2016•American Journal of Health-System PharmacyRequires access

Virological suppression after use of crushed tenofovir–emtricitabine and dolutegravir tablets in a patient with HIV infection

Lindsey Buscemi

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Abstract

Management of human immunodeficiency virus (HIV) in treatment-naive patients requires combination antiretroviral therapy, with a preferred recommendation including tenofovir, emtricitabine, and dolutegravir.1 While this regimen has demonstrated efficacy in treatment-naive HIV-infected patients, published evidence is limited in patients who cannot ingest oral tablets.1,2 The successful management of HIV and virological suppression in patients using crushed formulations has been previously described.3,–5 Currently, data are limited regarding the use of crushed formulations of dolutegravir. While a recent pharmacokinetic study determined that the bioavailability of dolutegravir granules can exceed that of the tablet formulation, clinical data in HIV-infected patients are lacking.6 We describe a successful virological response in an HIV-infected treatment-naive patient to crushed dolutegravir tablets, taken with coformulated tenofovir–emtricitabine. A 30-year-old African-American man began receiving care after receiving a diagnosis of HIV infection. He had a baseline viral load of 10,800 copies/mL and a CD4 T-lymphocyte count of 466 cells/mm3. Baseline genotyping showed the following mutations: K103S, R211K, L10I, L63Q, I64V, and V771. The patient was taking no medications before this diagnosis, and his medical history was limited. At his initial visit, the patient described lifelong difficulty swallowing medications and indicated that he would prefer a formulation that he could crush. After the results of the patient’s laboratory test were received, the patient was initiated on the fixed-dose combination tablet of tenofovir disoproxil fumarate 300 mg with emtricitabine 200 mg once daily as well as one dolutegravir 50-mg tablet daily. The patient reported pulverizing the tenofovir–emtricitabine and dolutegravir tablets with a pill crusher, adding the powder to applesauce, and swallowing the mixture immediately. The patient returned to the clinic four weeks after the initiation of therapy and reported that he experienced no adverse effects from the medications, took all doses, and was having success crushing the formulations. The viral load during this visit was reported as “none detected” (<20 copies/mL), and the CD4 T-lymphocyte count was 583 cells/mm3. Continued medication adherence was encouraged, and the patient was scheduled for routine follow-up after achieving virological suppression.

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What this paper is about

Management of human immunodeficiency virus (HIV) in treatment-naive patients requires combination antiretroviral therapy, with a preferred recommendation including tenofovir, emtricitabine, and dolutegravir.1 While this regimen has demonstrated efficacy in treatment-naive HIV-infected patients, published evidence is limited in patients who cannot ingest oral tablets.1,2 The successful management of HIV and virological suppression in patients using crushed formulations has been previously described.3,–5 Currently, data are limited regarding the use of crushed formulations of dolutegravir. While a recent pharmacokinetic study determined that the bioavailability of dolutegravir granules can exceed that of the tablet formulation, clinical data in HIV-infected patients are lacking.6 We describe a successful virological response in an HIV-infected treatment-naive patient to crushed dolutegravir tablets, taken with coformulated tenofovir–emtricitabine. A 30-year-old African-American man began receiving care after receiving a diagnosis of HIV infection. He had a baseline viral load of 10,800 copies/mL and a CD4 T-lymphocyte count of 466 cells/mm3. Baseline genotyping showed the following mutations: K103S, R211K, L10I, L63Q, I64V, and V771. The patient was taking no medications before this diagnosis, and his medical history was limited. At his initial visit, the patient described lifelong difficulty swallowing medications and indicated that he would prefer a formulation that he could crush. After the results of the patient’s laboratory test were received, the patient was initiated on the fixed-dose combination tablet of tenofovir disoproxil fumarate 300 mg with emtricitabine 200 mg once daily as well as one dolutegravir 50-mg tablet daily. The patient reported pulverizing the tenofovir–emtricitabine and dolutegravir tablets with a pill crusher, adding the powder to applesauce, and swallowing the mixture immediately. The patient returned to the clinic four weeks after the initiation of therapy and reported that he experienced no adverse effects from the medications, took all doses, and was having success crushing the formulations. The viral load during this visit was reported as “none detected” (<20 copies/mL), and the CD4 T-lymphocyte count was 583 cells/mm3. Continued medication adherence was encouraged, and the patient was scheduled for routine follow-up after achieving virological suppression.

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Available abstract

Management of human immunodeficiency virus (HIV) in treatment-naive patients requires combination antiretroviral therapy, with a preferred recommendation including tenofovir, emtricitabine, and dolutegravir.1 While this regimen has demonstrated efficacy in treatment-naive HIV-infected patients, published evidence is limited in patients who cannot ingest oral tablets.1,2 The successful management of HIV and virological suppression in patients using crushed formulations has been previously described.3,–5 Currently, data are limited regarding the use of crushed formulations of dolutegravir. While a recent pharmacokinetic study determined that the bioavailability of dolutegravir granules can exceed that of the tablet formulation, clinical data in HIV-infected patients are lacking.6 We describe a successful virological response in an HIV-infected treatment-naive patient to crushed dolutegravir tablets, taken with coformulated tenofovir–emtricitabine. A 30-year-old African-American man began receiving care after receiving a diagnosis of HIV infection. He had a baseline viral load of 10,800 copies/mL and a CD4 T-lymphocyte count of 466 cells/mm3. Baseline genotyping showed the following mutations: K103S, R211K, L10I, L63Q, I64V, and V771. The patient was taking no medications before this diagnosis, and his medical history was limited. At his initial visit, the patient described lifelong difficulty swallowing medications and indicated that he would prefer a formulation that he could crush. After the results of the patient’s laboratory test were received, the patient was initiated on the fixed-dose combination tablet of tenofovir disoproxil fumarate 300 mg with emtricitabine 200 mg once daily as well as one dolutegravir 50-mg tablet daily. The patient reported pulverizing the tenofovir–emtricitabine and dolutegravir tablets with a pill crusher, adding the powder to applesauce, and swallowing the mixture immediately. The patient returned to the clinic four weeks after the initiation of therapy and reported that he experienced no adverse effects from the medications, took all doses, and was having success crushing the formulations. The viral load during this visit was reported as “none detected” (<20 copies/mL), and the CD4 T-lymphocyte count was 583 cells/mm3. Continued medication adherence was encouraged, and the patient was scheduled for routine follow-up after achieving virological suppression.

Key concepts: Dolutegravir, Emtricitabine, Medicine, Regimen, Tolerability, Human immunodeficiency virus (HIV), Tenofovir, Viral load

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