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Complera

Generic Name: Emtricitabine/Rilpivirine/Tenofovir Disoproxil Fumarate
Drug Category: NRTIs/NNRTIs
Litigation Alert Level: High
This drug has been approved for use by males and females over the age of 12 years old for a maximum duration of 104 weeks.

Approved Uses

Indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 35 kg:

• As initial therapy in those with no antiretroviral treatment history with HIV-1 RNA less than or equal to 100,000 copies/mL at the start of therapy or

• To replace a stable antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable antiretroviral regimen for at least 6 months with no treatment failure and no known substitutions associated with resistance to the individual components of COMPLERA

The following points should be considered when initiating therapy with COMPLERA in adult patients with no antiretroviral treatment history:

  • More rilpivirine-treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure (HIV-1 RNA ≥ 50 copies/mL) compared to rilpivirine-treated subjects with HIV-1 RNA less than or equal to 100,000 copies/mL
  • Regardless of HIV-1 RNA level at the start of therapy, more rilpivirine-treated subjects with CD4+ cell count less than 200 cells/mm3 experienced virologic failure compared to rilpivirine-treated subjects with CD4+ cell count greater than or equal to 200 cells/mm3
  • The observed virologic failure rate in rilpivirine-treated subjects conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz
  • More subjects treated with rilpivirine developed tenofovir and lamivudine/emtricitabine associated resistance compared to efavirenz

The following points should be met when considering replacing the current regimen with COMPLERA in virologically-suppressed adults:

  • Patients should have no history of virologic failure
  • Patients should have been stably suppressed (HIV-1 RNA < 50 copies/mL) for at least 6 months prior to switching therapy
  • Patients should currently be on their first or second antiretroviral regimen prior to switching therapy
  • Patients should have no current or past history of resistance to any of the three components of COMPLERA

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including tenofovir disoproxil fumarate, a component of COMPLERA. 

Prior to or when initiating COMPLERA, test patients for hepatitis B virus infection.

COMPLERA is not approved for the treatment of chronic hepatitis B virus (HBV) infection. Severe acute exacerbations of hepatitis B have been reported in patients coinfected with HIV-1 and HBV who have discontinued EMTRIVA or VIREAD, two of the components of COMPLERA. Hepatic function should be monitored closely in these patients. If appropriate, initiation of anti-hepatitis B therapy may be warranted.

Patients with estimated creatinine clearance below 50 mL per minute should not receive COMPLERA.

Renal impairment, including cases of acute renal failure and Fanconi syndrome (renal tubular injury with severe hypophosphatemia), has been reported with the use of tenofovir DF.

The adverse reaction depressive disorders (depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicidal ideation) has been reported with rilpivirine.

Severe skin and hypersensitivity reactions have been reported during the postmarketing experience, including cases of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) with RPV-containing regimens.

Cases of osteomalacia associated with proximal renal tubulopathy, manifested as bone pain or pain in extremities and which may contribute to fractures, have been reported in association with the use of TDF.

Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including the components of COMPLERA.

In clinical trials in HIV-1-infected adults, TDF, a component of COMPLERA, was associated with slightly greater decreases in bone mineral density (BMD) and increases in biochemical markers of bone metabolism, suggesting increased bone turnover relative to comparators. Serum parathyroid hormone levels and 1,25 Vitamin D levels were also higher in subjects receiving TDF.

COMPLERA is a complete regimen for the treatment of HIV-1 infection; therefore, COMPLERA should not be administered with other antiretroviral medications for treatment of HIV-1 infection.

COMPLERA should be avoided with concurrent or recent use of a nephrotoxic agent (e.g., high-dose or multiple nonsteroidal anti-inflammatory drugs [NSAIDs]).

Co-administration of RPV and drugs that induce CYP3A may result in decreased plasma concentrations of RPV and loss of virologic response and possible resistance to RPV or to the class of NNRTIs.

Co-administration of RPV and drugs that inhibit CYP3A may result in increased plasma concentrations of RPV.

COMPLERA should not be co-administered with the following drugs:

  • the anticonvulsants carbamazepine, oxcarbazepine, phenobarbital, phenytoin
  • the antimycobacterials rifampin, rifapentine
  • proton pump inhibitors, such as dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole
  • the glucocorticoid systemic dexamethasone (more than a single dose)
  • St. John’s wort (Hypericum perforatum)

Based on prospective reports to the APR of exposures to RPV-containing regimens during pregnancy (including over 290 exposed during first trimester and over 160 exposed in the second/third trimester), there was no significant increase in overall risk of major birth defects with RPV compared to the background birth defect rate of 2.7% in the U.S. reference population of the MACDP.

Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving COMPLERA.

GoToSource

Off-label Uses

• Use in patients under the age of 12. GoToSource

• Hepatitis B. GoToSource

Adverse Events

Liver damage, suicidal ideation and suicide attempts and immune reconstitution syndrome (inflammatory disorders with paradoxical worsening of preexisting infectious processes). GoToSource

Kidney failure. GoToSource

Abnormal dreams and nightmares. GoToSource

Lactic acidosis, hyperlipidemia (elevated lipid (fat) levels in blood) and lipodystrophy (loss of subcutaneous fat in the face and extremities and/or accumulation of fat under skin). GoToSource

Osteopenia (low bone mineral density) and osteoporosis (bones become weak and break easily). GoToSource

Insomnia. GoToSource

Litigation

Lawsuits filed for kidney disease and bone density loss.

The material contained in GoToPills is for informational purposes only and not intended to replace the judgment, evaluation and treatment of physicians, pharmacists and other healthcare providers. GoToPills does not provide medical advice, diagnoses or treatment. Always seek the advice of your physician or other qualified health provider regarding a medical condition or treatment.

 

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Site Last Updated March 29, 2024