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APTIVUS is a protease inhibitor of HIV-1 belonging to the class of 4-hydroxy-5,6-dihydro-2-pyrone sulfonamides.
The chemical name of tipranavir is 2-Pyridinesulfonamide, N-[3-[(1R)-1-[(6R)-5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl). It has a molecular formula of C31H33F3N2O5S and a molecular weight of 602.7. Tipranavir has the following structural formula and is a single stereoisomer with the 1R, 6R configuration.
Tipranavir is a white to off-white to slightly yellow solid. It is freely soluble in dehydrated alcohol and propylene glycol, and insoluble in aqueous buffer at pH 7.5.
APTIVUS soft gelatin capsules are for oral administration. Each capsule contains 250 mg tipranavir. The major inactive ingredients in the capsule are dehydrated alcohol (7% w/w or 0.1 g per capsule), polyoxyl 35 castor oil, propylene glycol, mono/diglycerides of caprylic/capric acid and gelatin.
APTIVUS oral solution is available in a strength of 100 mg/mL of tipranavir. APTIVUS oral solution is a yellow, viscous clear liquid with a buttermint-butter toffee flavor. The major inactive ingredients in the oral solution are polyethylene glycol 400, vitamin E polyethylene glycol succinate (TPGS), purified water, and propylene glycol. Each milliliter of APTIVUS oral solution contains 116 IU of vitamin E, and when taken at the recommended maximum dose of 500 mg/200 mg tipranavir/ritonavir BID results in a daily dose of 1160 IU.
If you take too much Aptivus, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
If Aptivus is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.
- Store Aptivus capsules in a refrigerator at approximately 36°F to 46°F (2°C to 8°C). Once the bottle is opened, the contents must be used within 60 days. Patients may take the bottle with them for use away from home so long as the bottle remains at a temperature of approximately 59°F to 86°F (15°C to 30°C). You can write the date of opening the bottle on the label. Do not use after the expiration date written on the bottle.
- Store Aptivus oral solution at approximately 59°F to 86°F (15°C to 30°C). Do not refrigerate or freeze. The solution must be used within 60 days after first opening of the bottle.
- Keep Aptivus and all medicines out of the reach of children.
What is tipranavir?
Tipranavir is an antiviral medication called a protease (PRO-tee-ayz) inhibitor. Tipranavir prevents human immunodeficiency virus (HIV) cells from multiplying in your body.
Tipranavir is used to treat HIV, which causes the acquired immunodeficiency syndrome (AIDS). Tipranavir is not a cure for HIV or AIDS. Tipranavir is used together with a similar drug called ritonavir (Norvir).
Tipranavir may also be used for purposes not listed in this medication guide.
What is the most important information I should know about tipranavir?
You should not use tipranavir if you have moderate to severe liver disease.
Life-threatening side effects can occur if you take tipranavir with: alfuzosin, amiodarone, cisapride, flecainide, sildenafil (Revatio for pulmonary arterial hypertension), atorvastatin, lovastatin, simvastatin, propafenone, rifampin, quinidine, pimozide, midazolam (Versed), triazolam, St. John's wort, or an ergot medicine such as Ergomar, Ergotrate, Cafergot, D.H.E. 45, Migranal, or Methergine.
Tipranavir is taken in combination with ritonavir (Norvir). However, some people taking these medicines have developed fatal medical problems including liver damage and bleeding in the brain. Stop taking this medicine and get emergency medical attention if you have: unusual bleeding, sudden severe headache, numbness, problems with speech or vision, nausea, upper stomach pain, tired feeling, loss of appetite, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).
What other drugs will affect tipranavir?
Tell your doctor about all medicines you use, and those you start or stop using during your treatment with tipranavir, especially:
fluticasone (Flonase), sildenafil (Viagra), quetiapine (Seroquel), tadalafil (Cialis), vardenafil (Levitra);
birth control pills or hormone replacement therapy; or
medicine used to prevent blood clots--alteplase, clopidogrel, dipyridamole, ticlopidine, urokinase, warfarin (Coumadin, Jantoven);
This list is not complete. Many drugs can interact with tipranavir, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with tipranavir. Give a list of all your medicines to any healthcare provider who treats you.
