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Pharmacology > 4.2 - Autocoids - Serotonin > Flashcards

4.2 - Autocoids - Serotonin Flashcards

1
Q

Biosynthesis

A
  • Precursor
  • Locations
  • Steps
  • Receptors
  • Drugs
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2
Q

Precursor

A

L-Tryptophan

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3
Q

Locations

A 
• Enterochromaffin cells
 – GIT
 – > 90% of 5-HT
• Platelets
• CNS
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4
Q

Steps

A

L-tryptophan ➡️1️⃣ 5-hydroxytryptophan ➡️2️⃣ 5-hydroxytryptamine

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5
Q

1️⃣

A

Hydroxylation

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6
Q

2️⃣

A

Decarboxylation

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7
Q

Effects

A
  • Central

* Peripheral

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8
Q

Central

A
  • Mood regulation
  • BP regulation
  • Thermoregulation
  • Emesis
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9
Q

Peripheral

A
  • GIT
  • Blood vessels
  • Platelets
  • Brochi
  • Uterine SM
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10
Q

GIT

A

Peristalsis

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11
Q

Blodo vessels

A

Vasoconstriction

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12
Q

Platelets

A

Platelet aggregation

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13
Q

Bronchi

A

Bronchospasm

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14
Q

Uterine SM

A

Contraction — Oxytosis

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15
Q

Receptors

A
  • 5-HT1a
  • 5-HT1B/1D
  • 5-HT2a/2B
  • 5-HT3
  • 5-HT4
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16
Q

5-HT1a

— pre-synaptic (CNS)

A

INHIBITION of 5-HT release

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17
Q

5-HT1B/1D

— Peripheral Blood vessels

A

Vasoconstriction

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18
Q

5-HT2a/2B

— Smooth Muscles

A

Contraction

  • Vasoconstriction
  • Oxytocic effect
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19
Q

5-HT3

— Area postrema of the brain (CTZ)

A

Emesis

20
Q

5-HT4

— GIT

A

⬆️ GI motility

21
Q

Drugs

A
  • 5-HT1a
  • 5-HT1B/1D
  • 5-HT2a/2B
  • 5-HT3
  • 5-HT4
22
Q

5-HT1a

A

Partial Agonist
– Buspirone
- Anxiolytic

23
Q

5-HT1B/1D: AGONISTS

— -triptan

A 
• Sumatriptan
• Zolmitriptan
• Naratriptan
• Rizatriptan
(Vasoconstriction)
24
Q

⬆️est BA

A

Naratriptan

25
Q

Use: 5-HT1B/1D AGONISTS

A

Mgt of acute migraine HA

26
Q

S/E: 5-HT1b/1D

A

⬆️ BP

27
Q

C/I: 5-HT1b/1D

A
  • HTN

* CAD

28
Q

5-HT2a/2B

A
  • Antagonist

* Agonists

29
Q

5-HT2a/2B: AGONIST

A 
Ergotamine
(Vasoconstriction)
 – PO
 – PR
 – Nasal
 – SQ
30
Q

Use: 5-HT2a/2B Agonist

— Ergotamine

A

• Mgt of acute migraine HA
- Ergotamine/ Ergonavine
• Mgt of post partum hemorrhage
- Ergonovine

31
Q 
‼️ 
– Claviceps purpurea
– Rye
– Vasoconstriction
  – Ergot Toxicity (St. Anthony's Fire)
A

Ergot

32
Q

S/E: Ergot derivatives

A
  • ⬆️ BP

* Oxytocic effect

33
Q

5-HT2a/2B: ANTAGONIST

A
  • Methysergide
  • Ketansiren

– Vasodilation

34
Q

– Use: Prophylaxis for migraine HA

– S/E: Retroperitoneal fibrosis

A

Methysergide

35
Q

– Europe
– Antihypertensive
– a1 antagonist

A

Ketansiren

36
Q

5-HT3: ANTAGONISTS
— -setron
— anti-emetics

A
  • Granisetron
  • Ondnasetron
  • Palonosetron
  • Dolasetron
37
Q

Transdermal patch

A

Granisetron

38
Q

– T 1/2: 40 hrs

– Single dose: 5 days

A

Palonosetron

39
Q

Use: 5-HT3 ANTAGONISTS

A

Mgt of Chemotherapy-induced N & V

40
Q

Route:

A
  • IV

* PO

41
Q

– GIT

– Mgt of irritable bowel syndrome with diarrhea

A

Alosetron

42
Q

5-HT4

A
  • Partial Agonists

* Full Agonist

43
Q

Partial Agonists

A
  • Tegaserod

* Cisapride

44
Q

Use: PARTIAL AGONISTS

A

Mgt of irritable bowel syndrome with predominant constipation

45
Q

Full Agonist:

— Prucalopride

A

Mgt of chronic constipation

Pharmacology (21 decks)

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