natgillin/translations-raw huggingface dataset:
Blandt de co- inficerede patienter stoppede 3% i efavirenz - gruppen og 2% i kontrolgruppen på grund af sygdomme i lever og galdeveje.
Among co-infected patients, 3% of those treated with efavirenz-containing regimens and 2% in the control arm discontinued from the study because of liver or biliary system disorders.
4. 4).
Reasons for discontinuation among co-infected recipients of efavirenz included abnormalities in hepatic enzymes; there were no discontinuations reported in this study for cholestatic hepatitis, hepatic failure, or fatty liver (see section 4.4).
I en undergruppe på 1. 008 patienter i en klinisk undersøgelse, blev der set asymptomatiske stigninger i serumamylase niveauet, til mere end 1, 5 gange den øvre normalgrænse hos 10% af de patienter, der blev behandlet med efavirenz og 6% af de patienter, der blev behandlet med kontrolregimer.
Amylase: in the clinical trial subset of 1,008 patients, asymptomatic increases in serum amylase levels greater than 1.5 times the upper limit of normal were seen in 10% of patients treated with efavirenz and 6% of patients treated with control regimens.
Der sås forhøjelser af totalkolesterol på 10 – 20% hos en del ikke- inficerede frivillige, der fik efavirenz.
Lipids: increases in total cholesterol of 10 - 20% have been observed in some uninfected volunteers receiving efavirenz.
21 – 31%, 23 – 34% og 23 – 49%).
In clinical trials of various efavirenz-containing regimens in treatment naive patients, total cholesterol, HDL-cholesterol, and triglycerides increased over 48 weeks of treatment (21 – 31%, 23 – 34%, and 23 – 49%, respectively).
Andelen af patienter med et forhold mellem totalkolesterol/ HDL- kolesterol på mere end 5, var uændret.
The proportion of patients with a total cholesterol/ HDL-cholesterol ratio greater than 5 was unchanged.
Størrelsen af ændringerne i lipidniveauer kan være påvirket af faktorer såsom varighed af behandlingen og andre komponenter i det antiretrovirale regimen.
The magnitude of changes in lipid levels may be influenced by factors such as duration of therapy and other components of the antiretroviral regimen.
Efavirenz binder sig ikke til cannabinoidreceptorer.
Cannabinoid test interaction: efavirenz does not bind to cannabinoid receptors.
Der er rapporteret falsk positive resultater af urinprøver for cannabinoid hos ikke- inficerede frivillige, som fik efavirenz.
False positive urine cannabinoid test results have been reported in uninfected volunteers who received efavirenz.
Falsk positive prøveresultater sås kun med CEDIA DAU Multi- Level THC test, som anvendes til screening, og er ikke set med andre anvendte cannabinoid- tests inklusive tests anvendt til bekræftelse af positive resultater.
False positive test results have only been observed with the CEDIA DAU Multi-Level THC assay, which is used for screening, and have not been observed with other cannabinoid assays tested including tests used for confirmation of positive results.
Cerebellare
Postmarketing experience with efavirenz has shown the following additional adverse reactions to occur in association with efavirenz-containing antiretroviral treatment regimens: cerebellar coordination and balance disturbances, delusion, hepatic failure, neurosis, photoallergic dermatitis, psychosis and completed suicide.
Hos børn var bivirkningerne generelt de samme som hos voksne patienter.
19 Paediatric patients: undesirable effects in children were generally similar to those of adult patients.
Der rapporteredes oftere om udslæt hos børn (i en klinisk undersøgelse, der omfattede 57 børn, som fik efavirenz i en periode på 48 uger, blev der rapporteret om udslæt hos 46%) og var oftere mere omfattende end hos voksne (alvorligt udslæt blev rapporteret hos 5, 3% af børnene).
Rash was reported more frequently in children (in a clinical study including 57 children who received efavirenz during a 48-week period, rash was reported in 46%) and was more often of higher grade than in adults (severe rash was reported in 5.3% of children).
I en undersøgelse, der omfattede 57 børn oplevede 3, 5% symptomer fra nervesystemet af moderat intensitet, fortrinsvis svimmelhed.
In the study of 57 children, 3.5% of patients experienced nervous system symptoms of moderate intensity, predominantly dizziness.
Behandling af overdosis med efavirenz bør bestå i almindelige, støttende foranstaltninger inklusive monitorering af objektive symptomer og observation af patientens kliniske tilstand.
