natgillin/translations-raw huggingface dataset:
Baseret på in vitro - og in vivo- undersøgelser elimineres raltegravir hovedsageligt ved metabolisme via UGT1A1- medieret glucuronidering.
Based on in vitro and in vivo studies, raltegravir is eliminated mainly by metabolism via a UGT1A1-mediated glucuronidation pathway.
Der er observeret betydelig inter - og intra- individuel variabilitet i raltegravirs farmakokinetik.
Considerable inter- and intra-individual variability was observed in the pharmacokinetics of raltegravir.
Raltegravirs virkning på andre lægemidlers farmakokinetik Raltegravir havde i interaktionsundersøgelser ingen klinisk relevant virkning på farmakokinetikken af tenofovir, hormonel antikonception og midazolam.
Effect of raltegravir on the pharmacokinetics of other medicinal products In interaction studies, raltegravir did not have a clinically meaningful effect on the pharmacokinetics of tenofovir, hormonal contraceptives, or midazolam.
Andre lægemidlers virkning på raltegravirs farmakokinetik Forudsat at raltegravir er metaboliseret primært via UGT1A1, bør der udvises forsigtighed, når ISENTRESS administreres sammen med potente inducere af UGT1A1 (f. eks. rifampicin).
Effect of other agents on the pharmacokinetics of raltegravir Given that raltegravir is metabolised primarily via UGT1A1, caution should be used when co-administering ISENTRESS with strong inducers of UGT1A1 (e. g., rifampicin).
4. 4).
However, if co-administration with rifampicin is unavoidable, a doubling of the dose of ISENTRESS can be considered (see section 4.4).
Mindre potente inducere (f. eks. efavirenz, neviparin, rifabutin, glukokortikoider, perikon, pioglitazon) kan anvendes sammen med den anbefalede dosis af ISENTRESS.
John's wort, pioglitazone) may be used with the recommended dose of ISENTRESS.
Administration af ISENTRESS sammen med lægemidler, der er kendt som potente UGT1A1 - hæmmere (f. eks. atazanavir), kan øge raltegravirs plasmakoncentrationer.
Co-administration of ISENTRESS with medicinal products that are known to be potent UGT1A1 inhibitors (e. g., atazanavir) may increase plasma levels of raltegravir.
Mindre potente UGT1A1 - hæmmere (f. eks. indinavir, saquinavir) kan også øge raltegravirs plasmakoncentration, men i mindre grad end atazanavir.
Less potent UGT1A1 inhibitors (e. g., indinavir, saquinavir) may also increase plasma levels of raltegravir, but to a lesser extent compared with atazanavir.
En stor del af patienterne i de kliniske undersøgelser fik atazanavir og/ eller tenofovir, og begge lægemidler medførte stigning i raltegravirs plasmakoncentrationer i de optimerede baggrundsregimer.
From the clinical trials, a large proportion of patients used atazanavir and / or tenofovir, both agents that result in increases in raltegravir plasma levels, in the optimised background regimens.
Den sikkerhedsprofil, der blev observeret
The safety profile observed in patients who used
4 hos patienter, som fik atazanavir og/ eller tenofovir, var sædvanligvis den samme som sikkerhedsprofilen hos patienter, der ikke fik disse lægemidler.
4 atazanavir and / or tenofovir was generally similar to the safety profile of patients who did not use these agents.
Samtidig administration af ISENTRESS med omeprazol hos raske forsøgspersoner øger raltegravirs plasmakoncentrationer.
In healthy subjects, co-administration of ISENTRESS with omeprazole increases raltegravir plasma levels.
Da det er uvist om forhøjet gastrisk pH påvirker absorptionen af raltegravir hos HIV- inficerede patienter, bør ISENTRESS kun bruges sammen med lægemidler, der øger gastrisk pH (f. eks. protonpumpehæmmere og H2- antagonister), hvis det er uundgåeligt.
