What are the adverse effects of integrase strand-transfer inhibitors in antiretroviral therapy of HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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As an antiretroviral class, INSTIs have a favorable safety and tolerability profile.  Common adverse effects include mild to moderate gastrointestinal effects (e.g., nausea, diarrhea) and headache. Drug-related insomnia may occur in up to 3.5% of patients receiving dolutegravir and 4% receiving raltegravir; hypersensitivity reactions, depression, and suicidal ideation may also occur in rare instances. [8, 85, 89]   

Elevations in creatine kinase levels (grade 2-4) were observed with raltegravir in phase III studies, along with rare cases of myopathy and rhabdomyolysis. [90, 85]  Raltegravir should be used with caution in patients receiving other medications that may increase the risk for myopathy and rhabdomyolysis. [85]

A relative risk of malignancy of 1.2 cases per 100 patient-years (95% CI, 0.4-4.1) has been reported in phase II and phase III clinical studies of raltegravir and requires continued surveillance. [90]  

Minor elevation in serum creatinine concentrations (0.1-0.2 mg/dL) is observed following initiation of dolutegravir, bictegravir, and elvitegravir regimens that contain cobicistat as a result of inhibition of renal transport proteins (OCT2, MATE1), leading to decreased clearance of creatinine by tubular secretion. [84, 87]

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