• Ritonavir, indinavir, and saquinavir, all human immunodeficiency virus-1 protease inhibitors with a potent antiviral effect during triple therapy, are extensively metabolized by liver cytochrome P450 3A4. (aspetjournals.org)
  • The aim of this study was to compare the inhibitory potential of the HIV protease inhibitors ritonavir, indinavir, and saquinavir against methadone and buprenorphine N -dealkylations catalyzed by P450 3A4 in a panel of human liver microsomes. (aspetjournals.org)
  • Although a spectrum of drug biotransformations can occur during first-pass, the most common are oxidations catalyzed by cytochromes P450. (nih.gov)
  • Objectives: The objective of this study was to explore potential drug-drug/food interactions of ciprofloxacin and grapefruit juice, known hepatic cytochrome P450 (CYP) 1A2 inhibitors, on single-dose oral pharmacokinetics of riluzole, a substrate of CYP 1A2 enzymes. (researchgate.net)
  • Smoking cessation Maintaining a healthy weight can go to rinse his Strong cytochrome P450 3A4 inhibitors. (naugachianews.com)
  • Human cytochrome P450 enzymes involved in the bioactivation of estragole to its proximate carcinogen 1′-hydroxyestragole were identified and compared to the enzymes of importance for 1′-hydroxylation of the related alkenylbenzenes methyleugenol and safrole. (tno.nl)
  • In vitro studies were performed to elucidate the human cytochrome P450 enzymes involved in the bioactivation of methyleugenol to its proximate carcinogen 1′-hydroxymethyleugenol. (tno.nl)
  • Possible metabolism of PLD-118 by rat, dog and human S9 liver homogenates and inhibition of human cytochrome P450 (CYP) enzymes were investigated. (tno.nl)
  • The presence in orange juice of compounds that specifically inhibit the P-glycoprotein (P-gp) drug efflux transporter, but not the cytochrome P450 (CYP) isozyme CYP3A4, was investigated. (aspetjournals.org)
  • Coadministration of other medicinal products known to prolong the QT interval and which are metabolised via the cytochrome P450 (CYP) 3A4 such as cisapride, astemizole, pimozide, quinidine, and erythromycin are contraindicated in patients receiving fluconazole (see sections 4.4 and 4.5). (tajgenerics.com)
  • Coadministration of other medicinal products known to prolong the QT interval and which are metabolised via the cytochrome P450 (CYP) 3A4 are contraindicated (see sections 4.3 and 4.5). (tajgenerics.com)
  • Formation of ODV is catalyzed by cytochrome P450 (CYP) 2D6, whereas N-demethylation is catalyzed by CYP3A4, 2C19 and 2C9. (illumina.com)
  • In this study, metabolic interactions between these protease inhibitors and methadone or buprenorphine were studied in vitro in a panel of 13 human liver microsomes. (aspetjournals.org)
  • As the prediction of in vivo metabolic drug interaction from in vitro data has made significant advances in the last decade ( Bertz and Granneman, 1997 ), in vitro data allow us to estimate the likelihood of metabolic interactions between three protease inhibitors and two opioid substitutes. (aspetjournals.org)
  • The relationship between the in vitro susceptibility of HIV-1 RT inhibitors and the inhibition of HIV replication in humans has not been established. (drugs.com)
  • Combining rifampicin and protease inhibitor-based second-line ART is problematic as rifampicin significantly reduces the bioavailability and increases the clearance of protease inhibitors by accelerating their metabolism via induction of cytochrome 3A4 (CYP3A4) enzymes. (biomedcentral.com)
  • It is also clear that some of the substrates for CYP3A4 (e.g., cyclosporine, midazolam, nifedipine, verapamil and saquinavir) undergo significant metabolic extraction by the gut wall. (nih.gov)
  • Inhaled corticosteroids are the preferred treatment to control saquinavir, ketoconazole, telithromycin) with fluticasone propionate and salmeterol people, but there is no cost Of Ventolin Compare to use and Prevention Program. (naugachianews.com)
  • In-vitro metabolic inhibition studies using rat and human liver microsomes and intestinal absorption studies of riluzole in a rat everted gut-sac model were conducted to elucidate the mechanism of interaction. (researchgate.net)
  • In-vitro metabolism studies demonstrated significant inhibition of riluzole metabolism when it was co-incubated with ciprofloxacin or grapefruit juice. (researchgate.net)
  • We applied a recently developed in vitro-in vivo extrapolation method, including hepatic metabolism and transport processes, herein referred to as the Extended Clearance Concept Classification System (ECCCS). (degruyter.com)
  • The ECCCS represents a powerful tool to anticipate the DDI potential of victim drugs based on in vitro drug metabolism and transport data. (degruyter.com)
  • 6. Camenisch G, Umehara K. Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug-drug interactions. (degruyter.com)
  • Cytochrome P-450 (CYP) enzymes are responsible for the metabolism of many drugs, and transporter systems allow for movement of many drugs across cell membranes. (fda.gov)
  • In vitro studies suggest CBD may inhibit a number of drug-metabolizing enzymes, including carboxylesterase 1 (CES1). (inra.fr)
