natgillin/translations-raw huggingface dataset:
Dog anses ætiologien for at være multifaktoriel (omfattende anvendelse af kortikosteroider, alkoholforbrug, svær immunosuppression, højere Body Mass Index (BMI)).
Although the aetiology is considered to be multifactorial (including corticosteroid use, alcohol consumption, severe immunosuppression, higher body mass index), cases of osteonecrosis have been reported particularly in patients with advanced HIV-disease and/or long-term exposure to combination antiretroviral therapy (CART).
Nedsat nyrefunktion Det er usandsynligt at nelfinavir vil fjernes signifikant ved hæmodialyse eller peritoneal dialyse, da nelfinavir i høj grad er bundet til plasmaproteiner.
Since nelfinavir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by haemodiaylisis or peritoneal dialysis.
Kombination med andre lægemidler:
Combination with other medicinal products:
4. 3, 4. 5 og 4. 8).
Caution is advised whenever VIRACEPT is co- administered with medicinal products which are inducers or inhibitors and/or substrates of CYP3A4; such combinations may require dose adjustment (see also sections 4.3, 4.5 and 4.8).
Derfor anbefales samtidig indtagelse af VIRACEPT og simvastatin eller lovastatin ikke, på grund af en forøget risiko for myopati inklusiv rhabdomyolyse.
The HMG (hydroxyl-3-methyl-glutaryl)-CoA reductase inhibitors simvastatin and lovastatin are highly dependent on CYP3A4 for metabolism, thus concomitant use of VIRACEPT with simvastatin or lovastatin is not recommended due to an increased risk of myopathy including rhabdomyolysis.
Der skal også udvises forsigtighed hvis VIRACEPT indtages samtidig med atorvastatin, som i mindre grad metaboliseres af CYP3A4.
Caution must also be exercised if VIRACEPT is used concurrently with atorvastatin, which is metabolised to a lesser extent by CYP3A4.
Potente induktorer af CYP3A (f. eks. phenobarbital og carbamazepin) kan nedsætte plasmakoncentrationerne af nelfinavir.
Potent inducers of CYP3A (e.g., phenobarbital and carbamazepine) may reduce nelfinavir plasma concentrations.
Absorption af nelfinavir kan blive reduceret i situationer, hvor den gastriske pH øges uanset årsagen hertil.
The absorption of nelfinavir may be reduced in situations where the gastric pH is increased irrespective of cause.
4. 5).
Co-administration of the combination oral contraceptive containing norethindrone and 17 α-ethinylestradiol with VIRACEPT resulted in a decrease in AUC of the contraceptive drug; therefore alternative contraceptive measure should also be considered (see section 4.5).
Hos nogle af disse patienter var hyperglykæmien af svær grad og i nogle tilfælde var hyperglykæmien associeret med ketoacidose.
In some of these the hyperglycaemia was severe and in some cases also associated with ketoacidosis.
21 Patienter med hæmofili:
21 Patients with haemophilia:
For patienter med hæmofili type A og B, som er under behandling med proteasehæmmere er der rapporteret øget blødning, herunder spontane hudblødninger og ledblødninger.
There have been reports of increased bleeding, including spontaneous skin haematomas and haemarthroses, in haemophiliac patients type A and B treated with PIs.
For interaktioner med nelfinavir og udvalgte lægemidler, se tabel 1 og tabel 2; tabel 1: for det co - administrerede lægemiddels indvirkning på farmakokinetiken og tabel 2: for andre lægemidlers indvirkning på nelfinavirs farmakokinetik.
Please refer to Table 1 and Table 2 for interactions of nelfinavir with selected compounds, Table 1 for impact on the pharmacokinetics of the co-administered compound, Table 2 for the impact of other drugs on pharmacokinetics of nelfinavir.
4. 3 og nedenfor): terfenadin, astemizol, cisaprid, amiodaron, kinidin, ergotaminderivater, pimozid, oral midazolam og triazolam
Co-administration with the following medicinal products that are substrates for CYP3A4 and which have narrow therapeutic windows is contraindicated (see section 4.3 and below): terfenadine, astemizole, cisapride, amiodarone, quinidine, ergot derivatives, pimozide, oral midazolam and triazolam.
Nukleosidanaloge reverse transkriptase hæmmere (NRTIs) Der er ikke observeret klinisk signifikante interaktioner mellem nelfinavir og nukleosidanaloger (specielt zidovudin plus lamivudin, stavudin og stavudin plus didanosin).
