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Pharmacology > Serotonin Agonist & Antagonists > Flashcards

Serotonin Agonist & Antagonists Flashcards

1
Q

Serotonin has biologic effects on which systems

A

CV & Platelets
GI tract
CNS

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2
Q

Disorders of the CNS, GI tract CV and others that affect the serotonin 5-HT receptor include:

A

CNS: migraines, depression, OCD, anxiety, schizophrenia, insomnia

GI tract: N/V, GERD

Obesity: Eating disorders

CV: smooth muscle contraction, stroke, coronary vasodilation, Bezold-Jarisch reflex (brady, hypotension, hypopnea, apnea)
Shivering
Premature ejaculation

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3
Q

Serotonin is synthesized from

A

L-tryptophan

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4
Q

L-tryptophan is obtained

A

in our diet

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5
Q

L-tryptophan is produced in what cells

A 
enterochromaffin cells (intestines)
serotonergic neurons
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6
Q

True or False

L-tryptophan is NOT synthesized

A

True

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7
Q

L-tryptophan is stored

A

Enterochromaffin cells

Platelets

CNS

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8
Q

Does L-tryptophan cross the BBB

A

No; must be synthesized in CNS

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9
Q

How is L-tryptophan biosynthesized

A

Hydoxylase»>decarboxylase»>serotonin (5-HT)

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10
Q

What are the modulators of 5-HT brain levels

A

Dietary intake (tryptophan)
consumption of competive aa
activity of alternate pathway of tryptophan degradation
** activity of degradation enzymes
activity of the 5-HT membrane transporter

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11
Q

Serotonin is metabolised by what intracellular enzyme and what gland

A

**MOA, type A»» 5-HIAA (measured in blood)

Pineal gland (forms melatonin via N-acetylation)

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12
Q

Reuptake occurs

A

serotonin trasporters

in the liver, lung endothelial cells

platelet accumulation

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13
Q

Serotonin effects on the CNS

A

enchances release of CRH via hypothalamus

Regulates temperature

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14
Q

What 5-HT receptor antagonist improves memory

A

5-HT6 receptor

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15
Q

The 5-HT1 receptors are primarily located

A

Hippocampus, basal gangllia, raphe nuclei

Decreases anxiety

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16
Q

5-HT2A receptors cause

A

CNS hallucinations
platelet aggregation
peripheral smooth muscle contraction

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17
Q

5-HT2B receptors cause

A

endothelium smooth muscle relaxation

Gastric fundus smooth muscle contraction

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18
Q

5-HT2C receptors cause

A

decreased appetite

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19
Q

** 5-HT3 receptors cause

A

Nausea NOT vomiting (area post rema)

Gastric empyting

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20
Q

***5-HT3 receptors are uniquely different than the other 5-HT receptors, how

A

5-HT 3 receptors are ligand-gated (Fast depolorizing channels)

All other 5-HT receptors are G-protein coupled receptors

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21
Q

Ecstasy works by

A

blocking serotonin transporters thereby significantly raising serotonin levels

22
Q

What is serotonin’s effect on sleep, anxiety, aggressiveness, and depression

A

cause sleep induction, decreases anxiety, decreases aggressiveness, and depression

23
Q

Serotonin’s effect on bronchiolar smooth muscle

A

contraction

24
Q

** Serotonin CV effect on 5-HT1 receptor stimulation

A

Vasodilation

inhibits NE release

25
Q

**Serotonin CV effects of 5-HT2 receptor stimulation

A

Contraction of most smooth muscle (bronchi, bladder) but

vasodiation of heart & skeletal muscle

26
Q

**Serotonin CV effects on 5TH3 receptor stimulation

A

Immediate Bradycardia

Immediate Vomiting

27
Q

*** Effect of serotonin on CV summary

A 
Vasoconstriction/ Vasodilation
Inc. contractility & heart rate
Incr. GI motility
Incr. blood viscosity
Incr. SV/ CO
Incr. PA pressure.
28
Q

Membrane bound 5-HT transporter does what

A

removes serotonin from plasma»stores in dense granules cells (protects from MOA degradation)
Once secreted, induces vasoconstriction

