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Pharm 2024 > Histamine, serotonin, depression > Flashcards

Histamine, serotonin, depression Flashcards

Exam 3

1
Q

What are the mediators in the autocoid group?

A

Histamine, serotonin, prostaglandins, leukotrienes

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2
Q

_____ is the mediator of allergic and inflammatory response

A

histamine

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3
Q

Histamine is released in response to what?

A
  1. Allergen binding to IgE on mast cells
  2. Displacement – morphine, tubucurarine
  3. Rupture of mast cells (mechanical)
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4
Q

Where are histamine H1 receptors located?

A

smooth muscle, endothelium, brain

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5
Q

Where are histamine H2 receptors located?

A

GI, cardiac muscle, mast cells, brain

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6
Q

Where are histamine H3 receptors located?

A

brain

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7
Q

Where are histamine H4 receptors located?

A

eosinophils, neutrophils, CD4 T cells

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8
Q

What are the 3 components of the triple response of allergy testing?

A

1- Wheal/welt development
2- flare/redness
3- Sensory nerve ending activation/itching

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9
Q

What is the physiologic antagonist of histamine?

A

Epinephrine

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10
Q

Differentiate between H1 antagonists, 1st vs 2nd gen

A

1st generation
- Sedative effects
- ANS blocking
- motion sickness, nausea
2nd generation
- Less sedation (↓ CNS distribution, doesn’t cross BBB)

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11
Q

What is the clinical use of H1 antagonists?

A

Prevent/treat symptoms of allergic response - Allergic rhinitis, urticaria

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12
Q

Why does morphine cause itching?

A

Histamine release

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13
Q

Histamine is released after __________ degranulation

A

mast cell

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14
Q

Which histamine receptors stimulate pain and itching?

A

H1 and H3

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15
Q

What histamine receptors are located in the stomach?

A

H2

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16
Q

Anti-muscarinic effects are more noted in the 1st generation or 2nd generation antihistamines?

A

1st generation (urinary retention and blurred vision)

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17
Q

Histamine effect on GI smooth muscle

A

contraction

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18
Q

Histamine effect on on CV system

A

vasodilation - decreases BP
reflex tachycardia

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19
Q

Histamine effect on on respiratory system

A

Bronchoconstriction

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20
Q

What are the 3 drugs that are 1st gen H1 antagonists?

A

Bendryl, Phenergan, Dramamine

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21
Q

What are the 3 drugs that are 2nd gen H1 antagonists?

A

Claritin, Allegra, Zyrtec

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22
Q

What class of drugs are OTC antacids?

A

H2 antagonists

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23
Q

Where is serotonin produced?

A

Raphe nuclei

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24
Q

Where is most of the serotonin stored in the body?

A

Gut - Enterochromaffin cells (90% of serotonin in body)

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25
Q

Serotonin effect on CV

A
  • Contraction of vascular SM
    • Exception: skeletal muscle, heart
  • Platelet aggregation
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26
Q

Serotonin effect on GI

A
  • Increases tone
  • Facilitates peristalsis
  • Overproduction - diarrhea
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27
Q

Serotonin effect on respiratory

A
  • Facilitate ACh release - constriction
  • Hyperventilation
28
Q

Serotonin effect on nervous system

A
  • Melatonin precursor
  • Vomiting reflex
  • Pain and itch (similar to histamine)
  • Chemoreceptor reflex
    • Bradycardia
    • Hypotension
29
Q

Which serotonin receptor is an ion channel?

A

5-HT3
- the other 6 are GPCRs

30
Q

Which serotonin receptors are agonist targets?

A

1A, 1B, 1D

31
Q

Which serotonin receptors are antagonist targets?

A

2A and 3

32
Q

What are the 2 serotonin agonist drugs? Which receptors do they target? What do they treat?

A
  1. Buspirone
    - 5-HT1A agonist (partial)
    - Non-benzodiazapine anxiolytic - no drowsiness
    - GAD, OCD
  2. Sumatriptan
    - 5-HT1D/1B agonist
    - Migraine HA
33
Q

What are the known components that contribute to migraines?

A

CGRP, Substance P, trigeminal nerves

34
Q

What are the symptoms of migraines?

A
  • Aura
  • Severe HA
  • N/V
  • Photophobia
  • Phonophobia
  • Speech abnormalities
35
Q

What are the 5 meds used for migraine treatment?

A
  1. Pain relief – ASA, NSAIDs, ASA+Caffeine, Opioids
  2. Triptans – 5-HTr Agonists
  3. Ergotamine – less effective than triptans
  4. Anti-nausea – chlorpromazine, ondansetron
  5. Glucocorticoids - prednisone
36
Q

How do triptans treat migraines?

A
  • Bind 5-HT1D/1B in cranial blood vessels
  • Prevent dilation and stretching of pain endings
  • Not prophylactic
37
Q

What are the drugs used to prevent migraines?

