L7

Question 1

What drugs are considered non-catecholamines? What should you know about dosing?

Answer 1

A & B agonists, indirect acting NE releasers
High doses needed b/c ↓potency
PO b/c can cross barriers (BBB)
Resistant to COMT & MAO - ↑duration of action

Question 2

What are the 3 indirect acting NE releasers?

Answer 2

Tyramine
Amphetamine
Ephedrine

Question 3

Use of tyramine

Answer 3

LAB
Prototype so not used clinically
- Interaction w/ MAO inhibitors

Question 4

Why use ephedrine to ↑NE

Answer 4

Decongestant
Vasopressor - NE @ alpha = vasoconstrict
Stress incontinence - NE @ A1 constricts sphincter

Question 5

Uses of amphetamines

Answer 5

Narcolepsy

Attention deficit disorders

Question 6

Mechanism of indirect acting NE releasers

Answer 6

Nonvesicular NE release

1. Drug gets into pre-synaptic neuron to release NE from vesicles into cytoplasm
2. Reverses NET to pump NE out w/o vesciular release

Question 7

Why are drug interactions between MAO inhibitors and indirect NE releasers important? What drug choice do you pick to ↓interaction risks?

Answer 7

B/c XMAO to ↓cytosolic NE at baseline, enlarged cytosolic pool of NE
NE releasers = MASSIVE NE release - moves into circulation –> hypertensive crisis
Happens with all NE-releasers especially tyramine
Use MAO-B inhibitors to ↓risk

Question 8

What are the acute SE of cocaine use?

Answer 8

A receptors 
- Coronary spasm --> ↓O2 delivery
A or B
- ↑BP
- ↑HR
- Together ↑O2 demand 
Net = ischemia, infarction, arrhythmia

Question 9

What are the 5 chronic effects of cocaine?

Answer 9

1. Dilated cardiomyopathy
2. Atherosclerosis
3. Necrosis
4. Persistent hyperthermia –> myoglobin release –> kidney damage
5. Neutropenia since cocaine cut with MAO/COMT inhibitors

Question 10

What are 2 unique feature to cocaine that aren’t release to NE actions?

Answer 10

1. ↓Na transport

2. Local anesthetic effect

Question 11

What is the 5-HT 2B receptors?

Answer 11

Subtype of serotonin receptor

Question 12

What are 5-HT 2B agonists

Answer 12

MDMA
Ergot derivatives
Dopamine agonists

Question 13

How does MDMA (5 HT 2B agonists) create heart damage?

Answer 13

Prolif of valve cells –> thickeing –> regurgatation & disease

Question 14

A1 agonist - name and 3 uses

Answer 14

Phenylephrine

1. Decongestant
2. ↑BP
3. Mydriasis

Question 15

A2 agonist - name and use

Answer 15

Clonidine

A2 autoreceptor - inhibits NR release (↑sympa response)

Question 16

What other action of A2 agonists will you see at high [ ]s?

Answer 16

A2 receptor agonism is relative to [ ]

↑[ ] actually see A1 receptor contraction of smooth muscle

Question 17

Why don’t we use isoproterenol to treat asthma anymore?

Answer 17

So short acting 
Heart SE (B1) as since B1/2 non-selective

Question 18

What is the major similarity and difference between albuterol and salmeterol and formoterol?

Answer 18

Both prefer B2 to dilate for bronchodilation w/o B1 SEs
Albuterol = short acting, symptomatic relief asthma
Salmeterol = long acting, prophylactic dosing
Fomoterol = fast, long acting

Question 19

B2 actions if inhaled in airway

Answer 19

Bronchodilation
↓Mast cell degen 
↓Plasma exudate 
↓Cholinergic neurotransmission
↑muco-ciliary clearance
↓neutrophil fxn
↓Bacterial adhere

Question 20

What are long action B agonists for asthma prescribed with?

Answer 20

Corticosteroids - just how laid out

Question 21

Use of ritodrine

Answer 21

B2 agonist

Delay early labor via uterine smooth muscle receptors - relax

Question 22

Adverse effects of systemic B2

Answer 22

Tachycardia
Termor
Hyperglycemia
Hypokalemia

Question 23

Which drug can give you skeletal muscle hypertrophy? 2 scenarios.

Answer 23

Clenbuterol
Farm animals = illegal
Body builders

Question 24

Do you use long acting beta 2 agonists for asthma? Why or why not?

Answer 24

NO

Fewer asthma attacks, but more severe and dangerous when they do happen

Question 25

Use of B3 agonists?

Answer 25

Overactive urinary bladder syndrome