There are multiple forms for buprenorphine (commonly called bupe), and this can prove confusing. Although we may never use most of these formulations in the emergency department, we should be familiar with them.
Sublingual Tablets and Film Strips
This is the primary formulation used in the emergency department and hospital as well as the most common form for those prescribed bupe for the treatment of opioid use disorder (OUD) and for patients who are prescribed bupe for pain. The film strips are preferred by my patients because they dissolve fast and tend to not taste too bitter.
The naloxone is included to prevent drug abusers from crushing the tab or strip and inhaling it or dissolving and injecting the medication. Naloxone has a very poor sublingual (SL) and oral bioavailability (less than 2 percent). However, naloxone has a very high intranasal and IV bioavailability, which is a deterrent to misuse of the medication. Patients and health care providers are often confused by the combination of bupe and naloxone because buprenorphine can precipitate withdrawal in opioid-dependent patients. However, buprenorphine-precipitated withdrawal is a feature of the pharmacology of bupe itself and has nothing to do with the naloxone component of Suboxone. When Suboxone is taken sublingually as intended, the naloxone has no bioavailability and no effect.
Bupe also has poor oral bioavailability—only about 15 percent if swallowed. Furthermore, it is important to remember that bupe tabs or strips must be placed sublingually, not anywhere else in the mouth; it’s not an oral dissolving tablet like ondansetron.
There is also a SL bupe mono-product, the most common brand name of which is Subutex, produced by Indivior, the same company that makes Suboxone. Subutex is only produced in tablet form. It is generally available in 2 mg and 8 mg strengths. Most generic forms are in the same dose formulations as the Suboxone or Subutex products (eg, 8 mg/2 mg or simply 8 mg, respectively).
When is the bupe mono-product indicated instead of the dual product? The most common clinical indication is pregnancy because the safety of routine naloxone exposure during pregnancy remains somewhat in question. However, recent small studies suggest the dual product is safe in pregnancy.1,2
The other common use of Subutex is in clinics, hospitals, etc., where the medication is administered by a nurse and there is no worry it will be crushed and injected. In my clinic and emergency department, we use only the generic mono-product bupe (administered by a nurse) because it is less expensive. We stock 8 mg and 2 mg SL tablets.
Many patients buy bupe, administering their own medication-assisted treatment. When patients speak of treating their symptoms or self-medicating with “strips,” they are usually speaking of 8 mg/2 mg bupe/naloxone film strips. Clearly, bupe does have street value. However, the street value of bupe is far less than that of other prescription opioids.
Injectable Buprenorphine
Buprenex, the common brand of injectable bupe, comes in 0.3 mg/1 mL vials. Bupe is a potent analgesic, and as an analgesic, bupe 0.3 mg IV is equivalent to about 7.5 mg of IV morphine. However, it has a much longer half-life. Of note, although the half-life of bupe as an analgesic is only about eight hours, its half-life when treating OUD is much longer (about 36 hours) but is dose-dependent.
The IV form of bupe is not commonly used in the United States but has been used as an IV analgesic in other parts of the world since the 1980s. The use of injectable bupe is growing in American veterinary medicine. Due to its much higher affinity for the mu receptor, IV bupe has also been used in some emergency departments to reverse acute opioid overdoses.3
Transdermal Buprenorphine Patches
Butrans is the brand name of the transdermal bupe patches used to treat chronic pain. While Butrans may be effective in treating OUD, it is not usually prescribed for OUD, and it has a U.S. Food and Drug Administration (FDA) indication only for chronic pain in the “opioid-experienced” patient. Generally, patients are switched to Butrans patches after developing a tolerance to traditional opioids.
The patches come in dosing strengths of 5, 7.5, 10, 15, and 20 mcg/hour and are changed every seven days. The 10 mcg/hour patch is approximately equianalgesic to 80 mg/day of oral morphine. Note that bupe patches, intended for the opioid-dependent patient, release much fewer mcg/hour of buprenorphine than fentanyl patches do of fentanyl.
