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Fundamentals of Pharmacology > Adrenergic Pharmacology 1 > Flashcards

Adrenergic Pharmacology 1 Flashcards

1
Q

What are the important control points in adrenergic nerve function?

A
  1. Synthesis of Norepinephrine
  2. Uptake into storage vesicles
  3. Release of Neurotransmitter
  4. Receptors
  5. Feedback
  6. Metabolism
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2
Q

What are the important control points in adrenergic nerve function: 1. Synthesis of Norepinephrine

A

Hydroxylation of tyrosine is the rate-limiting step

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3
Q

What are the important control points in adrenergic nerve function: 2. Uptake into storage vesicles

A
  • Dopamine enters a vesicle and is converted to norepinephrine
  • Norepinephrine is protected from degradation in the vesicle
  • Transport into the vesicle is inhibited by reserpine
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4
Q

What are the important control points in adrenergic nerve function: 3. Release of Neurotransmitter

A
  • Influx of Ca2+ causes fusion of the vesicle with the cell membrane via exocytosis
  • Release is blocked by guanethidine and bretylium
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5
Q

What are the important control points in adrenergic nerve function: 4. Receptors

A
  • Postsynaptic receptor is activated by the binding of neurotransmitter
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6
Q

What are the important control points in adrenergic nerve function: 5. Feedback

A
  • Released norepinephrine is rapidly taken into the neuron
  • Reuptake is inhibited by cocaine and imipramine
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7
Q

What are the important control points in adrenergic nerve function: 6. Metabolism

A
  • Norepinephrine is methylated by COMT and oxidised by MAO
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8
Q

What indirect-acting sympathomimetic amines and what are their roles?

A
  • Drugs that increase levels of catecholamines without directly acting on adrenergic receptors
  • Affect level of neurotransmitter itself rather than affecting receptor
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9
Q

What is the overall effect of cocaine and amphetamines?

A
  • Increased levels of noradrenaline, serotonin and dopamine at the synapse causing increased stimulation of corresponding adrenergic receptors
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10
Q

What is the role of monoamine oxidase (MAO)?

A
  • Involved in the degradation process of DA, serotonin and NE
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11
Q

What is the role of catechol-O-methyltransferase (COMT)?

A
  • Important for degradation of circulating adrenaline taken up by uptake 2
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12
Q

What does MAO and COMT do to NA?

A

Remove and metabolise

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13
Q

What are the roles of MAO and COMT inhibitors?

A
  • Increase levels of endogenous catecholamines or adrenergic drugs
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14
Q

Describe Uptake 1: Neuronal

A
  • Selective for NA (uses NET)
  • Acts between nerves at the synapse
  • Presynaptic nerve involved
  • OBJECTIVE: to have quick effect by removing NA from synapse
  • High affinity: low maximum rate
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15
Q

Describe Uptake 2: Extraneuronal (systems that take up neurotransmitters from the blood)

A
  • Non-neuronal tissue: smooth muscle, cardiac muscle, endothelium
  • Collect NA from blood
  • NA and Adrenaline then metabolised by MAO & COMT
  • Low affinity: high maximum rate
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16
Q

What are the classes of MAO inhibitors?

A
  • Selective MAO-A inhibitors
  • Selective MAO-B inhibitors
  • Non-selective
17
Q

What do α-adrenergic receptors respond to?

A

Mainly to noradrenaline

18
Q

Where are α1 receptors found and what are their effects?

A
  • Found in smooth muscle, heart and liver
  • Effects: vasoconstriction, intestinal relaxation, uterine contraction and pupillary dilation
19
Q

Where are α2 receptors found and what are their effects?

A
  • Found in: platelets, vascular smooth muscle, nerve termini, pancreatic islets
  • Effects: vasoconstriction, inhibition of NA release and of insulin secretion
20
Q

What do β-adrenergic receptors respond to?

A

Mainly adrenaline

21
Q

Where are β1 adrenergic receptors location and what do they target?

A
  • Located: mainly in heart
  • Target: many drugs prescribed for heart conditions
22
Q

Where are β2 adrenergic receptors location and what do they target?

A
  • Located: mainly in lungs, GI, liver, uterus, vascular smooth muscle and skeletal muscle
  • Target: Many drugs
23
Q

Where are β3 adrenergic receptors location and what do they target?

A
  • Located: fat cells
  • Target: not targets for drugs
24
Q

What are the physiological consequences of adrenergic receptor activation?

A
  • Activation of a receptors: smooth muscle contraction
  • Activation of β1 receptors (heart): smooth and cardiac muscle contraction
  • Activation of β2 receptors (airways): smooth muscle relaxation

Fundamentals of Pharmacology (21 decks)

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