Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

581 - Pharmacology I > Exam 6 - Adrenergic Agonists & Antagonists > Flashcards

Exam 6 - Adrenergic Agonists & Antagonists Flashcards

1
Q

Characteristics of adrenergic agonists

A
  • Derivatives of B-phenylethylamine

- stimulate fight/flight

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Catecholamines

A
  • 2 OH groups on ring
  • potent at B receptors
  • rapid inactivation by MAO/COMT
  • cannot give orally (too much COMT/MAO in gut)
  • do not enter CNS…too polar
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Noncatecholamines

A
  • only 1 or no OH groups
  • longer duration of action
    • only MAO breaks it down…not very well
  • greater access to CNS….less polar
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Substitutions on amine Nitrogen

A
  • more subs….more affinity for B receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Epinephrine

A
  • Adrenalin
  • endogenous neurotransmitter/hormone
  • released by adrenal medulla (80%….NE 20%)
  • BOTH alpha and beta
  • Increases HR/contractility/renin/CO
  • constricts skin/viscera vessels
  • dilates liver/skeletal muscle vessels
  • high dose = constrict (alpha)…low dose = dilate (B2)
  • HR up / systolic up…diastolic down / PVR down
  • bronchodilation / allergy inhibition
  • hyperglycemia (increase glucagon / decrease insulin..alpha)
  • Lipolysis (B3)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Epinephrine therapeutic uses

A
  • Cardiac arrest
  • Anaphylactic shock
  • Acute asthma attack / bronchospasm
  • With local anesthetics….to keep local
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Epi CPR dose

A

1 mg IV/IO every 3-5 min

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Epi bradycardia dose

A

2-10 ug/min IV to effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Epinephrine pharmacokinetics

A
  • Rapid onset, short duration
    • due to MAO/COMT….is a catecholamine
  • IM/IV/IO/SQ/inhalation/endotracheal….NOT orally
  • excreted by kidney
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Norepinephrine

A
  • Levophed (leave em dead)
  • endogenous neurotransmitter of adrenergic nerves
  • Alpha and B1
  • Intense vasoconstriction
  • Increase contractility BUT barrorecpetor reflex….so HR down
  • HR down / systolic up…diastolic up / PVR up
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

NE therapeutic uses

A
  • Vasodilatory shock

- Hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

NE dose

A

0.5-12 ug/min to titrated to effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

NE pharmacokinetics

A
  • lasts 1-2 minutes
  • rapidly metabolized by MAO/COMT
  • excreted via kidney
  • IV ONLY…extravasation cause necrosis…no peripheral veins
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Dopamine

A
  • endogenous precursor to NE…neurotransmitter and hormone
  • CNS/adrenal medulla
  • D (low= 1-2 ug/kg/min) > B (medium= 2-10) > alpha (high= >10)
  • HR up / contractility up
  • contracts at HIGH doses
  • dilates renal/splanchnic arteries
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Dopamine therapeutic uses

A
  • MAIN drug for cardiogenic/septic shock
  • Renal failure…increases renal flow
  • Hypotension/heart failure…especially if with renal failure
    • NE will decrease renal flow even more
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Dobutamine

A
  • Dobutrex
  • synthetic, direct catecholamine
  • B1
  • Increases CO/HR ( < dopamine)/Contractility ( >dopamine)
  • NO PVR effect
  • Less increase in O2 consumption
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Dobutamine therapeutic uses

A
  • Increase CO in acute heart failure

- short term “failure to wean” drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Isoproterenol

A
  • Isuprel
  • synthetic catecholamine
  • Nonselective B1 and B2
  • Increase contractility/HR
  • potent vaso/bronchodilator
  • Up HR / zero-little up systolic…down diastolic / down PVR
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Isoproterenol therapeutic uses

A
  • Second choice for cardiac emergency
  • bronchospasms during anesthesia
  • cardiac stimulant
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Phenylephrine

A
  • Neo-Synephrine
  • synthetic Alpha 1
  • lasts 20 min (longer than epi/NE)
  • constriction
  • Up systolic….up diastolic
  • Drops HR….due to reflex bradycardia…like NE
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Phenylephrine theraputic uses

A
  • Hypotension
  • Tachycardia
  • Nasal decongestant if topical/oral
  • VERY common to increase SVR and MAP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Neo dosing

A
  • Start with test dose (50-100 ug/ml)
  • LD = 50-500 ug
  • IV = 10-15 in 250 ml fluid (40-60 ug/ml)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Indirect adrenergic agonists

A
  • increase endogenous levels of Epi/NE
    • cause release / inhibit reuptake / inhibit degradation
  • Amphetamine / Tyramine / Cocaine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Amphetamine

