Monday, September 12, 2016

Aptivus 250 mg soft capsules





1. Name Of The Medicinal Product



APTIVUS 250 mg soft capsules


2. Qualitative And Quantitative Composition



Each soft capsule contains 250 mg tipranavir.



Excipients (per capsule): 100.0 mg ethanol, 455.0 mg macrogolglycerol ricinoleate and 12.6 mg sorbitol (constituent in « Sorbitol Special-Glycerin Blend »)



For a full list of excipients, see section 6.1.



3. Pharmaceutical Form



Soft capsule.



Each capsule is pink and is imprinted with “TPV 250”.



4. Clinical Particulars



4.1 Therapeutic Indications



APTIVUS, co-administered with low dose ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infection in highly pre-treated adults and adolescents 12 years of age or older with virus resistant to multiple protease inhibitors. APTIVUS should only be used as part of an active combination antiretroviral regimen in patients with no other therapeutic options.



This indication is based on the results of two phase III studies, performed in highly pre-treated adult patients (median number of 12 prior antiretroviral agents) with virus resistant to protease inhibitors and of one phase II study investigating pharmacokinetics, safety and efficacy of APTIVUS in mostly treatment-experienced adolescent patients aged 12 to 18 years (see section 5.1).



In deciding to initiate treatment with APTIVUS, co-administered with low dose ritonavir, careful consideration should be given to the treatment history of the individual patient and the patterns of mutations associated with different agents. Genotypic or phenotypic testing (when available) and treatment history should guide the use of APTIVUS. Initiation of treatment should take into account the combinations of mutations which may negatively impact the virological response to APTIVUS, co-administered with low dose ritonavir (see section 5.1).



4.2 Posology And Method Of Administration




APTIVUS must always be given with low dose ritonavir as a pharmacokinetic enhancer, and in combination with other antiretroviral medicinal products. The Summary of Product Characteristics of ritonavir must therefore be consulted prior to initiation of therapy with APTIVUS (especially as regards the contraindications, warnings and undesirable effects sections).


APTIVUS should be prescribed by physicians who are experienced in the treatment of HIV-1 infection.



APTIVUS with ritonavir should not be used in treatment-naïve patients.



Posology



Patients should be advised of the need to take APTIVUS and ritonavir every day as prescribed. If a dose is missed by more than 5 hours, the patient should be instructed to wait and then to take the next dose of APTIVUS and ritonavir at the regularly scheduled time. If a dose is missed by less than 5 hours, the patient should be instructed to take the missed dose immediately, and then to take the next dose of APTIVUS and ritonavir at the regularly scheduled time.



Adults



The recommended dose of APTIVUS is 500 mg, co-administered with 200 mg ritonavir (low dose ritonavir), twice daily.



Doses of ritonavir lower than 200 mg twice daily should not be used as they might alter the efficacy profile of the combination.



Paediatric population



Adolescents from 12 years of age



The recommended dose of APTIVUS is 500 mg, co-administered with 200 mg ritonavir (low dose ritonavir), twice daily (see section 4.4 for precautionary measures in adolescents).



Doses of ritonavir lower than 200 mg twice daily should not be used as they might alter the efficacy profile of the combination.



Since currently only limited efficacy and safety data are available for adolescents (see section 5.1) close monitoring of virologic response and tolerance is particularly warranted in this patient group.



Children under 12 years of age:



The safety and efficacy of APTIVUS capsules in children aged 2 to 12 years has not been established.



Currently available data are described in section 5.1 and 5.2 but no recommendation on a posology can be made.



Also, appropriate dose adjustments for children under 12 years cannot be achieved with APTIVUS capsules. APTIVUS oral solution is available for children between 2 and 12 years of age (please refer to the respective SPC for further details).



The safety and efficacy of APTIVUS in children under 2 years of age has not been established. No data are available.



Elderly



Clinical studies of APTIVUS did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects (see section 5.2).



