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Flashcards in Pharm 9.1 Deck (141)
1

norepinephrin is an

adrinergic neurotransmitter (except in sweat glands)

2

Epinephrine is hormone secreted by

the adrenal madula

3

Dopamine a neurotransmitter is found in

the basal ganglia, limbic system, CTZ, and anterior pituitary

4

difference btw norepinephrine and epiephrine

NE is an NT secreted by neurons and does not act on beta 2 rec, Epi is a hormone secreted by adrenal medulla and acts on all recptros (low dose acts on beta rec)

5

Epinephrine, norepinephrine, and dopamine (catecholamines) synthesized form

tyrosine

6

what is the rate limiting step in the synthesis of catecholamines

tyrosine hydroxylase

7

Fates of NE

binds alpha 1 rec post synaptically, binds alpha 2 rec presynaptically for auto inhibition, gets metabalized by MAO in axoplasm and COMT in snapse, reuptake back into primary neuron

8

tyrosine to dopamine happens in

axoplasm

9

dopamine is stored in

vesicles to prevent degredation

10

dopamine to NE in

vesicles

11

transport of dopamien into vesicles is inhibited by

reserpine

12

release of NT from axon termila is caused by

influx of ca causing fusion of the vesicle with the cell membrane

13

release of catecholamine vesicle is blocked by

guanethidine and bretylium

14

reuptake of catecholamines is inhibited by

cocain and imipramine

15

where is dopamine beta hydroxylase

dopamine beta hydroxilase is in vesicles to convert dopamine to NE

16

how is Ne coverted to Epi

by PNMT (phenylethanolamine N methyltransferase) only in the adrenal medulla bc epinephrine is important in flight, fright, fight

17

granules take up dopamine from the

cytoplasme

18

conversion of dopamine to NE occurs in granules by

dopamine beta hydroxylase

19

where are the granules

in the adrenergic termina (NE is stored in them)

20

how are NE and other catecholamines released

exocytosis in response to stimulatory signal

21

indirectly acting amines like tyramine and amphetamines induce

release of NE by displacing it from the nerve endings

22

efficient mechanism of release of NE

uptake of Ca

23

the most important mechanism for the ermination of the NE action

axonal uptake-->i.e. reuptake

24

what ihibits reuptake

cocaine and imipramine

25

NE can bind all receptors EXCEPT

BETA 2

26

metabolism of NE occurs by two enzyme systmes

MAO and COMT

27

MAO

monoamine oxidase

28

COMT

catechol-O-methyl transferase

29

NE is acted upon by MAO in the

axoplasm

30

COMT acts on NE when

NE it diffuses out in circulation, mainly in the liver and in the blood stream

31

MAO-A is present

in the nerve/liver mainly or anywhere

32

MAO-A metabolizes

NE, 5HT, tyramine

33

MAO-A inhibitors

Phenelzine, Tyranylcypromine (antidepressants)

34

MAO-B is present in the

Brain

35

MAO-B metabolizes preferentially

dopamine

36

MAO-B inhibitor

Selegiline (antiparkinson)

37

COMT inhibitors

Tolcapone, Entacapone

38

Tolcapone is

long acting

39

Entacapone is

Short acting

40

major metabolites excreted in the urine are

VMA (Vanillyl mandelic acid), metanephrine, and dihydroxy mandelic acid

41

when do you see an increase in adrenergic metabolites

pheochromocytoma - tumor of adrenal gland

42

does metabolism play a significant role in the termination of action of NE?

NO

43

what inteferes with the synthesis of catecholamines by intefering with tyrosine hydrolase

Metyrosine

44

what causes a blockade of storage in granule or granular uptake of catecholamines

Reserpine

45

what causes Displacement of NE from vesicles

amphetamine, tyramine (indirect sympathomimetic agents)

46

what causes Prevention of release of catecholamines

bertylium, guanethidine

47

wht causes block of reuptake at nerve terminal of chatecholamines

cocaine and imipramine

48

adrenergic receptors

alpha beta dopamine

49

aplpha receptors

alpha 1 (usually post synaptic) , alpha 2 (usually pre synaptic)

50

beta receptors

beta 1, 2, 3

51

dopamine receptors

D1, D2

52

type of receptors that adrenergic receptors are

g-proteins coupled receptors

53

adrenergic receptors act by either

increasing or decreasing syn of cAMP OR through IP3, DAG, and Ca2+ as second messengers

