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Sublocade is an extended release Buprenorphine product
designed to be injected once a month subcutaneously in the abdominal area
Buprenorphine is and agonist-antagonist of the
Mu opioid receptors and is utilized for pain management, opioid addiction, and off-label
The commonly known name for buprenorphine is
Subutex or Suboxone if it is combined with Naloxone. That medication is used
for opioid use disorder to prevent relapse and withdrawal as a a part of
Medication assisted therapy of addiction.
Buprenorphine is a partial Mu opioid receptor
agonist and an antagonist at the Kappa opioid receptor. This allows the
buprenorphine to stimulate the opioid receptor, for example, to give some pain
relief as a full agonist such as morphine would do, yet it prevents complete
activation thereby preventing a person from getting high.
Buprenorphine-naloxone combination prevents
abuse of the drug by causing the naloxone to be released in the blood if the
medication is injected as some patients with addiction may attempt. Likewise,
if the medication is swallowed, a similar event may happen.
If buprenorphine-naloxone is administered to a
person fully loaded with an opioid such as heroin or oxycodone, the person will
have partial withdrawals as the antagonist part of buprenorphine takes effect,
causing withdrawing effects
The issue with oral mediation assistance for
addiction is that people can choose not to take the medication and relapse.
Success with mediation treatment in addiction can be 90% success if the patient
can maintain, without relapse, the medication program of buprenorphine. On the
other hand, detox without medication results in a 90% relapse rate to addiction
and high level of death from overdose.
Sublocade is produced by indivior, is a straight
buprenorphine product that is injected monthly into the subcutaneous area of
Patient must be on a suboxone and stable at an 8mg-2mg dosing for at least a
week prior to initiating Sublocade injections. (Note: Buprenorphine –naloxone
medication mixtures are dosed in a 4:1 pattern I.e. 8 mg buprenorphine:2mg
naloxone of 4mg buprenorphine:1 mg Naloxone
as examples.) Straight Buprenorphine is
usually used in pregnancy.
Sublocade is a Buprenorphine product in 300 mg
and 100 mg dosing contained in an Atragel slow release compound that allows
monthly injections . The medication is released slowly over a 30 day cycle.
Studies demonstrate that even after a single injection and no further
treatment, the ‘liking index’ for opioids is near 0 after 6 months. This means
there is minimal withdrawal or cravings in most patients if they were to
receive only a single injection.
The medication, once injected, enforces
compliance as it is in a depot formulation. Cravings for opioid are low and
even if you were to inject heroin or another opioid, it would be hard to
override the partial blocking effect of the buprenorphine. This decreases the
chance of overdose by other means of drug use.
Side effects include possible death if injected
into a vein as the Atragel will congeal if it is in the blood stream. Allergic
reaction is unlikely, but possible. Infection is another possibility.
Buprenorphine is safe in pregnancy.
The Sublocade can be removed after injection by
excision of the area within the first 15 days if needed.
If you were to need a surgery, you would require
higher doses of pain medication to overcome the Sublocade.
Sublocade is delivered to a physician office
refrigerated. It is warmed up at the time of injection, given by a 20 G 1 inch