Edurant (Rilpivirine) – Oral

What Is Edurant?

Edurant (rilpivirine) is an orally administered non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat human immunodeficiency virus type 1 (HIV-1). HIV-1 uses reverse transcriptase to convert its ribonucleic acid (RNA) genetic material into deoxyribonucleic acid (DNA).

By binding to this reverse transcriptase protein, Edurant prevents the virus from replicating, which is making more copies of itself.

Edurant is an HIV treatment option for people with the following characteristics:

• 12 years of age or older
• Weight of at least 77 pounds (35 kilograms)
• HIV treatment-naive (never received any HIV treatment)
• 100,000 HIV-1 RNA copies per milliliter or less
• CD4—a type of immune cell—count of more than 200 cells per millimeter cubed

Although Edurant is an HIV treatment option by itself, it’s typically used in combination with other medications to lower the risk of the virus becoming resistant to treatment.

Edurant is available as an orally administered prescription tablet.

What Is Edurant Used For?

HIV is a virus that attacks the immune system, which is the part of the body that helps fight off infections. Within the first couple of weeks of an HIV infection, many people only experience flu-like symptoms.

In fact, most people with HIV will not have any complaints until they have life-threatening infections and even some cancers due to a severely weakened immune system. This late-stage condition is called acquired immunodeficiency syndrome (AIDS).

In 2019 in the United States, around 1.2 million people who are at least 13 years of age have HIV—with about 160,000 undiagnosed individuals. While there is no cure for HIV, many treatment options provide appropriate medical care and help many people live healthy and long lives.

One of these options is Edurant, which is commonly used in combination with other medications to treat HIV-1.

The Food and Drug Administration (FDA) also approved Edurant to be used short-term with Vocabria (cabotegravir) before switching over to Cabenuva, which is an extended-release injection that contains rilpivirine and cabotegravir.

Cabotegravir is an integrase strand transfer inhibitor (INSTI) that binds to the HIV integrase protein and blocks the HIV DNA from combining with human DNA in infected immune cells. By blocking this step, cabotegravir also prevents the HIV virus from making copies of itself.

In order to switch to the Cabenuva monthly injection, you must meet the following criteria:

• Low amount of HIV-1 RNA of fewer than 50 copies/milliliter from another HIV combination therapy
• No history of an HIV infection resistant to rilpivirine or cabotegravir
• No history of an HIV infection that did not respond to treatment 

Edurant can also be used with Vocabria if you are going to miss a monthly Cabenuva injection at your healthcare provider’s office.

How to Take Edurant

Take Edurant once daily with a meal at the same time every day. If you take Edurant, experts recommend avoiding proton pump inhibitors (PPIs) like omeprazole.

Calcium-, magnesium-, or aluminum-containing antacids, such as Tums, Maalox, or Mylanta, should be taken either two hours before or four hours after Edurant.

H2-blockers, such as the antacid/antihistamine famotidine, should be taken at least 12 hours before or four hours after Edurant.

Storage

Because Edurant is a noncontrolled medication, your healthcare provider may give you refills for up to one year from the originally written date on the prescription. Since your healthcare provider will want to get regular labs from you every few months, your healthcare provider can authorize fewer refills.

When you receive your Edurant prescription from the pharmacy, protect the medication from light. Also, keep the medication at an approximate temperature of 77 degrees F, which is within the room temperature range.

If necessary, however, Edurant can be safely stored between 59 to 86 degrees F for a short period of time.

Before traveling with Edurant, become familiar with your final destination’s regulations. In general, however, keep your medication in the same container from your pharmacy that contains your name on the label. Also, make a copy of your Edurant prescription and keep it with you.

Off-Label Uses

Although Edurant is an HIV treatment option, it’s typically used in combination with other medications to lower the risk of the virus becoming resistant to treatment.

In fact, Edurant is usually found in a combination tablet with emtricitabine and tenofovir. Both emtricitabine and tenofovir are nucleoside reverse transcriptase inhibitors (NRTIs).

