Tipranavir
Tipranavir is an antiretroviral protease inhibitor used, always with ritonavir, to treat HIV-1 infection in treatment-experienced adults and children who have virus resistant to multiple other protease inhibitors.
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
Tipranavir (Aptivus), on the U.S. market since about 2005, is a specialist HIV protease inhibitor (it blocks protease, an enzyme HIV needs to make infectious copies of itself) for people whose HIV resists more than one other protease inhibitor, always taken with ritonavir and never alone. It tends to be harder on the stomach than newer HIV medicines, and diarrhea and nausea are what most people notice. Its boxed warning covers serious liver damage, more likely with hepatitis B or C, and bleeding inside the brain, so treat yellowing eyes, dark urine or a sudden severe headache as urgent. Expect regular liver blood tests.
Clinical pearls
- Take it with a meal alongside the ritonavir, and swallow the capsules whole without opening, crushing or chewing them.
- Simvastatin, lovastatin, rifampin, St. John's wort and amiodarone are off-limits, so every prescriber should know you take it.
- Skip high-dose vitamin E supplements, and flag any blood thinner or antiplatelet drug, because tipranavir can add to bleeding risk.
- Tipranavir contains a sulfonamide component, so mention any sulfa drug allergy before the first dose.
⚠️ FDA Boxed Warning — the FDA’s strongest safety alert ▾
Aptivus carries a serious boxed warning for two rare but life-threatening risks: liver damage and brain bleeding.
Serious liver disease — including liver failure and death — has occurred in people taking Aptivus with ritonavir. The risk is highest in people who also have chronic hepatitis B or hepatitis C. Watch for symptoms like yellowing of the skin or eyes, unusual fatigue, nausea, dark urine, or stomach pain, and report them to your doctor immediately.
Both fatal and non-fatal bleeding inside the brain (intracranial hemorrhage) have been reported. Seek emergency care right away if you experience a sudden severe headache, sudden weakness, vision changes, or confusion.
Patient information guide A plain-language walkthrough of Tipranavir, written from its FDA label.
What Tipranavir is used for
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Tipranavir is an antiretroviral medication used as part of combination HIV therapy in people whose virus has stopped responding to other treatments.
- Aptivus capsules are approved to treat HIV-1 infection in treatment-experienced adults whose virus is resistant to more than one protease inhibitor — always taken together with ritonavir and other HIV medications.
- Aptivus capsules are also approved for treatment-experienced pediatric patients weighing 36 kg or more with multi-protease-inhibitor-resistant HIV-1, again always combined with ritonavir.
- Aptivus is not recommended for treatment-naïve patients (people who have never taken HIV medications before).
- Resistance testing is strongly recommended before starting Aptivus, since the number of existing mutations in the virus affects how well the drug will work.
How Tipranavir works
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Tipranavir is a protease inhibitor. HIV uses an enzyme called protease to cut long chains of viral proteins into the pieces it needs to build new, mature virus particles. Tipranavir blocks this enzyme, so HIV can only produce immature, non-infectious copies of itself — slowing the spread of the virus through the body.
One reason tipranavir is valuable in treatment-experienced patients is its ability to remain active against HIV strains that have already developed resistance to other protease inhibitors. However, the number of existing mutations in the virus still affects how well it works, and cross-resistance with other protease inhibitors is possible.
Tipranavir dosage
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Aptivus is taken by mouth twice daily and must always be co-administered with ritonavir — taking it without ritonavir results in levels too low to suppress HIV. When Aptivus capsules are taken together with ritonavir tablets, they must be taken with a meal. Capsules must be swallowed whole and never opened or chewed.
- Aptivus is taken twice a day (roughly every 12 hours).
- Always take ritonavir at the same time as Aptivus — never skip the ritonavir.
- Children must be able to swallow capsules whole before Aptivus capsules are prescribed.
- Store unopened bottles of Aptivus capsules in the refrigerator.
Dosing details from the FDA-approved label
From the Tipranavir prescribing information (“Dosage and Administration”). Doses are set by your prescriber for your product, condition, kidney function and age — never change a dose on your own.
