Ethanolamine oleate

1-10%

Esophageal ulcer (2.1%)

Pleural effusion (2.1%)

Pyrexia (1.8%)

Retrosternal pain (1.6%)

Esophageal stricture (1.3%)

Pneumonia (1.2%)

Frequency not defined

Fever

Esophagitis

Sloughing of the mucosa overlying the injected varix

Anaphylactic shock

Acute renal failure (reversible)

Pregnancy Category: C

Lactation: excretion in milk unknown; use with caution

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Mechanism of Action

Sclerosing agent, produces a sterile inflammatory response leading to fibrosis and vein occlusion

Oleic acid is the inflammatory component

Ethanolamine oleate is injected directly into the vein. You will receive this injection in a hospital or emergency setting.

This medication is usually given during a bleeding episode and again at 1 week, 6 weeks, 3 months, and 6 months afterward.

Do not miss any follow-up visits to your doctor.

Since ethanolamine oleate is given by a healthcare professional in an emergency setting, an overdose is unlikely to occur.

Since ethanolamine oleate is given by a healthcare professional in an emergency setting, you are not likely to miss a dose.

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.

When injected intravenously, ETHAMOLIN (ethanolamine oleate) 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 (ethanolamine oleate) Injection also rapidly diffuses through the venous wall and produces a dose-related extravascular inflammatory reaction.

The oleic acid component of the ETHAMOLIN (ethanolamine oleate) 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 (ethanolamine oleate) has not been demonstrated.

After injection, ETHAMOLIN (ethanolamine oleate) disappears from the injection site within five minutes via the portal vein. When volumes larger than 20 mL are injected, some ETHAMOLIN (ethanolamine oleate) 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 (ethanolamine oleate) Injection administered intravenously to rabbits is 130 mg/kg.

In dogs, ETHAMOLIN (ethanolamine oleate) 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 (ethanolamine oleate) 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).

You should not use this medication if you are allergic to ethanolamine oleate or oleic acid (oleo).

Ethanolamine oleate will not treat any underlying liver disease.

If possible before you receive ethanolamine oleate, tell your doctor if you have:

• kidney disease;
• heart disease; or
• lung disease.

FDA pregnancy category C. It is not known whether ethanolamine oleate will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

It is not known whether ethanolamine oleate passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

In an emergency situation it may not be possible before you are treated with ethanolamine oleate to tell your caregivers if you are pregnant or breast feeding. Make sure any doctor caring for your pregnancy or your baby knows you have received this medication.

You should not use this medication if you are allergic to ethanolamine oleate or oleic acid (oleo).

Ethanolamine oleate will not treat any underlying liver disease.

If possible before receiving this medication, tell your doctor if you have kidney disease, heart disease, or lung disease.

In an emergency situation it may not be possible before you are treated to tell your caregivers about your health conditions or if you are pregnant or breast feeding. Make sure any doctor caring for you afterward knows that you have received this medication.

Serious side effects of ethanolamine oleate include severe pain or burning in your upper stomach, stabbing chest pain, feeling short of breath, fever, chills, cough with yellow or green mucus, or cough or hiccups (may be a sign of fluid buildup around the lungs).

Applies to ethanolamine oleate: injectable solution

Get emergency medical help if you have any of these signs of an allergic reaction while taking ethanolamine oleate: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Tell your caregivers at once if you have a serious side effect such as:

• cough or hiccups (may be a sign of fluid buildup around the lungs);

• fever, chills, cough with yellow or green mucus;

• stabbing chest pain, feeling short of breath; or

• severe pain or burning in your upper stomach.

Less serious side effects of ethanolamine oleate may include:

• low fever; or

• trouble swallowing.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Consider the lowest possible effective dose in patients with severe hepatic dysfunction (Child Class C).