dolutegravir (Rx)

Brand and Other Names:Tivicay
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 50mg
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HIV Infection

Indicated in combination with other ARTs

  • Integrase strand transfer inhibitor (INSTI) indicated in combination with other ARTs for treatment of HIV-1 infection in adults and pediatric patients who weigh ≥30 kg
  • Treatment-naïve or treatment-experienced INSTI-naïve: 50 mg PO qDay
  • INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50 mg PO BID

Indicated in combination with rilpivirine

  • Indicated in combination with rilpivirine as a complete regimen for the treatment of HIV-1 infection to replace the current ART regimen in adults who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable ART regimen ≥6 months with no history of treatment failure or known substitutions associated with resistance to dolutegravir or rilpivirine
  • 50 mg PO qDay

Dosage Modifications

Coadministration with potent UGT1A/CYP3A inducers

  • Treatment-naïve or treatment-experienced INSTI-naïve when coadministration with potent UGT1A/CYP3A inducers (eg, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin): Increase dose to 50 mg PO BID

Hepatic impairment

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

Renal impairment

  • Plasma concentrations were decreased in subjects with severe renal impairment
  • No dosage adjustment required for treatment-naïve or treatment-experienced and INSTI-naïve patients with mild, moderate, or severe renal impairment or for INSTI-experienced patients (with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance) with mild or moderate renal impairment
  • Severe renal impairment in for INSTI-experienced patients with resistance: Not recommended; decrease in dolutegravir concentrations may result in loss of therapeutic effect and development of resistance

Dosing Considerations

Poor virologic response was observed in subjects treated with TIVICAY 50 mg BID with an INSTI-resistance Q148 substitution plus 2 or more additional INSTI-resistance substitutions, including L74I/M, E138A/D/K/T, G140A/S, Y143H/R, E157Q, G163E/K/Q/R/S, or G193E/R

In patients with underlying hepatitis B or C, measure hepatic enzymes before initiating therapy and periodically thereafter

Dosage Forms & Strengths

tablet

  • 10mg
  • 25mg
  • 50mg
more...

HIV Infection

Indicated in combination with other ARTs for treatment-naïve or treatment-experienced INSTI-naïve children who weigh ≥0 kg

<30 kg: Safety and efficacy not established

≥30 kg to <40 kg: 35 mg PO qDay (ie, one 25-mg tablet and one 10-mg tablet)

≥40 kg: 50 mg PO qDay

Dosage Modifications

Treatment-naïve or treatment-experienced INSTI-naïve when coadministration with potent UGT1A/CYP3A inducers (eg, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin): Increase weight-based dose to twice daily

Dosing Considerations

Safety and efficacy have not been established in pediatric patients weighing <30 kg or in pediatric patients who are INSTI-experienced with documented or clinically suspected resistance to other INSTIs (ie, raltegravir, elvitegravir)

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Interactions

Interaction Checker

and dolutegravir

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 cholesterol and triglycerides (up to 17%)

            1-10%

            Increased lipase (1-8%)

            Hyperglycemia (<1-7%)

            Increased creatinine kinase (3-4%)

            Increased AST (2-3%)

            Insomnia (<1-3%)

            Increased ALT (2%)

            Increased bilirubin (<1-2%)

            Headache (<1-2%)

            GI disorders (<2%)

            Fatigue (<2%)

            Hepatitis (<2%)

            Myositis (<2%)

            Renal impairment (<2%)

            Pruritus (<2%)

            Nausea (<1-1%)

            <1%

            Abnormal dreams

            Dizziness

            Diarrhea

            Rash

            Vertigo

            Postmarketing Reports

            Arthralgia

            Myalgia

            Hepatobiliary

            Disorders

            Acute liver failure, hepatotoxicity

            Musculoskeletal

            Psychiatric

            Anxiety

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            Warnings

            Contraindications

            Documented hypersensitivity

            Coadministration with dofetilide due to the potential for increased dofetilide plasma concentrations and the risk for serious and/or life-threatening events

            Cautions

            Hypersensitivity reactions reported; characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury (see Contraindications)

            Hepatic adverse events reported; patients with underlying hepatitis B or C may be at increased risk for worsening or development of transaminase elevations; in some cases, transaminase elevations were consistent with immune reconstitution syndrome or hepatitis B reactivation particularly in the setting where antihepatitis therapy was withdrawn

            Hepatic toxicity, including elevated serum liver biochemistries, hepatitis, and acute liver failure reported without pre-existing hepatic disease or other identifiable risk factors; drug-induced liver injury leading to liver transplant reported; monitoring for hepatotoxicity recommended

            Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy; may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, cytomegalovirus, Pneumocystis jiroveci pneumonia [PCP], or tuberculosis) or autoimmune disorders (eg, Graves’ disease, polymyositis, and Guillain-Barre’ syndrome)

            Drug interaction overview

            • Coadministration with certain drugs may result in known or potentially significant drug interactions, some of which may lead to loss of therapeutic effect and possible resistance, or significant adverse reactions of other from increase systemic exposure
            • Inducers of UGT1A1 and CYP3A (eg, oxcarbazepine, phenytoin, phenobarbital, carbamazepine, St John’s wort, rifampin) decrease dolutegravir
            • Coadministration with medications containing polyvalent cations decrease dolutegravir systemic exposure; give dolutegravir 2 hr before or 6 hr after polyvalent cations (eg, antacids, laxatives, sucralfate, iron supplements, calcium supplements, buffered medications)
            • Dolutegravir may increase plasma concentrations of drugs eliminated via OCT2 or MATE1 (dofetilide and metformin)
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            Pregnancy & Lactation

            Pregnancy

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

            There are insufficient human data on use during pregnancy to inform a drug-associated risk of birth defects and miscarriage; given the limited number of pregnancies exposed to dolutegravir-based regimens reported to APR, no definitive conclusions can be drawn on safety in pregnancy, and continued monitoring is ongoing through the APR

            In animal reproduction studies, no evidence of adverse developmental outcomes was observed during organogenesis

            Lactation

            The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection; not known whether drug is present in human breast milk, affects human milk production, or has effects on breastfed infant; when administered to lactating rats, dolutegravir was present in milk

            Because of potential for (1) HIV-1 transmission (in HIV-negative infants), and (2) developing viral resistance (in HIV-positive infants), instruct mothers not to breastfeed if they are receiving drug therapy

            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

            Integrase strand transfer inhibitor (INSTI); inhibits catalytic activity of HIV-1 integrase, an HIV encoded enzyme required for viral replication

            Absorption

            Peak plasma time: 2-3 hr

            Peak plasma concentration: 3.67-4.15 mcg/mL

            AUC 53.6-75.1 mcg•h/mL

            Distribution

            Protein bound: ≥98.9%

            Vd: 17.4 L; 4-232 ng/mL (CSF)

            Metabolism

            Metabolized by UGT1A1 with some contribution from CYP3A

            Elimination

            Half-life: 14 hr

            Clearance: 1 L/hr

            Excretion: 53% feces (unchanged); 31% urine (as ether glucuronide, benzylic carbon, or N-dealkylation product); <1% urine (unchanged)

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            Administration

            Oral Administration

            May take with or without food

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            Images

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            Formulary

            FormularyPatient Discounts

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
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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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