Pharm Module 1 Adrenergic Agonist And Antagonists

Front 1

how is Tyrosine transported into nerve endings

Back 1

actively

Front 2

what is Tyrosine converted to once it enters the nerve endings

Back 2

dihydroxyphenylalanine(DOPA)

Front 3

what is DOPA converted to

Back 3

dopamine (DA)

Front 4

what converts DOPA into dopamine (DA)

Back 4

decarboxylase

Front 5

DA is then converted to what?

Back 5

Norepinephrine (NE)

Front 6

what converts DA to NE

Back 6

beta hydroxylase

Front 7

how is NE stored?

Back 7

in granules

Front 8

what is NE that is not stored in granules called

Back 8

mobile pool

Front 9

explain the NE life cycle

Back 9

- MAO can inactivate NE(mobile pool)

- During depolarization, Ca++enters the presynaptic terminal via the voltage dependent Ca++channels

- causes degranulation of the storage granules (vesicles)

- NE released via exocytosis into neuroeffectorjunction

- NE can activate the postsynaptic receptors

Front 10

Termination of Norepinephrine action is due primarily to what?

Back 10

removal from the neuroeffector junction back to presynaptic terminal via a specific transporter system

Front 11

how is it removed?

Back 11

through feedback regulation system

Front 12

Sympathetic nervous system exerts its effects by acting on_________

Back 12

a and β receptors

Front 13

two types of alpha receptors

Back 13

•a1 and a2 subtypes

Front 14

a1 is further divided into what

Back 14

•alpha1a & alpha1b

Front 15

β receptors include

Back 15

β1, β2 and β3 subtypes

Front 16

D receptors include

Back 16

D1 like (D1 and D5)

D2 like (D2 –D4)

Front 17

alpha 1 receptors couple to___

Back 17

Gq

Front 18

a1 coupled with Gq activate____

Back 18

IP3-DAG pathway

Front 19

alpha 2 receptor couples to____

Back 19

Gi

Front 20

a2 coupled with Gi does what

Back 20

inhibits adenylcyclase

Front 21

β receptors couple to______

Back 21

Gs

Front 22

β coupled with Gs does what

Back 22

activates adenylcyclase

Front 23

D1 receptors couple to_____

Back 23

Gs

Front 24

D1 coupled to Gs does what

Back 24

activates adenylcyclase

Front 25

location of alpha1 receptors?

what are they also responsible for?

Back 25

all blood vessels

mucosa

eye

skin

hyperglycemia

Front 26

alpha 1 receptors in blood vessels do what

Back 26

vasoconstriction

increase TPR

Front 27

alpha1 receptors in mucosa do what

Back 27

decongestion

Front 28

alpha1 receptors in the eye target what

Back 28

radial muscle

iris

mydriasis

Front 29

alpha1 receptors in the skin do what

Back 29

contract pilomotor muscles

Front 30

alpha2 receptors are found where

Back 30

presnyaptic and CNS

Front 31

what are they responsible in those locations

Back 31

presynaptic- reduce release

CNS - reduce sympathetic outflow

Front 32

where are DA receptors found

Back 32

splanchnic area

Front 33

what do they do there

Back 33

vasodilation

Front 34

where are beta1 receptors found

Back 34

heart and renal JG cells

Front 35

what are they responsible for in the heart

Back 35

increases rate

increases force of contraction

increases velocity of conduction

Front 36

where are beta2 receptors found?

what are they responsible for?

Back 36

pulmonary and coronary blood vessels

bronchial muscle

uterus

hyperglycemia and lactic acidemia

Front 37

what occurs in the pulmonary and coronary blood vessels

Back 37

vasodilation

Front 38

what occurs in bronchial muscle

Back 38

bronchiodilation

Front 39

where are beta3 receptors located

Back 39

adipose tissue

Front 40

what occurs at those receptors

Back 40

thermogenesis

lipolysis

Front 41

what occurs in the uterus with beta2 receptors

Back 41

relaxation

Front 42

role of adrenergic drugs

Back 42

Important regulator of the activities of heart and peripheral vasculature, especially in response to stress

Front 43

drugs that mimic the actions of epinephrine and norepinephrine are called what

Back 43

sympathomimetic drugs

Front 44

sympathomimetic drugs are also called what

Back 44

adrenergic drugs

Front 45

adrenergic drugs can be grouped by_____and ____.

Back 45

their mode of action

the spectrum of receptors that they activate

Front 46

adrenergic drugs act_____and____.

Back 46

direct and indirect mode

Front 47

2 examples of adreneric drugs acting directly

Back 47

epinephrine and norepinephrine

Front 48

which mode directly interacts with and activate adrenoceptors

Back 48

direct mode

Front 49

which mode actions are dependent on the release of endogenous catecholamines.