Treatment of overdose with efavirenz should consist of general supportive measures, including monitoring of vital signs and observation of the patient ’ s clinical status.
Non- nukleoside reverse transkriptasehæmmere.
Non-nucleoside reverse transcriptase inhibitors.
Efavirenz er en NNRTIer af HIV- 1.
Mechanism of action: efavirenz is a NNRTI of HIV-1.
Efavirenz er en nonkompetetiv hæmmer af HIV- 1 reverse transkriptase (RT) og hæmmer ikke signifikant HIV- 2 RT eller cellulære DNA - polymeraser (α, β, γ eller δ).
Efavirenz is a non-competitive inhibitor of HIV-1 reverse transcriptase (RT) and does not significantly inhibit HIV-2 RT or cellular DNA polymerases (α, β, γ or δ).
Den frie koncentration af efavirenz, der er nødvendig for 90 – 95% hæmning af vildtype - eller zidovudinresistente laboratorieisolater og kliniske isolater in vitro var fra 0, 46 til 6, 8 nM i lymfoblastoide cellelinier, perifere mononukleare blodlegemer (PBMCer) og makrofag - / monocytkulturer.
Antiviral activity: the free concentration of efavirenz required for 90 to 95% inhibition of wild type or zidovudine-resistant laboratory and clinical isolates in vitro ranged from 0.46 to 6.8 nM in lymphoblastoid cell lines, peripheral blood mononuclear cells (PBMCs) and macrophage/ monocyte cultures.
Ved cellekultur var potensen af efavirenz over for virusvarianter med aminosyresubstitutioner på positionerne 48, 108, 179, 181 eller 236 i RT eller varianter med aminosyresubstitutioner i proteasen lig den, der sås over for vildtype- virusstammer.
Resistance: the potency of efavirenz in cell culture against viral variants with amino acid substitutions at positions 48, 108, 179, 181 or 236 in RT or variants with amino acid substitutions in the protease was similar to that observed against wild type viral strains.
De enkelte substitutioner, der resulterede i den største resistens over for efavirenz ved cellekultur, svarer til en leucin- til- isoleucin forandring på position 100 (L100I, 17 til 22 gange så stor resistens) og en lysin- til - asparagin på position 103 (K103N, 18 til 33 gange så stor resistens).
The single substitutions which led to the highest resistance to efavirenz in cell culture correspond to a leucine-to-isoleucine change at position 100 (L100I, 17 to 22-fold resistance) and a lysine-to-asparagine at position 103 (K103N, 18 to 33-fold resistance).
Mere end 100 gange mindre følsomhed sås over for HIV- varianter, der eksprimerer K103N foruden andre aminosyresubstitutioner i RT.
Greater than 100-fold loss of susceptibility was observed against HIV variants expressing K103N in addition to other amino acid substitutions in RT.
K103N var den hyppigst sete RT- substitution i virale isolater fra patienter, som oplevede markant reboundfænomen af virus i blodet i løbet af kliniske undersøgelser af efavirenz i kombination med indinavir eller zidovudin + lamivudin.
K103N was the most frequently observed RT substitution in viral isolates from patients who experienced a significant rebound in viral load during clinical studies of efavirenz in combination with indinavir or zidovudine + lamivudine.
Der blev også observeret substitutioner på RT - positionerne 98, 100, 101, 108, 138, 188, 190 eller 225, men med lavere frekvenser og ofte kun i kombination med K103N.
Substitutions at RT positions 98, 100, 101, 108, 138, 188, 190 or 225 were also observed, but at lower frequencies, and often only in combination with K103N.
Mønstret for aminosyresubstitutioner i RT, der er forbundet med resistens
The pattern of amino acid substitutions in RT associated with resistance to efavirenz was independent of the other antiviral medications used in combination with efavirenz.
23 over for efavirenz var uafhængigt af de andre antivirale medikamenter, der anvendtes i kombination med efavirenz.
Cross resistance: cross resistance profiles for efavirenz, nevirapine and delavirdine in cell culture demonstrated that the K103N substitution confers loss of susceptibility to all three NNRTIs.
Krydsresistens:
20 the K103N substitution.
Virale isolater, der er indhentet fra PBMCer fra patienter, der var inkluderet i kliniske efavirenzundersøgelser, som viste tegn på behandlingssvigt (reboundfænomen af virus i blodet) blev vurderet med henblik på følsomhed over for NNRTI’ ere.
Viral isolates recovered from PBMCs of patients enrolled in efavirenz clinical studies who showed evidence of treatment failure (viral load rebound) were assessed for susceptibility to NNRTIs.
