (increase force of contraction) (Beta 1 effects)
  4. Adverse effects: tachycardia & arrhythmias
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4
Q

Dobutamine (Class, Receptor Affinity, Uses, Adverse effects)

A
  1. Class: Selective Beta-1 Agonist
  2. Receptor Affinity: Beta 1 > Beta 2&raquo_space;» Alpha
  3. Uses: Acute heart failure, (potent inotropic agent) & Cardiac stress testing
  4. Adverse: HTN & tachycardia
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5
Q

Albuterol, Levalbuterol & Salmeterol (Class, Effects, Uses)

A
  1. Class: Selective Beta 2 Agonist
  2. Effects: Bronchodilation
  3. Uses: Asthma & COPD
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6
Q

Terbutaline (Class, Route of Administration: Effects & Uses)

A
  1. Class: Selective Beta 2 Agonist
  2. ROA: Effects & Uses:
    - PO = Bronchodilation; Asthma
    - IV = Uterus smooth muscle relaxation; Delay premature labor
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7
Q

Phenylephrine (Class, Route of Administration: Effects & Uses)

A
  1. Class: Selective Alpha 1 Agonist
  2. ROA: Effects & uses
    - IV: Vasoconstriction; Hypotension & Shock
    - PO: OTC decongestant
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8
Q

Oxymetazoline (Class, Uses & Adverse Effects)

A

“Afrin” Nasal Spray

  1. Class: Selective Alpha 1 Agonist
  2. Uses: Topical nasal decongestant
  3. Adverse effects: Rebound congestion (Tachyphylaxis) if used more than several days
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9
Q

Clonidine (Class, Uses & ROA)

A
  1. Class: Selective Alpha 2 Agonist
  2. Uses: Centrally acting anti-HTN agent & Attenuating substance withdrawal symptoms
  3. PO or Transdermal patch
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10
Q

Alpha-Methyldopa (Class & Uses)

A
  1. Class: Selective Alpha 2 Agonist
  2. Uses: Centrally acting anti-HTN agent
  3. Useful during pregnancy
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11
Q

Amphetamine & Methamphetamine (Class, Mechanism, Effects & Chemical Characteristics)

A
  1. Class: Indirect Adrenergic Agonist
  2. Mechanism: Stimulate presynaptic NE & Dopamine release
  3. Effects:
    - Stimulatory on mood/alertness
    - Apetite depressant
    - Peripheral vasoconstriction
    - Cardiac stimulant
  4. Chemical Characteristics: Lipid soluble, thus enters CNS
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12
Q

Methylphenidate (Class, Mechanism, Effects & Chemical Characteristics)

A

“Ritalin”: Amphetamine derivative w/ similar action

  1. Class: Indirect Adrenergic Agonist
  2. Mechanism: Stimulate presynaptic NE & Dopamine release
  3. Effects:
    - Stimulatory on mood/alertness
    - Apetite depressant
    - Peripheral vasoconstriction
    - Cardiac stimulant
  4. Chemical Characteristics: Lipid soluble, thus enters CNS
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13
Q

Cocaine (Class, Mechanism & Effects)

A

Similar to Amphetamine: shorter/more intense

  1. Class Indirect Adrenergic Agonist
  2. Mechanism: Blocks NET & DAT reuptake of NE, Dopamine & Serotonin
  3. Effects:
    - Peripheral vasoconstriction
    - Cardiac stimulant
    - Local anesthetic (ocular surgery)
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14
Q

Tyramine (Class, Mechanism & Adverse effects)

A

Naturally occurring amine found in fermented products (cheese, sausage, red wine, beer, bananas, avocados, canned meats, sardines & yeast supplements)

  1. Class: Indirect Adrenergic Agonist
  2. Mechanism: Increases NE release
  3. Adverse effects: can cause HTN crisis w/ MAO inhibitors (used for depression)
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15
Q

Dopamine (Class, Receptor Affinity, Dose-Dependent Effects, Uses & Adverse Effects)

