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Pharm > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Synthesis of NT in Adrenergic nerve terminal

A
  1. tyrpsine is actively transported into nerve endings
  2. is converted into DOPA by tyrosine hydroxyls (Rate-limiting step)
  3. DOPA is converted to dopamine by DOPA decarboxylase
  4. DA is metabolized to NE via Dopamine beta decarboxylase
  5. NE is taken up & stored in granules; NE not stored in granules is called the mobile pool–this can be inactivated by MAO

During depolarization, Ca2+ enters the presynaptic terminal via the voltage-dependent Ca channels–>degranulation of storage vesicles–>NE released via exocytosis into synaptic junction

Actions:

  1. NE can activate pre junctional receptors = alpha 2 receptors (feedback regulation system–>inhibition of further release)
  2. can activate postsynaptic receptors (alpha 1 & beta 1-3 receptors)
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2
Q

Termination of NE action

A
  1. mainly by reuptake (via NET= NE transporter)

2. Diffusion away from receptor site with eventual metal by catechol-o-methyl transferase (COMT) in plasma or liver

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3
Q

MAO inhibitors

A

increase the pre junctional levels of NE

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4
Q

Displacers

A

indirect acting sympathomimetics displace the stored NE

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5
Q

uptake inhibitors

A

indirect actinv sympathomimetics inhibit the uptake into nerve cell–>increases post junctional levels/actions of NE

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6
Q

alpha 2 receptor

A

pre-synaptic autoreceptor

coupled to G2–>inhibition of adenyl cyclase–>decrease cAMP

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7
Q

D1 receptors

A

activates adenyl cyclase–>increases cAMP

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8
Q

alpha 1 receptors

A

coupled to Gq–>stimulates PLC–>activates IP3 & DAG pathway

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9
Q

beta receptors

A

coupled to Gs–>activation of adenyl cyclase–>increased cAMP

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10
Q

Things that affect PVR

A

alpha 1: vasoconstriction–>increase TPR–>Increase BP

beta 2: vasodilation–>decrease TPR–>decrease diastolic BP

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11
Q

alpha 1 receptor locations & actions

A
  1. most vascular smooth muscle–>vasoconstriction–> Increase TPR & Increase BP
  2. Pupillary dilator muscle–>contraction–>dilates pupil
  3. Prostate (ductus deferens & seminal vesicles)–> contraction–>ejaculation
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12
Q

alpha 2 receptor locations & actions

A
  1. postsynaptic CNS adrenoceptors–>probably multiple
  2. presynaptic nerve terminals–>inhibition of NT release–> decrease sympathetic outflow
  3. some vascular smooth muscle (nasal mucosa)–> nasal decongestion
  4. fat cells–> inhibition of lipolysis
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13
Q

beta 1 receptor locations & actions

A
  1. heart–> increase F & rate of contraction

2. juxtaglomerular cells–> increase renin release

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14
Q

beta 2 receptor locations & actions

A
  1. bronchial relaxation–>bronchodilation
  2. uterine relaxation
  3. vascular bed in skeletal muscle

vasodilation–>decrease TPR

  1. skeletal muscle–>promotes K uptake
  2. human liver–>activates glycogenolysis
  3. increase pancreas insulin secretion
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15
Q

beta 3 receptor locations & actions

A

Fat cells–>activates lipolysis

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16
Q

D1 receptor locations & actions

A

dilates renal bv

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17
Q

D2 receptor locations & actions

A

nerve endings–> modulates NT release

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18
Q

Indirect agonist types:

A
  1. act via displacement of stored catecholamines from adrenergic nerve ending
    ex) amphetamine & tyramine
  2. act via inhibition of repute of catecholamines already released
    ex) cocaine & TCAs

some drugs may have direct & indirect actions

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19
Q

Indirect acting adrenergic agonists

A
  1. tyramine
  2. amphetamine
  3. ephedrine*
  4. metaraminol*
    1-4 increase release of NE
  5. cocaine (blocks reuptake
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20
Q

Nonspecific Adrenergic Agonists

A
  1. NE: a1=a2, B1»B2
  2. Epi: a1=a2=b1=b2
  3. Dopamine: D1=D2>B1»a
  4. Ephedrine: a1=a2=b1=b2
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21
Q

a1=a2=b1=b2

A

Epi & Ephedrine

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22
Q

alpha 1 agonists

A
  1. phenylephrine
  2. methoxamine
  3. metaraminol
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23
Q

alpha 2 agonists

A

clonidine

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24
Q

non-specific beta agonists

A

isoproterenol; B1=B2

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25
Q

beta 1 agonists

A

dobutamine

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26
Q

beta 2 agonists

A
  1. terbutaline*
  2. albuterol*
  3. metaproterenol
  4. ritodrine*
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27
Q