Man fandt, at 5 af disse NNRTI- resistente isolater havde K103N - eller en valin- til- isoleucin- substitution på position 108 (V108I) i RT.
Five of these NNRTI-resistant isolates were found to have K103N or a valine-to-isoleucine substitution at position 108 (V108I) in RT.
3 af de testede efavirenz- behandlingssvigtisolater forblev følsomme over for efavirenz ved cellekultur og var også følsomme over for nevirapin og delavirdin.
Three of the efavirenz treatment failure isolates tested remained sensitive to efavirenz in cell culture and were also sensitive to nevirapine and delavirdine.
Potentialet for krydsresistens mellem efavirenz og PI' ere er lille på grund af de forskellige enzymmål, der er involverede.
The potential for cross resistance between efavirenz and PIs is low because of the different enzyme targets involved.
Potentialet for krydsresistens mellem efavirenz og NRTI’ ere er lille på grund af de forskellige bindingssteder på målet og virkningsmekanismen.
The potential for cross-resistance between efavirenz and NRTIs is low because of the different binding sites on the target and mechanism of action.
Efavirenz er ikke undersøgt i kontrollerede undersøgelser med patienter med fremskreden HIV- sygdom, det vil sige CD4 tal < 50 celler/ mm3 eller med PI - eller NNRTI- erfarne patienter.
Efavirenz has not been studied in controlled studies in patients with advanced HIV disease, namely with CD4 counts < 50 cells/ mm3, or in PI or NNRTI experienced patients.
1 års varighed med efavirenz i kombination med NRTI’ ere og/ eller PI' ere har vist en reduktion i mængden af virus i blodet til under detektionsgrænsen i assayet og stigning i CD4 lymfocytter hos antiretroviral behandlingsnaive og NRTI- behandlede HIV- inficerede patienter.
Two controlled studies (006 and ACTG 364) of approximately one year duration with efavirenz in combination with NRTIs and/ or PIs, have demonstrated reduction of viral load below the limit of quantification of the assay and increased CD4 lymphocytes in antiretroviral therapy-naïve and NRTI-experienced HIV-infected patients.
I disse undersøgelser var efavirenzdosis 600 mg en gang dagligt; indinavirdosis på 1. 000 mg hver 8. time blev anvendt i kombination med efavirenz, og 800 mg hver 8. time blev anvendt uden efavirenz.
In these studies the dose of efavirenz was 600 mg once daily; the dose of indinavir was 1,000 mg every 8 hours when used with efavirenz and 800 mg every 8 hours when used without efavirenz.
Standarddoserne af NRTI’ ere, givet hver 12. time, blev anvendt i hver af disse studier.
The standard doses of NRTIs given every 12 hours were used in each of these studies.
Undersøgelse 006, en randomiseret, ublindet undersøgelse, sammenlignede efavirenz + zidovudin + lamivudin eller efavirenz + indinavir med indinavir + zidovudin + lamivudin hos 1. 266 patienter, som ikke tidligere var behandlet med efavirenz, lamivudin, NNRTI’ ere eller PI´ere.
Study 006, a randomized, open-label trial, compared efavirenz + zidovudine + lamivudine or efavirenz + indinavir with indinavir + zidovudine + lamivudine in 1,266 patients who were required to be efavirenz-, lamivudine-, NNRTI-, and PI-naive at study entry.
Det gennemsnitlige CD4 celletal ved baseline var 341 celler/ mm3, og gennemsnitligt HIV- RNA niveau var 60. 250 koPI' er/ ml.
The mean baseline CD4 cell count was 341 cells/ mm3 and the mean baseline HIV-RNA level was 60,250 copies/ ml.
I analysen af responsraten (non- completer lig med failure analysen[ NC = F]), blev patienter, der udgik af studiet tidligt uanset grund, patienter som manglede en HIV- RNA måling som enten var forudgået eller blev efterfulgt af en måling over assaygrænsen, formodet at have HIV- RNA over 50 eller over 400 koPI' er/ ml på de manglende tidspunkter.
In the analysis of responder rates (the non-completer equals failure analysis [NC = F]), patients who terminated the study early for any reason, or who had a missing HIV-RNA measurement that was either preceded or followed by a measurement above the limit of assay quantification were considered to have HIV-RNA above 50 or above 400 copies/ ml at the missing time points.
