Deoxycholic Acid Injection - Get Away With That Double Chin

Overview

Deoxycholic acid is a bile acid that helps in the emulsification of the dietary fats in the intestine. Deoxychyouolic acid injection is an artificial form of the acid found in the body that helps in the absorption of fats. However, when injected subcutaneously, it damages the cell membrane of the fat cells.

In April 2015, Deoxycholic acid was approved by the FDA (Food and Drug Administration) for the treatment of submental fat or double chin to improve the appearance by reducing facial fullness. It is marketed by Kythera Biopharma and is the 1st drug for submental fat reduction.

How Does Deoxycholic Acid Injection Work?

Deoxycholic acid injection emulsifies the fat in the intestine. When injected, it stimulates the breakdown of fat cells (adipocytes) and tissues by disrupting their cell membranes and causing adipocytolysis (breaking down of fat cells). This leads to inflammatory reaction and clearing of the adipose tissue residue by the macrophages. The action of Deoxycholic acid is reduced by proteins such as albumin and other tissue-associated proteins; thus, its effect is limited to the protein-less subcutaneous fat tissue. The tissues which are protein-rich such as the muscles and skin, are not affected by Deoxycholic acid, making it safe to use.

Uses of Deoxycholic Acid Injection:

Deoxycholic acid is indicated for the following -

• As emulsifiers in the food industry.

• To dissolve and prevent the formation of gallbladder stones.

• It is under research to be used as a biological detergent.

• In mesotherapy, to produce lipolysis.

• As an injection to reduce the submental fat (double chin).

Limitations

The safety and efficacy of Deoxycholic acid injection for the treatment of subcutaneous fat apart from the submental region have not been confirmed and are not recommended as well.

Dosage Restrictions:

1. Route of Administration - Subcutaneous injection.

2. Dosage Strengths - Deoxycholic injection is 10 mg/mL and is used as an area-adjusted dose of 2 mg/cm square.

• A single treatment comprises a maximum of fifty injections, 0.2 mL each, distributed 1 cm apart.

• Around six single treatments are to be administered at 1-month-apart intervals.

3. Dosage Forms - Deoxycholic acid is a clear, colorless solution free of any particulate matter supplied in 2 mL vials for single-patient use. Each milliliter of the solution contains ten milligrams of Deoxycholic acid.

Special Considerations:

• Pregnancy - No comprehensive data on administering Deoxycholic acid injections in pregnant women is present regarding the drug-associated risk. However, the risk of congenital disabilities in the United States population was two to four percent, and miscarriages were around 15 to 20 percent of clinically recognized pregnancies. Therefore, it might be related to maternal toxicity, as seen in animal reproduction studies involving rats and rabbits.

• Lactation - No data is available suggesting the presence of synthetic Deoxycholic acid in human milk, the effects of the drug on infants, and milk production.

• Pediatric - The use of Deoxycholic acid in kids below eighteen years of age has not been studied. Deoxycholic acid is not supposed to be used in kids or adolescents.

• Geriatric - The selection of doses for elderly individuals should be made carefully, starting from the lowest dose.

Contraindications:

The Deoxycholic acid injection is contraindicated in case of an infection at the injection site.

Warnings and Precautions:

• Marginal Mandibular Nerve Injury - Marginal mandibular nerve injury exhibiting an asymmetric smile or weakness of the facial muscles has been reported during clinical trials. To avoid nerve injury, the injection should not be injected near the marginal mandibular branch of the facial nerve. These injuries were found to resolve on their own.

• Dysphagia: Difficulty in swallowing occurs at the site of administration reactions, causing pain, swelling, and hardening of the submental area. Deoxycholic acid injection should be avoided with past or present history of dysphagia as it may exaggerate the condition.

• Injection Site Hematoma/Bruising - Certain individuals treated with Deoxycholic acid injection experienced hematoma or bruising. The drug should be cautiously used in individuals with bleeding abnormalities or who are under antiplatelet or anticoagulant therapy, as this may lead to excessive bleeding during treatment.

• The Risk of Injecting Near Vulnerable Anatomic Structures - Deoxycholic acid should not be injected into or adjacent to salivary glands, lymph nodes, and muscles.

• Injection Site Alopecia - Alopecia has been reported with the administration of Deoxycholic acid injection. The onset and adverse reaction may differ from individual to individual.

• Necrosis and Ulcerations - Superficial injections might lead to skin ulcerations and necrosis. The drug should not be administered into the affected area until complete resolution.

