Version July 2025
HIV-1 infection, treatment: Note: Must be given in combination with other antiretroviral agents.
Treatment naive or treatment-experienced integrase strand transfer inhibitor (INSTI)-naive: Oral: 50 mg once daily.
Treatment naive or treatment-experienced INSTI-naive when coadministered with carbamazepine, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin: Oral: 50 mg twice daily.
INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: Oral: 50 mg twice daily.
Virologically suppressed (HIV-1 RNA <50 copies/mL) patients switching to dolutegravir plus rilpivirine: Oral: 50 mg once daily.
HIV-1 infection, postexposure prophylaxis (off-label use): Oral: 50 mg once daily for 28 days (in combination with other antiretroviral agents). Initiate therapy within 72 hours of exposure (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Note: Patients with CrCl <30 mL/minute exhibited reduced dolutegravir exposures (~40%) in a single-dose pharmacokinetic study (Ref); the mechanism for this is unknown and no dosage adjustments have been proposed (Ref); however, use with caution in integrase strand transfer inhibitor (INSTI)–experienced patients (with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance) (Ref).
Altered kidney function: Oral: No dosage adjustment necessary for any degree of kidney dysfunction (Ref).
Hemodialysis, intermittent (thrice weekly): Minimally dialyzable (~7%) (Ref):
Oral: No supplemental dose or dosage adjustment necessary (Ref).
Peritoneal dialysis: Not expected to be significantly dialyzable (Ref):
Oral: No dosage adjustment necessary (Ref).
CRRT: Oral: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): Oral: No dosage adjustment necessary (Ref).
Mild-to-moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.
Severe impairment (Child-Pugh class C): Use is not recommended (has not been studied).
Refer to adult dosing; use with caution.
(For additional information see "Dolutegravir: Pediatric drug information")
Note: Dolutegravir tablets (Tivicay) and soluble tablets for oral suspension (Tivicay PD) are not bioequivalent and are not substitutable on a mg per mg basis.
HIV-1 infection, treatment: Note: Use in combination with other antiretroviral (ARV) agents. Gene mutation and ARV resistance patterns should be evaluated (refer to https://www.iasusa.org for more information) when necessary.
Treatment-naive or treatment-experienced and integrase strand transfer inhibitor (INSTI)-naive:
Infants and Children weighing 3 to <14 kg: Oral:
Soluble tablets for oral suspension (Tivicay PD):
3 to <6 kg: 5 mg once daily.
6 to <10 kg: 15 mg once daily.
10 to <14 kg: 20 mg once daily.
Infants, Children, and Adolescents weighing ≥14 kg: Oral:
Soluble tablets for oral suspension (Tivicay PD): Preferred in patients <20 kg:
14 to <20 kg: 25 mg once daily.
≥20 kg: 30 mg once daily.
Tablets (Tivicay):
14 to <20 kg: 40 mg once daily.
≥20 kg: 50 mg once daily.
INSTI-experienced with any INSTI-associated resistance mutation or clinically suspected INSTI resistance: Limited data available (Ref):
Children and Adolescents weighing ≥40 kg: Oral: Tablets (Tivicay): 50 mg twice daily.
HIV-1 nonoccupational postexposure prophylaxis (nPEP): Limited data available (Ref): Adolescents weighing ≥40 kg: Oral: Tablets (Tivicay): 50 mg once daily for 28 days in combination with other antiretroviral agents. Initiate therapy within 72 hours of exposure.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Treatment-naive or treatment-experienced integrase strand transfer inhibitor (INSTI)-naive: Infants, Children, and Adolescents: Mild, moderate, or severe impairment: No dosage adjustment required.
INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: There are no dosage adjustments in the manufacturer's labeling; based on experience in adult patients, use with caution in severe renal impairment since the reduction in dolutegravir concentrations may result in loss of therapeutic effect and development of resistance to dolutegravir or other coadministered antiretroviral agents.
End-stage renal disease including hemodialysis: There are no dosage adjustments in the manufacturer's labeling (has not been studied).
Infants, Children, and Adolescents:
Baseline:
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Not recommended (has not been studied).
Hepatoxicity during therapy: If asymptomatic hepatitis, consider discontinuation of therapy for ALT or AST >5 times ULN; if symptomatic hepatitis, discontinue therapy (Ref).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported with combination therapy.
