Poloxamer 188 as vehicle for injectable diazepam. 1980

A V Prancan, and B Ecanow, and R J Bernardoni, and M S Sadove

The significant occurrence of thrombophlebitis in patients administered diazepam intravenously was described recently. This side effect has been attributed to the crystallization of diazepam and its subsequent precipitation upon contact with blood or intravenous fluids. The current study was designed to reveal whether the solubilizing capability of poloxamer 188 reduces the incidence of thrombotic and inflammatory effects of diazepam in rabbits. The incidence of early (3-hr) ear vein necrosis was 72% in the diazepam-treated ears, while the incidence of necrosis in the ears that received poloxamer 188 as a vehicle for diazepam was 25%. The occurrence of thrombosis and loss of vessel integrity also was higher in diazepam-treated ears than in those treated with diazepam plus poloxamer 188. Solubilization of diazepam with poloxamer 188 may decrease the incidence of the tested side effects.

UI MeSH Term Description Entries
D007267 Injections Introduction of substances into the body using a needle and syringe. Injectables,Injectable,Injection
D008297 Male Males
D009336 Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.
D011060 Poloxalene A copolymer of polyethylene and polypropylene ether glycol. It is a non-ionic polyol surface-active agent used medically as a fecal softener and in cattle for prevention of bloat. Oxyethylene Oxypropylene Polymer,Polyoxyethylene Polyoxypropylene Polyoxyethylene Polymer,Bloat Guard,Poloxalene 2930,Proxanol,SK&F-18667,Tergitol,Therabloat,Oxypropylene Polymer, Oxyethylene,Polymer, Oxyethylene Oxypropylene,SK&F 18667,SK&F18667
D011092 Polyethylene Glycols Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS. Macrogols,Polyoxyethylenes,Carbowax,Macrogol,Polyethylene Glycol,Polyethylene Oxide,Polyethyleneoxide,Polyglycol,Glycol, Polyethylene,Glycols, Polyethylene,Oxide, Polyethylene,Oxides, Polyethylene,Polyethylene Oxides,Polyethyleneoxides,Polyglycols,Polyoxyethylene
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D003975 Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,Apaurin,Diazemuls,Faustan,Relanium,Seduxen,Sibazon,Stesolid,Valium
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013924 Thrombophlebitis Inflammation of a vein associated with a blood clot (THROMBUS). Phlegmasia Alba Dolens,Dolens, Phlegmasia Alba,Thrombophlebitides
D013927 Thrombosis Formation and development of a thrombus or blood clot in BLOOD VESSELS. Atherothrombosis,Thrombus,Blood Clot,Blood Clots,Thromboses

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