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Buprenorphine is a semi-synthetic opiate with partial agonist actions at the mu opioid receptor and antagonist actions at other opioid receptors. Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, available generally as Temgesic 0.2 mg sublingual tablets, and as Buprenex in a 0.3 mg/ml injectable formulation. In October 2002, the Food and Drug Administration (FDA) of the United States of America additionally approved Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations for opioid addiction, and as such the drug is now also used for this purpose. In the European Union, Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations were approved for opioid addiction treatment in September 2006. In the Netherlands, Buprenorphine is a List II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. In the USA, it has been a Schedule III drug under the United Nations' Convention on Psychotropic Substances since it was rescheduled from Schedule V just before FDA approval of Suboxone and Subutex. In recent years, buprenorphine has been introduced in most European countries as a transdermal formulation for the treatment of chronic pain.
Commercial preparations
British firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations, no active additives) and Buprenex (parenteral, no active additives). Two more recent formulations from Reckitt Benckiser have been approved for opioid addiction treatment throughout most of the world, instead of Methadone. Subutex (white color, oval shape, bitter, no active additives) and Suboxone (orange color, hexagonal shaped tablet, lemon-lime flavored, one part naloxone for every four parts buprenorphine). Subutex and Suboxone are available in 2 mg and 8 mg sublingual dosages. On October 8, 2009 Roxane laboratories won FDA approval for a generic preparation of Subutex and as of October 23, 2009 announced that it is ready for distribution nation wide in 2 mg and 8 mg sublingual dosages.
In India: Tidigesic-0.2 mg (slow release)or 0.3 mg/mL injectable by Sun Pharmaceuticals;Bupregesic (0.3 mg/mL) by Neon Laboratories; Morgesic (0.3 mg/mL) by Samarth Pharma; Norphin (0.3 mg/mL) Unichem Laboratories.
Suboxone contains buprenorphine as well as the opioid antagonist naloxone to deter the abuse of tablets by intravenous injection. Controlled trials in human subjects suggest that buprenorphine and naloxone at a 4:1 ratio will produce unpleasant withdrawal symptoms if taken intravenously by patients who are addicted to opioids, but has no such effect when taken sublingually. However, the Suboxone formulation still has potential to produce an opioid agonist "high" if injected by non-dependent persons which may provide some explanation to street reports indicating that the naloxone is an insufficient deterrent to injection of suboxone.
A solution for injection (usually by the intramuscular route) is marketed for the British veterinary market by Alstoe Animal Health as Vetergesic , licensed for analgesia and sedation in dogs.
Since 2001 buprenorphine is also available transdermally as 35, 52.5 and 70 mcg per hour transdermal patches that deliver the dose over ninety-six hours. This application form is marketed as Transtec in most European countries by Grunenthal (Napp Pharmaceuticals in the UK, Norpharma in Denmark) for the treatment of moderate to severe cancer pain and severe non-cancer pain not responding to non-opioids. Moreover, a new 5, 10 and 20 mcg per hour patch is marketed as Butrans or Norspan , a once-weekly patch for severe chronic pain not responding to non-opioids, marketed by Napp Pharmaceuticals Ltd., and Mundipharma and Grunenthal respectively.
A novel implantable formulation of buprenorphine (Probuphine), using a polymer matrix sustained-release technology, has been developed to offer treatment for opioid dependence while minimizing risks of patient noncompliance and illicit diversion.
In addition a new formulation of Buprenorphine is being developed using Biodelivery Sciences FDA Approved BEMA (BioErodible MucoAdhesive)technology and will be developed both for acute pain conditions such as postoperative pain and chronic pain conditions such as low back, osteoarthritis, and neuropathic pain.
