Effects of probenecid: A Synthesis of Findings from 24 Studies

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Original Abstract of the Article

Major Research Findings

Probenecid has been shown to affect the way various drugs move throughout the body in multiple studies. 14 showed that probenecid reduces renal clearance of adefovir and benzylpenicillin by inhibiting OAT1 and OAT3, proteins involved in drug excretion in the kidneys. This study found that probenecid inhibited uptake of adefovir and benzylpenicillin in the kidney, leading to a 45% decrease in adefovir clearance and a 78% decrease in benzylpenicillin clearance. 2 found that probenecid protects enteric glial cells in the gut from damage and improves intestinal motility. This is thought to be achieved by inhibiting P2X7 receptors and pannexin-1 channels in enteric glial cells. 18 found that probenecid can reduce inflammatory responses in the trigeminal nucleus caused by nitroglycerin. 4 found that probenecid increases the blood concentration of the antibiotic cephalexin, making it more effective. 17 found that probenecid increases the blood concentration of the immunosuppressant mizoribine, making it more effective. 9 found that probenecid improves motor function in a mouse model of Parkinson's disease induced by MPTP/p. This is thought to be due to the protective and regenerative effects of probenecid on nerve cells. 19 found that probenecid extends survival and improves motor function in a transgenic mouse model of Huntington's disease. This effect is thought to be due to probenecid's ability to regulate membrane transport, which protects nerve cells. 1 found that probenecid inhibits the proliferation and migration of pulmonary artery smooth muscle cells induced by PDGF-BB. 23 found that probenecid inhibits the activity of UDP-glucuronosyltransferases, a group of enzymes. 3 found that probenecid suppresses inflammation after spinal cord injury, protecting nerve cells and improving locomotor function. 5 found that probenecid inhibits the growth of prostate cancer cells. found that probenecid inhibits the growth of Plasmodium falciparum, a parasite that causes malaria. 16 found that probenecid lowers blood pressure. This is thought to be achieved by inhibiting the activity of α-adrenergic receptors. 15 found that probenecid may affect drug excretion in the kidneys when renal function is impaired or when other drugs are used concurrently. 7 found that probenecid increases the blood concentration of tenofovir disoproxil fumarate and emtricitabine, which are used to prevent HIV infection. 6 found that probenecid affects drug transport in the liver and kidneys. 12 found that probenecid enhances the anti-cancer effects of bisphosphonates, a group of drugs. 13 found that probenecid increases the blood concentration of canagliflozin, a drug used to treat type 2 diabetes. 11 found that probenecid improves motor function in a mouse model of Parkinson's disease. This is thought to be due to the protective and regenerative effects of probenecid on nerve cells. 8 found that probenecid increases the blood concentration of flucloxacillin, an antibiotic, making it more effective. 21 found that probenecid affects the activity of nerve cells in the brain. 20 found that probenecid protects nerve cells in a mouse model of Parkinson's disease. This is thought to be due to probenecid's ability to stimulate nerve cell regeneration. 10 found that probenecid increases the blood concentration of nemonoxacin, an antibiotic. 22 found that probenecid increases the blood concentration of fexofenadine, an antihistamine. 24 found that probenecid reduces the impact of the antiviral cidofovir on the kidneys.

Benefits and Risks

Benefit Summary

Probenecid has been shown to affect the way various drugs move throughout the body in multiple studies. For example, it has been reported to prolong the effectiveness of antibiotics, protect nerve cells, and enhance anti-cancer effects. 4 , 9 , 19 , 12 Probenecid can potentially prolong the effectiveness of various drugs, protect nerve cells, and enhance anti-cancer effects. 4 , 9 , 19 , 12 However, probenecid can interact with other drugs and needs to be used with caution. 15 Probenecid can potentially be helpful in treating various diseases. However, probenecid can interact with other drugs and needs to be used with caution. 15 , 7 Additionally, probenecid can impact kidney function. 24

Risk Summary

Probenecid can interact with various drugs. 15 , 7 Additionally, probenecid can impact kidney function. 24 When taking probenecid, consult a doctor and follow their instructions.

