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Drug profiles: generic names A–Z
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Note: Atripla is tenofovir disoproxil, efavirenz and emtricitabine; Complera is tenofovir disoproxil, emtricitabine and rilpivirine; Truvada is tenofovir disoproxil and emtricitabine. See also separate profile for tenofovir disoproxil in combination with cobicistat, elvitegravir and emtricitabine.
Drug profiles: generic names A-Z
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Note: Atripla is tenofovir disoproxil, efavirenz and emtricitabine; Complera is tenofovir disoproxil, emtricitabine and rilpivirine; Truvada is tenofovir disoproxil and emtricitabine. See also separate profile for tenofovir disoproxil in combination with cobicistat, elvitegravir and emtricitabine.
Rilpivirine
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
RPV should be taken with a meal, which increases absorption significantly (Crauwels et al., 2013a). Specifically, a normal breakfast resulted in best RPV absorption; whereas a high-fat breakfast was nearly as good. Fasting or only a high-protein drink (Ensure) achieved absorption ~ 60% less than that achieved with a meal (Crauwels et al., 2013a). It is interesting that the Edurant® (RPV only) approval suggests that it should be taken with a meal, whereas Complera® (RPV with tenofovir and emtricitabine) is approved to be taken with food.
Lipid–drug conjugates and associated carrier strategies for enhanced antiretroviral drug delivery
Published in Pharmaceutical Development and Technology, 2020
Funanani Takalani, Pradeep Kumar, Pierre P. D. Kondiah, Yahya E. Choonara, Viness Pillay
TDF is a prodrug form of tenofovir (TFV) phosphonate which has been developed to improve the oral bioavailability of TFV (Spinks et al. 2017). This prodrug is activated intracellularly through the phosphorylation process to achieve its therapeutic efficacy. During this process, TDF gets converted to its active form (TDF-DP) by cellular enzymes. As compared to TFV which has the solubility of ∼5 mg/mL in aqueous medium, the solubility of TDF is ∼2.5-fold higher at 13.4 mg/mL (Spinks et al. 2017). When tested in vitro, TDF showed increased antiretroviral activity by more than 100-fold and increased TFV-DP concentrations by more than 1000-fold compared to TFV (Hoang et al. 2018). Therefore, due to its increased potency in comparison with TFV, TDF was first approved by the U.S. FDA in 2001 for the treatment of HIV infections and sold under the brand name Viread® (Clercq 2018). It then became available as pills which combine several antiviral drugs into a single dose. This include: (1) Truvada® (combination of TDF and emtricitabine) which was approved in 2004 for treatment of HIV infections and in 2012 for prophylaxis of HIV infections. In 2016, Truvada® was also approved by the EU for prophylaxis infections (2) Atripla® (combination of TDF, emtricitabine, and efavirenz) approved in 2006 (3) Complera® in the USA and Eviplera® in the EU (combination of TDF, emtricitabine, and rilpivirine) approved in 2011 and, (4) Stribild® (combination of TDF, emtricitabine, elvitegravir, and cobicistat) approved in 2012; all for HIV infections (Clercq 2018).
Evaluating emtricitabine + rilpivirine + tenofovir alafenamide in combination for the treatment of HIV-infection
Published in Expert Opinion on Pharmacotherapy, 2020
Ying Mu, Michelle Pham, Anthony T. Podany, Theodore J. Cory
The use of tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC) plus a third agent has been recommended by various guidelines: the WHO suggests TDF+ lamivudine (3TC) or FTC containing regimens as a preferred first-line regimen for ART naïve adults and adolescents [6]. The US Department of Health and Human Services (DHHS) guidelines suggested that Complera®, a fixed dose combination of rilpivirine (RPV), FTC and TDF, may be used as initial therapy for ART naïve patients with HIV-1 RNA ≤100,000 copies/ml or to serve as a substitute regimen for patients who are virologically suppressed (HIV-1 RNA <50 copies/ml, CD4 cell count>200) with other regimens for at least 6 month [9].