Pharmacology and pharmacokinetics
Buprenorphine is a thebaine derivative with powerful analgesia approximately twenty-five to forty times as potent as morphine, and its analgesic effect is due to partial agonist activity at μ-opioid receptors, i.e., when the molecule binds to a receptor, it is less likely to transduce a response in contrast to a full agonist such as morphine. Buprenorphine also has very high binding affinity for the μ receptor such that opioid receptor antagonists (e.g. naloxone) only partially reverse its effects. These two properties must be carefully considered by the practitioner, as an overdose cannot be easily reversed. Overdose is unlikely in addicted patients or people with tolerance to opioids who use the drug sublingually as meant in the case of Subutex/Suboxone, especially if there is no alcohol involved. Concomitant use of alcohol with any opioid increases the risk of overdose. One French study showed a higher incidence of fatal overdose in patients who injected both buprenorphine and benzodiazepines, specifically, temazepam, together. Buprenorphine can be safely taken with prescribed benzodiazepines at normal dosage, as long as the patient is tolerant to either opioids or benzodiazepines, and the drugs are taken in the dosages prescribed and by the route of administration prescribed, and not injected. Use in persons physically dependent on full-agonist opioids may trigger opioid withdrawal that also cannot be easily reversed and can last over twenty-four hours, as the drug's mean half-life is thirty-seven hours.
Buprenorphine is also a κ-opioid receptor antagonist, and partial/full agonist at the recombinant human ORL1 nociceptin receptor.
Buprenorphine hydrochloride is administered by intramuscular injection, intravenous infusion, via a transdermal patch, as a sublingual tablet or an ethanolic liquid oral solution. It is not administered orally, due to very high first-pass metabolism.
Buprenorphine is metabolised by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N -dealkylation). The glucuronidation of buprenorphine is primarily carried out by UGT1A1 and UGT2B7, and that of norbuprenorphine by UGT1A1 and UGT1A3. These glucuronides are then eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20–73 hours (mean 37). Due to the mainly hepatic elimination, there is no risk of accumulation in patients with renal impairment.
Buprenorphine's main active metabolite, norbuprenorphine, is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, as well as a and a κ-opioid receptor partial agonist.
Plasma concentrations after application of transdermal buprenorphine increase steadily and the minimum effective therapeutic dose (100 pg/ml) is reached at eleven hours and twenty-one hours for a single 35 and 70 μg/h patch, respectively. Peak plasma concentration (Cmax) is reached in about sixty hours (305 and 624 pg/ml for the 35 and 70 μg/h strength patch, respectively), and is markedly longer than with 0.3 mg intravenous buprenorphine (0.41 hours). Transdermal buprenorphine has a half-life of approximately thirty hours, and a bioavailability of approximately 50%, which is comparable to sublingual buprenorphine.
Clinical use
Indications
Pain indications
Depending on the application form, buprenorphine is indicated for the treatment of moderate to severe chronic pain (pain that has outlived its use to prevent injury and after three months) or for peri-operative analgesia. For the treatment of chronic pain, the transdermal formulations (not currently available in the U.S.A and Canada as of January 2010) are nowadays preferred, which can be used both for chronic cancer pain as well as chronic non-malignant pain, such as musculosceletal and neuropathic pain. The intravenous formulation is mainly used in postoperative pain (for example, as patient controlled analgesia (PCA)) and the sublingual formulation is, for example, used as breakthrough medication for patients with basic transdermal treatment. Advantages of buprenorphine in the treatment of chronic pain are, from a clinical perspective, its relatively long half-life, the option of sublingual and transdermal application and the excellent safety profile (ceiling effect for respiratory depression, lack of immunosuppressive effect, low pharmacokinetic interaction potential, no accumulation in renal impairment). Although not enough western literature is available, use of inj. buprenorphine in 'spinal' anaesthesia is rising in countries like India. Up to 150 micrograms of the drug (0.5 ml) of the preservative free solution is added to the local anaesthetic bupivacaine, and a smoother analgesia is obtained with the benefit of the patient remaining pain-free until up to eight to ten hours of the spinal being given.
Antidepressant potential
A clinical trial conducted at Harvard Medical
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