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825 therapuetics > exam 1 lecture 6-7-8 sympathomimetics > Flashcards

exam 1 lecture 6-7-8 sympathomimetics Flashcards

1
Q

sympathomimetics

A

mimicking sympathetic activity
adrenergic agonists

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2
Q

monoamine

A

amine connected to aromatic carbon by 2-carbon chain
serotonin, dopamine, norepinephrine, epinephrine

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3
Q

catecholamine

A

monoamine with a catechol ring (benzene w/ 2-hydroxy)
DA, NE, E

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4
Q

biosynthesis of catecholamines

A

L-tyrosine –> L-dopa –> dopamine –> NE (presynaptic vesicle) –> E (adrenal medulla)

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5
Q

NE neurotransmission

A

tyrosine transported in –> dopa (tyrosine hyrdoxylase) –> dopamine (dopa decarboxylase)
dopamine into VMAT gets converted to NE by dopamine hydroxylase
release of NE when action potential opens Ca+ channels
NE releases and binds adrenergic R + regulatory R
NE that diffuses out of cleft gets reuptaken and metabolized by MAO
NE diffuses away from cleft metabolized by COMT

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6
Q

COMT

A

oral drugs
high activity in liver
metabolizes catecholamines

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7
Q

MAO

A

high neuronal
high activity in nerve terminal
metabolizes monoamines

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8
Q

stereochemistry

A

NE + E have R conformation on B-carbon. required for high affinity binding to receptor

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9
Q

A1 R

A

vasoconstriction
pupillary dilation
ejaculation
inhibit urination
GI inhibit

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10
Q

A2 R

A

prejunctional inhibition of NE release
decrease in CV SNS input (CNS)
vasoconstriction (minor)

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11
Q

B1 R

A

cardiac stimulation
secretion of renin (increase BP)

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12
Q

B2 R

A

bronchodilation
uterine relaxation
vasodilation
GI inhibit
cardiac stimulation (minor)

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13
Q

direct acting adrenergic receptor agonists

A

NE + E

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14
Q

norepinephrine

A

a1(vasoconstriction), a2(inhibit NE release), B1( cardiac stim)
substrate for MAO + COMT –> fast metabolism
parenteral admin + sodium bisulfite to prevent oxidation

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15
Q

epinephrine

A

a1(vasoconstriction), a2, B1(cardiac stim), B2 (bronchodilation)
substrate MAO + COMT
sodium bisulfite to prevent oxidation
uses: anaphylaxis /cardiac arrest
combo with local anesthetics to cause vasoconstriction –> prevent spread of anesthesia
low conc: targets B1 + B2 high conc: target A1

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16
Q

dopamine

A

low dose: D1 - vasodilation for blood flow B1 - cardiac stimulation
high dose: A1 - vasoconstriction
uses: shock + acute heart failure

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17
Q

dobutamine

A

B1 + a1 receptor agonist
B1 - cardiac stimulation
a1 - vasoconstriction
racemic mixture –> to exert stronger effect
metabolized by COMT not MAO
uses:

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18
Q

A1 receptor subtypes (Gq)

A

main function mediates vasoconstriction
agonist: nasal decongestant, vascular failure in shock, supraventricular tachycardia
antagonist: hypertension, benign prostatic hyperplasia, pheochromocytoma (tumor)

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19
Q

A1 direct acting receptor agonist

A

phenylephrine
methoxamine
oxymetazoline

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20
Q

phenylephrine

A

1 hydroxy on benzene ring –> a1 selectivity
use: nasal decongestant, mydriasis, pressor, vasoconstriction
admin: parenteral, local, oral (not substrate for COMT)

21
Q

2-aralkylimidazolines

A

direct a1 adrenergic agonist
vasoconstriction
r - substituted aromatic ring structure
x - methylene or amino