24 Tabel 3:
Table 3:
Effektresultat for undersøgelse 006
Efficacy results for study 006
Respons hyppigheder (NC = Fa) Plasma HIV- RNA
Responder rates (NC = Fa) Plasma HIV-RNA
Middelændring fra baseline- CD4 celletal
Mean change from baseline-CD4 cell count
< 400 koPI' er/ ml (95% C. I.) b
400 copies/ ml (95% C. I. b)
< 50 koPI' er/ ml (95% C. I.) b
< 50 copies/ ml (95% C. I. b)
Celler/ mm3 (S. E. M.) c
cells/ mm3 (S. E. M. c)
Beha
Treatme
ndlings - n
nt n
regimed EFV + ZDV + 3TC
Regimend EFV +
67% (60%, 73%)
67%
62% (55%, 69%)
62%
EFV + IDV
ZDV + 3TC EFV + IDV
54% (47%, 61%)
%, 73%) 54%
48% 41%, 55%)
(55%, 69%) 48%
177 (11, 3)
(11.8) 177
IDV + ZDV + 3TC a
IDV +
45% (38%, 52%)
45%
40% (34%, 47%)
40%
153 (12, 3)
153
NC = F, noncompleter = failure b C. I., konfidensinterval. c S. E. M.
C. I., confidence interval.
Standard afvigelse på middelværdi d EFV, efavirenz; ZDV, zidovudin, 3TC, lamivudin; IDV, indinavir.
S. E. M., standard error of the mean. d EFV, efavirenz; ZDV, zidovudine; 3TC, lamivudine; IDV, indinavir.
Langtidsresultater efter 168 uger i Undersøgelse 006 (160 patienter fuldførte undersøgelsen med EFV+IDV, 196 med EFV+ZDV+3TC og 127 patienter med IDV+ZDV+3TC) tyder på varigt respons med hensyn til mængden af patienter med HIV RNA < 400 koPI' er/ ml, HIV RNA < 50 koPI' er/ ml og med hensyn til middelændring fra baseline af CD4 celletal.
Long-term results at 168 weeks of study 006 (160 patients completed study on treatment with EFV +IDV, 196 patients with EFV + ZDV + 3TC and 127 patients with IDV + ZDV + 3TC, respectively), suggest durability of response in terms of proportions of patients with HIV RNA < 400 copies/ ml, HIV RNA < 50 copies/ ml and in terms of mean change from baseline CD4 cell count.
Lægen kunne skifte patienternes NRTI regime ved indgangen til studiet.
Physicians were allowed to change their patient ’ s NRTI regimen upon entry into the study.
Responsraten var højest for de patienter, som skiftede NRTI’ ere.
Responder rates were highest in patients who switched NRTIs.
Effektresultater for undersøgelserne ACTG 364 og 020
Efficacy results for studies ACTG 364 and 020
Respons hyppigheder (NC = Plasma HIV- RNA
Responder rates (NC = Fa)
Fa)
Plasma HIV-RNA
Middelændring fra baseline- CD4 celletal
baseline-CD4 cell count
ndersøgelsesnr. / n
%
% (95% C. I. c)%
(95
celler/ mm3 (S. E. M. d)
cells/ mm3 (S. E. M. d)
Behandlingsregimerb Undersøgelse ACTG 364 48 uger
Study ACTG 364 48 weeks
< 500 koPI' er/ ml
< 500 copies/ ml
< 50 koPI' er/ ml
< 50 copies/ ml
EFV + NFV + NRTI’ ere EFV + NRTI’ ere NFV + NRTI’ ere
EFV + NFV + NRTIs EFV + NRTIs NFV + NRTIs
70 (59, 82) 58 (46, 70) 30 (19, 42)
70 58 30
< 400 koPI' er/ ml
< 400 copies/ ml
EFV + IDV + NRTI’ ere IDV + NRTI’ ere a
EFV + IDV + NRTIs IDV + NRTIs a
49 (41, 58) 38 (30, 45)
49 38
NC = F, non- completer = failure b EFV, efavirenz; ZDV, zidovudin; 3TC, lamivudin; IDV, indinavir; NRTI, nucleoside reverse transkriptasehæmmer; NFV, nelfinavir c C. I., konfidensinterval for antal patienter med respons d S. E. M., Standard afvigelse på middelværdi --- Ikke udført
NC = F, noncompleter = failure. b EFV, efavirenz; ZDV, zidovudine; 3TC, lamivudine; IDV, indinavir; NRTI, nucleoside reverse transcriptase inhibitor; NFV, nelfinavir. c C. I., confidence interval for proportion of patients in response. d S. E. M., standard error of the mean. ---, not performed.
