Histamine, Serotonin Flashcards

Test 3

1
Q

Describe autocoid transmission

A

local release and action of mediators like histamine, serotonin, prostaglandins, and leukotrienes

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2
Q

Describe Neuropathic vs psychogenic pruitis

A

Neuropathic: autacoid group binding to receptor

Psychogenic: thinking about itching makes you itch

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3
Q

Histamine is ________ stored & inactivated

A

rapidly

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4
Q

What do histamine receptors in the stomach produce?

A

Hydrochloric acid

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5
Q

What drugs induce histamine release?

A

Morphine
Tubocurarine

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6
Q

_____ can induce histamine release

A

trauma

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7
Q

Where are H1, H2, H3 receptors

A

H1 - blood vessels
H2 - stomach
H3 - brain

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8
Q

List the major organ system effects of histamine and serotonin.

A

Histamine: CVS: vasodilation & increased permeability
Respiratory: bronchoconstriction
GI: stimulating gastric acid secretion

Serotonin: CNS: regulating mood, sleep, and appetite
CVS: vasoconstriction/dilation
GI: promoting peristalsis

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9
Q

List the effects seen in the Triple Response of allergy testing and mediators.

A

** injecting small amounts of allergens to see what has a positive reaction**

Redness (due to capillary dilation)

Flare (a wider area of redness due to arteriolar dilation)

Wheal (a raised area due to increased vascular permeability) Mediators involved include histamine and other inflammatory substances

Itch

These are mediated by the release of histamine and other inflammatory mediators from mast cells.

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10
Q

List H1 antagonist

A

1st generation: Benadryl, phenergan, dramamine (crosses BBB - sedative effects - can be used for nausea)

2nd: Claritin, allegra, zyrtec (no CNS effects)

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11
Q

What drug counters histamine but not on the H-Receptors?

A

Epi

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12
Q

List H2 antagonists

A

OTC antacids

-dine

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13
Q

Children may have _______ effects with H1 antagonist

A

reverse

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14
Q

T/F: Platelet degranulation releases serotonin

A

T

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15
Q

Where is most of our serotonin stored?

A

90% stored in enterochromaffin cells in the gut

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16
Q

Describe the pharmacology of the 2 groups of H1 antihistamines and list prototypical agents for each group

A

a. First generation (sedating): Cross blood-brain barrier, have anticholinergic effects.

i. Prototypes include diphenhydramine (Benadryl) and chlorpheniramine.

b. Second generation (non-sedating): Do not cross blood-brain barrier as readily, fewer anticholinergic effects.

i. Prototypes include cetirizine (Zyrtec) and loratadine (Claritin).

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17
Q

Where is serotonin produced in the brain?

A

raphe nuclei

18
Q

Serotonin is a derative of _________. and _____________ is a derative of serotonin

A

tryptophan

melatonin

19
Q

What does increase in 5-HIAA in stool indicate?

A

tumor that is overproducing 5-HT vs infection causing diarrhea

20
Q

List the uses of the H2 antihistamines, contrast PPIs, and name 2 members of this group.

A

H2 antihistamines reduce gastric acid secretion in conditions like peptic ulcers and gastroesophageal reflux disease (GERD).

PPIs: Proton pump inhibitors (PPIs), (e.g. omeprazole) are more effective at reducing gastric acid secretion and have a longer duration of action compared to H2 antihistamines.

21
Q

Describe serotonin effects in neural and non-neural tissues.

A

a. Neural: In the brain, serotonin regulates mood, anxiety, and sleep

i. Appetite, pain, itch can also be affected

b. Non-neural: Platelet aggregation, vasoconstriction, gastrointestinal motility

i. Remember, SERO (Serum) TONIN (tone) so vessel tone is how it received its name originally

22
Q

Describe the serotonin receptors

A

5-HT 1-7

All are GPCRs except 5-HT3 which is an ion channel

23
Q

What Serotonin receptor is associated with nausea? where is it located?

A

5-HT3

postrema in the brain

24
Q

List the source of serotonin in the brain, three main 5-HT agonist targets, two main 5-HT antagonist targets, and drugs in each category.

