dinalbuphine sebacate dinalbuphine sebacate dinalbuphine sebacate (dns), also known as nalbuphine sebacate or as sebacoyl dinalbuphine ester (sde) and sold under the brand name naldebain, is a non-controlled opioid analgesic which is used as a 7-day long-acting injection in the treatment of moderate to severe postoperative pain. dinalbuphine sebacateclinical dataother namesdns; nalbuphine sebacate; sebacoyldinalbuphine; sdn; sebacoyl dinalbuphine ester; sde; lt-1001routes ofadministrationintramuscular injectiondrug classopioid analgesicpharmacokinetic databioavailability• im: 85.4% (relative to nalbuphine)metabolismhydrolysismetabolitesnalbuphineelimination half-life• dns: 83.2 hours (mean absorption time: 145.2 hours)• nalbuphine: 4.0 hoursidentifiers iupac name bisisoquinoline-9-yl] decanedioate cas number311768-81-7pubchem cid9962795chemspider8138394unii464oxx39y6chemblchembl1823241chemical and physical dataformulac52h68n2o10molar mass881.120 g·mol−13d model (jsmol)interactive image smiles c1cc(c1)cn2cc345(cc3(2cc6=c4c(=c(c=c6)oc(=o)ccccccccc(=o)oc7=c8c9=c(c12(9(ccn1cc1ccc1)(o8)(cc2)o)o)c=c7)o5)o)o inchi inchi=1s/c52h68n2o10/c55-35-19-21-51(59)39-27-33-15-17-37(45-43(33)49(51,47(35)63-45)23-25-53(39)29-31-9-7-10-31)61-41(57)13-5-3-1-2-4-6-14-42(58)62-38-18-16-34-28-40-52(60)22-20-36(56)48-50(52,44(34)46(38)64-48)24-26-54(40)30-32-11-8-12-32/h15-18,31-32,35-36,39-40,47-48,55-56,59-60h,1-14,19-30h2/t35-,36-,39+,40+,47-,48-,49-,50-,51+,52+/m0/s1key:aloioagkuoqnid-itcixcfhsa-n the compound is a diester of nalbuphine (nubain) joined via a sebacic acid linker, and acts as a long-lasting prodrug of nalbuphine via slow hydrolysis. it was developed to extend the duration of action of nalbuphine, which has a short duration and requires frequent injections. whereas nalbuphine must be injected every 4 to 6 hours, a single injection of dns lasts for up to 7 to 10 days. it was invented by professor oliver yoa-pu hu (national defense medical center) and codeveloped with lumosa therapeutics. naldebain received market approvals from taiwan fda in march 2017, health sciences authority of singapore in december 2020, the ministry of public health of thailand in december 2021, and the drug control authority of malaysia in 2022. development is ongoing in the united states, china, korea, ukraine, the philippines, and brunei. medical uses naldebain is indicated for the relief of moderate to severe acute postsurgical pain, administered intramuscularly. the product is available in single-use vials; 2 ml single use vial (75 mg/ml) for im injection is packaged in a carton. pack shot of naldebain pharmacology pharmacodynamics nalbuphine, and hence dns, acts as a mixed agonist/antagonist opioid modulator, or more specifically as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor. pharmacokinetics the release mechanism of dinalbuphine sebacate (dns) upon im injection is as follows: the injected naldebain is first forming an oil depot in the muscle the oil depot gradually dispersed to small droplets in the surrounding tissues the prodrug dns diffused out from the surface of oil droplets, and once released, a small portion of the prodrug get hydrolyzed by esterases to release the active ingredient, nalbuphine, in the surrounding tissue cells, while the majority of the prodrug would enter the blood stream through local tissue drainage (e.g., lymph flow) and get hydrolyzed to nalbuphine in the blood.