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Pain > Opioid analgesics and antagonists > Flashcards

Opioid analgesics and antagonists Flashcards

1
Q

Difference between opiate and opioid?

A

OPIATE – active alkaloids naturally found in opium (Morphine / Codeine)

OPIOID - anything like morphine (opiate, partial/total synthetic)

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2
Q

Where does opium grow in the wild?

A

poppy plant. Morphine (12%)

o Codeine

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3
Q

semisynthetic opioids

A

oxycodone, hydromorphone

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4
Q

Fully synthetic opioids

A

fentanyl, methadone, loperamide

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5
Q

Non Opioid agonists

A

tramadol

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6
Q

3 types of opioid receptors: (and type)

A

o μ (mu) (“MOR”)
o δ (delta) (“DOR”)
o κ (kappa) (“KOR”)

GPCRs (Gi or Go)

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7
Q

Which receptor is used in pain meds?

A

MU

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8
Q

What type of **orphin goes with each type of receptor

A 
mu = endorphins
delta = enkaphalins
kappa = dynorphins
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9
Q

how do opioids work?

2 Pathways?

A

bind on presynaptic terminal and interfere with Ca2+ release
Gi-> decrease cAMP-> decrease PKA -> less active Ca channels
Go->increased free betaGamma subunits-> increased K (more common in the post synaptic side)

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10
Q

Central effects of opioids

A

inhibitions in the periaquaductal gray matter, and in the dorsal horn,

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11
Q

What drug activates kappa receptors as a side effect

A

morphine

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12
Q

Buprinorphin receptors

A

Mu activator, kappa and delta ANTAGONIST

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13
Q

Methadone non-opiod receptors

A

NMDA

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14
Q

Tramadol effects on nonopioid receptors

A

reduce 5HT (seratonin) uptake

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15
Q

Why are high doses necessary?

A

because there is a high first pass metabolism

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16
Q

what breaks down parent opioid drugs?

A

Liver breaks em down, kidney filters metabolites out

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17
Q

Major effects of μ receptor agonists

A 
CNS: analgesia, drowsiness
CV: Vasodialation
GI: decrease motility/ secretions
Gu/Gyn: less pee ( more ADH)
Skin: Flushed and warm
Immune: altered wbc production
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18
Q

Anti-dyspneic

A

opiods can be used to help make breathing easier

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19
Q

Morphine: Mechanism and clinical use in analgesia

A

Full mu agonist (weak kappa agonist)

    • Chronic (non-neuropathic pain)
    • best for acute trauma and cancer tx pain
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20
Q

Morphine metabolism

A

low bioavailability

two metabolites morphine6 = potent analgesic and morphine3 interferes with GABA

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21
Q

Adverse effects of morphine

A

sedation, nausea, constipation, respiratory depression, siezure, dry mouth, urinary retention

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22
Q

Morphine: Precautions and contraindications

A

GI bugs = may worse due to less motility
Hepatic impairment
Renal Impairment
Respiratory disease or head injury

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23
Q

Codeine mechanism , clinical use, adverse effects, and adverse effects

A

weak mu agonist
used for analgesia, cough, antiDiarrheal
Adverse = nausea, vomiting , pruritus
metabolism = creates lots of morphine in high metabolizers and not helpful in weak metabolizers

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24
Q

Oxycodone mechanism , clinical use, adverse effects, and adverse effects

A

weak MU agonist with STRONG metabolite oxymorphone MU agonist
used for analgesia,
Adverse - creates lots of analgesia in high metabolizers and not helpful in weak metabolizers

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25
Q

CYP2D6

A

Oxycodone

26
Q

Percocet?

A

oxycodone plus acetominophen

27
Q

people with renal and liver disease should get what opiod? why?

A

Hydromorphone (no active metabolites), Fentanyl, or methadone

28
Q

Heroin

A

crosses blood brain barrier rapidly and turns quickly into morphine

29
Q

Fentanyl safety advantage?

A

no histamine release and no active metabolites

30
Q

which drug is bad for dyspnea

A

hydromorphone

31
Q

Loperamide has what effect on the CNS? What is it used for?

