Classifications: antiretroviral agent; hiv protease inhibitor; Therapeutic: antiretroviral; protease inhibitor
Pregnancy Category: C
250 mg capsules
A non-peptide protease inhibitor. It inhibits virus-specific processing of the viral polyproteins in HIV-1 infected cells,
thus preventing the formation of mature viral particles.
Helps decrease viral load of HIV-1 strains resistant to other protease inhibitors.
Treatment of HIV-1 infection in adults with evidence of viral replication who are highly treatment-experienced or have HIV-1
strains resistant to multiple protease inhibitors. Tipranavir should be used in combination with ritonavir 200 mg and other
Known hypersensitivity to any of the ingredients in tipranavir; moderate to severe (Child-Pugh class B and C, respectively)
hepatic insufficiency; pancreatitis; pregnancy (category C); lactation. Safety and efficacy in children have not been established.
Hypersensitivity to sulfonamides; patients with chronic hepatitis B or hepatitis C coinfection; hemophilia; coagulopathy;
elevated liver enzymes; diabetes mellitus or hyperglycemia; hyperlipidemia; concurrent administration with HMG-CoA inhibitors.
Route & Dosage
Adult: PO 500 mg (with 200 mg ritonavir) b.i.d.
- Coadminister with 200 mg ritonavir. Give with food.
- Store at 15°30° C (59°86° F). Once opened, use contents of bottle within 60 d.
Adverse Effects (≥1%)Body as a Whole: Fatigue
, pyrexia. CNS:
, headache, insomnia
Abdominal pain, diarrhea,
nausea, vomiting. Hematologic:
Decreased white blood cell levels, risk of hemorrhage. Hepatic: Elevated liver enzymes (amylase, ALT, AST). Metabolic: Increased cholesterol, increased triglycerides. Respiratory: Bronchitis
, cough. Skin:
may decrease tipranavir absorption. azole antifungal agents
, clarithromycin, erythromycin,
and other inhibitors of CYP3A4 may increase tipranavir levels. Efavirenz, loperamide, nrtis
, and rifamycins
) may decrease tipranavir levels. Tipranavir increases rifabutin
levels. Coadministration of tipranavir and tenofovir
decreases the levels of both compounds. Tipranavir increases the concentration of benzodiazepines
, desipramine, ergot alkaloids
, and numerous antiarrhythmic agents (amiodarone, flecainide, propafenone, quinidine).
Tipranavir may decrease ethinyl estradiol
levels by 50%. Combination use of tipranavir and hmg coa reductase inhibitors
increases the risk of myopathy. Tipranavir capsules contain alcohol
that can produce disulfiram-like reactions with metronidazole
and disulfiram. Food:
Food enhances the bioavailability of tipranavir. Herbal: St. John's wort
decreases the levels of tipranavir.
3 h. Distribution:
>99.9% protein bound. Metabolism:
oxidation to inactive metabolites (when given alone); minimal metabolism
(when given with ritonavir). Elimination:
Fecal (primary) and renal
Assessment & Drug Effects
- Monitor for and report immediately S&S of liver toxicity.
- Monitor for S&S of adverse drug reactions and toxicity from concurrently administered drugs. Many drugs interact with tipranavir.
- Monitor diabetics for loss of glycemic control.
- Use barrier contraceptive if using hormonal contraceptive.
- Lab tests: Baseline and frequent LFTs, especially in those with hepatitis B or C; periodic lipid profile and fasting plasma
- Monitor blood levels of anticoagulants with concurrent therapy.
Patient & Family Education
- Follow directions for taking the drug (see Administration). If a dose is missed, take it as soon as possible and then return
to the normal schedule. Never double a dose.
- Inform physician of all medications and herbal products you are taking.
- Protect against sunlight exposure to minimize risk of photosensitivity.
- Report any of the following to physician: fatigue, weakness, loss of appetite, nausea, jaundice, dark urine, or clay colored