emtricitabine/rilpivirine/tenofovir disoproxil fumarate
nucleoside reverse transcriptase inhibitors
non nucleoside reverse transcriptase inhibitors
- Management of HIV infection in treatment-naïve patients with HIV-1 RNA <100,000 copies/mL at the start of therapy (for use as a complete regimen)
- Management of HIV infection in patients on a stable antiretroviral regimen with HIV-1 RNA <50 copies/mL (to replace their current antiretroviral regimen)
- Emtricitabine– Phosphorylated intracellularly where it inhibits HIV reverse transcriptase, resulting in viral DNA chain termination
- Rilpivirine– Inhibits HIV-replication by noncompetitively inhibiting HIV reverse transcriptase
- Tenofovir– Phosphorylated intracellularly where it inhibits HIV reverse transcriptase resulting in disruption of DNA synthesis
Slowed progression of HIV infection and decreased occurrence of sequelae
Absorption: Rapidly and extensively absorbed; 93% bioavailable
Metabolism and Excretion: Some metabolism, 86% renally excreted, 14% fecal excretion
Half-life: 10 hr
Absorption: Well absorbed following oral administration
Protein Binding: 99.7%
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A enzyme system); 25% excreted in feces unchanged, <1% excreted unchanged in urine
Half-life: 50 hr
Absorption: Tenofovir disoproxil fumarate is a prodrug, which is split into tenofovir, the active component
Distribution: Absorption is enhanced by food
Metabolism and Excretion: 70–80% excreted unchanged in urine by glomerular filtration and active tubular secretion
TIME/ACTION PROFILE (blood levels)
|emtricitabine PO||rapid||1–2 hr||24 hr|
|rilpivirine PO||unknown||4–5 hr||24 hr|
|tenofovir PO||unknown||2 hr*||24 hr|
- Drugs that may significantly ↓ rilpivirine levels (may ↓ virologic response, ↑ risk of resistance and cross-resistance);
- Concurrent use of other antiretrovirals;
- Concurrent use of carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, proton pump inhibitors, dexamethasone (>1 dose), or St. John's wort;
- Concurrent use of other products containing emtricitabine, rilpivirine (unless dose adjustment needed with rifabutin), tenofovir, lamivudine, or adefovir;
- CCr <50 mL/min;
- Lactation: HIV-infected patients should not breast feed.
Use Cautiously in:
- History of suicidal ideation or depression;
- History of pathologic fractures/osteoporosis/bone loss;
- OB: Use during pregnancy only if potential benefit justifies potential fetal risk;
- Pedi: Children <12 yr (safety and effectiveness not established).
Adverse Reactions/Side Effects
GU: renal impairment
MS: ↓ bone density
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS)
Misc: POST-TREATMENT ACUTE EXACERBATION OF HEPATITIS B, immune reconstitution syndrome
CNS: SUICIDAL THOUGHTS, depression, insomnia, headache
CNS: abnormal dreams, depression, dizziness, fatigue, headache, insomnia
F and E: hypophosphatemia
GI: LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, diarrhea, nausea
GU: ACUTE RENAL FAILURE/FANCONI SYNDROME
MS: bone pain, ↓ bone mineral density, muscle pain, osteomalacia
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- May ↑ risk of nephrotoxicity with other nephrotoxic drugs; avoid if possible.
- Strong CYP3A4 inducers, including carbamazepine, oxcarbazepine, phenobarbital, phenytoin, dexamethasone (more than a single dose), rifabutin, rifampin, and rifapentine may ↓ levels and effectiveness; concurrent use contraindicated.
- Proton pump inhibitors including esomeprazole, lansoprazole, omeprazole, pantoprazole, and rabeprazole ↑ gastric pH and may ↓ blood levels and effectiveness; concurrent use contraindicated.
- Antacids including aluminum hydroxide, magnesium hydroxide, and calcium carbonate ↑ gastric pH and may ↓ blood levels; administer at least 2 hr before or 4 hr after.
- Blood levels and effectiveness may be ↓ by H2 -receptor antagonists including cimetidine, famotidine, nizatidine, and ranitidine; administer 12 hr after or 4 hr before.
