L7 Flashcards
What drugs are considered non-catecholamines? What should you know about dosing?
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
What are the 3 indirect acting NE releasers?
Tyramine
Amphetamine
Ephedrine
Use of tyramine
LAB
Prototype so not used clinically
- Interaction w/ MAO inhibitors
Why use ephedrine to ↑NE
Decongestant
Vasopressor - NE @ alpha = vasoconstrict
Stress incontinence - NE @ A1 constricts sphincter
Uses of amphetamines
Narcolepsy
Attention deficit disorders
Mechanism of indirect acting NE releasers
Nonvesicular NE release
- Drug gets into pre-synaptic neuron to release NE from vesicles into cytoplasm
- Reverses NET to pump NE out w/o vesciular release
Why are drug interactions between MAO inhibitors and indirect NE releasers important? What drug choice do you pick to ↓interaction risks?
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
What are the acute SE of cocaine use?
A receptors - Coronary spasm --> ↓O2 delivery A or B - ↑BP - ↑HR - Together ↑O2 demand Net = ischemia, infarction, arrhythmia
What are the 5 chronic effects of cocaine?
- Dilated cardiomyopathy
- Atherosclerosis
- Necrosis
- Persistent hyperthermia –> myoglobin release –> kidney damage
- Neutropenia since cocaine cut with MAO/COMT inhibitors
What are 2 unique feature to cocaine that aren’t release to NE actions?
- ↓Na transport
2. Local anesthetic effect
What is the 5-HT 2B receptors?
Subtype of serotonin receptor
What are 5-HT 2B agonists
MDMA
Ergot derivatives
Dopamine agonists
How does MDMA (5 HT 2B agonists) create heart damage?
Prolif of valve cells –> thickeing –> regurgatation & disease
A1 agonist - name and 3 uses
Phenylephrine
- Decongestant
- ↑BP
- Mydriasis
A2 agonist - name and use
Clonidine
A2 autoreceptor - inhibits NR release (↑sympa response)
What other action of A2 agonists will you see at high [ ]s?
A2 receptor agonism is relative to [ ]
↑[ ] actually see A1 receptor contraction of smooth muscle
Why don’t we use isoproterenol to treat asthma anymore?
So short acting Heart SE (B1) as since B1/2 non-selective
What is the major similarity and difference between albuterol and salmeterol and formoterol?
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
B2 actions if inhaled in airway
Bronchodilation ↓Mast cell degen ↓Plasma exudate ↓Cholinergic neurotransmission ↑muco-ciliary clearance ↓neutrophil fxn ↓Bacterial adhere
What are long action B agonists for asthma prescribed with?
Corticosteroids - just how laid out
Use of ritodrine
B2 agonist
Delay early labor via uterine smooth muscle receptors - relax
Adverse effects of systemic B2
Tachycardia
Termor
Hyperglycemia
Hypokalemia
Which drug can give you skeletal muscle hypertrophy? 2 scenarios.
Clenbuterol
Farm animals = illegal
Body builders
Do you use long acting beta 2 agonists for asthma? Why or why not?
NO
Fewer asthma attacks, but more severe and dangerous when they do happen
