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PHARM.E2.Serotonin and Dopamine Drugs > Serotonin Synthesis > Flashcards

Serotonin Synthesis Flashcards

1
Q

Cascade of events for precursors-who?

A

L-tryptophan is the main precursor

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2
Q

Rate-limiting enzyme

A

TPH (tryptophan hydroxylase)-not normally saturated so tryptophan intake can influence 5-HT production

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3
Q

5-HTP

A

OTC nutraceutical used for depression

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4
Q

What is the active NT?

A

Serotonin (5-HT)

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5
Q

5-HTP –> 5-HT, enzyme?

A

5-HT decarboxylase

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6
Q

What are the important receptors?

A 
5-HT 1A
5-HT1D
5-HT2A/2C
5-HT3
5-HT4
5-HTtransporter
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7
Q

5-HT 1A effect

A

in the cortex and hypothalamus affect mood, cognitive fxn, neuro.endo fxn

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8
Q

5-HT 1D Effect

A

vasoCONSTRICTION on cerebral VSM, inhibition on NT release on certain nerve terminals

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9
Q

5-HT 2A/2C

A

in striatum and frontal cortex, antagonists that act here can produce hallucinations. Also inhibit dopamine release

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10
Q

5-HT 3

A
  • on enteric chromaffin cells (of the gut)–>stimulate sertonin release through these.
  • area postrema
  • emetic center-can stimulate vomiting (as defense mech)
  • nausea and vomiting of chemo, can play with these receptors
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11
Q

5-HT 4

A

-myenteric plexus (enteric nervous system)-gut motility via agonists

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12
Q

5-HT transporter

A

-increase serotonin presence in the synapse to help improve mood

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13
Q

Drug Examples

A 
5-HT 1A-BUSPIRONE
5-HT1D-SUMATRIPTAN
5-HT2A/2C-TRAZODONE, RISPERIDONE
5-HT3-ONDANSETRON
5-HT4-MOSAPRIDE
5-HT transporter-FLUOXETINE, SERTRALINE
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14
Q

5-HT 1A Agonists

A

numerous 1A receptors…ones in cortex mediate anti-depressant effects

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15
Q

1A: BUSPIRONE

A

Indications: generalized anxiety disorder; OFF label use: with SSRI for major depression
MOA: unknown, but likely due to activatoin of post-synaptic receptors in cortical regions, partial agonist 1A R
SE:can increase anciety during intial tx, drowsiness (but less than benzos), nausea

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16
Q

1D: SUMATRIPTAN

A

MOA: inhibition of **inflamm mediator release, cerebrovasoconstriction…coupled to alpha TWO (no systemic effect because its in brain, BUT coronary arteries have some action)
Indication: Prophylactic for migraine
SE: coronary vasoCONSTRICTION
Ci: pt with CAD

17
Q

What do SSRIs do to 5-HT?

A

Increases [5-HT] at synapse because they inhibit the uptake which also activates autoreceptors

18
Q

SSRI: FLUOXETINE and SERTRALINE ppttRV

A

Indications: depression, PTSD, OCD
MOA:
Ci: serotonin syndrome=excess serotonin..hyperthermia, thermoregulatory receptors in the hypothamlamus that willg et overactivated, mental status changes (can develop seizures-life threatening)

19
Q

SARI (Serotonin ANTagonist-reuptake inhibitor): TRAZADONE

A

increase serotonin and block its bad effects, facilitate good effects at 1A

MOA: 2A/2C antagonist + SSRI hypnotic, SSRI, blocks side effects associated with SSRIs
Indication: anxiety, depression (in combination of SSRI)
SE: warning of suicidality in young adults at initiation or treatment (black box-for early pt of tx)
Ci: MAO inhibitors

20
Q

2nd Gen ANTI-psychotics: RISPERIDONE

A

targets mesolimbic system

MOA:2A/D2.3 antagonist suppresses DA release in mesolimbic pathway, but increases DA release in mesocortical pathway
Indication: Schizophrenia with psychosis
SE: weight gain, anxiety, akathisia, psychosis with abrupt discontinuation

21
Q

Where is the majority of serotonin found?

A

90% is found in enterochromaffin cells of the gut. Release of 5-HT can be activated by various mechs: chemo (..nausea response)

22
Q

5-HT3 R ANTAgonist Drug: ONDANSETRON

A

important site: in the gut, stimulate vagal afferents to start firing, will stimulate nausea an vomiting

Indication:chemo induced emesis
MOA:block 3 R
SE:well tolerated :) :) :)

23
Q

5-HT 4

A

MOSAPRIDE (not in the US)
CISAPRIDE (discontinued)

MOA: 5-HT4 induced stimulation of ACH release in the myenteric plexus
Indication: gastroparesis
SE: arrythmia (long QT syndrome)***

24
Q

Dopaminergic System 4 places that are targeted?

A
  1. Mesocortical-ventral tegmentum to cortex (reduce in activity, leads to lack of affect in schizo, cant perseve emotional responses in other indivs)
  2. Mesolimbic-psychotic aspects (delirium, delusions in schizo)
  3. Nigrostriatal-hypOactive in pt with Parkinson’s
  4. Chemoreceptor Trigger Zone (also activated with 5-HT)-to stop nausea
25
Q

Dopamine Synthesis precursor?

A

L-tyrosine=AA precursor

26
Q

Can Dopamine cross BBB?

A

active NT CANNOT

27
Q

Rate limiting enzyme for dopamine synthesis?

A

tyrosine hydroxylase makes L-DOPA-precursor used in Parkinson rx

28
Q

What are the enzyme inhibitors used in Parkinson’s?

A

COMT! (convert dopamine into 3-methoxytyramine)–inhibit this will provide more dopamine

29
Q

2 main families of 5 DA receptor subtypes

A

D1 and D2 (both transmembrane proteins)

30
Q

Main Dopaminergic drugs

A 
L-DOPA--Park
BROMOCRIPTINE--Park
CARBIDOPA
SLEGILINE--Park
TALCOPONE--Park
METHYLPHERIDATE
METACHLOPRAMIDE
HALOPERIDOL
DOPAMINE
31
Q

Mechanism of Park

A

hh

32
Q

Define dyskinesia

A

motor issues

33
Q

CARBIDOPA

A

increase L-DOPA t1/2=it has better chance of getting into the brain (doesn’t get changed into dopamine which can be quickly metabolized–this way we don’t have to use such a huge dose of L-DOPA)

MOA:
Indication:
SE:

34
Q

BROMOCRIPTINE

A

MOA:
Indication:
SE:

35
Q

SELEGILINE

A

MOA:
Indication:
SE:

36
Q

TOLCAPONE

A

MOA:
Indication:
SE:

37
Q

HALOPERIDOL

A

***Antipsychotic potency of drugs strongly related to their D2 AFFINITY

MOA:
Indication:
SE:

38
Q

METHYLPHENIDATE

A

MOA:
Indication:
SE:

39
Q

METACLOPRAMIDE

A

MOA:
Indication:
SE:

PHARM.E2.Serotonin and Dopamine Drugs (1 decks)

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