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darunavir (Rx)Brand and Other Names:Prezista

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 75mg
  • 150mg
  • 600mg
  • 800mg

oral suspension

  • 100mg/mL
more...

HIV Infection

Coadministered with ritonavir and in combination with other antiretroviral agents for HIV infection

Treatment-naive or antiretroviral treatment-experienced (with no darunavir resistance associated substitutions): 800 mg + ritonavir 100 mg PO qDay with food

Treatment-experienced (with at least 1 DRV mutation) or genotyping not obtained: 600 mg + ritonavir 100 mg PO q12hr with food

Pregnant females

  • Recommended: 600 mg + ritonavir 100 mg PO q12hr with food
  • 800 mg + ritonavir 100 mg PO qDay should only be considered in certain pregnant patients who are already on a stable darunavir 800 mg + ritonavir 100 mg qDay regimen prior to pregnancy, are virologically suppressed (ie, HIV-1 RNA <50 copies/mL), and in whom a change to the twice daily regimen may compromise tolerability or compliance

Dosage Modifications

Renal impairment

  • Mild-to-moderate (≥ 30 mL/min): No dosage adjustment required
  • Severe (≤ 30 mL/min): Data not available, but renal clearance is limited and decreased total body clearance not expected

Hepatic impairment

  • Mild-to-moderate impairment (Child-Pugh class A or B): No dosage adjustment required
  • Severe (Child-Pugh class C): Not recommended

Dosing Considerations

In treatment-experienced patients, treatment history, genotypic and/or phenotypic testing is recommended to assess drug susceptibility of the HIV-1 virus

Obtain appropriate laboratory testing (eg, serum liver biochemistries) before initiating darunavir

Patients with underlying chronic hepatitis, cirrhosis, or those who have pretreatment liver enzyme should be monitored for elevated transaminases, especially during the first several months

Dosage Forms & Strengths

tablet

  • 75mg
  • 150mg
  • 600mg
  • 800mg

oral suspension

  • 100mg/mL
more...

HIV Infection

Coadministered with ritonavir and in combination with other antiretroviral agents for HIV infection

<3 years: Safety and efficacy not established

Must take with food

Also see Administration

Treatment-naive or antiretroviral treatment-experienced (with no darunavir resistance associated substitutions)

  • NOTE: The HIV treatment guidelines differ from the prescribing information and recommend that once-daily darunavir dosing should NOT be used as initial therapy in children <12 yr; a switch to once-daily therapy may be considered in patients who have undetectable viral loads on twice-daily therapy to enhance ease of use and support compliance
  • Weight 10 kg to <15 kg
    • Use oral suspension
    • ≥10 kg to <11 kg: 350 mg (3.6 mL)* + ritonavir 64 mg (0.8 mL) PO qDay
    • ≥11 kg to <12 kg: 385 mg (4 mL)* + ritonavir 64 mg (0.8 mL) PO qDay
    • ≥12 kg to <13 kg: 420 mg (4.2 mL) + ritonavir 80 mg (1 mL) PO qDay
    • ≥13 kg to <14 kg: 455 mg (4.6 mL)* + ritonavir 80 mg (1 mL) PO qDay
    • ≥14 kg to <15 kg: 490 mg (5 mL)* + ritonavir 96 mg (1.2 ml) PO qDay
    • *NOTE: Doses that were rounded up to nearest measurable suspension dose
  • Weight ≥15 kg
    • ≥15 kg to <30 kg: 600 mg + ritonavir 100 mg PO qDay
    • &ge:30 kg to <40 kg: 675 mg + ritonavir 100 mg PO qDay
    • ≥40 kg: 800 mg + ritonavir 100 mg PO qDay

Antiretroviral treatment-experienced with at least 1 darunavir resistance associated substitution

  • Weight 10 kg to <15 kg
    • Use oral suspension
    • ≥10 kg to <11 kg: 200 mg (2 mL) + ritonavir 32 mg (0.4 mL) PO BID
    • ≥11 kg to <12 kg: 220 mg (2.2 mL) + ritonavir 40 mg (0.4 mL) PO BID
    • ≥12 kg to <13 kg: 240 mg (2.4 mL) + ritonavir 32 mg (0.5 mL) PO BID
    • ≥13 kg to <14 kg: 260 mg (2.6 mL) + ritonavir 40 mg (0.5 mL) PO BID
    • ≥14 kg to <15 kg: 280 mg (2.8 mL) + ritonavir 48 mg (0.6 mL) PO BID
  • Weight ≥15 kg
    • ≥15 kg to <30 kg: 375 mg + ritonavir 48 mg PO BID
    • &ge:30 kg to <40 kg: 450 mg + ritonavir 60 mg PO BID
    • ≥40 kg: 600 mg + ritonavir 100 mg PO BID