Back 49

indirect mode

Front 50

indirectly acting drugs work by either____

Back 50

Displacement of stored catecholamines

or

Inhibition of reuptake of catecholamines already released

Front 51

drugs that work by displacement

Back 51

amphetamine and tyramine

Front 52

drug that works by inhibition of reuptake

Back 52

cocaine

Front 53

T/F

some drugs have both direct and indirect actions

Back 53

true

Front 54

both types of sympathomimetics will ultimately do what

Back 54

activate adenoreceptors

Front 55

this activation leads to what

Back 55

characteristic effects of catecholamines

Front 56

6 examples of catacholamines

Back 56

epinephrine

norepinephrine

dopamine

phenylethylamine

isoproterenol

catechol

Front 57

The net effect of a given drug in the intact organism depends on_______

Back 57

1.Its relative receptor affinity (aor β)

2.Intrinsic activity of the drug

3.The compensatory reflexes evoked by its direct actions

Front 58

vascular smooth muscle is regulated by

Back 58

adrenoreceptors

Front 59

Catecholaminesare important in controlling

Back 59

PVR & venous capacitance

Front 60

a1 stimulation does what to resistance in blood vessels

Back 60

increases

Front 61

β2 receptors promote what in blood vessels

Back 61

smooth muscle relaxation

Front 62

β2 stimulation does what to resistance in blood vessels

Back 62

decreases

Front 63

The skin & splanchnic vessels have predominantly what type of receptors

Back 63

alpha receptors

Front 64

those receptors will cause what in the presence of epinephrine and norepinephrine

Back 64

constriction

Front 65

if beta receptors are activated, what happens in blood vessels of skeletal muscles

Back 65

dilation

Front 66

Overall effects of a sympathomimetic drug on blood vessels depends on what

Back 66

relative actions at a and βreceptors.

Front 67

Direct effects on the heart are determined largely by what receptors

Back 67

β1receptors

Front 68

Beta-receptor activation in the heart results in what

Back 68

increased calcium influx in cardiac cells

Front 69

this influx does what

Back 69

increases rate of contraction and force of contraction of the myocardium.

Front 70

positive chronotropic effect occurs when_____.

Back 70

Pacemaker activity is increased

Front 71

positive inotropic effect occurs when

Back 71

Intrinsic contractility is increased

Front 72

Activation of a1 receptors _____ peripheral arterial resistance and _______ venous capacitance

Back 72

increases

decreases

Front 73

that activation leads to what

Back 73

dose-dependent rise in blood pressure

Front 74

Stimulation of βreceptors in the heart increases cardiac output and _________.

Back 74

will increase BP

Front 75

do Catecholamines enter the CNS effectively?

Back 75

no

Front 76

Some drugs e.g. amphetamine enters the CNS and produces what kind of effects

Back 76

stimulant

Front 77

adrenergic action in the CNS starts how?

Back 77

Starts by reducing fatigue and progresses into anorexia, euphoria and insomnia

Front 78

at very high does what can happen

Back 78

aggressiveness, marked anxiety and convulsions

Front 79

The radial pupillary dilator muscle of the iris contains what kind of receptors

Back 79

alpha receptors

Front 80

activation can cause what

Back 80

mydriasis

Front 81

what is mydriasis

Back 81

great dilation of the pupil

Front 82

aand βstimulants also have important effects on what

Back 82

intraocular pressure

Front 83

a agonists_______ the outflow of aqueous humor from the eye

Back 83

increase

Front 84

β antagonists _________the production of aqueous humor

Back 84

decrease

Front 85

The blood vessels of the upper respiratory tract mucosa contain what type of receptors

Back 85

alpha

Front 86

what action of adrenoceptor stimulants is clinically useful

Back 86

decongestion

Front 87

Bronchial smooth muscle(lower respiratory tract) contains which receptors

Back 87

β2

Front 88

their activation causes what

Back 88

bronchodilation

Front 89

The β2 receptors in the uterus do what

Back 89

relax the uterus

Front 90

this relaxation is clinically important because

Back 90

it can delay premature delivery

Front 91

The bladder base, urethral sphincter, and prostate contain which receptors

Back 91

a(a1A)

Front 92

these receptors do what

Back 92

mediate contraction and therefore promote urinary retention.

Front 93

The β2 receptors of the bladder wall do what

Back 93

mediate relaxation

Front 94

this relaxation does what

Back 94

promotes retention

Front 95

Ejaculation depends upon what

Back 95

normal a-receptor activation in the ductus deferens, seminal vesicles, and prostate

Front 96

Activation of β3 receptors in the fat cells leads to what

Back 96

lipolysis

Front 97

β3 receptor are _____ that could be useful in what?

Back 97

selective agonists

some metabolic disorders

Front 98

β receptors and a2receptorsare expressed where?

Back 98

pancreatic islets

Front 99

which receptor INCREASES insulin secretion

Back 99

β receptors

Front 100

which receptor DECREASES insulin secretion

Back 100

alpha receptors