Rilpivirine - Uses, Dosage, Side Effects, Drug Warnings, and Precautions

What Is Rilpivirine?

Rilpivirine is a medicine used to treat HIV or AIDS (acquired immunodeficiency syndrome, a condition where the immune system becomes very weak). It belongs to a group called second-generation non-nucleoside reverse transcriptase inhibitors (NNRTIs), drugs that stop the virus from making copies of itself.

Rilpivirine is very strong and works longer in the body compared with older NNRTIs like Efavirenz. It also has fewer side effects. However, Rilpivirine cannot cure HIV or AIDS.

The pharmaceutical company Tibotec developed Rilpivirine. In the United States, it is approved for patients who have a viral load (amount of virus in the blood) of 100,000 copies per milliliter or less when starting treatment.

Rilpivirine is always used together with other HIV medicines. In the European Union, Rilpivirine is approved to be used with another drug, Cabotegravir, for long-term maintenance therapy in adults with a viral load of fewer than 50 copies per milliliter, which is considered undetectable in the blood.

How Does Rilpivirine Work?

When HIV enters a cell, an enzyme called reverse transcriptase [a protein that helps the virus make DNA from its RNA] turns the virus’s single-stranded RNA into double-stranded DNA. This DNA then joins the host’s DNA, and the cell starts making more viruses.

Rilpivirine is a diaryl pyrimidine non-nucleoside reverse transcriptase inhibitor. It stops the virus from making DNA and copying itself by blocking the reverse transcriptase enzyme. This prevents HIV from multiplying in the body.

What Are the Uses of Rilpivirine?

Rilpivirine treats HIV-1 infection in adults and teenagers over 12 years old who have more than 100,000 copies of HIV per milliliter of blood. It is always combined with other antiretroviral drugs.

Rilpivirine is also used as postexposure prophylaxis for HIV infection [medicine taken after possible exposure to prevent infection] in two ways:

• Occupational Exposure – If someone is exposed to HIV at work, for example, through a needle stick, a cut from a sharp object, or contact with blood or other fluids.

• Non-occupational Exposure – If someone is exposed outside work, like through sexual contact or contact with infected body fluids.

What Is the Dosage of Rilpivirine?

Rilpivirine comes as tablets or long-acting injections into a muscle. Injections are given once a month or every two months. Tablets are given for four weeks first to see if the person tolerates the medicine well.

Pediatric Dose

Teens over 12 years old, 25 mg Rilpivirine once daily for teenagers over 12 years old weighing more than 35 kg.

Combination tablets include:

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir Afenamide 25 mg – One tablet once a day.

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir DF 300 mg – One tablet once a day.

Adult Dose

• 25 mg Rilpivirine once daily

Combination Tablets:

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir Afenamide 25 mg – One tablet once a day.

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir DF 300 mg – One tablet once a day.

Post-Exposure Prophylaxis:

• Occupational Exposure – Start within 72 hours of exposure. Example: 25 mg Rilpivirine once daily with two other antiretroviral drugs for four weeks.

• Non-occupational Exposure – One combination tablet daily for 28 days. Must be started within 72 hours of exposure.

Warnings

• Allergic Reactions – Severe reactions like rashes, swelling, skin blisters, eye inflammation, and organ problems can occur.

• Depression – Can cause depression, mood changes, or suicidal thoughts.

• Liver Problems (Hepatotoxicity) – Some patients can develop liver issues even if they did not have liver disease before.

• Fat Changes (Adipogenic Effects) – Changes in body fat, like weight gain in the belly, face, or breasts, or fat loss in arms and legs.

• Immune Reconstitution Syndrome – Sometimes, autoimmune diseases (when the body attacks itself) can happen months after starting treatment.

For Patients

What Is HIV-1 Infection?

HIV-1 is a virus that attacks the immune system. HIV-1 is more common than HIV-2. Both can lead to AIDS, but HIV-2 spreads less easily and progresses more slowly. HIV-1 destroys CD4 cells (cluster of differentiation 4 cells are immune cells that fight infections), weakening the immune system. Without any treatment, HIV-1 keeps reducing CD4 cells, making the body vulnerable to infections and certain cancers.

How Is HIV-1 Spread?

