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Pharm 2024 > Histamine, serotonin, depression > Flashcards

Histamine, serotonin, depression Flashcards

Exam 3 (67 cards)

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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
Serotonin effect on CV
- Contraction of vascular SM - Exception: skeletal muscle, heart - Platelet aggregation
26
Serotonin effect on GI
- Increases tone - Facilitates peristalsis - Overproduction - diarrhea
27
Serotonin effect on respiratory
- Facilitate ACh release - constriction - Hyperventilation
28
Serotonin effect on nervous system
- Melatonin precursor - Vomiting reflex - Pain and itch (similar to histamine) - Chemoreceptor reflex - Bradycardia - Hypotension
29
Which serotonin receptor is an ion channel?
5-HT3 - the other 6 are GPCRs
30
Which serotonin receptors are agonist targets?
1A, 1B, 1D
31
Which serotonin receptors are antagonist targets?
2A and 3
32
What are the 2 serotonin agonist drugs? Which receptors do they target? What do they treat?
1. Buspirone - 5-HT1A agonist (partial) - Non-benzodiazapine anxiolytic - no drowsiness - GAD, OCD 2. Sumatriptan - 5-HT1D/1B agonist - Migraine HA
33
What are the known components that contribute to migraines?
CGRP, Substance P, trigeminal nerves
34
What are the symptoms of migraines?
- Aura - Severe HA - N/V - Photophobia - Phonophobia - Speech abnormalities
35
What are the 5 meds used for migraine treatment?
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
How do triptans treat migraines?
- Bind 5-HT1D/1B in cranial blood vessels - Prevent dilation and stretching of pain endings - Not prophylactic
37
What are the drugs used to prevent migraines?
1. Beta-blockers, CCBs, ACEi 2. Antidepressants – SSRIs, TCAs 3. Anti-seizure – Valproate, Topiramate 4. Botox 5. MAbs - Aimovig (CGRP)
38
What are the 3 hyperthermic syndromes?
1. Serotonin syndrome 2. Neuroleptic malignant syndrome 3. Malignant hyperthermia
39
What are the non-serotonin drugs used for weight loss?
- Liraglutide – GLP-1 agonist (diabetes) - Orlistat – GI Lipase inhibitor
40
What drugs can cause serotonin syndrome?
Antidepressants (SSRIs, SNRIs, MAOIs), opioids, illicit drugs, St. John's wort, ginseng
41
What is the treatment for serotonin syndrome?
Sedation (benzos), paralysis, intubation, and ventiliation
42
What drugs can cause neuroleptic malignant syndrome?
D2-blocking antipsychotics
43
How is neuroleptic malignant syndrome treated?
Parenteral Benadryl (diphenhydramine) cooling, sedation (benzos)
44
What drugs can cause malignant hyperthermia?
Volatile anesthetics, sux
45
What is the treatment for malignant hyperthermia?
Dantrolene, cooling
46
What are the 3 drugs classified as serotonin antagonists? What receptors do they act at? What is their clinical use?
Phenoxybenzamine, Cyproheptadine - 5-HT2 - Carcinoid tumors - Cold induced urticaria Ondansetron - 5-HT3 - Prevent N/V for Surgery and CA chemotherapy
47
Dopamine is a _____ derivative
tyrosine
48
What are the dopamine receptors?
5 receptor types (D1–D5, all metabotropic)
49
What are the 3 major dopamine pathways?
1. Nigrostriatal - Motor movement 2. Mesolimbic - Reinforcement and Addiction 3. Mesocortical - Working memory and planning
50
What are the 5 types of depression?
- Dysthymia - Psychosis - Postpartum - Seasonal affective disorder (SAD) - Bipolar disorder
51
What are the 4 types of anxiety?
- Generalized Anxiety Disorder (GAD) - Obsessive-Compulsive Disorder (OCD) - Post-Traumatic Stress Disorder (PTSD) - Social Phobia
52
What are the 4 major classes of antidepressants?
1. Selective serotonin reuptake inhibitors (SSRIs) 2. Selective serotonin-NE reuptake inhibitors (SNRIs) 3. Tricyclic antidepressants (TCAs) 4. Monoamine oxidase inhibitors (MAOIs)
53
All antidepressant's increase _______ NT levels within the synapse
monoamine
54
SSRIs inhibit ______
SERT
55
SNRIs inhibit ____
SERT and NET
56
TCAs inhibit _____
Inhibit SERT, NET, some anticholinergic effects
57
SSRI drugs
Fluoxetine (Prozac) Sertraline (Zoloft)
58
SNRI drugs
Desvenlafaxine (Pristique) Duloxetine (Cymbalta) - More severe depression and pain disorders
59
TCA drug
Amitriptyline (Elavil)
60
MAOIs are used to treat _______ but are rarely used due to _____
Refractory depression, unresponsive to others Lethal drug interactions
61
What are the adverse effects of antidepressants?
Suicidal, drug interactions, N/V/D, Sexual dysfunction
62
Serotonin is a derivative of _______
tryptophan
63
What are the serotonin drugs that are no longer used for weight loss?
(Dex)Fenfluramine - 5-HT2 agonist Lorcaserin – 5-HT2C agonist
64
What are the alternative therapies for anxiety and depression?
St. John’s Wort, Talk therapy, Electroconvulsive
65
What are NDRIs? What are the drugs given in class and what do they treat?
- Buproprion (Wellbutrin), Solriamfetol (Sunosi) - Inhibits NE and DA reuptake - Depression, ADHD, GAD, daytime sleepiness
66
What are the antipsychotics? What are their uses?
Major depression (with SSRIs) Aripiprazole (Abilify) Amisulpride - Schizophrenia - D2 receptor antagonist
67
If your patient has a history of Prinzmetal angina then they should not take ______ for their migraines
Sumatriptan

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