Pharm 8: Adrenergic

Front 1

Alpha 2 agonists are anti-hypertensive agents. How do they work? Give two examples

Back 1

A2 agonists activate A2 receptors in the CNS and supress the outflow of the sympathetic nervous system. Examples 1. Clonidine 2. Methyldopa

Front 2

carvedilol class and receptors

Back 2

adrenergic antagonsit-receptor blocker, B1, B2, A1 (third generation)

Front 3

carvedilol use

Back 3

chronic heart failure, hypertension, acute MI

Front 4

labetalol class and receptors

Back 4

adrenergic antagonsit-receptor blocker, B1, B2, A1 (third generation)

Front 5

labetalol use

Back 5

3rd generation B1 B2, A1
hypertension, hypertensive emergencies

Front 6

Third generation B blockers such as ____ and ____ have additional CV effects compared to 1st and 2nd. Why do they have these effects

Back 6

labetalol, carvedilol, have A1 receptor blocking propertie which blocks constriction of peripheral vasculature, gives additional anti-hypertensive effects

Front 7

Give two examples of B1 selective adrenergic receptor antagonists (2nd generation)

Back 7

Metoprolol, Esmolol

Front 8

Esmolol class/ receptors

Back 8

B1 selective adrenergic antagonist

Front 9

Esmolol uses

Back 9

B1 selective antagonist, treats tachycardia, supraventricular tachy

Front 10

Metoprolol class/ receptors

Back 10

B1 selective antagonist, treats tachycardia, supraventricular tachy

Front 11

Metoprolol use

Back 11

B1 selective antagonist, treats hypertension, angina, tachycardia, acute MI, chronic heart failure

Front 12

timolol class/ receptors

Back 12

non selective B antagonsit

Front 13

timolol uses

Back 13

non selective B antagonist, treats hypertension, congestive heart failure, acute MI, migrane prophylaxis, wide angle glaucoma

Front 14

Timolol can be used to treat wide angle glaucoma without the effects of miotics. Why?

Back 14

Timolol is a non selective B-blocker. it treats glaucoma by blocking sympathetic stimulation leading to secretion of aqueous humor. Miotics such as epinephrine (A1, A2, B1, B2) and phenylephrine (A1) cause dilation (mydriasis) and impair accommodation which can lead to blurred vision and night blindness

Front 15

Give two examples of non-subtype selective Beta blockers

Back 15

propranolol, timolol

Front 16

propranolol class/ receptors

Back 16

non-subtype specific beta antagonist

Front 17

propranolol uses

Back 17

non-subtype specific beta antagonist, treats hypertension, angina, cardiac arrhythmias/ tachycardia, ventricular arrhythmias/tachy, PVCs, acute MI, pheochromocytoma, migrane prophylaxsis

Front 18

propranolol side effects

Back 18

CHF, heartblock/ bradycardia, bronchospasm, blunt recognition of hypoglycemia

For hypoglycemia look for sweating because it is the only cholinergic mediated sign of hypo, the adrenergic effects are blocked

Front 19

Bronchospasm is a side effect of propranolol. Why?

Back 19

non-selective B blocker
blockage of B2 receptors impaires ability of sympathetic system to stimulate bronchodilaiton

Front 20

Delayed recovery from insulin induced hypoglycemia is a side effect of propranolol. Why

Back 20

Propranolol is a non-subtype selective B blocker. Blockage of the B2 receptors on the liver and skeletal muscle prevent sympathetic stimulation of GNG and glycogeneolysis

Front 21

Give two examples of selective A1 blockers

Back 21

prazosin, tamsulosin

Front 22

Both prazosin and tamsulosin are effective treatments for BPH. By what mechanism? Why does tamsulosin have less propensity for side effects

Back 22

Prazosin and tamsulosin are selective A1 receptor blockers.Blocking the A1 receptors relaxes the A1 mediaed contraction of the prostate and bladder neck that ihibits urine flow with BPH. A major side effect of these drugs is orthostatic hypotension which occurs because of blocking of peripheral A1 receptors on the BV"s which prevents the constriction that is necessary to maintain BP when changing position. Tamsulosin has less propensitiy for OH because it is more selective for the A1A receptors  on the prostate than the A1B receptors on the BVs

Front 23

tamsulosin class/ receptor

Back 23

A1 selective antagonist

Front 24

tamsulosin use

Back 24

BPH w/ minimal orthostatic hypertension due to A1a selectivity for prostate

Front 25

Prazosin class/receptors

Back 25

A1 selective antagonist

Front 26

Prazosin uses

Back 26

A1 selective antagonist, treats hypertension, CHF (decreases preload and afterload) BPH

Front 27

salt and water retntion is a major side effect of prazosin. why

Back 27

A1 blocker
Blockaged of the A1 receptor  leads to a decrease in BP because constriction of the blood vessels is blocked, there is also a decrease in preload and afterlaod. The decrease in BP triggers renin release and an eventual increase in salt and water retention.

