Dolutegravir
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]
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Overview
Dolutegravir is a antiviral that is FDA approved for the treatment of HIV-1 infection. Common adverse reactions include {{{adverseReactions}}}.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Dolutegravir in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Dolutegravir in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Treatment-naïve or Treatment-experienced INSTI-naïve
The recommended dose of TIVICAY in pediatric patients aged 12 years and older and weighing at least 40 kg is 50 mg administered orally once daily.
If efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin are coadministered, the recommended dose of TIVICAY is 50 mg twice daily.
Safety and efficacy of TIVICAY have not been established in pediatric patients younger than 12 years or weighing less than 40 kg, or in pediatric patients who are INSTI-experienced with documented or clinically suspected resistance to other INSTIs (raltegravir, elvitegravir).
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Dolutegravir in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Dolutegravir in pediatric patients.
Contraindications
TIVICAY is contraindicated in patients:
- with previous hypersensitivity reaction to dolutegravir
- receiving dofetilide due to the potential for increased dofetilide plasma concentrations and the risk for serious and/or life-threatening events.
Warnings
Hypersensitivity Reactions
Hypersensitivity reactions have been reported and were characterized by rash, constitutional findings, and sometimes organ dysfunction, including liver injury. The events were reported in less than 1% of subjects receiving TIVICAY in Phase 3 clinical trials. Discontinue TIVICAY and other suspect agents immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters or peeling of the skin, oral blisters or lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing). Clinical status, including liver aminotransferases, should be monitored and appropriate therapy initiated. Delay in stopping treatment with TIVICAY or other suspect agents after the onset of hypersensitivity may result in a life-threatening reaction. TIVICAY is contraindicated in patients who have experienced a previous hypersensitivity reaction to dolutegravir.
Effects on Serum Liver Biochemistries in Patients with Hepatitis B or C Coinfection
Patients with underlying hepatitis B or hepatitis C may be at increased risk for worsening or development of transaminase elevations with use of TIVICAY. In some cases the elevations in transaminases were consistent with immune reconstitution syndrome or hepatitis B reactivation particularly in the setting where anti-hepatitis therapy was withdrawn. Appropriate laboratory testing prior to initiating therapy and monitoring for hepatotoxicity during therapy with TIVICAY are recommended in patients with underlying hepatic disease such as hepatitis B or hepatitis C.
Fat Redistribution
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. The mechanism and long-term consequences of these events are currently unknown. A causal relationship has not been established.
Immune Reconstitution Syndrome
Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including TIVICAY. During the initial phase of combination antiretroviral treatment, patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia [[[PCP]]], or tuberculosis), which may necessitate further evaluation and treatment.
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.
Adverse Reactions
Clinical Trials Experience
Treatment‑emergent Adverse Drug Reactions (ADRs)
Treatment-naïve Subjects: The safety assessment of TIVICAY in HIV‑1‑infected treatment-naïve subjects is based on the analyses of 96-week data from 2 international, multicenter, double-blind trials, SPRING-2 (ING113086) and SINGLE (ING114467) and 48-week data from the international, multicenter, open-label FLAMINGO (ING114915) trial.
In SPRING-2, 822 subjects were randomized and received at least 1 dose of either TIVICAY 50 mg once daily or raltegravir 400 mg twice daily, both in combination with fixed-dose dual nucleoside reverse transcriptase inhibitor (NRTI) treatment (either abacavir sulfate and lamivudine [EPZICOM®] or emtricitabine/tenofovir [TRUVADA®]). There were 808 subjects included in the efficacy and safety analyses. Through 96 weeks, the rate of adverse events leading to discontinuation was 2% in both treatment arms.
In SINGLE, 833 subjects were randomized and received at least 1 dose of either TIVICAY 50 mg with fixed-dose abacavir sulfate and lamivudine (EPZICOM) once daily or fixed-dose efavirenz/emtricitabine/tenofovir (ATRIPLA®) once daily. Through 96 weeks, the rates of adverse events leading to discontinuation were 3% in subjects receiving TIVICAY 50 mg once daily + EPZICOM and 12% in subjects receiving ATRIPLA once daily.
Treatment-emergent ADRs of moderate to severe intensity observed in at least 2% of subjects in either treatment arm in SPRING-2 and SINGLE trials are provided in Table 2. Side-by-side tabulation is to simplify presentation; direct comparisons across trials should not be made due to differing trial designs.
Postmarketing Experience
There is limited information regarding Dolutegravir Postmarketing Experience in the drug label.
Drug Interactions
There is limited information regarding Dolutegravir Drug Interactions in the drug label.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Dolutegravir in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Dolutegravir in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Dolutegravir during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Dolutegravir in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Dolutegravir in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Dolutegravir in geriatric settings.
Gender
There is no FDA guidance on the use of Dolutegravir with respect to specific gender populations.
Race
There is no FDA guidance on the use of Dolutegravir with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Dolutegravir in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Dolutegravir in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Dolutegravir in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Dolutegravir in patients who are immunocompromised.
Administration and Monitoring
Administration
There is limited information regarding Dolutegravir Administration in the drug label.
Monitoring
There is limited information regarding Dolutegravir Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Dolutegravir and IV administrations.
Overdosage
There is limited information regarding Dolutegravir overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Dolutegravir Pharmacology in the drug label.
Mechanism of Action
There is limited information regarding Dolutegravir Mechanism of Action in the drug label.
Structure
There is limited information regarding Dolutegravir Structure in the drug label.
Pharmacodynamics
There is limited information regarding Dolutegravir Pharmacodynamics in the drug label.
Pharmacokinetics
There is limited information regarding Dolutegravir Pharmacokinetics in the drug label.
Nonclinical Toxicology
There is limited information regarding Dolutegravir Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Dolutegravir Clinical Studies in the drug label.
How Supplied
There is limited information regarding Dolutegravir How Supplied in the drug label.
Storage
There is limited information regarding Dolutegravir Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Dolutegravir Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Dolutegravir interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Dolutegravir Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Dolutegravir Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.