- Adults
- 500 mg (two 250 mg capsules) of APTIVUS co-administered with 200 mg of ritonavir, twice daily
- APTIVUS co-administered with ritonavir tablets must be taken with meals; capsules must be swallowed whole, not opened or chewed
- Pediatric patients weighing 36 kg or higher
- 500 mg (two 250 mg capsules) of APTIVUS co-administered with 200 mg of ritonavir, twice daily
- Children should be assessed for their ability to swallow capsules before prescribing; must be taken with meals when co-administered with ritonavir tablets
Read the label’s full dosing text
2 DOSAGE AND ADMINISTRATION Adults: 500 mg APTIVUS, co-administered with 200 mg ritonavir, twice daily ( 2.2 ) Pediatric patients (weighing 36 kg or higher): 500 mg APTIVUS, co-administered with 200 mg ritonavir twice daily. ( 2.2 ) APTIVUS taken with ritonavir tablets must be taken with meals ( 2.1 ) APTIVUS capsules must be swallowed whole and must not be opened or chewed ( 2.1 ) Children should be assessed for their ability to swallow capsules before prescribing APTIVUS capsules. ( 2.1 ) Store unopened bottles of APTIVUS capsules in the refrigerator. ( 16 ) 2.1 Dosage and Administration Overview APTIVUS must be co-administered with ritonavir to exert its therapeutic effect. Failure to correctly co-administer APTIVUS with ritonavir will result in plasma levels of tipranavir that will be insufficient to achieve the desired antiviral effect and will alter some drug interactions [see Warnings and Precautions (5.1) ] . Children should be assessed for their ability to swallow capsules before prescribing APTIVUS capsules [see Use in Specific Populations (8.4) ] . APTIVUS co-administered with ritonavir tablets must only be taken with meals [see Clinical Pharmacology (12.3) ] . APTIVUS is supplied as capsules. APTIVUS capsules must be swallowed whole and must not be opened or chewed. Due to the need for co-administration of APTIVUS with ritonavir, please refer to the ritonavir prescribing information. 2.2 Recommended Dosage in Adults and Pediatric Patients Weighing 36 kg or Higher The recommended dosage in adults and pediatric patients weighing 36 kg or higher is 500 mg (two 250 mg capsules) of APTIVUS co-administered with 200 mg of ritonavir, twice daily.
Read the full Dosage and Administration section on DailyMed →
Tipranavir side effects
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The most common side effects reported in clinical trials include:
Common side effects
- Diarrhea
- Nausea
- Vomiting
- Fever (pyrexia)
- Fatigue
- Headache
- Abdominal (stomach) pain
- Rash
- Elevated cholesterol and triglycerides (fats in the blood)
When to get medical help
- Call your doctor right away if you notice yellowing of the skin or eyes, dark urine, pale stools, stomach tenderness, or extreme tiredness — these can be signs of serious liver problems.
- Seek emergency help immediately for sudden severe headache, confusion, weakness on one side of the body, or any signs of bleeding in the brain (intracranial hemorrhage).
- Stop taking Aptivus and get medical help if you develop a severe skin rash, especially one with fever, joint pain, throat tightness, or skin peeling.
- Tell your doctor if you notice unusual bleeding or bruising, especially if you have hemophilia.
- Contact your doctor if you develop signs of high blood sugar such as increased thirst, frequent urination, or blurred vision.
- Let your doctor know if you experience new or worsening symptoms of infection after starting treatment — this could be immune reconstitution syndrome.
More serious reactions — including liver toxicity, brain bleeding, and severe rash with skin peeling or mucosal involvement — have also been reported and require immediate medical attention. Elevated liver enzymes were seen in a meaningful proportion of patients and increased over time, so regular liver monitoring is essential.
Tipranavir warnings and precautions
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- Liver toxicity: Serious liver inflammation and failure, including deaths, have occurred. Risk is about doubled in people with hepatitis B or C co-infection. Liver function must be tested before and regularly during treatment. Stop Aptivus and seek care immediately if liver warning signs appear.
- Brain bleeding (intracranial hemorrhage): Both fatal and non-fatal cases have been reported. No specific risk factor pattern has been identified, so all patients should be alert to sudden severe headache, weakness, or confusion.