Pædiatrisk undersøgelse:
Paediatric trial:
ACTG 382 er en igangværende ukontrolleret undersøgelse af 57 NRTI - erfarne, pædiatriske patienter (3 - 16 år), som beskriver farmakokinetik, antiviral aktivitet og sikkerhed af efavirenz i kombination med nelfinavir (20- 30 mg/ kg indgivet 3 gange om dagen) og et eller flere NRTI’ ere.
ACTG 382 is an ongoing uncontrolled study of 57 NRTI-experienced paediatric patients (3 - 16 years) which characterises the pharmacokinetics, antiviral activity and safety of efavirenz in combination with nelfinavir (20 - 30 mg/ kg given three times a day) and one or more NRTIs.
Initialdosis af efavirenz svarede til en dosis på 600 mg (justeret efter kalkuleret
The starting dose of efavirenz was the equivalent of a 600 mg dose (adjusted from calculated body size based on weight).
Responshyppigheden, der er baseret på NC = F analyse af den procentdel af patienter med plasma HIV- RNA < 400 koPI' er/ ml efter 48 uger var 60% (95%, C. I.
The response rate, based on the NC = F analysis of the percentage of patients with plasma HIV-RNA < 400 copies/ ml at 48 weeks was 60% (95%, C. I.
47, 72) og 53% (C. I.
47, 72), and 53% (C. I.
40, 66) baseret på procentdelen af patienter med plasma HIV- RNA < 50 koPI' er/ ml.
40, 66) based on percentage of patients with plasma HIV-RNA < 50 copies/ ml.
Middel CD4 celletallene øgedes med 63 ± 34, 5 celler/ mm3 fra baseline.
The mean CD4 cell counts were increased by 63 ± 34.5 cells/ mm3 from baseline.
5. 2 Farmakokinetiske egenskaber
22 5.2 Pharmacokinetic properties
De højeste efavirenz- plasmakoncentrationer på 1, 6 - 9, 1 μM blev nået senest 5 timer efter orale enkeltdoser på 100 – 1. 600 mg, der blev indgivet til ikke- inficerede frivillige.
Absorption: peak efavirenz plasma concentrations of 1.6 - 9.1 μ M were attained by 5 hours following single oral doses of 100 mg to 1,600 mg administered to uninfected volunteers.
Stigningerne var mindre end proportionale, hvilket tyder på formindsket absorption ved højere doser.
Dose related increases in Cmax and AUC were seen for doses up to 1,600 mg; the increases were less than proportional suggesting diminished absorption at higher doses.
Tiden indtil peak plasmakoncentrationerne (3 - 5 timer) ændredes ikke efter multiple doseringer, og steady- state plasmakoncentrationer blev nået på 6 - 7 dage.
Time to peak plasma concentrations (3 - 5 hours) did not change following multiple dosing and steady-state plasma concentrations were reached in 6 - 7 days.
For HIV- inficerede patienter i steady- state var middel- Cmax, middel- Cmin og middel- AUC lineære ved en daglig dosis på 200 mg, 400 mg og 600 mg.
In HIV infected patients at steady state, mean Cmax, mean Cmin, and mean AUC were linear with 200 mg, 400 mg, and 600 mg daily doses.
Hos 35 patienter, der fik efavirenz 600 mg 1 gang daglig var det gennemsnitlige steady- state Cmax 12, 9 ± 3, 7 μM (29%) [gennemsnit ± S. D.
In 35 patients receiving efavirenz 600 mg once daily, steady state Cmax was 12.9 ± 3.7 μ M (29%) [mean ± S. D.
(% C. V.)], steady- state Cmin 5, 6 ± 3. 2 μM (57%) og AUC 184 ± 73 μM⋅t (40%).
(% C. V.)], steady state Cmin was 5.6 ± 3.2 μ M (57%), and AUC was 184 ± 73 μ M·h (40%).
4. 4).
Effect of food: the bioavailability of a single 600 mg dose of efavirenz hard capsules in uninfected volunteers was increased 22% and 17%, respectively, when given with a meal of high fat or normal composition, relative to the bioavailability of a 600 mg dose given under fasted conditions (see section 4.4).
Efavirenz har en høj bindingsgrad (cirka 99, 5 - 99, 75%) til humane plasmaproteiner, fortrinsvis albumin.