A

a. Serotonin in the brain is primarily produced in the raphe nuclei.

b. Main 5-HT agonist targets:
i. 5-HT1A e.g. buspirone (anxiety)
ii. 5-HT1B/1D e.g. sumatriptan (migraine)
iii. 5-HT2 e.g. Phenoxybenzamine (platelet aggregation, smooth muscle)

c. Main 5-HT antagonist targets:
i. 5-HT3 e.g. ondansetron (nausea/vomiting)

25
Q

Compare and contrast preventatives and treatments for migraine headache

A

Preventatives: beta blockers, CCB, antidepressants, anti-seizure medications, and CGRP monoclonal antibodies, glucocorticoids (prednisone), botox

Tx: Triptans (sumatriptan), NSAIDs (ibuprofen), ergots (ergotamine and dihydroergotamine), and antiemetics (metoclopramide)

26
Q

Describe the action and indication for the use of sumatriptan.

A

5-HT1B/1D agonist used migraines

vasoconstriction of cranial blood vessels and block pain signaling to treat the headache and associated symptoms.

27
Q

what neurotransmitters are associated with migraines?

A

CGRP
Substance P
Trigeminal nerves

28
Q

What effect does St. John warts have on serotonin levels?

A

increases them

29
Q

List the three categories of hyperthermia disorders, contributing factors, and treatments.

A

Serotonin Syndrome: triggered by serotonergic medications = SSRIs, MAOIs, and certain recreational drugs; serotonin excess
-Tx: Benzodiazepine, paralyze, intubate

Neuroleptic Malignant Syndrome: associated with antipsychotic medications, particularly those that block dopamine receptors.
Tx: Diphenhydramine IV, cooling

Malignant Hyperthermia: triggered by certain anesthetic agents, such as succinylcholine and volatile anesthetics
Tx: Dantrolene, cooling

30
Q

dopamine is a derivative of ________

A

tyrosine

31
Q

Describe the Dopamine receptors

A

D1-5
Located all over body
All metabotropic
D1 is postsynaptic
D2-5 are autoreceptors and postsynaptic

32
Q

Recall the dopamine mesolimbic pathway for reinforcement of behaviors.

Vs Nigrostriatal and Mesocortical

A

pathway associated with reinforcement and reward in the brain

Plays a role in addiction/negative and positive reinforcement of behaviors

Nigrostriatal- movement

Mesocortical- memory/planning

33
Q

Depression is ______ energy; anxiety is ________

A

lack of energy

excess of energy/worrying

34
Q

Differentiate between anxiety and depression, and list major types of each.

A

Depression: dysthmia, psychosis, postpartum, seasonal, bipolar

Anxiety: generalized, obsessive- compulsive, PTSD, Social phobia

35
Q

List the four categories of antidepressant medications in order of treatment severity.

A

Selective serotonin reuptake inhibitors (SSRIs)
Serotonin-norepinephrine reuptake inhibitors (SNRIs)
Tricyclic antidepressants (TCAs)
Monoamine oxidase inhibitors (MAOIs)

36
Q

List SSRI

A

Inhibit SERT (Serotonin transporter)

Fluoxetine (Prozac)
Sertraline (Zoloft)

37
Q

List SNRI

A

Inhibit SERT and NET (Serotonin&NE transporter)

Cymbalta
Pristique

38
Q

List Tricyclic Antidepressants

A

inhibit SERT, NET, and anticholinergic effects

Elavil

39
Q

List Monoamine oxidase inhibitors

A

MAOIs

inhibit all transporters; rarely used
LETHAL DRUG INTERACTIONS

Nardil - irreversible
Selegiline

40
Q

List alternative therapies for depression.

A

-psychotherapy
-lifestyle changes
-electroconvulsive therapy
-light therapy for seasonal affective disorder
-herbal supplements: St. John’s Wort.

41
Q

What is the major black box warning on all antidepressant?

A

Can cause suicidal ideation within the first 1-2 months of taking, especially in adolescence