As the effects of increasing gastric pH on the absorption of raltegravir in HIV-infected patients are uncertain, use ISENTRESS with medicinal products that increase gastric pH (e. g., proton pump inhibitors and H2 antagonists) only if unavoidable.
Lægemidler i henhold til terapeutisk område
Medicinal products by therapeutic area ANTI-RETROVIRAL Protease inhibitors (PI)
atazanavir / ritonavir (raltegravir 400 mg BID)
atazanavir / ritonavir (raltegravir 400 mg BID)
raltegravir raltegravir raltegravir
raltegravir AUC ↑ 41% raltegravir C12hr ↑ 77% raltegravir Cmax ↑ 24%
Dosisjustering er ikke nødvendig for ISENTRESS.
No dose adjustment required for ISENTRESS.
(UGT1A1- hæmning)
(UGT1A1 inhibition)
tipranavir / ritonavir (raltegravir 400 mg BID)
tipranavir / ritonavir (raltegravir 400 mg BID)
raltegravir AUC ↓24% raltegravir C12t ↓55% raltegravir Cmax ↓18%
raltegravir AUC ↓ 24% raltegravir C12hr ↓ 55% raltegravir Cmax ↓ 18%
(UGT1A1- induktion) Non- nukleoside reverse transkriptasehæmmere (NNRTIer)
(UGT1A1 induction) Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
efavirenz (raltegravir 400 mg SD)
efavirenz (raltegravir 400 mg SD)
raltegravir AUC ↓36% raltegravir C12t ↓21% raltegravir Cmax ↓36%
raltegravir AUC ↓ 36% raltegravir C12hr ↓ 21% raltegravir Cmax ↓ 36%
Dosisjustering er ikke nødvendig for ISENTRESS.
No dose adjustment required for ISENTRESS
(UGT1A1- induktion)
(UGT1A1 induction)
Nukleoside/ tide reverse transkriptasehæmmere
Nucleoside/ tide reverse transcriptase inhibitors
tenofovir (raltegravir 400 mg BID)
tenofovir (raltegravir 400 mg BID)
raltegravir AUC ↑49% raltegravir C12t ↑3% raltegravir Cmax ↑64% (interaktionsmekanisme ukendt)
raltegravir AUC ↑ 49% raltegravir C12hr ↑ 3% raltegravir Cmax ↑ 64%
Dosisjustering er ikke nødvendig for ISENTRESS eller tenofovirdisoproxilfumarat.
No dose adjustment required for ISENTRESS or tenofovir disoproxil fumarate.
tenofovir AUC ↓10% tenofovir C12t ↓13% tenofovir Cmax ↓23% ANTIMIKROBIELLE LÆGEMIDLER Svampemidler
tenofovir AUC ↓ 10% tenofovir C12hr ↓ 13% tenofovir Cmax ↓ 23% ANTIMICROBIALS Antimycobacterial
rifampicin (raltegravir 400 mg SD)
rifampicin (raltegravir 400 mg SD)
raltegravir AUC ↓40% raltegravir C12t ↓61% raltegravir Cmax ↓38%
raltegravir AUC ↓ 40% raltegravir C12hr ↓ 61% raltegravir Cmax ↓ 38%
Rifampicin reducerer ISENTRESS 'plasmakoncentrationer.
Rifampicin reduces plasma levels of ISENTRESS.
4. 4).
doubling of the dose of ISENTRESS can be considered (see section 4.4).
5 Lægemidler i henhold til terapeutisk område
5 Medicinal products by therapeutic area SEDATIVE
(raltegravir 400 mg BID)
midazolam (raltegravir 400 mg BID)
MAVESÅRSMEDICIN
These results indicate that raltegravir is not an inducer or inhibitor of CYP3A4, and raltegravir is thus not anticipated to affect the pharmacokinetics of medicinal products which are CYP3A4 substrates.
omeprazol (raltegravir 400 mg SD)
omeprazole (raltegravir 400 mg SD)
raltegravir AUC ↑ 212% raltegravir C12t ↑ 46% raltegravir Cmax ↑ 315%
raltegravir AUC ↑ 212% raltegravir C12 hr ↑ 46% raltegravir Cmax ↑ 315%
Samtidig administration af protonpumpehæmmere eller anden mavesårsmedicin kan øge raltegravirs plasma - koncentrationer.
