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Pmcol 200 > L18 > Flashcards

L18 Flashcards

1
Q

Opium

Opiates

A

Opium = dried latex obtained from the poppy Opiates = any drug derived from opium

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2
Q

Opioid

Examples

A

any drug that binds to an opioid receptor

Includes opiates, as well as synthetic opioid agonists (fentanyl,heroin, oxycontin)

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3
Q

Narcotic Originally referred to

Now used by law enforcement as

A

Originally referred to any drug with sleep inducing properties
now usually used by law enforcement to refer to illegal use of opioids for non-medical purposes.

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4
Q

Morphine

____ opiate because it’s found in ___ extract

A

Morphine

Natural opiate because it’s found in poppy extract

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5
Q

Heroin

A

Semisynthetic opiate - not found in poppy extract

Synthesized from morphine; acetyl groups are added to morphine

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6
Q

Fentanyl

A

Opioid NOT opiate because this and semisynthetic precursors are found in poppy extracts

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7
Q

Opioid receptors are

A

inhibitory
G-protein coupled receptors
(GPCR)

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8
Q

Activation of opioid receptors: inhibit of _____ channels, activate of _____ channels and inhibit of ___ ____ →neuronal ____ and _____ transmitter release

A

Activation of opioid receptors: inhibit of calcium channels, activate of K+ channels and inhibit of adenylyl cyclase →neuronal inactivation and reduced transmitter release

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9
Q

Types of opiod r

A

Mu, kappa, delta, nop/orl 1

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10
Q

all are Gi GPCRs, but produce very similar/different effects when activated
• differences are due to receptor ___ (different neurons, different brain circuits)
• ligand specificity: drugs are selective for _____ opioid receptors

A 
receptor distribution (different neurons, different brain circuits)
selective for different opioid receptors
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11
Q

Orl 1 widely expressed in___

was the last opioid receptor to be identified based on ___ ____ (not function)

A

Cns

Sequence homology

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12
Q

Orl 1 well/poorly studied
Does/doesn’t share functional similarities with other opioid receptors
Involved in___ processing

A

Poorly
Doesn’t
Fear processing

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13
Q

Mu agonist - ARCAR

3 drug exmaples

A

Analgesia, reward, antitussive, respiratory depression, constipation

Morphine, codeine, heroine

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14
Q

Mu antagonist - APB

1 eg

A

Aversive
prevent reward
Block overdose
Eg. Naloxone

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15
Q

Delta agonist

dAS

A

analgesia for chronic pain (migraine), seizure inducing

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16
Q

Delta antagonist

A

no effects

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17
Q

Kappa agonist
AHA
1 eg

A

aversive, hallucinogenic, anxiogenic

eg. salvia

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18
Q

Kappa antagonist

A

antidepressant/anxiolytic

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19
Q

Full mu opioid receptor agonists include (4)

A

morphine, methadone, fentanyl, and heroin.

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20
Q

•Buprenorphine is a __ agonist at the ___ opioid receptor, mild to moderate ___ efficacy, but ____ therapeutic index

A

•Buprenorphine is a partial agonist at the mu opioid receptor, mild to moderate analgesic efficacy, but safer therapeutic index

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21
Q

full agonists can have similar/different potencies (fentanyl versus morphine)

A

full agonists can have different potencies (fentanyl versus morphine)

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22
Q

T/f: like efficacy, potency applies to all aspects of the drug

A

T

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23
Q

Buprenorphine activity at mu, delta, kappa r

A

buprenorphine is a partial agonist at the mu opioid receptor
antagonist at the delta and kappa opioid receptor

24
Q

Buprenorphine commonly used as

What is this therapy called

A

Treatment for pain and opioid addiction

Opioid agonist therapy

25
Q

• Beta-arrestins are a family of extra/intracellular proteins important for regulating signal transduction at ___

A

Intracellular

GPCR

26
Q

• Following ___ activation and ____ cleavage, GPCR is ____, which signals β- arrestin to ____

A

• Following receptor activation and G- protein cleavage, GPCR is phosphorylated, which signals β- arrestin to bind