NE

A

non-specific adrenergic agonist: a1=a2; B1»B2

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28
Q

Fendolopam

A

D1 agonist

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29
Q

Adrenergic effect on BV
a1 –>
B2–>

A

a1–> increases arterial resistance
b2–>promote sm relaxation–>decrease arterial resistance

skin & splanchnic vessels have predominantly alpha receptors & constrict in the presence of Epi & NE

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30
Q

Adrenergic effect on Heart

A
  1. direct effects via B1 receptors–>increased Ca influx into cardiac cells = Pacemaker activity increased (+ chronotropic effect)
  2. conduction velocity in AV node increased
  3. intrinsic contractility is increased (+ inotropic effect)
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31
Q

Beta & alpha receptors in pancreatic islets

A

b receptors–>increase insulin secretion

alpha2 receptors–>decrease insulin secretion

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32
Q

Effect of Insulin

A
  1. Increased glycogen synthesis: insulin forces storage of glucose in liver (and muscle) cells in the form of glycogen; 2. lowered levels of insulin cause liver cells to convert glycogen to glucose and excrete it into the blood.
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33
Q

+ inotropic effect

A

intrinsic contractility increased

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34
Q

+ chronotropic effect

A

pacemaker activity increased

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35
Q

Phenylephrine effect on BP

A

alpha 1–>increase TPR –> Increase BP

also decreases venous capacitance

this leads to a dose-dependent rise in BP

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36
Q

Stimulation of B1 receptors in heart

A

increase CO & BP

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37
Q

Affect of stimulation of b2 receptors on BP

A

decrease peripheral resistance via vasodilation in certain vascular beds

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38
Q

Isoproterenol effect on CO & BP

A

increase CO; decrease peripheral resistance by activating B2 receptors

lowers BP via B2; raises HR via B1

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39
Q

Phenylephrine effect on BP & HR

A

raises BP (via alpha 1 receptors) but not HR bc no effect on beta receptors

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40
Q

Epi effect on BP & HR

A

increases BP & HR

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41
Q

antimuscarinics vs alpha 1 effect on eye

A

alpha 1–>only mydriasis, no cycloplegia

antimuscarinics–>cycloplegia

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42
Q

increased alertness, reduced fatigue, anorexia, euphoria, insomnia

A

effect of non-catecholamines (i.e. amphetamines) on CNS

in very high doses: aggressiveness, marked anxiety, convulsions

catecholamines don’t enter CNS

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43
Q

effect of stimulating receptors located on radial pupillary dilator muscle of iris

A

alpha receptors; stimulation–>mydriasis (dilation)

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44
Q

phenylephrine use

A

used as mydriatic for retinoscopy

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45
Q

epinephrine use in glaucoma

A

non-selective agonist used to increase the outflow of aqueous humor via uveocleral veins (obsolete) in treating glaucoma

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46
Q

apraclonidine use

A

alpha 2 selective agonist used to decrease aqueous secretion in the treatment of glaucoma

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47
Q

brimonidine use

A

alpha 2 selective agonist used to decrease aqueous secretion in the treatment of glaucoma

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48
Q

timolol

A

beta antagonist used to treat glaucoma: decrease the production of aqueous humor

(affects beta receptors in ciliary body)

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49
Q

beta 2 receptor stimulation in bronchial smooth muscle:

effect & use

A

bronchodilation; used to treat bronchial asthma

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50
Q

Adrenergic affects on Respiratory tract

A
  1. decongestant action of adrenoreceptor stimulants (via alpha receptors)
  2. B2–>bronchodilation of bronchial sm
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51
Q

Adrenergic affects on GU tract

A
  1. B2 receptors in uterus–>relaxation; used in premature labor
  2. alpha1A receptors in bladder base, urethral sphincter & prostate mediate contraction–>promotes urinary continence
  3. B2 receptors in bladder wall–>relaxation
  4. alpha receptor activation in ductus deferens, seminal vesicles & prostate –>ejaculation
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52
Q

Epi

A
  1. very potent vasoconstrictor & cardiac stimulant
  2. increase in systolic BP due to positive inotropic (Increase FOC) and chronotropic (Increase HR) effects via B1
  3. effect on skeletal m bv
53
Q

low-dose epi which receptors predominate

A

beta 1, 2

54
Q

high-dose epi which receptors predominate

A

alpha 1, 2, b1 no beta 2

55
Q

EPI affect on skeletal m bv

A

activates B2 receptors–>dilation–>decrease TPR–>decrease diastolic BP

contributes to increased blood flow during exercise

56
Q

NE

A
  1. more alpha action than beta
  2. relatively little action on b2
  3. increase TPR & BP (systolic & diastolic) via alpha 1
  4. compensatory baroreflex activation–>overcomes direct positive chronotropic (increase HR) effects of NE
  5. positive inotropic (increase FOC or contractility) effects on heart via B1
57
Q

