TIPRANAVIR

TIPRANAVIR
(ti-pra'na-vir)
Aptivus
Classifications: antiretroviral agent; hiv protease inhibitor;
Therapeutic: antiretroviral
; protease inhibitor
Prototype: Saquinavir
Pregnancy Category: C

Availability

250 mg capsules

Action

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.

Therapeutic Effect

Helps decrease viral load of HIV-1 strains resistant to other protease inhibitors.

Uses

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 antiretroviral agents.

Contraindications

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.

Cautious Use

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

HIV-1 Infection
Adult: PO 500 mg (with 200 mg ritonavir) b.i.d.

Administration

Oral
  • 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: Asthenia, depression, headache, insomnia. GI: 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: Rash.

Interactions

Drug: Aluminum- and magnesium-based antacids may decrease tipranavir absorption. azole antifungal agents, clarithromycin, erythromycin, and other inhibitors of CYP3A4 may increase tipranavir levels. Efavirenz, loperamide, nrtis, and rifamycins (e.g., rifampin) 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.

Pharmacokinetics

Peak: 3 h. Distribution: >99.9% protein bound. Metabolism: Extensive hepatic oxidation to inactive metabolites (when given alone); minimal metabolism (when given with ritonavir). Elimination: Fecal (primary) and renal (minimal). Half-Life: 6 h.

Nursing Implications

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 glucose.
  • 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 stools.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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