Pharmacology Flashcards

1
Q

What neurotransmitter(s) is used in preganlionic neurons in the sympathetic and parasympathetic nervous system?

A

Acetyl Choline

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1
Q

What neurotransmitter is used in the sympathetic nervous system at the end organ?

A

Norepinepherine

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2
Q

What does the adrenal medulla secrete?

A

Systemic epinephrine and norepinephrine

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3
Q

What neurotransmitter does the SNS secrete at the adrenal medulla to cause endocrine secretion?

A

Acetyl Choline

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4
Q

What does sympathetic activation cause in the body?

A

“Fight or Flight”

Increase HR

Dilate eyes

Relax bronchioles

Decrease GI motility and tone

Generalized secretion of sweat glands

Increased blood flow systemically

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5
Q

What kind of autonomic receptors will you find on skeletal muscle?

A

Nicotinic ACh (muscular variant)

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6
Q

What kind of neurotransmitter receptor will you find on a parasympathetic post ganglionic neuron?

A

Muscarinic

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7
Q

What does parasympathetic activation cause in the body?

A

“Rest and Digest”

Decreased HR

Contraction of bronchioles

Increaesd GI tract motility and tone

Localized sweat secretion

Contraction of iris

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8
Q

What do presynaptic muscarinic receptors do?

A

Block Ca2+ channels from allowing Ca2+ into the cell, effectively preventing vesicle fusion and ACh release

  • they also cause secondary messenger cascades depending on type of receptor (odd or even)
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9
Q

Describe how the nicotinic receptor works

A

It is an ionotropic receptor

  • Made up of 5 subunits that form an ion channel
  • Binding of ACh (or nicotine) to receptor opens the channel and allows Na+ to flow into the cell
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10
Q

What kind of neurotransmitter receptors do sweat glands have?

A

Sympathetic ACh muscarinic (this is an exception to the rule)

Sympathetic end organ receptors are usually adrenergic.

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11
Q

What is the mechanism for muscarinic cholinergic receptors at the end organ?

A

M1, M3, M5:
Activation of the odd muscarinic receptors results in g-coupled protein cascades that activate the formation of IP3 and DAG, leading to increased intracellular calcium

M2, M4:
Activation of the even muscarinic receptors results in g-coupled protein cascades that activate opening of K+ Chanels, and inhibition of adenylyl cyclase (resulting in decrease of cAMP)

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12
Q

What iris muscles are under sympathetic control? What do they do?

A

Radial muscles cause iris to dialate when they contract mydriasis.

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13
Q

What iris muscle is under parasympathetic control? What does it do?

A

The sphincter muscle (sayswhat?) tightens and causes myosis.

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14
Q

How do cocaine and tricyclic antidepressants affect NE levels?

A

Increase activity at the terminal by blocking reuptake by NE Transporters (NET).

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15
Q

How and where does NE form?

A

Adrenal medulla and sympathetic post ganglionic terminals.

Tyrosine–>DOPA–>Dopamine–>NE–>

Epinepherine (only in adrenal medula)

16
Q

What is COMT and what does it do?

A

Catecholo-methyl transferase.

It’s located in the liver and inactivates endogenous and exogenous catecholamines.

17
Q

What does MAO do and where is it located?

(monoamine oxidase)

A

Oxidizes NE if not repackaged in a vessicle after it is reabsorbed by the nerve terminal.

It decreases free NE levels.

It is located in the mitochondria in the post ganglionic sympathetic neurons.

18
Q

How does amphedamine elicit it’s effect at the cellular level?

A

It enters the nerve terminal and NE storage vessicles and forces NE out.

It also blocks MAO.

19
Q

Where are adrenergic receptors found (generally)?

(Alpha, beta, and dopamine)

A

Found on cardiac tissue, smooth muscle, and glands

Alpha:
a1 = post-synaptic
a2 = pre- or post-synaptic (ß cells of pancreas)

Beta:
ß1 = post-synaptic
ß2 = extra-junctional on end organs
(circulating EPI acts on ß2)

Dopamine:
D1 = post-synaptic
D2 = pre- and post-synaptic

20
Q

What receptors does Epinepherine act on?

A

Beta 1, 2, 3

Alpha 1 and 2

21
Q

What receptors does NE work on?

A

Alpha 1, Alpha 2, and Beta 1

22
Q

What receptors does dopamine act on?

A

D1, D2, and B1

23
Q

What adrenergic receptors are found on the blood vessels and what do they do?

A

Alpha 1 - Arteriolar constriction, Venoconstriction

Alpha 2 - Vasoconstriction

Beta 2 - Arteriolar dialation in skeletal muscle and liver and venodialation

D1- Kidney and Mesentaric dialation

24
What adrenergic receptors are found on the heart?
Alpha1 and ß1
25
Where do you find B1 receptors? What do they respond to?
Only on the Heart, adipose, and Juxtaglomerular cells in the kidney. They are responsive to Epi, NE, and dopamine
26
Where do you find B2 receptors?
``` Respiratory, urine, and vascular smooth muscle (relaxation) Skeletal muscle (increases K+ uptake) Human liver (glycogenolysis) ``` The respond to EPI Extrajunctional (not at a nerve ending)
27
Where do you find A1 receptors?
Smooth muscle constriction (vasoconstriction) Iris - mydrisis GI sphincter - tightening Liver - gluconeogenisis Heart - increases force of contraction \*\*\*Skin vessels have only A1 receptors!\*\*\*
28
Where do you find A2 receptors?
Postsynaptic CNS neurons Platelets (aggregation) Adrenergic and cholinergic nerve terminals (inhibits transmitter release) Some vascular smooth muscle (contraction) Fat cells (inhibits lipolysis) Responds to EPI and NE
29
Where do you find B3 receptors, what is it sensitive to, and what does it trigger?
Adipocytes (B1, B3) Triggers Lypolysis Sensitive only to Epinepherine
30
What is the mechanism of Alpha 2 adronergic receptors?
Activated by NE, Epi ## Footnote **Activation of Gi1,2, or 3** --\> inactivates adenylyl cyclase --\> cAMP drops --\> PKA drops --\> phosphatase activation --\> relaxation **Activation of Gibeta and gamma** --\> increase K+ channel activity --\> relaxation
31
What is the mechanism of Alpha 1 receptors?
Activated by NE, Epi Triggers Gq protein--\>activates PLc PLc cleaves PIP into IP3 and DAG IP3 releases Ca++ stored in ER
32
What is the mechanism for B receptors?
Binding --\> Gs --\> Adenylyl Cyclase--\> ATP to cAMP --\> PKA --\> phosphorlase activated Also activates L-type calcium channels
33
Why are Positive Inotropic drugs used?
Positive Inotropic drugs increase [Ca2+] in the cell, increasing contractility --\> This leads to improved cardiac performance, inculding larger stroke volume
50
What are indications for Positive Inotropes?
- Intravenous agents: **Cardiogenic Shock**: inadequate CO due to pump failure SBP \< 100 Cardiac Index \< 2.2 L/min/m2 high preload, yet poor urine output despit diuretics **Heart failure** refractory to oral agents - Oral agents: * *Chronic heart failure** with symptoms
51
What are the groups of Positive Inotropic agents?
- Sympathomimetics (ß adrenergic agonists) - Phosphodiesterase Inhibitors - Cardiac Glycosides (Digoxin)
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