Clinically significant interactions have not been observed between nelfinavir and nucleoside analogues (specifically zidovudine plus lamivudine, stavudine, and stavudine plus didanosine).
Andre proteasehæmmere( PI)
Other Protease Inhibitors (PIs):
Se tabel 1 og tabel 2 for yderligere information.
See Tables 1 and 2 for more information.
22 Non- nukleosidanaloge reverse transcriptasehæmmere (NNRTI)
22 Non-nucleoside Analogue Reverse Transcriptase Inhibitors (NNRTIs):
Sikkerheden af denne kombination er ikke dokumenteret, og kombinationen anbefales ikke.
The safety of this drug combination has not been established and this combination is not recommended.
Andre potente CYP3A fremmere (f. eks. phenobarbital, carbamazepin) kan også reducere nelfinavirs plasmakoncentrationer.
Other potent inducers of CYP3A (e.g., phenobarbital, carbamazepine) may also reduce nelfinavir plasma concentrations.
Det er nødvendigt at nedsætte doseringen af rifabutin til 150 mg en gang daglig, når det ingives sammen med nelfinavir 750 mg tre gange daglig eller 1250 mg to gange daglig.
Dosage reduction of rifabutin to 150 mg once a day is necessary when nelfinavir 750 mg TID or 1250 mg BID and rifabutin are co-administered.
Prikbladet perikum (Hypericum perforatum):
John’s wort (Hypericum perforatum):
Hvis patienten allerede tager prikbladet perikum, skal brug af prikbladet perikum ophøre og virusmængden og, om muligt, nelfinavirniveauet kontrolleres.
Nelfinavir levels may increase on stopping St.
Nelfinavirniveauet kan stige ved ophør med prikbladet perikum og det kan blive nødvendigt at justere VIRACEPT dosis.
The inducing effect of St.
4. 3).
John’s wort may persist for at least 2 weeks after cessation of treatment (see section 4.3).
Baseret på de metaboliske profiler forventes der ingen kliniske relevante interaktioner med andre specifikke hæmmere af CYP3A (f. eks. fluconazol, itraconazol, claritromycin og erytromycin); muligheden kan dog ikke udelukkes.
Based on the metabolic profiles, a clinically relevant drug interaction would not be expected with other specific inhibitors of CYP3A (e.g., fluconazole, itraconazole, clarithromycin, erythromycin); however, the possibility cannot be excluded.
5. 2).
Co-administration of nelfinavir with inhibitors of CYP2C19 (e.g., fluconazole, fluoxetine, paroxetine, lansoprazole, imipramine, amitriptyline and diazepam) may be expected to reduce the conversion of nelfinavir to its major active metabolite M8 (tert-butyl hydroxy nelfinavir) with a concomitant increase in plasma nelfinavir levels (see section 5.2).
4. 3).
23 The absorption of nelfinavir may be reduced in conditions where gastric pH is increased, therefore concomitant use of VIRACEPT with Proton Pump Inhibitors is not recommended (see section 4.4), except for omeprazole which is contra-indicated (see section 4.3).
HMG- CoA- reduktasehæmmere som i høj grad er afhængige af CYP3A4 metabolisme, såsom lovastatin og simvastatin, forventes at øge plasmakoncentrationen væsentligt, når disse stoffer indtages sammen med VIRACEPT.
HMG-CoA reductase inhibitors which are highly dependent on CYP3A4 metabolism, such as lovastatin and simvastatin, are expected to have markedly increased plasma concentrations when co-administered with VIRACEPT.
Kombinationer af disse produkter og VIRACEPT anbefales ikke, da forhøjede koncentrationer af HMG- CoA reduktasehæmmere kan forårsage myopati inklusiv rhabdomyolyse.
Since increased concentrations of HMG-CoA reductase inhibitors may cause myopathy, including rhabdomyolysis, the combination of these medicinal products with VIRACEPT is not recommended.
Metabolisering af atorvastatin er mindre afhængig af CYP3A4.
Atorvastatin is less dependent on CYP3A4 for metabolism.
Metabolisering af pravastatin og fluvastatin er ikke afhængig af CYP3A4 og interaktioner forventes ikke med proteasehæmmere.
The metabolism of pravastatin and fluvastatin is not dependent on CYP3A4, and interactions are not expected with PIs.