In general, caution should be exercised in the administration and monitoring of APTIVUS in elderly patients reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other therapy. (see section 4.4)



Liver impairment



Tipranavir is metabolised by the hepatic system. Liver impairment could therefore result in an increase of tipranavir exposure and a worsening of its safety profile. Therefore, APTIVUS should be used with caution, and with increased monitoring frequency, in patients with mild hepatic impairment (Child-Pugh Class A). APTIVUS is contraindicated in patients with moderate or severe (Child-Pugh Class B or C) hepatic impairment (see sections 4.3, 4.4 and 5.2).



Renal impairment



No dosage adjustment is required in patients with renal impairment (see sections 4.4 and 5.2).



Method of administration



APTIVUS soft capsules co-administered with low dose ritonavir should be taken with food (see section 5.2).



4.3 Contraindications



Hypersensitivity to the active substance or to any of the excipients.



Patients with moderate or severe (Child-Pugh B or C) hepatic impairment.



Combination of rifampicin with APTIVUS with concomitant low dose ritonavir is contraindicated (see section 4.5).



Herbal preparations containing St John's wort (Hypericum perforatum) must not be used while taking APTIVUS due to the risk of decreased plasma concentrations and reduced clinical effects of tipranavir (see section 4.5).



Co-administration of APTIVUS with low dose ritonavir, with active substances that are highly dependent on CYP3A for clearance, and for which elevated plasma concentrations are associated with serious and/or life-threatening events, is contraindicated. These active substances include antiarrhythmics (amiodarone, bepridil, quinidine), antihistamines (astemizole, terfenadine), ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), gastrointestinal motility agents (cisapride), neuroleptics (pimozide, sertindole), sedatives/hypnotics (orally administered midazolam and triazolam. For caution on parenterally administered midazolam see section 4.5) and HMG-CoA reductase inhibitors (simvastatin and lovastatin). Also contraindicated is the use of the alpha-1 adrenoceptor antagonist alfuzosin, and sildenafil when used for the treatment of pulmonary arterial hypertension. In addition, co-administration of APTIVUS with low dose ritonavir, and medicinal products that are highly dependent on CYP2D6 for clearance, such as the antiarrhythmics flecainide, propafenone and metoprolol given in heart failure, is contraindicated (see section 4.5).



4.4 Special Warnings And Precautions For Use



APTIVUS must be administered with low dose ritonavir to ensure its therapeutic effect (see section 4.2). Failure to correctly co-administer tipranavir with ritonavir will result in reduced plasma levels of tipranavir that may be insufficient to achieve the desired antiviral effect. Patients should be instructed accordingly.



APTIVUS is not a cure for HIV-1 infection or AIDS. Patients receiving APTIVUS or any other antiretroviral therapy may continue to develop opportunistic infections and other complications of HIV-1 infection.



Patients should be advised that there is still a risk of passing HIV to others through blood or sexual contact when taking APTIVUS. Appropriate precautions should continue to be employed.



Switching from APTIVUS capsules to the oral solution: APTIVUS capsules are not interchangeable with the oral solution. Compared to the capsules, tipranavir exposure is higher when administering the same dose as oral solution. Also, the composition of the oral solution is different from that of the capsules, with the high vitamin E content being especially noteworthy. Both of these factors may contribute to an increased risk of adverse reactions (type, frequency and/or severity). Therefore patients should not be switched from APTIVUS capsules to APTIVUS oral solution (see sections 5.1 and 5.2).



Switching from APTIVUS oral solution to the capsules: APTIVUS oral solution is not interchangeable with the capsules. Compared to the oral solution, tipranavir exposure is lower when administering the same dose as capsules. However, children previously treated with APTIVUS oral solution and becoming 12 years of age should be switched to capsules, particularly because of the more favourable safety profile of the capsules. It has to be noted that the switch from the oral solution to the capsule formulation of APTIVUS could be associated with decreased exposure. Therefore, it is recommended that patients switching from APTIVUS oral solution to capsules at the age of 12 years are closely monitored for the virologic response of their antiretroviral regimen (see sections 5.1 and 5.2).



Elderly: Clinical studies of APTIVUS did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects (see section 5.2).



