What: Suboxone = buprenorphine/naloxone. Bupe is a partial agonist(mu) and antagonist(kappa). Bupe has higher mu affinity that most opiates, including some antagonists(naloxone, naltrexone). Its higher affinity allows you to shoot suboxone tablets. It also may cause precipitated withdrawals if you are dependant on other opiates. Also, its higher affinity blocks the affects of other opiates when taken in conjunction with bupe.
Dose: Depends on tolerance. 1-2mgs is a typical recreational dose for someone with no tolerance. If you're using bupe to taper off of another opiate, you should dose once you're experiencing wd's(typically 36-48 hrs. for most opiates). Start with 2-4mgs and dose at 2mg increments every 30-45minutes until a dose holds you. Most people take their full dose once a day.
Withdrawal: Typical physical and psychological symptoms associated with opiate withdrawal. Insomnia, chills, diarrhea, depression, anxiety, lacrimation, sweating, increased heart rate, etc. They are not as strong as a full agonist's symptoms, but may last longer. Physical symptoms last 1-2 weeks on average and psychological symptoms may last months.
As most opiates, it's recommended to taper down to the lowest dose possible before stopping. <1mg is ideal. The best way to dose at that level is to crush up a tablet and divide the powder into lower doses.
Ceiling: 24-32mgs
Bioavailability:
jasoncrest said:
Buprenorphine bioavailabilities:
intraduodenal: 9.7%
intrahepatoportal: 49%
intramuscular: 68%
"The observed mean intramuscular bioavailability was 68%"
"Studies of buprenorphine bioavailability have also examined the intramuscular (bioavailability, 50%–100%)"
intranasal: 50%
"Studies of buprenorphine bioavailability have also examined the [...] intranasal (bioavailability, 48%)
"The bioavailability of buprenorphine, HCl (BPP) in sheep after nasal administration of two formulations has been studied. 0.9 mg BPP in 150 microl was administered nasally and compared to 0.6 mg i.v. The test solutions were formulated with 30% polyethylene glycol 300 (PEG 300) and 5% dextrose, respectively. The bioavailability for PEG 300 was 70% (S.D.+/-27%, n=6), whereas the bioavailability for 5% dextrose was 89% (S.D.+/-23%, n=6)."
"Mean intranasal bioavailability was 48.2 +/- 8.35% (mean +/- s.e.m.) of the intravenous value"
intrarectal: 54%
"bioavailability of the drug was found to be: [... ]intrarectal (54%)..."
"Relative to the 100% bioavailability from the intraarterial route the mean bioavailabilities were [...] intrarectal, 54%..."
intravenous: 98%-100%
oral: 10%
"the oral bioavailability for buprenorphine is state to be 10%"
"due to extensive first-pass metabolism, buprenorphine has very poor oral bioavailability (10% of the intravenous route) if swallowed"
sublingual: ~30%
"Buprenorphine is well absorbed sublingually, with 60% to 70% of the bioavailability of intravenous doses"
"Study results indicate that bioavailability of sublingual buprenorphine is approximately 30%"
"Literature on bioavailability of sublingual buprenorphine presents variable numbers ranging from. 19–58% of the administered dose."
"Relative to the 100% bioavailability from the intraarterial route the mean bioavailabilities were [...] sublingual, 13%"
transdermal: 15%
Other Notes:
- Bupe is CIII in the US.
- Metabolized by CYP3A4(see potentiation thread for potentiators).
- Half-life: 37 hours.
- Drug tests: Not detected by regular 5 panel tests.
- A interesting thread by 'medicine cabinet' about a new version of Suboxone that's currently being tested can be found here.
- Buprenorphine gets metabolized into norbuprenorphine and into conjugated buprenorphine and norbuprenorphine.
Images:
Subutex
Suboxone
Generic Subutex Manufacturer: Roxane
Generic 2mg Manufacturer: Teva | Generic 8mg Manufacturer: Teva
Suboxone Film Strips
Temgesic, 0.2mg
Buprenex Ampules
Locate a doctor that prescribes Suboxone.
Suboxone Assistance Program - Free Suboxone for Low Income Patients
