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raltegravir (Rx)Brand and Other Names:Isentress

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, film-coated

  • 400mg
more...

HIV-1 Infection

Indicated in combination with other antiretroviral agents for HIV-1 infection

400 mg PO BID with or without food

Dosage Modifications

Coadministration with rifampin: 800 mg PO BID

Dosing Considerations

Combination regimen is based on analyses of plasma HIV-1 RNA levels in 3 double-blind controlled studies; 2 of these studies were conducted in clinically advanced, 3-class antiretroviral (NNRTI, NRTI, PI) treatment-experienced adults through 96 wk and 1 study was conducted in treatment-naïve adults through 240 wk

The use of other active agents with raltegravir is associated with a greater likelihood of treatment response

Dosage Forms & Strengths

tablet, film-coated

  • 400mg

tablet, chewable

  • 25mg
  • 100mg (scored)

powder for oral suspension

  • 100mg/packet
more...

HIV-1 Infection

Indicated in combination with other antiretroviral agents for HIV-1 infection in children and adolescents aged 4 weeks or older

Film-coated tablet (weight ≥25 kg): 400 mg PO BID

Chewable tablet

  • 10 to <14 kg: 75 mg PO BID
  • 14 to <20 kg: 100 mg PO BID
  • 20 to <28 kg: 150 mg PO BID
  • 28 to <40 kg: 200 mg PO BID
  • ≥40 kg: 300 mg PO BID

Powder for oral suspension

  • Age at least 4 weeks and weight 3-20 kg
  • 3 to <4 kg: 20 mg (1 mL) PO BID
  • 4 to <6 kg: 30 mg (1.5 mL) PO BID
  • 6 to <8 kg: 40 mg (2 mL) PO BID
  • 8 to <11 kg: 60 mg (3 mL) PO BID
  • 11 to <14 kg: 80 mg (4 mL) PO BID
  • 14 kg to <20 kg: 100 mg (5 mL) PO BID

Dosing Considerations

Combination regimen is based on safety, tolerability, pharmacokinetic parameters, and efficacy data through at least 24-wk in a multicenter, open-label, noncomparative study in HIV-1 infected children and adolescents aged 4 wk to 18 yr

Administration

May administer with or without food

Chewable tablets and film-coated tablets are not bioequivalent; and therefore, are not interchangeable

Powder for oral suspension

  • Suspend 1 packet (100 mg) in 5 mL of water; final concentration of 20 mg/mL
  • Administer suspension within 30 minutes of mixing
  • Discard any remaining suspension
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Interactions

Interaction Checker

raltegravir and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
             activity indicator 
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            Adverse Effects

            >10%

            Total cholesterol increased (16%)

            1-10%

            AST increased (9%)

            Glucose increased (9%)

            Hyperbilirubinemia (9%)

            Fatigue (8%)

            Nasopharyngitis (6%)

            Abdominal pain (5%)

            Cough (5%)

            Rash (5%)

            Dizziness (4%)

            Insomnia (4%)

            Vomiting (4%)

            Arthralgia (3%)

            Extremity pain (3%)

            Influenza (3%)

            Nausea

            Diarrhea

            Pyrexia

            <1%

            Asthenia

            GI disorders

            Lipodystrophy

            Skin disorders

            Drug related hypersensitivity

            Thrombocytopenia

            Renal failure

            Suicidal ideation

            Postmarketing Reports

            Cerebellar ataxia

            Diarrhea

            Hepatic failure

            Thrombocytopenia

            Rhabdomyolysis

            Psychiatric disorders: anxiety, depression (particularly in patients with a pre-existing history of psychiatric illness), including suicidal ideation and behaviors, paranoia

            Skin: rash, Steven’s-Johnson syndrome

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            Warnings

            Contraindications

            None

            Cautions

            Risk of immune reconstitution syndrome if used with HAART

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

            Concomitant medications known to increase risk of myopathy or rhabdomyolysis

            Coadministration with drugs that are strong inducers of UGT1A1 may result in reduced plasma concentrations of raltegravir

            Drug rash with eosinophilia and systemic symptoms (DRESS) reported

            Severe, potentially life-threatening and fatal skin reactions reported; skin reactions include cases of Stevens-Johnson syndrome, hypersensitivity reaction and toxic epidermal necrolysis; immediately discontinue treatment if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely

            Phenylketonurics: Chewable tablets contain phenylalanine, a component of aspartame

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: HIV+ women shouldn't 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

            Inhibits catalytic activity of HIV-1 integrase, an HIV encoded enzyme required for viral replication

            Absorption

            Peak Plasma Time: 3 hr in fasted state

            Distribution

            Protein Bound: 83%

            Metabolism

            Liver

            Elimination

            Half-Life: 9 hr

            Excretion: Feces 51%; urine 32%

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            Images

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            Formulary

            FormularyPatient Discounts

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            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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