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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Tipranavir is a protease inhibitor used to treat HIV. It is an FDA category C drug. The Antiretroviral Registry included only 13 first trimester pregnancies exposed to tipranavir; none of the infants had congenital anomalies (Antiretroviral Registry, 2018).
The use of antiviral drugs in children
Published in Journal of Chemotherapy, 2022
Marco Antonio Motisi, Agnese Tamborino, Sara Parigi, Luisa Galli, Maurizio de Martino, Elena Chiappini
The FDA and EMA have recently approved blood dosing of raltegravir (RAL) for babies born at a gestational age ≥37 weeks and weighing ≥2 kg. Dosing information for RAL is not available for preterm or low birth weight infants. RAL is metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, the same enzyme responsible for the elimination of bilirubin. UGT enzyme activity is low at birth and RAL elimination is prolonged in infants. Bilirubin and RAL may compete for albumin binding sites, so extremely high neonatal plasma concentrations of RAL could pose a risk of kernicterus [24]. Paediatric formulations of protease inhibitors are available for lopinavir/ritonavir, darunavir, tipranavir and fosamprenavir; however, the use of these drugs is recommended in newborns with a postmenstrual age of 42 weeks from at least 14 days after birth, due to a lack of information on dosing and safety. In literature, ritonavir/lopinavir therapy has been associated with heart block (reversible upon discontinuation) and adrenal insufficiency with life-threatening dyselectrolycaemia to the point of cardiogenic shock [24].
Dolutegravir plus rilpivirine dual therapy in treating HIV-1 infection
Published in Expert Opinion on Pharmacotherapy, 2018
Amedeo F. Capetti, Maria V. Cossu, Laura Paladini, Giuliano Rizzardini
DTG AUC decreases by 39% if coadministered with calcium carbonate and by 54% with ferrous fumarate in fasting conditions. Taking DTG 2 h before or 6 h after these minerals or with a high-fat meal effectively counteracts such effect [27]. The same effect results from the intake of antacids [22]. Concomitant administration of rifampicin, carbamazepine, or tipranavir reduces DTG Cmin by ≥75%, requiring 50 mg of DTG twice daily. Etravirine (ETV) also reduces DTG Cmin by 88%, but studies have demonstrated that in the presence of a boosted PI (unconventional triple therapy), the effect becomes clinically irrelevant [28]. On the other hand, concomitant administration of ATV resulted in increased DTG concentrations [22,29]. Moreover, the introduction of cobicistat (Cobi) as a booster seems to exert a slight boosting effect toward DTG [30]. In a recent study, DTG had no effect on the outcome of HCV therapy with directly acting agents compared to other third agents used in ART [31]. Finally, DTG has been shown to profoundly alter the pharmacokinetics of metformin; however, the clinical value of this interaction is low [32].
Safety considerations in the management of hepatitis C and HIV co-infection
Published in Expert Opinion on Drug Safety, 2023
Vicente Soriano, Víctor Moreno-Torres, Ana Treviño, Pablo Barreiro, Fernando de Jesus, Octavio Corral, Carmen de Mendoza
CYP450 is by far the major source of drug interactions using either HIV or HCV protease inhibitors, especially when boosted with ritonavir. Drugs that share their metabolism with this liver enzyme may exhibit unique drug concentrations and therefore result in serious toxicities. There is a contraindication of HCV protease inhibitors with the old HIV non-nucleoside reverse transcriptase inhibitors efavirenz, nevirapine, and etravirine. Likewise, HIV protease inhibitors should not be used with HCV protease inhibitors. The exceptional case of tipranavir, which could exhibit a distinct PK profile, nowadays is not relevant since the drug is no longer available.