22
Q

a2 receptor agonist

A

inhibit sympathetic output: inhibit release of NE + decrease CV SNS input
agonist: HTN, pain, glaucoma0
brainstem controls CV action, a2 inhibits output from brain

23
Q

clonidine

A

selective a2 receptor agonist
decrease SNS output to heart + blood vessels

24
Q

guanbenz + guanfacince

A

open-ring, bridge decreases pka –> unionized –> cross BBB

25
Q

methyldopa + methyldopate

A

methyldopa: prodrug, good for CNS bc no b-hydroxy (more lipophillic), HTN
methyldopate: more water soluble ester –> parenteral use

26
Q

brimodine

A

glaucoma –> a2 R agonist in eye –> to inhibit aqueous humor production

27
Q

B1 receptor function (Gs)

A

increase HR, conduction, contraction
increase renin release
agonist: shock, congestive heart failure
antagonist: HTN, angina, arrthymias, congestive heart failure

28
Q

B2 receptor function (Gs)

A

bronchodilation + vasodilation
agonist: asthma + COPD
antagonist: glaucoma

29
Q

B3 receptor function (Gs)

A

urinary bladder relaxation
agonist: OAB

30
Q

isoproterenol

A

nonselective B receptor antagonist
B1 (cardiac stim) + B2(vaso + bronchodilation)
COMT not MAO metabolized
emergency use: increase HR + bradycardia

31
Q

baroreceptor - decrease BP

A

reflex tachycardia: increase in HR (B1)
vasoconstriction (a1)
net: increase BP

32
Q

baroreceptor - increase BP

A

reflex bradycardia

33
Q

baroreceptor - NE (a1 + b1)

A

a1 - vasoconstricts
b1 - cardiac stimulation (increase HR)
hr decreases; bp increase bc of reflex tachycardia

34
Q

baroreceptor - E (a1, b1, b2)

A

a1 - vasoconstricts
b1 - cardiac stim hr increase
b2 - vasodilates + bronchodilates
hr increase, bp stays same

35
Q

baroreceptor - isoproterenol (b1 + b2)

A

B1 - cardiac stimulation
B2 - vasodilator
Hr increases, BP decreases

36
Q

B2 agonist

A

‘erol’
bronchodilation
not metabolized by MAO + COMT
albuterol, salmeterol, formeterol, metaproterenol

37
Q

SAR

A

MAO: NE > E > Isoproterenol > colterol
catechol: B
meta OH : a1
meta-hydroxymethyl: b2
two meta OH: b2

38
Q

b3 agonist

A

mirabegron - OAB

39
Q

indirect sympathomimetics

A

does not bind NE receptor
promotes NE by reverse action PM transporter –> lot of NE at synapse

40
Q

amphetamines

A

ADHD –> no catechol, chirality, b-hydroxy
use: ADHD + nacrolepsy
ejects NE to synapse for prolonged stim
treatment overdose: acidify urine = increase secretion

41
Q

phentermine/topiramete

A

approved for weightloss

42
Q

ephredrine

A

b-hydroxy –> direct binding to a + b R –> use for weightloss + increase muscle strength
increase HR + BP
do not take with MAOI

43
Q

sudafed

A

L-config of b-hydroxy –> nasal decongestant
increase HR + BP
no MAOI

44
Q

MAOI

A

avoid with ephedrine + sudafed
NE will not get metabolized –> hypertensive crisis

45
Q

wine/cheese effect

A

thymine = indirect sympathomimetic agent
MAOI decreases breakdown of thymine –> bolus release of thymine\

46
Q

NET inhibitors

A

cocaine, methylphenidate, atomoxetine

47
Q

cocaine

A

blocks NET, decreases uptake + enhance NE signalling
local anesthetic
sides: increase BP + HR

48
Q

methylphenidate

A

DAT + NET inhibitor, so more DA + NE at synaptive cleft
ADHD + narcolepsy

49
Q

atomoxetine

A

NET inhib to enhance NE levels

825 therapuetics (8 decks)

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