Dosage Modifications

Renal impairment

  • Mild-to-moderate: No dosage adjustment required
  • Severe: Data not available, but renal clearance is limited and decreased total body clearance not expected

Hepatic impairment

  • Mild-to-moderate impairment: No dosage adjustment required
  • Severe: Not recommended

Dosing Considerations

In treatment-experienced patients, treatment history, genotypic and/or phenotypic testing is recommended to assess drug susceptibility of the HIV-1 virus

Obtain appropriate laboratory testing (eg, serum liver biochemistries) before initiating darunavir

Patients with underlying chronic hepatitis, cirrhosis, or those who have pretreatment liver enzyme should be monitored for elevated transaminases, especially during the first several months

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Interactions

Interaction Checker

darunavir and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Increased total cholesterol (10-25%)

            Increased triglycerides (3-10%)

            1-10%

            Diarrhea (9%)

            Headache (7%)

            Rash (6%)

            Abdominal pain (6%)

            Nausea (4%)

            Vomiting (2%)

            Anorexia (2%)

            <1%

            Fatigue

            Frequency Not Defined

            Gastrointestinal disorders: Acute pancreatitis, dyspepsia, flatulence

            General disorders and administration site Conditions: Asthenia

            Hepatobiliary disorders: Acute hepatitis (eg, cytolytic hepatitis, hepatotoxicity)

            Immune dystem disorders: Hypersensitivity, immune reconstitution syndrome

            Metabolism and nutrition disorders: Diabetes mellitus

            Musculoskeletal and connective tissue disorders: Myalgia, osteonecrosis

            Psychiatric disorders: Abnormal dreams

            Skin and subcutaneous tissue disorders: Angioedema, pruritus, Stevens-Johnson Syndrome, urticaria

            Postmarketing Reports

            Body fat redistribution

            Rhabdomyolysis (associated with statin coadministration)

            Toxic epidermal necrolysis and acute generalized exanthematous pustulosis

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            Warnings

            Contraindications

            Hypersensitivity

            Concomitant CYP3A4 substrates that are toxic in excess

            Concurrent strong CYP3A4 inducers (eg, St John's wort, rifampin)

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

            Cautions

            Must be taken with ritonavir and food, since dose is based on the fact that darunavir is metabolized by CYP3A4 and ritonavir is a potent CYP3A4 inhibitor

            Severe skin reactions, accompanied by fever and/or elevations of transaminases reported (0.4%); Stevens-Johnson Syndrome (<0.1%), toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms, and acute generalized exanthematous pustulosis also reported

            Caution with elderly patients

            Caution with hepatic impairment (not recommended if severe)

            Contains a sulfa moiety; monitor patients with a known sulfonamide allergy

            Increase in total cholesterol and triglycerides reported; screen before therapy and throughout treatment

            Pancreatitis reported; use caution in patients at risk for pancreatitis (those with elevated triglycerids, history of pancreatitis, or advanced HIV disease

            Risk of immune reconstitution syndrome

            Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients receiving antiretroviral therapy

            Patients with hemophilia may develop increased bleeding events

            Not for use in patients < 3 years of age; toxicity may occur

            Hepatoxicity

            • Risk of hepatotoxicity including drug induced hepatitis: acute hepatitis, cytolytic hepatitis
            • Especially with preexisting liver dysfunction (chronic hepatitis B or C)
            • Interrupt or discontinue treatment if new/worsening liver dysfunction develops
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            Pregnancy & Lactation

            Pregnancy Category: C

            Antiretroviral Pregnancy Registry has been established:1-800-258-4263.

            Lactation

            Not known whether distributed into milk. Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed.

            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.

            more...
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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: with ritonavir: 82%; without ritonavir: 37%

            Peak Plasma Time: 2.5-4 hr

            Protein Bound: 95%

            Metabolism: CYP3A4

            Half-life, elimination: 15 hr

            Excretion: Urine (14%) feces (80%)

            Pharmacogenomics

            Genotyping is recommended to determine if darunavir resistance mutations are present in treatment experienced patients

            Increase dose if 1 of the following resistance associated substitutions is present: V11I, V32I, L33F, I47V, I50V, I54L, I54M, T74P, L76V, I84V, and L89V

            Genetic testing laboratories

            • The following companies provide genetic testing for antiretrovirals
            • Monogram Biosciences (http://www.monogrambio.com/200HIVProducts.aspx)
            • Virco (http://www.vircolab.com/)
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            Administration

            Oral Administration

            Swallow tablet whole; do not chew, crush, or split

            Must take with food; food increases the area under the curve (AUC) and maximum plasma concentration (Cmax) by 30%

            Assess ability to swallow; use oral suspension for adults or children who cannot swallow the tablet whole

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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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