>10%: Gastrointestinal: Increased serum lipase (2% to 11%)
1% to 10%:
Dermatologic: Pruritus (<2%)
Endocrine & metabolic: Hyperglycemia (≤9%)
Gastrointestinal: Abdominal distress (<2%), abdominal pain (<2%), diarrhea (≤2%), flatulence (<2%), nausea (≤1%), upper abdominal pain (<2%), vomiting (<2%)
Hematologic & oncologic: Neutropenia (4%; grades 3/4: 2% to 3%)
Hepatic: Hepatitis (<2%), hyperbilirubinemia (≤3%), increased serum alanine aminotransferase (1% to 4%), increased serum aspartate aminotransferase (1% to 5%)
Nervous system: Depression (≤1%), fatigue (≤2%), headache (≤2%), insomnia (≤7%), suicidal ideation (<2%), suicidal tendencies (<2%)
Neuromuscular & skeletal: Increased creatinine phosphokinase in blood specimen (2% to 7%), myositis (<2%)
Renal: Renal insufficiency (<2%)
<1%:
Dermatologic: Skin rash
Hypersensitivity: Hypersensitivity reaction
Nervous system: Abnormal dreams, dizziness
Frequency not defined:
Endocrine & metabolic: Increased HDL cholesterol, increased LDL cholesterol, increased serum cholesterol, increased serum triglycerides
Renal: Increased serum creatinine
Postmarketing:
Endocrine & metabolic: Diabetes mellitus (Hirigo 2022, O’Halloran 2022), weight gain
Hepatic: Acute hepatic failure, hepatotoxicity
Immunologic: Immune reconstitution syndrome
Nervous system: Anxiety
Neuromuscular & skeletal: Arthralgia, myalgia
Hypersensitivity to dolutegravir or any component of the formulation; concurrent use with dofetilide.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Concurrent use with organic cation transporter 2 substrates with narrow therapeutic windows (eg, fampridine).
Concerns related to adverse effects:
• Hepatotoxicity: Hepatic adverse events, including elevated serum liver biochemistries, hepatitis, and acute liver failure, have been reported; these events have occurred in patients without underlying hepatic disease or other risk factors. Patients with hepatitis B or C may be at increased risk for worsening or development of increased transaminases; sometimes these increases were consistent with immune reconstitution syndrome or hepatitis B reactivation (particularly when anti-hepatitis therapy was withdrawn). Drug-induced liver injury has been reported with dolutegravir in combination with abacavir and lamivudine. Monitor patients for signs/symptoms of hepatotoxicity.
• Hypersensitivity reactions: Rash, constitutional findings, and organ dysfunction (eg, liver injury) have been reported. Discontinue immediately if signs of hypersensitivity (eg, severe rash, rash with fever, malaise, fatigue, muscle/joint aches, blistering or peeling of skin, oral blisters/lesions, conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing) occur. Monitor clinical status and liver function tests, and initiate supportive therapy as appropriate. If hypersensitivity occurs, do not reinitiate therapy with dolutegravir.
• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.
Disease-related concerns:
• Hepatic impairment: Not recommended for use in patients with severe hepatic impairment (has not been studied).
• Renal impairment: Use with caution in integrase strand transfer inhibitor (INSTI)-experienced patients with severe renal impairment; decreases in dolutegravir concentrations were observed and may result in loss of therapeutic effect and development of resistance to dolutegravir or other coadministered antiretroviral agents.
Dosage form specific issues:
• Product interchangeability: Dolutegravir tablets and soluble tablets for oral suspension (Tivicay PD) are not bioequivalent and not interchangeable on a milligram-per-milligram basis. If a patient switches from one formulation to another, adjust dose for the new dosage formulation. Incorrect dosing may result in underdosing, loss of therapeutic effect, and possible development of resistance, or adverse reactions from increased exposure to dolutegravir.
Other warnings/precautions:
• Appropriate use: Use in INSTI-experienced patients should be guided by the number and type of baseline INSTI substitutions. Efficacy with 50 mg twice daily is reduced in patients with an INSTI-resistance Q148 substitution plus 2 or more additional INSTI-resistance substitutions, including T66A, L74I/M, E138A/K/T, G140S/A/C, Y143R/C/H, E157Q, G163S/E/K/Q, or G193E/R.