A
  • reverse NE reuptake channels on presynaptic terminal

- more release of NE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Cocaine
- binds and blocks reuptake NE receptors
26
Mixed action adrenergic agonists
Ephedrine (if no epi) > Pseudoephedrine (decongestant) - release stored NE...AND - directly stimulate alpha/beta - Like epi...less potent....longer duration - vasoconstriction / cardiac stimulation / Up systolic AND diastolic - Mild CNS
27
Side effects of adrenergic agonists
- arrhythmia - headache - hyperactivity - insomnia - nausea - tremors
28
Dopaminergic agonists
- Levodopa - goes into CNS...turns into dopamine...stays in CNS - useful for Parkinson's
29
Direct Adrenergic Agonist Drugs
- Epinephrine (Adrenalin) - NE (Levophed) - Dopamine - Dobutamine (Dobutrex) - Isoproterenol (Isuprel) - Phenylephrine (Neo-Synephrine)
30
Indirect Adrenergic Agonist Drugs
- Amphetamine - Tyramine - Cocaine
31
Mixed Action Adrenergic Drugs
- Ephedrine | - Pseudoephedrine
32
Dopaminergic Agonist Drugs
- Levodopa
33
Adrenergic Antagonists
- no need to use on B2 - sympatholytics - alpha and beta blockers
34
Alpha blockers
- vasodilates - severely drops BP - causes reflex tachycardia
35
Alpha 1 receptors
- increase vascular tone - smooth muscle vasculature - on effector organ - constricts when stimulated
36
Alpha 2 receptors
- presynaptic - control release of NE - inhibitory autoreceptors - stimulation blocks NE release
37
Phenoxybenzamine
- Dibenzyline - Nonselective alpha blocker - Noncompetitive....covalently bonds - irreversible...long lasting - vasodilates / reflex tachycardia - blocks inhibitory alpha2 receptors on heart...more NE...up CO Uses: - Pheochromocytoma: too much adrenaline from adrenal gland - DONT use for hypertension...it increases CO
38
Phentolamine
- Regitine - Nonselective alpha blocker - competitive - short lasting...4 hours Uses: - short term pheochromocytoma - locally to prevent dermal necrosis...NE extravasation - Epi reversal... blocks alpha effects of Epi
39
Nonspecific alpha blocker side effects
- orthostatic hypotension - tachycardia - dizzy/headache - sexual dysfunction
40
Selective Alpha 1 blockers
- Prazosin (minipress) - Terazosin (Hytrin) - Doxazosin (Cardura) - used for hypertension w/ other things...also BPH - competitive - decrease PVR and lower BP - minimal changes to CO (no B) - first dose may cause orthostatic hypotension
41
Selective alpha 2 blockers
- Yohimbine - competitive - more sympathetic to periphery - treats impotence/aphrodisiac
42
Beta blockers
- think -olol - competitive - widely used - patient specific dosing (usually judge via HR)
43
Beta blocker uses
- hypertension - angina - arrhythmias - MI - heart failure - hyperthyroidism - glaucoma - migraine prophylaxis
44
Propranolol
- Inderal - Gold standard - blocks B1 and B2 equally - down HR / contractility / CO / oxygen consumption - PVR up initially...but normal or decrease with long term use - due to reflex peripheral constriction
45
Propranolol bronchial effects
- constriction | - DON'T use for COPD
46
Propranolol glucose effects
- Hypoglycemia - decrease glucagon secretion - careful with diabetic patients
47
Propranolol drug interactions
- blocks isoproterenol (B agonist) - no cardiac stimulation (B1) - no drop in MAP and diastolic BP (B2) - blocks SOME Epi - leaves alpha 1 alone.... vasoconstriction action unimpaired
48
Propranolol therapeutic uses
- hypertension (drops work of heart and PVR over time) - angina (less O2 used) - MI (better recovery and preventative for future MI) - migraine (prophylactically) - hyperthyroidism - stage fright / anxiety
49
Propranolol adverse effects
- bronchoconstriction - arrhythmias (receptor upregulation / DO NOT stop abrupt) - sexual dysfunction - metabolic disturbance (high LDL / low HDL / more fat...B3) - CNS effects: - depression / dizzy / weak / tired / hallucination / STML
50
Nadolol
- Corgard - blocks B1 and B2 equal - nonselective - similar to propranolol but MORE potent - longer duration....12-24 hours Uses: -Hypertension
51
Selective B1 blockers
- can effect B2 with high dose...still careful w/ COPD - less bronchoconstriction at low dose Uses: - lower BP in hypertension...especially w/ impaired pulmonary - increase exercise in angina - chronic angina therapy - chronic heart failure - Bisoprolol / Metoprolol (extd. release)
52
Esmolol
- Brevibloc - B1 blocker - very short half life - IV - used for BP or rhythm in surgery
53
Selective B1 blocker w/ partial agonist activity
- Acebutolol (Sectral) - ISA - Intrinsic sympathomimetic activity - weakly activates AND blocks from other potent binding - leads to decrease in cell activity...not total block - less effect on CO/HR but minimal lipid/carb disturbance Uses: - hypertension w/ bradycardia ...drop in HR is less
54
Nonselective B block w/ alpha-1 blocking actions
- Labetalol (Trandate) - Carvedilol (Coreg) - peripheral dilation (block alpha 1) - reduce BP Uses: - Hypertensive emergency (IV) - Pregnancy hypertension
55
Non Selective alpha blockers
"-amine" - Phenooxybenzamine (Dibenzyline) - Phentolamine (Regitine)
56
Selective alpha 1 blockers
"-azosin" - Prazosin (Minipress) - Terazosin (Hytrin) - Doxazosin (Cardura)
57
Selective alpha 2 blocker
- Yohimbine
58
Non Selective B blockers
- Propranolol (Inderal) | - Nadolol (Corgard)
59
Selective B1 Blockers
- Esmolol (Brevibloc) - Atenolol (Tenormin) - Metoprolol (Lopressor) - Bisoprolol (Zebeta)
60
Selective B1 blockers w/ partial agonist activity
- Acebutolol (Sectral)
61
Non Selective B Blockers w/ Alpha-1 block activity
- Labetalol (Trandate) | - Carvedilol (Coreg)

581 - Pharmacology I (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions