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Pharmacology > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

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1
Q

What agonist drug inhibits reuptake of Dopamine and NE

A

cocaine (indirect)

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2
Q

What agonist drugs inhibits MAO so more NE is available

A

Selegiline (eldepryl)

Phenelzine (Nardil)

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3
Q

What agonist drugs reverse uptake to increase NE and dopamine release?

A

Amphetamines

Methylphenidate (Ritalin)

Tyramine (diagnostic, not a drug)

ALL highly addictive

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4
Q

What is ephedrine

A

direct agonist and indirect releasing drug of NE and dopamine

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5
Q

What drugs are beta agonists?

A

Dobutamine (Dobutrex)

Isoproterenol (Isuprel)

Albuterol (Ventolin)

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6
Q

What drugs are alpha agonists

A

Phenylephrine (Neo-Synephrine)

Clonidine (Catapres)

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7
Q

What drugs are mixed alpha and beta agonists

A

norepinephrine (Levophed)

epinephrine (Adrenalin)

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8
Q

Difference between direct and indirect agonists

A

indirect affects amount of NT at target site

direct interacts with receptors

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9
Q

What GPCR is alpha 1

A

Gq

phospholipase C–> IP3 and DAG

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10
Q

What GPCR is alpha 2

A

Gi

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11
Q

What GPCR is beta 1

A

Gs

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12
Q

What GPCR is beta 2

A

Gs

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13
Q

What GPCR is beta 3

A

Gs

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14
Q

What GPCR is D1

A

Gs

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15
Q

What GPCR is D2

A

Gi

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16
Q

Where are alpha 1 receptors

A

vascular smooth muscle–> contraction

pupillary dilator M–> contracts so pupil DILATES

prostate–> contraction

heart–> increase force (inotropy)

skeletal muscle (some)

skin vessels and mucous membranes (contract/decrease)