Front 28

orthostatic hypotension is a side effect of these 4 drugs. What do they have in common? it is also a side effect of a different class of drug. Which one

Back 28

Blockers of A1 receptors. Both A1/A2=phenoxybenzamine, phentolamine, A1 only= prazosin, tamsulosin, also an effect of  guanadrel, an adrenergic neuron blocker-blocks broad sympathetic effects

Front 29

Phenoxybenzamine class/ receptor

Back 29

A antagonist, irreversible

Front 30

Phentolamine class/ receptor

Back 30

A antagonist, reversible

Front 31

Phentolamine use

Back 31

A antagonist, use for hypertension, pheochromocytoma, shorten effect of lcoal+sympathomimetic

Front 32

Side effects of phenoxybenzamine and phentolamine

Back 32

tachycardia, salt/water retention, orthostatic hypotension

Front 33

Phenoxybenzamine and phentolamine are both A adrenergic antagonists. How do their mechanisms differ

Back 33

phenoxybenzamine-irreversible antagonist, long acting, phentolamine=competitive antagonist, shorter action

Front 34

tachycardia is a side effect of phenoxybezamine and phentolamine but is less signficant with prazosin. What causes the tachy? Why is there a difference

Back 34

Phenoxybenzamine, phentolamine, and prazosin are all alpha blockers. Phenoxybenzamine and phentolamine block A1 and A2, prazosin is a selective A1 blocker. Blockage of A2 receptors eliminates the NE negative feedback on the never terminal.  This leads to an increased secretion of NE which acts on the B1 receptors in the cardiac muscle leading to an increase in HR. prazosin does not lead to this effect because only the A1 receptors are blocked.

Front 35

reserpine class/ receptor,

Back 35

adrenergic neuron blocker

Front 36

reserpine mechanism

Back 36

adrenergic neuron blocker, inhibits VMAT2 which prevents the transport of dopamine into the vesicle for synthesis into NE. depletes the  nerve of NE.

Front 37

Reserpine use, side effects

Back 37

Hx used Tx hypertsion but major side effects, lipophilic= penetrates into CNS=suicidal tendencies

Front 38

guanadrel class/rece[tpr

Back 38

adrenergic antagonist, neuron blocker

Front 39

Guanadrel mechanism

Back 39

taken into adrenergic nerves by NET, replaces NE but has no agonist activity, acts as false transporter, blocks sympathetic effects

Front 40

Why do cocaine and tricyclic antidepressantsblock the action of Guanadrel

Back 40

guanadrel=adrenergic antagonist, neuron blocker
Cocaine and tricyclics block the action of NET which is required to bring guanadrel into the neuron

Front 41

guanadrel use

Back 41

adrenergic neuron blocker, Tx hypertension

Front 42

pseudoephedrine class/receptor

Back 42

mixed acting adrenergic agonist, A1

Front 43

pseudoephedrine use

Back 43

mixed adrenergic agonist A1,use as nasal decongestant

Front 44

ephedrine class/ receptor

Back 44

mixed adrenergic agonist, A, B

Front 45

define mixed adrenergic agonist and give 3 examples

Back 45

increases NE release and stimulates adrenergic receptors- amphetamine (A,B), ephedrine (A, B), Pseudoephedrine (A1)

Front 46

tyramine-class and mech

Back 46

indirect adrenergic agonist, releases NE from nerves, found in certain fermented foods, hypertensive crisis if pt is on MAOI

Front 47

albuterol class/ receptor

Back 47

B2 adrenergic agonist

Front 48

albuterol use

Back 48

B2 adrenergic agonist, short acting bronchodilator

Front 49

Salmeterol class/ receptor

Back 49

B2 adrenergic agonist

Front 50

Salmeterol use

Back 50

B2 adrenergic agonist, long acting brochodilator, COPD, nocturnal/ persistent asthma, not suitable as monotherapy for acute bronchospasm