In general, caution should be exercised in the administration and monitoring of APTIVUS in elderly patients reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other therapy (see section 4.2).



Liver disease: APTIVUS is contraindicated in patients with moderate or severe (Child-Pugh Class B or C) hepatic insufficiency. Limited data are currently available for the use of APTIVUS, co-administered with low dose ritonavir, in patients co-infected with hepatitis B or C. Patients with chronic hepatitis B or C and treated with combination antiretroviral therapy are at an increased risk for severe and potentially fatal hepatic adverse reaction. APTIVUS should be used in this patient population only if the potential benefit outweighs the potential risk, and with increased clinical and laboratory monitoring. In the case of concomitant antiviral therapy for hepatitis B or C, please refer also to the relevant Summary of Product Characteristics for these medicinal products.



Patients with mild hepatic impairment (Child-Pugh Class A) should be closely monitored.



Patients with pre-existing liver dysfunction including chronic active hepatitis have an increased frequency of liver function abnormalities during combination therapy and should be monitored according to standard practice. APTIVUS with ritonavir should be discontinued once signs of worsening liver function occur in patients with pre-existing liver disease.



APTIVUS co-administered with low dose ritonavir, has been associated with reports of clinical hepatitis and hepatic decompensation, including some fatalities. These have generally occurred in patients with advanced HIV disease taking multiple concomitant medicinal products. Caution should be exercised when administering APTIVUS to patients with liver enzyme abnormalities or with a history of hepatitis. Increased ALAT/ASAT monitoring should be considered in these patients.



APTIVUS therapy should not be initiated in patients with pre-treatment ASAT or ALAT greater than 5 times the Upper Limit Normal (ULN) until baseline ASAT/ALAT is stabilised at less than 5X ULN, unless the potential benefit justifies the potential risk.



APTIVUS therapy should be discontinued in patients experiencing ASAT or ALAT elevations greater than 10X ULN, or developing signs or symptoms of clinical hepatitis during therapy. If another cause is identified (eg acute hepatitis A, B or C virus, gallbladder disease, other medicinal products), then rechallenge with APTIVUS may be considered when ASAT/ALAT have returned to the patient's baseline levels.



Liver monitoring



Monitoring of hepatic tests should be done prior to initiation of therapy, after two, four and then every four weeks until 24 weeks, and then every eight to twelve weeks thereafter. Increased monitoring (i.e. prior to initiation of therapy, every two weeks during the first three months of treatment, then monthly until 48 weeks, and then every eight to twelve weeks thereafter) is warranted when APTIVUS and low dose ritonavir are administered to patients with elevated ASAT and ALAT levels, mild hepatic impairment, chronic hepatitis B or C, or other underlying liver disease.



Treatment-naïve patients



In a study performed in antiretroviral naïve adult patients, tipranavir 500 mg with ritonavir 200 mg twice daily, as compared to lopinavir/ritonavir, was associated with an excess in the occurrence of significant (grade 3 and 4) transaminase elevations without any advantage in terms of efficacy (trend towards a lower efficacy). The study was prematurely stopped after 60 weeks.



Therefore, tipranavir with ritonavir should not be used in treatment-naïve patients. (see section 4.2)



Renal impairment



Since the renal clearance of tipranavir is negligible, increased plasma concentrations are not expected in patients with renal impairment.



Haemophilia



There have been reports of increased bleeding, including spontaneous skin haematomas and haemarthrosis in patients with haemophilia type A and B treated with protease inhibitors. In some patients additional Factor VIII was given. In more than half of the reported cases, treatment with protease inhibitors was continued or reintroduced if treatment had been discontinued. A causal relationship has been evoked, although the mechanism of action had not been elucidated. Haemophiliac patients should therefore be made aware of the possibility of increased bleeding.



Bleeding



RESIST participants receiving APTIVUS with ritonavir tended to have an increased risk of bleeding; at 24 weeks the relative risk was 1.98 (95% CI=1.03, 3.80). At 48-weeks the relative risk decreased to 1.27 (95% CI=0.76, 2.12). There was no pattern for the bleeding events and no difference between treatment groups in coagulation parameters. The significance of this finding is being further studied.



