Version May 2024
Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HBV and HIV-1 and have discontinued emtricitabine or tenofovir disoproxil fumarate. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue antiretroviral treatment. If appropriate, initiation of anti-HBV therapy may be warranted.
HIV-1 infection, treatment: Oral: One tablet (emtricitabine 200 mg/rilpivirine 25 mg/tenofovir disoproxil fumarate 300 mg) once daily. Note: Do not use in patients with HIV RNA ≥100,000 copies/mL and/or CD4 count ≤200 cells/mm3 (Ref).
Missed dose: If ≤12 hours, take dose as soon as possible; if >12 hours, resume at next regularly scheduled time.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥50 mL/minute: No dosage adjustments necessary.
CrCl <50 mL/minute: Use is not recommended.
ESRD requiring dialysis: Use is not recommended.
Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustments necessary.
Severe impairment (Child-Pugh class C): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing.
(For additional information see "Rilpivirine, emtricitabine, and tenofovir disoproxil fumarate: Pediatric drug information")
Note: International Considerations: Doses are expressed as tenofovir disoproxil fumarate salt, consistent with US and Canadian labeling; in some other countries, dosing may be expressed as tenofovir disoproxil base. Tenofovir disoproxil fumarate 300 mg is equivalent to tenofovir disoproxil base 245 mg.
HIV-1 infection, treatment: Note: Gene mutation and antiretroviral resistance patterns should be evaluated (refer to https://www.iasusa.org/ for more information) when necessary.
Children and Adolescents weighing ≥35 kg: Oral: One tablet (emtricitabine 200 mg, rilpivirine 25 mg, tenofovir disoproxil fumarate 300 mg per tablet) once daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Children and Adolescents weighing ≥35 kg:
CrCl ≥50 mL/minute: No dosage adjustments necessary
CrCl <50 mL/minute: Use is not recommended
ESRD or requiring dialysis: Use is not recommended
Children and Adolescents weighing ≥35 kg:
Mild to moderate impairment: No dosage adjustments necessary.
Severe impairment: There are no dosage adjustments provided in manufacturer's labeling (has not been studied).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Observed in patients receiving the same doses of emtricitabine, rilpivirine, and tenofovir as the combination product; also see individual agents.
>10%:
Endocrine & metabolic: Increased serum cholesterol (≤14%), increased LDL cholesterol (1% to 13%)
Hepatic: Increased serum alanine aminotransferase (1% to 19%), increased serum aspartate aminotransferase (1% to 16%)
1% to 10%:
Central nervous system: Depression (2% to 9%), headache (2%), insomnia (2%), abnormal dreams (1%), dizziness (1%)
Dermatologic: Skin rash (1%)
Endocrine & metabolic: Adrenocortical insufficiency (7%), increased serum triglycerides (1%)
Gastrointestinal: Nausea (1%)
Hepatic: Increased serum bilirubin (1% to 6%)
Renal: Increased serum creatinine (≤6%)
Frequency not defined:
Central nervous system: Anxiety, drowsiness, fatigue, sleep disorder
Gastrointestinal: Abdominal distress, abdominal pain, cholecystitis, cholelithiasis, decreased appetite, diarrhea, vomiting
Renal: Glomerulonephritis (membranous and mesangioproliferative), nephrolithiasis
<1%, postmarketing, and/or case reports: DRESS syndrome, hypersensitivity reaction, immune reconstitution syndrome, severe dermatological reaction, suicidal ideation, suicidal tendencies, weight gain
Concurrent use of carbamazepine, systemic dexamethasone (>1 dose), oxcarbazepine, phenobarbital, phenytoin, proton pump inhibitors (PPIs) (eg, dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), rifampin, rifapentine, and/or St John's wort.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to emtricitabine, rilpivirine, tenofovir disoproxil fumarate or any component of the formulation.
Concerns related to adverse effects:
• Cardiac effects: In healthy subjects, supratherapeutic dosages of rilpivirine (75 mg once daily and 300 mg once daily) have been shown to prolong the QTc interval of the electrocardiogram; use caution when coadministering with drugs with a known risk of torsades de pointes.
• Decreased bone mineral density: In clinical trials, tenofovir disoproxil fumarate has been associated with decreases in bone mineral density in HIV-1 infected adults and increases in bone metabolism markers. Serum parathyroid hormone and 1,25 vitamin D levels were also higher. Decreases in bone mineral density have also been observed in clinical trials of HIV-1 infected pediatric patients. Observations in chronic hepatitis B infected pediatric patients (aged 12 to 18 years) were similar. Consider monitoring of bone density in adult and pediatric patients with a history of pathologic fractures or with other risk factors for bone loss or osteoporosis. Consider calcium and vitamin D supplementation for all patients; effect of supplementation has not been studied but may be beneficial. Long-term bone health and fracture risk unknown. If abnormalities are suspected, expert assessment is recommended.
