Manufacturer: Boehringer Ingelheim
Chemical Name: 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)-
CAS Number: 191150-83-1
Molecular formula: C31-H33-F3-N2-O5-S
C 61.78%, H 5.52%, F 9.46%, N 4.65%, O 13.27%, S 5.32%
Molecular weight: 602.66
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-(trifluoro-methyl). It has a molecular formula of C 31 H 33 F 3 N 2 O 5 S 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? is the brand name for tipranavir (TPV), a non-peptidic protease inhibitor (PI) of HIV belonging to the class of 4-hydroxy-5,6-dihydro-2-pyrone sulfonamides.
Tipranavir 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.
Tipranavir is an antiviral medication. It is in a category of HIV medicines called protease inhibitors. Tipranavir prevents HIV from maturing. When used with other anti-HIV medicines, tipranavir may reduce the amount of HIV in your blood and increase the number of CD4+ cells. Reducing the amount of HIV in the blood may keep your immune system healthy, so it can help fight infection.
.Tipranavir is used in combination with ritonavir (Norvir) to treat human immunodeficiency virus (HIV), which causes acquired immunodeficiency syndrome (AIDS).
.Tipranavir is not a cure for HIV or AIDS.
.Tipranavir may also be used for purposes other than those listed in this medication guide.
Dosage Form: Phase II clinical trials evaluated TPV in a 300 mg hard-gel capsule. This formulation, which required high doses and a high pill burden to obtain optimal plasma levels, was replaced with a 250 mg soft-gel capsule available in a Self-Emulsifying Drug Delivery System. Phase II clinical trials evaluated TPV/ritonavir at 500/100 mg, 500/200 mg, and 750/200 mg twice daily doses. Of these, the 500/200 mg dose was selected for further study in Phase III trials based on optimal pharmacokinetics, safety, and tolerability data.
Mechanism of Action
Storage: Store capsules at 2 C to 8 C (36 F to 46 F) prior to opening the bottle. After opening, store at 25 C (77 F); excursions permitted to 15 C to 30 C (59 F to 86 F). Use within 60 days after opening.
Tipranavir (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the virus-specific processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions.
What should I avoid while taking tipranavir?
.Tipranavir does not cure HIV infection or AIDS. The long-term effects of tipranavir are not known at this time. People taking tipranavir may still get infections or other conditions common in people with HIV (opportunistic infections). It is very important that you stay under the care of your doctor during treatment with tipranavir.
.Tipranavir does not reduce the chance of passing HIV to others through sexual contact, sharing needles, or being exposed to your blood. Continue to practice safer sex. Use a latex or polyurethane condom or other barrier method to lower the chance of sexual contact with any body fluids such as semen, vaginal secretions or blood. Never use or share dirty needles. Ask your doctor if you have any questions about safer sex or how to prevent passing HIV to other people.
What are the possible side effects of tipranavir?
.Tipranavir may cause serious side effects, including:
， liver problems, including liver failure and death;
， increased bleeding in patients with hemophilia;
， diabetes and high blood sugar (hyperglycemia);
， increased blood fat (lipid) levels;
， changes in body fat;
， stomach pain;
? Tell your doctor about any changes in your health. You should report any new or continuing symptoms to your doctor right away. Your doctor may be able to help you manage these side effects. The list of side effects is not complete. Ask your doctor or pharmacist for more information.
What other drugs will affect tipranavir?
.Some drugs are not recommended to be taken with tipranavir. Do not take tipranavir without first talking to your doctor if you are taking any of the following drugs:
， migraine headache medicines;
， triazolam (Halcion);
， astemizole (Hismanal);
， pimozide (Orap);
， cisapride (Propulsid);
， terfenadine (Seldane);
， midazolam (Versed);
， amiodarone (Pacenone);
， bepridil (Vascor);
， flecainide (Tambocor);
， propafenone (Rythmol); or
， quinidine (Quinaglute dura).
.Talk to you doctor if you are using estrogens for birth control or hormone replacement. Women who use estrogens for birth control or hormone replacement have an increased chance of developing a skin rash while taking tipranavir. If a rash occurs, it is usually mild to moderate, but you should talk to your doctor as you may need to temporarily stop taking either tipranavir or the other medicine that contains estrogen or female hormones.
.Tell your doctor about all the medicines you take including prescription and nonprescription medicines, vitamins and herbal supplements. Tipranavir and many other medicines can interact. Sometimes serious side effects will happen if tipranavir is taken with certain other medicines.