Adrenergic Agonists And Antagonists 1&2

Front 1

How are the adrenergic receptors classified?

Back 1

By their potencies of agonists

Front 2

Alpha receptor potency order?

Back 2

epi > norepi > Phen >> isoproterenol

Front 3

Beta receptor potency order?

Back 3

ISO > EPI ≥ NE > PE

Front 4

alpha 1 prototype agonist? alpha 1 mechanism?

Back 4

phenylephrine

increased PLC => increased DAG + IP3 => increased Ca+2 + PKC

Front 5

alpha 1 effects on organs?

Back 5

-vascular and genitourinary contraction

-increased arterial resistance

-decreased venous capacitance

-intestinal smooth muscle relaxation

-radial muscle contraction = mydriasis

-glycogenolysis + gluconeogenesis

Front 6

alpha 2 prototype agonist? alpha 2 mechanism?

Back 6

clonidine

inhibitory = decreases cAMP

Front 7

alpha 2 effects on organs?

Back 7

-decreases insulin secretion

-decreases NE release

-decreases sympathetic tone in the CNS

-causes platelet aggregation

Front 8

beta 1 prototype agonist? beta 1 mechanism?

Back 8

Dobutamine

g-protein > adenylate cyclase > increases cAMP

Front 9

Beta 1 effects on organs?

Back 9

inotropic

chronotropic

increased AV conduction

increased renin release

Front 10

beta 2 prototype agonist? beta 2 mechanism?

Back 10

albuterol

g-protein > adenylate cyclase > increases cAMP

Front 11

D1 prototype agonist? D1 mechanism? effects on organs?

Back 11

Dopamine

increases cAMP

dilates renal vasculature

Front 12

Effect of epi on:

TPR =

SBP =

DBP =

Average BP =

HR =

Back 12

TPR = decreased = B2 > a1

SBP = increased = beta1

DBP = decreased = B2>a1

Average BP = no change

HR = increased = B1

Front 13

Effect of norepi on:

TPR =

SBP =

DBP =

Average BP =

HR =

Back 13

TPR = increased = a1

SBP = increased = a1 + B1

DBP = increased = a1

Average BP = increased

HR = decreased = vagal reflex

Front 14

Effect of isoproterenol on:

TPR =

SBP =

DBP =

Average BP =

HR =

Back 14

TPR = decreased = B2

SBP = increased = B1

DBP = decreased = B2

Average BP = decreased

HR = increased = B1

Front 15

Indirect Agonist (Transmitter Releaser/False Transmitter)? Short term effects? Long term effects?

Back 15

Tyramine:

short term: in the presense of MAO inhibitors it will preciptate NE release and HTN

long term: it's metoblite octopamine replaces NE and can impair sympathetic funtion in the presence of MAOI's

Front 16

What are the 3 Indirect Agonist/Central Stimulants (Transporter Inhibitor/Releaser)?

Back 16

Cocaine, d-amphetamine, methylphenidate

Front 17

Mechanism of cocaine

Back 17

snorting (jk):

centrally active inhibitor of NE, Dopamine (and sert) reuptake

Front 18

Mechanism and uses of d-amphetamine

Back 18

aka dextroamphetamine:

-release NE and Dopamine

-acts directly on alpha and beta receptors

used for ADHD

Front 19

Mechanism and uses of methylphenidate

Back 19

-release NE and Dopamine

-acts directly on alpha and beta receptors

used for ADHD

Front 20

Therapeutic uses of adrenergic agonists

Cardiovascular? (4)

Back 20

1. Nasal decongestants (α1) Phenylephrine, pseudoephedrine

2. Slowing absorption of local anesthetics (α1; epinephrine)

3. Resuscitation after cardiac arrest (probably mainly α1; epinephrine)

4. Restoring blood pressure:
-Overdose of hypotensive agents (α1)
-Spinal damage or anesthesia (α1)
-Cardiogenic shock (β1; dopamine, dobutamine)

Front 21

Therapeutic uses of adrenergic agonists

Opthamology? (2)

Back 21

1. Mydriasis (α1) Epinephrine, phenylephrine

2. glaucoma (α,1 α2) Epinephrine, phenylephrine

Front 22

Therapeutic uses of adrenergic agonists

Allergic? (2)

Back 22

1. asthma = B2

2. anaphylactic shock = B2 + a1 to counteract bronchoconstriction and low BP

Front 23

Therapeutic uses of adrenergic agonists

Other? (3)

Back 23

-Obstetrics: Delay premature labor (β2)
-Treatment of opioid withdrawal (α2)
-Treatment of Attention Deficit Disorder (amphetamine, methylphenidate)

Front 24

Toxicity & Side Effects of Adrenergic Agonists (9)

Back 24

1. Vasoconstriction, ischemia (α1)
2. Hypertensive reactions, can cause cerebral
hemmorhage (α1)
3. Rebound nasal congestion (α1)
4. Tachycardia (β1)
5. Myocardial ischemia (β1)
6. Cardiac ventricular arrhythmias (β1)
7. CNS stimulation
8. Withdrawal syndrome (α2 agonists)
9. Increased risk of asthma exacerbaton with extended use of long=acting βagonists(β2)

Front 25

prototype alpha antagonist

Back 25

phentolamine

Front 26

prototype alpha 1 antagonist

Back 26

prazosin

Front 27

prototype beta antagonist

Back 27

propanolol

Front 28

prototype beta 1 antagonist

Back 28

metoprolol

Front 29

prototype Beta + alpha 1 antagonist

Back 29

carvedilol

Front 30

Therapeutic Uses of α-Antagonists (6)

Back 30

1. Treatment of hypertension
2. Treatment of pheochromocytoma
(β-blockers may also be used, but only after blocking α1-receptors)
3. Treatment of Raynaud s Disease (reduce digital vasospasm)
4. Treatment of heart failure (reduce vascular resistance)
5. Treatment of benign prostatic hyperplasia (BPH) α1 antagonism relaxes smooth muscle of prostate and bladder
6. Antidote to α-agonist vasoconstriction

Front 31

Side Effects of α-Antagonists

Back 31

Postural hypotension

GI stimulation

Inhibition of ejaculation

Front 32

Cause of postural hypotension

Back 32

due to inhibition of α-mediated vasoconstriction:
– Reflex tachycardia
– Myocardial ischemia (increased O2 demand from reflex tachycardia)
– Salt & water retention (β1 stimulation of renal AngII system)
– Peripheral edema

Front 33

Therapeutic Uses of β-Blockers (9)

Back 33

1. cardiac arrhythmias
2. Reducing mortality after myocardial infarction
3. heart failure
4. HTN (reduce cardiac output, inhibit renin production)
5. Angina (to control O2 demand)
6. Hyperthyroidism (propranolol)
7. Reducing anxiety ( stage fright )
8. Migraine prophylaxis
9. Treatment of open-angle glaucoma

Front 34

Toxicity & Side Effects of β-Blockers (7)

Back 34

1. Bronchoconstriction
2. Bradycardia
3. Withdrawal: exacerbation of angina, risk of sudden death
4. Fatigue
5. Cold extremities
6. Potentiation of epinephrine vasoconstriction
7. Precipitation of congestive heart failure