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Cited by 431HIV/AIDS drug development and treatmentPharmacogenetics and Drug MetabolismComplementary and Alternative Medicine Studies

The effect of garlic supplements on the pharmacokinetics of saquinavir

Piscitelli, Stephen C., Burstein, Aaron H., Welden, Nada, Gallicano, Keith D., Falloon, Judith·2002·Clinical Infectious Diseases
DOI 10.1086/324351
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Abstract

Herbal therapies are widely used, but there are few data on their interactions with conventional medications. This study evaluated the effect of garlic supplements on the pharmacokinetics of saquinavir. Ten healthy volunteers received 10 doses of saquinavir (Fortovase) at a dosage of 1200 mg 3 times daily with meals for 4 days on study days 1-4, 22-25, and 36-39, and they received a total of 41 doses of garlic caplets taken 2 times daily on study days 5-25. Blood samples were obtained on study days 4, 25, and 39 for determination of saquinavir plasma pharmacokinetic parameters. In the presence of garlic, the mean saquinavir area under the curve (AUC) during the 8-h dosing interval decreased by 51%, trough levels at 8 h after dosing decreased by 49%, and the mean maximum concentrations (Cmax) decreased by 54%. After the 10-day washout period, the AUC, trough, and Cmax values returned to 60%-70% of their values at baseline. Patients should use caution when combining garlic supplements with saquinavir when it is used as a sole protease inhibitor.

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Crossref · 10.1086/324351

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  • The ability of garlic bulb oil to scavenge DPPH free radical and reduce Fe3+ to Fe2+ could be suggested as a possible mechanism of action for its neuroprotective potential.

    “their ability to scavenge diphenyl-1-picrylhydrazyl (DPPH) free radical that are used to evaluate the compound’s ability to act as hydrogen donors or free radical scavengers and to assess the antioxidant activity of food [92] and reduce Fe3+ to Fe2+ could be suggested as the possible mechanism of action for their neuroprotective potential [86].”

    From Chemical Constituents and Pharmacological Activities of Garlic (Allium sativum L.): A Review (2020) · cites this paper as [86]

  • Garlic reduced the plasma concentrations of saquinavir by about 50% in healthy participants after 3-week garlic supplement uptake.

    “Piscitelli et al. [86] reported that garlic reduced the plasma concentrations of saquinavir by about 50% in healthy participants, after 3-week of a garlic supplement uptake, in addition to this, many researchers evaluated the antitumor and cytotoxic actions of garlic and its related constituents in vitro and in vivo.”

    From Chemical Constituents and Pharmacological Activities of Garlic (Allium sativum L.): A Review (2020) · cites this paper as [86]

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Authors
Piscitelli, S. C., Burstein, A. H., Welden, N., Gallicano, K. D., & Falloon, J.
Affiliations
National Institutes of Health (US)
ORCID
Venue
Clinical Infectious Diseases
Publisher
Oxford University Press (OUP)
Published
2002-01-15
Volume
34
Issue
2
Pages
234-238
ISSN
  • 1058-4838 (ISSN-L)
  • 1537-6591
DOI
10.1086/324351
OpenAlex
W2132806259
Cited by
431
References
14
Citations by year
2026: 4 · 2025: 7 · 2024: 7 · 2023: 10 · 2022: 12 · 2021: 11 · 2020: 14 · 2019: 11 · 2018: 4 · 2017: 7 · 2016: 11 · 2015: 13 · 2014: 25 · 2013: 20 · 2012: 27
FWCI
17.41
Type
journal article
Language
en
Open access
closed
Locations
  • Clinical Infectious Diseases (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Infectious Diseases › HIV/AIDS drug development and treatment
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
  • Health Sciences › Medicine › Complementary and alternative medicine › Complementary and Alternative Medicine Studies
Keywords
garlic supplements, saquinavir, pharmacokinetics, drug interactions, herbal medicine, protease inhibitors, HIV antiretroviral therapy, plasma drug concentration, washout period
MeSH terms
Administration, Oral, Adult, Cytochrome P-450 Enzyme System, Drug Administration Schedule, Drug Combinations, Female, Garlic, Humans, Intestine, Small, Longitudinal Studies, Male, Plant Extracts, HIV-1, HIV Infections, Saquinavir, Dietary Supplements, Enterocytes

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