Like NNRTIs, NRTI medications also block the reverse transcriptase protein, but they do so in a different way. While the HIV-1 reverse transcriptase tries to convert its RNA into DNA, emtricitabine and tenofovir interfere with this process.

By inserting themselves into the viral DNA, the medications make this DNA useless and prevent the virus from making more copies of itself.

These three medications are available as Complera or Odefsey combination products. Complera is the tenofovir disoproxil fumarate (TDF) version, which is linked with fewer negative effects on cholesterol. Odefsey, on the other hand, has tenofovir alafenamide (TAF), which may have fewer bone and kidney side effects.

The FDA also approved Edurant to be used short term with Vocabria (cabotegravir) before switching over to Cabenuva, which is an extended-release injection that contains rilpivirine and cabotegravir.

Cabotegravir is an integrase strand transfer inhibitor (INSTI) that binds to the HIV integrase protein and blocks the HIV DNA from combining with human DNA in infected immune cells. By blocking this step, cabotegravir also prevents the HIV virus from making copies of itself.

In order to switch to the Cabenuva monthly injection, you must meet the following criteria:

• Low amount of HIV-1 RNA of fewer than 50 copies/milliliter from another HIV combination therapy
• No history of an HIV infection resistant to rilpivirine or cabotegravir
• No history of an HIV infection that didn't respond to treatment 

Edurant can also be used with Vocabria if you are going to miss a monthly Cabenuva injection at your healthcare provider’s office.

What Are the Side Effects of Edurant?

This is not a complete list of side effects, and others may occur. A medical professional can advise you on side effects. If you experience other effects, contact your pharmacist or a medical professional. You may report side effects to the FDA at fda.gov/medwatch or 800-FDA-1088.

As with all medications, Edurant can cause side effects. Tell your healthcare provider about any side effects you experience while taking this medication.

Common Side Effects

Common side effects of Edurant include:

• Depression or mood changes
• Dizziness
• Headache
• Insomnia (trouble falling asleep)
• Nausea
• Rash

Severe Side Effects

Some possible severe side effects with Edurant may include:

• Severe allergic reaction and skin rash: While rash is a common side effect of Edurant, it can be serious. Signs of a severe allergic reaction are breathing difficulties and swelling of the face, lips, mouth, tongue, and throat. If you’re experiencing a rash, skin blisters, or a severe allergic reaction, get medical help right away. 
• Liver toxicity: Edurant can cause worsening liver function. Be on the lookout for jaundice (yellowing of the skin and whites of the eyes), appetite loss, right-sided stomach pain, dark-colored urine, light-colored stools, nausea, and vomiting. If you experience these symptoms, seek immediate medical attention.
• Depression or mood changes: Although depression and mood changes are common Edurant side effects, they can be serious. If you suspect that you’re experiencing depression or changes in your mood, let your healthcare provider know right away.
• Body fat changes: You might notice a redistribution of fat from your face, legs, and arms to your neck, back, breasts, and stomach. If this is happening, talk with your healthcare provider as soon as possible.
• Immune system changes: As you start taking Edurant, your immune system will become stronger again and might begin fighting off hidden infections in your body. Notify your healthcare provider right away if you notice any new symptoms—like inflammation (swelling), which is one of the body’s responses to infections.
  

Long-Term Side Effects

Similar to other HIV medications, Edurant has common side effects of dizziness and nausea. Edurant’s side effects are usually manageable. In fact, when compared to the drug efavirenz—another NNRTI—Edurant might have less worrisome side effects.

Additionally, dual combination HIV therapies—like rilpivirine and cabotegravir—are popular due to their long-term safety.

However, in animal studies, Edurant is linked to abnormal liver growth. Because of the possibility of liver toxicity in humans from rilpivirine, liver impairment might be a long-term side effect of this medication.

Fortunately, your healthcare provider will keep a close eye on your liver and regularly order liver-related labs to prevent liver toxicity problems.

Dosage: How Much Edurant Should I Take?

