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Neorologia > Adrenergic > Flashcards

Adrenergic Flashcards

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1
Q

NE synthesis rate limiting step

A

Tyrosine to DOPA via Tyrosine Hydroxylase

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2
Q

VMAT

A

Vesicular Monoamine Transporter:

Transports dopamine into vesicle

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3
Q

Which receptor type is primarily associated with autoreceptor feedback

A

Alpha2 adnrenergic

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4
Q

Autoregulation process

A

Alpha2 coupled to Gi gprotein, decreases cGMP, decreases calcium, decreased vesicular release

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5
Q

L-DOPA to Dopamine

A

Dopa decarboxylase

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6
Q

Dopamine to Noradtrenaline

A

Dopamine beta hydroxylase (DBH)

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7
Q

Noradrenaline to Adrenaline

A

Phenylethanolamine-N-methyltransferase (PNMT)

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8
Q

NE to Epi

A
  1. Some NE diffuses out of vesicle,
  2. is methylated by PHMT to Epi
  3. Epi diffuses back into vessicle
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9
Q

Why can’t pt on MAOI have smoked meat, wine, and fermented cheese?

A

Contains tyramine; A MAO-A inhibitor

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10
Q

Which MAO is more selective and what for?

A

MAO-B ; Dopamine

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11
Q

Reserpine (Serpasil)

MAO and Use

A

Blocks VMAT-2
Previously; CNS-dystonias
previously; anti-hypertensive

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12
Q

Carbidopa (Lodosyn)
MOA
Use
Distribution

A
  • Inhibits Dopa Decarboxylase
  • Adjunctive PD treatment
  • Prevents peripheral conversion of L-Dopa to dopamine
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13
Q

Alpha1
Type
Location
Response

A

Gq
Vascular Smooth Muscle
Glandular Smooth Muscle
Contraction

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14
Q

Alpha2
Type
Location
Response

A

Gi

  • Presynaptic Nerve Terminals
  • Decrease NE release
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15
Q

Beta1
Type
Location
Response

A
  • Gs
  • Cardiac Muscle
  • Increase HR and FOC
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16
Q

Beta 2
Type
Location
Response

A

-Gs
-Vascular Smooth Muscle - Relaxation
Bronchiole Smooth Muscle - Relaxation
Skeletal Muscle - Glycogenolysis
Liver -Glycogenolysis and Gluconeogenesis

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17
Q

Beta 3
Type
Location
Response

A

Gs
Adipose - lipolysis
Bladder SM - Relaxation

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18
Q

Atomoxetine (Strattera)

MOA

A

Selective NERI;

Indirect Agonism

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19
Q

Methylphenidate (Ritalin)

MAO

A

NET, DAT inhibitor;
Indirect Agonism;
Stimulant

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20
Q

COMT

A

Catecol-o-methyltranferase

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21
Q

MAO-A inhibitors consideration,

On-target ADR

A

MAO-A found in gut, dietary restriction may be necessary

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22
Q

Mechanisms to increase presynaptic release of NE and DA

A
  1. Alter VMAT function (direction)
  2. Displace NE from vessicles
  3. Reverse ditrection of NET/DAT
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23
Q

Pseudoephedrine MOA

A

Indirect Agonist + Direct Agonist

a) Displaces vesicles, increases NE/DA presynaptic release in CNS and PNS
b) Direct agonism on both A and B adrenergic receptors

