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dolutegravir (Tivicay, DTG)

Indications: - for use in combination with other antiretrovral agents (tenofovir (TDF) & lamivudine (3TC) or tenofovir (TDF) & emtricitabine (FTC) in treatment of HIV1 patients age 12 and older at least 40 kg who have not previously taken an integrase inhibitor [1] - dolutegravir is more effective, has fewer side effects, is easier to take, and is less likely to develop drug resistance compared with other antiretroviral drugs [5] - WHO recommends dolutegravir as the preferred 1st- & 2nd-line HIV1 treatment for all patients, including pregnant women & those of childbearing age [5] Contraindications: * previously avoid during pregnancy (data insufficient) [2] or conception [4] * WHO has determined that dolutegravir is safe during pregancny [5] Dosage: - PO QD Adverse effects: common - insomnia - headache - increase in serum creatinine due to decrease in tubular secretion, not GFR [3] - otherwise well tolerated [3] serious - hypersensitivity reactions - abnormal liver function in participants co-infected with hepatitis B &/or hepatitis C increased risk of neural tube defects in babies born to women who became pregnant while receiving the drug [4] Mechanism of action: - integrase strand transfer inhibitor

Interactions

drug adverse effects of antiretroviral agents

General

integrase inhibitor; integrase strand transfer inhibitor (InSTI)

Database Correlations

PUBCHEM correlations

References

  1. FDA News Release: Aug. 12, 2013 FDA approves new drug to treat HIV infection
  2. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  3. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  4. Sax PE Why the Dolutegravir Pregnancy Warning is Important - and What We Should Do Now NEJM Journal Watch. HIV and ID Observations. May 21, 2018 https://blogs.jwatch.org/hiv-id-observations/index.php/dolutegravir-pregnancy-warning-important-now/2018/05/20/
  5. World Health Organization (WHO). News Release. July 22, 2019 WHO recommends dolutegravir as preferred HIV treatment option in all populations. https://www.who.int/news-room/detail/22-07-2019-who-recommends-dolutegravir-as-preferred-hiv-treatment-option-in-all-populations - Zash R, Holmes L, Diseko M et al Neural-Tube Defects and Antiretroviral Treatment Regimens in Botswana. N Engl J Med. July 22, 2019 PMID: 31329379 https://www.nejm.org/doi/full/10.1056/NEJMoa1905230 - Raesima MM, Ogbuabo CM, Thomas V et al Dolutegravir Use at Conception - Additional Surveillance Data from Botswana. N Engl J Med. July 22, 2019 PMID: 31329378

Component-of

abacavir/dolutegravir/lamivudine dolutegravir/lamivudine (Dovato) dolutegravir/lamivudine/tenofovir dolutegravir/rilpivirine (Juluca)