Fatal and non-fatal intracranial haemorrhages (ICH) have been reported in patients receiving APTIVUS, many of whom had other medical conditions or were receiving concomitant medicinal products that may have caused or contributed to these events. However, in some cases the role of APTIVUS cannot be excluded. No pattern of abnormal haematological or coagulation parameters has been observed in patients in general, or preceding the development of ICH. Therefore, routine measurement of coagulation parameters is not currently indicated in the management of patients on APTIVUS.



An increased risk of ICH has previously been observed in patients with advanced HIV disease/AIDS such as those treated in the APTIVUS clinical trials.



In in vitro experiments, tipranavir was observed to inhibit human platelet aggregation at levels consistent with exposures observed in patients receiving APTIVUS with ritonavir.



In rats, co-administration with vitamin E increased the bleeding effects of tipranavir (see section 5.3 Preclinical safety data).



APTIVUS, co-administered with low dose ritonavir, should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery or other medical conditions, or who are receiving medicinal products known to increase the risk of bleeding such as antiplatelet agents and anticoagulants or who are taking supplemental vitamin E. Based on the limits of exposure available from observation in clinical trials, it is recommended not to co-administer to patients more than 1,200 IU vitamin E per day.



Diabetes mellitus/hyperglycaemia



New onset of diabetes mellitus, hyperglycaemia or exacerbations of existing diabetes mellitus has been reported in patients receiving antiretroviral therapy, including protease inhibitors. In some of these the hyperglycaemia was severe and in some cases also associated with ketoacidosis. Many of the patients had confounding medical conditions, some of which required therapy with agents that have been associated with the development of diabetes mellitus or hyperglycaemia.



Lipid elevations



Treatment with APTIVUS co-administered with low dose ritonavir and other antiretroviral agents has resulted in increased plasma total triglycerides and cholesterol. Triglyceride and cholesterol testing should be performed prior to initiating tipranavir therapy and during therapy. Treatment-related lipid elevations should be managed as clinically appropriate.



Fat redistribution



Combination antiretroviral therapy has been associated with the redistribution of body fat (lipodystrophy) in HIV infected patients. The long-term consequences of these events are currently unknown. Knowledge about the mechanism is incomplete. A connection between visceral lipomatosis and protease inhibitors, and lipoatrophy and nucleoside reverse transcriptase inhibitors, has been hypothesised. A higher risk of lipodystrophy has been associated with individual factors such as older age, and with factors related to the active substance such as longer duration of antiretroviral treatment and associated metabolic disturbances. Clinical examination should include evaluation for physical signs of fat redistribution. Consideration should be given to the measurement of fasting serum lipids and blood glucose. Lipid disorders should be managed as clinically appropriate (see section 4.8).



Immune reactivation syndrome



In HIV-infected patients with severe immune deficiency at the time of institution of combination antiretroviral therapy (CART), an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and cause serious clinical conditions, or aggravation of symptoms. Typically, such reactions have been observed within the first few weeks or months of initiation of CART. Relevant examples are cytomegalovirus retinitis, generalised and/or focal mycobacterial infections and Pneumocystis pneumonia. Any inflammatory symptoms should be evaluated and treatment instituted when necessary. In addition, reactivation of herpes simplex and herpes zoster has been observed in clinical studies with APTIVUS, co-administered with low dose ritonavir.



Rash



Mild to moderate rashes including urticarial rash, maculopapular rash, and photosensitivity have been reported in subjects receiving APTIVUS, co-administered with low dose ritonavir. At 48-weeks in Phase III trials, rash of various types was observed in 15.5% males and 20.5% females receiving APTIVUS co-administered with low dose ritonavir. Additionally, in one interaction trial, in healthy female volunteers administered a single dose of ethinyl oestradiol followed by APTIVUS co-administered with low dose ritonavir, 33% of subjects developed a rash. Rash accompanied by joint pain or stiffness, throat tightness, or generalized pruritus has been reported in both men and women receiving APTIVUS co-administered with low dose ritonavir. In the paediatric clinical trial, the frequency of rash (all grades, all causality) through 48 weeks of treatment was higher than in adult patients.



