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MAT TRAINING > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

mechanism of methadone

A

FULL AGONIST of mu opioid receptor

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2
Q

duration of action methadone

A

long acting (half-life 15-60 hours)

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3
Q

affinity of methadone at opioid receptor?

A

weak (can be displaced by partial agonists or antagonists like buprenorphine or naltrexone respectively)…CAN PRECIPIATE WITHDRAWAL if this happens

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4
Q

harmful side effects of methadone (2)

A
  • respiratory suppression
  • qt prolongation

monitor closely to prevent overdose

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5
Q

methadone metabolism

A
  • CYP3A4

- mostly metabolized by liver but small proportion can be found in urine (AND THEREFORE IN UDS)

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6
Q

buprenorphine metabolism

A

liver
CYP3A4
small excreition in urine so CAN be detectable in UDS (but sometimes need to be a send out or confirmatory test because it may not always show up)

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7
Q

active metabolite of buprenorphine and what is it’s clinical significance?

A

norbuprenorphine
sometimes you can get levels of buprenorphine and norbuprenorphine in UDS to assess how patient is taking their med; patients may tamper with urine and add a little buprenorphine but they will show low norbuprenorphine levels if they haven’t actually been taking the med

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8
Q

best admin route for buprenorphine

A 
NOT SWALLOWED (poor first pass metabolism)
can use other formulations like sublingual/subdermal implant/depot/tablets to help this
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9
Q

mechanism buprehnorphine

A

PARTIAL agonist at mu receptor

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10
Q

risk for respiratory suppression on buprenorphine

A

VERY LOW

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11
Q

duration of action buprenorphine

A

long acting, half life (24-36 hours)

and slow dissociation from receptor

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12
Q

affinity buprenorphine to opioid receptor

A

HIGH; can displace other opioids

ex: if you use heroin while on buprenorphine, you won’t get euphoric (buprenorphine displaces heroin)

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13
Q

So what are the benefits of using buprenorphine?

A
  • prevents withdrawal symptoms
  • decreases cravings
  • decreases effects of other opioids
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14
Q

Effectiveness of transdermal (patch) and IV buprenorphine

A

they have been approved for analgesia/pain; BUT NOT APPROVED for treatment of opioid use disorder

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15
Q

What is the advantage of prescribing buprenorphine+naloxone (suboxone)?

A

developed to DECREASE IV/injectionDRUG USE

  • less likely to be diverted
  • less euphoria

encouraged to use combo product

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16
Q

biochemical mechanism naltrexone

A

opioid receptor ANTAGONIST
(blocks receptor from action of other opioid…also has high affinity to receptor)

BUT CAN PRECIPIATE WITHDRAWAL so taper off or make sure patient is off opioids for several days before starting

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17
Q

disadvantage of naltrexone tablet?

A

poor compliance

DO THE INJECTABLE

18
Q

which kind of patients would naltrexone be good for?

A

patients who prefer not to be on any opioids

19
Q

behavioral mechanism of naltrexone

A

blockade of reinforcing effects of heroin leads to gradual extinction of drug seeking/craving

people who use opioids on naltrexone experience no effect of expogenous opioids and often stop using them

20
Q

pharmacological mechanism of naltrexone

A

decreases reactivity to drug-conditioned cues and decreases craving (i.e blocks endorphins) which minimizes pathological responses contributing to relapse

21
Q

disadvantage for buprenorphine

A

concern for diversion (so use combo meds like suboxone, they’re less likely to get diverted)

22
Q

what to consider if patient decides to halt naltrexone treatment?

A

if they use again, they may use the same amount they did before they stopped…despite their lower tolerance…which will put them at risk for OVERDOSE

23
Q

benefits of methadone

A

RETENTION IN TREATMENT (dose dependent)

how long patients decide to stay in treatment and longer abstinence

24
Q

treatment dosing buprenorphine

A

dose dependent rise so start at like 8 ish mg then get stable…if persistent cravings can go up to 16

25
Q

`Conclusions of Precription Opoioid Addiction Treatment STudy (POATS)

A
  1. prescription opioid depdendent patients most liekly to reduce use during buprenorphine treatment compared to standard medical mgmt
  2. if tapered off buprenorphine, even after 12 weeks, liklihood of unsuccessful outcome is high even in pts getting counseling
26
Q

most common adverse side effects buprenorphine

A
  1. headache (treat wiith ASA/motrin/tylenol)
  2. constipation
  3. dry mouth (side effect of fall opioids)
27
Q

effectiveness buprenorphine vs injection naltrexone

A

both meds appear comparably effective

but naltrexone more difficult to initiate due to need to get a patient through medically supervised withdrawal

28
Q

which three opioid rx meds has most drug drug interactions

A

METHADONE

29
Q

which drugs classes/drugs interact with methadone?

A

SSRIs (ESP FLUVOXAMINE), carbamazpine, TCAs, MAOIs

30
Q

interaction of SSRIs and methadone

A

some SSRIs (fluvox, fluoxetine, sertraline; CYP inhibitors) can inhibit metabolism of methadone -> inc methadone blood levels

if starting, monitor closely for signs of methadone overmedication when first starting treatment

31
Q

which SSRI to DEFINITELY avoid on methadone

A

fluvoxamine

32
Q

interaction of methadone and carbemazepine

A

carbemaz (inducer) increases methadone metabolism/breakdown -> lowered levels can precipitate withdrawal/loss of therapeutif effects

try to start VPA instead

33
Q

qtc risk for buprenorphine

A

VERY LITTLE compared to methadone; not clinically significant

34
Q

what happens if you’re taking an agonist then take buprenorphine

A

buprenorphine displaces full agonist and can precipitate withdrawal

35
Q

what happens if patient on buprenorphine starts using again (full agnoist)

A

buprenorphine stays on receptors and effect of agnoist is decreased

36
Q

what happens if patient on buprenorphine takes a blocker like naltrexone/naloxone

A

buprenorphine remains on receptors, effect of antagonist has lsower onset but will precipitate withdrawal

37
Q

what happens if patient on buprenorphine takes benzo?

A

more accidental injuries; usually otherwise safe if patient using THERAPEUTIC DOSES…but can be fatal if used in combination with high doses (not prescribed doses)

38
Q

buprenorphine risk for respiratory depression

A

not clinically significant…think CEILING EFFECT

39
Q

contraindication for use of benzos and buprenorphine/methadone?

A

NO (just be careful and make a good treatmentplan/educate pt on risks)
used to be an FDA blackbox warning for combined use, but in 2017 this was changed since risks outweighed by risk of untreated opioid addiction

40
Q

recommendation for alcohol and buprenorphine

A

generally avoid CNS depressants with buprenorphine

some evidence rx with buprenorphien can decrease craving for EtOH

41
Q

which formulation of buprenorphine (tablet/film/suboxone) is standard of care for general care and why?

A

COMBO PRODUCT (Suboxone) because there is huge risk for diversion of tablet (mono product)

usually start with combo and make sure they’re stable for a year before considering switching to mono product

42
Q

how long to be abstinent from opioids before starting naltrexone?

A

7-10 days; treat withdrawal symptoms in mean time with non opioid meds like clonidine/tylenol/loperamide

MAT TRAINING (1 decks)

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