2–8°C prior to opening bottle;1 after opening bottle, store at 25°C (may be exposed to 15–30°C) and use within 60 days.1Oral Solution
25°C (may be exposed to 15–30°C);1 do not refrigerate or freeze.1 After opening bottle, use within 60 days.1
Actions and Spectrum
Tipranavir must be administered in conjunction with low-dose ritonavir (ritonavir-boosted tipranavir).1
Tipranavir is extensively metabolized by CYP3A; ritonavir is a potent inhibitor of CYP3A.1 Concomitant use of these drugs results in decreased metabolism and increased plasma concentrations of tipranavir.1
Antiretroviral activity is due to tipranavir.1
Active against HIV-1;1 has some in vitro activity against HIV-2.13
Tipranavir inhibits replication of HIV-1 by interfering with HIV proteases.1
Tipranavir-resistant HIV-1, including strains with decreased susceptibility to other HIV PIs, has been reported.1
Before Using Aptivus
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Appropriate studies have not been performed on the relationship of age to the effects of tipranavir in children younger than 2 years of age. Safety and efficacy have not been established.
Although appropriate studies on the relationship of age to the effects of tipranavir have not been performed in the geriatric population, no geriatric-specific problems have been documented to date. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving tipranavir.
|All Trimesters||C||Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.|
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Interactions with Medicines
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
- Isavuconazonium Sulfate
- St John's Wort
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Ado-Trastuzumab Emtansine
- Brentuximab Vedotin
- Dabigatran Etexilate
- Doxorubicin Hydrochloride Liposome
- Irinotecan Liposome
- Tenofovir Alafenamide
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Aluminum Carbonate, Basic
- Aluminum Hydroxide
- Aluminum Phosphate
- Calcium Carbonate
- Conjugated Estrogens
- Dihydroxyaluminum Aminoacetate
- Dihydroxyaluminum Sodium Carbonate
- Esterified Estrogens
- Ethinyl Estradiol
- Magnesium Carbonate
- Magnesium Hydroxide
- Magnesium Oxide
- Magnesium Trisilicate
- Tenofovir Disoproxil Fumarate
Interactions with Food/Tobacco/Alcohol
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Bleeding problems (eg, hemophilia)—Use with caution. May increase the chance of bleeding.
- Diabetes mellitus or
- Hyperglycemia (high blood sugar)—May increase the amount of sugar in your blood.
- Hyperlipidemia (high cholesterol or fats in the blood) or
- Liver problems (including hepatitis B or C)—Use with caution. May make these conditions worse. .
- Liver disease, moderate or severe—Should not be used in patients with this condition.
- Sulfa allergy, known or suspected—Use with caution. May cause side effects to be worse.
Proper Use of Aptivus
Take this medicine exactly as directed by your doctor. Do not change your dose or stop using this medicine without checking first with your doctor. When your supply of this medicine is running low, contact your doctor or pharmacist ahead of time. Do not allow yourself to run out of this medicine.
This medicine comes with a patient information insert. Read and follow the instructions in the insert carefully. Ask your doctor if you have any questions.
Tipranavir is always taken with ritonavir (Norvir®). Take these two medicines at the same time, unless your doctor tells you otherwise.
If you are using this medicine with ritonavir capsules or oral liquid, you may take it with or without food. However, you should take this medicine with food if you are using it with ritonavir tablets.
Swallow the capsule whole. Do not break, crush, or chew it.
Measure the oral liquid with a marked measuring spoon, oral syringe, or medicine cup. The average household teaspoon may not hold the right amount of liquid.
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For treatment of HIV infection:
- For oral dosage forms (capsules or oral solution):
- Adults—500 milligrams (mg) (two capsules or 5 milliliters (mL)) of tipranavir and 200 mg of ritonavir (Norvir®) two times a day.
- Children 2 to 18 years of age—Dose is based on body weight or body size and must be determined by your doctor. The dose is usually 14 milligrams (mg) per kilogram (kg) of body weight of tipranavir plus 6 mg per kg of body weight of ritonavir (Norvir®), or 375 mg/m(2) of body size of tipranavir plus 150 mg/m(2) of body size of ritonavir two times a day. Your doctor may adjust your dose if needed. However, the dose should not be more than the recommended adult dose.
- Children younger than 2 years of age—Use and dose must be determined by your doctor.
- For oral dosage forms (capsules or oral solution):
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Store the capsules in the refrigerator until you are ready to open the bottle. Once you have opened the medicine bottle, you may store it at room temperature, away from heat, light, or moisture. The medicine is good for up to 60 days after you open the bottle. Throw away any unused capsules after 60 days and get a new bottle of medicine. .
Store the oral liquid at room temperature. Do not refrigerate or freeze it. The liquid must be used within 60 days after you open the bottle.
Before taking this medicine
You should not use Aptivus if you are allergic to tipranavir or ritonavir (Norvir, Kaletra), or if you have moderate to severe liver disease.