• False elevations in serum creatinine: May inhibit tubular secretion of creatinine without affecting actual renal glomerular function; observed onset was within the first 4 weeks of therapy followed by stability through at least 96 weeks. Use caution when interpreting serum creatinine values in patients with medical conditions or receiving drugs needing to be monitored with estimated CrCl.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
Tivicay: 10 mg [DSC], 25 mg [DSC], 50 mg
Tablet Soluble, Oral:
Tivicay PD: 5 mg
No
Tablet,Dispersible (Tivicay PD Oral)
5 mg (per each): $9.30
Tablets (Tivicay Oral)
50 mg (per each): $93.01
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
Tivicay: 10 mg [DSC], 25 mg [DSC], 50 mg
Tablet Soluble, Oral:
Tivicay: 5 mg
Oral: Administer without regard to meals. Administer 2 hours before or 6 hours after cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications. Alternatively, dolutegravir and supplements containing calcium or iron can be taken together with food.
Oral: May be administered without regard to meals. Take 2 hours before or 6 hours after cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications. Alternatively, dolutegravir and supplements containing calcium or iron can be taken together with food.
Soluble tablets (Tivicay PD): May be administered dispersed in water as an oral suspension or swallowed whole. If swallowing whole, do not swallow more than 1 tablet at a time to reduce risk for choking. Do not chew, cut, or crush tablets.
Oral suspension preparation: Fill provided cup with 5 mL (if using ≤3 tablets) or 10 mL (if using 4 to 6 tablets) of drinking water; add tablets to water and swirl the suspension gently for 1 to 2 minutes so that no lumps remain (will have cloudy appearance); administer using provided oral syringe in infants or directly from cup in children; to ensure the full dose is received, add another 5 mL of water to the cup, swirl, and administer from cup directly (children) or pull up remaining liquid into oral syringe for infants. Administer within 30 minutes of mixing. If any medication is spilled during preparation, discard dose and prepare a new dose.
Tablets (Tivicay): For patients that have difficulty swallowing tablets whole, tablets may be split into halves (with both halves then administered) or crushed, added to a small amount of semisolid food or liquid, and consumed immediately (Ref).
HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents in treatment-naïve or -experienced adult patients and treatment-naïve or -experienced pediatric patients (but integrase strand transfer inhibitor naïve) at least 4 weeks of age and weighing at least 3 kg, or in combination with rilpivirine in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies per mL) on a stable antiretroviral regimen for at least 6 months with no history of treatment failure or known substitutions associated with resistance to either antiretroviral agent.
HIV-1 infection, postexposure prophylaxis
Substrate of BCRP, CYP3A4 (Minor), P-glycoprotein (Minor), UGT1A1, UGT1A3, UGT1A9; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits MATE1/2-K, OCT2;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Aluminum Hydroxide: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral aluminum hydroxide. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after oral aluminum hydroxide. Risk D: Consider Therapy Modification
Antidiabetic Agents: Hyperglycemia-Associated Agents may decrease therapeutic effects of Antidiabetic Agents. Risk C: Monitor
Atazanavir: May increase serum concentration of UGT1A1 Substrates. Management: Do not use UGT1A1 substrates for which small increases in exposure can cause serious adverse effects together with atazanavir, and use caution with any UGT1A1 substrate, even when small changes in exposure are less likely to cause serious adverse effects. Risk D: Consider Therapy Modification
Atidarsagene Autotemcel: Antiretroviral Agents may decrease therapeutic effects of Atidarsagene Autotemcel. Risk X: Avoid
Belumosudil: May increase serum concentration of UGT1A1 Substrates. Management: Avoid coadministration of belumosudil with substrates of UGT1A1 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the UGT1A1 substrate may be required. Risk D: Consider Therapy Modification
Betibeglogene Autotemcel: Antiretroviral Agents may decrease therapeutic effects of Betibeglogene Autotemcel. Risk X: Avoid
Calcium Salts: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral calcium. Administer dolutegravir/rilpivirine at least 4 hours before or 6 hours after oral calcium salts. Alternatively, dolutegravir and oral calcium can be taken together with food. Risk D: Consider Therapy Modification