27
Q

β-arrestin binding ___ further G- protein signaling, redirects signaling to _____ pathways, and targets receptors for ____

A

β-arrestin binding blocks further G- protein signaling, redirects signaling to alternative pathways, and targets receptors for internalization

28
Q

beta arrestin arrests G protein signaling that leads to ____ following __ ___ use

A

beta arrestin arrests G protein signaling that leads to tolerance following chronic opioid use

29
Q

beta arrestin also activates its own ___ signaling pathways that contribute to some of the drug _____

A

beta arrestin also activates its own intracellular signaling pathways that contribute to some of the drug effects

30
Q

receptor selectivity

A

selectivity for different r subtypes

31
Q

functional selectivity

A

selectivity for different signalling pathways coupled to same r

32
Q

t/f: all opioid ligands lead to β- arrestin recruitment!

A

f

33
Q

t/f: Different opioid ligands can differently activate G-protein versus β-arrestin signaling pathways

A

t

34
Q

mu opioid receptor, G-protein signaling pathway drives ____, while β-arrestin signaling pathway drives ___ ___.

A

analgesia

respiratory depression

35
Q

most mu agonist opioids are __ ___ when taken orally

A

well absorbed

36
Q

____undergo extensive first-pass metabolism

A

morphine

37
Q

____effect not reduced by first pass metabolism so more effective orally

A

Codeine

38
Q

Opioid agonists are widely distributed through __ __, with highest concentrations in____ perfused tissues such as the brain, lungs, liver and kidney and spleen.

A

body tissues

highly

39
Q

opioids can Cross placental barrier - what happens

A

exert effects on fetus that can result in both respiratory depression and physical dependence in neonates

40
Q

morphine is metabolized by __ ___ __into __ __ __ and __ __ __

A

phase II glucuronidation
morphine-3- glucuronide
morphine-6-glucuronide

41
Q

the most important glucuronidation enzyme is

A

UGT2B7

42
Q

___ ___ ___is an active metabolite (can prolong morphine effects)

A

morphine-6-glucuronide

43
Q

codeine metabolized into morphine by___

what’s codeine

A

CYP2D6

prodrug

44
Q

Genetic polymorphisms of CYP2D6 (fast or slow metabolizers) linked to variation in____ and adverse responses among patients, particularly for___

A

analgesic

codeine

45
Q

Prevalence of CYP2D6 poor metabolizers is ~___% in white populations, lower in other groups (Asians ~2%)

A

6-10

46
Q

Polar metabolites, including___ conjugates (__ and ___) of opioid analgesics, are excreted mainly in the __.

A

Polar metabolites, including glucuronide conjugates (M3G and M6G) of opioid analgesics, are excreted mainly in the urine.

47
Q

t/f: Small amounts of unchanged polar drug may also be found in the urine.

A

t

48
Q

patients with renal impairment the effects of active polar metabolites (Morphine-6-Glucuronide) should be considered before the administration of potent opioids such as ___ due to the risk of ___ and __ ___.

A

morphine
sedation
respiratory depression.

49
Q

three types of endogenous opioid peptides

A

beta endorphins • enkephalins

• dynorphins

50
Q

Endogenous Opioid Peptides ___ distributed neurotransmitters that mediate __, __, __ and __, and ___

A

widely distributed neurotransmitters that mediate pain, reward, learning and memory, and cognition

51
Q

Endogenous opioid peptides are generated from a

Each precursor is subject to __ ___ __ that results in synthesis of multiple___ peptides

A

protein precursor

post-translational modifications
active

52
Q

all opioid peptides share common amino acid sequence of:

A

Tyr (tyrosine)-Gly (glycine)-Gly-Phe (phenylalanine)

53
Q

various extensions are added during post-translational modification yielding opioid peptides from _____in length

A

5 to 31 amino acids

54
Q

at mu opioid r:
agonist binding =
beta arrestin recruitment =

A

analgesia

respiratory depression, const

55
Q

people with poor codeine metabolizers

A

need higher dose of codeine

Pmcol 200 (12 decks)

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