Adrenergic Agonists (Ch. 6)

Front 1

What is the difference between direct acting adrenergic drugs and the indirectly acting?

Back 1

The direct acting adrenergics act directly on the adrenergic receptors whilst the indirect adrenergics increase the activity of endogenous adrenergics by enhancing their release or inhibiting their reuptake.

Front 2

What is the primary neurotransmitter in the adrenergic neuron?

Back 2

Norepinephrine

Front 3

What is another name of epinephrine?

Back 3

Adrenaline

Front 4

So what is the source of epinephrine?

Back 4

The adrenal gland converts 80% of its norepinephrine to epinephrine.

Front 5

What are the five steps in the process of adrenergic neurotransmission?

Back 5

Synthesis, Storage, Release, Receptor binding and Removal

Front 6

What are the steps in the synthesis of norepinephrine?

Back 6

Tyrosine enters the neuron by a sodium linked carrier. In the neuron the tyrosine is hydroxylated by tyrosine hydroxylase to form DOPA (Dihydroxyphenylalanine). The DOPA is then decarboxylated to form Dopamine. Dopamine is then taken up into the synaptic vesicles. In the vesicles dopamine is mostly converted to norepinephrine by hydroxylation.

Front 7

Which is the enzyme which hydroxylates dopamine to norepinephrine?

Back 7

Dopamine beta-hydroxylase.

Front 8

What is the content of the synaptic vesicles of the adrenergic system?

Back 8

Norepinephrine, dopamine, ATP, and beta-hydroxylase as well as other cotransmitters.

Front 9

How is epinephrine formed?

Back 9

Methylation of the amine group of norepinephrine.

Front 10

What are the different mechanisms by which norepinephrine may be removed from the synaptic cleft?

Back 10

Diffuse out and enter the genearl circulation.

Be metabolized in the cleft by catechol-O-methyltransferase, COMT.

Be reuptaken by a system that pumps the NE back into the neurono.

Front 11

Give examples of a few drugs which can inhibit the reuptake of the catecholamines into the neuron?

Back 11

Cocaine, TCAs, SSRIs and other antidepressants.

Front 12

What is the name of the drug which inhibits uptake of catcholamines into synaptic vesicles?

Back 12

Reserpine

Front 13

What are the names of the drugs which inhibit the release of catecholamines into the synaptic cleft?

Back 13

Guanethinide and bretylium

Front 14

Which is the PRIMARY method of ending the effect of norepinephrine?

Back 14

By reuptake.

Front 15

Which are the different adrenoceptors?

Back 15

alpha1, alpha2, beta1 and beta2 as well as other such as beta3

Front 16

What is the rank of order of potency at the alpha receptors?

Back 16

epinephrine > norepinephrine >> isoproterenol

Front 17

What is the rank of order of potency at the beta receptors?

Back 17

isoproterenol > epinephrine > norepinephrine

Front 18

What determines a compounds affinity for the beta receptors?

Back 18

The size of the amine group. The bigger the higher the affinity for beta receptors.

Front 19

Give examples of a few drugs which can inhibit the reuptake of the catecholamines into the neuron?

Back 19

Cocaine, TCAs, SSRIs and other antidepressants.

Front 20

What determines the potency at the receptors?

Back 20

The catechol group (The two hydroxyl groups on a benzene ring)

Front 21

What is the signalling system of alpha1 receptors?

Back 21

Alpha1 receptors, when stimulated, cause Phospholipase C to stimulate an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). The IP3 causes an increase in intracellular calcium levels.

Front 22

What is the name of the drug which inhibits uptake of catcholamines into synaptic vesicles?

Back 22

Reserpine

Front 23

Give examples of a few drugs which can inhibit the reuptake of the catecholamines into the neuron?

Back 23

Cocaine, TCAs, SSRIs and other antidepressants.

Front 24

What are the names of the drugs which inhibit the release of catecholamines into the synaptic cleft?

Back 24

Guanethinide and bretylium

Front 25

What is the name of the drug which inhibits uptake of catcholamines into synaptic vesicles?

Back 25

Reserpine

Front 26

What are the names of the drugs which inhibit the release of catecholamines into the synaptic cleft?

Back 26

Guanethinide and bretylium

Front 27

Which is the PRIMARY method of ending the effect of norepinephrine?

Back 27

By reuptake.

Front 28

Which is the PRIMARY method of ending the effect of norepinephrine?

Back 28

By reuptake.

Front 29

Which are the different adrenoceptors?