Osteonecrosis



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). Patients should be advised to seek medical advice if they experience joint aches and pain, joint stiffness or difficulty in movement.



Interactions



The interaction profile of tipranavir, co-administered with low dose ritonavir, is complex. For a description of the mechanisms and potential mechanisms contributing to the interaction profile of tipranavir, see section 4.5.



Abacavir and zidovudine: The concomitant use of APTIVUS, co-administered with low dose ritonavir, with zidovudine or abacavir, results in a significant decrease in plasma concentration of these nucleoside reverse transcriptase inhibitors (NRTIs). Therefore, the concomitant use of zidovudine or abacavir with APTIVUS, co-administered with low dose ritonavir, is not-recommended unless there are no other available NRTIs suitable for patient management (see section 4.5).



Protease inhibitors: Concomitant use of APTIVUS, co-administered with low dose ritonavir, with the protease inhibitors amprenavir, lopinavir or saquinavir (each co-administered with low dose ritonavir) in a dual-boosted regimen, results in significant decreases in plasma concentrations of these protease inhibitors. A significant decrease in plasma concentrations of atazanavir and a marked increase of tipranavir and ritonavir concentrations was observed when APTIVUS, associated with low dose ritonavir, was co-administered with atazanavir (see section 4.5). No data are currently available on interactions of tipranavir, co-administered with low dose ritonavir, with protease inhibitors other than those listed above. Therefore, the co-administration of tipranavir, co-administered with low dose ritonavir, with protease inhibitors is not recommended.



Oral contraceptives and oestrogens: Since levels of ethinyl oestradiol are decreased, the co-administration of APTIVUS co-administered with low dose ritonavir is not recommended. Alternative or additional contraceptive measures are to be used when oestrogen based oral contraceptives are co-administered with APTIVUS co-administered with low dose ritonavir (see section 4.5). Patients using oestrogens as hormone replacement therapy should be clinically monitored for signs of oestrogen deficiency. Women using oestrogens may have an increased risk of non serious rash.



Anticonvulsants: Caution should be used when prescribing carbamazepine, phenobarbital, and phenytoin. APTIVUS may be less effective due to decreased tipranavir plasma concentrations in patients taking these agents concomitantly.



Halofantrine, lumefantrine: Due to their metabolic profile and inherent risk of inducing torsades de pointes, administration of halofantrine and lumefantrine with APTIVUS co-administered with low dose ritonavir, is not recommended.



Disulfiram/metronidazole: APTIVUS soft capsules contain alcohol (7% ethanol, ie 100 mg per capsule or up to 200 mg per dose) which can produce disulfiram-like reactions when co-administered with disulfiram or other medicinal products which produce this reaction (eg metronidazole).



Fluticasone: Concomitant use of tipranavir, co-administered with low dose ritonavir, and fluticasone or other glucocorticoids that are metabolised by CYP3A4 is not recommended unless the potential benefit of treatment outweighs the risk of systemic corticosteroid effects, including Cushing's syndrome and adrenal suppression (see section 4.5).



Atorvastatin: tipranavir, co-administered with low dose ritonavir, increases the plasma concentrations of atorvastatin (see section 4.5). The combination is not recommended. Other HMG-CoA reductase inhibitors should be considered such as pravastatin, fluvastatin or rosuvastatin (see section 4.5). However, if atorvastatin is specifically required for patient management, it should be started with the lowest dose and careful monitoring is necessary.



Omeprazole and other proton pump inhibitors: The combined use of APTIVUS with ritonavir with either omeprazole, esomeprazole or with other proton pump inhibitors is not recommended (see section 4.5).



Colchicine:



The administration of colchicine and APTIVUS, co-administered with low dose ritonavir, is not recommended. (see section 4.5).



Salmeterol:



Concomitant use of salmeterol and APTIVUS, co-administered with low dose ritonavir, is not recommended (see section 4.5).