- Bleeding risk: Tipranavir can affect platelet function (blood clotting). Use with extreme caution in people who take blood thinners, antiplatelet drugs, or high-dose vitamin E, or who have hemophilia.
- Severe rash: Discontinue Aptivus immediately if a serious skin reaction develops, particularly one involving fever, joint pain, or skin breakdown.
- Cholesterol and triglycerides: Large increases in blood fats have been reported; these should be tested before and during treatment.
- Blood sugar: New or worsening diabetes and high blood sugar have been reported with protease inhibitor therapy.
- Immune reconstitution syndrome: When the immune system begins recovering on HIV therapy, it can over-react to hidden infections, causing new inflammation that needs evaluation.
Tipranavir interactions
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Aptivus/ritonavir affects and is affected by a wide range of medications — always review your full medication list with your doctor or pharmacist before starting.
- Completely contraindicated (must not combine): Amiodarone, quinidine, flecainide, propafenone, bepridil (heart rhythm drugs); lovastatin, simvastatin (cholesterol drugs); rifampin (antibiotic); ergot medications; cisapride; pimozide; lurasidone; oral midazolam or triazolam (sedatives); sildenafil (Revatio, used for pulmonary arterial hypertension); alfuzosin; St. John's Wort.
- Other HIV drugs: Etravirine should not be combined with Aptivus/ritonavir (levels drop too much). Other protease inhibitors combined with Aptivus/ritonavir are also not recommended. Dose adjustments or monitoring may be needed with abacavir, zidovudine, didanosine, raltegravir, and dolutegravir.
- Antifungals: Fluconazole raises tipranavir levels — doses above 200 mg/day are not recommended. Itraconazole and ketoconazole should be used with caution at no more than 200 mg/day.
- Antibiotics: Clarithromycin raises both tipranavir and clarithromycin levels; dose adjustments of clarithromycin may be needed in kidney impairment.
- Blood thinners and antiplatelet agents: Use with caution — Aptivus can affect clotting and increase bleeding risk.
- High-dose vitamin E supplements: May significantly increase bleeding risk — avoid.
Interactions listed in the FDA-approved label
From the Tipranavir prescribing information (“Drug Interactions”): what the manufacturer studied or reported to the FDA.
- Enfuvirtide: Tipranavir trough concentrations were approximately 45% higher in patients co-administered enfuvirtide in the Phase 3 trials; the mechanism is not known. Dose adjustments are not recommended.
- Etravirine: APTIVUS/ritonavir may cause a significant decrease in etravirine plasma concentrations and loss of its therapeutic effect. Etravirine and APTIVUS/ritonavir should not be coadministered.
- Rilpivirine: Not studied; concomitant use may increase rilpivirine plasma concentrations (inhibition of CYP3A enzymes); rilpivirine is not expected to affect Aptivus/ritonavir concentrations.
- Abacavir: Abacavir AUC decreased by approximately 40%. Clinical relevance not established; dose adjustment of abacavir cannot be recommended at this time.
- Didanosine (EC): Didanosine levels are decreased. Clinical relevance not established; for optimal absorption, separate didanosine from APTIVUS/ritonavir dosing by at least 2 hours.
- Zidovudine: Zidovudine AUC decreased by approximately 35%; ZDV glucuronide concentrations were unaltered. Clinical relevance not established; dose adjustment of zidovudine cannot be recommended at this time.
- Protease inhibitors (fosamprenavir, lopinavir, saquinavir; with 200 mg ritonavir): Decreased concentrations of amprenavir, lopinavir and saquinavir. Combining a protease inhibitor with APTIVUS/ritonavir is not recommended.
- Raltegravir: Raltegravir concentrations are decreased. No dose adjustment is needed for the 400 mg twice daily regimen; for all other regimens, refer to raltegravir prescribing information.
- Dolutegravir: Dolutegravir concentrations are decreased. Refer to dolutegravir prescribing information for dosage recommendations.
- Fluconazole: Fluconazole increases tipranavir concentrations; fluconazole concentrations are unchanged. Dose adjustments are not needed; fluconazole doses >200 mg/day are not recommended.
