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Pharmacolgy > Autocoids > Flashcards

Autocoids Flashcards

1
Q

autocoid definition

A

-hormone like substance produced close to where they have an effect

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2
Q

5 examples of autocoids

A
  • leukotrienes
  • prostaglandins
  • histamines
  • kinins
  • serotonin
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3
Q

leukotrienes

  • synthesis
  • target
  • involved in
  • therapeutic target
A
  • synthesis from arachadonic acid via lipooxygenase
  • binds to receptors in the respiratory tract
  • involved in inflammation conditions such as asthma
  • receptor agonists are used to treat asthma (as well as targetting LOX)
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4
Q

thromboxanes

  • synthesis
  • function
  • equal in amount with
A
  • made by COX1 using arachadonic acid
  • promote platelet aggregation and vasoconstriction
  • equal in concentration to PGI2 during health
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5
Q

PGE

  • synthesis
  • location of action
  • function
A
  • from arachadonic acid, catalyzed by COX1
  • located in the GI
  • production of the mucosal barrier
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6
Q 
function of prostaglandins in the kidney
-what are they made by
A
  • increased blood flow

- COX1 and COX2 are located in the kidney

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7
Q

prostacyclins (PGI2)

  • synthesis
  • function
  • inhibition of synthesis may lead to
A
  • from arachadonic acid via COX2
  • inhibits platelet aggregation and is a vasodilator
  • may lead to clot formation and possibly MI/thrombotic stroke
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8
Q

prostaglandins involved in pain, fever, and inflammation are made by

A

COX2

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9
Q

NSAIDs

  • function
  • mode of action
  • side effects, why
A
  • reduce pain, inflammation, fever by blocking COX
  • primary target is COX2 but will also block COX1 (this is what leads to the side effects of bleeding and GI ulcerations)
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10
Q

adverse kidney side effects with NSAIDs in the kidney

A
  • always a risk because the kidney has both COX1 and 2

- inhibits healthy blood flow to the kidney

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11
Q

COX2 inhibitors may shift the balance

A
  • of prostacylcins and thromboxanes

- this may lead to the risk of thrombosis since thromboxanes are at a higher concentration

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12
Q

selective COX1 inhibitors

-how does aspirin work

A
  • aspirin can be used in relatively small doses as a blood thinning agent via blocking thromboxane production
  • in order to treat pain and inflammation, a patient must take higher doses to overcome COX1 selectivity
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13
Q

H1 receptor

  • involved in
  • target for
A
  • involved in allergic reactions

- target of antihistamine drugs such as diphenhydramine (benadryl) or loratidine (claratin)

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14
Q

diphenhydramine vs loratidine

A

-diphenhydramine is sedating because it can cross the blood brain barrier

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15
Q

H1 antagonists have a propensity to antagonize

A

-muscarinic Ach receptors leading to anti-muscarinic effects

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16
Q

H2 receptors

  • found where
  • function
A
  • stomach

- when stimulated, cause gastric acid secretion

17
Q

H2 receptor antagonists

A
  • inhibit parietal cells

- available over the counter for dyspepsia or acid reflux

18
Q

bradykinins

-degraded by what

A

-degraded by ACE into kinins

19
Q

ACE does what

A

-facilitates the conversion of angiotensin 1 into the active form, angiotensin 2 which is a potent vasoconstrictor

20
Q

inhibiting ACE leads to

A
  • less conversion of bradykinins into kinins

- vasodilation

21
Q

ACE inhibitors end in

A

-pril

22
Q

an accumulation of bradykinins tends to

A

-irritate and inflame tissues leading to the cough associated with ACE inhibitors

23
Q

serotonins role in the GI tract

-serotonin antagonists in the GI

A
  • when stimulated, people experience nausea and vomiting
  • antagonists used to reduce those symptoms
  • ondansterone is the serotonin antiemetic prototype
24
Q

serotonins role in migraine

A

-a spike produces cerebral vasoconstriction which is followed by a rebound vasodilation effect causing a throbbing headache

25
Q

sumatriptan

A

-used for acute treatment of migraines, is an agonist which causes smooth muscle constriction

26
Q

broad functions of serotonin

A
  • nausea and vomiting in the GI
  • modulate sleep in the brain
  • constrict smooth muscle
  • dilates skeletal muscle leading to flushing

Pharmacolgy (12 decks)

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