Examples of using Tipranavir in English and their translations into German
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Interaction with tipranavir.
Plasma levels of tipranavir can be reduced by concomitant use of the herbal preparation St John' s wort Hypericum perforatum.
The active substance is tipranavir.
However, since the renal clearance of tipranavir is negligible, a decrease in total body clearance is not expected in patients with renal impairment.
Metabolic profile of tipranavir.
Tipranavir demonstrates antiviral activity in vitro against a broad panel of HIV-1 group M non-clade B isolates A, C, D, F, G, H, CRF01 AE, CRF02 AG, CRF12 BF.
Each capsule contains 250 mg tipranavir.
Carcinogenicity studies of tipranavir in mice and rats revealed tumourigenic potential specific for these species, which are regarded as of no clinical relevance.
Each soft capsule contains 250 mg tipranavir.
The predominant effects of repeated administration of tipranavir across all species toxicologically tested were on the gastrointestinal tract(emesis, soft stool, diarrhoea) and the liver hypertrophy.
Aptivus contains the active substance tipranavir.
Co-administration of APTIVUS and agents that induce CYP3A and/ orPgp may decrease tipranavir concentrations and reduce its therapeutic effect see list and details of considered agents, below.
The most abundant urinary metabolite, at 11.0% of urine radioactivity(0.5% of dose)was a glucuronide conjugate of tipranavir.
In vitro, there is an inverse correlation between the degree of resistance to tipranavir and the capacity of viruses to replicate.
As demonstrated in a dose- ranging evaluation in 113 HIV-negative healthy male and female volunteers, ritonavir increases AUC0- 12h,Cmax and Cmin and decreases the clearance of tipranavir.
Doses of ritonavirless than 200 mg twice daily should not be used with tipranavir as they might alter the efficacy of the combination.
In vitro metabolism studies with human liver microsomes indicated that CYP3A4is the predominant CYP isoform involved in tipranavir metabolism.
In a study conducted in rats with tipranavir at systemic exposure levels(AUC) equivalent to human exposure at the recommended clinical dose, no adverse effects on mating or fertility were observed.
HIV protease inhibitors other than atazanavir and darunavir(e.g., indinavir, saquinavir, tipranavir, lopinavir/ritonavir) are contraindicated see section 4.3.
In a 14C-tipranavir human study(14C-tipranavir/ ritonavir, 500 mg/ 200 mg twicedaily), unchanged tipranavir was predominant and accounted for 98.4% or greater of the total plasma radioactivity circulating at 3, 8, or.
An increase in gastric pH that may result from H2-receptor antagonist therapyis not expected to have an impact on tipranavir plasma concentrations.
There was an averagedecrease in susceptibility of 2-fold wild type(WT) for tipranavir, 12-fold WT for amprenavir, 55-fold WT for atazanavir, 41-fold WT for indinavir, 87-fold WT for lopinavir, 41- fold WT for nelfinavir, 195-fold WT for ritonavir, and 20-fold WT for saquinavir.
The influence of moderate(Child-Pugh B) or severe(Child-Pugh C)hepatic impairment on the multiple dose pharmacokinetics of either tipranavir or ritonavir has so far not been investigated.
From clinical samples of healthy volunteers and HIV-1 positive subjects who received tipranavir without ritonavir the mean fraction of tipranavir unbound in plasma was similar in both populations healthy volunteers 0.015%± 0.006%; HIV-positive subjects 0.019%± 0.076.
When APTIVUS, co-administered with low dose ritonavir, was co-administered with 20 ml of aluminium-and magnesium-based liquid antacid, tipranavir AUC12h, Cmax and Cmin were reduced by 25-29.
In studies where tipranavir co-administered with low-dose ritonavir was used with or without enfuvirtide, it has been observed that the steady-state plasma tipranavir trough concentration of patients receiving enfuvirtide were 45% higher as compared to patients not receiving enfuvirtide.
Herbal preparations containing St John' s wort(Hypericum perforatum) must not be used while taking APTIVUSdue to the risk of decreased plasma concentrations and reduced clinical effects of tipranavir see section 4.5.
Co-administration of APTIVUS and low dose ritonavir with agents primarily metabolised by CYP3Amay result in changed plasma concentrations of tipranavir or the other agents, which could alter their therapeutic and adverse effects see list and details of considered agents, below.
Nevirapine exhibited additive to synergistic anti-HIV-1 activity in combination with the protease inhibitors amprenavir, atazanavir, indinavir, lopinavir,saquinavir and tipranavir, and the NRTIs abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir and zidovudine.
Cross-resistance Darunavir has a< 10-fold decreased susceptibility against 90% of 3,309 clinical isolates resistant to amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir,saquinavir and/or tipranavir showing that viruses resistant to most PIs remain susceptible to darunavir.