Adrenergic Receptor- Agonists and Antagonists Flashcards

1
Q

Alpha-1 Receptor Organs

A

Vascular Smooth Muscle

Pupillary Dilator Muscle

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2
Q

Alpha-2 Receptor Organs

A

Adrenergic and cholinergic nerve terminals

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3
Q

Beta-1 Receptor Organs

A

Heart

Juxtaglomerular Cells

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4
Q

Beta-2 Receptor Organs

A

Respiratory Smooth Muscle
Uterine smooth muscle
Vascular smooth muscle
Somatic Motor nerve terminals

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5
Q

Dopamine 1 Receptors

A

Renal vessels

Sphlancinc Vessels

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6
Q

Alpha-1 signaling

A

Positively coupled to Phospholipase C by G-alpha-q to increase IP3 and DAG.
IP3 causes calcium channels to open and increase- activating calmodulin and MLCK for muscle contraction

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7
Q

Alpha-2 Signaling

A

Negatively coupled to adenylyl cyclase by G-alpha-i to inhibit PKA activation, cAMP and therefore calcium influx in order to reduce propagation and release of neurotransmitter in pre-synaptic neurons. Also in vascular smooth muscle- inactivated PKA= activated MLCK and therefore constriction.

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8
Q

Beta-1 Signaling

A

Positively coupled to adenylyl cyclase by G-alpha-s. Increasing cAMP and having positive chonotropic and ionotropic effects due to PKA activation and therefore high calcium.

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9
Q

SA Node

A

Beta-1 activated G-alpha-s. AC-cAMP-PKA causes increased calcium channel and IF to reduce threshold of activation and more rapid depolarization

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10
Q

Myocytes

A

Beta-1 activated G-alpha-s. AC-cAMP-PKA that increases L-type calcium channels, ryanodine receptor on SR and SERCA

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11
Q

Sympathetic nerve terminals

A

Negative feedback to alpha-2 G-alpha-i that inhibits AC, cAMP and PKA to decrease calcium propagation and therefore no NT release

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12
Q

Vascular smooth muscle

A

Alpha-1 coupled to G-alpha-q stimulates phospholipase C to increase PIP2 to IP3 and increase calcium for muscle contraction by MLCK

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13
Q

Direct Acting Adrenergic Agonists

A
A1- phenylephrine
A2- Clonidine
BNS- Isoproterenol
B1- Dobutamine
B2- Terbutaline, Albuterol
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14
Q

Indirect Acting Adrenergic Agonists

A

Releasing- amphetamine, methamphetamine, methylphenidate, ephedrine, pseudoephedrine, tyramine

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15
Q

alpha-1 affinities

A

Epinephrine >= Norepinephrine&raquo_space;» isoproterenol

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16
Q

alpha-2 affinities

A

Epinephrine >= Norepinephrine&raquo_space;» isoproterenol

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17
Q

beta-1 affinities

A

isoproterenol > epinephrine&raquo_space;» norepinephrine

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18
Q

beta-2 affinities

A

isoproterenol > epinephrine = norepinephrine

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19
Q

Epinephrine

A

Stimulates a1,a2,b1,b2, short half life
Low dose- decrease diastolic (b2), increase CO (b1)
High dose- increase diastolic (a1,a2>b2), increase CO
Bronchodilation (b2), decrease secretions (1a)
Toxicity - arrythmia
Use in anaphylaxis, cardiac arrest, bronchospasm
Contra- late term preggos

20
Q

Norepinephrine

A

Stimulates a1, a2, b1, short half life
Increase cardiac output and systolic (b1)
Increase resistance and diastolic (a1, a2) (increase MAP)
DECREASE HR (baroreceptor to constricted vessels)
Toxicity- ischemia
Indication- vasodilatory shock
Contra- pre-existing vasoconstriction/ischemia

21
Q

Dopamine

A

Stimulates D1, D1, a1, a2, b1, short half life
Low doses- increase CO (b1), decrease TPR (d1)
High dose- increase CO, increase TPR (reaches a1,a2)
-Will still relax sphlancninc/renal wit D1
Indications- cardiogenic shock
Toxicity- low blood pressure at low dose, ischemia at high dose
Contra- tachycardic arrythmia, V fib

