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Pharm Fall '24 > Test 3 - Histamine, Serotonin and Depression > Flashcards

Test 3 - Histamine, Serotonin and Depression Flashcards

1
Q

What is the autocoid group for puritis? examples (4)

A

Released locally and act locally. biological substances that are released from the cell in response to variety of stimuli.
-histamine
-serotonin
-prostaglandins
-leukotrienes

(non neural)

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2
Q

The autacoid group can be _____ in neural tissues

A

neurotransmitters

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3
Q

In pruritis what induces the itch response?

A

the autacoid group

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4
Q

Pruritis can be _____ or _____

A

neuropathic or psychogenic

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5
Q

Histamine

A

mediator of allergic and inflammatory response

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6
Q

what are the effects of histamine on the nervous system?

A

Stimulates pain and itching via H1 and H3

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7
Q

Histamine release can be from a chemical response or a mechanical response. Give an example of each.

A

Chemical: morphine or tubocurarine causing itching

mechanical: damage to mast cells

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8
Q

What kind of receptors are Histamine receptors?

A

GCPR

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9
Q

H1 receptor subtype is located where?

A

smooth muscle, endothelium, brain. Gq

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10
Q

H2 receptor subtype is located where?

A

Gastric mucosa, cardiac muscle, mast cells, brain. Gs

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11
Q

H3 receptor subtype is located where?

A

presynaptic: brain, myenteric plexus, and other neurons. Gi

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12
Q

H4 receptor subtype is located where?

A

Esoinophils, neutrophils, CD4 T cells. Gi

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13
Q

Cardiovascular effects of histamine

A

decrease in BP - vasodilation
increase HR - reflex tachycardia (indirect response)

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14
Q

What are the effects seen with the Wheal and Flare - “Triple Response”

A

-injecting allergens that people might be allergic to
-the wheal is a positive test
-flare is the redness from capillary endothelium

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15
Q

What affect does histamine have in the stomach?

A

Secretory, stimulates release of hydrochloric acid

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16
Q

What effects does histamine have in the lungs?

A

Bronchoconstriction

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17
Q

Effects of histamine in the GI smooth muscle

A

contraction (peristalsis)

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18
Q

What are the two groups of H1 antihistamines?

A
  1. first generation
  2. second generation
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19
Q

First generation H1 antagonists effects

A

-sedative effects (crosses BBB)
-ANS blocking

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20
Q

Second generation H1 antagonists effects

A

more of a systemic reaction..less sedation (decreased CNS distribution)

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21
Q

Benadryl, dramamine and phenergan are examples of what?

A

First generation H1 antihistamines

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22
Q

Allegra, claritin and Zyrtec are all examples of what?

A

Second-generation H1 antihistamines

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23
Q

Biggest difference between first and second generation H1 antagonists

A

1st - sleepy
2nd - no sleepy

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24
Q

What are the effects of dramamine. what receptor?

A

H1 antagonist. first generation.
-sedation (resembles antimuscarinic drugs)
-antinausea/antiemetic

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25
Q

first generation H1 receptor antagonist toxicities

A

Sedation.
Anti-muscarinic effects (urinary retention, blurred vision)

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26
Q

Do we have the anti-muscarinic effects from H1 receptor or H2 receptor?

A

H1 receptor antagonist

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27
Q

Uses for H2 receptor antagonists

A

will shut down the production of hydrochloric acid in the stomach

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28
Q

Zantac, pepcid and tagamet are examples of what?

A

H2 receptor antagonists

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29
Q

H2 receptor antagonists have what effect?

A

shut down production of hydrochloric acid

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30
Q

H2 receptor antagonists, like zantac, have largely been replaced by what?

A

PPI’s

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31
Q

Histamine causes a _____ response while serotonin causes a ______ response

A

vasodilation
vasoconstriction

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32
Q

Serotonin causes what in the gut. how much is there?

A

peristalsis. 90%

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33
Q

Why is serotonin released?

A

Mast cell degranulation

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34
Q

describe serotonin and platelet clotting process

A

Vasoconstriction.
Serotonin is released via platelet degranulation. causing transient vasoconstriction due to the release of serotonin and that will give us time to form a clot so we don’t bleed out.

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35
Q

True/false: serotonin has a role in migraine headaches

A

True

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35
Q

Serotonin is stored or ______

A

rapidly inactivated

36
Q

serotonin effects in the brain? (10)

A
  1. mood
  2. sleep
  3. appetite
  4. temp regulation
  5. pain perception
  6. blood pressure
  7. vomiting
  8. depression
  9. anxiety
  10. migraines
37
Q

Primary place of serotonin production in the brain?

A

Raphe nuclei

38
Q

What is the parent compound for serotonin?

A

L-Tryptophan

39
Q

Serotonin is the parent compound for ______

A

melatonin

40
Q

If were not getting enough sunlight, we wont produce enough _____ and this can cause depression (think seasonal depression)

A

melatonin

41
Q

How many different 5-HT receptors are there

A

seven

42
Q

how many of the 7 are GPCR and how many are ion channel?

A

6 GPCR
1 Ion (5-HT 3)

43
Q

What is special about 5-HT3?