Bosentan: Due to the marked hepatotoxicity of bosentan and the potential for increasing the liver toxicity associated with APTIVUS,co-administered with low dose ritonavir, this combination is not recommended.



Warnings related to certain excipients:



Due to APTIVUS containing small amounts of sorbitol, patients with rare hereditary problems of fructose intolerance should not take this medicine.



APTIVUS contains macrogolglycerol ricinoleate which may cause stomach upset and diarrhoea.



This medicinal product contains 7 vol % ethanol (alcohol), i.e. up to 400 mg per daily dose, equivalent to 8 ml of beer, or less than 4 ml of wine.



Harmful for those suffering from alcoholism.



To be taken into account in pregnant or breast-feeding women, children and high-risk groups such as patients with liver disease, or epilepsy.



4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction





The interaction profile of APTIVUS, co-administered with low dose ritonavir, is complex and requires special attention in particular in combination with other antiretroviral agents.



Interaction studies have only been performed in adults.



Metabolic profile of tipranavir:



Tipranavir is a substrate, an inducer and an inhibitor of cytochrome P450 CYP3A. When co-administered with ritonavir at the recommended dosage (see section 4.2) there is a net inhibition of P450 CYP3A. Co-administration of APTIVUS and low dose ritonavir with agents primarily metabolised by CYP3A may result in changed plasma concentrations of tipranavir or the other agents, which could alter their therapeutic and undesirable effects (see list and details of considered agents, below). Agents that are contraindicated specifically due to the expected magnitude of interaction and potential for serious adverse reactions are detailed in this section, and listed in section 4.3.



A cocktail study was conducted in 16 healthy volunteers with twice-daily 500 mg tipranavir with 200 mg ritonavir capsule administration for 10 days to assess the net effect on the activity of hepatic CYP 1A2 (caffeine), 2C9 (warfarin), 2D6 (dextromethorphan), both intestinal/hepatic CYP 3A4 (midazolam) and P-glycoprotein (Pgp) (digoxin). At steady state, there was a significant induction of CYP 1A2 and a slight induction on CYP 2C9. Potent inhibition of CYP 2D6 and both hepatic and intestinal CYP 3A4 activities were observed. Pgp activity is significantly inhibited after the first dose, but there was a slight induction at steady state. Practical recommendations deriving from this study are displayed below.



Studies in human liver microsomes indicated tipranavir is an inhibitor of CYP 1A2, CYP 2C9, CYP 2C19 and CYP 2D6. The potential net effect of tipranavir with ritonavir on CYP 2D6 is inhibition, because ritonavir is also a CYP 2D6 inhibitor. The in vivo net effect of tipranavir with ritonavir on CYP 1A2, CYP 2C9 and CYP 2C19, indicates, through a preliminary study, an inducing potential of tipranavir with ritonavir on CYP1A2 and, to a lesser extent, on CYP2C9 and P-gp after several days of treatment. Data are not available to indicate whether tipranavir inhibits or induces glucuronosyl transferases.



In vitro studies show that tipranavir is a substrate and also an inhibitor of Pgp.



It is difficult to predict the net effect of APTIVUS co-administered with low dose ritonavir on oral bioavailability and plasma concentrations of agents that are dual substrates of CYP3A and Pgp. The net effect will vary depending on the relative affinity of the co-administered substance for CYP3A and Pgp, and the extent of intestinal first-pass metabolism/efflux.



Co-administration of APTIVUS and agents that induce CYP3A and/or Pgp may decrease tipranavir concentrations and reduce its therapeutic effect (see list and details of considered agents, below). Co-administration of APTIVUS and medicinal products that inhibit Pgp may increase tipranavir plasma concentrations.



Known and theoretical interactions with selected antiretrovirals and non-antiretroviral medicinal products are listed in the table below.