For Patients:

What Is Submental Fullness?

Submental fullness, also known as double chin, refers to the fat in the submental region or the region under the chin and the front of the neck. Submental fat deposits with age, genetic predisposition, and obesity. It does not appeal aesthetically, adversely impacting psychology. The fat deposited in these areas is stubborn and unresponsive to diet and exercise alone. It is assessed by doctors with the help of a clinician-reported submental fat rating scale (CR-SMFRS).

Why Is Deoxycholic Acid Injection Prescribed for Submental Fullness?

The Deoxycholic acid injection is prescribed to improve the appearance of an individual with moderate to severe submental fat. It is a class of cytolytic medications which works by fat cell breakdown in the fatty tissues.

Facts One Should Know About Deoxycholic Acid Injection:

Deoxycholic acid is a clear, colorless solution free of any particulate matter supplied in 2 mL vials for single-patient use. Each milliliter of the solution contains 10 milligrams of deoxycholic acid.

How Is Deoxycholic Acid Injection Given?

A doctor injects the medication subcutaneously (under the skin). The doctor chooses the appropriate site to inject the medication to treat the condition. One might undergo around six sessions of the treatment, all spaced one month apart, depending on the condition and response of the individual.

What Should One Discuss With the Doctor Before Beginning Deoxycholic Acid Injection?

Before receiving the injection:

• The doctor should be aware if one is allergic to Deoxycholic acid or other medications.

• Inform the doctor about the other medications, vitamin supplements, nutritional supplements, and herbal products one is taking. Particular mention of medications such as anticoagulants or blood thinners, antiplatelet medications, and Aspirin should be made without fail.

• Inform the doctor about the presence of swelling or infection at the injection site to avoid injecting at the infected site.

• The doctor should be informed in case of any past cosmetic surgeries of the face, neck, or chin and any medical conditions of the face or neck.

• Inform the doctor in case of pregnancy or planning to conceive.

Is Deoxycholic Acid Injection Safe?

The Deoxycholic acid injection is safe but may cause side effects in certain individuals.

Is Deoxycholic Acid Injection Effective?

Studies have shown that Deoxycholic acid effectively treats localized fat deposits of the submental region.

What Side Effects Can One Expect With Deoxycholic Acid Injection?

Side effects associated with Deoxycholic acid injection include:

• Pain, bleeding, swelling, numbness, or bruising at the injection site.

• Hardness at the site of injection.

• Itching.

• Headache.

• Nausea.

Severe side effects include:

• Difficulty in swallowing.

• Tightness in the face or neck.

• Uneven smile.

• Weakness of the facial muscles.

Can One Stop Taking Deoxycholic Acid Injection Without the Doctor’s Approval?

The injection should be administered by a doctor and should not be stopped without their consent.

Are There Any Dietary Restrictions to Consider When Taking Deoxycholic Acid Injections?

A normal diet can be continued unless the doctor advises otherwise.

How To Store Deoxycholic Acid Injection?

The Deoxycholic acid injection vials should be stored at 20 to 25 degrees Celsius.

How To Dispose of Deoxycholic Acid Injection?

Each vial of Deoxycholic acid injection is for single-patient use only, after which the vial and injection should be discarded.

What To Do in Case of Overdose?

Excess doses of Deoxycholic acid injection might increase the risk of adverse reactions. However, the health coordinator should be contacted immediately in case of severe side effects.

For Doctors:

Indications -

• Deoxycholic acid is an indication of the following:

• As emulsifiers in the food industry.

• To dissolve and prevent the formation of gallbladder stones.

• It is under research to be used as a biological detergent.

• Mesotherapy (a therapy used to rejuvenate the skin) produces lipolysis (breakdown of lipid cells).

• As an injection to reduce the submental fat.

What Is the Pharmacology of Anastrozole?

Description -

The Deoxycholic acid injection is a clear, colorless, sterile solution for subcutaneous use. It consists of a cytolytic agent, Deoxycholic acid, as an active ingredient. The molecular formula of Deoxycholic acid is C24H40O4; the molecular weight is 392.57 g/mol.

Components -

1. Active Ingredients - 20 milligrams of synthetic Deoxycholic acid.

2. Inactive Ingredients -

• Benzyl alcohol.

• Dibasic sodium phosphate.

• Sodium chloride.

• Sodium hydroxide in water.