Comparison Between Studies

Commonalities in Studies

Many studies have shown that probenecid affects the way various drugs move throughout the body. 14 , 4 , 17 , 13 , 10 , 22 This is thought to be due to probenecid's inhibition of proteins involved in drug transport. 14 , 23 Additionally, probenecid has been shown to protect nerve cells. 9 , 19 , 20 This is thought to be due to probenecid's ability to promote nerve cell survival and regeneration. 9 , 19 , 20

Differences in Studies

The type of drug affected by probenecid and the strength of its effect vary between studies. 14 , 4 , 17 , 13 , 10 , 22 Also, the potential for probenecid to affect kidney function as a side effect varies between studies. 24

Consistency and Discrepancies in Results

Multiple studies have shown that probenecid affects the way various drugs move throughout the body. 14 , 4 , 17 , 13 , 10 , 22 However, the type of drug affected by probenecid and the strength of its effect vary between studies. 14 , 4 , 17 , 13 , 10 , 22 Also, the potential for probenecid to affect kidney function as a side effect varies between studies. 24

Cautions for Applying Findings to Real Life

Probenecid has been shown to affect the way various drugs move throughout the body in multiple studies. 14 , 4 , 17 , 13 , 10 , 22 However, probenecid can interact with other drugs and needs to be used with caution. 15 , 7 Additionally, probenecid can impact kidney function. 24 When taking probenecid, consult a doctor and follow their instructions.

Limitations of Current Research

There is still not enough research on probenecid. 14 , 2 , 18 , 4 , 17 , 9 , 19 , 1 , 23 , 3 , 5 , , 16 , 15 , 7 , 6 , 12 , 13 , 11 , 8 , 21 , 20 , 10 , 22 , 24 In particular, more research is needed on how probenecid interacts with various drugs and what potential side effects it may have. 15 , 7 , 24

Directions for Future Research

Probenecid has been shown to affect the way various drugs move throughout the body in multiple studies. 14 , 4 , 17 , 13 , 10 , 22 However, further research is needed to determine which drugs probenecid affects, the nature of its effects, and its potential side effects. 15 , 7 , 24 Specifically, detailed studies are required on probenecid's interactions with other drugs and its side effects. 15 , 7 , 24

Conclusion

Probenecid can potentially affect the way various drugs move throughout the body. 14 , 4 , 17 , 13 , 10 , 22 This is thought to be due to probenecid's inhibition of proteins involved in drug transport. 14 , 23 Additionally, probenecid has been shown to protect nerve cells. 9 , 19 , 20 However, probenecid can interact with other drugs and needs to be used with caution. 15 , 7 Additionally, probenecid can impact kidney function. 24 When taking probenecid, consult a doctor and follow their instructions.

Literature analysis of 24 papers
Positive Content
21
Neutral Content
1
Negative Content
2
Article Type
5
0
0
1
24
1.

[Effects of probenecid on the migration and proliferation ability of platelet derived growth factor-BB induced pulmonary artery smooth muscle cells in rats].

Author: NigalaAikeremu, GaoRui-Juan, TangXue-Chun, KongLiang-Jing-Yuan, GaoYi-Xuan, YuanJia-Yue, MaKe-Tao, LiLi, SiJun-Qiang

Inhibits PASMC migration
Inhibits PASMC proliferation

Probenecid effectively inhibited the migration and proliferation of platelet-derived growth factor-BB (PDGF-BB)-induced pulmonary artery smooth muscle cells (PASMCs) by blocking Pannexin-1.

English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : Chinese

3.

Neuroprotective Effects of the Pannexin-1 Channel Inhibitor: Probenecid on Spinal Cord Injury in Rats.

Author: QiQi, WangXiao-Xuan, LiJing-Lu, ChenYu-Qing, ChangJian-Rong, XiJin, LüHe-Zuo, ZhangYu-Xin

Improved Locomotion
Reduced Lesion

Probenecid, an inhibitor of the Pannexin-1 channel, was found to be beneficial in treating spinal cord injury (SCI) in a rat model. It reduced inflammation, lesion area, and demyelination, while improving locomotor function.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

4.

Probenecid effects on cephalexin pharmacokinetics and pharmacodynamics in healthy volunteers.

Author: EvertsRichard J, GardinerSharon J, ZhangMei, BeggRonald, ChambersStephen T, TurnidgeJohn, BeggEvan J

Increased cephalexin AUC
Prolonged effect

Probenecid increased the plasma concentration of cephalexin, potentially improving its effectiveness in treating bacterial infections.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

5.

Pleiotropic effects of probenecid on three-dimensional cultures of prostate cancer cells.

Author: UwadaJunsuke, MukaiShoichiro, TeradaNaoki, NakazawaHitomi, IslamMohammad Sayful, NagaiTakahiro, FujiiMasato, YamasakiKoji, TaniguchiTakanobu, KamotoToshiyuki, YazawaTakashi

Prostate cancer treatment

This study evaluated the effects of probenecid, a drug that inhibits multiple drug-efflux transporters, on prostate cancer cells in a three-dimensional (3D) culture model. Probenecid showed potential to sensitize prostate cancer cells to chemotherapy.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

7.

