Buprenorphine Flashcards
What type of drug is Buprenorphine
Partial agonist of Mu receptor
What is the half life of Buprenorphine
24 - 36 hour
long
What type of affinity does buprenorphine have to mu receptors
High
It will displace other Opioids - precipitated withdrawals
If you take this with Methadone or Heroine, you will not get full euphoria effect.
How is Buprenorphine metabolized
Liver
How is Buprenorphine taken
Sublingual due to low first pass
How does Buprenorphine work
High affinity displaces other opioids.
Slow dissociation allows for decrease withdrawal , decreased cravings and decreased effects of other opiods.
Types of Buprenorphine formularies used for analgesic
Patch
IV
Rationale to prescribe Buprenorphine/Naloxane
Reduce IV drug use
Major features of Naltroxene
High affinity for Mu receptors
Long acting: oral ( 24 hours), Injection (5 - 10 days)
Full antagonist
Need to be off of Opioids for several days prior to injection to prevent precipitated withdrawals.
How does naltrexone work:
it decreases craving of opioids (Behavioral component).
Usual dosage for Buprenorphine
4 - 32 mg (oral tab)
Usual dosage for Naltrexone
380 mg Depot Injection
Best option for anyone trying to avoid Opioids
Naltrexone
Relative, where do we see a good therapeutic dosage response for buprenorphine
8 - 12 mgs
Relative, what is the typical max dosage of mono buprenorphine?
16 mgs
Special consideration for Buprenorphine
Risk of diversion
Special consideration for Naltroxene
Patients must be opioid free before starting
Risk of overdose for patients who stop it
Pain management - non pharmological usage
Maintenance vs taper
Tapering seems to cause less retention. Maintenance treatment seems like best option for prevention of Opioid relapse.
Common side effects of Buprenorphine
Headaches - manage with OTC meds
Constipation - High fiber diet, hydration and stool softener
Dry mouth - Hydration, good oral mouth
Explain Buprenorphine role in causing clarity in patients and brightening affect
It is a kappa agonist which leads to this expression
Kappa antagonist would do the opposite of such
Can you overdose on Buprenorphine
Technically no. Although the med at higher doses can decrease respiration, it has not known to cause increase in carbon dioxide retention of the body.
Usually the cases is multiple drug interaction
Which is better: Buprenorphine or the injection of naltrexone
Both seemingly even in effectiveness. The caveat being, we have to get individuals pass the initial stage of detox to start them on an naltrexone injection.
What cytochrome is Buprenorphine metabolized by?
CYP3A4
What does CYP3A4 inducers do to Buprenorphine
It causes it to leave the blood stream a lot quicker
Consequence: withdrawal and cravings
What does CYP3A4 inhibitors do to Buprenorphine
It causes higher levels of the medication
Consequence: Sedation and nausea
Medication to watch out for when administering Buprenorphine
Anything that may cause sedations such as benzos
Think about alcoholism
What happens to receptors if Buprenorphine is used alone
It stays on that receptor
What happens if an opioid agonist follows buprenorphine
Buprenorphine will stay on that receptor. Agonist would have lesser effects
What happens if buprenorphine follows an opioid agonist
Buprenorphine will displace that agonist leading to precipitated withdrawals
What happens if buprenorphine is followed by an Opioid antagonist
Not much. Buprenorphine will remain on that receptor.
Antagonist will work slower leading to precipitated withdrawals
FDA recommendations when treating a patient with Buprenorphine, If they are in fact on a benzo
We should still give them it as it has not shown to cause over doses at therapeutic dose range.
Rationale: Overdosing on Opioids is a much more adverse event
Response: Educate, potentially taper the Benzo or CNS depressant, Verify the dx of the patient for taking these medications.
When to initiate Naltrexone when opioid free:
7 - 10 day wait period
Why is long acting injectable considered better option than oral Naltrexone
Better adherence with long acting
Lower risk of relapse
lower risk of overdose
Potential side effects after initiation of naltrexone injection
Subacute withdrawal but usually recovers after a week.
Pain at injection site
