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PTP&M: Neuro > Adrenergics > Flashcards

Adrenergics Flashcards

1
Q

Inhibitor: Tyrosine Hydroxylase

A

Catalyzes Tyrosine –> DOPA metabolism
RATE-LIMITING STEP

Metyrosine

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2
Q

Inhibitor: VMAT

A

Blocks H+/dopamine countertransport
Vesicular Monoamine Transporter (VMAT)

Reserpine

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3
Q

Inhibitor: Vesicle release

A

Inhibits VAMP/SNAP interaction + NE/ATP/P release

Bretylium
Guanethidine

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4
Q

Inhibitor: NET

A

Norepinephrine Transporter (NET)

Cocaine,
Tricyclic Antidepressants (TCAs)
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5
Q

Chatecholamines (3)

A
  1. ) Dopamine
  2. ) Norepinephrine
  3. ) Epinephrine
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6
Q

Indolamines (2)

A
  1. ) Serotonin (5-HT)

2. ) Melatonin

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7
Q

Reserpine

A

Inhibitor of VMAT transport
-depletes secretory vesicles of NTs
-prevents release into synapses
S/Sx: MAJOR depressive disorder (“no joy”)

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8
Q

MAO (MOA + 2 Classes)

A 
Monoamine Oxidase
-converts amine --> acid (inactivates)
-associated with mitochondria (intracellular)
MAO-A --> 5-HT + NE
MAO-B --> dopamine (DA)
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9
Q

COMT

A

Catechol-O-methyltransferase

  • methylates hydroxyl group (ring)
  • POST-synaptic membrane + cytosol
  • primarily extracellular**
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10
Q

Alpha-1 Receptors

A

Vascular SM

Fx: vasoconstriction

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11
Q

Alpha-2 Receptors

A

Brain
Fx: lowers blood pressure

“reduce sympathetic output”

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12
Q

Beta-1 Receptors

A

Heart

Fx: increased contraction force, increase HR

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13
Q

Beta-2 Receptors

A

Bronchial SM + Vascular SM

Fx: Dilation (both areas)

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14
Q

Beta-3 Receptors

A

Adipose tissue
Fx: lipolysis

VERY RARE

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15
Q

Beta-Adrenergic Receptors: GCPR Effect

A

Increase/stimulate Adenylate Cyclase (AC)

Increased [cAMP]

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16
Q

Alpha-Adrenergic Receptors: Adenylate Cyclase (AC)

A

Decreased/inhibits Adenylate Cyclase (AC)

Decreased [cAMP]

17
Q

Uses of Adrenergic Agonists

A

Cardiovascular (Shock, anaphylaxis, HTN)
Respiratory (COPD, asthma)
Ophthalmic (glaucoma, dilation)
CNS (ADHD, narcolepsy, pain, depression)

18
Q

NorEpi Therapy Problems (4)

A
  1. ) Non-selective (a1, a2, b1, b2)
  2. ) Rapid metabolism (COMT + MAO)
  3. ) Poor oral bioavailability
  4. ) Does not cross BBB
19
Q

NorEpi Alterations: Amino Substitution

A

Increases b-receptor affinity

-prevents MAO-A metabolism (blocks amino group)

20
Q

NorEpi Alteration: OH modification

A

Inhibits COMT-metabolism

  • increases oral bioavailability
  • increased duration of action
  • increases BBB penetration/permeability
21
Q

Epinephrine (modifications, receptor affinity)

A

Methyl group added to NorEpi NH2 (blocks MAO)

a1 = a2 = b1 ≈ b2

22
Q

Isoproterenol (modifications, receptor affinity)

A

Isopropyl group conjugated to NorEpi NH2
b1 = b2&raquo_space;»»>a1/2

Affinity to b receptors increases as group conjugated to amine increases in size (CH3 vs. CH(CH3)2)

23
Q

Adrenergic Agonist Effects: a1

A

a1 –> peripheral blood vessel SM (vasoconstriction)
Increased BP, peripheral resistance

Non-CV: decongestant, pupil dilation (phenylephrine)
NO EFFECT ON ACCOMMODATION

24
Q

Adrenergic Agonist Effects: a2

A

a2 –> post-synaptic receptors brain
Reduced sympathetic outflow, decreased BP

Non-CV: decongestant, glaucoma (brimonidine)

25
Q

Adrenergic Agonist Effects: b1

A

b1 –> heart/cardiac myocytes
increased HR, contractile force, increased BP

Non-CV: INCREASE aqueous humor secretion

26
Q

Adrenergic Agonist Effects: b2

A

b2 –> bronchiole + vascular SM
(dilation)
Vasodilation, decreased BP, decreased peripheral resistance

Non-CV: Bronchodilation (terbutaline)

27
Q

Timolol

A

Julie’s procedure

  • Non-selective (b1 + b2)
  • Increases aqueous humor production, but DECREASES amount going into eye (decreases pressure)
  • non-specific therefore some off-target effects (if in circulation)
28
Q

Betaxolol

A

b-1 selective glaucoma agent

29
Q

Tx: ADHD (3)

A
  1. ) Amphetamine
  2. ) Methylphenidate
  3. ) Atomoxetine (reuptake inhibitor)
30
Q

Tx: Appetite Suppression (3)

A
  1. ) Amphetamine
  2. ) Methamphetamine
  3. ) Phentermine
31
Q

Narcolepsy Tx

A

Modafinil

  • inhibits DA reputake
  • increases NE, 5-HT, orexin, histamine, glutamate (indirectly)
  • decreases GABA transmission
32
Q

Psychostimulants: ADEs

A

Cardiovascular (tachy, HTN, CAs)
CNS (hyper, anxiety, HA, weight loss)
GI (N/V, urinary retention)
Addiction

PTP&M: Neuro (5 decks)

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