Life-threatening side effects can occur if you take Aptivus with any of the following medications:
amiodarone (Cordarone, Pacerone);
atorvastatin (Lipitor, Caduet), lovastatin (Mevacor, Altoprev, Advicor), simvastatin (Zocor, Simcor, Vytorin, Juvisync);
flecainide (Tambocor), propafenone (Rythmol), quinidine (Quinaglute);
midazolam (Versed) or triazolam (Halcion);
rifampin (Rifadin, Rifamate, Rimactane);
sildenafil (Revatio for pulmonary arterial hypertension);
St. John's wort; or
ergot medicines for migraine headache (Ergomar, Cafergot, D.H.E. 45, Migranal, Ergotrate, or Methergine).
To make sure you can safely take Aptivus, tell your doctor if you have any of these other conditions:
liver disease (especially hepatitis B or C);
high cholesterol or triglycerides;
a bleeding disorder such as hemophilia; or
if you are allergic to sulfa drugs.
It is not known whether Aptivus will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication. HIV can be passed to your baby if you are not properly treated during pregnancy. Take all of your HIV medicines as directed to control your infection.
Aptivus can make birth control pills less effective. Ask your doctor about using a non-hormone method of birth control (such as a condom, diaphragm, spermicide) to prevent pregnancy while taking this medicine.
Women with HIV or AIDS should not breast-feed a baby. Even if your baby is born without HIV, the virus may be passed to the baby in your breast milk.
Aptivus should not be given to a child younger than 2 years old.
How should I take Aptivus?
Take Aptivus exactly as prescribed by your doctor. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.
Aptivus is taken in combination with ritonavir (Norvir). Use tipranavir and ritonavir regularly to get the most benefit. Get your prescriptions refilled before you run out of medicine completely.
Take your medicine with food if you take tipranavir with ritonavir tablets.
You may take your medicine with or without food if you take tipranavir with ritonavir capsules or liquid.
Swallow the Aptivus capsule whole. Do not break or chew it.
Measure Aptivus liquid with the dosing syringe provided, or with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.
Tell your doctor if the child using this medicine has any changes in height or weight. Tipranavir doses are based on body surface area (height and weight) in children, and any changes may affect your dose.
While using Aptivus, you may need frequent blood tests.
If you need surgery, tell the surgeon ahead of time that you are using Aptivus.
HIV/AIDS is usually treated with a combination of drugs. Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice. Every person with HIV or AIDS should remain under the care of a doctor.
Store an unopened bottle of Aptivus capsules in the refrigerator. Do not freeze.
After opening the bottle of capsules for the first time, you may store the medicine at room temperature. Store Aptivus liquid at room temperature away from moisture and heat. Do not store the liquid in the refrigerator.
Throw away any capsules or liquid you have not used within 60 days after you first opened the medicine bottle.
Aptivus dosing information
Usual Adult Dose for HIV Infection:
Tipranavir 500 mg plus ritonavir 200 mg orally twice a day
Usual Pediatric Dose for HIV Infection:
2 to 18 years: Tipranavir 14 mg/kg plus ritonavir 6 mg/kg or tipranavir 375 mg/m2 plus ritonavir 150 mg/m2 orally twice a day
Pediatric dosage should not exceed the usual adult dosage.
Tipranavir Pregnancy Warnings
Animal studies have revealed evidence of fetotoxicity (reduced sternebrae ossification and body weights), growth inhibition in pups, and maternal toxicity in rats at exposure levels about 0.8-fold human exposure (at recommended dose). There are no controlled data in human pregnancy. To monitor maternal-fetal outcomes of pregnant women exposed to antiretroviral therapy, an Antiretroviral Pregnancy Registry (APR) has been established. Healthcare providers are encouraged to prospectively register patients. For additional information: apregistry.com No conclusions regarding birth defect risk available; insufficient first-trimester exposures to this drug have been monitored in the APR. This drug adversely interacts with oral contraceptives; an alternative method of contraception is recommended during therapy. AU TGA pregnancy category B3: Drugs which have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malformation or other direct or indirect harmful effects on the human fetus having been observed. Studies in animals have shown evidence of an increased occurrence of fetal damage, the significance of which is considered uncertain in humans. US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
This drug should be used during pregnancy only if the benefit outweighs the risk to the fetus. AU TGA pregnancy category: B3 US FDA pregnancy category: C Comments: -A pregnancy exposure registry is available.
Tipranavir Breastfeeding Warnings
Breastfeeding is not recommended during use of this drug; if replacement feeding is not an option, a different drug may be preferred. Excreted into human milk: Unknown Excreted into animal milk: Yes Comments: -The effects in the nursing infant are unknown. -The US CDC, American Academy of Pediatrics, and manufacturer advise HIV-infected women not to breastfeed to avoid postnatal transmission of HIV to a child who may not yet be infected. -Local guidelines should be consulted if replacement feeding is not an option.
Increased transaminases (26-32%)
Abdominal pain (4%)
Weight loss (3%)