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In human liver microsome (HLM) samples, 7- and 8-hydroxyefavirenz accounted for 22.5 and 77.5% of the overall efavirenz metabolism, respectively. Summary This chapter provides the basic characteristics, FDA‐approved idications, side effects/toxicity and dosage information of the Sustiva (Efavirenz). Caution patient to use a condom, and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others.Instruct patient to report signs of kidney stones (renal calculi), including bloody urine, severe pain in the side and back, pain on urination, and a persistent urge to urinate.Advise patient about the likelihood of GI reactions, including nausea, vomiting, diarrhea, abdominal pain, heartburn, and loss of appetite. 72), which suggests continued non-inferiority of the lower efavirenz dose. Home Books Davis's Drug Guide for Rehabilitation Professionals. Sections; Print; Share. Although CYP2B6 was the main enzyme catalyzing efavirenz 8-hydroxylation, CYP2A6 also seems to contribute. Both 7- and 8-hydroxyefavirenz were further oxidized to novel dihydroxylated metabolite(s) primarily by CYP2B6. AIDS offers perhaps the greatest threat to humans by any infectious disease in his- tory. Instruct patient to report severe or prolonged GI reactions.Instruct patient to report other troublesome side effects such as prolonged or severe headache, sleep loss, abnormal dreams, or a decreased sense of touch (hypoesthesia). David W. Haas Departments of Medicine, Microbiology, and Immunology, and Center for Human Genetics Research, Vanderbilt University School of Medicine, Nashville, Tennessee (See the article by Tarr et al., on pages 1419-26.) Although efavirenz 8-hydroxylation by CYP2B6 remains the major clearance mechanism of efavirenz, CYP2A6-mediated 7-hydroxylation (and to some extent 8-hydroxylation) may also contribute. Efavirenz: Coadministration of efavirenz can alter the concentrations of other drugs and other drugs may alter the concentrations of efavirenz. If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to … Citation. Name /bks_53161_deglins_md_disk/raltegravir 02/17/2014 09:42AM Plate # 0-Composite pg 2 # 2 2015 F.A. Get Free Access Through Your Institution Report severe or unexpected skin reactions to the physician immediately.Monitor excessive headache or fatigue. Please consult the latest official manual style if you have any questions regarding the format accuracy.Pharmacologic: nonnucleoside reverse transcriptase inhibitorsHIV infection (in combination with one or more other antiretroviral agents).Inhibits HIV reverse transcriptase, which results in disruption of DNA synthesis. In human liver microsome (HLM) samples, 7- and 8-hydroxyefavirenz accounted for 22.5 and 77.5% of the overall efavirenz metabolism, respectively. In conclusion, efavirenz metabolism is complex, involving unique and novel secondary metabolism. If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus. Efavirenz may be a valuable dual phenotyping tool to study CYP2B6 and CYP2A6, and this should be further tested in vivo.This work was supported by the National Institutes of Health National Institute of General Medical Sciences [Grants GM078501, GM067308].Article, publication date, and citation information can be found at Thank you for sharing this Drug Metabolism & Disposition article.NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. Efavirenz and its primary and secondary metabolites that were identified in vitro were quantified in plasma samples obtained from subjects taking a single 600-mg oral dose of efavirenz. original article The new england journal of medicine n engl j med 349;11 www.nejm.org september 11, 2003 1036 Substitution of Nevirapine, Efavirenz, or Abacavir for Protease Inhibitors in Patients These dihydroxylated metabolite(s) were not the same as 8,14-dihydroxyefavirenz, a metabolite that has been suggested to be directly formed via 14-hydroxylation of 8-hydroxyefavirenz, because 8,14-dihydroxyefavirenz was not detected in vitro when efavirenz, 7-, or 8-hydroxyefavirenz were used as substrates.
Monitor skin rash and other skin reactions (sweating, pruritus). Explore More Sites Disclaimer: These citations have been automatically generated based on the information we have and it may not be 100% accurate. 8,14-Dihydroxyefavirenz was detected and quantified in these plasma samples, suggesting that the glucuronide or the sulfate of 8-hydroxyefavirenz might undergo 14-hydroxylation in vivo.
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