Modifications

Users should be aware of the following before beginning Edurant:

Pregnant parents: According to available data from the Antiretroviral Pregnancy Registry (APR), a pregnancy exposure registry for pregnant parents taking HIV medications, Edurant isn’t linked to a higher risk of negative effects on the unborn baby.

If you have less than 50 HIV-1 RNA copies/milliliter on Edurant before pregnancy, the manufacturer (Janssen) recommends taking the same dose of 25 milligrams by mouth every day with food. Since there is a possibility of less Edurant in the body during pregnancy, however, the manufacturer also recommends that healthcare providers closely monitor the number of HIV-1 RNA copies.

If you are pregnant, consider registering for the APR. Your healthcare provider can register you by calling 800-258-4263.

Nursing parents: Information is limited on the effectiveness and safety data of Edurant in nursing babies. In general, however, nursing is potentially linked to negative effects on the nursing baby. As a result, Janssen recommends against nursing while taking Edurant to prevent the following:

• Nursing can result in an HIV infection in HIV-negative babies.
• HIV-positive babies can develop a resistance to Edurant.

Older adults: While studies are limited, in general, caution should be used in the use of Edurant in older people due to the greater frequency of decreased kidney and failure function in this population.

Children: The safety and effectiveness of children younger than 12 or people weighing less than 77 pounds have not been established.

Missed Dose

If you accidentally forget to take your Edurant dose, take it as soon as you remember with food. If you missed your scheduled dose by more than 12 hours, however, then skip this missed dose and take the following dose at your next scheduled dosing time.

Don’t try to double up and take more than one dose to make up for the missed one.

To prevent HIV from making more copies of itself or being resistant to the medication, try not to miss too many doses in a row.

Overdose: What Happens If I Take Too Much Edurant?

There is limited data on Edurant overdose. If you accidentally take too many Edurant tablets, either call the Poison Control Center or get medical help right away.

General symptoms of a medication-related overdose include:

• Nausea or vomiting
• Appetite loss
• Sweating
• Bleeding
• Bruising
• Upper stomach pain
• Yellowing of the skin or whites of the eyes (jaundice)

Precautions

What Are Reasons I Shouldn't Take Edurant?

Edurant is not appropriate for everyone. You should not take this medication if you are allergic to rilpivirine hydrochloride or any of the inactive ingredients in Edurant.

Edurant may be used with caution in some people only if their healthcare provider determines it is safe. The manufacturer advises against nursing while taking Edurant.

If any of the following applies to you, Edurant is also not an ideal HIV treatment option for you:

• More than 100,000 HIV-1 RNA copies/milliliter
• CD4 count of fewer than 200 cells/millimeter cubed
• Rifamycin antibiotic use for tuberculosis (TB) 

Additionally, Edurant isn’t recommended with medications that can lower the amount of Edurant in the body.

Low amounts of Edurant in the body can also lower the effectiveness of this medication. As a result, HIV can become resistant to this medication or other medications and make more copies of itself.

What Other Medications May Interact With Edurant?

Talk with your pharmacist or healthcare provider about the following medications that interact with Edurant:

• CYP3A4-inducing medications: CYP3A4 is a type of protein in the liver that breaks down Edurant. If you take CYP3A4 inducers—like Saint-John’s-wort for mood or carbamazepine for seizures, these medications encourage CYP3A4 to quickly work and break down Edurant. Taking these medications with Edurant can lead to low amounts of Edurant in the body, which will also lower the effectiveness of Edurant against HIV. So, avoid these CYP3A4 inducers.
• CYP3A4-inhibitors: CYP3A4-inhibiting medications—like an erythromycin antibiotic—can block CYP3A4 from working as well. So, the high amounts of Edurant might lead to a higher risk of side effects.
• Medications that affect your stomach acidity: Proton pump inhibitors (PPIs), antacids, and histamine type-2 receptor antagonists (H2 blockers) are medications that change your stomach acidity. Taking PPIs like Prilosec (omeprazole) with Edurant can lead to low Edurant effectiveness against HIV. So, avoid all PPIs. Take antacids two hours before or four hours after Edurant. Take H2-blockers like famotidine 12 hours before or four hours after Edurant.
• Other NNRTIs: Edurant is in the NNRTI medication class. Edurant isn’t recommended to be used with other NNRTI medications, such as efavirenz or doravirine.
• Medications that are linked to an abnormal heart rhythm: Certain medications—like erythromycin—raise your risk for an abnormal heart rhythm. Combining these types of medications with Edurant further raises the likelihood of an abnormal heart rhythm condition called torsade de pointes.
  

