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Definition 1

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Definition 2

what kind of drug is NE?

a1, a2, B1 agonist

what kind of drug is epi?

a1, a2, B1, B2 agonist

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Definition 3

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Definition 4

what kind of drug is dopamine?

dopamine receptor, B agonist

what kind of drug is tyramine?

indirectly acting sympathomimetic

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Definition 5

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Definition 6

what kind of drug is ephedrine?

directly and indirectly acting sympathomimetic

what kind of drug is amphetamine?

indirectly acting sympathomimetic

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Definition 7

Term 8

Definition 8

what kind of drug is phenylephrine?

a1 agonist

what kind of drug is clonidine?

a2 agonist

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Definition 9

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Definition 10

what kind of drug is isoproterenol?

B1 and B2 agonist

what kind of drug is dobutamine?

B1 agonist

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Definition 11

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Definition 12

what kind of drug is metaproterenol?

B2 agonist

what kind of drug is albuterol?

B2 agonist

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Definition 13

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Definition 14

what kind of drug is terbutaline?

B2 agonist

prototype a1 agonist

phenylephrine

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Definition 15

Term 16

Definition 16

what drug is used when have a stuffy nose to clear airway?

phenylephrine (a1 agonist)

what is a drug that can be used in the ICU to increase peripheral resistance without increasing CO?

phenylephrine (a1 agonist)

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Definition 18

prototype drug for a2 receptor

clonidine

action of clonidine

at the neuroeffector junction - on the nerve terminus itself feeds back and binds a2 receptor of the neuron releasing NE and inhibits release of more NE feedback regulator of NE release

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prototype drug for B1 receptor

dobutamine

prototype drug for B2 receptor

terbutaline

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Definition 22

what are the 3 ways adrenergic agonists can have an effect?

1. act directly on adrenergic receptors 2. act by promoting release of endogenous NE 3. mixed actions

actions of a1 receptor agonists

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Term 24

arteriole effect of a1 receptor agonists

vasocontriction increases peripheral resistance and BP

venous effect of a1 receptor agonists

1. vasoconstriction increases peripheral resistance and BP 2. venoconstriction decreases capacitance and increases venous pressure and right heart filling pressure 3. contraction of the iris radial (dilator) Definition muscle 24 induces myddriasis 4. constriction of bladder and intestine sphincters venoconstriction decreases capacitance increases venous pressure and right heart filling pressure

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Definition 26

effect of a1 receptor agonists in the eye

contraction of the iris radial effect of a1 receptor agonists (dilator) muscle on bladder and intestine induces mydriasis

contraction of sphincters

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Definition 28

actions of a2 receptor agonists

inhibition of neuronal NE release - decrease BP

prototype a2 receptor agonist

clonidine developed to be an anti-HTN drug - decrease BP by inhibiting neuronal release of NE

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Definition 29

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Definition 30

prototype a1 receptor agonist

phenylephrine

effect of phenylephrine infusion?

BP increase BV are related to heart via baroreceptors constrict vessels --> decrease CO --> decrease HR and SV via baroreceptors reversible

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Definition 32

BP drops initially - a1 receptors cause constriction normal response to getting to stop from crashing up from laying down (getting need more blood - HR and up in the morning)? contractility increase vasoconstrict
Term 33 Definition 33

side effects of a1 blockage

orthostatic HTN and syncope - block normal phys that allows for vasoconstriction problem elderly woman on a1 receptor blocker for HTN can fall and break a hip
Definition 34

Term 34

a1 receptor mediates ____ in BV

peripheral tone

effect of a1 on veins

don't constrict - stiffen and decrease compliance causes - blood to be increased back to the heart and increase right heart filling pressure and thus preload
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Definition 35

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actions of B1 receptor agonists

1. increased cardiac contractility and HR 2. increased lipolysis 3. production of renin from the kidneys

effects of B1 receptor agonist on heart

increased contractility and HR

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Definition 38

increased renin production from kidneys effects of B1 receptor agonist on peripheral fat increased lipolysis effects of B1 receptor agonist on renin production kidneys are singly innervated by the arterioles that lead to them
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Definition 39

Term 40

action of B2 receptor agonists

Term 41

1. relaxation of vascular SM; vasodilation results in decreased peripheral vascular resistance and BP 2. reflexive tachycardia with B2 agonist infusion 3. bronchodilation 4. uterine SM relaxation 5. gluconeogenesis and glycogenolysis Definition in 41 the liver

effects of B2 receptor agonist on vasculature

relaxation of vascular SM vasodilation results in decreased peripheral vascular resistance and BP

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Definition 42

effects of B2 receptor agonist on heart

reflexive tachycardia

effects of B2 receptor agonist on lungs

bronchodilation

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Definition 44

effects of B2 receptor agonist on uterus

uterine SM relaxation

effects of B2 receptor agonist on liver

gluconeogenesis and glycogenolysis

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Definition 46

most B1 receptors are located on

heart - CO

what determines CO?

