Serotonin Agonist & Antagonists Flashcards Preview

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Flashcards in Serotonin Agonist & Antagonists Deck (52):
1

Serotonin has biologic effects on which systems

CV & Platelets
GI tract
CNS

2

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

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

3

Serotonin is synthesized from

L-tryptophan

4

L-tryptophan is obtained

in our diet

5

L-tryptophan is produced in what cells

enterochromaffin cells (intestines)
serotonergic neurons

6

True or False
L-tryptophan is NOT synthesized

True

7

L-tryptophan is stored

Enterochromaffin cells

Platelets

CNS

8

Does L-tryptophan cross the BBB

No; must be synthesized in CNS

9

How is L-tryptophan biosynthesized

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

10

What are the modulators of 5-HT brain levels

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

11

Serotonin is metabolised by what intracellular enzyme and what gland

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

Pineal gland (forms melatonin via N-acetylation)

12

Reuptake occurs

serotonin trasporters

in the liver, lung endothelial cells

platelet accumulation

13

Serotonin effects on the CNS

enchances release of CRH via hypothalamus
Regulates temperature

14

What 5-HT receptor antagonist improves memory

5-HT6 receptor

15

The 5-HT1 receptors are primarily located

Hippocampus, basal gangllia, raphe nuclei

Decreases anxiety

16

5-HT2A receptors cause

CNS hallucinations
platelet aggregation
peripheral smooth muscle contraction

17

5-HT2B receptors cause

endothelium smooth muscle relaxation
Gastric fundus smooth muscle contraction

18

5-HT2C receptors cause

decreased appetite

19

** 5-HT3 receptors cause

Nausea NOT vomiting (area post rema)
Gastric empyting

20

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

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

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

21

Ecstasy works by

blocking serotonin transporters thereby significantly raising serotonin levels

22

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

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

23

Serotonin's effect on bronchiolar smooth muscle

contraction

24

** Serotonin CV effect on 5-HT1 receptor stimulation

Vasodilation
inhibits NE release

25

**Serotonin CV effects of 5-HT2 receptor stimulation

Contraction of most smooth muscle (bronchi, bladder) but

vasodiation of heart & skeletal muscle

26

**Serotonin CV effects on 5TH3 receptor stimulation

Immediate Bradycardia

Immediate Vomiting

27

*** Effect of serotonin on CV summary

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

28

Membrane bound 5-HT transporter does what

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

29

5-HT2 receptors on platelets

enhances aggregation during bleeding

30

5-HT4 receptors on GI tract

ACH release
Prokinetic effect
anti-emetic effects

31

Too much serotonin causes

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

32

Too little serotonin causes

Bulimia, panic, OCD, and depression

33

** Suicide receptor

5-HT2A

34

Pharm management of depression

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

*TCAs- Reuptake inhibitors

" ptyline, and pramine"
Amitriptyline
Doxepin
Imipramine
Clomipramine
Timipramine

36

* SSRIs- Reuptake inhibitors

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

*MAO inhibitors-Degradation inhibitors

Marplan
Nardil
Parnate
Selegiline

38

Augmenter Drugs

Buspar-agonist
Ariza-agonist
Sediel- agonist
Serzone-antagonist
Desyrel-antagonis

39

*SNRIs- Reuptake inhibitors

Pristiq
Cymbalta
Effexor
Ixel

40

NaSSAs

Tolvon
Remeron

41

NRIs

Strattera
Mazanor
Edronax
Vivalan

42

SSREs

Stablon
Coaxil
Tatinol

43

Melatonergic Agonists

Valdoxan
Melitor
thymanax

44

5-HT3 antagonists

"setron"

Block receptor and cause immediate relief from nausea

45

5-HT1b & 5-HT 1d agonists

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

46

5-HT 2b agonists

"fen"
Anti-obesity

47

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

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

Apfel score establishes risk for

PONV

49

What are the risk factors for PONV

PONV hx
female
nonsmoker
postop opioids

50

5-HT3 antagonists & Dexamethasone

Most effective against PONV

* Dose: zofran 4-8 mg: Dexam 8-10 mg adults

51

Serotonin syndrome

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

Signs & Symptoms of SS and Treatment

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