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Opioid analgesics and antagonists Flashcards

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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
CYP2D6
Oxycodone
26
Percocet?
oxycodone plus acetominophen
27
people with renal and liver disease should get what opiod? why?
Hydromorphone (no active metabolites), Fentanyl, or methadone
28
Heroin
crosses blood brain barrier rapidly and turns quickly into morphine
29
Fentanyl safety advantage?
no histamine release and no active metabolites
30
which drug is bad for dyspnea
hydromorphone
31
Loperamide has what effect on the CNS? What is it used for?
No effect on the CNS | used to treat diarrhea (could cause gi pain)
32
Tramadol: mechanism of action 6
``` 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
Adverse effects of tramadol
Nausea/vomiting, sweating, sexual dysfunction, lower seizure | threshold
34
how is tramadol different than other opiods
NO respiratory depression, sedation, | drowsiness and constipation are less common
35
what are the low efficacy opioids
codeine
36
what are the moderate efficacy opioids
oxycodone, tramadol, buprenorphine
37
What effects never develop tolerance?
``` sedation/resp. depression constipation Miosis (pupil constriction) ```
38
two steps in changing drugs
1 Calculate the equianalgesic dose | 2 Adjust the dose for incomplete cross-tolerance by cutting by 50%
39
Sched 1 drugs
Drugs with no currently accepted medical use in US | HEROINE, LSD, MARY J
40
Sched 2 drugs
Drugs with a high potential for abuse which may lead to severe psychological or physical dependence MORPHINE, HYDROMORPHONE, METHADONE, OXY
41
What pathway is involved in addiction? what is the result
Mesolimbic (REWARD) Pathway | Increased dopaminergic neurotransmission
42
How do opiods make you feel so good?
They inhibit GABA (which inhibits dopminergic neurons)
43
How long before you can call a drug problem a opiod use disorder
12 months
44
Factors affecting probability of addiction
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
Where did the video stop?
1:49:50
46
How does methadone work/ mechanism?
Full MU receptor agonist NMDA glutamate receptor Great for chronic pain Help for detox
47
Delivery of methadone
tablet, liquid, IV
48
Methadone Pharmacokinetics
``` 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
adverse effects due to NMDA agonist?
Confusion Hallucinations/Paranoia Depression/Apathy and Suicidal Ideation Anorexia
50
Methadone cardiac adverse rxns
Prolonged QTc Cardiac arrhythmias Seizures
51
Which drug has an NMDA agonist ?
methadone
52
What criteria make someone eligible for methadone? 3
>= 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
Buprenorphine mechanism
partial agonist (so it is hard to overdose)
54
Urine drug screening for Opioids
False positives for poppy seeds, rifampin, quinolones detects morphine, heroin, codeine, methadone best for identifying chronic users
55
bUPRENORPHINE delivery
sublingual because of low bioavailability
56
What is another name of hydromorphone
Dilauted
57
Nalaxone
opioid antagonist -> will cause withdrawal reverses opioid depression short half-life (need to readminister)
58
Suboxone:
Naloxone + Buprenorphine | decreases likelyhood of abuse
59
Naltrexone
opioid antagonist -> may decrease alcohol craving as well Precipitates severe withdrawal
60
half life of Naltrexone
Half-life 4 hrs (oral naltrexone) 13 hrs (metabolite of oral naltrexone) 5-10 days (IM Vivitrol)
61
Naltrexone: Adverse Effects
Adverse effects: Nausea, headache, anxiety More rare side effects: Deep vein thrombosis, hepatitis, eosinophilic pneumonia, Depression, suicidal thinking
62
Who should not get Naltrexone
those with liver failure

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