• Depressive disorders: Rilpivirine may cause depression, depressed mood, dysphoria, major depression, mood changes, negative thoughts, suicide attempts, or suicidal ideation. Promptly evaluate patients with severe depressive symptoms and reevaluate risk versus benefit of continued combination therapy.
• Hepatotoxicity: Hepatotoxicity has been reported with rilpivirine-containing regimens. Patients with hepatitis B or C or increased baseline liver function tests may be at greater risk, although some cases have occurred in patients with no preexisting disease or hepatic disease risk factors. Evaluate liver function tests in patients with increased baseline liver function tests or with hepatitis B or C prior to treatment initiation and periodically during therapy; also consider evaluation of patients with no preexisting hepatic disease or hepatic disease risk factors.
• Hypersensitivity: Hypersensitivity and severe skin reactions have been reported, including severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis or eosinophilia, or drug reaction with eosinophilia and systemic symptoms (DRESS) with regimens containing rilpivirine. Some skin reactions were accompanied by constitutional symptoms (eg, fever); other skin reactions were associated with organ dysfunction (eg, hepatic serum biochemistry elevations). In clinical trials, treatment-related rashes ≥ grade 2 were reported in 1% of patients. Most rashes were Grade 1 or 2 and occurred within the first 4 to 6 weeks of therapy. Monitor laboratory parameters and clinical status; discontinue if any severe hypersensitivity or skin rash develop.
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
• Lactic acidosis/hepatomegaly: Lactic acidosis and severe hepatomegaly, sometimes fatal, have been reported with the use of nucleoside analogs, alone or in combination with other antiretrovirals. Suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (marked transaminase elevation may/may not accompany hepatomegaly and steatosis).
• Osteomalacia and renal dysfunction: Tenofovir disoproxil fumarate may cause osteomalacia with proximal renal tubulopathy. Bone pain, extremity pain, fractures, arthralgias, weakness, and muscle pain have been reported. In patients at risk for renal dysfunction, persistent or worsening bone or muscle symptoms should be evaluated for hypophosphatemia and osteomalacia.
• Renal toxicity: May cause renal toxicity (acute renal failure and/or Fanconi syndrome); avoid use with concurrent or recent nephrotoxic therapy (including high dose or multiple NSAID use). Acute renal failure has occurred in HIV-infected patients with risk factors for renal impairment who were on a stable tenofovir disoproxil fumarate regimen to which a high dose or multiple NSAID therapy was added. Consider alternatives to NSAIDS in patients taking tenofovir disoproxil fumarate and at risk for renal impairment. Assess serum creatinine, estimated CrCl, urine protein, and urine glucose prior to initiation of therapy and as clinically appropriate during therapy. Monitor serum phosphorus in patients with chronic kidney disease. IDSA guidelines recommend discontinuing tenofovir (and substituting with alternative antiretroviral therapy) in HIV-infected patients who develop a decline in GFR (a >25% decrease in GFR from baseline and to a level of <60 mL/minute/1.73 m2) during use, particularly in presence of proximal tubular dysfunction (eg, euglycemic glycosuria, increased urinary phosphorus excretion and hypophosphatemia, proteinuria [new onset or worsening]) (IDSA [Lucas 2014]).
Disease-related concerns:
• Chronic hepatitis B: [US Boxed Warning]: Safety and efficacy during coinfection of HIV-1 and HBV have not been established; acute, severe exacerbations of HBV have been reported following discontinuation of antiretroviral therapy. Not indicated for treatment of chronic hepatitis B. Closely monitor hepatic function with clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue this therapy. If appropriate, anti-hepatitis B therapy may be warranted , especially in patients with advanced hepatic disease or cirrhosis (post-treatment exacerbation of hepatitis may lead to hepatic decompensation or liver failure). All patients with HIV should be tested for HBV prior to initiation of treatment.
• Renal impairment: Use is not recommended in patients with CrCl <50 mL/minute.
Other warnings/precautions:
• Appropriate use: When used to replace an antiretroviral treatment regimen in virologically-suppressed patients currently on a stable regimen, patients must have no history of virologic failure; prior to regimen replacement, must have been suppressed for at least 6 months; must be currently on their first or second antiretroviral regimen, and have no history of resistance to emtricitabine, rilpivirine, or tenofovir.