For hiv- negative patienter i vedligeholdelsesbehandling med methadon resulterede samtidig indtagelse af nelfinavir 1250 mg to gange daglig og methadon 80 + / - 21 mg en gang daglig i et fald på 47% i metadon AUC.
Co-administration of nelfinavir 1250 mg BID with methadone 80 +/- 21 mg once a day in HIV negative methadone maintenance patients resulted in a 47% decrease in methadone AUC.
Dog kan det på grund af farmakokinetiske ændringer imidlertid forventes, at nogle patienter, som får denne kombination, udvikler abstinenssymptomer og behøver en højere methadondosis.
None of the subjects experienced withdrawal symptoms in this study; however, due to the pharmacokinetic changes, it should be expected that some patients who received this drug combination may experience withdrawal symptoms and require an upward adjustment of the methadone dose.
Da nelfinavir øger terfenadins plasmakoncentration, må VIRACEPT ikke indgives samtidigt med terfenadin på grund af muligheden for alvorlige og/ eller livstruende hjerte arrytmier.
Nelfinavir increases terfenadine plasma concentrations; therefore, VIRACEPT must not be administered concurrently with terfenadine because of the potential for serious and/or life-threatening cardiac arrhythmias.
Da lignende interaktioner er sandsynlige for astemizol og cisaprid, må VIRACEPT ikke indgives samtidigt med disse lægemidler.
Because similar interactions are likely with astemizole and cisapride, VIRACEPT must not be administered concurrently with these drugs.
Hvis VIRACEPT administreres samtidig med parenteral midazolam, skal det gøres på en intensivafdeling eller tilsvarende, som sikrer tæt klinisk monitorering og fornøden lægebehandling i tilfælde af respirationsdepression og/ eller forlænget sedation.
If VIRACEPT is co-administered with parenteral midazolam, it should be done in an intensive care unit (ICU) or similar setting which ensures close clinical monitoring and appropriate medical management in case of respiratory depression and/or prolonged sedation.
Patienter bør derfor monitoreres med henblik på toksiske reaktioner forbundet med sådanne lægemidler.
For other compounds that are substrates for CYP3A (e.g., calcium channel blockers including bepridil, immunosuppressants including tacrolimus and ciclosporin, and sildenafil) plasma concentrations may be elevated when co-administered with VIRACEPT; therefore, patients should be monitored for toxicities associated with such medicinal products.
7 dages indgift af nelfinavir 750 mg tre gange daglig og et oralt kombinationskontraceptiv, som indeholdt 0, 4 mg norethindron og 35 μg 17 α- ethinyløstradiol, medførte en reduktion af ethinyløstradiol- plasma AUC på 47% og en reduktion af norethindron - plasma AUC på 18%.
Oral contraceptives: administration of nelfinavir 750 mg TID and a combination oral contraceptive which included 0.4 mg of norethindrone and 35 μg of 17 α-ethinylestradiol for 7 days resulted in a 47% decrease in ethinylestradiol and an 18% decrease in norethindrone plasma AUC.
24 Tabel 1:
24 Table 1:
Lægemiddel interaktioner: ændringer i farmakokinetiske parametre for lægemidler co - administrerede i tilstedeværelse af nelfinavir Co- administerede Nelfinavir dosis lægemidler, dosis
Changes in Pharmacokinetic Parameters for Co-administered Drug in the Presence of Nelfinavir Co-administered Drug, Dose
Kommentar Andre Proteasehæmmere (PIs) Ritonavir 500 mg enkeltdosis
Comment Other Protease Inhibitors (PIs) Ritonavir 500 mg 750 mg TID single dose X 6 doses
750 mg 3 gange daglig i 7 dage
↑
Sikkerheden af kombinationen af indinavir + nelfinavir er ikke fastslået
trough at 8 The safety of hrs combination ↑ 500% indinavir + nelfinavir has not been established.
Der behøves ingen dosisjustering for nogen af lægemidlerne
No dosage adjustment needed for
Non- nukleosidanaloge reverse transcriptasehæmmere (NNRTI) Efavirenz 600 mg en gang daglig
either product Non-nucleoside Analogue Reverse Transcriptase Inhibitors (NNRTIs) Efavirenz 600 mg 750 mg TID QD
gange daglig eller 1250 mg 2 gange daglig og rifabutin er co- administreret.
1250 mg BID and rifabutin are co- administered.
