Complera

Primary Uses

Complera is a complete treatment regimen for Human Immunodeficiency Virus type 1 (HIV-1). It combines three different antiviral medications—emtricitabine, rilpivirine, and tenofovir disoproxil fumarate—into a single daily pill. These medicines belong to a class of drugs called antiretrovirals, which work by preventing the virus from multiplying in the body.

Patient Eligibility

Healthcare providers typically prescribe Complera for two specific groups of patients:

• New Treatment: Individuals who have never taken HIV medications before and have a viral load (HIV-1 RNA) of 100,000 copies/mL or less.
• Treatment Switch: Individuals who are currently on a stable HIV treatment regimen, have had an undetectable viral load (less than 50 copies/mL) for at least six months, and have no history of treatment failure or known resistance to the components of Complera.

This medication is approved for use in adults and pediatric patients who weigh at least 77 pounds (35 kg). By reducing the amount of HIV in the blood, the medication helps the immune system function better and increases the number of CD4 (T) cells. It is important to note that Complera is a treatment to manage the infection and is not a cure for HIV or AIDS.

Mechanism of Action

Complera is a combination of three antiretroviral medications: emtricitabine, rilpivirine, and tenofovir disoproxil fumarate. These drugs work together to interfere with the replication cycle of the human immunodeficiency virus (HIV-1).

The virus requires a specific enzyme called reverse transcriptase to convert its viral RNA into DNA, a necessary step for the virus to multiply and infect new cells. The components of Complera block this enzyme in two distinct ways:

• NNRTI Action: Rilpivirine is a non-nucleoside reverse transcriptase inhibitor. It binds directly to the reverse transcriptase enzyme and physically prevents it from working.
• NRTI Action: Emtricitabine and tenofovir are nucleoside/nucleotide reverse transcriptase inhibitors. They mimic the natural building blocks the virus uses to create DNA. When the virus incorporates these decoy blocks into its DNA chain, the chain is terminated, and the virus cannot complete its replication process.

By inhibiting the reverse transcriptase enzyme, Complera reduces the amount of HIV in the bloodstream, which is referred to as the viral load. Lowering the viral load helps protect the immune system and may increase the number of CD4 cells, which are white blood cells vital for fighting off other infections. While this treatment helps manage the virus, it is not a cure for HIV or AIDS.

Common Side Effects

Many people using this medication experience mild side effects. These may include:

• Headache
• Nausea or diarrhea
• Trouble sleeping (insomnia)
• Dizziness
• Tiredness or fatigue
• Rash
• Stomach pain

Serious Side Effects

Seek medical attention immediately if you experience any of the following serious side effects:

• Liver problems: Symptoms include yellowing of the skin or eyes (jaundice), dark urine, light-colored stools, loss of appetite, or pain in the upper right side of the stomach.
• Lactic acidosis: A buildup of acid in the blood that can cause unusual muscle pain, weakness, coldness in the arms and legs, trouble breathing, or a fast or irregular heartbeat.
• Kidney problems: Signs may include little or no urination, swelling in the feet or ankles, or feeling short of breath.
• Mental health changes: Severe depression, anxiety, or suicidal thoughts.
• Bone problems: Bone pain or bones that break easily.
• Immune system changes: As the immune system gets stronger, it may react to hidden infections, causing new symptoms to appear.

Boxed Warnings

Complera includes a boxed warning regarding the risk of severe acute exacerbations of hepatitis B (HBV) in patients co-infected with HIV-1 and HBV who discontinue the medication. Liver function should be monitored closely for several months after stopping therapy. Additionally, lactic acidosis and severe hepatomegaly with steatosis (fatty liver), including fatal cases, have been reported with the use of nucleoside analogs.

Contraindications

This medication should not be used with certain other drugs because they can significantly decrease the levels of rilpivirine in the blood, potentially leading to treatment failure. Prohibited medications include proton pump inhibitors (such as omeprazole or lansoprazole), certain anticonvulsants (such as carbamazepine or phenytoin), and certain antibiotics (such as rifampin).

Skin and Hypersensitivity Reactions

Severe skin and hypersensitivity reactions have been reported, including Stevens-Johnson syndrome and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS). Treatment must be discontinued immediately if a severe rash or a rash accompanied by systemic symptoms, such as fever or organ dysfunction, occurs.

Depressive Disorders

Depressive disorders, including depression, anxiety, and suicidal ideation or behavior, have been observed in patients taking rilpivirine-containing products. Immediate medical evaluation is recommended for patients experiencing severe depressive symptoms.