Front 51

Clonidine use

Back 51

A2 selective adrenergic agonist, acts on A2 receptors in CNS to block sympathetic outflow, leads to decrease in BP=anti-hypertensive agent

Front 52

Clonidine class/ receptor

Back 52

A2 selective adrenergic agonist

Front 53

Clonidine adverse effects

Back 53

A2 selectie adrenergic agonist, dry mouth ,sedation, sexual dysfunction, orthostatic hypotension

Front 54

phenylephrine class/ receptor

Back 54

A1 adrenergic agonist

Front 55

describe the CV effects of phenylephrine

Back 55

A1 agonist=vasoconstriction=increase in Systolic and diastolic BP, decrease in blood flow, reflex bradycardia

Front 56

Despite the fact that  norepinephrine and phenylephrine are sympathomimetics, they lead to a decrease in heart rate. Why is this ?

Back 56

NE (A1, A2, B1, mainly A1)-overall increase in peripheral resistance leads to an increase in BP (no B2 receptors to lower diastolic), the increase in BP activates barroreceptors leading to a vagally mediated decrease in HR. phenylephrine (A1) has a similar effect

Front 57

methyldopa class/receptor

Back 57

adrenergic agonist, A2

Front 58

methyldopa use

Back 58

A2 agonsit, anti-hypertensive, activation of A2 receptor in CNS reduced sympathetic outflow, can be used in pregnant women

Front 59

dobutamine receptor/ class

Back 59

Beta adrenergic agonist

Front 60

dobutamine CV effects

Back 60

increased HR, contractility, CO (B1), minimal change in PR and BP (no a1 effect)

Front 61

dobutamine use

Back 61

B agonist, Tx cardiac decompensation, can use in cardiac stress testing

Front 62

Dopamine class/ receptor

Back 62

adrenergic agonist, DA1, B1, A1

Front 63

Dopamine CV effects

Back 63

low=DA1=vasodilation of renal and mesenteric aa., decrease in PR; medium=B1=increased HR, force, CO; high=A1=vasoconstriction, increase PR

Front 64

Dopamine use

Back 64

adrenergic agonsit (DA1, B1, A1), severe decompensated heart failure, shock (cardiogenic, septic)

Front 65

Isoproterenol class/ receptor

Back 65

adrenergic agonsit, Beta receptors

Front 66

isoproterenol use

Back 66

adreneric agonist B1, B2

in emergencies to stimulate HR and during bradycardia or heart block

Front 67

isoproterenol CV effects

Back 67

B1/B2 agonist=decrease in PR (B2 on skeletal mm.) increase in HR (B1) decrease in BP (no a1 effect)

Front 68

Norepinephrine, epinephrine and isoproterenol are all sympathomimetics but they each have  a different  net effect on mean  BP. What is the effect of each and why?

Back 68

NE (A1, A2, B1)-net increase because of A1 constriction, no B2 dilation; Epi (A1, A2, B1, B2)-no change, A1 constriction countered by B2 dilation, isoproterenol (B1, B2)- decrease-B2 dilation with no a1 constriction

Front 69

epinephrine class/ receptor

Back 69

adrenergic agonist, A1, A2, B1, B2

Front 70

epinephrine CV effects

Back 70

increase HR, force, CO (B1), increase systolic (A1) decrease diastolic (B2) no net change in BP

Front 71

epinephrine metabolic effects

Back 71

agonist, A1, A2, B1, B2
hyperglycemia (B2 stimulation= GNG, glycogenolysis, A2= inibition of insulin release), Lipolysis (b1, B2, B3)

Front 72

Epinephrine uses

Back 72

hypersensitivity, increase duration of local's, bradyarrhythmia, ophthalmic (mydriatic, decrease hemorrage, conjuctival decongestion)

Front 73

norepinephrine class/ receptors

Back 73

adrenergic agonist, A1, A2, B1,

Front 74

norepinephrine CV effecs

Back 74

A1, A2, B1, mostly A1 mediated, vasoconstriction, increase BP (no B2 to dilate), reflex bradycardia

Front 75

List some general side effects of adrenergic agonists. Which receptors are responsible

Back 75

alpha agonists-headache (vasoconstriction) cerebral hemorrhage (high BP), restlessness, anxiety

Beta-high HR, angina, cardiac arrhythmia, restlessness, anxiety

Front 76

amphetamine class

Back 76

mixed adrenergic agonist alpha and beta