A

it is the only ion channel and it acts in an area in the brain to prevent nausea (ondansetron)

44
Q

Serotonin effects in the nervous system

A

-melatonin precursor
-vomiting reflex
-pain and itch response
-chemoreceptor reflex (bradycardia and hypotension)

45
Q

Serotonin effects in the respiratory system (2)

A

-Facilitate ACh release - constriction
-hyperventilation

46
Q

CV affects of serotonin

A

-contraction of vascular SM (not skeletal or heart)
-platelet aggregation

47
Q

Serotonin affects in the GI system

A

-increase tone
-facilitates peristalsis
-overproduction (diarrhea)
-Enteric nervous system (gut feeling)

48
Q

Two main 5-HT agonists targets

A
  1. 5-HT 1A (anxiety)
  2. 5-HT 1B/D (migraine)
49
Q

Two main 5-HT antagonists targets

A
  1. 5-HT2A
  2. 5-HT3 (antiemetic)
50
Q

Buspirone acts on which 5-HT receptor. what is it used for?

A

1A.
anxiety or OCD.
It is a non-benzodiazapine anxiolytic (wont make us sleepy)

51
Q

Sumatriptan works on which 5HT receptor? what is it used for?

A

5-HT 1D/1B agonist
migraine HA

52
Q

What can we use as pain relief for migraine (4)

A

ASA, NSAIDS, ASA+Caffeine, opiods

53
Q

Triptans are used to treat migraines. Which 5HT receptor does this act on? What does it do?

A

5-HT 1B/1D. Treats the aura as well as prevent dilation and stretching of pain endings

54
Q

What can be given as a preventative for migraines (6)

A
  1. glucocorticoids - prednisone
  2. beta blockers
  3. antidepressants
  4. anti-seizure
  5. botox
  6. MAbs
55
Q

Triptans for migraines are not _____

A

Prophylactic

56
Q

Triptans for migraines can cause what toxicity

A

Serotonin syndrome which is a hyperthermic reaction with excess amounts of serotonin.

57
Q

What are the three categories of hyperthermia disorders

A
  1. serotonin syndrom
  2. Neuroleptic malignant syndrome
  3. malignant hyperthermia
58
Q

Treatment for serotonin syndrome

A

sedation (benzo), paralysis, intubation, ventilation

59
Q

treatment for neuroleptic malignant syndrome

A

dihenhydramine

60
Q

treatment for malignant hyperthermia

A

dantrolene

61
Q

What are some drugs that can induce serotonin syndrome?

A

Anything that increases serotonin

  1. SSRI
  2. MAOI
  3. sumatriptan
  4. MDMA (molly)
  5. St Johns wort
62
Q

What can cause neuroleptic malignant syndrome

A

D2 blocking antipsychotics

63
Q

what can cause malignant hyperthermia?

A

ryanodine receptor stays open for longer. volatile anesthetics, succinylcholine

64
Q

Serotonin and weight loss

A

used to be used for weight loss but no longer used

65
Q

Phenoxybenzamine and cyproheptadine work on which 5-HT receptor?

A

5-HT2 antagonist

66
Q

Ondansetron works on what 5-HT

A

5-HT3 antagonists. ion channel. prevent N/V

67
Q

dopamine mesolimbic pathway

A

reinforcement and addiction.

68
Q

What is DAT?

A

dopamine reuptake transporter

69
Q

women in regards to depression and anxiety

A

women are affected twice as often as men by both

70
Q

Depression is ____ energy. Anxiety is _____ energy

A

lack of
abundance of

71
Q

major types of depression (5)

A
  1. dysthymia (overall depression)
  2. psychosis
  3. postpartum
  4. seasonal
  5. bipolar
72
Q

major types of anxiety (4)

A
  1. generalized
  2. OCD
  3. PTSD
  4. social phobia
73
Q

Four categories of antidepressant medications

A
  1. SSRI (selective serotonin reuptake inhibitor)
  2. SNRI (selective serotonin-NE reuptake inhibitor
  3. TCA (Tricyclic antidepressants)
  4. MAOI (monoamine oxidase inhibitors) (WE WANT TO AVOID THESE - severe side effects)
74
Q

The pharmacology for all antidepressant medications is that they all …

A

increase monoamine neurotransmitter levels within the synapse

75
Q

Prozac, celexa, paxil, zoloft and lexapro are examples of what?

A

SSRI

76
Q

How do SSRI work?

A

inhibit SERT. allow serotonin to be in the synapse for longer.

77
Q

Cymbalta and Pristique are what class of drugs? how do they work?

A

SNRI. Inhibit SERT and NET useful for more severe depression

78
Q

Amitriptyline is an example of what? how does it work

A

TCA. Inhibit SERT, NET and some anticholinergic effects

79
Q

uses and adverse effects of MAOI’s

A

refractory depression.
lethal drug interactions (CNS and PNS)

80
Q

What bad side effect do all antidepression meds have in common?

A

suicidal ideation (first 1-2 months)

81
Q

SERT

A

reuptake system for serotonin

82
Q

MOA for MAOI’s

A

work on the enzyme in the presynaptic cell to inhibit the breakdown of serotonin, dopa and norepi

83
Q

Other meds for depression

A
  1. NDRI (keep us awake)
  2. benzo (very sleepy)
  3. antipsychotics
84
Q

True/false: All of the antidepressants mentioned have a black box warning

A

true

85
Q

Alternative treatments for depression

A
  1. psychotherapy - “talk therapy”
  2. electroconvulsive therapy
  3. St Johns wort
86
Q

What are the enterochromaffin cells? how do they relate to serotonin?

A

They are the cells that line the GI tract. 90% of serotonin is stored there

87
Q

Adverse effects for antidepressants

A

-black box warning
1. drug interactions
2. N/V/D
3. sexual disfunction

88
Q

pharmacokinetics for antidepressants

A

good bioav
plasma protein binding
liver M
renal CL

Pharm Fall '24 (7 decks)

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