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Colin CPR II > DSA - Adrenergic Drugs > Flashcards

DSA - Adrenergic Drugs Flashcards

1
Q

What is an adrenergic drug?

A

Drugs that modulate adrenergic transmission and primarily control the function of the sympathetic nervous system

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2
Q

What are adrenomimetic drugs?

A

AKA sympathomimetics, adrenomimetic drugs that activate adrenergic transmission by mimicking or promoting the effects of norepinephrine/epinephrine/dopamne at adrenergic receptors in the sympathetic nervous system

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3
Q

What are antiadrenergic drugs?

A

AKA sympatholytics, antiadrenergic drugs inhibit adrenergic transmission by preventing the effects of norepinephrine/epinephrine/dopamine at adrenergic receptors in the sympathetic nervous system.

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4
Q

What are the types of adrenergic receptors?

A
  • Alpha Adrenergic Receptors
  • Beta Adrenergic Receptors
  • Dopamine Receptors
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5
Q

What are the types of Alpha Adrenergic Receptors and what variation of receptor are they?

A

Alpha 1 Receptors - Gq receptors - PLC promotes breakdown of PIP2 into IP3 and DAG

  • Alpha 1A
  • Alpha 1B
  • Alpha 1D

Alpha 2 Receptors - Gi receptors - inhibit cAMP accumulation

  • Alpha 2A
  • Alpha 2B
  • Alpha 2C
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6
Q

What are the types of Beta Adrenergic Receptors and what variation of receptors are they?

A

All are Gs receptors, increase cAMP

Beta 1 Receptors
Beta 2 Receptors
Beta 3 Receptors

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7
Q

What are the types of Dopamine receptors and what variation of receptors are they?

A

D1 Receptor
D5 Receptor
- Gs receptor - increases cAMP

D2 Receptor
D3 Receptor
D4 Receptor
- Gi receptor - decreases cAMP

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8
Q

What is the signal transduction cascade of Gq receptors?

A

Agonist binds to Alpha 1 receptor

Gq protein exchanges a GDP for a GTP and the alpha subunit is separated from the Gq protein.

Gaq activates PLC

PLC converts PIP2 into IP3 and DAG

IP3 signals the release of stored calcium into the cytoplasm
- Calcium-dependent Kinases become activated and phosphorylate their target substrates

DAG activates PKC

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9
Q

What is the signal transduction cascade of Gs receptors?

A

Agonist binds to Beta Adrenergic Receptor

Gs protein exchanges GDP for GTP and the alpha subunit is separated from the Gs protein.

Gas subunit activates Adenylyl Cyclase (AC)

AC increases synthesis of cAMP

cAMP activates PKA

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10
Q

What is the signal transduction cascade of Gi receptors?

A

Agonist binds to Alpha 2 receptor

Gi protein exchanges GDP for GTP and the alpha subunit is separated from the Gi protein

Gai subunit inhibits Adenylyl Cyclase (AC)

This prevents AC from increasing cAMP synthesis and thus preventing PKA activation

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11
Q

What adrenergic receptor is primarily found in vascular smooth muscle and what is its function?

A

Alpha 1 receptors are found in vascular smooth muscle

Gq receptor

Causes vasoconstriction

(as opposed to renal blood vessel smooth muscles which have D1 dopamine receptors which are Gs receptors and cause vasodilation)

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12
Q

What adrenergic receptor is found in renal blood vessel smooth muscles and what is its function?

A

D1 Dopamine Receptors are found in renal blood vessel smooth muscles

Gs receptor

Causes vasodilation

(as opposed to non-renal vascular smooth muscle, which has Alpha 1 receptors which are Gq receptors and cause vasoconstriction)

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13
Q

What adrenergic receptors are found on the heart and what are their functions?

A

Alpha 1 adrenergic receptors

  • Gq receptor
  • Causes increased force of contraction

Beta 1 adrenergic receptors
- Gs receptor
Causes increased force AND rate of contraction

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14
Q

What is a direct-acting adrenergic drug?

A

Direct-acting adrenergic drugs produce their effects via direct interaction with adrenergic receptors

  • Adrenergic receptor agonist
  • Adrenergic receptor antagonist
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15
Q

What is an indirect-acting adrenergic receptor drug?

A

Indirect-acting adrenergic receptor drugs produce their effects by increasing or reducing the concentration of norepinephrine at target receptors.

  • Work by altering neurotransmitter concentrations at target site
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16
Q

How does cocaine affect adrenergic signaling?

A

Cocaine is an Indirect-Acting Adrenergic Drug

It is a norepinephrine-reuptake blocker
- Helps retain norepinephrine in synapse

17
Q

What are Monoamine Oxidase Inhibitors?

A

Monoamine Oxidase Inhibitors (MOAs) are Indirect-Acting Adrenergic Drugs

Monoamine Oxidase enzymes are responsible for the breakdown of NE in the presynaptic neuron.

MOA Inhibitors prevent the breakdown of NE, making them more readily available for release into the synapse

Example of MOA Inhibitor:
- Phenelzine

Colin CPR II (12 decks)

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