Isoproterenol

A
  1. very potent beta receptor agonist; little effect on alpha
    • chronotropic & inotropic actions
  3. potent vasodilator (bc activates beta receptors almost exclusively)–>increase in CO assoc w fall in diastolic & MAP
58
Q

Dopamine

A
  1. activates D1 receptors in several vascular beds–> vasodilation
    2.
59
Q

Dobutamine

A

relatively B1 selective synthetic catecholamine

60
Q

low doses of dopamine (2-5mcg)

A

acts primarily on dopaminergic receptors–> increased renal, coronary & cerebral blood flow

61
Q

infusion rate of dopamine above 5mcg

A

stimulates beta receptors and increases release of NE–> increase in cardiac contractility

62
Q

high doses of dopamine (infusion rate between 10-20mcg)

A

begins to act on alpha receptors–>vasoconstriction

63
Q

amphetamine

A

indirect acting CNS stimulant; peripheral actions mediated through release of catecholamines

Sx: stimulant effect on mood

64
Q

methamphetamine

A

very similar to amphetamine with a higher ration of central to peripheral action

65
Q

dextroampheramine aka

A

adderall

66
Q

methylphenidate aka

A

ritalin

67
Q

ephedrine MOA & use

A

found in various plants i.e. ma huang; mild stimulant in CNS;
MOA= displaces NE from storage vesicles in presynaptic neurons

68
Q

pseudoephedrine

A

aka sudafed; narrows bv–>decreases swelling & congestion

69
Q

phenylephrine

A

relatively pure alpha agonist

used as nasal decongestant & mydriatic

70
Q

xylometazoline & oxymetazoline

A

direct acting alpha agonists

used as topical decongestants bc promote constriction of nasal mucosa

71
Q

Clonidine

  1. receptor type
  2. use
  3. side effects
  4. warnings/special uses
A
  1. alpha 2 selective agonist
  2. used in HTN, diabetic diarrhea, narcotic addicts & to treat benzodiazepam withdrawals
  3. postural hypotension, dry mouth, sedation, rebound hypertension
  4. don’t stop treatment abruptly bc withdrawal & rebound hypertension
72
Q

methyldopa

  1. receptor type
  2. use
  3. side effects
  4. warnings/special uses
A
  1. alpha 2 selective agonis
  2. used in HTN, diabetic diarrhea, narcotic addicts & to treat benzodiazepam withdrawals; DOC IN PREGNANCY
  3. postural hypotension, dry mouth, sedation, rebound hypertension
  4. DOC in pregnancy
73
Q

apraclonidine

A

clonidine derivative used in glaucoma

74
Q

bromonidine

A

clonidine derivative used in glaucoma

75
Q

tyramine

A

normal byproduct of tyrosine metabolism in the body; has similar effect to NE;

found in high concentrations in fermented foods i.e. cheese & smoked/aged fish

when given parenterally–>indirect sympathomimetic action bc of release of stored catecholamines

Clinical: greatly intensified in patients treated with MAOI–> marked increase in BP, so patients on MAOI should be careful eating tyramine-containing foods i.e. smoked/pickled fish & cheese

76
Q

example of physical antagonism

A

activated charcoal–>adsorbs

77
Q

example of chemical antagonism

A

antacids

78
Q

bronchospasm, mucous membrane congestion, angioedema & severe hypotension

A

anaphylaxis

Tx: IM epinephrine .3-.5mg; supplemented by glucocorticoids & antihistamines

79
Q

anaphylaxis is mediated by

A

Type 1 immune reaction; IgE-mediated reaction

80
Q

Tx of acute hypotension

A

usually of short duration while giving IV fluids

NE, Phenylephrine when vasoconstriction is desired

81
Q

massive MI can lead to

A

cardiogenic shock and acute HF;

positive inotropic agents (–>increase FOC) used to avoid this: dopamine or dobutamine

82
Q

drugs used in emergency management of complete heart block & cardiac arrest

A

isoproterenol & epi

83
Q

drugs used to avoid cariogenic shock & acute HF following massive MI

A

dopamine or dobutamine

84
Q

modafinil use

A

new amphetamine substitute used to treat narcolepsy

85
Q

albuterol uses

A

beta 2 agonist

used to treat bronchial asthma, premature labor & threatened abortion

86
Q

salmeterol use

A

beta 2 agonist used to treat bronchial asthma

87
Q

phenylephrine use

A

used for fundus exam

88
Q

clonidine use

A

moderate to severe hypertension

89
Q

epinephrine use

A

to prolong duration of local anesthetics (i.e. lidocaine) & reduce systemic toxicity