• Monitoring: If used as therapy replacement in virologically suppressed patients meeting criteria, additional HIV-1 RNA and regimen tolerability monitoring is recommended to assess potential virologic failure or rebound.
Emtricitabine-associated hyperpigmentation may occur at a higher frequency in pediatric patients compared to adults (children: 32%; adults: 2% to 6%).
Incidence of some adverse reactions may be higher in pediatric patients 12 to 18 years of age receiving rilpivirine as compared to adults. In a small, phase 2 pediatric clinical trial (n=36), adverse reactions following receipt of rilpivirine in combination with other antiretrovirals were similar to those in adults, with a higher incidence of some reactions (eg, headache, dizziness, depression); most were grade 1 or 2. For depressive disorders, the incidence of grade 3 and 4 depressive disorders (regardless of causality) was 5.6% (vs 1% in adults), including 1 suicide attempt. None of these pediatric patients discontinued therapy due to their depressive symptoms.
Tenofovir disoproxil fumarate (TDF) disrupts vitamin D metabolism and has been associated with decreased bone mineral density (BMD) in adults and children. Plasma concentrations of the TDF metabolite tenofovir (TFV) have been associated with endocrine disruption and low BMD; tenofovir alafenamide (TAF) is associated with lower TFV concentrations and less decline in BMD than TDF. Data suggest the impact may be greater in children who are less mature (eg, Sexual Maturity Ratings [SMRs] 1 to 2 [previously Tanner Stages]) than in those with more advanced pubertal development (SMR ≥3). The potential for BMD loss during the important period of rapid bone accrual in childhood and early adolescence is concerning and favors use of abacavir or TAF in children with SMRs 1 to 3 (children with perinatally-acquired HIV are already at risk for low peak bone mass). Prior to initiation of therapy, assessment of benefits versus potential risk should be assessed; with TDF therapy, monitor plasma vitamin D concentrations; supplement with vitamin D as needed; calcium carbonate supplementation may also be considered. Monitoring of BMD may be considered in patients with additional risk factors for decreased bone density (HHS [pediatric] 2022).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Complera: emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir disoproxil fumarate 300 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]
No
Tablets (Complera Oral)
200-25-300 mg (per each): $144.93
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Complera: emtricitabine 200 mg, rilpivirine 25 mg, and tenofovir disoproxil fumarate 300 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]
Oral: Administer with food (>390 kcal (Ref)); a protein drink is not a substitute for food.
Oral: Administer with a moderate to high-fat meal (children: ≥500 kcal; adolescents: ≥390 kcal); a protein drink alone is not sufficient (Ref).
Missed dose: If ≤12 hours since dose due, take dose as soon as possible; if >12 hours, resume at next regularly scheduled time.
HIV-1 infection, treatment: Treatment of HIV-1 infection (as a complete regimen) in adult and pediatric patients >35 kg as initial therapy in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL at the start of therapy, and in certain virologically suppressed (HIV-1 RNA <50 copies/mL) patients on a stable antiretroviral regimen for ≥6 months with no treatment failure or substitutions due to resistance to emtricitabine, rilpivirine, or tenofovir disoproxil fumarate in order to replace their current antiretroviral treatment regimen.