HMG- CoA reduktatsehæmmere Simvastatin 20 mg 1250 en gang daglig
Simvastatin 20 mg 1250 mg BID QD∞
Atorvastatin 10 mg en gang daglig
Atorvastatin 1250 mg BID 10 mt QD∞
Pravastatin eller fluvastatin anbefales, hvis behandling med HMG- CoA reductasehæmmere er indiceret i kombination med nelfinavir
If treatment with HMG-CoA reductase inhibitors is indicated in combination with nelfinavir, pravastatin or fluvastatin is recommended.
Tabel 2:
25 Table 2:
Ritonavir 500 mg BID X 3 doser
Other Protease Inhibitor (PIs) Ritonavir
Enkelt dosis 750 mg
Single dose
25 Co- administerede lægemidler, dosis
Ritonavir 100 or 1250 mg BID 200 mg BID (morning
Nelfinavir dosis
↑ 20%
Ændring i farmakokinetiske parametre for nelfinavir
AUC of M8 metabolite* ↑ 74%
Ritonavir 100 or 200 mg BID
administration)
1250 mg 2 gange daglig (morgen administration)
See Sec.
1250 mg 2 gange daglig (aften administration)
↑ 39%
↑ 39% AUC af M8 metabolit * ↑ 86% Se pkt.
AUC of M8 metabolite* ↑ 86%
↑ 83% Elimination halveringstid ↑ 22% Sikkerheden af denne kombination er ikke fastslået
↑ 83%
Saquinavir 1200 mg 3 gange daglig
Saquinavir 1200 mg TID
↔ Der behøves ingen dosisjustering for nogen af lægemidlerne
No dosage adjustment needed for either product
For at undgå overførelse af hiv anbefales det at hiv- smittede kvinder ikke under nogen omstændigheder ammer deres spædbørn.
It is recommended that HIV-infected women must not breast-feed their infants under any circumstances in order to avoid transmission of HIV.
VIRACEPT påvirker ikke eller i ubetydelig grad evnen til at føre motorkøretøj eller betjene maskiner.
Mothers must be instructed to discontinue breast-feeding if they are receiving VIRACEPT.
26 4. 8 Bivirkninger
26 4.7 Effects on ability to drive and use machines
De uønskede virkninger præsenteret i rækkefølge efter faldende alvorlighed indenfor hver frekvensgruppering.
Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
27 Vaskulære sygdomme:
27 Metabolism and nutrition disorders:
Sjælden (≥ 0, 01% - ≤ 0, 1%): oppustet mave Ikke almindelig (≥ 0, 1% - ≤ 1%): opkastning; pancreatitis/ forhøjet blodamylase.
Rare (≥ 0.01% - ≤ 0.1%): abdominal distension, Uncommon (≥ 0.1% - ≤ 1%): vomiting, pancreatitis/blood amylase increased.
Sjælden (≥ 0, 01% - ≤ 0, 1%): hepatitis, abnorme leverenzymer og ikterus, når nelfinavir er anvendt i kombination med andre antiretrovirale stoffer.
Rare (≥ 0.01% - ≤ 0.1%): hepatitis, abnormal liver enzymes and jaundice when nelfinavir is used in combination with other antiretroviral agents.
Meget sjælden (≤ 0, 01%), herunder enkeltstående indberetninger: erythema multiforme
Erythema multiforme.
Antiretroviral kombinationsbehandling er blevet associeret med metaboliske abnormaliteter så som hypertriglyceridæmi, hyperkolesterolæmi, insulinresistens, hyperglykæmi og hyperlaktæmi (se pkt.
Combination antiretroviral therapy has been associated with metabolic abnormalities such as hypertriglyceridaemia, hypercholesterolaemia, insulin resistance, hyperglycaemia and hyperlactaemia.
Hos hiv- inficerede patienter med svær immuninsufficiens kan der ved påbegyndelse af antiretroviral kombinationsbehandling (CART) opstå en inflammatorisk reaktion på asymptomatiske eller residuale opportunistiske infektioner (se pkt.
In HIV-infected patients with severe immune deficiency at the time of initiation of combination antiretroviral therapy (CART), an inflammatory reaction to asymptomatic or residual opportunistic infections may arise.
Farmakoterapeutisk klassifikation: direkte virkende antivirale lægemidler, ATC kode:
Pharmacotherapeutic group: direct acting antivirals, ATC code:
J05 A E04
J05AE04
Nelfinavir bindes reversibelt til
The cleavage of these viral polyproteins is essential for the maturation of infectious virus.
