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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
An integrase inhibitor, elvitegravir is used to treat HIV infection. 213 women used it during the first trimester (Antiretroviral Registry, 2018). The frequency of congenital anomalies was not increased above background (www.apregistry.com/forms/interim_report.pdf).
Elvitegravir
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
Mary W. Montgomery, Paul E. Sax
Elvitegravir is approved by the US FDA and European commission to treat HIV-1 infection as part of combination therapy in treatment-naive and treatment-experienced patients. See Table 250.5 for a summary of major clinical trials of elvitegravir.
Antiretroviral treatment for HIV infection: Swedish recommendations 2019
Published in Infectious Diseases, 2020
Jaran Eriksen, Christina Carlander, Jan Albert, Leo Flamholc, Magnus Gisslén, Lars Navér, Veronica Svedhem, Aylin Yilmaz, Anders Sönnerborg
Dolutegravir does not affect CYP450 enzymes and treatment is therefore not expected to affect the pharmacokinetics of other drugs to the same extent as PI and NNRTI. An important exception is the commonly used medicine metformin, which increases in concentration in co-treatment and must therefore be given at a low dose. Dolutegravir is eliminated mainly through UGT1A1 but is also metabolized to a certain extent through CYP 3A4 and other medicines may therefore affect dolutegravir exposure. Dolutegravir exposure decreases in co-treatment with inducers such as efavirenz, carbamazepine, and rifampicin. In such co-treatment in patients without INSTI resistance dolutegravir should be given twice daily. The co-treatment should not be given in patients with suspected or confirmed INSTI resistance. Raltegravir and elvitegravir interact similarly to dolutegravir. Note that elvitegravir is given in fixed combinations containing cobicistat, which inhibits CYP3A and thereby interacts with several other medicines (see PI above).
Beyond one pill, once daily: current challenges of antiretroviral therapy management in the United States
Published in Expert Review of Clinical Pharmacology, 2019
Mary Clare Masters, Karen M. Krueger, Janna L. Williams, Lindsay Morrison, Susan E. Cohn
Treatment of active tuberculosis (TB), latent TB and nontuberculous mycobacterium (NTM) infections in PWH may have a substantial impact on ART selection. Rifamycins are the backbone of TB therapy and potent inducers of the CYP450, P-glycoprotein and uridine diphosphate glucuronosyltransferase (UGT) 1A1 enzymes which cause increased metabolism of antiretrovirals. The current US Department of Health and Human Services (DHHS) Guidelines do not recommend the use of rifampin and rifapentine with PIs, both boosted and unboosted, because of the potential for reduced levels of antiretroviral activity [10]. On the other hand, rifabutin, which is a substrate of the CYP450 enzyme system, may be used with PIs but requires dose-reduction (rifabutin 150 mg daily). Among the NNRTIs, only efavirenz (EFV) is recommended for use with rifamycins. With regards to INSTIs, BIC and cobicistat-boosted elvitegravir (EVG) are contraindicated with rifamycins. However, RAL can be administered with rifamycins [47]. Raltegravir should be increased to 800 mg twice daily if used with rifampin but can be given at 400 mg twice daily when used with a rifabutin-containing TB regimen [10]. Dolutegravir can also be used but current data suggest that increasing the dose to 50 mg twice a day is recommended when used with rifampin but no dose increased was needed with rifabutin even at 300 mg daily [1,10,48,49]. Within the NRTIs, TDF, ABC, 3TC, and FTC can be given together with rifampin-containing TB treatment without dose adjustment. TAF should be used with caution since PK and virologic efficacy with ART and TB regimens have not yet been completed [10].
Pharmacological approaches to prevent vertical transmission of HIV and HBV
Published in Expert Review of Clinical Pharmacology, 2022
Emanuela Zappulo, Agnese Giaccone, Nicola Schiano Moriello, Ivan Gentile
Elvitegravir (EVG) when boosted with cobicistat showed drug levels below the inhibitory concentration during the third trimester and postpartum, and a consistent incidence of viral breakthroughs has been reported [Momper 2018, Boyd 2019]. Based on these data, EVG/c is not recommended for initial use in pregnancy. Limited data are available concerning the EVG safety in this setting: despite sporadic birth defects have been reported in infants exposed to EVG in utero, a clearly increased risk of adverse outcomes has never been observed [61].