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Term III: Pharmacology > Adrenergic Agonists > Flashcards

Adrenergic Agonists Flashcards

1
Q

List order of synthesis to get norepi, epi, dopamine, and isoproterenol starting with the initial compound they are all formed from.

A

L-Tyrosine –> L-Dopa –> Dopamine –> Norepinephrine –> Epinephrine –> Isoproterenol

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2
Q

Where are B3 receptors found?

A

Adipose (lipolysis), skeletal muscle (thermogenesis), gallbladder, urinary bladder (relax), CNS

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3
Q

Order the following in terms of smallest group on amine to largest. Isoproterenol, norepinephrine, epinephrine

A

Norepinephrine, epinephrine, isoproterenol

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4
Q

What receptors do blood vessels to skeletal muscle have?

A

a1 and B2

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5
Q

Why do local anesthetics contain epinephrine?

A

To achieve local vasoconstriction (via a1) to keep the anesthetic locally for a longer duration

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6
Q

What is the dominant receptor on veins?

A

a1 - constriction (storing blood)

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7
Q

How much epinephrine is released per day in a normal body?

A

20-100 ug

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8
Q

What is the effect of epinephrine on immune system?
A. Up- regulate
B. Down- regulate

A

B

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9
Q

Does dopamine increase contractility (stroke volume) or heart rate more? What does this minimize?

A

Contractility (stroke volume)

This minimizes oxygen demand/consumption

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10
Q

Does dopamine cross the blood-brain barrier?

A

No

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11
Q

What drug can you give to people with Parkinson’s disease?

A

L-DOPA - gets converted to dopamine in nerve terminals

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12
Q

What is the rate-limiting step in synthesis of dopamine, norepi, and epi?

A

Tyrosine hydroxylase (conversion of L-tyrosine –> L-dopa)

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13
Q

Phenylephrine (Neo-synephrine/Sudafed)

A

a1 agonist

Vasoconstrictor

  • during surgery to raise BP
  • nasal decongestants
  • priapism
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14
Q

Clonidine (Catapres)

A

a2 agonist - inhibits further release of NE

Emergency anti-hypertensive, used frequently in ERs

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15
Q

Alpha-methyldopa (Aldomet)

A

a2 agonist - inhibits further release of NE

Choice anti-hypertensive in pregnant women

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16
Q

What are 2 side effects of Sudafed/Phenylephrine?

A

high BP, urinary retention

17
Q

Dobutamine (Dobutrex)

A

B1 agonist - increases CO

Used in cardiogenic and septic shock to increase CO; also used for cardiac stress test and acute CHF

18
Q

Albuterol (***terol)

A

B2 agonist

Asthma, COPD (relieve bronchospasm) - bronchodilator

19
Q

Salmeterol, Formoterol. Metaproterenol

A

LABAs - Long-acting B2 agonists

Bronchodilator
Asthma, COPD

20
Q

Ritodrine (Yutopar)

A

B2 agonist

Relaxes smooth muscle of uterus by reducing uterine contractions - prevents premature deliveries

21
Q

What is the drug of choice to treat anaphylactic shock? Name target receptors and how they help.

A

Epinephrine (epi pen!)

a1 - constricts blood vessels
B1 - CO increases
B2 - bronchodilates & inhibits degranulation of mast cells

22
Q

What are 5 adverse effects of adrenergic agonists?

A

Increased blood pressure, tachycardia & cardiac arrhythmias, nervousness/anxiety, hyperglycemia, exaggerated effects with cocaine

23
Q

What is rebound HTN?

A

High BP when a drug is stopped abruptly

24
Q

What is a potential adverse side effect of a2 agonists?

A

Rebound HTN

25
Q

What do Beta 3 agonists do? Where are the receptors located?

A

Promote breakdown of triglycerides - lose weight!

Mostly in adipose tissue and skeletal muscle

26
Q

Ephedrine

A

Structural analogs that increase NE levels

Nasal decongestant, used during surgeries to raise BP

27
Q

What part of the brain do ADD drugs target?

A

RAS - reticular activating system in midbrain

28
Q

Tyramine

A

Precursor to NE - rich in wines and cheeses

Indirect acting agonist - structural analog that increases NE levels and mimics its actions

Contraindicated with MAO inhibitors

29
Q

What are the neurotransmitter issues in the following conditions?

  1. Alzheimer’s
  2. Depression
  3. Parkinson’s
  4. Schizophrenia
  5. ADD
A
  1. Alzheimer’s - too little ACh
  2. Depression - too little serotonin, NE
  3. Parkinson’s - too little dopamine
  4. Schizophrenia - too much dopamine
  5. ADD - too little NE and DA in RAS
30
Q

What is the treatment for the following conditions:

  1. Alzheimer’s
  2. Depression
  3. Parkinson’s
  4. Schizophrenia
  5. ADD
A
  1. Increase ACh with esterase inhibitors
  2. SSRIs, TCAs
  3. L-dopa
  4. Dopamine (D2) blockers
  5. Ritalin, Adderall
31
Q

Isoproterenol (Isuprel)

A

Beta-1 = Beta-2 = Beta-3 agonist

Causes vasodilation (why there is marked decreased diastolic pressure), but also increases cardiac force and rate (increase in systolic pressure)

Reference drug

32
Q

Dopamine (Intropin)

A

D1, D2 > Beta-1 > alpha-1 agonist

(D1, Gs, high cAMP, EPSP) and
(D2, Gi, low cAMP, IPSP)

Low dose (0.5-2.0 ug/min) - D1 - vasodilation in renal, mesenteric, coronary, and cerebral vasculature, promotes Na+ and H2O excretion

Med dose (5-10 ug/min) - D1 & B1 - increase CO

High dose (10-50 ug/min) - a1 - vasoconstriction

TREATS: Cardiogenic & hypovolemic shock, CHF

33
Q

Epinephrine (Adrenaline)

A

alpha-1, alpha-2, beta-1, beta-2, beta-3 agonist

Higher concentration - a1 - vasoconstriction

Lower concentration- B2 - vasodilation

Increases heart rate and contractility (so systolic pressure increases), but dilates blood vessels (so diastolic decreases)

34
Q

Norepinephrine (Levofed)

A

alpha-1, alpha-2, beta-1 agonist

Reflex bradycardia - constricts all blood vessels, increasing peripheral resistance, so reflex is to reduce heart rate to try and reduce this pressure

35
Q

Methylphenidate (Ritalin)

A

1 drug ADHD

Indirect acting agonist - structural analog that increases NE & dopamine levels and mimic their actions

36
Q

D-Amphetamine (Adderall)

A

2 drug aDHD

Indirect acting agonist - structural analog that increases NE & dopamine levels and mimic their actions

Term III: Pharmacology (19 decks)

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