Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor
Rilpivirine is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved for HIV-1 treatment-naive adult patients in combination with other antiretroviral agents. The recommended dose is a 25 mg tablet once daily taken orally with a meal. Due to cytochrome P450 3A4 enzyme inducti...
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Veröffentlicht in: | Journal of antimicrobial chemotherapy 2013-02, Vol.68 (2), p.250-256 |
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description | Rilpivirine is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved for HIV-1 treatment-naive adult patients in combination with other antiretroviral agents. The recommended dose is a 25 mg tablet once daily taken orally with a meal. Due to cytochrome P450 3A4 enzyme induction or gastric pH increase, rilpivirine cannot be coadministered with a number of other drugs (anticonvulsants, rifabutin, rifampicin, rifapentine, proton pump inhibitors, systemic dexamethasone and St John's wort). Rilpivirine should be used with caution when coadministered with a drug with a known risk for torsade de pointes. Rilpivirine has a better tolerability than a comparative NNRTI, efavirenz, in clinical trials, with fewer central nervous system adverse effects, rashes, lipid abnormalities and discontinuation rates. Virological failure occurs more commonly with higher baseline viral loads (>100,000 copies/mL) and lower baseline CD4 counts ( |
doi_str_mv | 10.1093/jac/dks404 |
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The recommended dose is a 25 mg tablet once daily taken orally with a meal. Due to cytochrome P450 3A4 enzyme induction or gastric pH increase, rilpivirine cannot be coadministered with a number of other drugs (anticonvulsants, rifabutin, rifampicin, rifapentine, proton pump inhibitors, systemic dexamethasone and St John's wort). Rilpivirine should be used with caution when coadministered with a drug with a known risk for torsade de pointes. Rilpivirine has a better tolerability than a comparative NNRTI, efavirenz, in clinical trials, with fewer central nervous system adverse effects, rashes, lipid abnormalities and discontinuation rates. Virological failure occurs more commonly with higher baseline viral loads (>100,000 copies/mL) and lower baseline CD4 counts (<50 cells/mm(3)). Seventeen NNRTI mutations have been associated with decreased susceptibility to rilpivirine: K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, H221Y, F227C, M230I/L, Y188L and the combination L100I + K103N. Resistance to rilpivirine largely excludes future use of the NNRTI class.</description><identifier>ISSN: 0305-7453</identifier><identifier>EISSN: 1460-2091</identifier><identifier>DOI: 10.1093/jac/dks404</identifier><identifier>PMID: 23099850</identifier><language>eng</language><publisher>England: Oxford Publishing Limited (England)</publisher><subject>Anticonvulsants ; Antiretroviral drugs ; Clinical trials ; Drug Interactions ; Drug Resistance, Viral ; Drug Therapy, Combination - methods ; Drug use ; HIV ; HIV Infections - drug therapy ; HIV Infections - virology ; HIV-1 - drug effects ; Human immunodeficiency virus ; Human immunodeficiency virus 1 ; Humans ; Nitriles - adverse effects ; Nitriles - pharmacology ; Nitriles - therapeutic use ; Pyrimidines - adverse effects ; Pyrimidines - pharmacology ; Pyrimidines - therapeutic use ; Reverse Transcriptase Inhibitors - adverse effects ; Reverse Transcriptase Inhibitors - pharmacology ; Reverse Transcriptase Inhibitors - therapeutic use ; Rilpivirine ; Treatment Outcome ; Virology</subject><ispartof>Journal of antimicrobial chemotherapy, 2013-02, Vol.68 (2), p.250-256</ispartof><rights>Copyright Oxford Publishing Limited(England) Feb 2013</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23099850$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sharma, Mamta</creatorcontrib><creatorcontrib>Saravolatz, Louis D</creatorcontrib><title>Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor</title><title>Journal of antimicrobial chemotherapy</title><addtitle>J Antimicrob Chemother</addtitle><description>Rilpivirine is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved for HIV-1 treatment-naive adult patients in combination with other antiretroviral agents. The recommended dose is a 25 mg tablet once daily taken orally with a meal. Due to cytochrome P450 3A4 enzyme induction or gastric pH increase, rilpivirine cannot be coadministered with a number of other drugs (anticonvulsants, rifabutin, rifampicin, rifapentine, proton pump inhibitors, systemic dexamethasone and St John's wort). Rilpivirine should be used with caution when coadministered with a drug with a known risk for torsade de pointes. Rilpivirine has a better tolerability than a comparative NNRTI, efavirenz, in clinical trials, with fewer central nervous system adverse effects, rashes, lipid abnormalities and discontinuation rates. Virological failure occurs more commonly with higher baseline viral loads (>100,000 copies/mL) and lower baseline CD4 counts (<50 cells/mm(3)). Seventeen NNRTI mutations have been associated with decreased susceptibility to rilpivirine: K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, H221Y, F227C, M230I/L, Y188L and the combination L100I + K103N. Resistance to rilpivirine largely excludes future use of the NNRTI class.