Refer to individual components.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Acyclovir-Valacyclovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Acyclovir-Valacyclovir. Risk C: Monitor therapy
Adefovir: May diminish the therapeutic effect of Tenofovir Products. Adefovir may increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Adefovir. Risk X: Avoid combination
Aminoglycosides: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Aminoglycosides. Risk C: Monitor therapy
Aminosalicylic Acid: May decrease the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
Antacids: May decrease the serum concentration of Rilpivirine. Management: Administer antacids at least 2 hours before or 4 hours after oral rilpivirine when used with most rilpivirine products. However, administer antacids at least 6 hours before or 4 hours after the rilpivirine/dolutegravir combination product. Risk D: Consider therapy modification
Antihepaciviral Combination Products: May increase the serum concentration of Rilpivirine. Risk X: Avoid combination
Asciminib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Atazanavir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Use boosted atazanavir in adults; give combo (atazanavir/ritonavir or atazanavir/cobicistat with tenofovir) as a single daily dose with food. Pediatric patients, pregnant patients, and use of H2-blockers require dose changes. See Lexi Interact monograph. Risk D: Consider therapy modification
Betibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Betibeglogene Autotemcel. Risk X: Avoid combination
Cabozantinib: MRP2 Inhibitors may increase the serum concentration of Cabozantinib. Risk C: Monitor therapy
CarBAMazepine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Cidofovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Cidofovir. Risk C: Monitor therapy
Cladribine: Agents that Undergo Intracellular Phosphorylation may diminish the therapeutic effect of Cladribine. Risk X: Avoid combination
Cobicistat: Tenofovir Disoproxil Fumarate may enhance the adverse/toxic effect of Cobicistat. More specifically, cobicistat may impair proper tenofovir disoproxil fumarate monitoring and dosing. Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Rilpivirine. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Rilpivirine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for reduced rilpivirine efficacy (eg, loss of virologic response or resistance). Risk X: Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Rilpivirine. Risk C: Monitor therapy
Darolutamide: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Darunavir: Tenofovir Disoproxil Fumarate may increase the serum concentration of Darunavir. Darunavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
DexAMETHasone (Systemic): May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Didanosine: Tenofovir Disoproxil Fumarate may diminish the therapeutic effect of Didanosine. Tenofovir Disoproxil Fumarate may increase the serum concentration of Didanosine. Management: Avoid use of tenofovir disoproxil fumarate and didanosine when possible. If combined in adults with CrCL greater than 60 mL/min, decrease didanosine to 250 mg daily if 60 kg or more or to 200 mg if less than 60 kg. Avoid if CrCL is less than 60 mL/min. Risk D: Consider therapy modification
Didanosine: Rilpivirine may decrease the absorption of Didanosine. Didanosine may decrease the absorption of Rilpivirine. More specifically, simultaneous coadministration of these drugs creates a conflict between recommendations to administer with (rilpivirine) and without (didanosine) food. Management: Administer didanosine on an empty stomach at least 2 hours before or 4 hours after rilpivirine, due to the requirement that rilpivirine be administered with food. Risk D: Consider therapy modification
Elacestrant: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Elivaldogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid combination
Eltrombopag: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Ergonovine: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Ergonovine. Specifically, this would be most likely with delavrdine, while other Non-Nucleoside Reverse Transcriptase Inhibitors may be more likely to decrease the concentration of Ergonovine. Risk X: Avoid combination
Fosphenytoin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Futibatinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Ganciclovir-Valganciclovir: Tenofovir Products may increase the serum concentration of Ganciclovir-Valganciclovir. Ganciclovir-Valganciclovir may increase the serum concentration of Tenofovir Products. Risk C: Monitor therapy
Gilteritinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Histamine H2 Receptor Antagonists: May decrease the serum concentration of Rilpivirine. Management: Administer histamine H2 receptor antagonists (H2RAs) at least 12 hours before or 4 hours after oral rilpivirine. Risk D: Consider therapy modification
Inhibitors of the Proton Pump (PPIs and PCABs): May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Ketoconazole (Systemic): May increase the serum concentration of Rilpivirine. Rilpivirine may decrease the serum concentration of Ketoconazole (Systemic). Risk C: Monitor therapy
Ledipasvir: May increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Avoid this combination if TDF is used as part of the elvitegravir/cobicistat/emtricitabine/TDF product. Consider alternatives when TDF is used with a ritonavir or cobicistat boosted protease inhibitor. Monitor for increased TDF toxicities if combined. Risk D: Consider therapy modification
Leflunomide: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Leniolisib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination
Levoketoconazole: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Levoketoconazole. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Levomethadone: Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of Levomethadone. Management: Levomethadone dosage adjustments will likely be required with efavirenz and nevirapine, and may be necessary with rilpivirine as well. Risk C: Monitor therapy
Lopinavir: May enhance the nephrotoxic effect of Tenofovir Disoproxil Fumarate. Lopinavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
Lovotibeglogene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Lovotibeglogene Autotemcel. Risk X: Avoid combination
Macrolide Antibiotics: May increase the serum concentration of Rilpivirine. Management: Consider the use of azithromycin or another non-macrolide alternative when appropriate to avoid this potential interaction. Risk D: Consider therapy modification