Co-administration of proton pump inhibitors or other antiulcer medicinal products may increase plasma levels of raltegravir.
Brug ikke ISENTRESS med et lægemiddel, der øger gastrisk pH, medmindre det er uundgåeligt.
Do not use ISENTRESS with medicinal products that increase gastric pH unless this is unavoidable.
HORMONEL ANTIKONCEPTION Ethinylestradiol Norelgestromin (raltegravir 400 mg BID)
HORMONAL CONTRACEPTIVES Ethinyl Estradiol Norelgestromin (raltegravir 400 mg BID)
Ethinylestradiol AUC ↓ 2% Ethinylestradiol Cmax ↑ 1% Norelgestromin AUC ↑ 14% Norelgestromin Cmax ↑ 29%
Ehinyl Estradiol AUC ↓ 2% Ehinyl Estradiol Cmax ↑ 1% Norelgestromin AUC ↑ 14% Norelgestromin Cmax ↑ 29%
Dosisjustering er ikke nødvendig for ISENTRESS eller hormonelle antikonceptionsmidler (østrogen - og/ eller progesteronbaserede).
No dosage adjustment required for ISENTRESS or hormonal contraceptives (estrogen- and/ or progesterone-based)
Graviditet Der er ikke tilstrækkelig dokumentation for anvendelse af raltegravir til gravide.
Pregnancy There are no adequate data from the use of raltegravir in pregnant women.
Antiretroviralt graviditetsregister Der er oprettet et antiretroviralt graviditetsregister med henblik på monitorering af maternelle/ føtale resultater fra patienter, der uforvarende har fået ISENTRESS under graviditeten.
Anti-retroviral Pregnancy Registry To monitor maternal-foetal outcomes in patients inadvertently administered ISENTRESS while pregnant, an Anti-retroviral Pregnancy Registry has been established.
Amning Det vides ikke, om raltegravir udskilles i modermælk.
Lactation It is not known whether raltegravir is secreted in human milk.
3 gange højere end i maternelt plasma.
In rats, at a maternal dose of 600 mg/ kg/ day, mean active substance concentrations in milk were approximately 3-fold greater than in maternal plasma.
Desuden anbefales det, at HIV- inficerede mødre ikke ammer deres spædbørn for at undgå risikoen for postnatal overførsel af HIV.
In addition, it is recommended that HIV-infected mothers should not breastfeed their infants to avoid risking postnatal transmission of HIV.
Der er ikke foretaget undersøgelser af ISENTRESS 'virkning på evnen til at føre motorkøretøj eller betjene maskiner.
No studies have been performed on the effects of ISENTRESS on the ability to drive and use machines.
4. 8).
However, dizziness has been reported in some patients during treatment with regimens containing ISENTRESS, which may influence some patients' ability to drive and use machines (see section 4.8).
6 4. 8 Bivirkninger
6 4.8 Undesirable effects
Behandlingserfaring Sikkerhedsvurderingen af ISENTRESS til behandlingserfarne patienter er baseret på poolede sikkerhedsdata fra tre randomiserede undersøgelser.
Treatment-experienced The safety assessment of ISENTRESS in treatment-experienced patients is based on the pooled safety data from three randomised clinical studies.
I disse undersøgelser blev den anbefalede dosis på 400 mg to gange dagligt anvendt i kombination med optimeret baggrundsterapi (OBT) hos 507 patienter sammenlignet med 282 patienter, der fik placebo i kombination med OBT.