A

No effect on the CNS

used to treat diarrhea (could cause gi pain)

32
Q

Tramadol: mechanism of action 6

A 
MOR agonist (but weak)
o Serotonin releasing agent
o Norepinephrine reuptake inhibitor
o NMDA receptor antagonist
o Nicotinic receptor antagonist
o M1 and M3 muscarinic acetylcholine receptor antagonist
33
Q

Adverse effects of tramadol

A

Nausea/vomiting, sweating, sexual dysfunction, lower seizure

threshold

34
Q

how is tramadol different than other opiods

A

NO respiratory depression, sedation,

drowsiness and constipation are less common

35
Q

what are the low efficacy opioids

A

codeine

36
Q

what are the moderate efficacy opioids

A

oxycodone, tramadol, buprenorphine

37
Q

What effects never develop tolerance?

A 
sedation/resp. depression
constipation
Miosis (pupil constriction)
38
Q

two steps in changing drugs

A

1 Calculate the equianalgesic dose

2 Adjust the dose for incomplete cross-tolerance by cutting by 50%

39
Q

Sched 1 drugs

A

Drugs with no currently accepted medical use in US

HEROINE, LSD, MARY J

40
Q

Sched 2 drugs

A

Drugs with a high potential for abuse which may lead to severe psychological or physical dependence
MORPHINE, HYDROMORPHONE, METHADONE, OXY

41
Q

What pathway is involved in addiction? what is the result

A

Mesolimbic (REWARD) Pathway

Increased dopaminergic neurotransmission

42
Q

How do opiods make you feel so good?

A

They inhibit GABA (which inhibits dopminergic neurons)

43
Q

How long before you can call a drug problem a opiod use disorder

A

12 months

44
Q

Factors affecting probability of addiction

A

Personal or family history of substance use disorder
Male
Poor social support
History of conviction related to drugs or DWI
Pre-adolescent history of sexual abuse
Comorbid psychiatric disorder

45
Q

Where did the video stop?

A

1:49:50

46
Q

How does methadone work/ mechanism?

A

Full MU receptor agonist
NMDA glutamate receptor

Great for chronic pain
Help for detox

47
Q

Delivery of methadone

A

tablet, liquid, IV

48
Q

Methadone Pharmacokinetics

A 
varies greatly based on genetics
Metabolized by p450 enzymes 
CYP3A4 in particular
LONG LONG HALF LIFE (can persist in liver)
renal and fecal excretion
49
Q

adverse effects due to NMDA agonist?

A

Confusion
Hallucinations/Paranoia
Depression/Apathy and Suicidal Ideation
Anorexia

50
Q

Methadone cardiac adverse rxns

A

Prolonged QTc
Cardiac arrhythmias
Seizures

51
Q

Which drug has an NMDA agonist ?

A

methadone

52
Q

What criteria make someone eligible for methadone? 3

A

> = 18 yrs
dependent on opioids > 1 year
Enrolled in methadone maintenance program

1 year requirement can be waived for pregnant patients, previously treated patients, or following prison release.

53
Q

Buprenorphine mechanism

A

partial agonist (so it is hard to overdose)

54
Q

Urine drug screening for Opioids

A

False positives for poppy seeds, rifampin, quinolones
detects morphine, heroin, codeine, methadone
best for identifying chronic users

55
Q

bUPRENORPHINE delivery

A

sublingual because of low bioavailability

56
Q

What is another name of hydromorphone

A

Dilauted

57
Q

Nalaxone

A

opioid antagonist -> will cause withdrawal
reverses opioid depression
short half-life (need to readminister)

58
Q

Suboxone:

A

Naloxone + Buprenorphine

decreases likelyhood of abuse

59
Q

Naltrexone

A

opioid antagonist ->
may decrease alcohol craving as well
Precipitates severe withdrawal

60
Q

half life of Naltrexone

A

Half-life
4 hrs (oral naltrexone)
13 hrs (metabolite of oral naltrexone)
5-10 days (IM Vivitrol)

61
Q

Naltrexone: Adverse Effects

A

Adverse effects:
Nausea, headache, anxiety

More rare side effects: Deep vein thrombosis, hepatitis, eosinophilic pneumonia, Depression, suicidal thinking

62
Q

Who should not get Naltrexone

A

those with liver failure

Pain (8 decks)

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