CarBAMazepine: May decrease serum concentration of Dolutegravir. Management: Increase dolutegravir to 50 mg twice/day in adults. Increase weight-based dose to twice daily in pediatric patients. Specific recommendations vary for combination products; see interaction monograph for details. Risk D: Consider Therapy Modification
Clofarabine: OCT2 Inhibitors may increase serum concentration of Clofarabine. Risk C: Monitor
Dalfampridine: OCT2 Inhibitors may increase serum concentration of Dalfampridine. Management: Consider alternatives to this combination. Carefully weigh the risk of seizures against the benefit of combining OCT2 inhibitors with dalfampridine. Risk D: Consider Therapy Modification
Dofetilide: Dolutegravir may increase serum concentration of Dofetilide. Risk X: Avoid
Efavirenz: May decrease serum concentration of Dolutegravir. Management: Increase dolutegravir to 50 mg twice/day in adults. Increase weight-based dose to twice daily in pediatric patients. Recommendations vary for combo products; see interaction monograph for details. Not recommended with Dovato or Juluca brand combos. Risk D: Consider Therapy Modification
Elivaldogene Autotemcel: Antiretroviral Agents may decrease therapeutic effects of Elivaldogene Autotemcel. Management: Avoid use of antiretroviral medications for at least one month, or for the amount of time required for elimination of the retroviral medication, prior to stem cell mobilization and until the all apheresis cycles are finished Risk X: Avoid
Etravirine: May decrease serum concentration of Dolutegravir. Management: Avoid etravirine with dolutegravir unless with atazanavir/ritonavir, darunavir/ritonavir or lopinavir/ritonavir; avoid use with Dovato brand combination. Canada recommends using dolutegravir 50 mg twice daily when with etravirine. Risk D: Consider Therapy Modification
Fosamprenavir: May decrease serum concentration of Dolutegravir. Specifically, Fosamprenavir/Ritonavir may decrease the serum concentration of Dolutegravir. The individual contributions of Fosamprenavir and Ritonavir to this effect are unknown. Management: Increase dolutegravir to 50 mg twice/day in adults. Increase weight-based dose to twice daily in pediatric patients. Recommendations vary for combo products; see interaction monograph for details. Not recommended with Dovato or Juluca brand combos. Risk D: Consider Therapy Modification
Fosphenytoin-Phenytoin: May decrease serum concentration of Dolutegravir. Risk X: Avoid
Iron Preparations: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral iron. Administer dolutegravir/rilpivirine at least 4 hours before or 6 hours after oral iron. Alternatively, dolutegravir and oral iron can be taken together with food. Risk D: Consider Therapy Modification
Isoniazid: Dolutegravir may increase adverse/toxic effects of Isoniazid. Dolutegravir may increase serum concentration of Isoniazid. Risk C: Monitor
Lovotibeglogene Autotemcel: Antiretroviral Agents may decrease therapeutic effects of Lovotibeglogene Autotemcel. Risk X: Avoid
Magnesium Salts: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral magnesium salts. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after oral magnesium salts. Risk D: Consider Therapy Modification
MetFORMIN: Dolutegravir may increase serum concentration of MetFORMIN. Management: Consider alternatives to this combination or use of lower metformin doses. Carefully weigh the risk of metformin toxicities (including lactic acidosis) against the benefit of combining dolutegravir with metformin. Risk D: Consider Therapy Modification
Mitapivat: May decrease serum concentration of UGT1A1 Substrates. Risk C: Monitor
Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after multivitamins. Administer the dolutegravir/rilpivirine product at least 4 hours before or 6 hours multivitamins. Alternatively, dolutegravir and multivitamins can be taken together with food Risk D: Consider Therapy Modification
Multivitamins/Minerals (with AE, No Iron): May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after multivitamins. Administer the dolutegravir/rilpivirine product at least 4 hours before or 6 hours multivitamins. Alternatively, dolutegravir and multivitamins can be taken together with food Risk D: Consider Therapy Modification
Nevirapine: May decrease serum concentration of Dolutegravir. Management: Prescribing information suggests avoiding the concomitant use of dolutegravir and nevirapine. HIV treatment guidelines suggest these drugs can be combined without dose adjustment. Monitor for reduced dolutegravir concentrations/effects if combined. Risk D: Consider Therapy Modification
Orlistat: May decrease serum concentration of Antiretroviral Agents. Risk C: Monitor
OXcarbazepine: May decrease serum concentration of Dolutegravir. Risk X: Avoid
