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Efavirenz
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
Alan C. Street, Irani Thevarajan
Rilpivirine is well tolerated but compared with efavirenz, it is less effective and associated with more frequent development of resistance in patients with a baseline HIV viral load > 100,000 copies/ml. All treatment guidelines advise that rilpivirine should be used only for initial therapy in patients with a baseline viral load ≤ 100,000 copies/ml and that it should be administered as the fixed-dose combination of tenofovir plus emtricitabine plus rilpivirine; in the 2015 US Department of Health and Human Services (DHHS) guidelines, it is listed as an alternative agent if the baseline CD4 cell count is > 200/μl (Panel on Antiretroviral Guidelines for Adults and Adolescents, 2015), in the 2014 US IAS-USA guidelines as a recommended agent (Gunthard et al., 2014), in the 2015 UK guidelines as a preferred agent (British HIV Association, 2015), and in the 2015 European guidelines as a recommended agent if the baseline CD4 cell count is > 200/μl (European AIDS Clinical Society Guidelines Panel, 2015).
Optimising Antiretroviral Therapy Via Pharmacokinetics
Published in Anne George, K. S. Joshy, Mathew Sebastian, Oluwatobi Samuel Oluwafemi, Sabu Thomas, Holistic Approaches to Infectious Diseases, 2017
Like other NNRTIs, rilpivirine binds to the reverse transcriptase enzyme to terminate the viral DNA replication. It is effective against most of the HIV-1 patients who are resistant to other NNRTIs. This is believed to be the result of its internal conformational flexibility and the plasticity of its interaction with the binding site. Relpivirine mainly undergoes oxidative metabolism followed by sulfate conjugation. It causes cytochrome P450 3A4 enzyme induction due to which combination with other drugs should be made carefully. Rilipivirine has better tolerance and only a few CNS side effects compared to other NNRTIs. Adult oral dosage is 25 mg once a day (Lewis, 2000).
Cabotegravir and rilpivirine for the treatment of HIV
Published in Expert Review of Anti-infective Therapy, 2020
David Rial-Crestelo, Adriana Pinto-Martínez, Federico Pulido
Rilpivirine (Tibotec Medicinal Compound 278, TMC278), a diarylpyrimidine derivative, is a second-generation NNRTI, with activity against wild type and NNRTI-resistant HIV-1 [28]. Oral rilpivirine is approved for the treatment of HIV-1-infected individuals with VL<100,000 copies/mL, at a 25 mg daily dose [29–31]. The LA injectable preparation has been developed as a particle with a size of approximately 200 nm in a poloxamer suspension of 300 mg/mL of rilpivirine. Like cabotegravir, rilpivirine is composed of the pure compound and it is not wrapped in a nanoparticle micelle. The dose proposed in prevention trials is 1200 mg, requiring 2 × 2 mL intramuscular (IM) gluteal injections. For treatment, LA rilpivirine is being evaluated at doses of 600 mg (1 × 2 mL) q4 w, and 900 mg (1 × 3 mL) q8 w [26,32]. The pharmacokinetic profile of LA rilpivirine exhibits an extended half-life and plasma concentrations, enabling dosing every one or 2 months [28].
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
Rilpivirine Rilpivirine (TMC-278) safety, antiviral activity, and efficacy were evaluated in several Phase I/II trails. In a Phase, IIa 7-day study of treatment-naïve HIV-infected adults, antiviral activity of rilpivirine was assessed at doses of 25, 50, 100, or 150-mg daily. Each of the doses studied was shown to be efficacious against HIV with a median viral load decline of 1.199 log10 copies per mL; however, no dose-response relationship could be established. The doses studied were well tolerated and no dose-related adverse events developed [42]. A larger 96-week Phase IIb study of 368 patients evaluated the efficacy and safety of rilpivirine in the treatment-naïve HIV-infected individuals. Rilpivirine doses of 25, 75, and 150 mg were compared with efavirenz 600 mg, all once daily with two nucleosides. Each of the rilpivirine doses demonstrated non-statistically significant differences in viral efficacy compared with efavirenz at both 48 and 96 weeks. Again, no dose-response relationship was observed for either efficacy or safety [43].
Community-acquired bacterial pneumonia in adult HIV-infected patients
Published in Expert Review of Anti-infective Therapy, 2018
Catia Cillóniz, Carolina García-Vidal, Asunción Moreno, José M. Miro, Antoni Torres
Azithromycin may cause abnormal changes in the electrical activity of the heart and can induced QTc interval prolongation and Torsade de pointes. This adverse event should be taken into account when antiretrovirals can increase its exposure (like ritonavir-boosted protease inhibitors) or can also increase QT interval (rilpivirine). Azithromycin is mainly eliminated via biliary excretion and animal data suggest this may occur via P-glycoprotein and MRP2. Ritonavir-boosted regimens could potentially increase azithromycin exposure (inhibition of P-glycoprotein and MRP2); however, no a priori dosage adjustment is recommended for azithromycin. Cobicistat is not expected to inhibit hepatic P-gp and MRP2 at clinically relevant concentrations and can be given concomitantly with azithromycin. Rilpivirine (an NNRTIs drug) should be used with caution when coadministered with a drug with a known risk of Torsade de Pointes. In healthy subjects, supratherapeutic doses of rilpivirine (75 mg once daily and 300 mg once daily) have been shown to prolong the QTc interval.