A
  1. Class: Mixed Adrenergic Agonist
  2. Receptor Affinity: D1 = D2&raquo_space; Beta 1&raquo_space; Alpha 1
  3. Dose-Dep Effects:
    - Low dose: D receptor (increase renal blood flow)
    - Med dose: D + Beta 1 receptors
    - High dose: D + Beta 1 + Alpha 1 receptors
  4. Uses: Cardiogenic shock & Acute renal failure
  5. Adverse effects @ high doses: tremor, palpitations, headache & arrhythmias
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16
Q

Ephedrine (Class, Mechanism, Effects)

A

Natural product in Ma-Haung plant

  1. Class: Mixed Adrenergic Agonist
  2. Mechanism: Alpha & Beta receptor Agonist + NE release
  3. Effects: Similar to Epinephrine @ high doses
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17
Q

Psuedoephedrine (Class, Mechanism, Uses & Adverse Effects)

A

“Sudafed”: Ephedrine stereoisomer

  1. Class: Mixed Adrenergic Agonist
  2. Mechanism: Alpha & Beta receptor + NE release
  3. Uses: Restricted OTC decongestant (primary ingredient in methamphetamine)
  4. Adverse Effects: Avoid in patients w/ HTN or cardiomyopathy
18
Q

Phenoxybenzamine (Class, Mechanism, Receptor Affinity, Uses & Adverse Effects)

A
  1. Class: Non-Selective Alpha Blockers
  2. Mechanism: Non-Competitive, Irreversible Antagonist
  3. Receptor Affinity: Alpha 1 > Alpha 2
  4. Uses: Pheochromocytoma (adrenal medulla tumor = catecholamine excess)
  5. Adverse: Postural hypotension & Reflex tachycardia
19
Q

Phentolamine (Class, Mechanism, Receptor Affinity, Uses, Adverse Effects)

A
  1. Class: Non-Selective Alpha Blockers
  2. Mechanism: Competitive, Reversible Antagonist
  3. Receptor Affinity: Alpha 1 = Alpha 2
  4. Uses: Pheochromocytoma & Ischemia reversal (caused by extravasation/epinephrine injection)
  5. Adverse Effects: Postural hypotension & Reflex tachycardia
20
Q

Prazosin, Terazosin & Doxazosin (Class, Effect, Uses & Adverse Effects)

A
  1. Class: Selective Alpha 1 Blockers
  2. Effects: Relax vascular, bladder & prostate smooth muscle
  3. Uses: BPH & 3rd rate HTN-agent (increased morbidity)
  4. Adverse: 1st dose syncope (pt must lay down) & reflex tachycardia
21
Q

Tamsulosin (Class, Effect & Uses)

A

“Flomax”

  1. Class: Selective Alpha 1 Blocker (Specific to Prostate Gland)
  2. Effect: Less vasodilation than other Alpha-1 blockers; little effect on BP @ normal dose
  3. Uses: BPH (decrease urinary obstruction)
22
Q

Propranolol (Class, Receptor Affinity, Effects, Uses, Adverse Effects)

A
  1. Class: Non-selective Beta Blockers
  2. Receptor Affinity: Beta 1 = Beta 2
  3. Effects:
    - Negative inotropic (cardiac contractility)
    - Chronotropic (heart rate)
    - Bronchoconstriction
    - Decreased glycogenolysis
  4. Uses: HTN, Arrhythmias, Angina, Migraines, Essential Tremor
  5. Adverse: Bradycardia, Insomnia, Heart failures, Asthma & Diabetes

Other:

  • Highest lipid solubility (CNS penetration)
  • Highest 1st pass effect: oral dose&raquo_space; IV dose
23
Q

Nadolol (Class, Other)

A

“Corgrad”

  1. Class: Non-Selective Beta Blockers
  2. Other:
    - Low lipophilicity = less adverse CNS effects than propranolol
    - Renal excretion
    - Long T 1/2
24
Q