Read the label’s full interactions text
7 DRUG INTERACTIONS Co-administration of APTIVUS can alter the concentrations of other drugs and other drugs may alter the concentration of tipranavir. The potential for drug-drug interactions must be considered prior to and during therapy. ( 4 , 5.4 , 7 ) 7.1 Potential for APTIVUS/ritonavir to Affect Other Drugs APTIVUS co-administered with ritonavir at the recommended dose is a net inhibitor of CYP3A and may increase plasma concentrations of agents that are primarily metabolized by CYP3A. Thus, co-administration of APTIVUS/ritonavir with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events is contraindicated [see Contraindications (4) ] . Co-administration with other CYP3A substrates may require a dose adjustment or additional monitoring [see Drug Interactions (7) ] . Clinically significant drug-drug interactions of APTIVUS co-administered with ritonavir are summarized in Table 4 below. A phenotypic cocktail study was conducted with 16 healthy volunteers to quantify the influence of 10 days of APTIVUS/ritonavir capsule administration on the activity of hepatic CYP1A2 (caffeine), 2C9 (warfarin), 2C19 (omeprazole), 2D6 (dextromethorphan) and the activity of intestinal and hepatic CYP3A4/5 (midazolam) and P-glycoprotein (P-gp) (digoxin). This study determined the first-dose and steady-state effects of 500 mg of APTIVUS co-administered with 200 mg of ritonavir twice daily in capsule form. There was no net effect on CYP2C9 or hepatic P-gp at first dose or steady state. There was no net effect after first dose on CYP1A2, but there was moderate induction at steady state. There was modest inhibition of CYP2C19 at the first dose, but there was marked induction at steady state. Potent inhibition of CYP2D6 and both hepatic and intestinal CYP3A4/5 activities were observed after first dose and steady state.
Excerpted — the section continues on the label. Read the full Drug Interactions section on DailyMed →
Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.
Before taking Tipranavir
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- Tell your doctor if you have any liver disease, hepatitis B, or hepatitis C — you are at higher risk for liver damage and will need close monitoring.
- Do not take Aptivus if you have moderate or severe liver impairment (Child-Pugh Class B or C).
- Disclose a sulfa (sulfonamide) allergy — tipranavir contains a sulfonamide component and cross-sensitivity is possible.
- Tell your doctor if you have hemophilia — increased bleeding has been reported in hemophilia patients on protease inhibitors.
- Share your complete medication list, including supplements and herbal products — Aptivus has many significant interactions.
- Pregnancy: A pregnancy exposure registry exists (call 1-800-258-4263). Discuss risks carefully with your doctor; available data are very limited.
- Children must be confirmed able to swallow capsules whole before Aptivus capsules are prescribed; pediatric use is supported for patients weighing 36 kg or more who are treatment-experienced.
- Tell your doctor if you are at elevated risk for bleeding or take anticoagulants or antiplatelet medications.
Tipranavir overdose
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There is no known antidote for a tipranavir overdose. If an overdose is suspected, treatment focuses on supportive care — monitoring vital signs and clinical status closely. If the overdose was recent, a healthcare provider may try to reduce further absorption of the drug.
Because tipranavir binds very strongly to proteins in the blood (more than 99.9%), dialysis is not expected to remove a meaningful amount of the drug from the body.
What Tipranavir does in the body
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Tipranavir works by blocking HIV's protease enzyme, preventing the virus from producing mature, infectious particles. In clinical studies, there was a clear relationship between the drug's concentration relative to the virus's sensitivity (called the Inhibitory Quotient) and how much the viral load dropped after 48 weeks of treatment — higher drug-to-virus ratios were associated with better responses.
At standard doses, Aptivus/ritonavir produced only a small effect on a heart electrical measure called the QTc interval (the time it takes the heart to recharge between beats), which was not considered clinically significant.
How your body processes Tipranavir
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Tipranavir is taken by mouth but is absorbed to a limited extent on its own — co-administration with ritonavir is essential because ritonavir dramatically increases tipranavir blood levels (about 29-fold) by blocking the liver enzyme (CYP3A) that would otherwise break tipranavir down. Steady-state blood levels are typically reached within 7–10 days of twice-daily dosing, and tipranavir has a half-life (the time for levels to fall by half) of roughly 5–6 hours.