• Hydrochloric acid and additional sodium hydroxide are added to adjust the pH to 8.3.

Clinical Pharmacology:

1. Mechanism of Action - The Deoxycholic acid injection is a cytolytic drug. When injected, it destroys the cell membranes of the adipocytes, causing lysis.

2. Pharmacodynamics - Cardiac electrophysiology, Deoxycholic acid injection does not prolong the QTc interval at therapeutic doses.

3. Pharmacokinetics - The levels of endogenous Deoxycholic acid differ from person to person. Most of the drug is sequestered in the enterohepatic circulation loop.

• Mean Cmax - 1024+/- 304 ng/mL.

• Median Tmax - 18 minutes.

(Cmax- Maximum concentration achieved by a drug in the blood, cerebrospinal fluid, or target organ after administration of a dose)

(Tmax- Time taken for a drug to reach maximum concentration after administration of a dose)

A. Distribution-

• Steady-state Plasma Levels- 1.6 fold higher than the steady levels after a single dose.

• Time to Approach Steady-state Levels- Returned to the endogenous range within twenty-four hours.

• Binding to Plasma Proteins- 98 %.

B. Metabolism-

• Endogenous Deoxycholic acid is a product of cholesterol metabolism.

• Deoxycholic acid is not significantly metabolized under normal conditions.

C. Excretion-

• Deoxycholic acid becomes a part of the endogenous bile pool and is excreted along with the endogenous deoxycholic acid.

• Deoxycholic acid is excreted intact in the feces.

Special Considerations:

• Hepatic Impairment - The pharmacokinetics of Deoxycholic acid injection is unlikely to be influenced by hepatic impairment.

• Gender: Deoxycholic acid pharmacokinetics have not been found to be influenced by gender.

Drug Interactions:

• Abciximab - The severity of the side effects is increased when Abciximab is combined with Deoxycholic acid.

• Acenocoumarol - The risk of bleeding and bruising is increased when Acenocoumarol is combined with Deoxycholic acid.

• Acetylsalicylic Acid - The side effects increase when Acetylsalicylic acid is combined with Deoxycholic acid.

What Have Clinical Trials Shown With Regard to Anastrozole?

• Two randomized, multi-center, double-blind, placebo-controlled trials were conducted to evaluate the use of Deoxycholic acid injection in the improvement of the facial appearance associated with submental fat.

• Healthy adults with moderate or severe submental fullness associated with submental fat were enrolled.

• They received up to six treatments with Deoxycholic acid at 1-month intervals.

• The volume of injection was 0.2 mL per injection site, spaced at 1 cm into the submental area, given in 2 mg/cm square doses per area.

• A maximum of one hundred milligrams was allowed over the entire treatment area.

• The individuals were administered an average of 6.4 mL during the first treatment session.

• Those who received all six treatments were administered around 4.4 mL in the sixth session.

Results-

As evaluated by MRI, a greater number of individuals treated with Deoxycholic acid injection had around 10 percent reduction in the submental fat.

Patient Counseling Information:

• The patient should be advised to go through the FDA-approved patient information.

• The patient should be advised to contact the healthcare provider in case of developing any signs of marginal mandibular nerve paresis, difficulty in swallowing, or worsening of the existing side effects.

• The patient should also be advised to contact the healthcare provider in case of the development of open sores or drainage from the treatment site.

Administration Instructions -

• A doctor should administer a Deoxycholic acid injection after screening the patients for causes of submental fullness, such as thyromegaly and cervical lymphadenopathy.

• Cautious injection administration in patients with skin laxity, prominent platysmal bands, or other conditions in which submental fat reduction might result in unaesthetic results.

• Cautious administration in patients with past surgeries or cosmetic treatments of the submental area.

• The presence of scar tissue might impact the safe administration of Deoxycholic acid injection.

• The vials should be inspected for the presence of particulate matter or discoloration. Discard the vial in case of color change or the presence of particulate matter.

• Discard the vial after use.

• Use each vial for a single patient without dilution.

Complications or Side Effects -

Side effects associated with Deoxycholic acid injection include:

• Pain, bleeding, swelling, numbness, or bruising at the injection site.

• Hardness at the site of injection.

• Itching.

• Headache.

• Nausea.

• Trouble swallowing.

• Tightness in the face or neck.

• Crooked smile.

• Weakness of the facial muscles.

• Nerve injury.

• Hypertension.

• Loss of hair around the treated areas.