HIV Protease Inhibitors

Publication Title: 
The American Journal of Tropical Medicine and Hygiene

Most malaria endemic regions are co-infested with HIV infection. Treatment of one may affect outcome of the other in co-infected individuals. HIV protease inhibitors, indinavir or nelfinavir, are important antiretroviral drugs and artemisinin is central to malaria treatment. We show these protease inhibitors augment the antimalarial activity of artemisinin against P. falciparum in vitro.

Author(s): 
Mishra, Lokesh C.
Bhattacharya, Amit
Sharma, Manish
Bhasin, Virendra K.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

A multiple dose, parallel group study was conducted to assess for a drug-drug interaction between the pyronaridine/artesunate (PA) combination antimalarial and ritonavir. Thirty-four healthy adults were randomized (1:1) to receive PA for 3 days or PA with ritonavir (100 mg twice daily for 17 days, PA administered on Days 8-10). Pharmacokinetic parameters for pyronaridine, artesunate, and its active metabolite dihydroartemisinin (DHA) were obtained after the last PA dose and for ritonavir on Days 1 and 10.

Author(s): 
Morris, Carrie A.
Lopez-Lazaro, Luis
Jung, Donald
Methaneethorn, Janthima
Duparc, Stephan
Borghini-Fuhrer, Isabelle
Pokorny, Rolf
Shin, Chang-Sik
Fleckenstein, Lawrence
Publication Title: 
The New England Journal of Medicine

BACKGROUND: Human immunodeficiency virus (HIV) protease inhibitors show activity against Plasmodium falciparum in vitro. We hypothesized that the incidence of malaria in HIV-infected children would be lower among children receiving lopinavir-ritonavir-based antiretroviral therapy (ART) than among those receiving nonnucleoside reverse-transcriptase inhibitor (NNRTI)-based ART.

Author(s): 
Achan, Jane
Kakuru, Abel
Ikilezi, Gloria
Ruel, Theodore
Clark, Tamara D.
Nsanzabana, Christian
Charlebois, Edwin
Aweeka, Francesca
Dorsey, Grant
Rosenthal, Philip J.
Havlir, Diane
Kamya, Moses R.
Publication Title: 
AIDS patient care and STDs

The use of complementary and alternative medicine (CAM) therapies is widespread in many chronic illnesses, including human immunodeficiency virus (HIV) infection. The objective of this study was to determine the impact of increasingly effective antiretroviral therapy on the use of CAM in an HIV-positive patient population. A written survey was given to 191 HIV-positive outpatients. Participation was voluntary and anonymous. One hundred twenty-eight patients (67%) used CAM at some time to control HIV and 76 (40%) of the patients were currently using CAM.

Author(s): 
Duggan, J.
Peterson, W. S.
Schutz, M.
Khuder, S.
Charkraborty, J.
Publication Title: 
The American Journal of Pathology

Clinical use of human immunodeficiency virus protease inhibitors such as ritonavir may be associated with cardiovascular disease. The objective of this study was to determine the effects and molecular mechanisms of ritonavir on cholesterol efflux from human macrophage-derived foam cells, which is a critical factor of atherogenesis. Human THP-1 monocytes and peripheral blood mononuclear cells were preincubated with acetylated low-density lipoprotein and [(3)H]cholesterol to form foam cells, which were then treated with apolipoprotein A-I for cholesterol efflux assay.

Author(s): 
Wang, Xinwen
Mu, Hong
Chai, Hong
Liao, Dan
Yao, Qizhi
Chen, Changyi
Publication Title: 
The Journal of Pharmacy and Pharmacology

Ritonavir, a protease inhibitor drug, is commonly used in AIDS therapy. As with other chemotherapeutic drugs that cause gastrointestinal adverse effects, ritonavir treatment is associated with significant nausea and vomiting. This study investigated whether Scutellaria baicalensis, and its active flavonoid constituent, baicalein, attenuate the gastrointestinal effects of ritonavir. The effects of herb administration were evaluated in ritonavir-treated rats using a rat pica model, which simulates nausea and vomiting in humans.

Author(s): 
Mehendale, Sangeeta
Aung, Han
Wang, Chong-Zhi
Tong, Robin
Foo, Adela
Xie, Jing-Tian
Yuan, Chun-Su
Publication Title: 
BMC complementary and alternative medicine

BACKGROUND: Complementary and alternative medicine (CAM) use is prevalent among HIV-infected patients to reduce the toxicity of antiretroviral therapy. Ginseng has been used for treatment of hyperglycemia and insulin resistance, a common side effect of some HIV-1 protease inhibitors (PI). However, it is unknown whether American ginseng (AG) can reverse insulin resistance induced by the PI indinavir (IDV), and whether these two agents interact pharmacologically.

Author(s): 
Andrade, Adriana S. A.
Hendrix, Craig
Parsons, Teresa L.
Caballero, Benjamin
Yuan, Chun-Su
Flexner, Charles W.
Dobs, Adrian S.
Brown, Todd T.
Publication Title: 
Toxicologic Pathology

Metabolic complications associated with HIV infection and treatment frequently present as a relative lack of peripheral adipose tissue associated with dyslipidemia and insulin resistance. In this review we explain the connection between abnormalities of intermediary metabolism, observed either in vitro or in vivo, and this group of metabolic effects. We review molecular mechanisms by which the HIV protease inhibitor (PI) class of drugs may affect the normal stimulatory effect of insulin on glucose and fat storage.

Author(s): 
Flint, Oliver P.
Noor, Mustafa A.
Hruz, Paul W.
Hylemon, Phil B.
Yarasheski, Kevin
Kotler, Donald P.
Parker, Rex A.
Bellamine, Aouatef
Publication Title: 
The American Journal of Pathology

The objective of this study was to determine the effects of highly active antiretroviral therapy (HAART) drugs on pulmonary endothelial function. Porcine pulmonary arteries or human pulmonary arterial endothelial cells (HPAECs) were incubated with eight HAART drugs [ritonavir, indinavir, lopinavir, zidovudine (AZT), abacavir, stavudine, didanosine (ddI), and lamivudine] individually or in combination [three HAART drugs (3-plex; indinavir, stavudine, and ddI)] at their clinical plasma concentrations for 24 hours.

Author(s): 
Wang, Xinwen
Chai, Hong
Lin, Peter H.
Yao, Qizhi
Chen, Changyi
Publication Title: 
Biochemical Pharmacology

HIV protease inhibitor (PI)-associated cardiovascular risk, especially atherosclerosis, has become a major concern in the clinic. Macrophages are key players in the inflammatory response and atherosclerosis formation. We have previously shown that HIV PIs induce endoplasmic reticulum (ER) stress, activate the unfolded protein response (UPR), and increase the synthesis of the inflammatory cytokines, TNF-alpha and IL-6, by regulating the intracellular translocation of RNA binding protein HuR in macrophages. However, the underlying signaling mechanisms remain unclear.

Author(s): 
Chen, Li
Jarujaron, Sirikalaya
Wu, Xudong
Sun, Lixin
Zha, Weibin
Liang, Guang
Wang, Xuan
Gurley, Emily C.
Studer, Elaine J.
Hylemon, Phillip B.
Pandak, William M.
Zhang, Luyong
Wang, Guangji
Li, Xiaokun
Dent, Paul
Zhou, Huiping

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