54

alpha 1 is a

Gq - inc PLC --> inc IP3, DAG, Ca2+

55

alpha 2 is a

Gi - dec Adenylyl cyclase --> dec cAMP

56

beta1/2 and D1 receptors are

Gs - inc Adenylyl cyclase --> inc cAMP

57

alpha 1 subtypes

A B D

58

alpha 2 subtypes

A B C

59

where do you find the alpha 1 subtype

SM of urethra -- use drugs targetting this recptors in obstructions in BPH

60

alpha 1 on

eye (radial/dialator) muscle, Arterioles (skin, viscera), Veins, Bladder trigone and sphincter, Male sex organs, Liver, Kidney

61

alpha 1 in eye/dialator muscle

contraction - mydriasis

62

alpha 1 in the arterioles (skin, viscera)

contraction - incTPR - inc diastolic pressure - inc afterload --want to shunt blood away from the skin and viscera and more available for the heart

63

alpha 1 in the veins

contraction - inc venous return - inc preload

64

alpha 1 bladder trigone and sphincter

contraction - urinary retension

65

alpha 1 in male sex organs

vas deferens - ejaculation

66

alpha 1 in liver

inc glycogenolysis

67

alpha 1 in kidney

dec renin release

68

alpha 2 receptors are found in

prejunctional nerve terminals, platelets, pancrease

69

alpha 2 in prejunctional never terminals

dec transmitter release and NE synthesis

70

alpha 2 in platelets

aggregation - makes sense bc in fight or flight you want to prevent bleeding out

71

alpha 2 in pancreas

dec insuline secretion

72

beta 1 in the

heart, Kidney

73

beta 1 in the SA node

inc HR - positive chronotropy

74

beta 1 in the AV node

inc conduction velocitiy (positive dromotropy)

75

beta 1 in artiral and ventricular muscle

in force of contraction (positive inotropy), conduction velocity, CO and oxygen consumption

76

beta 1 in His-Purkinje

inc automaticity and conduction velocity

77

beta 1 in Kidney

inc renin release

78

beta 2 in the

blood vessels, uterus, bronchioles, skeletal muscle, liver, pancres

79

beta 2 in the blood vessels

vasodialation - dec TPR - dec diastolic pressure - dec afterload

80

beta 2 in the uterus

relaxation

81

beta 2 in the bronchioles

dialation

82

beta 2 in the skeletal muscle

inc glycogenolysis - contractility (tremor)

83

beta 2 in the liver

inc glycogenolysis

84

beta 2 in the pancreas

inc insuline secretion

85

what receptor is most important for glycogenolysis

beta 2 then alpha 1

86

D1 peripheral receptor actos on

renal, mesenteric, coronary vasculature, causing vasodialation, inc renal blood flow, inc GFR, inc Na secretion(natriuresis)

87

slective agonist of Alpha 1 receptors - alpha 1 mimetics

phenylephrine, methoxamine

88

selective antagonist of alpha 1 receptors

prazosin, doxazosin, tamsulosin (on alpha 1A)

89

alpha 2 receptor agonsit

clonidine, guanfancine, methyldopa

90

alpha 2 antagonist

yohimibine

91

beta receptors

beta 1, 2, 3

92

beta 1 rec

on heart

93

beta 2 on

SM

94

beta 3 on

fat cells (adipocytes)

95

selective beta 1 agonist

dobutamine

96

slective beta 1 antagonist

atenolol, metoprolol

97

beta 2 receptors are mostly

not innervated

98

selective beta 2 agonsit

albuterol (salbutamol), salmenterol (longer acting), terbutaline

99

selective beta 2 antagonist

butoxamine

100

why would a beta 2 antaganist be used

treat bronchospasm (w/ butoxamine) bc remember beta 2 dialate, they are the enemies of alpha 1 that constrict

101

classification of adrenergic drugs

direct, indirect, mixed

102

direct actiong adrenergic drugs

epinephrine, norepinephrine, phenylephrine (beta 1), albuterol (beta 2)

103

indirect acting adrenergic drugs

acts by releasing NE, Tyramine, Amphetamine

104

Mixed acting adrenergic drugs

Ephedrine, Phenylpropanolamine (not on market bc caued stroke after it was in cough mixture)