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24
Q

Ephedrine t1/2 compared to NE

A

10X longer, not a substrate for MAO or COMT

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25
``` Ephedrine Actions A1 B1 B2 B2/3 ```
A1 - Vasoconstriction, increased TPR, decreased pulmonary secretions +B1 - Increased FOC +B2 - Bronchiole SM relaxation +B2/3 - Thermogenesis
26
Phentermine (Fastin; Qsymia phentermine/topiramate) | MOA
Increase presynaptic release of NE and DA
27
Phenteramine ADR
Increased BP, Tachycardia, heart palpitations, HA, insomnia. Any surprises here?
28
Amphetamine (Dexedrine, Adderol) | MOA
Increases presynaptic release of NE and DA by Reversing direction of DAT -Also weak inhibitor of MAO
29
Amphetamine therapeutic use
ADHD, Narcolepsy, short term appetite suppression
30
Methamphetamine (Desoxyn) MOA Meth significance FDA approved indication
MOA similar to amphetamine, - Methyl group extends half life - Narcolepsy
31
Modafinil (Provigil) | MOA
Similar to amphetamines, more selective for DA (+) Neurons in Wakefullness areas of hypothalamus
32
Modafinil approved uses
- Shift-work disorder | - Off label: excessive fatigue, anti depressant, adhd, bipolar, militarty
33
Modafinil ADRs
Rash
34
Modafinil selling point over methamphetamine
Equivalent wakefulness, no hyperactivity
35
Phenylephrine | MOA
Selective Alpha-1 Agonist
36
Phenylephrine Use and PK
Not as potent as NE Longer t1/2 Nasal decongestant
37
Phenylephrine 10% opthalmic solution
Mydriatic
38
Extended use of phenylephrine
rhinitis medicomentosa, "afrin addiction"
39
Other Alpha-1 agonist uses
- Orthostatic Hypotention - Surgical bleeding control - Allergic reaction: decrease secretion of mediators (histamine) - STRESS INCONTINENCE
40
Clonidine (Catapres) | MOA
Selective Alpha-2 agonist | Reduces sympathetic outflow @CNS (Locus Ceruleus) and locally
41
Clonidine most common use
HTN secondary to increased SNS outflow
42
Alpha-2 agonist common use
HTN secondary to increased SNS outflow | Indirect skeletal muscle relaxant (CNS level)
43
Alpha - 2 (Clonidine) agonist ADRs
- Anticholinergic - like - sedation, - hypotension
44
Selective Alpha -1 ANTagonist Drugs
Doxazosin (Cardura) Terazosin Tamsulosin (Flomax)
45
Doxazosin Selectivity
1000x higher for Alpha - 1 verses Alpha - 2 | Non-selective among blocking A1a, A1b, A1c
46
Alpha blockers and HTN
Decrease TPR by blockade of A1b and A1c on VSM
47
Tamsulosin (Flowmax)
Selective for A1a receptors | -Located in the trigone muscle --> relaxation of internal urinary sphincter
48
Rx for Pt with HTN and BPH
Use non-selective Alpha blocker such as Doxazosin or Terazosin
49
Rx for pt w/ Orthostatic Hypotension and BPH
Use Tamsulosin (Flowmax) to avoid dangerously low hypotension
50
What happened with 5alpha reductase inhibitors and BPH
Turned off effects of testosterone, caused ED. ED still an issue after therapy d/c
51
Alpha1 blocker ADRs
- Orthostatic hypotension - Nocturia - Runny nose
52
A1a and eye surgery
Intra-operative floppy iris syndrome | Tamsulosin only -->A1a
53
Selective Alpha -2 antagonists | Eg, Yohimbine
Increase sympathetic outflow through a central mechanism
54
Selective Beta -2 Agonists Use Overuse
SYMPTOMATIC treatment of asthma and COPD Over use - status asthmaticus -->pharmacodynamic tolerance by down regulation of Beta2
55
Eg, Beta2 Agonists:
Albuterol (Proventil, Ventolin)
56
Metaproterenol (Alupent) Concerns
Has some Beta1 affinity --> Cardio ADRs --> Avoid in pt at risk for MI
57
Why not use Long Acting Beta Agonists alone?
Only treats symptoms. Doesn't address underlying cause of inflammation
58
LABA use
12 h half life, Good for pt w/ problems at night or when exercising NOT for acute attacks
59
Mirabegron (Myrbetriq) | MOA
Selective Beta-3 Agonist
60
Mirabegron effect
Relaxes Detrusor muscle;
61
Mirabegron Metabolism
CYP3A4 and CYP2D6
62
Mirabegron ADRs
Increased HR and BP
63
Mirabegron is 2-3x more expensive than Muscarinic antagonists. Why use Mirabegron?
Preferred for use in pt with comorbid dementia or on cusp of dementia Muscarinic antagonist inhibit congative function
64
Pt with stage fright. How to choose a Beta blocker
Choose one that does not cross the BBB.
65
Beta antagonist therapeutic uses
- Hypertension - Angina - Cardiac Arrhythmias - Ischemic Heart diseases - Hyperthyroidism - Prophylaxis for migraine - Acute panic attack
66
Beta antagonist Cardio Actions
Reduced HG, FOC, BP | Slowed Conduction at AV
67
Beta Antagonist ADRs
- Bradycardia - Increased bronchoconstriction - Cold extremities - Hypoglycemia - Weight Gain - Fatigue, insomnia, depression, nightmares, fever
68
Beta Blocker Rebound Hypersensitivity
- HTN - Angina - MI - Fatal Arrhythmias
69
ISA beta blockers and rebound hypersensitivity
Less common. Partial agonist does not cause upregulation in receptor density
70
Carvediol (Coreg)
A competative antagonist of alpha1 and beta2 receptors ISA and partial agonist to Beta1 - Vasodiation - Contraindicated in asthmatitics
71
Selective Beta1 ANTagonist | Eg
Metoprolol (Lopressor)
72
Metoprolol Fun Facts
No ISA Extensive first pass metabolism BEST CHOICE FOR ASTHMATICS But watch out for rebound hypersensitivity
73
Onobotulinum Toxin Type A (Botox)
Cleaves SNAP-25 | Indirect nicotinic and muscarinic receptor antagonist
74
Rimabotulinum Toxin Type B (Myobloc)
Cleaves VAMP/Synaptobrevin (vesicular associated protein) Indirectly cause relaxation of skeletal and smooth muscle Treatments repeated every 2-3 months
75
Muscarinic Agonists: | Common uses
+Non-obstructive gastrointestinal disorders with immobility +Non-obstructive urinary bladder disorders with immobility +Xerostomia +Miosis: iris constriction
76
Atropine and Mycetism
In Mushroom poinsoning use Non-selective, competitive mAChr antagonist (Atropine)
77
mACh Agonist contraindications
``` +PUD +Asthma +Recovering from MI +BPH +PD ```
78
mACh ANTagonists: | Common Uses
GI antispasmotic - relaxes GI and decreases secretions +IBS +PUD +Overactive Bladder/Nocturnal enuresis +Sinus Bradycardia (IV atropine following MI +Opthamoology - Mydriasis
79
Additional mAChR Antagonist uses
+Adjunctive therapy in PD +Asthma: Decreased secretions and slight bronchodilation. Ajunct to Beta2 agonists +Surgery: decrease secretions
80
Bethanachol (Urecholine) | MOA
M3 mACh agonist with poor GI absorption --> Slows GI motility and Decreased secretions
81
Bethanachol uses:
GI/Bladder emptying disorder in Spinal chord injury patients *Doesn't cross BBB FYI
82
Propranolol MOA
Non-selective beta-blocker Competitive Antagonist (No ISA)
83
Propranolol use
Anti-hypertensive, anti-arrythmic

Neorologia (12 decks)

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