These studies used the recommended dose of 400 mg twice daily in combination with optimised background therapy (OBT) in 507 patients, in comparison to 282 patients taking placebo in combination with OBT.
Under dobbeltblind behandling var den samlede opfølgning på 504, 1 patientår for gruppen, der fik ISENTRESS 400 mg to gange dagligt, og 202, 5 patientår for placebogruppen.
During double-blind treatment, the total follow-up was 504.1 patient-years in the ISENTRESS 400 mg b. i. d. group and 202.5 patient-years in the placebo group.
Diarré hos henholdsvis 17, 6% og 20, 6%, kvalme hos 11, 2% og 15, 2%, hovedpine hos 10, 1% og 12, 4%, pyreksi hos 6, 3% og 11, 0% af patienterne.
For patients in the ISENTRESS 400 mg twice daily + OBT arm and the comparator placebo + OBT arm, the most commonly reported adverse reactions (> 10% in either group), of all intensities and regardless of causality were: diarrhoea in 17.6% and 20.6%, nausea in 11.2% and 15.2%, headache in 10.1% and 12.4%, pyrexia in 6.3% and 11.0% of patients, respectively.
I denne poolede analyse var hyppigheden for afbrydelse af behandling på grund af bivirkninger 2, 4% hos patienter, der fik ISENTRESS + OBT og 2, 8% hos patienter, der fik placebo + OBT.
In this pooled analysis, the rates of discontinuation of therapy due to adverse reactions were 2.4% in patients receiving ISENTRESS + OBT and 2.8% in patients receiving placebo + OBT.
De kliniske bivirkninger, som investigatorerne anså for at være relateret til ISENTRESS (alene eller i kombination med OBT) er nævnt nedenfor i henhold til Systemorganklasse.
Adverse reactions considered by investigators to be causally related to ISENTRESS (alone or in combination with OBT) are listed below by System Organ Class.
Alle termer, der indeholder mindst én alvorlig bivirkning, er mærket med en dolk (†).
Any term that includes at least one serious adverse reaction is identified with a dagger (†).
Bivirkninger, der er rapporteret efter markedsføring, er skrevet med kursiv.
Adverse reactions identified from post-marketing experience are included in italics.
Hyppighed er defineret som almindelig (≥1/ 100 til < 1/ 10), ikke almindelig (≥1/ 1. 000 til < 1/ 100) og ikke kendt (kan ikke estimeres ud fra de tilgængelige data).
Frequencies are defined as common (≥ 1/ 100 to < 1/ 10), uncommon (≥ 1/ 1,000 to < 1/ 100), and not known (cannot be estimated from the available data).
ISENTRESS (alene eller i kombination med OBT) Infektioner og parasitære sygdomme
ISENTRESS (alone or in combination with OBT) Infections and infestations
Genital herpes †, folliculitis, herpes simplex, herpes virusinfektion, herpes zoster, influenza, molluscum contagiosum
genital herpes†, folliculitis, herpes simplex, herpes virus infection, herpes zoster, influenza, molluscum contagiosum
Jernmangelanæmi,
iron deficiency anaemia
Lægemiddeloverfølsomhed †,
Immune system disorders Metabolism and nutrition disorders
Central adipositas, nedsat appetit, diabetes mellitus, dyslipidæmi, hyperkolesterolæmi, øget appetit
drug hypersensitivity† central obesity, decreased appetite, diabetes mellitus, dyslipidaemia, hypercholesterolaemia, increased appetite
Insomnia
insomnia
Unormale drømme, angst, depression, afbrudt søvnmønster, søvnforstyrrelser
abnormal dreams, anxiety, depression, middle insomnia, sleep disorder
Suicidale tanker og suicidal adfærd (især hos patienter med psykisk sygdom i anamnesen)
suicidal ideation, suicidal behaviour (particularly in patients with a pre-existing history of psychiatric illness)
Karpaltunnelsyndrom, opmærksomhedsforstyrrelse, postural svimmelhed, dysgeusi, hypersomnia, hypæstesi, letargi, neuropati, perifer neuropati, paræstesi, somnolens, spændingshovedpine, tremor
carpal tunnel syndrome, disturbance in attention, dizziness postural, dysgeusia, hypersomnia, hypoaesthesia, lethargy, neuropathy, neuropathy peripheral, paraesthesia, somnolence, tension headache, tremor
Øjne
Eye disorders Ear and labyrinth disorders Cardiac disorders Respiratory, thoracic and mediastinal disorders