Inhibitory Effects of Probenecid on Pharmacokinetics of Tenofovir Disoproxil Fumarate and Emtricitabine for On-Demand HIV Preexposure Prophylaxis.

Author: LiuStephanie N, GuffordBrandon T, LuJessica Bo Li, BushmanLane R, AndersonPeter L, BergstromRichard F, DestaZeruesenay, GuptaSamir K

Increased TFV-DP concentrations

This study compared the pharmacokinetic profiles of a single dose of probenecid (PRO)-boosted tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) (test) with the current on-demand HIV preexposure prophylaxis regimen from the IPERGAY study (control). PRO significantly increased the plasma concentrations of tenofovir and emtricitabine. However, the intracellular concentrations of tenofovir-diphosphate were higher at 24 hours but lower at 72 hours in the test group compared to the control.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Probenecid and food effects on flucloxacillin pharmacokinetics and pharmacodynamics in healthy volunteers.

Author: EvertsRichard J, BeggRonald, GardinerSharon J, ZhangMei, TurnidgeJohn, ChambersStephen T, BeggEvan J

Improved pharmacodynamics
Increased flucloxacillin exposure

Probenecid increases flucloxacillin exposure, leading to pharmacodynamic effects greater than pharmacokinetic effects. It may improve the applicability of oral flucloxacillin regimens.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

Effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in healthy Chinese volunteers.

Author: ZhangYi-Fan, DaiXiao-Jian, YangYong, ChenXiao-Yan, WangTing, TangYun-Biao, TsaiCheng-Yuan, ChangLi-Wen, ChangYu-Ting, ZhongDa-Fang

Nemonoxacin pharmacokinetics
Cimetidine
Probenecid

Probenecid reduced the renal clearance and increased the plasma exposure of nemonoxacin by 22.6% and 26.2%, respectively, but these effects are unlikely to be clinically meaningful at therapeutic doses. Cimetidine had weaker effects on the pharmacokinetics of nemonoxacin, which are also unlikely to be clinically meaningful.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

Probenecid as a sensitizer of bisphosphonate-mediated effects in breast cancer cells.

Author: EbertRegina, Meissner-WeiglJutta, ZeckSabine, MäättäJorma, AuriolaSeppo, Coimbra de SousaSofia, MentrupBirgit, GraserStephanie, RachnerTilman D, HofbauerLorenz C, JakobFranz

Bone metastasis treatment
Breast cancer survival
Tumor relapse reduction

This study hypothesized that enhancing intracellular pyrophosphate accumulation via inhibition of probenecid-sensitive channels and transporters would sensitize tumor cells for bisphosphonates anti-tumor efficacy.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

13.

Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants.

Author: DevineniDamayanthi, VaccaroNicole, MurphyJoe, CurtinChristopher, MamidiRao N V S, WeinerSveta, WangShean-Sheng, AriyawansaJay, StieltjesHans, WajsEwa, Di ProsperoNicholas A, RothenbergPaul

Drug interactions

Three independent studies evaluated the effects of rifampin, probenecid, and cyclosporine A on the pharmacokinetics of canagliflozin, a sodium-glucose co-transporter 2 inhibitor. The results demonstrated that coadministration of these drugs significantly affected canagliflozin exposures.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

14.

Inhibitory effects of p-aminohippurate and probenecid on the renal clearance of adefovir and benzylpenicillin as probe drugs for organic anion transporter (OAT) 1 and OAT3 in humans.

Author: MaedaKazuya, TianYing, FujitaTomoe, IkedaYasuhiko, KumagaiYuji, KondoTsunenori, TanabeKazunari, NakayamaHideki, HoritaShigeru, KusuharaHiroyuki, SugiyamaYuichi

Probe drugs for OAT1 and OAT3
PAH modulation

Adefovir and benzylpenicillin are selective probe substrates for OAT1 and OAT3, respectively. A clinical study showed that probenecid and PAH inhibited the renal clearance of adefovir, while probenecid reduced the clearance of benzylpenicillin, and PAH unexpectedly increased it. These findings suggest that adefovir and benzylpenicillin can be used as probe drugs for OAT1 and OAT3, and PAH can be used to investigate the role of OAT1 in drug excretion.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

15.

Towards quantitation of the effects of renal impairment and probenecid inhibition on kidney uptake and efflux transporters, using physiologically based pharmacokinetic modelling and simulations.