Once in the bloodstream, tipranavir binds very tightly to blood proteins (over 99.9%). In the presence of ritonavir, very little tipranavir is actually metabolized — more than 98% circulates unchanged. The drug is eliminated mainly through the feces, with very little appearing in urine.
How to store Tipranavir
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APTIVUS capsules should be stored in a refrigerator 2°C-8°C (36°F-46°F) prior to opening the bottle. stored at 20°C-25°C (68°F-77°F); excursions permitted to 15°C-30°C (59°F-86°F ) and must be used within 60 days after first opening of the bottle.
Written from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
Supplements & herbs that interact with Tipranavir
212 supplements and herbal products have documented interactions with Tipranavir in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 3
- Moderate · 165
- Minor · 44
Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.
Tipranavir: pharmacist answers to common questions
Quick, plain-English answers to the questions patients ask most about Tipranavir — the kind of thing our pharmacy team would talk through with you at the counter.
Why do I have to take ritonavir with Aptivus? Can I skip it if I feel fine?
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Does it matter if I take Aptivus with food or on an empty stomach?
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What liver warning signs should I watch out for?
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I've heard Aptivus can cause brain bleeding — how serious is that, and how would I know?
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Are there common medications I shouldn't take with Aptivus?
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I'm pregnant or thinking about getting pregnant. Is Aptivus safe?
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Is Tipranavir available over the counter?
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When was Tipranavir first available?
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Answers drafted from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
More about Tipranavir on HelloPharmacist
Tipranavir forms and strengths (how it comes)
Tipranavir is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Capsule
How this form is used
- Aptivus capsules are used to treat HIV-1 infection in treatment-experienced adults whose virus is resistant to more than one protease inhibitor, always taken together with ritonavir.
- Aptivus capsules are used in pediatric patients weighing 36 kg or more with multi-protease-inhibitor-resistant HIV-1, co-administered with ritonavir.
- Aptivus capsules are not recommended for people who have never been on HIV therapy (treatment-naïve patients).
- Aptivus capsules must be swallowed whole — do not open, break, or chew them.
- Aptivus capsules taken with ritonavir tablets must be taken with a meal.
- For Aptivus capsules taken with ritonavir capsules, no strict food requirement was observed, but follow your prescriber's specific instructions.
- Store unopened bottles of Aptivus capsules in the refrigerator; children should be confirmed able to swallow capsules whole before this form is prescribed.
Tipranavir on the U.S. market: products, makers and brands
How Tipranavir appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
The FDA lists Tipranavir products, mostly as capsule; the earliest marketing or approval year on record is 2005. Brand names on the directory include Aptivus; the rest are generics.
Also listed with the FDA, not a patient dose form: Powder (1) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.
Tipranavir side effects reported to the FDA (FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Tipranavir — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Tipranavir in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
Tipranavir FDA approval history
How Tipranavir went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
Tipranavir recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
The FDA’s enforcement reports list no Tipranavir recalls since July 2021.
✅No Tipranavir recalls on record since July 2021Source: FDA enforcement (recall) reports, via openFDA; our copy was last updated Sep 24, 2026.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 190548 2 dose forms · 2 strengths
-
Dose form (SCDF) Oral Capsule RxCUI 577211In current FDA listingsClinical drug / strength (SCD) 250 MGRxCUI 577212 -
Dose form (SCDF) Oral Solution RxCUI 802320No current FDA listingClinical drug / strength (SCD) 100 MG/MLRxCUI 802321
Look up RxCUI 190548 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
Tipranavir supply and shortage status
Whether Tipranavir is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
Tipranavir brand names
Tipranavir is sold under one brand name in the FDA directory — Aptivus. A brand and its generic contain the same active ingredient; the brand name belongs to one company's product.
Tipranavir drug class (RxNorm)
Tipranavir belongs to the Protease Inhibitor class.
Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.
Sources for this Tipranavir page
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How this page is built
HelloPharmacist combines public FDA and NLM records and does not author the underlying clinical facts. The plain-language sections are written with AI from the FDA-approved label text and reviewed by our pharmacy team before publication. Boehringer Ingelheim Pharmaceuticals, Inc. is the representative DailyMed label linked for verification and dates. This is general education, not medical advice: always talk to your doctor or pharmacist about your own medicines. How we build and review drug pages →