Aptivus (Tipranavir) Oral: Uses, Side Effects, Dosages

What Is Aptivus?

Aptivus (tipranavir) is in a class of medications called protease inhibitors. It is used to treat human immunodeficiency virus, commonly known as HIV.

Aptivus is an antiviral drug. It can prevent the virus from replicating by blocking an enzyme called protease. Without the protease enzyme, the virus can no longer break down large viral proteins into smaller pieces required for the virus to grow and multiply (replicate). As a result, it reduces the amount of HIV in your body.

When combined with another anti-HIV medication called Norvir (ritonavir), tipranavir helps prevent the disease from worsening, reduces possible side effects, and keeps your immune system safe.

You can get Aptivus by prescription. It is available as a capsule taken by mouth.

What Is Aptivus Used For?

The U.S. Food and Drug Administration (FDA) approved Aptivus to treat HIV in treatment-experienced people (who have previously taken another antiretroviral therapy) and are infected with HIV-1 strains resistant to more than one protease inhibitor.

It is used in combination with another antiretroviral therapy called ritonavir.

How to Take Aptivus

Take this medication as instructed by your healthcare provider.

Aptivus is a capsule that must be swallowed whole by mouth. Do not open, chew, or crush the capsules, which can prevent the medication from working.

Typically, you will take two 250-milligram capsules in the morning, followed by two more capsules 12 hours later. This adds up to 1000 milligrams per day.

Your healthcare provider will prescribe another HIV medication called ritonavir with tipranavir. You should take your ritonavir tablets with meals, although the capsule and liquid formulations can be taken without regard to food in adults. However, it is recommended that children always take their dose with food. Taking your medications with food can also help prevent nausea.

Storage

When you first get Aptivus, store the container in the fridge. After opening it, store the medication at room temperature (68 F to 77 F) for 60 days. Write the expiration date on the container. Properly dispose of any remaining medication in open containers after 60 days.

You can dispose of unused or expired medication by dropping it off at a drug take-back site, location, or program in your area or following the disposal instructions on the medication’s package insert. If no other options are available, you can trash medications using the following steps:

• Mix (do not crush) the capsules with an unappealing substance, like dirt, cat litter, or used coffee grounds.
• Put the mixture in a sealed plastic bag or container.
• Throw it away in a home trash container.
• Remove personal information from the prescription label on empty bottles or packaging before throwing them in the trash.

You can talk to your pharmacist for more information on the safe disposal of medications.

As always, ensure your medication is stored securely, out of reach of children and pets. Contact your pharmacy or healthcare provider to request a refill if you need more medication.

Off-Label Uses

Currently, Aptivus does not have any off-label uses.

What Are the Side Effects of Aptivus?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or a healthcare provider. You may report side effects to the FDA at www.fda.gov/medwatch or 800-FDA-1088.

Common Side Effects

The side effects commonly reported while taking Aptivus include:

• Headache
• Fatigue
• Diarrhea
• Upset stomach
• Abdominal pain
• Fever
• Rash

Severe Side Effects

Contact your healthcare provider immediately if you are experiencing any severe side effects. Call 911 if you feel your life is at risk or need medical assistance. Rare but serious side effects may include:

• Liver problems: This medication has a boxed warning (the FDA’s highest safety warning) about liver toxicity risks. Signs may include dark urine or yellowing of the skin/eyes (jaundice).
• Intracranial hemorrhage (bleeding within the skull), mostly in people with other medical conditions: This medication has a boxed warning about the increased risk of intracranial hemorrhage. Symptoms include a worsening headache, vomiting, dizziness, loss of consciousness, slurred speech, and loss of movement on one side of the body.
• An allergic reaction: Symptoms may include hives, itching, or closing of the throat.
• Nervous system disorders, such as peripheral neuropathy: Symptoms may include weakness, numbness, and pain in the hands and feet.
• Low blood platelet count (thrombocytopenia): Symptoms may include excessive bruising or prolonged bleeding from cuts.
• Insomnia (trouble sleeping)
• Metabolic disorders, such as diabetes, hyperglycemia (high blood sugar), or changes in body fat (lipodystrophy syndrome)
• Increased bleeding in people with hemophilia (a rare blood-clotting disorder)

Long-Term Side Effects

While Aptivus can help you manage your HIV infection, long-term use of tipranavir can put you at risk of liver toxicity. It is important to talk to your healthcare provider if you notice signs of liver problems, such as dark urine, feeling tired, light-colored stools, or yellowing of the skin or eyes.

