{"id":15012,"date":"2011-05-01T11:00:19","date_gmt":"2011-05-01T11:00:19","guid":{"rendered":"http:\/\/i-base.info\/htb\/?p=15012"},"modified":"2014-09-09T13:39:48","modified_gmt":"2014-09-09T13:39:48","slug":"lopinavirr-reduces-levels-of-rifabutin","status":"publish","type":"post","link":"https:\/\/i-base.info\/htb\/15012","title":{"rendered":"Lopinavir\/r reduces levels of rifabutin"},"content":{"rendered":"

HIV-druginteractions.org<\/strong><\/p>\n

This preliminary study investigated rifabutin and LM565 (25 O desacetyl rifabutin) exposures in 14 HIV\/TB coinfected patients starting LPV\/r (400\/100 mg twice-daily) and rifabutin (150 mg 3 times weekly). Control values for rifabutin alone (300 mg once-daily) were obtained prior to starting LPV\/r. Control values for LPV\/r alone were obtained 10 weeks after stopping rifabutin. Pharmacokinetic parameters (median, range) are shown in the Table 1.<\/p>\n

Rifabutin AUC was below the target of 4.5 \u00b5g.h\/ml in 42% of patients at week 2 of therapy and in 28% of patients at week 6 of therapy. The change in LM565 AUC was significantly greater than the change in rifabutin AUC. When given with LPV\/r, rifabutin 150 mg three times weekly may result in low rifabutin concentrations.<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Table 1: Rifabutin, LM565 and lopinavir levels administered separately and together<\/caption>\n
<\/td>\nRifabutin alone<\/th>\nRifabutin + LPV\/r week 2<\/th>\nRifabutin + LPV\/r week 6<\/th>\nLPV\/r alone<\/th>\n<\/tr>\n
Median (range) Rifabutin<\/th>\n<\/tr>\n
AUC 0-24h (g.h\/mL)<\/th>\n330 (106-1950)<\/td>\n4.2 (1.9-5.5)<\/td>\n2.4 (1.3-6.4)<\/td>\n<\/td>\n<\/tr>\n
Ctrough (ng\/mL)<\/th>\n91 (11-152)<\/td>\n87 (20-104)<\/td>\n42 (8-114)<\/td>\n<\/td>\n<\/tr>\n
Cmax (ng\/mL)<\/th>\n330 (106-1950)<\/td>\n309 (106-564)<\/td>\n239 (151-526)<\/td>\n<\/td>\n<\/tr>\n
Median (range) LM565<\/th>\n<\/tr>\n
AUC 0-24h (g.h\/mL)<\/th>\n0.7 (0.18-2.4)<\/td>\n1.6 (0.35-2.6)<\/td>\n1.6 (0.79-2.4)<\/td>\n<\/td>\n<\/tr>\n
Ctrough (ng\/mL)<\/th>\n4 (3-10)<\/td>\n33 (10-71)<\/td>\n30 (13-75)<\/td>\n<\/td>\n<\/tr>\n
Cmax (ng\/mL)<\/th>\n52 (32-72)<\/td>\n115 (90-190)<\/td>\n122 (40-221)<\/td>\n<\/td>\n<\/tr>\n
Median (range) LPV<\/th>\n<\/tr>\n
AUC 0-24h (g.h\/mL)<\/th>\n<\/td>\n143 (86-278)<\/td>\n137 (47-303)<\/td>\n124 (75-139)<\/td>\n<\/tr>\n
Ctrough (ng\/mL)<\/th>\n<\/td>\n10 (5.6-20)<\/td>\n8.8 (1-17.6)<\/td>\n7.8 (5.1-9)<\/td>\n<\/tr>\n
Cmax (ng\/mL)<\/th>\n<\/td>\n14.4 (9.2-34)<\/td>\n16.3 (15.4-33)<\/td>\n13.7 (7.8-20.9)<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

comment<\/h2>\n

This study highlights the importance of the active metabolite when rifabutin is given with LPV\/r.<\/strong><\/p>\n

Reference:<\/p>\n

Cusato M et al.\u00a0\u00a0Pharmacokinetic evaluation of rifabutin and its active metabolite LM565 coadministered with lopinavir\/r in HIV infected patients.\u00a012th International Workshop on Clinical Pharmacology of HIV Therapy, 13\u0096-15 April 2011, Miami. Oral abstract: O_14.<\/p>\n","protected":false},"excerpt":{"rendered":"

HIV-druginteractions.org This preliminary study investigated rifabutin and LM565 (25 O desacetyl rifabutin) exposures in 14 HIV\/TB coinfected patients starting LPV\/r (400\/100 mg twice-daily) and rifabutin (150 mg 3 times weekly). Control values for rifabutin alone (300 mg once-daily) were obtained …<\/p>\n","protected":false},"author":2,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[4,3,34],"tags":[135],"class_list":["post-15012","post","type-post","status-publish","format-standard","hentry","category-conference-reports","category-antiretrovirals","category-pk-and-drug-interactions","tag-pk-workshop-12th-2011"],"_links":{"self":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/15012","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/users\/2"}],"replies":[{"embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/comments?post=15012"}],"version-history":[{"count":0,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/posts\/15012\/revisions"}],"wp:attachment":[{"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/media?parent=15012"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/categories?post=15012"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/i-base.info\/htb\/wp-json\/wp\/v2\/tags?post=15012"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}