Distribution: efavirenz is highly bound (approximately 99.5 - 99.75%) to human plasma proteins, predominantly albumin.
Hos HIV- 1- inficerede patienter (n = 9), som fik efavirenz 200 - 600 mg 1 gang dagligt i mindst 1 måned, lå koncentrationerne i cerebrospinalvæsken mellem 0, 26 til 1, 19% (gennemsnit 0, 69%) af den tilsvarende plasmakoncentration.
In HIV-1 infected patients (n = 9) who received efavirenz 200 to 600 mg once daily for at least one month, cerebrospinal fluid concentrations ranged from 0.26 to 1.19% (mean 0.69%) of the corresponding plasma concentration.
3 gange højere end den ikke- proteinbundne (frie) fraktion af efavirenz i plasma.
This proportion is approximately 3-fold higher than the non-protein-bound (free) fraction of efavirenz in plasma.
In vitro- undersøgelserne tyder på, at CYP3A4 og CYP2B6 er de isoenzymer, der hovedsageligt er ansvarlige for efavirenz- metaboliseringen, og at det hæmmede P450 isoenzymerne 2C9, 2C19 og 3A4.
The in vitro studies suggest that CYP3A4 and CYP2B6 are the major isozymes responsible for efavirenz metabolism and that it inhibited P450 isozymes 2C9, 2C19, and 3A4.
Efavirenz plasmaeksponering kan øges hos patienter med homozygot- G516T, der er en genetisk variant af CYP2B6- isoenzymet.
Efavirenz plasma exposure may be increased in patients with the homozygous G516T genetic variant of the CYP2B6 isoenzyme.
Det er påvist, at efavirenz inducerer P450- enzymer, hvilket medfører induktion af dets egen metabolisering.
Efavirenz has been shown to induce P450 enzymes, resulting in the induction of its own metabolism.
Hos ikke- inficerede frivillige resulterede multiple doser på 200 - 400 mg per dag i 10 dage i en lavere grad af akkumulation (22 – 42% lavere) end forudset samt kortere halveringstid sammenlignet med enkeltdosisadministration( se nedenfor).
In uninfected volunteers, multiple doses of 200 - 400 mg per day for 10 days resulted in a lower than predicted extent of accumulation (22 - 42% lower) and a shorter terminal half-life compared with single dose administration (see below).
Efavirenz har en forholdsvis lang halveringstid på mindst 52 timer efter enkeltdoser og 40 - 55 timer efter multiple doser.
Elimination: efavirenz has a relatively long terminal half-life of at least 52 hours after single doses and 40 – 55 hours after multiple doses.
14 – 34% af en isotopmærket dosis af efavirenz blev genfundet i urinen, og mindre end 1% af dosis blev udskilt i urinen som uomdannet efavirenz.
Approximately 14 - 34% of a radiolabelled dose of efavirenz was recovered in the urine and less than 1% of the dose was excreted in urine as unchanged efavirenz.
Hos den enkelte patient med svær leverinsufficiens (Child Pugh grad C), der blev undersøgt, blev halveringstiden fordoblet, hvilket indikerer et potentiale for en langt større grad af akkumulering.
In the single patient studied with severe hepatic impairment (Child Pugh Grade C), half life was doubled indicating a potential for a much greater degree of accumulation.
Hos 49 pædiatriske patienter, der fik en dosis ækvivalent med 600 mg efavirenz (dosis justeret ud fra beregnet legemsstørrelse på basis af vægt) var steady- state Cmax 14, 1 μM, steady- state Cmin 5, 6 μM og AUC 216 μM⋅t.
Paediatric pharmacokinetics: in 49 paediatric patients receiving the equivalent of a 600 mg dose of efavirenz (dose adjusted from calculated body size based on weight), steady state Cmax was 14.1 μ M, steady state Cmin was 5.6 μ M, and AUC was 216 μ M·h.
Farmakokinetik for efavirenz hos pædiatriske patienter var lig den hos voksne.
The pharmacokinetics of efavirenz in paediatric patients were similar to adults.
Køn, race, ældre:
23 Gender, race, elderly:
Der er set misdannelser hos 3 ud af 20 fostre/ nyfødte fra efavirenzbehandlede cynomolgusaber, der fik indgivet en dosis der resulterede i efavirenzkoncentrationer i plasma lig dem set hos mennesker.
Malformations were observed in 3 of 20 foetuses/ newborns from efavirenz-treated cynomolgus monkeys given doses resulting in plasma efavirenz concentrations similar to those seen in humans.