PHENobarbital: May decrease serum concentration of Dolutegravir. Risk X: Avoid
Pilsicainide: Dolutegravir may increase serum concentration of Pilsicainide. Management: Consider alternatives to this combination if possible. Risk D: Consider Therapy Modification
Primidone: May decrease serum concentration of Dolutegravir. Specifically, the Primidone metabolite phenobarbital may decrease Dolutegravir serum concentrations. Risk X: Avoid
Rifabutin: May decrease serum concentration of Dolutegravir. Risk C: Monitor
RifAMPin: May decrease serum concentration of Dolutegravir. Management: Increase dolutegravir to 50 mg twice/day in adults. Increase weight-based dose to twice daily in pediatric patients. Specific recommendations vary for combination products; see interaction monograph for details. Risk D: Consider Therapy Modification
Rifapentine: Dolutegravir may increase adverse/toxic effects of Rifapentine. Rifapentine may decrease serum concentration of Dolutegravir. Risk C: Monitor
Selenium: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral selenium. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after oral selenium. Risk D: Consider Therapy Modification
St John's Wort: May decrease serum concentration of Dolutegravir. Risk X: Avoid
Sucralfate: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after sucralfate. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after sucralfate. Risk D: Consider Therapy Modification
Tipranavir: May decrease serum concentration of Dolutegravir. Specifically, Tipranavir/Ritonavir may decrease the serum concentration of Dolutegravir. The individual contributions of Tipranavir and Ritonavir to this effect are unknown. Management: Increase dolutegravir to 50 mg twice/day in adults. Increase weight-based dose to twice daily in pediatric patients. Recommendations vary for combo products; see interaction monograph for details. Not recommended with Dovato or Juluca brand combos. Risk D: Consider Therapy Modification
Valproic Acid and Derivatives: May decrease serum concentration of Dolutegravir. Risk C: Monitor
Zinc Salts: May decrease serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after oral zinc salts. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after oral zinc salts. Risk D: Consider Therapy Modification
Contraception is not required to initiate or continue antiretroviral therapy.
Dolutegravir is a preferred integrase strand transfer inhibitor (INSTI) for patients with HIV who are not yet pregnant but are trying to conceive. Use is not recommended in persons with prior use of long acting cabotegravir for preexposure prophylaxis unless INSTI genotype testing shows no INSTI-resistance mutations.
Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Prior to pregnancy, select or make changes to a specific antiretroviral regimen as part of a shared decision-making process. In most cases, recommendations based on data obtained from cisgender women can be applied to transgender and gender diverse people assigned female sex at birth.
Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2024).
Dolutegravir has a high level of transfer across the human placenta.
No increased risk of overall teratogenic effects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry.
Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth weight, and small for gestational age infants. High viral loads are also associated with adverse outcomes, including preterm birth and pregnancy loss. Treatment improves the health of the pregnant patient and reduces the risk of perinatal transmission. Do not withhold appropriate maternal ART due to concerns for adverse neonatal outcomes. Closely monitor for pregnancy complications. Document in utero ART exposure in the long-term medical record of a child born without HIV; evaluate for potential metabolic dysfunction if significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) develop.
Dolutegravir is a preferred integrase strand transfer inhibitor (INSTI) for pregnant patients with HIV who are antiretroviral-naive, who have had ART therapy in the past but are restarting, and who require a new ART regimen (due to poor tolerance or poor virologic response of current regimen). Patients who become pregnant while taking dolutegravir may continue if viral suppression is effective and the regimen is well tolerated. Use is not recommended in persons with prior use of long acting cabotegravir for preexposure prophylaxis unless INSTI genotype testing shows no INSTI-resistance mutations. Dolutegravir is also a preferred component of an initial regimen when early (acute/recent) HIV infection is detected during pregnancy (regardless of trimester) in persons without prior use of long acting cabotegravir for preexposure prophylaxis.
