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Pharmacology Test 4 > Chapter 16: Histamine, Serotonin, Depression > Flashcards

Chapter 16: Histamine, Serotonin, Depression Flashcards

1
Q

Histamines, serotonins, prostaglandins, and leukotrienes are part of what group?

A

Autacoid Group

NT in the non-neural tissues

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2
Q

What is a key characteristic the autacoid group is responsible for?

A

Pruritis (Itchiness)- can be neuropathic or psychogenic (just the thought of being itchy)

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3
Q

What are the two main mediators of the itch response?

A

Histamine and Serotonin

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4
Q

What is a mediator of allergic inflammatory response that stimulate pain, itiching?***

A

Histamine

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5
Q

What amino acid is histamine from?

A

Histidine

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6
Q

Where is the primary storage of vesicles filled with histamine?***

A

The mast cells - these are the cells that degranulate during an allergic response.

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7
Q

Besides the mast cells where are two other sources of histamine?***

A

Brain (neurotransmitter)
Stomach (control acid release)

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8
Q

What type of histamine receptors are in the periphery?***

What about the stomach?***

A

Histamine Type 1 Receptor

Histamine Type 2 Receptor in the stomach.

*All histamine receptors are GPCRs

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9
Q

Where is Histamine Type 1 receptor located?***

A

Smooth muscle (dilation of vascular smooth muscle)

Periphery

Endothelium (becomes more leaky)

Brain

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10
Q

Where is Histamine Type 2 receptor located?***

Where is Histamine Type 3 receptor located?

Where is Histamine Type 4 receptor located?

A

Stomach (H2 receptor)

Brain (H3 receptor)

WBC (H4 receptor)

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11
Q

What are the cardiovascular effects of histamine?***

A

Decrease in BP d/t vasodilation

Increase in HR d/t reflex tachycardia and partially because there are H2 receptors on the heart.

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12
Q

What autocoid hormone can cause vasoconstriction?

A

Serotonin

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13
Q

What is the Wheal (Welt) and Flare “Triple Response”?***

A

A patient has been inoculated with different compounds for allergy testing.

Three components involved
1. Microcirculation smooth muscle (becomes leaky)
2. Capillary endothelium (leaky)
3. Sensory nerve endings (flare)

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14
Q

Histamine can produce secretory effects in the stomach which can lead to ______.

A

Diarrhea

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15
Q

What effects does histamine produce in the lungs?**

What does histamine do to Gi smooth muscles?

A

Bronchoconstriction

Contraction (movement of food)

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16
Q

What is a physiological reversal of histamine effects?

A

Epinephrine working alpha 1 receptors to constrict blood vessels.

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17
Q

What are the two categories of histamine-1 receptor antagonist drugs?***

What is the clinical use of antihistamines?

A

First generation (Sedative effects and ANS blocking-Benadryl)
Second generation (Less sedation, increase CNS distribution)

Allergy (#1 use)
Second generation are near equal efficacy has first generation

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18
Q

List 4 first generation antihistamines

A

Dramamine - anti-motion sickness/ anticholinergic activity (causes sedation)

Diphenhydramine (Benadryl)- same as dramamine

Promethazine (Phenergan) - antiemetic

Cyproheptadine (Periactin)- anti-serotonin activity

(most first generations have marked sedation d/t crossing the BBB)

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19
Q

List 3 second generation antihistamines

A

Allegra
Claritin
Zyrtec

(no sedation effect/ does not cross BBB)

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20
Q

What are other uses for antihistamines besides relieving allergy symptoms?***

A

Sedation (resembles, antimuscarinic drugs, sleep aid)
Antinausea/Antiemetic (motion sickness, morning sickness)

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21
Q

List 3 Toxicity Effects of H1 Receptor Antagonist (Antihistamine)

A
  1. Sedation
  2. Antimuscarinic Effects
  3. Less Common: Excitation, Convulsion, Postural Hypotension
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22
Q

What are H2 Receptor Antagonist used for? ***

A

H2 blockers to block stomach acid production, not as effective as PPI, heavy OTC use.

PPI are more expensive

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23
Q

Describe how stomach acid is produced.

A
  1. Parietal cells in the stomach have H2 receptors that stimulates cAMP when histamine is bound to it.
  2. cAMP will stimulate PKA.
  3. PKA activates the proton pump.
  4. Proton pump, pumps protons (H+) from inside the cell to the outside through the H+/K+ ATPase pump.(PPI blocks this pump)
  5. H+ will bind with Cl- to form hydrochloric acid.
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24
Q

What are some H2 receptor blockers?

A

Cimetidine
Ranitidine
Nizatidine
Famotidine (pepcid)

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25
Q

What is the chemical name for Serotonin?