22
Q

Isoproterenol

A

non- selective beta agonist- higher half life
Decrease TPR with b2
Initial increase CO with b1 but low low diastolic will bring down systolic and therefore decrease MAP
Increase HR- baroreceptor reflex to vasodilation
Bronchodilation (b2)
Toxicity- tachyarrythmias
Indication- bradycardia, heart block with high TPR
Contra- angina + arrythmias

23
Q

Dobutamine

A
selective b1 (some b2 stimulation at higher doses)
increase CO (b1) for cardiogenic shock 
Toxicity- hypotension at HIGH doses due to b2 stim
Indications- short term for CHF, cardiogenic shock
24
Q

Beta-2 Signaling

A

Positively coupled to G-alpha-s proteins that will activate adenylyl cyclase and increase cAMP and activate PKA that INACTIVATES MLCK–>relaxation of muscle

25
Q

Indirect Adrenergic Agonists (Releasing)

A

Amphetamine: COMT resistant with long half-life, cross BBB
Taken up by re-uptake proteins, cause reversal of the re-uptake mechanism and release NT in a CALCIUM-INDEPENDENT manner.
Cardio- NE release, peripheral vasoconstriction (increase diastoic) and positive ionotropy/conotropy (increase systolic)
CNS- stimulant, anorexic agent
Toxicity- Tachycardia
Use- ADD, narcolepsy, nasal congestion
Contra- Rx with MAO inhibitors withing previous 2 weeks, hypertension

26
Q

Terbutaline

A

Selective b2 agonist
Prevent/reverse bronchospasm in asthma, bronchitis and emphysema
Eliminates via urine

27
Q

Phenylephrine

A

Selective a1 agonist
Pressor for anesthesia, nasal congestion, pupil dilator, supraventricular tachycardia, HTN
Less than 1 hr half life, eliminated by MAO

28
Q

Clonidine

A

Selective a2 agonist

Treat HTN, eliminated via urine with a long half life

29
Q

Beta- adrenergic antagonists

A

Non-selective- propranalol,. timolol, nadolol
B1 cardio selective- atenolol, metoprolol, esmolol
Partial Agonist- pindolol

30
Q

Propranolol

A

Non-selective b-blockers
Treat HTN, angina due to atherosclerosis, MI
4 hour half life, eliminated by liver

31
Q

Metoprolol

A

Cardioselective B1-blockers

Treat HTN, long term angina

32
Q

Pindolol

A

Partial Agonist b-blocker

Treat HTN

33
Q

Alpha-adrenergic antagonists

A

Non-selective- phenoxybenazmine, phentolamine

Selective A1- prazosin, doxazosin, terazosin

34
Q

Penoxybenazmine

A

Non-selective alpha-antagonists

Irreversible alpha-blocker to treat pheochrome-cytoma

35
Q

Prazosin

A

A1 antagonist

treat HTN

36
Q

Albuterol

A

B2- agonist

Use for bronchial relaxation durin asthma attack

37
Q

Nadolol

A

Beta- blocker for long term angina and hypertension with a long half life (a day)

38
Q

Timolol

A

Beta blocker for glaucoma

39
Q

Atenolol

A

Cardioselective B1 blocker for hypertension, angina and MI

40
Q

Esmolol

A

Emergency used b1 blocker with a short half life to treat supraventricular tachycardia

41
Q

Phentolamine

A

Reversible alpha-blocker to test for pheochrome-cytoma

Treat rx for pheo. before surgery

42
Q

Doxazosin

A

alpha 1 antagonist

43
Q

Terazosin

A

a1 blocker for prostatic hyperplasia and HTN

44
Q

Methylphenidate

A

Indirect sympathomimetic

Treat ADHD

45
Q

Ephedrine

A

Indirect sympathomimetic

Pressor durin anesthesia

46
Q

Psuedo-ephedrine

A

Indirect sympathomimetic

Treat nasal congestion

47
Q

Tyramine

A

Super short half life that displaces NE and increases ints activity in the synaptic cleft, MAO degrades it