Ikke almindelig
uncommon uncommon uncommon uncommon
Synsforstyrrelse
visual disturbance vertigo palpitations, ventricular extrasystoles dysphonia, epistaxis, nasal congestion, pharyngeal erythema
Øre og labyrint
7
Vertigo
Frequency
Ikke almindelig
ISENTRESS (alone
Palpitationer, ventrikulære ekstrasystoler
Adverse reactions or in combination with OBT)
Ikke almindelig Almindelig
common
Dysfoni, epistaxis, nasal kongestion, faryngeal erytem Abdominal distention, abdominal smerte, obstipation, diarré, flatulens, kvalme, opkastning
abdominal distention, abdominal pain, constipation, diarrhoea, flatulence, nausea, vomiting
Gastritis †, abdominale gener, øvre abdominal smerte, anale gener, mundtørhed, dyspepsi, eructatio, gastroøsofageal refluks, glossitis, odynofagi, oral smerte, akut pankreatit, ulcus pepticum, rektal blødning, mavegener
gastritis†, abdominal discomfort, abdominal pain upper, anal discomfort, dry mouth, dyspepsia, eructation, gastrooesophageal reflux disease, glossitis, odynophagia, oral pain, pancreatitis acute, peptic ulcer, rectal haemorrahage, stomach discomfort
Hud og subkutane væv
Hepato-biliary disorders Skin and subcutaneous tissue disorders
Almindelig
uncommon common
Hyperhidrose, nattesved, pruritus, udslæt
hepatitis† hyperhidrosis, night sweats, pruritus, rash
atrofi, lipoatrofi, erhvervet lipodystrofi, lipohypertrofi, prurigo, generaliseret pruritus, makuløst udslæt, makulopapuløst udslæt, kløende udslæt, xeroderma
acne, dermatitis acneiforme, dry skin, erythema, facial wasting, lipoatrophy, lipodystrophy acquired, lipohypertrophy, prurigo, pruritis generalised, rash macular, rash maculo-papular, rash pruritic, xeroderma
Stevens- Johnsons syndrom
Stevens Johnson syndrome
Rygsmerter, muskelatrofi, smerter i knogler, led og muskler, myalgi, myositis, smerter i ekstremiteterne, tendinitis
back pain, muscle atrophy, musculoskeletal pain, myalgia, myositis, pain in extremity, tendonitis
Nyreinsufficiens †, interstitiel nefritis, nefrolitiasis, nykturi, pollakisuri
renal failure†, nephritis interstitial, nephrolithiasis, nocturia, pollakiuria
Det reproduktive system og mammae Almene symptomer og reaktioner på
Reproductive system and breast disorders
Erektil dysfunktion, gynækomasti, menopausesymptomer Asteni, træthed
erectile dysfunction, gynaecomastia, menopausal symptoms
administrationsstedet
asthenia, fatigue
Gener i brystet, kuldegysninger, ansigtsødem, øget fedtvæv, varmefølelse, anspændthed, pyreksi, xerose
chest discomfort, chills, face oedema, fat tissue increased, feeling hot, feeling jittery, pyrexia, xerosis
Øget ALAT, øget ASAT, øget mængde af triglycerider i blodet, øget serumkreatininkinase, øget lipase
alanine aminotransferase increased, aspartate aminotransferase increased, blood triglycerides increased, serum creatinine kinase increased, lipase increased
Reduceret absolut neutrofilværdi, forhøjet blodamylase, forhøjet kolesteroltal, stigning i serumkreatinin, stigning i blodsukker, stigning i karbamidkvælstof, stigning i fasteblodsukker, sukker i urinen, stigning i HDL, stigning i LDL, fald i antal blodplader, positiv test for røde blodlegemer i urinen, vægtøgning, fald i antal hvide blodlegemer
absolute neutrophil count decreased, blood amylase increased, blood cholesterol increased, blood creatinine increased, blood glucose increased, blood urea nitrogen increased, fasting blood glucose increased, glucose urine present, high density lipoprotein increased, low density lipoprotein increased, platelet count decreased, red blood cells urine positive, weight increased, white blood cell count decreased
Traumer, forgiftninger og behandlingskomplikationer †
Injury, poisoning and procedural complications †
Uforsætlig overdosering †
accidental overdose†
omfatter mindst én alvorlig bivirkning
includes at least one serious adverse reaction
8 Cancer blev rapporteret hos behandlingserfarne patienter, som startede i behandling med ISENTRESS og OBT; flere af tilfældene var recidive.
