Treatment of HIV-infected adults who have trouble swallowing pills: Liquid, chewable, and crushable formulations
- Amy L Graziani, PharmD
Amy L Graziani, PharmD
- Associate Professor in Pharmacy, Adjunct Faculty
- University of Pennsylvania School of Medicine and University of the Sciences, Philadelphia, PA
Antiretroviral therapy (ART) is recommended in all HIV-infected patients, regardless of CD4 cell count . However, some patients may have trouble taking combination regimens if they have difficulty swallowing due to other comorbidities, such as candidal esophagitis, or more permanent disabilities, such as stroke.
Fortunately, many antiretroviral medications are available as liquid preparations. In addition, for some medications there are methods for dissolving or crushing tablets, which are effective without losing drug potency.
Medication dosing options for the patient who has difficulty swallowing is reviewed below. Information about the general approach to selecting combination ART is reviewed elsewhere. (See "Selecting antiretroviral regimens for the treatment-naïve HIV-infected patient".)
It is important to understand that the milligram dosing of a liquid preparation may differ from the milligram dose of a tablet formulation, so a direct conversion shouldn’t be expected. A summary of the available liquid formulations is found in the accompanying table (table 1).
The manufacturer does not usually provide a measuring device in the packaging for most of these liquid products. In addition, pharmacists generally do not provide instruction or measuring devices unless specifically asked and they may not have time to properly instruct patients on how to use them. Therefore, patients often use whatever they consider to be a teaspoon, tablespoon, or ounce, all of which are significantly inaccurate. The volume of liquid delivered via various household teaspoons can range from 2 mL to 9 mL.
- http://www.aidsinfo.nih.gov/guidelines/ (Accessed on June 13, 2012).
- http://www.aidsinfo.nih.gov/guidelines/ (Accessed on June 29, 2012).
- Thompson MA, Aberg JA, Hoy JF, et al. Antiretroviral treatment of adult HIV infection: 2012 recommendations of the International Antiviral Society-USA panel. JAMA 2012; 308:387.
- Tenofovir product labeling, Gilead Sciences, 2012.
- Bristol-Myers Squibb, 2011, personal communication.
- King J, et al. Assessment of Bioequivalence of Tenofovir, Emtricitabine, and Efavirenz Fixed-dose Combination Tablet Compared with a Compounded Oral Liquid Formulation Derived from the Tablet. 17th CROI, 16-19 February 2010, San Francisco. Poster abstract 605. http://www.retroconference.org/2010/Abstracts/37400.htm (Accessed on April 10, 2012).
- Etravirine product labeling, Tibotec Pharmaceuticals, March 2012.
- Data on file, BMS, 2012.
- Darunavir product labeling, Tibotec Therapeutics, December 2011.
- Scholten S, Mauruschat S, Hindermann S, Ranneberg B. Administration of darunavir tablets in patients with difficulties in swallowing - two case reports. J Int AIDS Soc 2010; 13(suppl 4):114.
- Liu W, Klein CE, Marsh KC, et al. Predicted pharmacokinetics of lopinavir after multiple dose administration of lopinavir/ritonavir tablet to pediatric patients. Poster presented at the 8th International Conference on Drug Therapy in HIV Infection. November 12-16, 2006, Glasgow, UK. Abstract #366.
- Diep H, et al. Pharmacokinetics of lopinavir/ritonavir crushed versus whole tablets in children. 17th CROI, 16-19 February 2010, San Francisco. Poster abstract 877. http://www.retroconference.org/2010/Abstracts/37445.htm (Accessed on April 10, 2012).
- Tipranavir Product Labeling, Boehringer Ingelheim, 2012.
- GENERAL BACKGROUND
- AVAILABILITY OF ALTERNATIVE FORMULATIONS
- NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
- Tenofovir (Viread)
- Emtricitabine (Emtriva)
- Truvada (tenofovir-emtricitabine)
- Abacavir (Ziagen)
- Lamivudine (Epivir, 3TC)
- Zidovudine (Retrovir, ZDV, AZT)
- Combivir (zidovudine-lamivudine)
- NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
- Efavirenz (Sustiva)
- Atripla (efavirenz-emtricitabine-tenofovir)
- Rilpivirine (Edurant)
- Rilpivirine-emtricitabine-tenofovir coformulation (Complera)
- Etravirine (Intelence)
- Nevirapine (Viramune, Viramune XR)
- PROTEASE INHIBITORS
- Atazanavir (Reyataz)
- Darunavir (Prezista)
- Fosamprenavir (Lexiva)
- Ritonavir (Norvir)
- Lopinavir-ritonavir (Kaletra)
- Tipranavir (Aptivus)
- INTEGRASE INHIBITORS
- Raltegravir (Isentress)
- CCR5 INHIBITORS
- Maraviroc (Selzentry)
- FUSION INHIBITORS
- Enfuvirtide (Fuzeon, T20)
- SUMMARY AND RECOMMENDATIONS