 What
is Aptivus
•
Aptivus is an anti-HIV medication. It is in a category of
HIV medicines called protease
inhibitors (PIs). Aptivus prevents cells infected by HIV from producing new
virus. This reduces the amount of virus in your body.
•
Aptivus must be used in combination with Norvir
(ritonavir) and at least two other anti-HIV drugs.
•
Aptivus, manufactured by Boehringer Ingelheim, was approved
for the treatment of HIV by the U.S. Food and Drug Administration (FDA) in June
2005. Aptivus/ritonavir is only approved for HIV-infected people who have tried
and failed other anti-HIV drug regimens (including those containing protease inhibitors)
in the past. It is not approved for HIV-infected people starting anti-HIV treatment,
or a protease inhibitor, for the first time (unless they were infected with a
strain of HIV resistant to multiple protease inhibitors).
What
is known about Aptivus
•
Aptivus has a different structure than other protease inhibitors and is active
against strains of the virus that are resistant to the other protease inhibitors
that are currently available.
• The
correct dose of Aptivus is 500mg twice a day (two 250mg capsules twice daily)
. To help keep levels of Aptivus high in the blood, which is very important for
the drug to be effective, it is necessary to combine Aptivus with low doses (200mg
twice daily) of the protease inhibitor Norvir (ritonavir).
• Aptivus/ritonavir should be taken with
food, preferably a complete nutritious meal, to ensure proper absorption of the
drug into the bloodstream.
• Aptivus
is recommended by the U.S. Department of Health and Human Services (DHHS) for
HIV-positive people who have tried and failed other protease inhibitors in the
past. It is not recommended by the DHHS for patients who are new to anti-HIV treatment
or starting a protease inhibitor for the first time.
•
Clinical trials have demonstrated that Aptivus is an effective option for patients
who are not likely to respond to older protease inhibitors, especially when it
is combined with other anti-HIV medications that a patient's virus is still at
least partially sensitive to.
• Aptivus/ritonavir
works best when it is combined with anti-HIV drugs that the virus is still sensitive
to. However, this can be challenging for HIV-positive people who have tried and
failed several anti-HIV drug regimens in the past. Drug resistance tests, such
as genotypic assays and phenotypic assays, can be very useful in figuring out
which anti-HIV drugs the virus is still likely to respond to. Drug-resistance
tests are recommended when putting together a regimen that contains Aptivus/ritonavir.
In clinical trials, Aptivus/ritonavir worked best when it was combined with Fuzeon
(enfuvirtide; T-20), particularly in people who had not been on Fuzeon in
the past.
Drug
and Food Interactions
•
Absorption of tipranavir increases when taken with a high-fat
meal. Antacids reduce absorption of tipranavir, requiring timing adjustments of
antacid use. •
Tipranavir/ritonavir at the recommended dosage is an inhibitor
of CYP 3A and may thus increase plasma concentrations of agents that are primarily
metabolized by this enzyme. Coadministration of tipranavir/ritonavir with drugs
that are highly dependent on CYP 3A for clearance are contraindicated. These drugs
include amiodarone, bepridil, flecainide, propafenone, quinidine, rifampin, dihydroergotamine,
ergonovine, ergotamine, methylergonamine, cisapride, St. John's wort, lovastatin,
simvastatin, pimozide, midazolam, and triazolam. •
When used with other antiretrovirals in vitro, tipranavir
was shown to be additive to antagonistic with other PIs, generally additive with
non nucleoside reverse transcriptase inhibitors (NNRTIs) and nucleoside reverse
transcriptase inhibitors (NRTIs), and synergistic with the fusion inhibitor enfuvirtide
(Fuzeon). •
Patients should tell their doctor about any other medications
they are taking, including prescription, nonprescription (over-the-counter), or
herbal medications. It is particularly important for doctor s to know if a patient
is allergic to sulfa drugs, because people with sulfa allergies may be at a higher
risk of having an allergic reaction to tipranavir.
Potential
Adverse Events and Side Effects
WARNING
APTIVUS
CO-ADMINISTERED WITH 200 MG RITONAVIR HAS BEEN ASSOCIATED WITH REPORTS OF BOTH
FATAL AND NON-FATAL INTRACRANIAL HEMORRHAGE. (SEE WARNINGS)APTIVUS
CO-ADMINISTERED WITH 200 MG RITONAVIR HAS BEEN ASSOCIATED WITH REPORTS OF CLINICAL
HEPATITIS AND HEPATIC DECOMPENSATION INCLUDING SOME FATALITIES. EXTRA VIGILANCE
IS WARRANTED IN PATIENTS WITH CHRONIC HEPATITIS B OR HEPATITIS CO-INFECTION, AS
THESE PATIENTS HAVE AN INCREASED RISK OF HEPATOTOXICITY. (SEE WARNINGS) |
•
Like all anti-HIV drugs, tipranavir may cause some unwanted
side effects. The most common side effects are diarrhea, nausea, fatigue, headache,
and vomiting. •
Adverse effects leading to discontinuation of treatment
were reported in 7.8 percent of individuals receiving tipranavir. Other adverse
effects include rash, elevated lipid levels, fat redistribution, and immune reconstitution
syndrome. Women using estrogens may have an increased risk of non serious
rash. Individuals with hemophilia may have increased risk of bleeding. •
Tipranavir
in combination with ritonavir has been associated clinical hepatitis (liver inflammation)
and hepatic decompensation, including some fatalities. Extra vigilance is warranted
in individuals with advanced HIV disease or those with chronic hepatitis B or
hepatitis C co-infection [with HIV] as these individuals have an increased risk
of hepatotoxicity. Symptoms of hepatitis include fatigue, malaise, anorexia, nausea,
jaundice, bilirubinemia, acholic stools, liver tenderness, or hepatomegaly.
Dosing
Information
•
Tipranavir is available in 250 mg soft gel capsules and is
taken with ritonavir. The recommended dosing regimen is 500 mg tipranavir taken
with 200 mg ritonavir twice daily.
|