Cancers were reported in treatment-experienced patients who initiated ISENTRESS with OBT; several were recurrent.
Type og hyppighed af de specifikke cancerformer var de, som kan forventes i en yderst immundeficient population (mange havde et CD4- celletal under 50 celler/ mm3, og de fleste havde AIDS- diagnoser fra tidligere).
The types and rates of specific cancers were those expected in a highly immunodeficient population (many had CD4 cell counts below 50 cells/ mm3 and most had prior AIDS diagnoses).
Cancerformerne omfattede kaposisarkom, lymfom, spinocellulært karcinom, hepatocellulært karcinom samt analcancer.
The cancers included Kaposi’ s sarcoma, lymphoma, squamous cell carcinoma, hepatocellular carcinoma and anal cancer.
De fleste patienter havde andre risikofaktorer for cancer inklusive tobaksbrug, papillomavirus og aktiv hepatitis B- virusinfektion.
Most patients had other risk factors for cancer including 8 tobacco use, papillomavirus and active hepatitis B virus infection.
4. 4).
It is unknown if these cancer diagnoses were related to ISENTRESS use (see section 4.4).
Der blev observeret abnorme laboratorieværdier for kreatinkinase, grad 2- 4, hos forsøgspersoner, der blev behandlet med ISENTRESS.
Grade 2-4 creatine kinase laboratory abnormalities were observed in subjects treated with ISENTRESS.
Der er rapporteret om myopati og rhabdomyolyse; forholdet mellem ISENTRESS og disse hændelser er dog ikke kendt.
Myopathy and rhabdomyolysis have been reported; however, the relationship of ISENTRESS to these events is not known.
4. 4).
Use with caution in patients who have had myopathy or rhabdomyolysis in the past or have any predisposing issues including other medicinal products associated with these conditions (see section 4.4).
Der har været rapporteret om tilfælde af osteonekrose hos især patienter med generelt kendt risikofaktorer, fremskreden HIV- sygdom eller langvarig eksponering for antiretroviral kombinationsbehandling (CART).
Cases of osteonecrosis have been reported, particularly in patients with generally acknowledged risk factors, advanced HIV disease or long-term exposure to combination antiretroviral therapy (CART).
Patienter koinficeret med hepatitis B - og/ eller hepatitis C- virus Patienter med kronisk aktiv hepatitis B - og/ eller hepatitis C- koinfektion fik adgang til at deltage i fase III- undersøgelser (N=113/ 699 eller 16, 2%; HBV=6%, HCV=9%, HBV+HCV=1%), forudsat at prøverne vedrørende ASAT, ALAT og alkalisk phosphatase ikke oversteg 5 gange den øvre normalgrænse.
