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Pharmacology > Serotonin Agonist & Antagonists > Flashcards

Serotonin Agonist & Antagonists Flashcards

(52 cards)

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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

Study These Flashcards
A

blocking serotonin transporters thereby significantly raising serotonin levels

22
Q

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

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A

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

23
Q

Serotonin’s effect on bronchiolar smooth muscle

24
Q

** Serotonin CV effect on 5-HT1 receptor stimulation

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A

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

Pharmacology (27 decks)

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