Related Experiment Video
Updated: Aug 9, 2026
10:29
Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Lopinavir-ritonavir: effects on endothelial cell function in healthy subjects
Jessica R Grubb1, André Dejam, Jocelyn Voell
1Critical Care Medical Department, Clinical Center, National Institutes of Health, Bethesda, Maryland 20892, USA.
The Journal of Infectious Diseases
|May 3, 2006
Summary
Lopinavir-ritonavir, an antiretroviral, did not directly impair endothelial cell function in HIV-negative subjects. Forearm blood flow responses to vasodilators improved, suggesting no short-term endothelial dysfunction from this treatment.
Area of Science:
- Cardiovascular Science
- Pharmacology
- Infectious Diseases
Background:
- Antiretroviral drugs can have complex effects on cardiovascular health.
- Endothelial dysfunction is a concern with some HIV treatments.
- Differentiating direct drug effects from secondary effects is crucial.
Purpose of the Study:
- To assess the direct impact of lopinavir-ritonavir on endothelial function.
- To distinguish drug-specific endothelial effects from other treatment-related changes.
Main Methods:
- Forearm blood flow was measured in 6 HIV-negative subjects.
- Acetylcholine (endothelium-dependent vasodilator) was used to assess function.
- Nitric oxide synthase inhibition was employed to further evaluate endothelial pathways.
Main Results:
- Lopinavir-ritonavir treatment significantly increased forearm blood flow responses to acetylcholine (P=.03).
- Inhibition of nitric oxide synthase led to a greater decrease in forearm blood flow post-treatment.
- These findings suggest no direct endothelial cell dysfunction.
Conclusions:
- Short-term lopinavir-ritonavir treatment did not appear to directly cause endothelial dysfunction in this cohort.
- Further research is needed to fully understand the cardiovascular implications of antiretroviral therapy.
Related Concept Videos
01:26Pharmacokinetics: Drug–Food and Drug–Viral Interactions
A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of many...
01:15Bioavailability Study Design: Healthy Subjects Versus Patients
Bioavailability studies are essential for evaluating a drug's therapeutic efficacy and understanding its absorption patterns under various physiological conditions. Conducting such studies on target patient populations provides more relevant data by simulating real-world disease states. However, practical challenges often necessitate the use of young, healthy adult volunteers as study subjects.Patients may exhibit altered drug absorption patterns due to the effects of the disease itself,...
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...
01:22Effect of Hepatic Disease on Pharmacokinetics: Pathophysiologic Assessment and Liver Function Test
In clinical practice, the direct measurement of hepatic blood flow to evaluate liver function presents significant challenges due to the intricate and specialized nature of the necessary techniques. Consequently, healthcare professionals often rely on empirical estimates derived from thorough patient examinations and liver function tests to gauge liver health. Among the tools at their disposal, the Child–Pugh and MELD scoring systems stand out for their ability to categorize and assess the...
01:22Antiviral Nucleoside Inhibitors
Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...
01:25Antihypertensive Drugs: Direct Renin Inhibitors
The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...