Methadone: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the metabolism of Methadone. Management: Methadone dosage adjustments will likely be required with efavirenz and nevirapine, and may be necessary with rilpivirine as well. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose due to a potential risk of acute renal failure. Diclofenac appears to confer the most risk. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents (Topical): May enhance the nephrotoxic effect of Tenofovir Products. Risk C: Monitor therapy
Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy
Osimertinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Oteseconazole: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
OXcarbazepine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Pacritinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
PHENobarbital: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Phenytoin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Pretomanid: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Primidone: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Regorafenib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Reverse Transcriptase Inhibitors (Non-Nucleoside): May enhance the adverse/toxic effect of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Reverse Transcriptase Inhibitors (Non-Nucleoside) may decrease the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, efavirenz and nevirapine may decrease the serum concentrations of other non-nucleoside reverse transcriptase inhibitors. Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of other Reverse Transcriptase Inhibitors (Non-Nucleoside). Specifically, delavirdine may increase the serum concentration of etravirine. Risk X: Avoid combination
Rifabutin: May decrease the serum concentration of Rilpivirine. Management: Increase rilpivirine dose to 50 mg/day during rifabutin treatment. Use of rifabutin with emtricitabine/rilpivirine/tenofovir alafenamide product is not recommended. Use with IV cabotegravir/rilpivirine is contraindicated. Risk D: Consider therapy modification
RifAMPin: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Rifapentine: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Rolapitant: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Management: Monitor patients receiving rolapitant for increased exposure to and/or effects of BCRP/ABCG2 substrates. Use the lowest effective rosuvastatin dose when used in combination with rolapitant. Risk C: Monitor therapy
Saquinavir: Rilpivirine may enhance the arrhythmogenic effect of Saquinavir. Saquinavir may increase the serum concentration of Rilpivirine. Risk X: Avoid combination
Sparsentan: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination
St John's Wort: May decrease the serum concentration of Rilpivirine. Risk X: Avoid combination
Tacrolimus (Systemic): Tenofovir Products may enhance the nephrotoxic effect of Tacrolimus (Systemic). Risk C: Monitor therapy
Tafamidis: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Taurursodiol: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination
Tedizolid: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Teriflunomide: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy
Tipranavir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Tipranavir. Tipranavir may decrease the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
Voxilaprevir: Tenofovir Disoproxil Fumarate may increase the serum concentration of Voxilaprevir. Voxilaprevir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor therapy
See individual agents.
The Health and Human Services (HHS) perinatal HIV guidelines consider this fixed-dose combination an alternative regimen for patients with HIV who are not yet pregnant but are trying to conceive (HHS [perinatal] 2023).
Refer to individual monographs for additional information.
The Health and Human Services (HHS) perinatal HIV guidelines recommend this fixed-dose combination an alternative regimen for initial use in pregnant patients with HIV who are antiretroviral naive, who have had antiretroviral therapy (ART) in the past but are restarting, or who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). Patients who become pregnant while taking this combination may continue if viral suppression is effective and the regimen is well tolerated. More frequent monitoring is recommended during pregnancy. This fixed-dose combination may be considered for patients when significant drug interactions would occur with preferred agents or in patients who need the convenience of a co-formulated single dose tablet in a once-daily regimen but are not eligible for preferred agents. This combination should only be used in pregnant patients with a pretreatment HIV RNA ≤100,000 copies/mL or CD4 cell count ≥200 cells/mm3 (HHS [perinatal] 2023).
Refer to individual monographs for additional information.
Emtricitabine and tenofovir disoproxil fumarate are present in breast milk; it is not known if rilpivirine is present in breast milk.
Refer to individual monographs for additional information.
Take with food. Consider calcium and vitamin D supplementation.
CBC with differential, reticulocyte count, creatine kinase, CD4 count, HIV RNA plasma levels; serum phosphorus (chronic kidney disease patients), serum creatinine, estimated creatine clearance, urine glucose, urine protein (prior to initiation and as clinically indicated during therapy); hepatic function tests, bone density (patients with a history of bone fracture or have risk factors for bone loss); fever, skin reactions, and/or hypersensitivity reactions; testing for HBV is recommended prior to the initiation of antiretroviral therapy; weight (children). If used as therapy replacement in virologically suppressed patients meeting criteria, additional HIV-1 RNA and regimen tolerability monitoring is recommended to assess potential virologic failure or rebound.
Patients with HIV and HBV coinfection should be monitored for several months following tenofovir discontinuation.
Non-nucleoside, nucleoside, and nucleotide reverse transcriptase inhibitor combination; rilpivirine binds to reverse transcriptase and does not require intracellular phosphorylation for antiviral activity; emtricitabine is a cytidine analogue while tenofovir disoproxil fumarate (TDF) is an analog of adenosine 5'-monophosphate. Each drug interferes with HIV viral RNA dependent DNA polymerase activities resulting in inhibition of viral replication.
Using the combination tablet, the Cmax and AUC of rilpivirine increased 34% and 9% when taken with a light meal (390 kcal; 12 g fat) and 26% and 16% when taken with a standard meal (540 kcal; 21 g fat); tenofovir Cmax and AUC increased 12% and 28% with a light meal and 32% and 38% with a standard meal.
Also see individual agents.
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