How many receptor families does serotonin have?***

A

5-Hydroxytryptamine (5-HT)

Serotonin receptors are called 5-HT receptors.
There are 7 receptor families. All are GPCRs except 5-HT3

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26
Q

What are the functions of 5-HT?

A

-Plays a role as a important NT in the Ralph Nuclei
-Stored and rapidly inactivated
-90% of 5-HT is in the GUT
-5-HT is involved in the Platelet Clotting Process
-Plays a role in Migraine HA in the CNS

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27
Q

90% of the serotonin are in the ___________ cells. ***

What is the function of these cells?

What is an indication that there is a tumor in these cells?

A

Enterochromaffin

Enterochromaffin Cells have a function of increasing movement along the gastrointestinal tract.

If there is a tumor in these cells, they are producing too much 5-HT which will increase movement along the GI tract causing diarrhea.

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28
Q

__________ will degranulate and release serotonin and cause constriction. ***

How will this contribute to blood loss?

A

Platelets.

After plugging up the hole, platelets will degranulate and cause constriction decrease blood loss.

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29
Q

What does Serotonin in the Raphe Nuclei mediate? ***

A

Regulates mood, sleep, appetite, temp, pain perception, BP, depression, anxiety, migraines

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30
Q

Serotonin is a derivative of ______***

A

Tryptophan

31
Q

What is the breakdown of 5-HT?

What can the break product of 5-HT be used for in diagnosing?

A

5-Hydroxyindoleacetic acid (5-HIAA)

5-HIAA can be used to detect Enterochromaffin tumors

32
Q

Most serotonin receptors are GPCR’s except for the ________receptor.

What happens if serotonin is released into the area postrema?

What will block this response?

A

5-HT3, it is an ion channel for Na+ and K+. Rapid response with this receptor.

This will induce vomiting.

5-HT3 blocker like zofran/ondansetron.

33
Q

What are serotonin’s effect on the NS?***

What are serotonin’s effect on the Respiratory System?

What are serotonin’s effect on the CV?

What are serotonin’s effect on the GI?

A

Nervous system: vomiting reflex, pain/itch, chemoreceptor reflex (bradycardia, hypotension)

Respiratory: Facilitates ACh release (constriction), hyperventilation

CV: Inotrope, platelet aggregation.

GI: Increase peristalsis

34
Q

What are the three primary serotonin agonist targets?***

A

5-HT1A (Raphe nuclei) - Buspirone non-benzo anxiolytic (GAD/OCD)

5-HT1B (Brain)-targets for migraine/HA
5-HT1D (Brain)-targets for migraine/HA

35
Q

What are the two primary serotonin antagonist targets?

A

5-HT2A- smooth muscle, cerebral cortex -phenoxybenzamine, cyproheptadine

5-HT3- Area postrema, only receptor that is not a GPCR, ion channel. Zofran.

36
Q

What receptor does Buspirone act on?

Whats the function of this drug?

A

It is a partial serotonin agonist 5-HT1A.

Non-benzodiazapine anxiolytic (GAD, OCD)-non sedative

This drug will slow the release of serotonin in the raphe nuclei, decreasing the amount of serotonin.

37
Q

What receptor does Sumatriptan act on?

What is the function of this drug?

A

Serotonin serotonin agonist that binds to 5-HT1D and 5-HT1B

Treats Migraine HA - causing vasoconstriction.

38
Q

What is happening during a migraine HA?

A

Caused by dilation of the blood vessels in the brain.

Sumatriptan/Imitrex will bind to 5-HT1B and 1D and cause vasoconstriction to relieve the migraine HA.

39
Q

The causes of migraine is unknown, but what pain mediators is it associated with?

What are symptoms of Migraine?

A

CGRP
Substance P
Trigeminal Nerve

Sx: Aura, Severe HA, HV, Photophobia, phonophobia, speech abnormalities.

40
Q

What are 5 treatments for migraine?***

A
  1. Pain relief - ASA, ASA + Caffeine, NSAIDS, Opioids
  2. Triptans- (Agonist)5-HT1B/1D
  3. Ergotamine- less effect than triptans
  4. Anti-nausea- chlorpromazine, ondansetron.
  5. Glucocorticoids- prednisone (preventative measures)

**PETA-G

41
Q

How do Triptans work on migraines?

A

They bind to 5-HT 1D/1B receptors in the cranial blood vessels and prevent dilation and stretching of pain endings.

Triptans are not use preventatively, they are used for the migraine attack itself.

42
Q

What are 5 drugs that can be for preventative measures for Migraines?