29
Q

5-HT2 receptors on platelets

A

enhances aggregation during bleeding

30
Q

5-HT4 receptors on GI tract

A

ACH release
Prokinetic effect
anti-emetic effects

31
Q

Too much serotonin causes

A

Anxiety, insomnia, Sexual dysfunction, GI disturbances, Seronoin syndrome»>death

32
Q

Too little serotonin causes

A

Bulimia, panic, OCD, and depression

33
Q

** Suicide receptor

A

5-HT2A

34
Q

Pharm management of depression

A

TCA
SSRI
MOA inhibitors
SNRIs
Noradrenergic & Specific Serotonergic Antidepressants (NaSSAs)
Norepinephrine Reuptake inhibitors (NRIs)
Norepinephrine Dopamine Reuptake Inhibitors (NDRIs)
Selective Serotonin Reuptake Enhancers (SSREs)
Melatonergic Agonists

35
Q

*TCAs- Reuptake inhibitors

A 
" ptyline, and pramine"
Amitriptyline
Doxepin
Imipramine
Clomipramine
Timipramine
36
Q
  • SSRIs- Reuptake inhibitors
A 
Prozac
luvox
Paxil
Zoloft
Celexa
Lexapro
  • sertraline (zoloft), and warfarin
  • inhibition of P450 system
  • beware of patients on 2 or more SSRIs
  • anticoagulants»incr. PT
  • other antidepressants
  • Lithium»CNS toxicity
  • Antivirals»increased SSRI levels
  • **Foods include: Banannas, kiwi, pineapple, plums, tomatoes incr. serotonin levels.
37
Q

*MAO inhibitors-Degradation inhibitors

A

Marplan
Nardil
Parnate
Selegiline

38
Q

Augmenter Drugs

A 
Buspar-agonist
Ariza-agonist
Sediel- agonist
Serzone-antagonist
Desyrel-antagonis
39
Q

*SNRIs- Reuptake inhibitors

A

Pristiq
Cymbalta
Effexor
Ixel

40
Q

NaSSAs

A

Tolvon

Remeron

41
Q

NRIs

A

Strattera
Mazanor
Edronax
Vivalan

42
Q

SSREs

A

Stablon
Coaxil
Tatinol

43
Q

Melatonergic Agonists

A

Valdoxan
Melitor
thymanax

44
Q

5-HT3 antagonists

A

“setron”

Block receptor and cause immediate relief from nausea

45
Q

5-HT1b & 5-HT 1d agonists

A

” Triptans”
Migrane regraine relief
*Contraindicated in CAD- Vasospasm

46
Q

5-HT 2b agonists

A

“fen”

Anti-obesity

47
Q

List the emetic centers in the brain that when ANTAGONIZED, decrease NAUSEA.

A

NTS- histamine, enkephalin, muscarinic
Area postrema (AP)- DA2, 5-HT3, opioid
CTZ- enkephalin, opioid, and DA2
NK 1- NK1 antagonist (Aprepitant) blocks substance P

48
Q

Apfel score establishes risk for

A

PONV

49
Q

What are the risk factors for PONV

A

PONV hx
female
nonsmoker
postop opioids

50
Q

5-HT3 antagonists & Dexamethasone

A

Most effective against PONV

  • Dose: zofran 4-8 mg: Dexam 8-10 mg adults
51
Q

Serotonin syndrome

A

Serotonin syndrome is a potentially life threatening drug reaction that causes the body to have too much serotonin
Serotonin syndrome most often occurs when two drugs that affect the body’s level of serotonin are taken together at the same time

52
Q

Signs & Symptoms of SS and Treatment

A 
Symptoms are progressive and include: 
Agitation or restlessness
Diarrhea
Fast heart beat and high blood pressure
Hallucinations
Increased body temperature
Loss of coordination
Nausea
Overactive reflexes
Rapid changes in blood pressure
Vomiting
Muscle rigidity
Tremor
Nystagmus
Myoclonus

TX: DC all Serotonergic drugs, Supportive

Pharmacology (27 decks)

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