Back 29

alpha1, alpha2, beta1 and beta2 as well as other such as beta3

Front 30

Give examples of a few drugs which can inhibit the reuptake of the catecholamines into the neuron?

Back 30

Cocaine, TCAs, SSRIs and other antidepressants.

Front 31

Which are the different adrenoceptors?

Back 31

alpha1, alpha2, beta1 and beta2 as well as other such as beta3

Front 32

What is the rank of order of potency at the alpha receptors?

Back 32

epinephrine > norepinephrine >> isoproterenol

Front 33

What is the name of the drug which inhibits uptake of catcholamines into synaptic vesicles?

Back 33

Reserpine

Front 34

What is the rank of order of potency at the beta receptors?

Back 34

isoproterenol > epinephrine > norepinephrine

Front 35

What are the names of the drugs which inhibit the release of catecholamines into the synaptic cleft?

Back 35

Guanethinide and bretylium

Front 36

What is the rank of order of potency at the alpha receptors?

Back 36

epinephrine > norepinephrine >> isoproterenol

Front 37

What determines a compounds affinity for the beta receptors?

Back 37

The size of the amine group. The bigger the higher the affinity for beta receptors.

Front 38

Which is the PRIMARY method of ending the effect of norepinephrine?

Back 38

By reuptake.

Front 39

What is the rank of order of potency at the beta receptors?

Back 39

isoproterenol > epinephrine > norepinephrine

Front 40

What determines a compounds affinity for the beta receptors?

Back 40

The size of the amine group. The bigger the higher the affinity for beta receptors.

Front 41

Which are the different adrenoceptors?

Back 41

alpha1, alpha2, beta1 and beta2 as well as other such as beta3

Front 42

What determines the potency at the receptors?

Back 42

The catechol group (The two hydroxyl groups on a benzene ring)

Front 43

What is the signalling system of alpha1 receptors?

Back 43

Alpha1 receptors, when stimulated, cause Phospholipase C to stimulate an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). The IP3 causes an increase in intracellular calcium levels.

Front 44

What determines the potency at the receptors?

Back 44

The catechol group (The two hydroxyl groups on a benzene ring)

Front 45

What is the rank of order of potency at the alpha receptors?

Back 45

epinephrine > norepinephrine >> isoproterenol

Front 46

What is the rank of order of potency at the beta receptors?

Back 46

isoproterenol > epinephrine > norepinephrine

Front 47

What is the signalling system of alpha1 receptors?

Back 47

Alpha1 receptors, when stimulated, cause Phospholipase C to stimulate an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). The IP3 causes an increase in intracellular calcium levels.

Front 48

What determines a compounds affinity for the beta receptors?

Back 48

The size of the amine group. The bigger the higher the affinity for beta receptors.

Front 49

What determines the potency at the receptors?

Back 49

The catechol group (The two hydroxyl groups on a benzene ring)

Front 50

What is the signalling system of alpha1 receptors?

Back 50

Alpha1 receptors, when stimulated, cause Phospholipase C to stimulate an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). The IP3 causes an increase in intracellular calcium levels.

Front 51

Give examples of a few drugs which can inhibit the reuptake of the catecholamines into the neuron?

Back 51

Cocaine, TCAs, SSRIs and other antidepressants.

Front 52

What is the name of the drug which inhibits uptake of catcholamines into synaptic vesicles?

Back 52

Reserpine

Front 53

What are the names of the drugs which inhibit the release of catecholamines into the synaptic cleft?

Back 53

Guanethinide and bretylium

Front 54

Which is the PRIMARY method of ending the effect of norepinephrine?

Back 54

By reuptake.

Front 55

Which are the different adrenoceptors?

Back 55

alpha1, alpha2, beta1 and beta2 as well as other such as beta3

Front 56

What is the rank of order of potency at the alpha receptors?

Back 56

epinephrine > norepinephrine >> isoproterenol

Front 57

What is the rank of order of potency at the beta receptors?

Back 57

isoproterenol > epinephrine > norepinephrine

Front 58

What determines a compounds affinity for the beta receptors?

Back 58

The size of the amine group. The bigger the higher the affinity for beta receptors.

Front 59

What determines the potency at the receptors?

Back 59

The catechol group (The two hydroxyl groups on a benzene ring)

Front 60

What is the signaling system of alpha1 receptors?

Back 60

Alpha1 receptors, when stimulated, cause Phospholipase C to stimulate an increase in inositol triphosphate (IP3) and diacylglycerol (DAG). The IP3 causes an increase in intracellular calcium levels.