A
  1. Beta Blockers, CCB, ACE inhibitors
  2. Antidepressants - SSRIs, TCAs
  3. Anti-seizure- Valproate, Topiramate
  4. Botox - will paralyze dilation of blood vessels
    5 Monoclonal Antibodies - Aimovig- blocks CGRP receptors
43
Q

What are the 3 toxicities of triptans?

A
  1. Recurrence of Migraine
  2. Coronary Vasospasm (rare)
  3. Serotonin Syndrome (especially taking triptans with/ SSRI or MAOIs)
44
Q

What is serotonin syndrome?***

What is the precipitating drug?

Clinical presentation?

Treatment?

A

Excess amount of serotonin that will lead to a hyperthermic response in the body.

Precipitating drugs: Anything that will increase 5HT, SSRI, St. John’t Wort, Ginseng

Clinical presentation: HTN, Hyperreflexia, hyperthermia, onset w/i hours.

Treatment: Sedation and use paralysis to slow down muscle movements. Intubation/Ventilation. Use of cyproheptadine (antihistamine 5HT blocker) or chlorpromazine, cooling.

45
Q

What is the cause of Neuroleptic Malignant Syndrome? ***

What are the clinical presentation?

Treatment?

A

D-2 blocking antipsychotics (chlorpromazine, haloperidol)

Clinical presentation: hyperthermia

Treatment: Diphenhydramine and cooling

46
Q

What is the caused of Malignant Hyperthermia? ***

Clinical presentation?

Treatment?

A

Genetic condition affected by volatile anesthetics and SCh, targets the RYR to release Ca2+ leading to more contraction.

Clinical presentation: Hyperthermia

Treatment: Muscle relaxant, dantrolene, and cooling.

47
Q

What symptoms are consistent between MH, Neuro Malignant Syndrome, and Serotonin Syndrome?

A

Increase body temperature (hyperthermia)

48
Q

Are there any serotonin drugs that are used during weight loss?

How effective where they?

Other non-serotonin weight loss drugs?***

A

Most have recalled (Fen-phen) d/t cardiac insufficiency and valvular disorders. These were 5-HT2 agonist.

Lorcaserin - 5HT2C agonist

5-10% effective over 1 year

Liraglutide GLP-1 agonist (diabetes)
Orlistat- GI Lipase Inhibitor

49
Q

What is a serotonin antagonist drugs used to treat carcinoid tumors? ***

What is a serotonin antagonist drugs used to treat carcinoid tumor and cold induced urticaria?

What serontonin antagonist is an anti-emetic?

A

Phenoxybenzamine -also an alpha 1 inhibitor (irreversible). Blocks 5-HT2

Cyproheptadine - also an antihistamine, treats cold induced urticaria and carcinoid tumbors, Blocks 5HT2

Odansetron blocks 5-HT3

50
Q

What receptor does Zofran work on?

Use of Zofran?

A

Zofran is a 5HT3 inhibitor
Prevents nausea and vomiting
Also used in chemo pt to relieve nausea

51
Q

What is the reinforcing neurotransmitter? This is usually released when we do something good and has a rewarding effect.**

A

Dopamine

52
Q

What is the biosynthesis of dopamine?***

A

Amino Acid (Tyrosine) converted to L-DOPA through tyrosine hydroxylase
L-DOPA is converted to Dopamine through DOPA Decarboxylase

Dopamine can further be converted to NE and Epi

53
Q

What reuptakes dopamine?***

A

DAT (Dopamine Transporter)

54
Q

How many receptor types of Dopamine are there?***

A

Five (D1-D5, all metabotropic) all in CNS.

D1 and D2 are usually in the periphery as well.

55
Q

Where does the pathway of dopamine usually start? Two spots.

A

Substantia nigra
Ventral Tegmental area

56
Q

What dopamine pathway deals with motor movement? ***

What dopamine pathway deals with reinforcement and addiction?***

What dopamine pathway deals with working memory and planning?***

A

Nigrostriatal

Mesolimbic

Mesocortical

57
Q

What are our happy chemicals? (Five)***

A

Dopamine, Serotonin, Norepinephrine (Loveheim cube of emotions)
Endorphins
Oxytocin (love chemical)

58
Q

What is the difference between depression and anxiety?

A

Depression deals with sadness, 4th highest cause of disability.

Anxiety deals with activity and anxiousness, feeling the need to do something or correct something.

In both depression and anxiety, women are affected twice as often as men.