90
Q

alpha 1 receptor agonist effects on BP & HR

A

i.e. phenylephrine, methoxamine
increase BP
decrease HR

91
Q

alpha 2 receptor agonist use

A

ie clonidine, alpha-methyl dopa

decrease BP, used as anti-hypertensives

92
Q

beta 1 & beta 2 agonist use

A

increase HR, SV, CO

ie isoproterenol, dobutamine (b1>b2)

93
Q

beta 2 agonist use

A

decrease TPR, bronchodilation

ie salmeterol, albuterol, terbutaline

94
Q

Dobutamine

A

beta 1 stimulator

95
Q

alpha 1 effect in the prostate

A

contraction of the ductus deferens & seminal vesicles (resulting in ejaculation)

96
Q

alpha 2 affect on fat cells

A

inhibition of lipolysis

97
Q

alpha 2 affect on some vascular smooth muscle cells in the nasal mucosa

A

nasal decongestion

98
Q

beta 2 affect on skeleton muscle

A

promotes K+ uptake

99
Q

beta 2 affect on the human liver

A

activates glycogenolysis

increases pancreas insulin secretion

100
Q

D1 affect on smooth muscle

A

dilates renal blood vessels

101
Q

D2 affect on nerve endings

A

modulates NT release

102
Q

alpha 1 increases PVR by affecting arterial or venous resistance

A

ARTERIAL (it increases arterial resistance!!!)

103
Q

beta 2 affects PVR by?

A

promotes smooth muscle relaxation–> decreases arterial resistance

104
Q

beta 1 affects the heart BY

A

increasing calcium influx into cardiac cells

105
Q

the skin & splanchnic vessels are predominantly _____ receptors and _____ in the presence of NE & E

A
  1. alpha 1 receptors

2. constrict

106
Q

NE acts best on

A

alpha 1 = alpha 2 = beta 1; VERY LITTLE effect on beta 2!

107
Q

_____ receptors result in increased insulin secretion

A

beta receptors

108
Q

______ receptors result in decreased insulin secretion

A

alpha 2

109
Q

phenylephrine’s effect on BP

A

phenylephrine = alpha 1 –> increases TPR–> increase BP

it also DECREASES venous capacitance

this leads to a dose-dependent rise in BP

110
Q

stimulation of beta 1 receptors in the heart–>

A

increases HR & CO–> increases BP

111
Q

stimulation of beta 2 receptors in the heart–>

A

decreased peripheral resistance (via vasodilation in certain vascular beds)

112
Q

a nonselective agonist like isoproterenol will—>

A
  1. increase in CO (by activating beta 1 receptors) but also

2. decreases peripheral resistance by activating beta 2 receptors

113
Q

phenylephrine use

A

mydriatic for retinoscopy

114
Q

epinephrine use

A

glaucoma bc increases outflow of aqueous humor via uveocleral veins (obsolete)

remember mystics also increase outflow (i.e. pilocarpine, physostigmine, carbechol)

115
Q

alpha 2 selective agonist examples and uses in treating glaucoma

A
  1. apraclonidine & brimonidine

2. decrease aqueous secretion

116
Q

beta antagonists ie timolol use in treating glaucoma

A

decrease the production of aqueous humor (affects bet ain ciliary)

117
Q

useful in premature labor

A

beta 2 receptors in uterus mediate relaxation

118
Q

receptors stimulated to promote urinary continence

A
  1. alpha 1a: located in bladder base, urethral sphincter & prostate
  2. beta 1 receptors in the bladder wall also mediate relaxation
119
Q

receptor in the bladder wall that mediates relaxation and is use??

A
  1. beta 2

2. used to promote urinary continence

120
Q

stimulation of _____ receptor stimulates renin secretion

A

beta 1

121
Q

what will happen to systolic & diastolic BP with epinephrine use

A
  1. systolic BP increases: vasoconstriction from alpha 1 stimulation
  2. diastolic BP may decrease: beta 2 receptors in skeletal muscles–> dilation of vessels

remember #2 promotes blood flow to muscles during exercise

122
Q

High dose of epinepherine

A

NO beta 2 just alpha 1= alpha 2 = beta 1 –>high dose Epi = NE

123
Q

low dose epinephrine

A

beta 1 & beta 2 & alpha 1 & alpha 2; so low dose epinephrine = same beta effects as isoproterenol

124
Q

how does dopamine affect BP

A

D1 in vascular beds–> vasodilation

125
Q

Does methamphetamine has a higher ratio of central or peripheral actions

A

central

126
Q

low doses of dopamine (2-5 mug)

A

act primarily on dopaminergic receptors–>increased renal, coronary and cerebral blood flow

127
Q

doses of dopamine above 5mcg/min

A

dopamine stimulates beta receptors and increases release of NE–> increase cardiac contractility

128
Q

doses of dopamine between 10-20mcg/min

A

dopamine acts at alpha receptors–>vasoconstriction

Pharm (32 decks)

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