- Nephrotoxic agents, including NSAIDs ↑ risk of nephrotoxicity; avoid concurrent use.
- Concurrent use of other drugs that ↑ risk of torsade de pointes may ↑ risk of serious arrhythmias.
- May alter requirements for methadone maintenance.
- Blood levels and risk of adverse effects may be ↑ by clarithromycin, and erythromycin; consider azithromycin as an alternative.
- Ledipasvir/sofosbuvir and sofosbuvir/velpatasvir may ↑ tenofovir levels.
St. John's wort may ↓ blood levels and effectiveness; concurrent use contraindicated.
PO: (Adults and Children ≥12 yr and ≥35 kg): 1 tablet once daily. Concurrent rifabutin therapy– Give an additional 25 mg of rilpivirine once daily.
Tablets: emtricitabine 200 mg/rilpivirine 25 mg/ tenofovir disoproxil fumarate 300 mg
- Assess for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy.
- Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression.
- Monitor bone mineral density in patients who have a history of pathologic bone fracture or are at risk for osteoporosis or bone loss. Calcium and vitamin D supplementation may be beneficial for all patients.
- Monitor for signs or symptoms of severe skin or hypersensitivity reactions (severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis or eosinophilia). Discontinue Complera immediately if signs develop.
Lab Test Considerations: Monitor viral load and CD4 cell count regularly during therapy.
- Assess for hepatitis B virus (HBV). Complera is not approved for administration in patients with HIV and HBV.
- Monitor liver function tests before and periodically during therapy, especially in patients with underlying liver disease or marked ↑ transaminase. May cause ↑ serum creatinine, AST, ALT, total bilirubin, total cholesterol, LDL, and triglycerides. May cause lactic acidosis and severe hepatomegaly with steatosis. These events are more likely to occur if patients are female, obese, or receiving nucleoside analogue medications for extended periods of time. Monitor patient for signs (increased serum lactate levels, elevated liver enzymes, liver enlargement on palpation). Therapy should be suspended if clinical or laboratory signs occur.
- Calculate creatinine clearance (CCr), urine glucose, and urine protein prior to therapy. CCr should be >70 mL/min before starting therapy. Monitor CCr, urine glucose, and urine protein in all patients periodically during therapy and serum phosphorous in patients at risk for renal impairment. Assess patients with persistent or worsening bone pain, pain in extremities, fractures and/or muscular pain or weakness for proximal renal tubulopathy; evaluate renal function promptly.
- PO: Administer once daily with food
- Emphasize the importance of taking Complera as directed, at the same time each day. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses with a meal if remembered <12 hr from the time it is usually taken, then return to regular schedule. If more than 12 hr from time dose is usually taken, omit dose and resume dosing schedule; do not double doses. Advise patient to read Patient Information prior to starting therapy and with each Rx refill in case of changes.
- Advise patient to take antacids 2 hr before or 4 hr after and H2 -antagonists 12 hr before or 4 hr after Complera.
- Instruct patient that Complera should not be shared with others.
- Inform patient that Complera does not cure AIDS or prevent associated or opportunistic infections. Rilpivirine does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of Complera are unknown at this time.
- Advise patient to notify health care professional immediately if symptoms of lactic acidosis (nausea, vomiting, unusual or unexpected stomach discomfort, and weakness) occur.
- Inform patients and families of risk of suicidal thoughts and behavior and advise that behavioral changes, emergency or worsening signs and symptoms of depression, unusual changes in mood, or emergence of suicidal thoughts, behavior, or thoughts of self-harm should be reported to health care professional immediately.
- Immune reconstitution syndrome may trigger opportunistic infections or autoimmune disorders. Notify health care professional if symptoms occur.
- May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
- Rep: Advise patients to notify health care professional if pregnancy is planned or suspected. Advise patient to avoid breast feeding during Complera therapy. Encourage women who become pregnant during Complera therapy to enroll in Antiviral Pregnancy Registry by calling 1-800-258-4263.
- Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects.
- Delayed progression of AIDS and decreased opportunistic infections in patients with HIV.
- Decrease in viral load and increase in CD4 cell counts.
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