Patients co-infected with hepatitis B and/ or hepatitis C virus In Phase III studies, patients with chronic active hepatitis B and/ or hepatitis C co-infection (N = 113/ 699 or 16.2%; HBV=6%, HCV=9%, HBV+HCV=1%) were permitted to enrol provided that AST, ALT, and alkaline phosphatase tests did not exceed 5 times the upper limit of normal.
Generelt var sikkerhedsprofilen for ISENTRESS hos patienter med hepatitis B - og/ eller hepatitis C- viruskoinfektion den samme som hos patienter uden hepatitis B og/ eller hepatitis C viruskoinfektion.
In general the safety profile of ISENTRESS in patients with hepatitis B and/ or hepatitis C virus co- infection was similar to that in patients without hepatitis B and/ or hepatitis C virus co-infection.
Abnorme laboratorieværdier af grad 2 eller højere, som viser en forværring af ASAT, ALAT eller totalbilirubin i forhold til baseline, forekom hos henholdsvis 31%, 31% og 16% af de raltegravirbehandlede og koinficerede forsøgspersoner sammenlignet med henholdsvis 9%, 8% og 8% af alle andre raltegravirbehandlede forsøgspersoner.
Grade 2 or higher laboratory abnormalities that represent a worsening from baseline of AST, ALT or total bilirubin occurred in 31%, 31% and 16%, respectively, of raltegravir-treated co-infected subjects as compared to 9%, 8% and 8% of all other raltegravir-treated subjects.
Der findes ingen specifik information om behandling af overdosering i forbindelse med ISENTRESS.
No specific information is available on the treatment of overdosage with ISENTRESS.
I tilfælde af overdosering er det hensigtsmæssigt at anvende understøttende standardiserede foranstaltninger, f. eks. fjerne uabsorberet lægemiddel fra mave- tarmkanalen, foretage klinisk monitorering (inklusive elektrokardiogram) og igangsætte understøttende behandling, hvis dette er nødvendigt.
In the event of an overdose, it is reasonable to employ the standard supportive measures, e. g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.
Det vides ikke, i hvilken grad ISENTRESS er dialyserbart.
The extent to which ISENTRESS may be dialysable is unknown.
Antiviralt lægemiddel til systemisk anvendelse, Andre antivirale lægemidler, ATC- kode:
Antiviral for systemic use, Other Antivirals, ATC code:
Virkningsmekanisme Raltegravir er en HIV- integrasehæmmer af genoverførsel, som virker mod human immundefekt virus (HIV- 1).
Mechanism of action Raltegravir is an integrase strand transfer inhibitor active against the Human Immunodeficiency Virus (HIV-1).
Raltegravir hæmmer den katalytiske aktivitet af integrase, som er et HIV- kodet enzym, der er nødvendig for viral replikation.
Raltegravir inhibits the catalytic activity of integrase, an HIV-encoded enzyme that is required for viral replication.
Hæmning af integrase hindrer den kovalente insertion, eller integration, af HIV- genomet i værtscellegenomet.
Inhibition of integrase prevents the covalent insertion, or integration, of the HIV genome into the host cell genome.
HIV- genomer, som ikke integrerer, kan ikke lede produktionen af nye infektiøse viruspartikler, så integrationshæmning hindrer udbredelse af virusinfektionen.
HIV genomes that fail to integrate cannot direct the production of new infectious viral particles, so inhibiting integration prevents propagation of the viral infection.
9 Antiviral aktivitet in vitro Raltegravir i koncentrationer på 31 ± 20 nM resulterede i 95% hæmning (IC95) af HIV- 1 replikation (i forhold til en ubehandlet virusinficeret kultur) i humane T- lymfoide cellekulturer inficeret med cellelinie- adapteret HIV- 1 variant H9IIIB.
Antiviral activity in vitro Raltegravir at concentrations of 31 ± 20 nM resulted in 95% inhibition (IC95) of HIV-1 replication (relative to an untreated virus-infected culture) in human T-lymphoid cell cultures infected with the cell-line adapted HIV-1 variant H9IIIB.