Interaction table



Interactions between APTIVUS and co-administered medicinal products are listed in the table below (increase is indicated as “↑”, decrease as “



Unless otherwise stated, studies detailed below have been performed with the recommended dosage of APTIVUS/r (i.e. 500/200 mg BID). However, some PK interaction studies were not performed with this recommended dosage. Nevertheless, the results of many of these interaction studies can be extrapolated to the recommended dosage since the doses used (eg. TPV/r 500/100 mg, TPV/r 750/200 mg) represented extremes of hepatic enzyme induction and inhibition and bracketed the recommended dosage of APTIVUS/r.

































































































Drugs by therapeutic area




Interaction Geometric mean change (%)




Recommendations concerning co-administration




Anti-infectives


  


Antiretrovirals


  


Nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs)


  


Since there is no significant impact of nucleoside and nucleotide analogues on the P450 enzyme system no dosage adjustment of APTIVUS is required when co-administered with these agents.


  


Abacavir 300 mg BID



(TPV/r 750/100 mg BID)




Abacavir Cmax



Abacavir AUC



The clinical relevance of this reduction has not been established, but may decrease the efficacy of abacavir.



Mechanism unknown.




The concomitant use of APTIVUS, co-administered with low dose ritonavir, with abacavir is not recommended unless there are no other available NRTIs suitable for patient management. In such cases no dosage adjustment of abacavir can be recommended (see section 4.4).




Didanosine 200 mg BID,



(TPV/r 250/200 mg BID)



(TPV/r 750/100 mg BID)




Didanosine Cmax



Didanosine AUC



Didanosine Cmax



Didanosine AUC ↔



The clinical relevance of this reduction in didanosine concentrations has not been established.



Mechanism unknown.




Dosing of enteric-coated didanosine and APTIVUS soft capsules, co-administered with low dose ritonavir, should be separated by at least 2 hours to avoid formulation incompatibility.




Lamivudine 150 mg BID



(TPV/r 750/100 mg BID)




No clinically significant interaction is observed.




No dosage adjustment necessary.




Stavudine



40 mg BID > 60 kg



30 mg BID < 60 kg



(TPV/r 750/100 mg BID)




No clinically significant interaction is observed.




No dosage adjustment necessary.




Zidovudine 300 mg BID



(TPV/r 750/100 mg BID)




Zidovudine Cmax



Zidovudine AUC



The clinical relevance of this reduction has not been established, but may decrease the efficacy of zidovudine.



Mechanism unknown.




The concomitant use of APTIVUS, co-administered with low dose ritonavir with zidovudine is not recommended unless there are no other available NRTIs suitable for patient management. In such cases no dosage adjustment of zidovudine can be recommended (see section 4.4).




Tenofovir 300 mg QD



(TPV/r 750/200 mg BID)




No clinically significant interaction is observed.




No dosage adjustment necessary.




Non-nucleoside reverse transcriptase inhibitors (NNRTIs)


  


Efavirenz 600 mg QD




No clinically significant interaction is observed.




No dosage adjustment necessary.




Nevirapine



No interaction study performed




The limited data available from a phase IIa study in HIV-infected patients suggest that no significant interaction is expected between nevirapine and TPV/r. Moreover a study with TPV/r and another NNRTI (efavirenz) did not show any clinically relevant interaction (see above).




No dosage adjustment necessary.




Protease inhibitors (PIs)


  


According to current treatment guidelines, dual therapy with protease inhibitors is generally not recommended


  


Amprenavir/ritonavir 600/100 mg BID




Amprenavir Cmax



Amprenavir AUC



Amprenavir Cmin



The clinical relevance of this reduction in amprenavir concentrations has not been established.



Mechanism unknown.




The concomitant use of APTIVUS, co-administered with low dose ritonavir, with amprenavir/ritonavir is not recommended.



If the combination is nevertheless considered necessary, a monitoring of the plasma levels of amprenavir is strongly encouraged (see section 4.4).




Atazanavir/ritonavir 300/100 mg QD



(TPV/r 500/100 mg BID)




Atazanavir Cmax



Atazanavir AUC



Atazanavir Cmin



Mechanism unknown.



Tipranavir Cmax ↑ 8%



Tipranavir AUC ↑ 20%



Tipranavir Cmin ↑ 75%



Inhibition of CYP 3A4 by atazanavir/ritonavir and induction by tipranavir/r.