Dolutegravir in combination with abacavir and lamivudine is a preferred INSTI regimen for initial therapy in antiretroviral-naive pregnant patients. INSTIs can rapidly suppress viral load. A regimen with dolutegravir may be useful when drug interactions or the potential for preterm delivery with protease inhibitors are a concern. In addition, use of dolutegravir may be beneficial in patients with HIV who are not on ART and present for care late in pregnancy.
Pharmacokinetics of dolutegravir may be altered, but dose adjustments are not needed during pregnancy.
ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of an ultrasensitive assay detection, and reduce the risk of perinatal transmission. Start ART prior to conception or as soon as possible during pregnancy. During pregnancy, select or make changes to a specific antiretroviral regimen as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitor pregnant patients more frequently than nonpregnant patients. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations based on data obtained from cisgender women can be applied to transgender and gender diverse people assigned female sex at birth.
Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Enroll all patients exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263).
Health care providers caring for pregnant patients with HIV infection and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2024).
Dolutegravir is present in breast milk.
Dolutegravir is a recommended component of an initial regimen for early (acute/recent) HIV infection in postpartum patients. Interrupt breastfeeding immediately if seroconversion is suspected and do not continue if infection is diagnosed. Breast milk may be expressed and stored while waiting for test results.
Provide patient-centered evidence-based counseling for infant feeding options as early as possible in pregnancy.
• Using properly prepared formula or pasteurized banked donor milk eliminates the risk of postnatal HIV transmission via breastfeeding.
• Counsel patients on antiretroviral therapy (ART) who achieve and maintain a consistently undetectable plasma viral load during pregnancy and postnatally about feeding options, including breastfeeding, formula feeding, or banked donor milk. Maintaining maximum viral suppression decreases but does not eliminate the risk of HIV transmission via breast milk. Temporary discontinuation of breastfeeding and use of replacement feeding may be required if maternal viral load becomes detectable or if mastitis or bleeding nipples develop. Permanent discontinuation of breastfeeding is recommended if the maternal HIV RNA is ≥200 copies/mL.
• Formula feeding or banked donor milk is recommended for persons with HIV who are not on ART and/or do not have sustained viral suppression. Provide the infant presumptive ART throughout breastfeeding and for up to 6 weeks after the last exposure to breast milk if the breastfeeding parent does not have sustained viral suppression but breastfeeding is continued; conduct infant virologic diagnostic testing at specified intervals.
• When the HIV status at delivery is not known, breast milk may be expressed and stored until a negative test is available.
• Discontinue breastfeeding immediately if HIV infection is diagnosed after breastfeeding has been initiated.
• Evaluate and provide support for maternal conditions that would make adherence to postpartum ART difficult.
Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations based on data obtained from cisgender women can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2024).
Take 2 hours before or 6 hours after cation-containing antacids or laxatives, sucralfate, oral supplements containing iron or calcium, or buffered medications. Alternatively, dolutegravir and supplements containing calcium or iron can be taken together with food.
Viral load, CD4 count, lipid profile; liver aminotransferases (baseline and during therapy); monitor for hypersensitivity.
Binds to the integrase active site and inhibits the strand transfer step of HIV-1 DNA integration necessary for the HIV replication cycle.
Note: The pharmacokinetics of dolutegravir in HIV-1-infected pediatric patients ≥4 weeks of age weighing ≥3 kg were similar to those observed in HIV-1-infected adults.
Absorption: Food increased the extent of absorption and slowed the rate of absorption of dolutegravir. Low-, moderate-, and high-fat meals increased dolutegravir AUC by 33%, 41%, and 66%, respectively; increased Cmax by 46%, 52%, and 67%, respectively; and prolonged Tmax to 3, 4, and 5 hours from 2 hours under fasted conditions, respectively.
Distribution: Vd/F = ~17.4 L.
Protein binding: ≥98.9%.
Metabolism: Primarily metabolized via UGT1A1 with some contribution from CYP3A.
Bioavailability: The relative bioavailability of the oral suspension is ~1.6-fold higher than the tablets.
Half-life elimination: ~14 hours.
Time to peak: 1 to 3 hours.
Excretion: Feces (53% as unchanged drug); urine (31% as metabolites, <1% as unchanged drug).