Implantable Buprenorphine
Probuphine is a long-term implantable form of buprenorphine that delivers a continuous, stable blood level of bupe for the treatment of OUD. Four implants inserted subdermally in the upper arm (in an office procedure) release a total dose of bupe similar to a daily sublingual 8 mg dose for six months. The dose equivalent of only 8 mg/day SL is lower than the effective dose for most patients treated for OUD with bupe SL. This low equivalent dose along with the cost and the need to obtain insurance approval are factors that prevent more widespread use.
Depot Subcutaneous Buprenorphine
Sublocade is the newest long-acting form of bupe on the market, FDA-approved in late 2017 for treating OUD. This depot form of bupe is injected monthly in 100 mg and 300 mg doses into the abdominal subcutaneous tissue to continuously release a dosage equivalent to 8–24 mg/day of SL bupe. Although more patients with OUD could more easily remain compliant in bupe medication-assisted treatment, the number of patients receiving Sublocade remains low. The cost and the need to obtain insurance approval are factors that prevent more widespread use.
There may be a future role for depot injectable forms of bupe in the emergency department to ensure sustained opioid withdrawal management for patients after discharge from the emergency department or to serve as a longer bridge of sobriety for referral to an opioid addiction treatment clinic.
Read the drug summary for Suboxone.
Dr. Ketcham is medical director of the opioid addiction treatment service via New Mexico Treatment Services in Farmington, co-medical director of EMS agencies of San Juan County, and a staff emergency physician at San Juan Regional Medical Center in Farmington and Los Alamos Medical Center
References
- Debelak K, Morrone WR, O’Grady KE, et al. Buprenorphine + naloxone in the treatment of opioid dependence during pregnancy-initial patient care and outcome data. Am J Addict. 2013;22(3):252-254.
- Nguyen L, Lander LR, O’Grady KE, et al. Treating women with opioid use disorder during pregnancy in Appalachia: initial neonatal outcomes following buprenorphine + naloxone exposure. Am J Addict. 2018;27(2):92-96.
- Zamani N, Hassanian-Moghaddam H. Intravenous buprenorphine: a substitute for naloxone in methadone-overdosed patients? Ann Emerg Med. 2017;69(6):737-739.
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10 Responses to “A Quick Guide to Buprenorphine Products”
November 7, 2019
Linda TrpletteAll I want to know is which is stronger soboxin 8 mg or belbuca 75 mcg
August 24, 2020
AmandaMcg is micrograms and mg is milligrams, mg is more!
October 25, 2020
Cody LehnerWhile that is true, it doesn’t make one medication in milligrams strings than a different medication doses in micrograms. They don’t have the exact same conversion.
January 11, 2020
TDavisIs there a such thing as buprenorphine strips
September 22, 2020
AlexiThere is a form of this medication that comes in a dark orange what feels like plastic. Its not the film. How is this form used? Is it like the films?
September 22, 2020
ALEXII meant to ask my own question. Not reaspond to yours.
July 12, 2020
KevinYes the strips come in 2mg,4mg,8mg and 12mg. The max dose allowed per day is 24mg so depending on your need the doctor will prescribe all the way up to that amount and divide it up such as an 8mg three times a day or a 12mg twice a day.
August 6, 2020
KenWho manufactures the best sublingual buprenorphine tablet product? Meaning one that dissolves and has the best bioavailability. The ones we are using don’t completely dissolve in an hour.
August 28, 2020
Deborah MooreKen is it for pain or addiction. It’s beyond me why the fda seperates it buprenorphine is buprenorphine but anyway look into belbuca.
October 10, 2020
JodyI’m currently on 8mg buprenorphine sl tablets 3x a day but just stumbled onto the knowledge of there being transdermal patches of buprenorphine as well.. im not very good at taking my meds on time, basically remembering only when the sickness creeps over my body that I’m late on my does. ive read there is 5mcg all the way too 20mcg for the transdermal patches.. would this be an option I could potentially ask about? what is the equivalence from an X amount mcg per hr, 7 day transdermal patch to my current 8mg sl tablet, 3x a day does? all I can find is equivalence charts on everything else “opioid” but nothing on the same drug just different in the way its prescribed to be taken.