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Brand Name: Aptivus
Common Name: tipranavir (TPV)
Class: HIV protease inhibitor
Standard Dose: Two 250 mg capsules with two 100 mg capsules of Norvir, both twice daily. Take with food. Take missed dose as soon as possible but do not double up on your next dose.
AWP: $1,072.80 / month for Aptivus only
Manufacturer contact: Boehringer-Ingelheim,
www.aptivus.com, 1 (800) 274–8651
AIDSInfo:1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
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| Potential side effects and toxicity: |
Mostly gastrointestinal-related: mild diarrhea, nausea, vomiting and fatigue. In clinical trials symptoms have been managed by having a light snack with the drug. Other side effects include headaches, dry mouth, rash, and dizziness. Recent reports of liver problems in people taking it who also have hepatitis. Be sure to know your hepatitis status if you are about to or are taking this drug! During clinical studies, bleeding in the brain occurred in people taking Aptivus/Norvir who had medical conditions or were receiving other medications that may have increased the risk of this. Use with caution by people who may be at risk of increased bleeding from trauma, surgery or other medical conditions, or who are receiving medications known to increase the risk of bleeding such as antiplatelet drugs or anticoagulants. Aptivus has a “sulfa” component to it, so it should be used cautiously in patients with “sulfa” allergies.
As seen with other protease inhibitors, there can be increased levels of cholesterol and triglycerides (except possibly unboosted Reyataz) which may be associated with an increased risk of heart disease. Other possible side effects are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts and sometimes the upper back), onset of new cases or worsening of diabetes (see your doctor promptly), and increased bleeding in hemophiliacs. See Norvir for more details on potential side effects.
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| Potential drug interactions: |
Aptivus/Norvir interacts with many other drugs, so it is important to tell your healthcare professional of the medications you are taking. See the manufacturer package insert. Do not take with Tambocor, Rythmol, Cordarone, quinidine, Versed, Halcion, Rifadin, Orap, ergot derivatives (such as Cafergot, Wigraine and Methergine, D.H.E. 45), or the herb St. John’s wort. Do not use Zocor or Mevacor; lipid-lowering alternatives are Lipitor, Lescol, and Pravachol, but they should be used with caution due to potential for liver toxicity. Increased levels of the inhaled and nasal sprays with fluticasone (found in Advair, Flonase, Flovent), can occur with Aptivus/Norvir and therefore should be used with caution.
This drug is metabolized by the liver (same as most of the other protease inhibitors). Should not be given with other protease inhibitors because it greatly lowers their blood levels.
Cialis, Levitra, and Viagra levels are increased; doses should not exceed 10 mg Cialis per 72 hours, 2.5 mg Levitra per 72 hours, or 25 mg Viagra per 48 hours.
Norvir may decrease levels of methadone, but withdrawal rarely occurs. Methadone doses may need to be increased. A lower dose of Desyrel is recommended. The blood pressure medications called calcium channel blockers such as Norvasc, Procardia, and others should be monitored for side effects. Monitoring may be required when taking Coumadin or immunosuppressants. Tegretol, Dilantin or phenobarbital may decrease Aptivus, so alternate seizure medications should be used and monitoring of Aptivus drug levels is recommended. Caution must be exercised when using Sporanax or Diflucan (fluconazole). Rifabutin requires a reduced dose. The Norvir and Aptivus capsules contain alcohol (but should not be enough to trigger relapse), so be cautious with Antabuse or Flagyl, which can cause flushing, vomiting, etc. |
| Tips: |
Take with food to minimize stomach problems. Do not take at the same time as antacids. This drug does its best when used with T-20 (enfuvirtide, Fuzeon). Unlike adding 1+1 = 2, with Aptivus and Fuzeon, 1+1 = 3! This drug is only for experienced patients or those with resistance to multiple protease inhibitors. Tipranavir is expected to do less well for people with combinations of certain protease-related mutations. See package insert or www.aptivus.com for a list of mutations. Although tipranavir has to be taken with 200 mg twice daily of Norvir, it actually lowers the blood levels of Norvir. So, you may not see as much of the GI side effects as you might expect. The capsules should be refrigerated prior to opening. Once the bottle is opened, Aptivus can be stored at temperatures less than 77°F and must be used within 60 days.—Patrick G. Clay, Pharm.D.
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| Doctor |
| Tipranavir (TPV) is indicated only for use in patients with drug-resistant HIV. It is not recommended for use in treatment-naïve subjects. The Resist Trials documented the superiority of TPV-based regimens compared to optimized background regimens using other boosted protease inhibitors in patients with no more than two PI-resistance mutations at codons 33, 82, 84, or 90. Benefit was enhanced when Fuzeon was included for Fuzeon-naïve patients. It is unclear how generalizable the data would be for a patient with greater numbers of key PI-related mutations. Problems with TPV include the requirement of 200 mg of ritonavir twice a day for boosting, a consistent negative effect on the levels of other protease inhibitors if used concurrently as well as a modest negative interteraction with AZT and abacavir, risk for significant liver damage, possible increased risk for intracranial hemorrhage, possible cross-sensitivity for persons with a sulfa allergy, and high cost. The availability of darunavir and the looming availability of TMC-125, MK-0518, and maraviroc will likely contribute to minimal interest in use of TPV.—Keith Henry, MD |
| Activist |
| This drug was a welcome option for people in salvage situations when it first hit the market. It received approval from the FDA specifically for its use in people who have significant resistance to other PIs. Unfortunately, it has to be taken with a hefty dose of ritonavir (two 100 mg capsules) twice a day, and like many other HIV drugs, it has its share of side effects, including diarrhea, high cholesterol and triglycerides, and a potential for moderate to severe liver toxicity. Anyone taking this drug should have their liver function monitored regularly. A key point to remember when considering this drug is to make sure that your doc does resistance testing on you before starting treatment. Aptivus works best when there are other active drugs in the background. Another caveat of this drug is that it tends to pick fights with some other drugs when they are used together, so a careful review of known drug-drug interactions associated with Aptivus before starting is critical.—Cathy Olufs |
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