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pmcol ii > Opioids I > Flashcards

Opioids I Flashcards

1
Q

Opium

A

Dried latex from the opium poppy
Untransformed

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2
Q

Opiates

A

Any drug derived from opium
(Morphine and Heroin)

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3
Q

Opioid

A

Any drug that binds to an opioid receptor (Includes opiates and synthetic opioid agonists)
(Fentanyl and Heroin)

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4
Q

Narcotic

A

Used to refer to drugs with sleep inducing properties

Now is referred to illegal use of opioids with non-medical purposes

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5
Q

What are the 4 opioid receptors

A

Mu
Delta
Kappa
Orphanin receptor ligand (ORL-1) or NOP

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6
Q

What differs between the different opioid receptor types

A

Receptor distribution

Ligand specificity

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7
Q

Where are Mu Opioid Receptors? What are they responsible for?

A

Subcortical cortex, thin vertical line near centre

Emotional reactions

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8
Q

Where are Kappa Opioid Receptors? What are they responsible for?

A

Cortex region, outlines the edges of the cortex

Coordination and sensory info

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9
Q

Where are Delta Opioid Receptors? What are they responsible for?

A

Cortex region, horizontal lines spanning both cortical and subcortical cortex

Coordination and sensory info

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10
Q

Where are ORL-1 Opioid Receptors? What are they responsible for?

A

Wildly expressed in the central nervous system, basically everywhere in the brain

May be involved in fear processing

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11
Q

Describe homology between opioid receptors

A

The centres of opioid receptors are highly conserved and are identical regions between all opioid receptors

The ends of the opioid receptors differ between the different types, this difference dictates what ligand specificity and what ligand binds for different opioid receptors

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12
Q

What is the most common opioid receptor

A

Mu opioid receptors

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13
Q

What are the effects of a Mu agonist, give some examples

A

Analgesia
Reward
Cough suppressant
Respiratory depression
Constipation

Morphine, heroine, codeine

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14
Q

What are the effects of a Mu antagonist, give some examples

A

Aversive
Prevents reward
Blocks overdose

Naloxone

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15
Q

What are the effects of a Delta agonist

A

Not rewarding
No analgesia effects
Seizure inducing

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16
Q

What can delta agonists potentially treat, what are the side effects

A

Could potentially treat chronic migraines, leads to unregulated cortical activity, causes seizures

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17
Q

What are the effects of a Kappa agonist, give some examples

A

Aversive
Hallucinogenic
Anxiogenic (Causes anxiety)

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18
Q

What are the effects of a Kappa antagonist

A

Potential antidepressant and reverses anxiety (anxiolytic)

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19
Q

What are the best analgesics

A

Opioids are great at blocking acute pain

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20
Q

List a partial agonist at the mu opioid receptor, what are its benefits

A

Buprenorphine, mild to moderate analgesic efficacy, has a safer therapeutic index

Only partially inhibits breathing complex, impossible to overdose

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21
Q

List some full agonists at the mu opioid receptor

A

Morphine, methadone, fentanyl, heroine

22
Q

What has a higher potency, morphine or fentanyl. What does this mean?

A

Fentanyl has a higher potency meaning it has higher analgesic effects and more side effects at a lower dosage

23
Q

What kind of ligand is buprenorphine. What does it bind to and what are its effects

A

Mixed agonist-antagonist

Partial agonist at mu opioid receptor
Used to stabilize people addicted to full opioid agonists (morphine, fentanyl). and alleviates withdrawal symptoms

Antagonist at delta and kappa opioid receptors
Antidepressant through antagonist effects at kappa receptor

24
Q

What are Beta-arrestins and what do they do

A

Intracellular proteins that regulate signal transduction in G-protein coupled receptors by binding to phosphorylated receptors

Internalizes receptors
Arrests G-protein receptors and redirect signaling to alternative pathways

25
Q

What is the mechanism behind beta-arrestins

A

GPCR is activated by ligand binding –> G-protein is cleaved forming two subunits -> Receptor is phosphorylated –> signals beta-arrestin to bind

Beta-arrestin binds blocking further G-protein signaling –> Redirects signaling to alternative pathways –> Targets receptor for internalization

26
Q

In opioids what are the effects of G-protein biased agonists

A

Analgesic effects

27
Q

In opioids what are the effects of beta-arrestin biased agonists

A

Respiratory depression and Constipation

28
Q

What kind of drug is codeine and what is it metabolized into

A

Prodrug and is metabolized into morphine by liver enzymes

29
Q

What is impacted more by first pass metabolism
Codeine or Morphine

A

Morphine

30
Q

Where are opioid agonists most widely distributed

A

Highly perfused tissues (Brain, lungs, liver, kidney, and spleen)

31
Q

Order these administration of opioids from largest effect to smallest effect

SQ, PO, IV

A

Intravenous (IV) > Subcutaneous (SQ) > Mouth (PO)

32
Q

What is morphine metabolized into, what is the percentage of each metabolite

A

Morphine-3-glucuronide (M3G)
90%
Morphine-6-glucuronide (M6G)
10%

33
Q

Morphine metabolism enzyme

A

UGT2B7

34
Q

What are the efects of M6G

A

Active metabolite that prolongs the effects of morphine

35
Q

What metabolizes codeine into morphine

A

CYP2D6

36
Q

Why do different people have different reactions to codeine

A

Genetic Polymorphisms of CYP2D6
Different people either have a slow or fast metabolizer

Variation in analgesic and adverse responses

37
Q

What are polar metabolites, how are they mainly excreted

A

Glucuronide conjugates (M3G and M6G) of opioid analgesics are excreted mainly through urine

38
Q

How are uncharged drugs excreted

A

Morphine, an uncharged drug is found in small amount in urine

39
Q

How can renal impairment affect opioid use

A

If someone has impairment of renal functions they will not be able to excrete out metabolites of potent opioids.

Can cause sedation and respiratory depression due to an accumulation of active polar metabolites (M6G)

40
Q

What are the three types of endogenous opioid peptides. What do endogenous opioid peptides do?

A

Beta endorphins
Enkephalins
Dynorphins

Neurotransmitters that mediate pain, reward, learning, memory, and cognition

41
Q

How are endogenous opioid peptides formed

A

Proteases cleave a protein precursor

42
Q

What is the protein precursor of enkephalins? Where are they found?

A

Proenkephalin

Brain, adrenal chromaffin cells

43
Q

What is the protein precursor of dynorphins? Where are they found?

A

Prodynorphin

Pituitary/adrenal medulla

44
Q

What is the protein precursor of beta-endorphins? Where are they found?

A

Proopiomelanocortin

Pituitary

45
Q

What do all opioid peptides share in common

A

A common amino acid sequence

Tyr-Gly-Gly-Phe
Various extensions are added during post-translational modification

46
Q

What are the different variations of beta-endorphins

A

Just beta-endorphins

47
Q

What are the different variations of dynorphins

A

Dynorphins A
Dynorphins B
Neoendorphins

48
Q

What are the different variations of Enkephalins

A

Met Enkephalins
Leu Enkephalins

49
Q

What the opioid receptor affinity for Enkephalins

A

Delta > Mu > > > Kappa

50
Q

What is the opioid receptor affinity for Dynorphins

A

Kappa > > > Mu = Delta

51
Q

What is the opioid receptor affinity for Beta-endorphins

A

Mu = Delta > > > Kappa

52
Q

What does it mean when opioid peptides have different affinities

A

The peptides have different preferences to different receptors, they can bind to all of them, its just they select certain ones that they prefer

pmcol ii (10 decks)

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