HIV-1 spreads through body fluids like blood, semen, vaginal fluids, rectal fluids, and breast milk. It can enter the body through the blood or the mucous membranes in the genitals, anus, or mouth. Common ways of transmission include unprotected sex, sharing needles, or from mother to child during pregnancy, birth, or breastfeeding.

Stages of HIV Infection

• Acute Stage – Occurs shortly after exposure. High virus levels and flu-like symptoms appear.

• Chronic Stage – No symptoms are seen, but the virus continues attacking the immune system.

• AIDS – Happens when CD4 count drops below 200 cells/mm³, leaving the immune system very weak. Opportunistic infections can develop.

Learn More About Rilpivirine

When and Why Switch to Rilpivirine?

Rilpivirine is a second-generation NNRTI taken once daily. It is strong, lasts longer in the body, and has fewer side effects than older drugs like Efavirenz. Switching to Rilpivirine is recommended only if the patient is doing well on current therapy and has no resistant virus strains.

How Effective Is Rilpivirine?

Rilpivirine works well with other HIV medicines, even in people with advanced HIV, low CD4 counts, or past treatment failures. It is less toxic, stronger, and more durable than Efavirenz.

Things to Inform the Doctor

• Allergies or skin reactions.

• Liver problems like Hepatitis B or C.

• Kidney disease.

• Depression or mental health issues.

Starting Rilpivirine

How to Take It?

Take Rilpivirine exactly as prescribed. Usually, one tablet is taken with a full meal each day. If taking Cabotegravir injections, start with 28 days of tablets first. Regular medical tests are required.

Do’s and Don’ts

• Visit the doctor regularly to track improvement.

• Do not change the dose without medical advice.

• Take with food to help absorption.

• Rilpivirine does not prevent HIV spread. Avoid unprotected sex or sharing needles, razors, or toothbrushes.

• Inform the doctor if allergic reactions, liver problems, or mood changes occur.

• Report any side effects.

Advice for Caregivers

Caregivers should inform the doctor if the patient has allergic reactions, chest pain, rashes, depression, or other unwanted effects.

Diet Modifications

No special diet is needed unless advised. A healthy, balanced diet is recommended. Avoid alcohol and tobacco during treatment.

Side Effects

Common Side Effects:

• Sleep problems.

• Allergic reactions like rashes, hives, or swelling.

• Skin peeling or blistering.

• Mood changes, anxiety, depression.

• Liver problems, yellowing of skin (jaundice), dark urine, and upper right stomach pain.

• Headache.

Less Common Side Effects:

• Indigestion.

• Stomach pain.

• Irritability.

• Loss of appetite.

• Fever.

• Blurred vision.

• Chest tightness.

Staying on Rilpivirine

Tips to Stay on Track

• Take the medicine on schedule; skipping doses affects treatment.

• Follow up with the doctor and report improvements or side effects.

For Doctors

Indications

Rilpivirine is used to treat HIV-1 infection in adults and adolescents over 12 years old. It is always given together with other antiretroviral drugs [medicines that stop HIV from multiplying].

Rilpivirine is also used as postexposure prophylaxis [medicine given after possible HIV exposure to prevent infection] in two situations:

• Occupational Exposure – if a healthcare worker or other professional gets a needlestick, cuts from sharp objects, or comes into contact with blood or other body fluids that may have HIV.

• Non-occupational Exposure – if someone is exposed outside work, for example, through contact with blood, genital secretions, or other infected body fluids.

Mechanism of Action

• When HIV enters a cell, an enzyme called reverse transcriptase (which helps the virus make DNA from its RNA) converts the virus’s single-stranded RNA into double-stranded DNA. This DNA then joins the host cell’s DNA, which allows the virus to make copies of itself.

• Rilpivirine is a diaryl pyrimidine non-nucleoside reverse transcriptase inhibitor. It stops reverse transcriptase from working properly and prevents HIV from multiplying. Essentially, it blocks the virus from completing the process of turning its RNA into DNA.

Pharmacodynamics

If the drug is used at too low a dose, it can stop working properly, and the virus may become resistant to Rilpivirine or similar drugs. This is why it must always be used with other antiretroviral drugs. Information on Rilpivirine’s effect after stopping treatment is not available.