</description><subject>Anticonvulsants</subject><subject>Antiretroviral drugs</subject><subject>Clinical trials</subject><subject>Drug Interactions</subject><subject>Drug Resistance, Viral</subject><subject>Drug Therapy, Combination - methods</subject><subject>Drug use</subject><subject>HIV</subject><subject>HIV Infections - drug therapy</subject><subject>HIV Infections - virology</subject><subject>HIV-1 - drug effects</subject><subject>Human immunodeficiency virus</subject><subject>Human immunodeficiency virus 1</subject><subject>Humans</subject><subject>Nitriles - adverse effects</subject><subject>Nitriles - pharmacology</subject><subject>Nitriles - therapeutic use</subject><subject>Pyrimidines - adverse effects</subject><subject>Pyrimidines - pharmacology</subject><subject>Pyrimidines - therapeutic use</subject><subject>Reverse Transcriptase Inhibitors - adverse effects</subject><subject>Reverse Transcriptase Inhibitors - pharmacology</subject><subject>Reverse Transcriptase Inhibitors - therapeutic use</subject><subject>Rilpivirine</subject><subject>Treatment Outcome</subject><subject>Virology</subject><issn>0305-7453</issn><issn>1460-2091</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0EtLw0AUBeBBFFurG3-ABNy4ib2TebsrxRcUBNF1mWRucGo6iTNJxX9vwLpx4-py4OPAuYScU7imYNh8Y6u5e08c-AGZUi4hL8DQQzIFBiJXXLAJOUlpAwBSSH1MJgUDY7SAKVk8-6bzOx99wJvMZgE_s9CGPAxVg23yDrOIO4wJsz7akKrou96OyYc3X_q-jafkqLZNwrP9nZHXu9uX5UO-erp_XC5WeVdA0eeiVgK1QyqERVUqRzlHrVxdMupqhlyitUaWgleVVLqGQpdSiMoJOUIp2Yxc_fR2sf0YMPXrrU8VNo0N2A5pTRnV0kihiv9poZgAWWg20ss_dNMOMYxDRiWNMgI4jOpir4Zyi27dRb-18Wv9-0f2Dfx7c5I</recordid><startdate>201302</startdate><enddate>201302</enddate><creator>Sharma, Mamta</creator><creator>Saravolatz, Louis D</creator><general>Oxford Publishing Limited (England)</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7QL</scope><scope>7QO</scope><scope>7T7</scope><scope>7U7</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>NAPCQ</scope><scope>P64</scope><scope>7X8</scope><scope>7TM</scope></search><sort><creationdate>201302</creationdate><title>Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor</title><author>Sharma, Mamta ; 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The recommended dose is a 25 mg tablet once daily taken orally with a meal. Due to cytochrome P450 3A4 enzyme induction or gastric pH increase, rilpivirine cannot be coadministered with a number of other drugs (anticonvulsants, rifabutin, rifampicin, rifapentine, proton pump inhibitors, systemic dexamethasone and St John's wort). Rilpivirine should be used with caution when coadministered with a drug with a known risk for torsade de pointes. Rilpivirine has a better tolerability than a comparative NNRTI, efavirenz, in clinical trials, with fewer central nervous system adverse effects, rashes, lipid abnormalities and discontinuation rates. Virological failure occurs more commonly with higher baseline viral loads (>100,000 copies/mL) and lower baseline CD4 counts (<50 cells/mm(3)). Seventeen NNRTI mutations have been associated with decreased susceptibility to rilpivirine: K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, H221Y, F227C, M230I/L, Y188L and the combination L100I + K103N. Resistance to rilpivirine largely excludes future use of the NNRTI class.</abstract><cop>England</cop><pub>Oxford Publishing Limited (England)</pub><pmid>23099850</pmid><doi>10.1093/jac/dks404</doi><tpages>7</tpages></addata></record> |
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source | MEDLINE; Oxford University Press Journals All Titles (1996-Current); EZB-FREE-00999 freely available EZB journals; Alma/SFX Local Collection; Free Full-Text Journals in Chemistry |
subjects | Anticonvulsants Antiretroviral drugs Clinical trials Drug Interactions Drug Resistance, Viral Drug Therapy, Combination - methods Drug use HIV HIV Infections - drug therapy HIV Infections - virology HIV-1 - drug effects Human immunodeficiency virus Human immunodeficiency virus 1 Humans Nitriles - adverse effects Nitriles - pharmacology Nitriles - therapeutic use Pyrimidines - adverse effects Pyrimidines - pharmacology Pyrimidines - therapeutic use Reverse Transcriptase Inhibitors - adverse effects Reverse Transcriptase Inhibitors - pharmacology Reverse Transcriptase Inhibitors - therapeutic use Rilpivirine Treatment Outcome Virology |
title | Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor |
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