28 den aktive del af hiv protease og forebygger spaltning af polyproteiner, hvilket medfører dannelsen af umodne, ikke- smittende viruspartikler.
Nelfinavir reversibly binds to the active site of HIV protease and prevents cleavage of the polyproteins resulting in the formation of immature non-infectious viral particles.
I de kliniske studier blev isolater fra udvalgte patienter, som var behandlet med nelfinavir alene eller i kombination med reverse transcriptasehæmmere, monitoreret i 2 til 82 uger for fænotypiske (n=19) og genotypiske forandringer (n=195, heraf kunne 157 vurderes).
HIV isolates from selected patients treated with nelfinavir alone or in combination with reverse transcriptase inhibitors were monitored for phenotypic (n=19) and genotypic (n=195, 157 of which were assessable) changes in clinical trials over a period of 2 to 82 weeks.
Der blev opdaget en eller flere virale proteasemutationer ved aminosyrepositionerne 30, 35, 36, 46, 71, 77 og 88 hos > 10% af patienterne med vurderbare isolater.
One or more viral protease mutations at amino acid positions 30, 35, 36, 46, 71, 77 and 88 were detected in > 10% of patients with assessable isolates.
Det er dokumenteret, at behandling med nelfinavir alene eller I kombination med andre antiretrovirus midler nedsætter virusbelastningen og øger CD4- celletællingen hos hiv- 1 seropositive patienter.
Clinical pharmacodynamic data: treatment with nelfinavir alone or in combination with other antiretroviral agents has been documented to reduce viral load and increase CD4 cell counts in HIV-1 seropositive patients.
Fald i hiv RNA observeret ved nelfinavir monoterapi var mindre udpræget og af kortere varighed.
Decreases in HIV RNA observed with nelfinavir monotherapy were less pronounced and of shorter duration.
Nelfinavirs virkning (alene eller kombineret med andre antiretrovirale midler) på biologiske markører, CD4- celletal og virus RNA blev evalueret I adskillige undersøgelser af hiv- 1 smittede patienter.
The effects of nelfinavir (alone or combined with other antiretroviral agents) on biological markers of disease activity, CD4 cell count and viral RNA, were evaluated in several studies involving HIV-1 infected patients.
Effekten af BID- regimet er evalueret overfor TID- regimet med VIRACEPT 250 mg tabletter, hovedsageligt hos PI- naive patienter.
29 The efficacy of the BID regimen has been evaluated versus the TID regimen with VIRACEPT 250 mg tablets primarily in patients naïve to PIs.
29 Antal patienter med hiv RNA under LOQ (sensitive og ultrasensitive assays) ved uge 48 Assay
Proportion of patients with HIV RNA below LOQ (sensitive and ultrasensitive assays) at Week 48 Assay
Analysis Observerede data
Analysis Observed data
Små, ikke statistisk signifikante forskelle observeredes for andre farmakokinetiske parametre uden tendens til at favorisere det ene regi fremfor det andet.
Small, non-statistically significant differences were observed in other pharmacokinetic parameters with no trend favouring one regimen over the other.
I et studie af 297 hiv- 1 seropositive patienter som fik zidovudin og lamivudin sammen med nelfinavir (i to forskellige doser) eller zidovudin eller lamivudin alene, var gennemsnits baseline CD4 celletallet 288 celler/ mm³ og gennemsnits plasma baseline var hiv RNA 5, 21 log10 kopier/ ml (160. 394 kopier/ ml).
In a study of 297 HIV-1 seropositive patients receiving zidovudine and lamivudine plus nelfinavir (2 different doses) or zidovudine and lamivudine alone, the mean baseline CD4 cell count was 288 cells/mm3 and the mean baseline plasma HIV RNA was 5.21 log10 copies/ml (160,394 copies/ml).
Middel- CD4- celletallet efter 24 uger steg med hhv. 150 og 95 celler/ mm3i gruppen, der fik 750 mg nelfinavir tre gange daglig sammen med zidovudin og lamivudin sammenlignet med gruppen, der fik zidovudin og lamivudin.
Mean CD4 cell counts at 24 weeks were increased by 150 and 95 cells/mm3 for the groups treated with nelfinavir 750 mg TID plus zidovudine and lamivudine or zidovudine and lamivudine, respectively.
Det mediane baseline CD4+ celletal var 232 celler/ mm3 i begge grupper.
