tipranavir (Rx)

Brand and Other Names:Aptivus
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 250mg

oral solution

  • 100mg/mL

HIV Infection

500 mg PO q12hr; coadministration with ritonavir 200 mg PO q12hr is required (boosted therapy)

Administration with ritonavir essential to achieve correct dosing and adequate blood levels

Renal Impairment

Dose adjustment not necessary

Hepatic Impairment

Mild (Child-Pugh class A): Dose adjustment not necessary

Moderate-to-severe (Child-Pugh class B or C): Concurrent use contraindicated

Dosage Forms & Strengths

capsule

  • 250mg

oral solution

  • 100mg/mL

HIV Infection

Indicated for treatment of HIV-1 infected patients who are treatment-experienced and infected with HIV-1 strains resistant to more than one protease inhibitor; must be used with ritonavir in addition to other antiretrovirals

<2 years: Safety and efficacy not established

≥2 years: 14 mg/kg plus ritonavir 6 mg/kg PO q12hr, OR  

375 mg/m² plus ritonavir 150 mg/m² PO q12hr  

Not to exceed adult dose of 500 mg plus ritonavir 200 mg PO q12hr

Administration with ritonavir essential to achieve correct dosing and adequate blood levels

Dose reduction

  • If not tolerated, may reduce dose if patient does not have resistant to multiple protease inhibitors
  • 12 mg/kg plus ritonavir 5 mg/kg PO q12hr, OR
  • 290 mg/m² plus ritonavir 115 mg/m² PO q12hr
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Interactions

Interaction Checker

and tipranavir

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Diarrhea (15%)

            Rash (3-21%)

            Hypertriglyceridemia (61%)

            Increased transaminases (26-32%)

            1-10%

            Abdominal pain (4%)

            Dyspnea (2%)

            Epistaxis (4%)

            Dehydration (2%)

            Fatigue (6%)

            Headache (5%)

            Weight loss (3%)

            Nausea (5-9%)

            Pyrexia (6%)

            Anemia (3%)

            Vomiting (6%)

            Myalgia (2%)

            <1%

            Dizziness

            Hepatitis

            Decreased apetite

            Flu-like syndrome

            Hyperbilirubinemia

            Insomnia

            Increased lipase

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            Warnings

            Black Box Warnings

            Hepatitis and hepatic decompensation, including some fatalities, reported; extra vigilance warranted with chronic hepatitis B or hepatitis C coinfection because of increased risk of hepatotoxicity

            Intracranial hemorrhage, both fatal and nonfatal, reported

            Contraindications

            Hypersensitivity

            Moderate-severe hepatic impairment (Child-Pugh Class B & C)

            Drugs that are contraindicated with tipranavir (when coadministered 'boosted' with ritonavir) include alpha1-adrenoreptor agonists (eg, alfuzosin), antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine), rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, lovastatin, simvastatin, lurasidone, pimozide, sildenafil (when used for PAH), midazolam, and triazolam

            Cautions

            Caution in mild hepatic impairment

            Risk of severe, potentially fatal hepatotoxicity

            Not recommended in treatment-naive patients

            May have antiplatelet/anticoagulant action

            Risk of potentially fatal intracranial hemorrhage

            Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs

            Fat redistribution with "cushingoid appearance" and "buffalo hump" may occur

            Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) have also been reported to occur in the setting of immune reconstitution; however, the time to onset is more variable, and can occur many months after initiation of treatment

            Must be coadministered with ritonavir

            Sulfonamide allergy

            Coadministration with other CYP3A4 substrates (ritonavir inhibits CYP3A4 and increases toxicity risk for drugs metabolized by CYP3A4)

            Increased risk of rash, especially with hormonal contraceptives

            Use of drug may reduce efficacy of estrogen-based oral contraceptives; advise patients to use alternative methods of nonhormonal contraception

            Risk of large increase in total cholesterol and triglycerides

            Contains 116 IU/mL vitamin E (>RDA); limit supplemented vitamin E

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            Pregnancy & Lactation

            Pregnancy

            Pregnancy exposure registry monitors pregnancy outcomes in women exposed to drug during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263

            Prospective pregnancy data from the APR and an Expanded Access program are not sufficient to adequately assess risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes; tipranavir use during pregnancy has been evaluated in a limited number of women as reported by the APR and an Expanded Access program, and available data show no birth defects in 13 first trimester exposures compared with the background rate for major birth defects of 2.7% in the US reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP); rate of miscarriage not reported in the APR; methodological limitations of APR include the use of MACDP as the external comparator group; MACDP population is not disease-specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at less than 20 weeks gestation

            In animal reproduction studies, fetal toxicities were observed with tipranavir at maternally toxic doses with systemic exposures (AUC) less than those in humans at recommended human dose

            Based on prospective reports to APR and an Expanded Access program for approximately 17 live births following exposure to tipranavir-containing regimens (including 13 live births exposed in the first trimester and 4 live births exposed in the second/third trimester), there were no birth defects reported in live-born infants; tipranavir has been shown to cross placenta

            Lactation

            The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers in the United States not breast-feed their infants to avoid risking postnatal transmission of HIV-1 infection; there is no information regarding presence of tipranavir in human milk, effects on breastfed infant, or on milk production; tipranavir is present in rat milk; because of potential for (1) HIV-1 transmission (in HIV-negative infants), developing viral resistance (in HIV-positive patients), and any possible adverse effects of drug, mothers should not breastfeed if they are receiving drug

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Protease Inhibitor; inhibits cleavage of Gag-Pol polyprotein precursors, which in turn causes the formation of immature, noninfectious viral particles.

            Pharmacokinetics

            Bioavailability: Increased by food

            Protein Bound: 99.9%

            Vd: 7.7-10 L

            Half-Life: 5.5-6 hr

            Metabolism: primarily by liver CYP3A4

            Excretion: Feces (82.3% ); urine (4%)

            Peak plasma time: 3 hr

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            Administration

            Oral Administration

            Must be coadministered with ritonavir

            Adults or children taking tablets: Take with food

            Capsules or oral solution

            • Adults: May take with or without food
            • Children: Take with food

            Storage

            Capsules: Store unopened bottles of capsules refrigerated at 2-8°C (36-46°F); once bottle is opened, capsules can be kept at room temperature (maximum 77°F [25°C]) if used within 60 days

            Oral solution: Store at room temperature, 25°C (77°F); do not refrigerate or freeze; must be used within 60 days after the bottle is first opened

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.