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17
Q

Where are alpha 2 receptors

A

neurons–> modulate NT release

platelets–> aggregation

ad. and chol. nerve terminals–> inhibit NT release

some vascular smooth muscle–> contraction

fat cells–> inhibit lipolysis

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18
Q

Where are beta 1 receptors

A

heart–> increase force (inotropy) and rate (chronotropy) of contraction

juxtaglomerular cells–> INCREASE renin release

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19
Q

What is the overall effect of activating beta 1 receptors in the heart

A

increase BP and TPR

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20
Q

Where are beta 2 receptors

A

respiratory, uterine, vascular smooth muscle–> RELAX

skeletal muscle–> K+ uptake

liver–> + glycogenolysis and gluconeogenesis

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21
Q

Where are beta 3 receptors

A

bladder–> relax detrusor M

fat cells–> + lipolysis

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22
Q

Where are D1 receptors

A

kidney and brain smooth muscle–> dilates renal BV

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23
Q

Where are D2 receptors

A

nerve endings–> modulate NT release

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24
Q

Where does epinephrine act

A

a1=a2, b1=b2

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25
What is the function of epinephrine
increase inotropy, heart rate, conduction velocity at AV node (b1) increase systolic BP (no change in MAP) (a1) can decrease diastolic BP and TPR (b2) skin vessels and mucous membranes (a1) relaxes bronchial M (b2) decrease bronchial secretion and congestion within mucosa (a1) increase renin release (b1) increase FFA in blood (b3) increase blood glucose levels (b2)
26
How can epinephrine cause muscle tremors and hypokalemia?
activates B2 receptors that enhance K+ uptake in skeletal muscle --> hyperpolarizes muscles so can't get another AP, tremor and depletes blood potassium concentration less K+ excreted
27
What receptors does norephinephrine act on
a1=a2, B1
28
What does norephinephrine do
potent cardiac stimulant (b1) ---> DECREASES HR d/t vagal response potent vasoconstrictor (a1) no bronchodilaton or vasodilation (no b2) increase TPR and BP (a1 and b1) role in baroreflex
29
TPR in epi vs NE
increase in NE d/t a1 and b1 decrease in epi d/t b2
30
What receptors does phenylephrine act on
a1
31
What does phenylephrine do
role of baroreflex mydriatic (dilates pupil) and decongestant (a1) severe vasoconstriction (a1) increase BP (a1) severe bradycardia (d/t vagal response)
32
What receptor does clonidine act on
selective a2 agonist
33
What does clonidine do
presynaptic a2 in lower brainstem: decrease sympathetic output decrease BP bradycardia peripheral a2: vasoconstriction (when given IV before reaching CNS)
34
What is clonidine used to treat
HTN
35
What receptors do isoproterenol act on
non-selective beta agonist (b1 and b2)
36
What does isoproterenol do
+ inotropy and chronotropy (b1) increase cardiac output (b1) bronchodilation (b2) vasodilator--> decrease arterial pressure (b2)
37
What receptors does dobutamine act on
mostly B1, some a1 (rare)
38
What does dobutamine do
a1: - isomer agonist, + isomer antagonist potent inotropy (b1) less potent chronotropy c/t isoproterenol
39
What receptor does albuterol act on
b2
40
What does albuterol do
bronchodilation
41
What drugs are highly addictive
indirect agonist d/t increase in NE and DO in CNS --> lipophilic, easily cross BBB
42
What is the function of tyramine
should increase systolic BP when given IV metabolized by MAO in liver, tests peripheral adrenergic fxn
43
What drugs to give in hypotensive emergency (overdose, shock)
norepinephrine, phenylephrine
44
What drug to give for chronic HTN
ephedrine
45
What drug to give for cardiogenic shock
dobutamine
46
What drug to give for short-term heart failure
dobutamine
47
What drug to give for long-term HTN
alpha 2 agonist
48
What drugs to give for emergent AV block and cardiac arrest
epinephrine, isoproterenol | treat heart and dilates lungs
49
What drugs to treat depression
phenelzine, selegiline (MAO-)
50
What drugs to treat narcolepsy
amphetamines, methylphenidate (reverse uptake)
51
What drug to treat ADHD
methylphenidate
52
What drugs to treat obesity
ephedrine, amphetamines
53
What drug to treat asthma
albuterol
54
What drugs for decongestion
phenylephrine, ephedrine
55
What drug for anaphylaxis
epinephrine (acts on heart and lungs)
56
What drug to evaluate retina
phenylephrine (mydriasis)
57
What drug for glaucoma
selective a2 agonist
58
What drug for stress urinary incontinence
ephedrine
59
What drugs primarily work on CNS?
indirect agonists
60
Adverse effects of adrenergic agonists
increased BP and work of heart--> MI or HF tachycardia and v-arrhythmias--> sudden death insomnia, decreased appetite, anxiety, psychoses (via indirect agonists @ CNS) convulsions and hemorrhagic stroke (cocaine)
61
What adverse effects can cocaine cause
convulsions and hemorrhagic stroke
62
What drug inhibits NE release and prevents storage
guanethidine (ismelin) indirect antagonist
63
What drug inhibits tyrosine hydroxylase (no NE synthesis)
Metyrosine (Demser) indirect antagonist
64
What drugs are nonselective alpha antagonists
Phentolamine (OraVerse) Phenoxybenzamine (Dibenzyline)
65
What drugs are selective alpha 1 antagonists
Prazosin (Minipress) Tamsulosin (Flomax) Doxazosin (Cardura)
66
What drugs are mixed antagonists
Labetalol (Trandate) Carvedilol (Coreg) mainly B and alpha 1
67
What drugs are nonselective beta antagonists
Propranolol (Inderal) Pindolol (Visken) Nadolol (Corgard)
68
What drugs are selective B1 antagonists
Metoprolol (Toprol) Betaxolol (Kerlone) Acebutolol (Sectral) Atenolol (Tenormin)
69
What is the difference between phentolamine and phenoxybenzamine
BOTH nonselective alpha antagonists phentolamine reversible, short acting phenozybenzamine irreversible non-competitive, longer acting
70
Alpha antagonist effects
decrease TPR and BP postural hypotension reflex tachycardia prostate SM relaxation, decrease resistance to urine flow relax pupillary dilator M--> miosis (constrict pupil)
71
What drugs to treat pheochromocytoma (tumor adrenal medulla)
phentolamine phenozybenzamine metyrosine (antagonists)
72
What drugs to treat chronic HTN
prazosin doxazosin (no non-selective antagonists)
73
What drugs to treat erectile dysfunction
phentolamine plus nonspecific vasodilator (papaverine)
74
Drug to treat BPH
tamsulosin (a1 ant with little effect on BP) prazosin and doxazosin used but severely decrease BP
75
Adverse effects of alpha antagonists
seen less with a1 ant postural hypotension (inhibit a1 in venous SM) nasal stuffiness tachycardia retention of fluid and salt impaired ejaculation
76
Beta blocker effects
decrease inotropy and chronotropy slow conduction at AV node initial rise in TPR but decrease with chronic use inhibits renin release increased airway resistance reduce intraocular pressure by decreasing production of aqueous humor inhibit lipolysis increase VLDL, decrease HDL inhibit glycogenolysis and gluconeogenesis
77
What type of agonists are beta blockers with intrinsic sympathomimetic activity
partial agonists --> block sympathetic effects but have submaximal agonist effects--> blunted sympathetic response
78
Why give partial agonist vs antagonist
less risk for bradycardia, increased VLDL/HDL ration -->desired effect without causing too much "damage"
79
What beta blockers are antagonists
atenolol nadolol propranolol
80
What beta blockers are partial agonists
acebutolol labetalol pindolol
81
What beta blockers are inverse agonists
betaxolol metoprolol
82
What antagonists treat HTN
both mixed and beta blockers
83
What drugs to give to reduce frequency of angina and improve exercise intolerance
beta blockers -->decrease work and oxygen consumption
84
What drugs to give to prolong survival after MI
propranolol metoprolol
85
What drugs to give to eliminate a-flutter, a-fib, ventricular ectopic beats
beta blockers
86
What drugs to give or chronic HF
metoprolol carvedilol DO NOT use in acute or severe congestive HF
87
What drug to give for glaucoma
betaxolol NO propranolol
88
What drug to give for hyperthyroidism
propranolol
89
Adverse effects of beta blockers
sedation, sleep disturbances, depression switch to hydrophilic drug increased airway resistance, trigger bronchospasm and asthma attack in those at risk switch to b1 selective decrease HR, contractility and excitability switch to partial agonist increase VLDL, decrease HDL with chronic use switch to partial agonist hypoglycemia (although safer in Type 2 DM) swithc to b1 selective toxicity and hyperresponsiveness to ABRUPT discontinuation

Pharmacology (6 decks)

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