  • Kavalactones have been evaluated in vitro for their potential to alter the activity of various CYP450 enzymes but have undergone little systematic investigation as to their potential influence on esterases. (inra.fr)
  • In recent years, the most common application of hepatic clearance models has been the determination of maximum organ availability of a drug from in vitro derived estimates of intrinsic metabolic clearance. (nih.gov)
  • 5. Umehara K, Camenisch G. Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat. (degruyter.com)
  • The relative success of the in vitro-in vivo approach for both low and highly extracted drugs has led to a broader use by the drug industry for a priori predictions as part of the drug selection process. (nih.gov)
  • Indinavir and saquinavir also inhibited methadone N -demethylation ( K i about 3 and 15 μM, respectively) and buprenorphine N -dealkylation ( K i about 0.8 and 7 μM, respectively). (aspetjournals.org)
  • Use of transporter knockdown Caco-2 cells to investigate the in vitro efflux of statin drugs. (degruyter.com)
  • The drug-drug interaction (DDI) potential of mitragynine and related alkaloids have been evaluated for effects on the major cytochrome P450s (CYPs) via in vitro assays and limited clinical investigations. (inra.fr)
  • Minor) In vitro studies showed that therapeutic levels of aspirin, ASA increased the plasma concentrations of free buspirone by 23% through plasma protein binding displacement. (pdr.net)
  • Although the precise mechanisms underlying HIV lipodystrophy are not well understood, several hypotheses based on in vitro and human studies may explain the pathogenesis of the lipid changes that take place. (medscape.com)
  • Mutations resistant to darunavir [10-14], while infrequent, are more prevalent after treatment failure on amprenavir or saquinavir and as the number of failed PI regimens increases [15]. (thrombin-inhibitor.com)
  • In vitro anti-HIV-1 activity of delavirdine was assessed by infecting cell lines of lymphoblastic and monocytic origin and peripheral blood lymphocytes with laboratory and clinical isolates of HIV-1. (drugs.com)
  • Ill break down all the good and bad CHO cells in vitro or in the mouse feasible to ensure proper. (naugachianews.com)
  • Virological failure was more likely where patients had previously failed on both amprenavir and saquinavir and as the number of previously failed PI regimens increased. (thrombin-inhibitor.com)
  • Its primary mode of action is the inhibition of fungal cytochrome P-450-mediated 14-alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis. (mims.com)
  • Fluconazole has been shown to be more selective for fungal cytochrome P-450 enzymes than for various mammalian cytochrome P-450 enzyme systems. (mims.com)
  • Fluconazole is highly specific for fungal cytochrome P-450 dependent enzymes. (mims.com)
  • 8. A clinical drug-drug interaction study to evaluate the effect of a proton-pump inhibitor, a combined P-glycoprotein/cytochrome 450 enzyme (CYP)3A4 inhibitor, and a CYP2C9 inhibitor on the pharmacokinetics of vismodegib. (nih.gov)
  • In-silico analysis and in-vitro supersaturation test facilitated the selection of HPMC-AS as a best suited polymeric precipitation inhibitor (PPI) for formulating ATZ loaded SP-IM (ATZ-SP-IM). (researchsquare.com)
  • Saquinavir mesylate is an HIV Protease Inhibitor used in antiretroviral therapy. (adooq.com)
  • Bictegravir, also known as GS-9883, is a potent, unboosted, once-Daily HIV-1 Integrase Strand Transfer Inhibitor (INSTI) (IC50 - 1.6 nM) with improved pharmacokinetics and in vitro resistance profile. (adooq.com)
  • INVIRASE is contraindicated in patients with clinically significant hypersensitivity (e.g., anaphylactic reaction, Stevens-Johnson syndrome) to saquinavir, saquinavir mesylate, or any of its ingredients. (nih.gov)
  • This initiative is intended to stimulate investigator-initiated biomedical research on botanical/drug interactions in vitro, in animal models, and in phase I/II clinical studies relevant to the treatment of HIV-infection and its complications. (nih.gov)
  • The data on efficacy, pharmacokinetics, adverse effects, and drug interactions were obtained from in vitro studies, as well as open-label and controlled trials. (nih.gov)
  • In vitro, fluconazole displays antifungal activity against clinically common Candida species (including C. albicans, C. parapsilosis, C. tropicalis ). (mims.com)
  • Fluconazole also exhibits activity in vitro against Cryptococcus neoformans and Cryptococcus gattii as well as the endemic moulds Blastomyces dermatitidis , Coccidioides immitis , Histoplasma capsulatum and Paracoccidioides brasiliensis . (mims.com)
  • In-vitro dissolution data indicated that ATZ-SP-IM exhibits superior performance in 0.025N HCl and pH 6.8 over pure drug. (researchsquare.com)
  • [ 128 ] In addition, in vitro data show a synergistic effect of the PI with some antimalarials such as chloroquine and mefloquine (MQ), and controversial information exist on their potential interaction with artemisinin derivatives. (medscape.com)
  • in contrast, high passive permeability dominates over transporter-mediated uptake for saquinavir over the full concentration range. (aspetjournals.org)