What Medications Are Similar?

Since the early 1980s, there has been much advancement in HIV therapy, including with NNRTIs like Edurant. Other FDA-approved NNRTIs include:

• Rescriptor (delavirdine)
• Pifeltro (doravirine)
• Atripla (efavirenz, emtricitabine, tenofovir DF)
• Intelence (etravirine)
• Viramune (nevirapine)

Of all the NNRTI options, experts recommend doravirine, efavirenz, and Edurant as the go-to choices for some people in certain clinical situations. Edurant has some of the following desirable characteristics:

• Fewer negative effects on cholesterol
• Fewer side effects to efavirenz
• Available as one of the smallest combination tablets called Odefsey.
• No use restrictions for people taking methadone for substance use disorder (SUD)
• No use restrictions in people with HIV-associated dementia (HAD)

When taking Edurant:

• Take with food for better absorption.
• Consider not using rilpivirine if you have a history of mood conditions since Edurant can worsen these conditions.
• Consider not using Edurant ir you're taking medications that raise the risk of abnormal heart rhythms.
• Consider not using rilpivirine if you're taking rifamycin antibiotics for TB treatment.
• Do not take if you hava a CD4 count of fewer than 200 cells/millimeter cubed.
• Do not take if you have more than 100,000 HIV-1 RNA copies/milliliter.

Since all of these medications are NNRTIs, they’re not typically taken together. If you have any questions, discuss them with your healthcare provider.

How Can I Stay Healthy While Taking Edurant?

Taking care of yourself emotionally: While there have been many advances in HIV treatment, receiving a diagnosis of HIV from your healthcare provider can understandably take a toll on your emotions. 

Consider taking the first step by learning more about HIV and sharing your HIV status with trusted loved ones—when you are comfortable. Although you can’t control how people will react, you can benefit from telling others and forming a strong social support network. In addition to friends and family, there are local and online HIV support groups. A mental health professional can also share coping strategies to help change how you feel, react, and think about your medical condition.

Taking care of yourself physically: In addition to taking care of yourself emotionally, make sure to physically take care of yourself. 

Since HIV puts the body in a constant state of inflammation, many people with HIV experience heart disease and other medical conditions 10 to 15 years earlier than people without HIV. So, it’s important to find ways to lower your risk of these medical conditions and other infections.

To stay healthy and live long fulfilling lives, stay up-to-date on your immunizations, which can keep these vaccine-preventable infections at bay. Depending on your current CD4 count, however, some vaccines might be inappropriate for you.

If you have questions about vaccinations, talk with your pharmacist or healthcare provider. Also, to physically take care of yourself, try to regularly exercise, and quit smoking, which can prevent heart disease and bone loss. 

Along the lines of prevention, continue to regularly take your medications. Also, keep up with your lab work appointments to make sure that the HIV medications are blocking HIV’s ability from making more copies of itself.

If your medications are working, your immune system will remain strong to prevent the HIV infection from progressing to AIDS, which is a late-stage condition that is characterized by life-threatening infections.

Additionally, if your medications are working, your consistently undetectable viral load (less than 50 HIV-1 RNA copies/milliliter) will lower your risk of infecting others to zero. 

Taking care of yourself financially: With all the advances in HIV therapy, receiving appropriate HIV care can still be very expensive. Consider contacting the manufacturer of your medications for assistance or reaching out to your Ryan White HIV/AIDS state chapter to find out if you qualify for free HIV medications with the AIDS Drug Assistance Program (ADAP).