HR and SV

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Definition 48

increase HR increase contractility (force of contraction) components of SV? preload contractility afterload effects of infusing B1 agonist? afterload - NOT increased with selective B1 agonist preload - not increased directly by B1; determined by veins

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Definition 50

effect on afterload with selective B1 agonist?

NOT increased

why does preload increase with B1 receptor agonists?

not directly determined by veins

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Definition 52

B2 receptor locations

airway skeletal muscle BV BV going to liver NOT in central BV

which BV do not contain B2 receptors?

central BVs

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Definition 54

effect on HR with infusion of a1 receptor agonist?

reflexive bradycardia

effect on HR with infusion of B2 receptor agonist?

reflexive tachycardia

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Definition 55

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Definition 56

NE is an agonist to which receptors?

a1, a2, B2 adrenergic receptors

effect of NE in renal BV?

induces profound constriction of renal BV dangerously reduces renal blood flow problem in patient with low GFR

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Definition 57

Term 58

Definition 58

is NE effective in oral admin?

NO

why is NE not effective when administered orally?

degraded by acidic pH

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Definition 60

does NE cross the BBB?

NO

epi is an agonist to which receptors?

a1, a2, B1, B2 receptors

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Definition 62

what receptor mediates bronchodilator effect of epi?

B2

what complicates the B2 bronchodilator effect of epi?

cardiac stimulation - B1 and elevations in systolic BP - a1

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Definition 64

use of epi

emergency management of anaphylactic shock characterized by severe bronchial constriction and CV collapse included as a vasoconstrictor agent in most local anesthetic (procaine-like) preparations
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why is epi included in most local anesthetic preparations?

as a vasoconstrictor agent to limit diffusion of local anesthetic

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Definition 66

side effects of epi used parenterally in high doses?

can produce cardiac arrhythmia

when can epi produce cardiac arrythmias?

when used parenterally in high doses

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Definition 68

how is epi administered?

by parenteral injection - as cardiac stimulant in emergencies inhalation or injection - as bronchodilator

which receptor does NE not target physiologically?

B2 epi does - accounts for difference in CV response between the two

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Definition 70

which binds a2 with higher affinity: epi or NE?

epi

what is the physiologically more important location of a2 receptors?

neuroeffector junction

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Definition 72

NE epi is not released at the neuroeffector junction which what is the physiologically is the physiologically most most important ligand for a2 important location of a2 receptors? why? receptors epi can bind a2 - not its primary role

phenylephrine type

prototype a1 selective agonist

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phenylephrine local use

applied topically to the nasal mucosa - induces increase BP - induces a vasoconstriction to improve vagally-mediated reflex of phenylephrine systemic use air flow slowing the heart in patients works well for stuffy noses with paroxysmal tachycardia and common cold
Definition 75 Term 76 Definition 76

Term 75

clonidine and a-methyl-dopa type

agonist at presynaptic a2 adrenergic receptors

a-methyl-dopa is converted to ____ and stored in ____

a-methylnorepinephrine sympathetic nerve terminals

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Definition 78

what is the classic nonselective B adrenergic agonist?

isoproterenol

isoproterenol type

agonist of B1 and B2 adrenergic receptors

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Definition 80

isoproterenol use

by inhalation as a bronchial dilator

isoproterenol side effects

induces tachycardia more frequently than B2 selective agonists (lacks specificity)

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Definition 82

dobutamine tends to have ____ action on the _____ than dopamine

more heart

dobutamine type

agonist for B-adrenergic receptors

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Definition 84

dobutamine use

used to stimulate the heart in cardiogenic shock

metaproterenol, albuterol, terbutaline, and salmeterol type

selective agonist for B2 adrenergic receptors

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Definition 85

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Definition 86

metaproterenol, albuterol, terbutaline, and salmeterol use

used for bronchodilation in management of reversible airway diseases (asthma, COPD)

metaproterenol, albuterol, terbutaline, and salmeterol delivery

by inhalers - deliver meds to airway and avoid confounding effects

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Definition 88

who typically gets metaproterenol, albuterol, terbutaline, and salmeterol toxicity

patients with dyspnea and anxiety about not being able to breath - often take too much of the drugs

effects of taking too much metaproterenol, albuterol, terbutaline, and salmeterol

drives Na/K ATPase - can cause hypokalemia and problems that go along with it

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Definition 89

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Definition 90

effects of dompamine at moderate doses?