105

naturally occuring catecholamines includes

epinephrine, norepinephrine, dopamine

106

catecholamines sturcture

catechol moiety and an ethylamine side chain

107

catecholamines are rapidly inactivated by

MAO and COMT (inactivation starts from the gut)

108

the catecholamine epinephrine acts on

alpha 1, alpha 2, beta 1, beta 2

109

the catecholamine norepinephrine acts on

alpha 1, alpha 2, beta 1

110

the catecholamine isproterenol acts on

beta 1, beta2, like epinephrine on steroides bc it vasodialates and decreases heart rate? And there is a reflex tachycardia

111

the catecholamine dobutamine acts on

beta 1

112

the catecholamine dopamine acts on

D1 ( beta 1 and alpha 1 at high doses)

113

the non-catecholamines that work on alpha 1 only

oxymetazolin, phenylephrine, methoxamine

114

non catecholamines that work on beta 2 only

albuterol, pirbuterol, terbutaline, salmeterol, formeterol

115

non catecholamines that acts more on beta 2 than beta 1

metaproterenol

116

non catecholamines that work on alpha and beta

ephedrine, psuedoephedrine

117

action of alpha 1 agonists

inc TPR, inc BP, potential reflex bradycardia, no change in pulse pressure

118

when could you use an alpha 1 agonist

tachycardia

119

action of beta 2 agonists

beta 1 actions increase HR, SV, CO, and pulse pressure, beta 2 actions decrease TPR and BP, overall increase/widening in pulsepressure

120

normal SV is

70 ml/beat

121

Epinephrine is a potent activator of

alpha and beta adrenergic receptors and have prominent cardiovascular effects

122

Epinephrine is involved in the sympathetic

fight flight fright

123

epinephrine on beta 1 receptors in CVS

inc rate of depolarization in cardiac myocytes, inc inotropy, inc chronotropy, inc CO, inc in BP

124

how does activating beta 1 receptors in CVS lead to faster depolarization

cardiac myocytes always leak out potassium, but activation of beta 1 receptors closes the potassium gates faster, depolarizing the SA-AV purkinje, increasing the rate of contraction and heart reate

125

when is activating beta 1 receptors important

asystole (no contraction)

126

epinephrine on alpha 1 receptors in CVS

at high dose causes vasoconstriction (vasopressor effect) via alpha 1, but at low does epi causes vasodialation (vasodepressor effect) via beta 2, produces a biphasic response

127

biphasic response

different effect based on dose

128

Dale's vasomotor reversal (Epinephrine Reversal)

when alpha 1 receptors are blocked, epinephrine will produce hypotension because of unmasking of beta 2 receptor activation

129

low dose epiniephrine

beta 1 and beta 2 stimulation

130

high dose epinephrine

alpha 1, beta 1(beta2) stimulation ---but beta 2 effect is masked

131

high dose epinephrine on alpha 1

inc TPR, inc BP, potential reflex bradycarida

132

high dose epinephrine on beta 1

inc HR, inc SV, inc CO, inc pulse pressure

133

high dose epinephrine on beta 2

dec TPR, dec BP ---> masked at the high dose

134

epinephrine on beta 2 receptors in Respiratory system

bronchodialation

135

alpha 2 receptors work by

stimulating Gi path, decreasing cAMP, stimulating nitric oxide release

136

anaphylaxis

bronchospasm + anaphylactic shock or low BP

137

how is Epinephrine used in anaphylaxis

beta 2 action decreases bronchospasm increasing partial pressure of O2; alpha 1 action increases CO, systolic BP, pulse pressure, tissue perfusion; decrease in eosinophil count reducing anaphylatoxin release

138

Gs

increases cAMP that inhibits MLCK (myosin light chain kinase)

139

Epinephrine metabolic effect

hyperglycemia, lipolysis

140

hyperglycemia by epinephrine

inc glycogenolysis in muscle and liver (beta 2), inc in gluconeogenesis (due to inc release of glucagon -( beta 2), dec insulin secretion (alpha 2)

141

lipolysis by epinephrine

beta 3 - inc cAMP in adipose tissue stimulating hormone sensitive lipase, leading to hydrolysis of TGs to FFA and glycerol