A
  1. Beta-blockers, CCBs, ACEi
  2. Antidepressants – SSRIs, TCAs
  3. Anti-seizure – Valproate, Topiramate
  4. Botox
  5. MAbs - Aimovig (CGRP)
38
Q

What are the 3 hyperthermic syndromes?

A
  1. Serotonin syndrome
  2. Neuroleptic malignant syndrome
  3. Malignant hyperthermia
39
Q

What are the non-serotonin drugs used for weight loss?

A
  • Liraglutide – GLP-1 agonist (diabetes)
  • Orlistat – GI Lipase inhibitor
40
Q

What drugs can cause serotonin syndrome?

A

Antidepressants (SSRIs, SNRIs, MAOIs), opioids, illicit drugs, St. John’s wort, ginseng

41
Q

What is the treatment for serotonin syndrome?

A

Sedation (benzos), paralysis, intubation, and ventiliation

42
Q

What drugs can cause neuroleptic malignant syndrome?

A

D2-blocking antipsychotics

43
Q

How is neuroleptic malignant syndrome treated?

A

Parenteral Benadryl (diphenhydramine)
cooling, sedation (benzos)

44
Q

What drugs can cause malignant hyperthermia?

A

Volatile anesthetics, sux

45
Q

What is the treatment for malignant hyperthermia?

A

Dantrolene, cooling

46
Q

What are the 3 drugs classified as serotonin antagonists? What receptors do they act at? What is their clinical use?

A

Phenoxybenzamine, Cyproheptadine
- 5-HT2
- Carcinoid tumors
- Cold induced urticaria

Ondansetron
- 5-HT3
- Prevent N/V for Surgery and CA chemotherapy

47
Q

Dopamine is a _____ derivative

A

tyrosine

48
Q

What are the dopamine receptors?

A

5 receptor types (D1–D5, all metabotropic)

49
Q

What are the 3 major dopamine pathways?

A
  1. Nigrostriatal - Motor movement
  2. Mesolimbic - Reinforcement and Addiction
  3. Mesocortical - Working memory and planning
50
Q

What are the 5 types of depression?

A
  • Dysthymia
  • Psychosis
  • Postpartum
  • Seasonal affective disorder (SAD)
  • Bipolar disorder
51
Q

What are the 4 types of anxiety?

A
  • Generalized Anxiety Disorder (GAD)
  • Obsessive-Compulsive Disorder (OCD)
  • Post-Traumatic Stress Disorder (PTSD)
  • Social Phobia
52
Q

What are the 4 major classes of antidepressants?

A
  1. Selective serotonin reuptake inhibitors (SSRIs)
  2. Selective serotonin-NE reuptake inhibitors (SNRIs)
  3. Tricyclic antidepressants (TCAs)
  4. Monoamine oxidase inhibitors (MAOIs)
53
Q

All antidepressant’s increase _______ NT levels within the synapse

A

monoamine

54
Q

SSRIs inhibit ______

A

SERT

55
Q

SNRIs inhibit ____

A

SERT and NET

56
Q

TCAs inhibit _____

A

Inhibit SERT, NET, some anticholinergic effects

57
Q

SSRI drugs

A

Fluoxetine (Prozac)
Sertraline (Zoloft)

58
Q

SNRI drugs

A

Desvenlafaxine (Pristique)
Duloxetine (Cymbalta)
- More severe depression and pain disorders

59
Q

TCA drug

A

Amitriptyline (Elavil)

60
Q

MAOIs are used to treat _______ but are rarely used due to _____

A

Refractory depression, unresponsive to others
Lethal drug interactions

61
Q

What are the adverse effects of antidepressants?

A

Suicidal, drug interactions, N/V/D, Sexual dysfunction

62
Q

Serotonin is a derivative of _______

A

tryptophan

63
Q

What are the serotonin drugs that are no longer used for weight loss?

A

(Dex)Fenfluramine - 5-HT2 agonist
Lorcaserin – 5-HT2C agonist

64
Q

What are the alternative therapies for anxiety and depression?

A

St. John’s Wort, Talk therapy, Electroconvulsive

65
Q

What are NDRIs? What are the drugs given in class and what do they treat?

A
  • Buproprion (Wellbutrin), Solriamfetol (Sunosi)
  • Inhibits NE and DA reuptake
  • Depression, ADHD, GAD, daytime sleepiness
66
Q

What are the antipsychotics? What are their uses?

A

Major depression (with SSRIs)
Aripiprazole (Abilify)
Amisulpride - Schizophrenia
- D2 receptor antagonist

67
Q

If your patient has a history of Prinzmetal angina then they should not take ______ for their migraines

A

Sumatriptan

Pharm 2024 (28 decks)

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