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
Q

What adrenergic receptors are found on the heart?

A

Alpha1

and

ß1

25
Q

Where do you find B1 receptors?

What do they respond to?

A

Only on the Heart, adipose, and Juxtaglomerular cells in the kidney.

They are responsive to Epi, NE, and dopamine

26
Q

Where do you find B2 receptors?

A
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
Q

Where do you find A1 receptors?

A

Smooth muscle constriction (vasoconstriction)

Iris - mydrisis
GI sphincter - tightening
Liver - gluconeogenisis

Heart - increases force of contraction

***Skin vessels have only A1 receptors!***

28
Q

Where do you find A2 receptors?

A

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
Q

Where do you find B3 receptors, what is it sensitive to, and what does it trigger?

A

Adipocytes (B1, B3)

Triggers Lypolysis

Sensitive only to Epinepherine

30
Q

What is the mechanism of Alpha 2 adronergic receptors?

A

Activated by NE, Epi

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
Q

What is the mechanism of Alpha 1 receptors?

A

Activated by NE, Epi

Triggers Gq protein–>activates PLc

PLc cleaves PIP into IP3 and DAG

IP3 releases Ca++ stored in ER

32
Q

What is the mechanism for B receptors?

A

Binding –> Gs –> Adenylyl Cyclase–> ATP to cAMP –> PKA –> phosphorlase activated

Also activates L-type calcium channels

33
Q

Why are Positive Inotropic drugs used?

A

Positive Inotropic drugs increase [Ca2+] in the cell, increasing contractility

–> This leads to improved cardiac performance, inculding larger stroke volume

50
Q

What are indications for Positive Inotropes?

A
  • 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
Q

What are the groups of Positive Inotropic agents?

A
  • Sympathomimetics (ß adrenergic agonists)
  • Phosphodiesterase Inhibitors
  • Cardiac Glycosides (Digoxin)
52
Q
A
53
Q
A
54
Q
A