agonist of D1 dopaminergic receptors relaxes SM in renal BV and improves renal blood flow

effects of dopamine at high doses

agonist of cardiac B1 (and B2) receptors increases cardiac contractility

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Definition 92

effects of dopamine at VERY high doses

becomes an agonist of a1 adrenergic receptors produce vasoconstriction and raise BP

half life of dopamine

short - rapid inactivation by hepatic MAO and COMT

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Definition 94

inactivation of dopamine

rapid by hepatic MAO and COMT

ephedrine orgin

found in many plants used in China for >200 years introduced in West medicine in 1924 as the first orally active sympathomimetic

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Definition 95

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Definition 96

ephedrine structure

non-catechol phenylisopropylamine

half life of ephedrine

long

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Definition 98

ephedrine direct action

direct a1 and B2 adrenergic activity

ephedrine indirect action

mainly - indirectly to promote release of endogenous NE

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Definition 100

how does ephedrine mostly act?

indirectly promote release of endogenous NE

ephedrine effect on CNS?

stimulant

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Definition 102

use of ephedrine

NE - get reflexive bradycardia from peripheral what drug would cause vasoconstriction despite B1 principal use - decongestant slight decrease in HR, activation (from baroreceptor also recommended for increase in systolic, reflex) could be stress incontinence in diastolic, and mean BP, and phenylephrine - same BP women a large increase in peripheral response (maybe larger); HR resistance? reduced more because no B1 action

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Definition 104

what drug would cause slight increase in HR, increase in systolic BP, decrease in diastolic BP, very minimal increase in mean BP, and a slight decrease in peripheral resistance?
Term 105

epi - acts on B2 what drug would cause eliminates rise in BP seen significant increase in HR, with NE slight increase in systolic don't get reflexive BP, decrease in diastolic BP, bradycardia seen with NE slight decrease in mean BP, binds B1 - increases HR and a large decrease in B2 actions on BV - primarily peripheral resistance? in liver and skeletal muscle
Definition 105 Term 106

isoproterenol - B1 and B2 only; no a big increase in HR no vascoconstrictor response enormous change in peripheral resistance
Definition 106

peripheral resistance is the relationship between?

CO and BP

pressure from inflow (aortic flow) - resistance to pressure (outflow) =

peripheral resistance

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Definition 107

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Definition 108

B1 agonist effect on CO?

increases CO

what is tocolytic therapy?

use of B adrenergic agents to attenuate premature labor, delay delivery, allow fetal maturation thereby - reducing neonatal morbidity and mortality

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Definition 110

what is a common side effect of B-adrenergic tocolytic therapy for treatment of preterm labor?

hypokalemia

what drug is often used for tocolytic therapy?

terbutaline (B-adrenergic agonist)

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Definition 111

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Definition 112

how do B-adrenergic agonists control serum K?

activate Na/K ATPase by what can happen with abrupt increasing cAMP - take K out withdrawal of a B adrenergic of blood and store in cell --> agonist? hypokalemia

can get rebound hyperkalemia

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Definition 114

what are the major side effects of B agonists?

cardiac arrhythmias hypokalemia can precipitate angina insomnia anxiety tremor

what are the major side effects of a agonists?

headache **reflexive bradycardia excitability restlessness can precipitate angina

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ephedrine actions

direct and indirect agonist

tyramine type

indirect acting sympathomimetics

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Definition 118

tyramine origin

normal byproduct of tyrosine metabolism

where is tyramine found in high concentrations?

fermented foods (cheese)

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tyramine action

enters NE nerve terminal via the amine transporter and causes NE release

tyramine in converted to ____ by ______

octopamine dopamine-B-hydroxylase

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Definition 122

metabolism of tyramine

readily metabolized by MAO

in what patients are the effects of tyramine intensified?

patients treated with MAO inhibitors

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Definition 124

how does drug tolerance to tyramine develop?

develops as NE is completely replaced by octopamine

amphetamines type

indirect acting sympathomimetic

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Definition 126

amphetamines action

facilitate release of NE

do amphetamines have direct effect on adrenergic receptors?

NO

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Definition 128

effect of amphetamines on CNS?

stimulant

cocaine type

indirect acting sympathomimetic

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cocaine action

blocks neuronal uptake1 pathway for NE extends half life of NE at synaptic cleft

what is important to know about cocaine toxicity?

negative impact can be played out over 72-98 hours after ingested toxicity is potentially several days after use because of long half life