Buprenorphine SR-LAB - 5ml-1mg/ml
ZooPharm can provide sustained release Buprenorphine SR-LAB by prescription in a patented, sustained release system.
Buprenorphine SR-LAB releases over 72 hours and provides blood levels greater than 1.0 nanogram/ml in rodents for post operative analgesia.
Buprenorphine has produced excellent analgesic results in broad clinical applications for laboratory animals. It provides analgesia for management of perioperative / postoperative pain, as well as, tissue inflammation due to infection, tissue necrosis and trauma resulting from wounds. Amelioration of postsurgical pain has been substantiated in a variety of species. Due to its long duration of action, it is one of the most widely used opioid analgesics in laboratory animal medicine.
Buprenorphine is a thebaine derivative with powerful analgesia approximately twenty-five to forty times as potent as morphine. Its analgesic effect is due to partial agonist activity at -opioid receptors, i.e., when the molecule binds to a receptor, it is only partially activated 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. Its chemical name is 17 -(cyclopropylmethyl)-alpha-(1, I-dimethylethyl)-4,5-epoxy-1819-dihydro-3-hydroxy-6-methoxy-alpha -methyl-6, 14-ethenomorphinan-7 -methanol.
Buprenorphine is metabolized by the liver, via CYP3A4 (CYP2C8 seems to also 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.4 Buprenorphine's main active metabolite, norbuprenorphine, is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, with a κ-opioid receptor partial agonist. Buprenorphine antagonizes norbuprenorphine’s effects.
A published study in the Journal of the American Association for Laboratory Animal Science, tested this sustained-release formulation of buprenorphine in rats for analgesic efficacy and plasma concentration over a 72-h time period. Rats were injected subcutaneously with either 1.2 mg/kg sustained-release formulation (Bup-SR), or 0.2 mL/kg buprenorphine HCl (Bup-HCl) and tested in a thermal nociception model or a surgical postoperative pain model.2
In another published rat study using an incisional pain model, findings indicated that Bup-SR at 0.3 mg/kg or 1.2 mg/kg SC is effective in minimizing hypersensitivity with minimal sedation for at least 48 h (thermal hypersensitivity) and 72 h, respectively.3
Results in these models, showed evidence of Buprenorphine-SR providing analgesia for 2 to 3 d, reporting plasma concentrations of buprenorphine remaining over 1 ng/mL for 72 h after a single dose.
Buprenorphine SR-LAB is available from ZooPharm upon prescription at a concentration of 1 mg/ml in a 5 ml vial in a sustained release biodegradable matrix.
The recommended dose rates in rodent species [for a single, 72-hour SC injection] are as follows: Laboratory Rats§: 1.0 - 1.2 mg/kg; Laboratory Mice§: 0.5 – 1.0 mg/kg
These dose rates above have been determined based on daily dosing guidelines in published formulary, clinical research experience and formal studies. If administering Buprenorphine SR for the first time, it is suggested that initial dose determination be based on lowest dosing recommendations. Practitioners and clinicians should rely on their professional knowledge and judgment when prescribing Buprenorphine SR-LAB
While this novel Buprenorphine SR Lab formulation has been developed to eliminate the majority of injection site reactions in most rodent strains, skin reactions may occur in select strains. In the cases where such adverse events occur, we recommend that you discontinue use of the Buprenorphine SR Lab.
1. Roughan JV and Flecknell PA. 2002. Buprenorphine: a reappraisal of its antinociceptive effects and therapeutic use in alleviating post-operative pain in animals. Lab Anim 36:322-343.
2. Foley PL; LiangH; Crichlow AR Evaluation of a sustained release formulation of buprenorphine for analgesia in rats. JAALAS Vol 50, No 2, March 2011, 198–204
3. Chum, H. H. et al. Antinociceptive effects of sustained-release buprenorphine in a model of incisional pain in rats (Rattus norvegicus). J. Am. Assoc. Lab. Anim. Sci. 53, 193–7 (2014).
4.Moody DE; Fang Lin SN; Weyant DM; Strom SC and Omiecinski CJ Effect of Rifampin and Nelfinavir on the Metabolism of Methadone and Buprenorphine in Primary Cultures of Human Hepatocytes. Drug Metab Dispos December 2009 37:2323-29
5. Published Formulary reference sources: Flecknell & Jenkins (1985); Flecknell (1996); UCSF Lab Animal Guidelines (2012); IACUC Pain Management Committee (1992);