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BIOM*3090 > Midterm - Autonomic Pharmacology > Flashcards

Midterm - Autonomic Pharmacology Flashcards

1
Q

Autonomic nervous system

A
  • part of peripheral nervous system
  • SNS = fight or flight
  • PSNS = rest and digest
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2
Q

Where are SNS and PSNS not physiological ANTagonists?

A

smooth muscle, pilomotor, glands, blood vessels

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3
Q

Preganglionic vs postganglionic fibers

A
  • Preganglionic is closer to CNS (from spinal cord to ganglia)
  • Postganglionic is closer to tissue (innervates tissue from ganglia)
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4
Q

Structure of SNS ganglia

A
  • ganglia near the spinal cord
  • ONE short pre- to MANY long post- ganglionic fibers
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5
Q

Structuer of PSNS ganglia

A
  • ganglia close to or in target tissue
  • ONE long pre- to ONE short post- ganglionic fibers
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6
Q

PSNS neurotransmitters

A
  • cholinergic = release ACh
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7
Q

SNS neurotransmitters

A
  • adrenergic = release NE from postganglionic neurons (& EP from glands)
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8
Q

Balance of neurotransmission in cardiac muscle

A
  • Resting = PSNS = ACh is M2 (less B1 activated from SNS)
  • Active = SNS = NE is activating B1 (less M2 activated from PSNS)
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9
Q

ACh

A
  • one step to be synthesized by ChAT or to be degraded by AChE
  • activates muscarinic and nicotinic receptors
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10
Q

How do nicotinic receptors act?

A

Ion influx through Na+/K+ channel = depolarization

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11
Q

Norepinephrine synthesis

A

1) Tyrosine hydroxylase
2) Dopa decarboxylase
3) Dopamine Beta-hydroxylase

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12
Q

Norepinephrine degredation

A

1) Re-uptake (by MAO)
2) Diffusion away from synapse (by COMT)

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13
Q

Why is alpha2 different than alpha1, beta1, beta2 and M, N?

A

It is found on the PREsynaptic cleft (the others are on the POSTsynaptic)

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14
Q

Beta-hydroxylase

A

Converts dopamine into NE once transported into synaptic vesicles

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15
Q

Receptors of the eye

A
  • Constriction = M3 contracts the sphincter
  • Dilation = alpha1 contracts the dilator muscle
  • Secretion = beta increases and alpha decreases
  • Drainage = M3 contracts the ciliary muscle
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16
Q

Receptors of the heart

A

Heart rate = M2 decreases, Beta1 increases

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17
Q

Receptors of the blood vessels

A
  • Vasodilation = M3, M5
  • Vasoconstriction = Alpha1
  • Vasodilation of the BV in skeletal muscle = Beta2
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18
Q

Receptors of most organs & glands

A
  • M3 = contraction and secretion
  • Beta2 = relaxation of smooth muscle
  • Alpha1 = constriction of sphincters
19
Q

Why are the two indirect acting cholinergic agonists different?

A
  • Echothiophate = long-acting (irreversible bond to AChE)
  • Physostigmine = intermediate-acting (reversible bond to AChE)
20
Q

Which direct cholinergic agonists do NOT absorb and distribute well?

A

Acetylcholine, bethanechol

21
Q

Which direct cholinergic agonists DO absorb and distribute well?

A

Muscarine, pilocarpine, nicotine

22
Q

Which cholinergic agonists activate PSNS?

A

Muscarinic (with the exception of sweat glands which activate SNS)

23
Q

Which cholinergic agonists activates both PSNS and SNS?

A

Nicotinic (initially stimulates, then blocks)

24
Q

What does nicotine do at the ganglia?

A
  • activates both PSNS and SNS
  • increases ACh and NE release into tissue
25
Q

Tissues where SNS dominantes

A
  • blood vessels = no ACh-release (alpha1 = vasoconstriction in organs and skin, beta2 = vasodilation in skeletal muscle)
  • heart = rate and force increases
26
Q

Why does PSNS dominate in tissues that have both PSNS and SNS innervation?

A

Increased ACh amplifies effects at BOTH ganglia and tissue, unlike in SNS where increased ACh only amplifies at the ganglia (junction with tissue has NE not ACh)

27
Q

What do drugs that activate N receptors do?

A

Act at adrenal gland to amplify PSNS AND SNS activity:
- BV = SNS only, so alpha1 vasoconstricts in organs & skin and beta2 vasodilates in skeletal
- heart = increases heart rate

28
Q

What do indirect cholinergic agonists do to the heart?

A
  • inhibit AChE = increase ACh at ganglia and adrenal gland = activates Nn = stimulates PSNS and SNS
  • increased ACh = decreased rate & force of contraction
29
Q

Symptoms of muscarinic excess

A
  • Diarrhea
  • Urination
  • Miosis (pupil constriction)
  • Bradychardia
  • Bronchoconstriction
  • Excitation of CNS
  • Lacrimation (eye watering)
  • Sweating and salivation
30
Q

Nicotine toxicities

A
  • overexcitement of CNS can cause seizure
  • leads to eventual downregulation of N receptors (coma, respiratory depression)
  • PSNS activation = muscarinic excess symptoms
  • increased BP and heart rate
31
Q

Why are atropine and pralidoxime used to treat organophosphate poisoning?

A
  • symptoms come from muscarinic excess
  • these are muscarinic ANTagonists
32
Q

Atropine eye drops

A
  • Used to be used for cosmetics because they dilate the pupil
  • BUT they block M receptors across the whole body at the same time (causes dry mouth)
33
Q

Ganglionic blockers

A
  • antinicotinic
  • relieves pressure in vessels in emergency situations to decrease SNS activation in BV
  • eg. trimethaphan
34
Q

Neuromuscular blockers

A
  • antinicotinic
  • used in surgical procedures to reduce skeletal muscle contraction
    -eg. D-tubocurarine
35
Q

Glaucoma treatment

A

Pilocarpine, physostigmine, echothiophate

36
Q

How does the mechanism of action differ between pilocarpine and physostigmine?

A
  • Pilocarpine: direct agonist = binds and activates M3
  • Physostigmine: inhibits AChE = increase ACh = increase M3
37
Q

What cholinergic drug(s) should be avoided in an individual with glaucoma?

A

Any muscarinic antagonist (atropine, D-tubocurarine, trimethaphan)

38
Q

Factors influencing heart rate

A
  • cardiac output (CO) = heart rate x stroke volume
  • vascular tone = peripheral vascular resistance (PVR)

BP= CO x PVR

39
Q

Cholinomimetics vs sympathomimetics

A
  • Cholinomimetics = mimic action of
    ACh
  • Sympathomimetics = mimic
    action of NE/epinephrine
40
Q

Baroreceptors

A
  • monitors blood pressure
  • BP changes = baroreceptors initiate reflex pathways = moment to moment regulation of BP
41
Q

How would baroreceptors respond to low blood pressure?

A

Signal to CNS to decrease PSNS and increase SNS (SNS innervates BV)

42
Q

How does clonidine prevent diarrhea?

A

activates alpha2 = ↓ACh release = ↓M3 receptor activation = ↓GI tract motility (more time to absorb fluid)

43
Q

Toxicities of indirect CNS agonists

A

Multiple transmitters increased and multiple receptors activated = hyperactivity, tremor, seizures, etc.

44
Q

Baroreceptor reflex response

A
  • if beta1 is blocked, SNS increases by alpha1 (vasoconstriction)
  • if alpha1 is blocked, beta1 increases SNS (increased rate/force of contraction)

BIOM*3090 (3 decks)

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