Kidney and Bone Health

• Renal Impairment: New or worsening kidney impairment, including cases of acute renal failure and Fanconi syndrome, has occurred. Healthcare providers typically assess kidney function before and during treatment.
• Bone Effects: Decreases in bone mineral density and cases of osteomalacia (softening of the bones) have been reported. Bone monitoring may be considered for patients with a history of bone fractures or other risk factors for bone loss.

Immune Reconstitution Syndrome

Patients may develop an inflammatory response to previous or hidden infections (such as tuberculosis or fungal infections) shortly after starting antiretroviral therapy. Autoimmune disorders may also occur many months after starting treatment, requiring further medical evaluation.

Pregnancy

Data regarding the use of Complera during pregnancy are limited. While animal studies on the individual components of the drug have not shown a high risk of birth defects, human data are insufficient to confirm safety. It is important for pregnant individuals to discuss the risks and benefits of continuing HIV treatment with their healthcare provider.

Research indicates that levels of rilpivirine, one of the components of Complera, may be lower during the second and third trimesters of pregnancy. Because of this, healthcare providers may monitor viral loads more closely to ensure the virus remains suppressed. If the medication is not effectively controlling the virus, a change in treatment may be required.

There is an Antiviral Pregnancy Registry that collects data on pregnancy outcomes in individuals exposed to HIV medications. This registry helps healthcare professionals better understand the safety of these drugs during pregnancy.

Breastfeeding

In the United States and other regions where safe infant formula is available, health experts recommend that individuals with HIV avoid breastfeeding. This recommendation is intended to prevent the transmission of HIV to the infant through breast milk.

Furthermore, some components of Complera are known to pass into human breast milk. The effects of these drugs on a nursing infant are not fully understood, and there is a risk that the infant could develop resistance to HIV medications if they are exposed to low levels of the drug through milk. Discussing safe feeding alternatives with a healthcare provider is recommended.

Available Forms

Complera is supplied as a film-coated tablet. This medication is a fixed-dose combination product intended for oral use, containing active ingredients combined into a pill.

• Oral tablet

FDA Approval and Indications

Complera was approved by the U.S. Food and Drug Administration (FDA) in 2011. It is a fixed-dose combination tablet indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 35 kg. It is specifically used for patients who have not previously received antiretroviral therapy and have HIV-1 RNA levels of 100,000 copies/mL or less, or to replace a stable regimen in patients who are virologically suppressed.

Boxed Warning

The medication carries a boxed warning regarding the risk of severe acute exacerbations of hepatitis B (HBV). Patients co-infected with both HIV-1 and HBV have reported significant worsening of hepatitis B after stopping treatment with medications containing emtricitabine or tenofovir disoproxil fumarate, which are components of Complera. Close monitoring of liver function is required for these patients if the drug is discontinued.

Regulatory Status

Complera is classified as a prescription-only medication. While it does not require a Risk Evaluation and Mitigation Strategy (REMS), the FDA requires that a medication guide be provided to patients to communicate important safety information regarding its use and potential risks.

Insurance Coverage

Complera is a brand-name prescription medication. Most commercial insurance plans, Medicare Part D, and Medicaid provide coverage for this drug. However, the specific out-of-pocket cost will vary based on your plan's formulary, which determines the drug's tier and your required copayment or coinsurance. Some insurance providers may require prior authorization before they agree to cover the medication.

Factors Affecting Price

Several variables can influence the final price you pay for Complera:

• Pharmacy Selection: Prices can differ between retail pharmacies, mail-order services, and specialty pharmacies.
• Deductibles: If your insurance plan has a deductible, you may need to pay the full cost of the medication until that limit is reached.
• Generic Availability: Complera is a combination of three specific medications. While some individual components may be available as generics, the specific combination tablet is typically sold as a brand-name product, which generally costs more than generic alternatives.

Financial Assistance

For individuals who have difficulty affording their medication, there are several options to explore:

• Manufacturer Assistance: The pharmaceutical company that makes Complera may offer patient assistance programs or co-pay savings cards for eligible patients with commercial insurance.
• State Assistance Programs: The AIDS Drug Assistance Program (ADAP) is a state-run program that helps provide HIV medications to people with limited or no insurance coverage.
• Non-Profit Organizations: Certain foundations may provide grants or financial aid to help cover the costs of chronic disease medications.