Dosage: How Much Aptivus Should I Take?

Modifications

Before starting tipranavir, inform your healthcare provider of any health conditions you have and your medical history.

Common reasons your healthcare provider may adjust your dosage or change your treatment include the following:

• Liver problems: Your healthcare provider will first run tests to see if you’re a good fit to take Aptivus. However, if you know you have severe liver problems, you should not take tipranavir.
• Age: Although the FDA has approved tipranavir to treat HIV infections in children two years or older, recent guidelines do not recommend its use in this age group.

Missed Dose

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue your normal dose schedule. You must only take one dose at a time, so do not take two doses to make up for the missed dose. Taking more Aptivus than prescribed can put you at risk of liver toxicity. 

Overdose: What Happens If I Take Too Much Aptivus?

Due to limited information, there is not an established amount of Aptivus reported to cause an overdose. However, you should generally not take more than 1000 milligrams of tipranavir within 24 hours. Taking any amount greater per day can put you at risk of liver toxicity.

Precautions

What Are Reasons I Shouldn’t Take Aptivus?

You should not take Aptivus if:

• You have known allergies to sulfa medications
• You are diagnosed with liver problems
• You are pre-diabetic or currently have diabetes (speak to your healthcare provider before starting Aptivus)
• You have high cholesterol (talk to your healthcare provider before starting Aptivus, as this medication may significantly increase your cholesterol levels)

What Other Medications Interact With Aptivus?

When taking Aptivus, you must be aware that medications or supplements can worsen your side effects or lower your treatment’s effectiveness.

Avoid taking tipranavir with the following medications:

• Antiarrhythmics, such as Pacerone (amiodarone) and quinidine: The combination of antiarrhythmic drugs and tipranavir can cause serious and life-threatening heart problems.
• Cholesterol-lowering medications, such as Altoprev (lovastatin) and Zocor (simvastatin)
• Medications for tuberculosis, such as rifampin: When using rifampin and tipranavir together, this combination can lead to Aptivus not working or can make the HIV not responsive to the medication.
• Sedatives, such as midazolam or Halcion (triazolam): The combination of sedatives and tipranavir can cause serious adverse effects, such as slowed breathing. 

Before starting treatment, tell your healthcare provider about any other medicines you take or plan to take, including over-the-counter (OTC) nonprescription products, vitamins, herbs, supplements, and plant-based medicines.

What Medications Are Similar?

Other protease inhibitors used for HIV include:

• Norvir (ritonavir)
• Reyataz (atazanavir)
• Prezista (darunavir)
• Lexiva (fosamprenavir)
• Viracept (nelfinavir)

Darunavir or atazanavir coadministered with ritonavir are common first-line antiretroviral therapy choices. Ritonavir is typically prescribed as part of a combination treatment as it acts as a “booster,” enhancing the effects of other protease inhibitors.

Typically, when other HIV medications do not work, your healthcare provider will prescribe tipranavir. Compared to tipranavir and other protease inhibitors, atazanavir has fewer side effects.

How Can I Stay Healthy While Taking Aptivus?

To stay healthy while taking Aptivus, take your medication exactly as your healthcare provider prescribes.

Since HIV can weaken your immune system, you are at a higher risk of illness. Stay up-to-date with vaccinations recommended by the Centers for Disease Control and Prevention (CDC) for people living with HIV, including pneumococcal vaccines, influenza vaccines, and the herpes zoster vaccine, among others. Talk to your healthcare provider about immunizations.

Your mental well-being is also important for staying healthy. Getting diagnosed and living with HIV can be overwhelming and leave you feeling stressed. Try building a support team with the people you love, and talk to your healthcare team about what to expect. While living with HIV might be scary, following the appropriate treatment and care can help you live a long and healthy life.

The author would like to recognize and thank Alexya Rosas for contributing to this article.