59
Q

What are five forms of depression?***

A
  1. Dysthymia - Doom and gloom
  2. Psychosis - hallucinations
  3. Postpartum Depression (usually temporary)
  4. Seasonal affective disorder (SAD), usually a result of lacking Vit.D / sunlight
  5. Bipolar disorder

(DPS BP)

**Depression: think down or inactivity, inability to get things done.

60
Q

What are four forms of anxiety?***

A
  1. Generalized Anxiety Disorder (GAD) - Heart racing, palpitations
  2. Obsessive Compulsive Disorder (OCD)
  3. Post-Traumatic Stress Disorder (PTSD)
  4. Social Phobia

**Anxiety: think action and need to get things done.

61
Q

What are the 4 major classes of antidepressant treatments?***

A
  1. Selective Serotonin Reuptake Inhibitors (SSRIs) - mild side effects. Prozac, Zoloft
  2. Selective Serotonin-NE reuptake Inhibitors (SNRIs) - block SERT/ NET- Pristique, Cymbalta
  3. Tricyclic Antidepressants (TCAs)- inhibits SERT, NET, anticholinergic- Elavil
  4. Monoamine Oxidase Inhibitors (MAOIs)- indicated for major depressive disorder. - Nardil, Selegiline

All 4 will increase monoamine NT levels within the synapse.

62
Q

How do SSRIs work as first line treatment for depression?

What are some SSRI drugs?

A

Inhibition of the Serotonin Reuptake Transporter (SERT)

Fluxoetine (Prozac)
Citalopram (Celexa)
Paroxetine (Paxil)
Sertraline (Zoloft)
Escitalopram (Lexapro)

63
Q

How do SNRIs work?

When is this used?

Name two SNRI drugs.

A

SNRI work by inhibiting SERT and NET

Second line treatment for major depression and pain disorders (trigeminal neuralgia)

Desvenlafaxine (Pristique)
Duloxetine (Cymbalta)

64
Q

How do TCAs work?

What is the difference between TCAs and TeCAs?

Give an example of a TCA drug.

A

TCAs inhibit SERT, NET, and some anticholinergic effects

TCAs are 3-ring structures and TeCAs are 4-ring structures

Amitriptyline (Elavil)

65
Q

Why are MAOI’s rarely used, how do they work?

Who will take MAOIs?

What enzymes can be targeted?

Name two MAOI drugs.

A

D/t Lethal drug interactions. MAOIs work by blocking the breaking down of NE, Dopamine, Serotonin. Increasing all these NT at the synapse.

Refractory and major depression

Targets: MAO-A, MAO-B, or Both

Phenelzine (Nardil) - can be irreversible
Selegiline - new safer version, not as efficacious, can be used as a patch.

66
Q

What groups of antidepressants will block SERT?

How does MAOI work with serotonin?

A

SSRI, TCAs, and SNRIs. All three will increase 5-HT in the synapse.

MAOI will prevent the breakdown of 5-HT resulting in a greater release of that NT in the synapse.

67
Q

What groups of antidepressants will block NET?

How does MAOI work with NE?

What group of antidepressant will block alpha-1 receptors?

A

TCAs and SNRIs.

MAOI will prevent the breakdown of NE.

TCAs will block alpha-1 receptors.

68
Q

Name three groups of Atypical Antidepressants.

A
  1. NDRI (NE/Dopamine reuptake inhibitors)
  2. Benzodiazepines
  3. Antipsychotics
69
Q

How do NDRIs work? ***

Name two examples.

A

Inhibits NE and DA reuptake

Buproprion (Wellbutrin)
Solriamfetol (Sunosi) - used for daytime sleepiness

Can be used for Depression, ADHD, GAD.

70
Q

How do benzos treat anxiety?***

A

Suppress anxiety through sedation/hypnotic
Can impair cognitive function.

71
Q

What kind of depression will antipsychotics be used for? ***

Targets?

What are two examples of antipsychotic drugs?

A

Major severe depression, antipsychotics can be used in conjunction with SSRIs.

Antipsychotics are D2 receptor antagonist (chlorpromazine, haloperidol)

Aripiprazole (Abilify)
Amisulpride- used for Schizophrenia

72
Q

All antidepressants have a __________ warning. ***

What does this mean?

What age group does this apply to?

What are other adverse effects of antidepressants?***

A

Black Box

Increase in suicidal tendencies.

18-25-year-olds

Drug interactions (fatal with MAOIs), N/V/D, upset GI, Sexual Dysfunction (fairly common).

73
Q

What was believed to be causing the suicidal tendencies for people taking antidepressants.

A

Under dosing of the antidepressants medication

74
Q

What are 3 alternative treatments to depression?***

A
  1. Psychotherapy - “talk it out”, this will be instituted first before meds.
  2. Electroconvulsive Therapy- for severe depression
  3. St. John’s Wort - Top seller botanical product in the US

Pharmacology Test 4 (5 decks)

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