Ethanolamine Oleate - Indications, Pharmacology, Warnings, and Precautions

Overview:

Ethanolamine oleate is an effective choice for those with esophageal varices. In esophageal varices, the veins in the lower esophagus may swell up, possibly due to excess blood volume pushed through the tiny vessels in the esophagus that are not basically apt for taking up high blood load. Ethanolamine oleate is injected into these esophageal varices, and therefore, it can only be done through the endoscopic technique. The United States Food and Drug Administration (US FDA) has approved and licensed Ethanolamine oleate for its use in esophageal varices. Though Ethanolamine oleate’s role in esophageal varices has been discussed since 1937, the FDA approval came out only in 1988. The FDA approved it only after ensuring all the positive and negative aspects associated with the medicine.

Drug Group:

The sclerosing agent is Ethanolamine oleate’s drug group.

Available Doses and Dosage Forms:

Injection solution is the dosage form in which Ethanolamine oleate has to be used in esophageal varices. The dosage strength of the injection solution is five percent.

For Patients:

How Does Ethanolamine Oleate Work for Esophageal Varices?

Ethanolamine oleate is employed for esophageal varices as a remedy to seal off the bleeding that the esophageal varices have caused. That is accomplished because of the sclerosing property of the Ethanolamine oleate, which means that Ethanolamine can cause irritation in the esophageal veins upon introduction into them. The irritation can cause the vein to occlude, and as a result, the blood flow through it diminishes and even stops. By doing this, the bleeding from the esophageal varices can also be stopped and sealed off.

What Is the Dosage of Ethanolamine Oleate?

The dosage of Ethanolamine oleate for esophageal varices is based on the number of varices that are present in the patient’s esophagus. For each varix, the Ethanolamine oleate dose must be somewhere between 1.5 to five milliliters. The concerned doctor may decide on what dose has to be given precisely; slight variations must be there from patient to patient.

How Effective Is Ethanolamine Oleate?

Ethanolamine oleate is an appreciably effective remedy for esophageal varices. The active bleeding that often happens with esophageal varices can be promptly controlled with this medicinal agent. It is the best choice for closing the esophageal varices bleeding for a short period. However, there are possibilities for re-bleeding over time, and therefore, the long-term potential for this medicine is not that appreciable, and it often needs multiple sessions. The potential of Ethanolamine oleate to cause irritation is much superior to that of other sclerosing agents, and that is why it is often preferred. But at the same time, this added efficacy often comes at the cost of added side effects that are normally not present with other sclerosing agents. Therefore, it is often used when other choices fail to bring off the required outcome.

What Are the Things to Inform the Doctor Before Taking Ethanolamine Oleate?

Before using Ethanolamine oleate, it is better to have a thorough and transparent discussion with the concerned doctors. This discussion often helps the doctor identify the risks and take precautions to ensure the safety of patients while on it.

• Allergy to Ethanolamine oleate or other sclerosing agents, if any.

• Allergy to any medicines has been noted in the past.

• Diseases other than esophageal varices.

• Surgeries or treatment procedures done lately.

• Daily or regular medications, if any.

• Daily health supplements or plant-based supplements.

• Pregnancy status and future plans, if planning for recent pregnancy.

• Breastfeeding status.

How Is Ethanolamine Oleate Administered?

Administering Ethanolamine oleate is achieved through a special technique called endoscopy, in which a flexible tube (endoscope) is delivered through the body opening. This tube has an embedded camera that makes it possible for the doctors to see the inside organs and structures. For esophageal varices, the Ethanolamine oleate has to be injected into the varices that are situated in the esophagus, which is made possible through endoscopic technique. Therefore, it can only be done by trained healthcare personnel who are well-versed with this technique.

What Are the Side Effects of Ethanolamine Oleate?

• Fever of low grade.

• Burning or discomfort in the upper gut region.

• Chest pain.

• Shortness of breath.

• Swallowing issues.

• Ulcer in the esophagus.

• Esophageal puncture or perforation.

• Facial swelling.

• Skin rashes.

• Pneumonia (lung infection).

• Esophageal stricture (constriction of the esophagus passage).

• Chest cavity inflammation.

Dietary Considerations:

Try to have foods that are soft so that the irritation in the esophagus does not worsen further. These soft foods are also easy to swallow, so even if there are swallowing issues, they can go in without much effort or issues. Keep a limit on the spice level of the food; better avoid spicy foods as they can worsen the esophageal irritation. Similarly, do not take crunchy food items or hard and abrasive snacks, as these can cause more irritation and will not let the irritation subside.

Missed Dose:

Ethanolamine oleate is administered only in a medical setting and never at home. It can also be done by medical personnel, and the patient cannot take it by themselves. That is why it is always said that the missing dose of Ethanolamine oleate is quite rare, unlike other medicines that are taken by patients themselves.

Overdose:

When Ethanolamine oleate is injected into the varices in large quantities that are not considered apt and appropriate for the patient’s age, then there could be overdosing issues. However, medical professionals are always keen on it and keep track of the dose that they are using, and that is why the scope for such overdose events is said to be minimal.

Storage:

The most appropriate temperature setting for Ethanolamine is considered to be 59 to 86 degrees Fahrenheit. The Ethanolamine oleate injection solution is supplied in glass ampules, and each of these ampules is meant for single use only.

