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APTIVUS, co-administered with ritonavir, is indicated for combination antiretroviral treatment of HIV-1 infected patients who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor (PI).
This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of APTIVUS/ritonavir of 48 weeks duration in treatment-experienced adults and one open-label 48-week study in pediatric patients age 2 to 18 years. The adult studies were conducted in clinically advanced, 3-class antiretroviral (NRTI, NNRTI, PI) treatment-experienced adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
The following points should be considered when initiating therapy with APTIVUS/ritonavir:
- The use of APTIVUS/ritonavir in treatment-na´ve patients is not recommended [see WARNINGS AND PRECAUTIONS].
- The use of other active agents with APTIVUS/ritonavir is associated with a greater likelihood of treatment response [see CLINICAL PHARMACOLOGY and Clinical Studies].
- Genotypic or phenotypic testing and/or treatment history should guide the use of APTIVUS/ritonavir [see CLINICAL PHARMACOLOGY]. The number of baseline primary protease inhibitor mutations affects the virologic response to APTIVUS/ritonavir [see CLINICAL PHARMACOLOGY].
- Use caution when prescribing APTIVUS/ritonavir to patients with elevated transaminases, hepatitis B or C co-infection or patients with mild hepatic impairment [see WARNINGS AND PRECAUTIONS].
- Liver function tests should be performed at initiation of therapy with APTIVUS/ritonavir and monitored frequently throughout the duration of treatment [see WARNINGS AND PRECAUTIONS].
- The drug-drug interaction potential of APTIVUS/ritonavir when co-administered with other drugs must be considered prior to and during APTIVUS/ritonavir use [see CONTRAINDICATIONS and DRUG INTERACTIONS].
- Use caution when prescribing APTIVUS/ritonavir in patients who may be at risk for increased bleeding or who are receiving medications known to increase the risk of bleeding [see WARNINGS AND PRECAUTIONS].
- The risk-benefit of APTIVUS/ritonavir has not been established in pediatric patients < 2 years of age.
- There are no study results demonstrating the effect of APTIVUS/ritonavir on clinical progression of HIV-1.
DOSAGE AND ADMINISTRATION
APTIVUS must be co-administered with ritonavir to exert its therapeutic effect. Failure to correctly co-administer APTIVUS with ritonavir will result in plasma levels of tipranavir that will be insufficient to achieve the desired antiviral effect and will alter some drug interactions.
- APTIVUS co-administered with ritonavir capsules or solution can be taken with or without meals
- APTIVUS co-administered with ritonavir tablets must only be taken with meals [see CLINICAL PHARMACOLOGY]
APTIVUS may be administered as either capsules or oral solution to either pediatric or adult patients.
Due to the need for co-administration of APTIVUS with ritonavir, please refer to the ritonavir prescribing information.
The recommended adult dose of APTIVUS is 500 mg (two 250 mg capsules or 5 mL oral solution) co-administered with 200 mg of ritonavir, twice daily.
Pediatric Patients (age 2 to 18 years)
Healthcare professionals should pay special attention to accurate calculation of the dose of APTIVUS, transcription of the medication order, dispensing information and dosing instruction to minimize risk for medication errors, overdose, and underdose.
Prescribers should calculate the appropriate dose of APTIVUS for each individual child based on body weight (kg) or body surface area (BSA, m²) and should not exceed the recommended adult dose.
Before prescribing APTIVUS 250 mg capsules, children should be assessed for the ability to swallow capsules. If a child is unable to reliably swallow an APTIVUS capsule, the APTIVUS oral solution formulation should be prescribed.
The recommended pediatric dose of APTIVUS is 14 mg/kg with 6 mg/kg ritonavir (or 375 mg/m² co-administered with ritonavir 150 mg/m²) taken twice daily not to exceed a maximum dose of APTIVUS 500 mg co-administered with ritonavir 200 mg twice daily. For children who develop intolerance or toxicity and cannot continue with APTIVUS 14 mg/kg with 6 mg/kg ritonavir, physicians may consider decreasing the dose to APTIVUS 12 mg/kg with 5 mg/kg ritonavir (or APTIVUS 290 mg/m² co-administered with 115 mg/m² ritonavir) taken twice daily provided their virus is not resistant to multiple protease inhibitors [see ADVERSE REACTIONS, Use In Specific Populations, and Clinical Studies].
Body surface area can be calculated as follows:
Mosteller formula: BSA(m²)= √Height (cm) x Weight (kg)/3600
Dosage Forms And Strengths
Capsules: 250 mg, pink, oblong capsules imprinted with TPV 250
Oral solution: 100 mg/mL, yellow, viscous clear liquid with a buttermint-butter toffee flavor
Storage And Handling
APTIVUS capsules 250 mg are pink, oblong soft gelatin capsules imprinted in black with “TPV 250”. They are packaged in HDPE unit-of-use bottles with a child resistant closure and 120 capsules. (NDC 0597-0003-02)
APTIVUS oral solution is a clear yellow viscous buttermint-butter toffee flavored liquid containing 100 mg tipranavir in each mL. The solution is supplied in a unit-ofuse amber glass bottle providing 95 mL of solution with a child resistant closure. A 5 mL plastic oral dispensing syringe is also provided. (NDC 0597-0002-01).
APTIVUS capsules should be stored in a refrigerator 2°-8°C (36°-46°F) prior to opening the bottle. After opening the bottle, the capsules may be stored at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) and must be used within 60 days after first opening the bottle.
APTIVUS oral solution should be stored at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F). Do not refrigerate or freeze. The solution must be used within 60 days after first opening the bottle.
Store in a safe place out of the reach of children.
Distributed by: Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA
Last reviewed on RxList: 3/1/2012
This monograph has been modified to include the generic and brand name in many instances.
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