Absorption

Rilpivirine reaches its highest level in the blood within four to five hours. Taking it on an empty stomach or with a protein drink reduces how much the body absorbs by 30 to 40 percent compared with taking it with a full meal.

Distribution

Rilpivirine binds strongly to plasma proteins, mainly albumin, at 99.7 percent. How much of the drug reaches other body fluids like cerebrospinal fluid (around the brain and spine) or genital secretions is unknown.

Metabolism

Rilpivirine is broken down in the liver by the cytochrome P450 3A system [liver enzymes that process many drugs].

Elimination

The drug stays in the body for about 50 hours. After taking it by mouth, 85 percent leaves the body in feces and 6 percent in urine. Because Rilpivirine binds strongly to proteins in the blood, it cannot be removed by dialysis.

Warnings and Precautions

• Hypersensitivity Reactions – Severe allergic reactions like DRESS (a serious drug reaction with rash and organ problems), skin rashes, blisters, swelling of the face, eye inflammation, and other skin reactions can occur.

• Depression and Mood Disorders – Depression, sadness, changes in mood, or thoughts of suicide have been reported.

• Liver Problems (Hepatotoxicity) – Some patients develop liver issues even if they did not have liver disease before.

• Body Fat Changes (Adipogenic Effects) – Fat may accumulate in the belly or breasts, be lost in the face or limbs, causing changes in appearance.

• Immune Reconstitution Syndrome – Some autoimmune diseases (when the body attacks itself), like Graves’ disease, polymyositis, or Guillain-Barré syndrome, can occur months after starting therapy.

Indications and Uses

Treat HIV-1 infection in adults and adolescents over 12 years old with high viral loads.

Used for postexposure prophylaxis in occupational and non-occupational exposures.

Dosage Strength and Forms

Rilpivirine comes as a 25 mg white to off-white, round, film-coated tablet. Each tablet contains 27.5 mg of Rilpivirine hydrochloride, equivalent to 25 mg of Rilpivirine. It is available as tablets and long-acting injections given once a month or every two months. Tablets are given for four weeks first to check tolerance.

Dosage

Pediatric Dose - Adolescents over 12 years old.

25 mg Rilpivirine once daily for patients over 12 years old weighing more than 35 kg.

Combination Tablets:

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir Afenamide 25 mg – One tablet daily.

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir DF 300 mg – One tablet daily.

Adult Dose

25 mg Rilpivirine once daily

Combination Tablets:

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir Afenamide 25 mg – One tablet daily.

• Emtricitabine 200 mg / Rilpivirine 25 mg / Tenofovir DF 300 mg – One tablet daily.

Postexposure Prophylaxis (PEP)

• Occupational Exposure – Start within 72 hours. Take 25 mg Rilpivirine daily with two NRTIs for four weeks.

• Non-occupational Exposure – Take one combination tablet daily for 28 days. Must start within 72 hours.

Considerations for Administration

• Avoid Rilpivirine in patients with previous allergic reactions to it.

• Avoid in patients with liver diseases like Hepatitis B or C.

• Not recommended for patients with kidney problems.

Contraindication

Rilpivirine should not be given to patients with existing liver disease as it may worsen the condition.

Clinical Trial Results

Phase 3 trials showed most side effects appeared within 48 weeks of treatment. Rilpivirine was found to be potent, long-lasting, and safer than Efavirenz. Using too low a dose can lead to resistance, so it must always be combined with other antiretroviral drugs.

Drug Interactions

Rilpivirine can interact with:

• Drugs affecting liver enzymes or processed by the liver.

• Drugs are transported by P-glycoprotein.

• Drugs that increase stomach acid.

• Drugs that prolong the QT interval (heart rhythm changes seen on ECG - electrocardiogram).

• Drugs toxic to the kidneys are cleared through the kidneys.

Other Specifications

• Pregnancy – Not enough data to know the risks of birth defects.

• Lactation – HIV-positive women should not breastfeed due to the risk of transmission. The distribution of Rilpivirine in breast milk is unknown.

• Pediatric Use – Safety and effectiveness are not established for children under 12 years.

• Geriatric Use – Safety and effectiveness for people over 65 are unknown.

• Renal Impairment – Use cautiously in severe kidney problems or end-stage renal disease.