11. DSA Autonomic Pharmacology Flashcards

1
Q

What are common targets of drugs?

A

Proteins such as GF receptors, hormone receptor, NT receptors
DNA

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2
Q

What are the major NT and receptors for parasympathetic nervous system?

A

NT: Ach
Receptors: muscarinic (nicotinic)

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3
Q

What are the major NTs and receptors for sympathetic?

A

Norepinephrine, Epinephrine, (ACh) dopamine

Receptors adrenergic alpha/beta, nicotinic muscarinic

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4
Q

What is the same for all preganglionic fibers NTs in autonomic fibers?

A

Acetylcholine

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5
Q

What are the postganglionic sympathetic and parasympathetic NTs?

A

Symp: norepinephrine
Para: acetylcholine

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6
Q

Where does the sysnthesis of epinephrine occur?

A

mainly in the adrenal medulla

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7
Q

nAChR (ionotropic) and mAChR (metabotropic) are both receptors. where can each be found?

A

N: CNS, adrenal medulla, autonomic ganglia
FX: excitatory
M:CNS autonomic ganglia, effector organs
FX: excitatory and inhibitory

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8
Q

Muscarinic receptors are coupled to GPCRs which when acitvated do what?

A

a downstream event. either via activation of PLC (M1/3/5) or inhibition of adenylyl cyclase (M2/4)

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9
Q

Parasympathetic NS M2 and M3 receptors are mainly found where?

A

M2 are found in heart, nerves, smooth muscles

M3 are found in glands, smooth muscle and endothelium

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10
Q

What are the 4 main steps at the adrenergic nerve terminal?

A
  1. Synthesis (dopamine)
  2. Storage (dopamine converted to norepinephrine)
  3. Release (by AP)
  4. Reuptake (norepinephrine/epinerphrine instead o ACh)
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11
Q

How is norepinephrine made in the nerve terminal?

A

In cytoplasm, tyrosine becomes dopa which becomes dopamine

Dopamine transferred to vessicle where covereted to norepinephrine (can become epinephrine if in adrenal medulla

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12
Q

Na dependent tyrosine transporter brings it into nerve terminal cytoplasm. Once converted, transported into vesicle via vesicular monoamine transporter (VMAT-2). Then what happens?

A

The VMAT2 tranports anything into vesicles, NE released upon AP and CA influx, the NE transport or dopamine transporter (NET/DAT) reuptakes back into nerve terminal for reuse

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13
Q

What can block VMAT2?

A

Reserpine

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14
Q

What can block norepinephrine trasnporter (NET)?

A

Cocaine, increasing NE in synapse

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15
Q

What do monoamine oxidase and catechol o methyltransferase do along with NET and DAT?

A

Metabolize catecholamines (NE/E/Dope)

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16
Q

Catecholamines activate two subsets of adrenergic receptors, what are they and what kinds are there?

A
Alpha receptors (GPCR) types one and two
Beta receptors (GPCR) types one two and three
17
Q

Whats the one thing to remember about alpha-1 receptors?

A

Stimulates contraction of all smooth muscle

Vasuclar smooth muscle-vasoconstriction

18
Q

What is the one thing to remember about beta2receptors?

A

relax smooth muscle, vasodilation

19
Q

What is the one thing to remember about muscarinic receptors?

A

contract smooth muscle (different signal than alpha 1 receptors)

20
Q

The key thing to remember in autonomics is that smooth muscles in blood vessels have no parasympathetic innervation, however the endothelium does what?

A

The endothelium via M3 activates NO synthase in response to ACh which acts as a vasodialtor, to oppose the sympathetic A1 response and vasoconstriction

21
Q

Activation of mAChRs on endothelial cells causes production and release of endothelium-derived relaxing factor EDRF, also known as nitric oxide (NO). How does this occur?

A

ACh activates M3 receptors in intact endothelial cells, increasing Ca2+ levels, which increases NO, which diffuses to smooth muscles and causes vasodilation

22
Q

Pheylphrine is an A1 receptor agonist. Which increases?

A

Increases blood pressure via baroreceptor, increasing parasympathetic NS, decreasing sympathetic NS

23
Q

Histamine causes a decrease in blood pressure via baroreceptor reflex, which leads to?

A

a decrease in para NS activation and increase in sympathetic NS activation

24
Q

What are cholinomimetic agents?

A

drugs that mimic ACh

25
Q

What are cholinoceptor-blocking drugs?

A

AChR antagonists

26
Q

What are sympathomimetic agents?

A

drugs that mimic or enhance a/b receptor stimulation

27
Q

What are adrenoceptor blocking drugs?

A

a/b receptor antagonists

28
Q

What is something that activates the receptor signal as a direct result of binding to it, activate a receptor to produce all of the receptors biologic functions or selectively promote one receptor function more than another?

A

An AGONIST

29
Q

What is something that binds to receptors but does not activate generation of a signal, interefere with the ability of an agonist to activate the receptor, or suppress the basal signaling of receptors that are active?

A

An ANTAGONIST

30
Q

The key receptors on the heart for cardiac response (Increased heart rate and cardiac output) are the __ receptors.

A

B1 receptors are on the heart
B2 are vasodilation for smooth muscle
A1 are vasoconstriction for smooth muscle
A2 mainly presynaptic CNS, decreases sympathetic tone

31
Q

What kind of drug would block the decrease in heart rate seen with an A adrenergic receptor agonist?

A

Muscarinic antagonist (atropine) decreases HR

32
Q

What is a drug target that is prescribed that increases force and decreases rate of cardiac contraction. (positive inotropy and negative chronotropy respectively).

A

Digoxin! to block the Na/K ATPase, increasing intracellular Na and Ca, leading to an increased force

33
Q

What two drugs can be used to decrease the force and rate of cardiac contraction?

A

Either a B1 antagonist or a M2 agonist (because need less sympathetic and more parasympathetic)

34
Q

What do antihistamines block?

A

Muscarinic receptors, excessive amounts can block sweat glands which can lead to an increased temperature and cutaneous vasodilation

35
Q

What would you do to correct the overactive response to antihistamines?

A

muscarinic acetylcholine receptors agonists! or my Acholinesterase inhibitor to increase Ach to overcome M blockers