For Doctors:

Indication:

Esophageal varices (actively bleeding).

Dose:

1.5 to five milliliters (ml) of the Ethanolamine oleate injection solution is the preferred dose for each varix. So, the total dose of Ethanolamine oleate that a person receives is based on how many varices the person has, which is often confirmed by the doctor through the endoscopy technique.

Since Ethanolamine oleate is used to control the bleeding from the varices, its therapy is employed only during acute bleeding. At the time of acute bleeding, one week later, six weeks later, three months later, and six months later are the regular intervals that have to be kept between each injection.

Though the total dose is based on the number of varices, there is a cut-off dose for Ethanolamine oleate, which is estimated as 20 milliliters. Administering more than the cut-off dose can be harmful to the person and might bring off grave overdosing issues.

What Are the Pharmacological Aspects of Ethanolamine Oleate?

1. Mechanism of Action: The intimal layer of the esophageal vein gets irritated by the injected Ethanolamine oleate solution, and it is this irritation in the intima that turns on the inflammatory response. Because of this inflammation, the intimal layer develops scarring over time, and eventually, it leads to fibrosis.

Fibrotic changes and scarring in the vascular intima potentially occlude and seal off the vein. That is how Ethanolamine oleate manages and chokes the active esophageal bleeds that the varices have induced. However, it does not mean that Ethanolamine oleate can immediately shut off the bleeding, unlike other medicines that bring out its action in a few hours. Though the initial body response to Ethanolamine oleate is quite immediate, it takes time to induce fibrosis, which is at the end of an array of processes.

2. Pharmacodynamics: The inflammatory response that develops with Ethanolamine oleate is primarily because of the oleic acid, and it may also turn on the Hageman factor and even promote the liberation of tissue factor. Both of these trigger the coagulation pathway. However, Ethanolamine, the key component in Ethanolamine oleate, may chelate with the calcium ions and thereby prevent and block the development of fibrin clots, and that is how its ability to induce coagulation is managed.

3. Pharmacokinetics: Once the Ethanolamine oleate is injected into the varices, its actions are mostly restricted within that region where it is injected. That is why there is only limited systemic exposure to Ethanolamine oleate, and so are the systemic adverse outcomes. If the medicine gets into the systemic circulation, it will immediately be processed in the liver, where it is fragmented into smaller integrants. These products are then eliminated through the renal pathway; however, all these pharmacokinetic aspects are only for the drug portion that gets into the systemic circulation.

Warnings and Precautions:

Ethanolamine oleate is just made for esophageal varices, and its application in leg varicosities has not been investigated very deeply; therefore, not all its outcomes are known to date. Ethanolamine oleate may bring anaphylactic reactions, and there are reports of such happenings. Therefore, while having the sclerotherapy using Ethanolamine oleate, the patient must be monitored; any sign of anaphylaxis must be paid attention and appropriate medical management should be undertaken whenever needed. Acute renal failure instances may also happen with ethanolamine oleate, and the possibilities must be therefore assessed in advance.

Ethanolamine oleate can also cause injection necrosis, and its possibilities are greater when more volume of the agent is used for injection, mainly due to its sclerosing properties. So, always prefer the least effective dose that is appropriate for the person. Apart from necrosis, esophageal perforation and ulcerations are also noted, and these develop when the injection technique is wrong. Therefore, always ensure that the injection is given properly and not submucosally, as all the unwanted outcomes can come up with a submucosal injection of Ethanolamine oleate.

The dose and dosing frequency both must be kept minimal in case the person has cardiorespiratory disease and illnesses. Both should be kept at the lowest possible value. The technique through which the medicine is delivered is also important and ensures that it is correct.

What Are the Contraindications of Ethanolamine Oleate?

Anybody who has ever had an allergic response to the use of Ethanolamine oleate should never be given it again. Even if the allergy was to either Ethanolamine or oleate, then also should not be given.

Toxicity:

There are no reliable toxicity studies conducted on this medicine. Therefore, whether it can cause carcinogenic effects or mutagenic effects is not known or explored. Considering the fact that its actions are mostly limited to the site where it is injected, there are not many possibilities for harmful toxicities when it is used in the right amount through the right technique. Neurotoxic effects may come up when the medicine is injected into a nerve.

Specific Considerations:

Pregnancy

Ethanolamine oleate is generally not for those who are in their pregnancy period. It is given pregnancy category C as per the FDA guidelines. However, it can be considered if the benefit that it can have on the pregnant lady is much more than the possible risks that it could bring out.

Breastfeeding

It is not known whether Ethanolamine oleate can get into the baby’s body through breast milk. Similar is the case with its effect on milk secretion. So, to be on the safer side, it is better not to suggest Ethanolamine for such patients who are lactating.

Pediatric Use

Ethanolamine oleate use in kids and infants is not recommended generally, and there is no evidence to support that it is safe for them. However, under exceptional circumstances, Ethanolamine oleate usage can be considered for pediatric patients and the most important thing is that used only if its benefit is more than the risk that the child will have with its usage.

Geriatric Use

Its usage is generally acceptable for geriatric patients, and most of the outcomes were almost similar to those of an adult one. Therefore, many differences would not be there; however, the possibility of more side effects and complications must be kept in mind as geriatric patients might already have certain health issues that make them more likely to have complications.