Exam 3 - Histamine, Serotonin, Dopamine Flashcards

1
Q

What is autocoid transmission? What are some autocoids?

A

Endogenous chemicals that cause brief local effects like itching when in non-neural tissue: histamine, serotonin, prostaglandins, leukotrienes

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2
Q

What are the effects of histamine in the nervous system? What receptors are involved?

A

Stimulates pain and itching via H1 and H3 receptors

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3
Q

What are the effects of histamine in the cardiovascular system?

A

Decreases BP via vasodilation which causes reflexive tachycardia

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4
Q

What are the effects of histamine in the stomach, lungs and GI system?

A

Stomach - secretion of HCl
Lungs - bronchoconstriction
GI smooth muscle - contraction

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5
Q

Describe the effects seen in the Triple Response? What mediator causes this?

A

Also called “Wheal and Flare”
* Causes a wheal to form that increases in size with allergens the patient is sensitive to
* Also causes a flare, redness around the wheal, caused by capillary enodthelium inflammation-vasodilation.
* Sensory nerve endings are also activated leading to itchiness
* Histamine

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6
Q

What are serotonin’s effects in the nervous system?

A
  • Precursor to melatonin
  • Vomiting reflex mediated in the area postrema
  • Pain and itch
  • Chemoreceptor reflex = bradycardia and hypotension
  • Large effect on mood and mood disorders
  • Migraines
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7
Q

What is serotonin’s effects in the respiratory system?

A
  • Facilitates ACh release leading to bronchoconstriction
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8
Q

What is serotonin’s effects in the cardiovascular system?

A
  • Contraction of vascular smooth muscle (not heart or skeletal)
  • Leads to platelet aggregation
    Released initially during bleeding to constrict blood vessels while clotting cascade is starting.
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9
Q

What is serotonin’s effects in the GI system?
What is important to know about serotonin production here?

A
  • Increaes tone
  • Facilitates peristalsis
  • In excess causes diarrhea
    90% of serotonin in the body is in the enterochromaffin cells
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10
Q

How do H1 antagonists work? What is their indication?

A
  • Antagonize H1 receptors in the smooth muscle, endothelium, and brain - resemble antimuscarincs
  • Prevention and treatment of allergic response and motion sickness
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11
Q

What are the 1st generation H1 antagonists and their effects?

A

These all can cross the BBB and cause drowsiness and generate anti-cholinergic activity

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12
Q

What are the 2nd generation H1 antagonists and their effects?

A

Do not cross the BBB, have much less drowsiness associated with them

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13
Q

What are the major differences between 1st and 2nd generation H1 antagonists?

A

2nd generation do not cross the blood brain barrier and do not cause much drowsiness or produce anticholinergic effects.

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14
Q

What are the uses for H2 antagonists?
Compare them to PPIs?
What are 2 drugs in this class?

A
  • Treatment for indigestion by inhibition of HCl secretion
  • PPI’s are more effective like nexium and omeprazole
  • Rantidine (Zantac) and famotidine (Pepcid)
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15
Q

What is the source for serotonin in the brain?

A

Raphe nuclei in the brainstem

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16
Q

What are the 3 main 5-HT agonist targets and the drugs that affect them?

A

5-HT1A – Buspirone
5-HT1D/1B - Sumatriptan

17
Q

What are the 2 main 5-HT antagonsist targets and the drugs in this class?

A

5-HT2A – Phenoxybenzamine, Cyproheptadine
5-HT3 (only ion channel serotonin receptor)- Ondansetron

18
Q

What are the 4 main treatments for a migraine and it’s affects?

A
  1. Pain relief: ASA, NSAIDS, caffeine, opiods
  2. Triptans - block 5HT1B/1D
  3. Ergotamine - alpha 1 agonist, less effective than triptans
  4. Anti-emetics - chlorpromazine, ondansetron
19
Q

What are the 6 main preventatives for a migraine?

A
  1. Sympatholytics: BB, CCB, ACEi
  2. Antidepressants - SSRI, TCA
  3. Anti-seizures: valproate, topiramate
  4. Botox
  5. MAB’s - Aimovig, anti CGRP
  6. Glucocorticoids - prednisone

“BAM, GAS!”

20
Q

What is the indication and MOA of sumatriptan?

A
  • Treatment of migraine headaches
  • 5-HT1B/1D agonist in cranial blood vessels that prevents dilation and stretching of pain endings
21
Q

What are the 3 hyperthermia disorders?
What causes them?
What are the treatments?

A

Serotonin syndrome:
1. Caused by excess serotonin from a long list of drugs that increase amount of serotonin at the synapse
2. Treatment is sedation with benzos, paralysis, and intubation/ventilation
Neuroleptic malignant syndrome:
1. Caused by dopamine blocking antipsychotics
2. Treatment is IV benadryl
Malignant hyperthermia
1. Caused the RyR being open for a long time causing muscle rigidity (volatile anesthetics, succinylcholine)
2. Treatment is Dantrolene

22
Q

What dopaminergic pathway leads to reinforcement and addiction?

A

The mesolimbic pathway

23
Q

What are the differences between anxiety and depression? List some of the different types.

A

Depression is considered a low energy state, while anxiety is considered a high energy state.
Depression: dysthymia (long lasting depression). psychosis, postpartum, SAD, bipolar
Anxiety: Generalized anxiety disorder, OCD, PTSD, social phobia

24
Q

List the 4 categories of antidepressant medications in order of treatment severity (low to high)?

A
  1. SSRI
  2. SNRI
  3. TCA
  4. MAOI
25
Q

What is the MOA of TCA? Name a drug in this class?

A

Inhibits SERT, NET, and some anticholinergic effects
Ex: Amitriptyline (Elavil)

26
Q

What is the MOA of MAOIs?
What are some adverse effects?

A
  • Targets MAO-A, MAO-B, or both
  • Can be irreversible (Nardil)
  • Has many lethal drug an food interactions, as well as many harmful side effects
27
Q

What is the MOA of SSRIs?
What are some drugs in this class?

A
  • Inhibits SERT
  • Prozac, Celexa, Paxil, Zoloft, Lexapro
28
Q

What is the MOA of SNRI’s?
List the drugs in this category.

A
  • Inhibits SERT and NET
  • Useful for depression and pain disorders
  • Pristique and Cymbalta
29
Q

Describe the MOA of NDRI’s, drugs in this class, and their uses?

A
  • Inhibits NE and dopamie reuptake
  • Wellbutrin and Sunosi
  • Depression, ADHD, GAD, Daytime sleepiness
30
Q

What are alternative therapies to depression?

A
  • Benzos
  • Antipsychotics
  • Psychotherapy
  • Electroconvulsive therapy
  • St. Johns Wort (top selling botanical in US)