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ArticleEuropean journal of drug metabolism and pharmacokinetics2025

Exploring the Pharmacokinetic Profile of Antiretroviral Efavirenz in Low Protein Malnourished Condition in Wistar Rats.

Sachin V Tembhurne, Swarupa V Sul, Shubham N Gavade, Swati Jogdand

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Article in European journal of drug metabolism and pharmacokinetics, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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4 authors.

Sachin V TembhurneDepartment of Pharmacology, AISSMS College of Pharmacy, Kennedy Road, Pune, 411001, India. sachin_tembhurne@aissmscop.com.ORCID http://orcid.org/0000-0001-5850-1121
Swarupa V SulDepartment of Pharmacology, AISSMS College of Pharmacy, Kennedy Road, Pune, 411001, India.ORCID http://orcid.org/0009-0001-7511-4067
Shubham N GavadeDepartment of Pharmacology, AISSMS College of Pharmacy, Kennedy Road, Pune, 411001, India.ORCID http://orcid.org/0009-0004-5542-1360
Swati JogdandCAYMET's Siddhant College of Pharmacy, Sudumbare, Pune, India.ORCID https://orcid.org/0000-0003-2251-7599

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6 · The paper itself

Abstract

BACKGROUND AND

objectivesThe HIV infection in malnourished conditions raises the concerns with antiretroviral medications, which may worsen the already compromised physiological state. The alteration in the plasma protein binding in malnourished HIV patients exacerbates the unbound fraction of antiretroviral medications, resulting in alterations in the therapeutic effectiveness and toxicity. Thus, the present study investigates the effects of protein deficiency and protein-energy malnutrition on the pharmacokinetics of the antiretroviral efavirenz.

methodMalnutrition was induced in this study through a modified diet containing only 2% protein. The experiment involved 16 Wistar rats, divided into two groups of 8. The control group was provided with a standard pellet diet (AIN 93G) that contained 19% protein, while the second group was subjected to the low-protein (2%) diet for 90 days. Rats were fed ad libitum with their respective diets during this period. On the 90th day, efavirenz (200 mg/kg, p.o.) was administered, and pharmacokinetic parameters were assessed using HPLC analysis.

resultsThe findings indicate that the protein-deficient diet successfully created a model of malnutrition, evidenced by a significant reduction in body weight (26%), hemoglobin levels (33%), total protein (27%), and blood albumin (41%) compared to the control group on a standard diet. The pharmacokinetic analysis of efavirenz in the protein-deficient rats revealed an increase in half-life (T

conclusionThese findings indicate that the pharmacokinetic profile of efavirenz is significantly altered under protein-deficient conditions. Therefore, it is recommended that further pharmacokinetic studies be conducted in patients with protein deficiency to determine if standard dosing of efavirenz should be adjusted based on the individual's nutritional status.

Indexed as

Anti-HIV AgentsBenzoxazinesProtein-Energy MalnutritionAlkynesAnimalsCyclopropanesMaleRatsRats, WistarAlkynesAnti-HIV AgentsBenzoxazinesCyclopropanesefavirenz

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.