ETHAMOLIN- ethanolamine oleate injection, solution
QOL Medical, LLC.
DESCRIPTION
ETHAMOLIN� (Ethanolamine Oleate) Injection is a mild sclerosing agent. Chemically it is C17 H33 COOH�NH2 CH2 CH2 OH. It has the following structure:
Ethamolin Structure
(click image for full-size original)
The empirical formula is C20 H41 NO3 , representing a molecular weight of 343.55.
ETHAMOLIN Injection consists of ethanolamine, a basic substance, which when combined with oleic acid, forms a clear pale-yellow to straw-colored, deliquescent oleate. The pH ranges from 8.0 to 9.0.
ETHAMOLIN Injection is a sterile, apyrogenic, aqueous solution containing in each mL approximately 50 mg of ethanolamine oleate with benzyl alcohol 2% by volume as preservative.
CLINICAL PHARMACOLOGY
When injected intravenously, ETHAMOLIN Injection acts primarily by irritation of the intimal endothelium of the vein and produces a sterile dose-related inflammatory response. This results in fibrosis and possible occlusion of the vein. ETHAMOLIN Injection also rapidly diffuses through the venous wall and produces a dose-related extravascular inflammatory reaction.
The oleic acid component of ETHAMOLIN Injection is responsible for the inflammatory response, and may also activate coagulation in vivo by release of tissue factor and activation of Hageman factor. The ethanolamine component, however, may inhibit fibrin clot formation by chelating calcium, so that a procoagulant action of ETHAMOLIN has not been demonstrated.
After injection, ETHAMOLIN disappears from the injection site within five minutes via the portal vein. When volumes larger than 20 mL are injected, some ETHAMOLIN also flows into the azygos vein through the periesophageal vein. In human autopsy studies it was found that within four days after injection there is neutrophil infiltration of the esophageal wall and hemorrhage within six days. Granulation tissue is first seen at ten days, red thrombi obliterating the varices by twenty days, and sclerosis of the varices by two and a half months. The time course of these findings suggests that sclerosis of esophageal varices will be a delayed rather than an immediate effect of the drug.
The minimum lethal dose of ETHAMOLIN Injection administered intravenously to rabbits is 130 mg/kg.
In dogs, ETHAMOLIN injected into the right atrium at a dose of 1 mL/kg over one minute has been shown to increase extravascular lung water. The maximum recommended human dose is 20 mL, or 0.4 mL/kg for a 50-kg person. The concentration of ETHAMOLIN reaching the lung in human treatment will be less than in the dog studies, but pleural effusions, pulmonary edema, pulmonary infiltration and pneumonitis have been reported in clinical trials, and minimizing the total per-session dose, especially in patients with concomitant cardiopulmonary disease, is recommended (see PRECAUTIONS).
Ethamolin Indications and Usage
ETHAMOLIN Injection is indicated for the treatment of patients with esophageal varices that have recently bled, to prevent rebleeding.
ETHAMOLIN is not indicated for the treatment of patients with esophageal varices that have not bled. There is no evidence that treatment of this population decreases the likelihood of bleeding.
Sclerotherapy with ETHAMOLIN has no beneficial effect upon portal hypertension, the cause of esophageal varices, so that recanalization and collateralization may occur, necessitating reinjection.