The concomitant use of APTIVUS, co-administered with low dose ritonavir, with atazanavir/ritonavir is not recommended.



If the co-administration is nevertheless considered necessary, a close monitoring of the safety of tipranavir and a monitoring of plasma concentrations of atazanavir are strongly encouraged (see section 4.4).




Lopinavir/ritonavir 400/100 mg BID




Lopinavir Cmax



Lopinavir AUC



Lopinavir Cmin



The clinical relevance of this reduction in lopinavir concentrations has not been established.



Mechanism unknown.




The concomitant use of APTIVUS, co-administered with low dose ritonavir, with lopinavir/ritonavir is not recommended.



If the combination is nevertheless considered necessary, a monitoring of the plasma levels of lopinavir is strongly encouraged (see section 4.4).




Saquinavir/ritonavir 600/100 mg QD




Saquinavir Cmax



Saquinavir AUC



Saquinavir Cmin



The clinical relevance of this reduction in saquinavir concentrations has not been established.



Mechanism unknown.




The concomitant use of APTIVUS, co-administered with low dose ritonavir, with saquinavir/ritonavir is not recommended.



If the combination is nevertheless considered necessary, a monitoring of the plasma levels of saquinavir is strongly encouraged (see section 4.4).




Protease inhibitors other than those listed above




No data are currently available on interactions of tipranavir, co-administered with low dose ritonavir, with protease inhibitors other than those listed above.




Combination with APTIVUS, co-administered with low dose ritonavir, is not recommended (see section 4.4)




Fusion inhibitors


  


Enfuvirtide



No interaction study performed




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. No information is available for the parameters AUC and Cmax.



A pharmacokinetic interaction is mechanistically unexpected and the interaction has not been confirmed in a controlled interaction study.




The clinical impact of the observed data, especially regarding the tipranavir with ritonavir safety profile, remains unknown. Nevertheless, the clinical data available from the RESIST trials did not suggest any significant alteration of the tipranavir with ritonavir safety profile when combined with enfuvirtide as compared to patients treated with tipranavir with ritonavir without enfuvirtide.




Integrase strand transfer inhibitors


  


Raltegravir 400 mg BID




Raltegravir Cmax ↔



Raltegravir AUC 0-12↔



Raltegravir C12:



Despite an almost half reduction of C12, previous clinical studies with this combination did not evidence an impaired outcome.



The mechanism of action is thought to be induction of glucuronosyltransferase by tipranavir/r.




No particular dose adjustment is recommended.




Antifungals


  


Fluconazole 200 mg QD (Day 1) then 100 mg QD




Fluconazole ↔



Tipranavir Cmax ↑ 32%



Tipranavir AUC ↑ 50%



Tipranavir Cmin ↑ 69%



Mechanism unknown




No dosage adjustments are recommended. Fluconazole doses >200 mg/day are not recommended.




Itraconazole



Ketoconazole



No interaction study performed




Based on theoretical considerations tipranavir, co-administered with low dose ritonavir, is expected to increase itraconazole or ketoconazole concentrations.



Based on theoretical considerations, tipranavir or ritonavir concentrations might increase upon co-administration with itraconazole or ketoconazole.




Itraconazole or ketoconazole should be used with caution (doses >200 mg/day are not recommended).




Voriconazole



No interaction study performed




Due to multiple CYP isoenzyme systems involved in voriconazole metabolism, it is difficult to predict the interaction with tipranavir, co-administered with low-dose ritonavir.




Based on the known interaction of voriconazole with low dose ritonavir (see voriconazole SPC) the co-administration of tipranavir/r and voriconazole should be avoided, unless an assessment of the benefit/risk to the patient justifies the use of voriconazole.




Anti-gouts


  


Colchicine




Based on theoretical considerations, colchicine concentrations may increase upon co-administration with tipranavir and low dose ritonavir.



Colchicine is a substrate of CYP3A4 and P-gp (an intestinal efflux transporter).




The administration of APTIVUS with low dose ritonavir and colchicine is not recommended.




Antibiotics


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