Author: HsuVicky, de L T VieiraManuela, ZhaoPing, ZhangLei, ZhengJenny Huimin, NordmarkAnna, BerglundEva Gil, GiacominiKathleen M, HuangShiew-Mei

Drug elimination
Renal impairment

The kidney plays a significant role in drug elimination. Renal impairment or the use of transporter inhibitors can decrease active secretion and increase exposure to drugs that are substrates of kidney secretory transporters. This study utilized physiologically based pharmacokinetic (PBPK) modeling to evaluate the effects of patient factors on kidney transporters.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, U.S. Gov't, Non-P.H.S.Research funding provided by US government agencies other than the Public Health Service.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

16.

Anti-hypertensive effects of probenecid via inhibition of the α-adrenergic receptor.

Author: ParkJin Baek, KimSung-Jin

Gout treatment
High blood pressure relief
Not for normotensive patients

Probenecid, a medication used for gout, was found to have an anti-hypertensive effect in spontaneously hypertensive rats.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

17.

Effects of probenecid on the pharmacokinetics of mizoribine and co-administration of the two drugs in patients with nephrotic syndrome.

Author: UtsunomiyaY, HaraY, ItoH, OkonogiH, MiyazakiY, HashimotoY, HosoyaT

Nephrotic syndrome treatment

This study evaluated the effects of probenecid (PRB) co-administered with mizoribine (MZR) on the pharmacokinetics (PK) of MZR in patients with nephrotic syndrome. Co-administration with PRB prolonged the half-life of MZR, potentially enhancing its effect in these patients.

Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

19.

Neuroprotective effects of probenecid in a transgenic animal model of Huntington's disease.

Author: VamosEniko, VorosKrisztina, ZadoriDenes, VecseiLaszlo, KlivenyiPeter

Ameliorated motor activity
Improved HD survival
Reduced intranuclear aggregates
Reduced neuronal loss

Probenecid, a drug used to treat gout, was found to improve survival and reduce neuronal loss in a mouse model of Huntington's disease (HD). This suggests that probenecid may have neuroprotective effects and could potentially be used to treat HD.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

20.

Effects of endurance exercise on ventral tegmental area neurons in the chronic 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and probenecid-treated mice.

Author: AhmadS Omar, ParkJi-Hyuk, Stenho-BittelLisa, LauYuen-Sum

Protect VTA neurons

Exercise training is neuroprotective for dopaminergic neurons in the VTA in a chronic mouse model of Parkinson's disease with moderate neurodegeneration. 18 weeks of exercise restored the number of VTA neurons to a normal range.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

21.

Subchronic treatment with kynurenine and probenecid: effects on prepulse inhibition and firing of midbrain dopamine neurons.

Author: NilssonL K, LinderholmK R, ErhardtS

Disrupted PPI
Increased neuronal firing

This study investigated the effects of subchronic exposure to kynurenine and probenecid, which increase brain kynurenic acid (KYNA) turnover, on rat ventral tegmental area (VTA) dopamine neurons and prepulse inhibition (PPI). The study found that this treatment increased neuronal firing of VTA DA neurons and disrupted PPI, suggesting that the effects of acutely elevated KYNA levels on VTA DA neurons persist following subchronic exposure.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

22.

Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics.

Author: Yasui-FurukoriNorio, UnoTsukasa, SugawaraKazunobu, TateishiTomonori

Bioavailability increase
Renal clearance reduction

Verapamil increases fexofenadine exposure through P-glycoprotein inhibition, and probenecid slightly increases fexofenadine exposure by reducing renal clearance.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

23.

Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid.

Author: UchaipichatVerawan, MackenziePeter I, GuoXiao-Hui, Gardner-StephenDione, GaletinAleksandra, HoustonJ Brian, MinersJohn O

Inhibition of UGT isoforms

This study investigated the glucuronidation kinetics of two prototypic substrates, 4-methylumbelliferone (4MU) and 1-naphthol (1NP), by 11 human UDP-glucuronosyltransferases (UGTs). It found that all isoforms except UGT1A4 glucuronidated 4MU, while all but UGT 1A4, 2B15, and 2B17 metabolized 1NP. The kinetic models varied with the substrate and isoform. Diclofenac and probenecid inhibited all isoforms, while organic solvents generally had a minor effect on UGT activity.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

24.

Pharmacokinetics and renal effects of cidofovir with a reduced dose of probenecid in HIV-infected patients with cytomegalovirus retinitis.

Author: WolfDaniel L, RodríguezCarlos A, MucciMassimiliano, IngrossoAntonella, DuncanBarbara A, NickensDana J

Cidofovir pharmacokinetics
Renal protection
Nephrotoxicity
Probenecid side effects

A reduced-dose probenecid regimen provides renal protection after a single dose of cidofovir without significantly altering its pharmacokinetics, but further research is needed to assess its safety.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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