Median baseline CD4+ cell count was 232 cells/mm3
Den gennemsnitlige stigning fra baseline i CD4+ celletallet efter 48 uger var henholdsvis 195 celler/ mm3 og 207 celler/ mm3 i nelfinavir - og lopinavir/ ritonavirgrupperne.
The mean increase from baseline in CD4+ cell count at week 48 was 195 cells/mm3 and 207 cells/mm3 in the nelfinavir and lopinavir/ritonavir groups respectively.
Efter 48 ugers 30 behandling havde en statistisk signifikant større del af patienterne i lopinavir/ ritonavir armen < 50 kopier/ ml hiv- 1 RNA sammenlignet med nelfinavir armen.
Through 48 weeks of therapy, a statistically significantly higher proportion of patients in the lopinavir/ritonavir arm had HIV-1 RN A< 50 copies/ml compared to the nelfinavir arm.
Et farmakokinetisk studie hos hiv- positive patienter sammenlignede 1250 mg (5 tabletter á 250 mg) to gange daglig med 750 mg (3 tabletter á 250 mg) tre gange daglig, begge i 28 dage.
A pharmacokinetic study in HIV-positive patients compared multiple doses of 1250 mg twice daily (BID) with multiple doses of 750 mg three times daily (TID) for 28 days.
2, 2 ± 1, 3 μg/ ml og 0, 7 ± 0, 4 μg/ ml.
Patients receiving VIRACEPT BID (n=10) achieved nelfinavir Cmax of 4.0 ± 0.8 µg/ml and morning and evening trough concentrations of 2.2 ± 1.3 µg/ml and 0.7 ± 0.4 µg/ml, respectively.
De øgede plasmakoncentrationer i forbindelse med føde var uafhængige af måltidernes fedtindhold.
The increased plasma concentrations with food were independent of fat content of the
31 anvendt 250 mg filmovertrukne tabletter.
The effect of meal content on nelfinavir exposure was investigated in a study using the 250 mg film-coated tablets formulation.
Steady state nelfinavir AUC og Cmax var henholdsvis 15% og 20% højere, når dosis blev indtaget efter et måltid bestående af 800 kcal/ 50% fedt, i forhold til indtagelse af dosis efter et let måltid (350 kcal/ 33% fedt), hvilket antyder at måltidets fedtindhold har mindre betydning for tilgængeligheden af nelfinavir ved multipel dosering end det ville antages på baggrund af data fra enkeltdosisstudier.
Steady state nelfinavir AUC and Cmax were respectively 15% and 20% higher when doses followed a 800 kcal/50% fat meal compared to those following a light meal (350 kcal/33% fat), suggesting that meal content has less effect on nelfinavir exposures during multiple dosing than would be anticipated based on data from single dose studies.
Skønt der ikke er udført undersøgelser på mennesker viste undersøgelser med en enkelt 50 mg/ kg dosis 14C – nelfinavir på rotter, at koncentrationerne i hjernen var mindre end i andre væv, men oversteg in vitro EC95 for antiviral aktivitet.
Although no studies have been conducted in humans, studies with a single 50 mg/kg dose of 14C-nelfinavir in rats showed that concentrations in the brain were lower than in other tissues, but exceeded the in vitro EC95 for antiviral activity.
Uomdannet nelfinavir fandtes at være på 82- 86% af den totale plasma- radioaktivitet efter en enkel oral 750 mg dosis 14C – nelfinavir.
Metabolism: unchanged nelfinavir comprised 82-86% of the total plasma radioactivity after a single oral 750 mg dose of 14C-nelfinavir.
In- vitro er de forskellige isoformer af cytochrome P- 450, inklusive CYP3A, CYP2C19/ C9 og CYP2D6 ansvarlige for metaboliseringen af nelfinavir.
In vitro, multiple cytochrome P-450 isoforms including CYP3A, CYP2C19/C9 and CYP2D6 are responsible for metabolism of nelfinavir.
Hovedmetabolitten, M8 (tert- butyl hydroxynelfinavir), har in vitro antiviral aktivitet, som er lig moderstoffet, og dets dannelse er katalyseret af det polymorfe cytochrom CYP2C19.
The major oxidative metabolite, M8 (tert-butyl hydroxy nelfinavir), has in vitro antiviral activity equal to the parent drug and its formation is catalysed by the polymorphic cytochrome CYP2C19.