Timolol (Class, Uses)

A
  1. Class: Non-Selective Beta Blockers

2. Uses: Topical agent for Glaucoma

25
Q

Pindolol (Class, Other)

A
  1. Class: Non-Selective Beta Blocker

2. Other: Partial Beta 1 & Beta 2 Agonist (intrinsic sympathomimetic activity) = less bradycardia

26
Q

Metoprolol (Class, Receptor Affinity, Uses, Other)

A

“Cardioselective Beta-Blocker”

  1. Class: Selective Beta 1 Blocker
  2. Receptor Affinity: Beta 1&raquo_space; Beta 2
  3. Uses:
    - Angina
    - Low dose: Heart failure
    - High dose: HTN
  4. Other
    - Safer for asthma & diabetes than non-selective beta blockers
    - T 1/2 varies from 3-8 hrs depending on CYP2D6 phenotype
27
Q

Atenolol (Class, Other)

A
  1. Class: Selective Beta 1 Blocker
  2. Other:
    - Low lipophilicity = less CNS adverse effects than propranolol
    - Renal excretion
    - Long T 1/2
28
Q

Bisoprolol (Class, Other)

A

“Zebeta”

  1. Class: Selective Beta 1 Blocker
  2. Other: Moderate lipophilicity
29
Q

Esmolol (Class, Other)

A
  1. Class: Selective Beta 1 Blocker

2. Other: IV Only

30
Q

Acebutolol (Class, Other)

A
  1. Class: Selective Beta 1 Blocker

2. Other: Partial Beta 1 agonist (intrinsic sympathomimetic activity)

31
Q

Labetalol (Class, Receptor Affinity, Use, Other)

A
  1. Class: Alpha & Beta Blocker
  2. Receptor Affinity: Beta 1 = Beta 2; Alpha 1 > Alpha 2
  3. Use: Rapid BP reduction
  4. Other
    - IV or PO
    - More vasodilation than other Beta blockers due to Alpha 1 blockage
32
Q

Carvedilol (Class, Receptor Affinity, Use, Other)

A

“Coreg”

  1. Class: Alpha & Beta Blocker
  2. Receptor Affinity: Beta 1 = Beta 2; Alpha 1 > Alpha 2
  3. Use: Heart failure
  4. Other
    - IV or PO
    - More vasodilation than other Beta blockers due to Alpha 1 blockage
33
Q

Alpha 1 Receptor Effects (4)

A
  1. Vascular smooth muscle contraction (vasoconstriction)
  2. Iris dilator muscle (mydriasis = pupil dilation)
  3. Pilomotor smooth muscle contraction (goosebumps/hairs stand up)
  4. Lower urinary tract (urethra/prostate) smooth muscle contraction
34
Q

Alpha 2 Receptor Effects (4)

A
  1. Platelet aggregation
  2. Inhibition of Adrenergic/Cholinergic neurotransmitter release (feedback inhibition)
  3. Inhibition of lipolysis
  4. Some vascular smooth muscle contraction
35
Q

Beta 1 Receptor Effects (2)

A

Heart:

  1. Increase force & rate of contraction
  2. Increase conduction velocity
36
Q

Beta 2 Receptor Effects (3)

A
  1. Respiratory, Uterine & Vascular smooth muscle RELAXATION
  2. Skeletal muscle potassium uptake
  3. Liver glycogenolysis
37
Q

Beta 3 Receptor Effects (1)

A

Fat cells:

1. Lipolysis activation

38
Q

Dopamine 1 (D1) Effects (1)

A

Smooth muscle:

1. Dilation of RENAL blood vessels

39
Q

Dopamine 2 (D2) Effects (1)

A

Nerve endings:

1. Modulate NT release in CNS

40
Q

Why must Catecholamines be given paraenterally?

A

Because they are rapidly metabolized by MAO & COMT

Pharmacology- Block 1 (6 decks)

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