Pomelo enhances cyclosporine bioavailability in healthy male thai volunteers

Anlamlert, Wirin; Sermsappasuk, Pakawadee; Yokubol, Dhirayudh; Jones, Sirada

doi:10.1002/jcph.430

Cited by 12 publications

(7 citation statements)

References 37 publications

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“…37 Additionally, a recent clinical study also demonstrated that pomelo pulps inhibited intestinal P-gp or CYP3A, leading to increased bioavailability of cyclosporine in human. 26 The present study demonstrated that pomelo juice suppressed the expression of both Mdr1a gene in rat intestine without affecting their expression in rat liver. Previously, it was reported that furanocoumarins such as bergamottin and 6',7'dihydroxybergamottin could inhibit the activity of P-gp.…”

Section: Discussionsupporting

confidence: 51%

“…25 Recently, a clinical study demonstrated that pomelo pulp increased bioavailability of cyclosporine via intestinal CYP3A inhibition in Thai human volunteers. 26 Grapefruit juice has been shown to interact with several drugs though down-regulation of CYP3A4 in the small intestine. 27 The present study demonstrated that oral administration of pomelo juice twice daily for 7 days, suppressed rat hepatic CYP3a2, the isoform similar to human CYP3A4, catalytic activity.…”

Section: Discussionmentioning

confidence: 99%

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Effect of Pomelo Juice on the Pharmacokinetics of Simvastatin, CYP3A2 Activity and Mdr1a, Mdr1b and Slc21a5 Expressions in Rats

et al. 2019

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Background: Food-drug interaction can decrease drug effectiveness or increase risk of drug toxicity. Simvastatin is widely used for treatment of hypercholesterolemia and hypertriglyceridemia. Therefore, this study aimed to investigate the effects of pomelo juice on the pharmacokinetics of simvastatin, CYP3a2 activity and Mdr1a, Mdr1b and Slc21a5 expressions in rats. Methods: Rats were divided into 4 groups including (i) control, (ii) pomelo that received pomelo juice orally twice daily for 7 days, (iii) simvastatin that received simvastatin on day 8, and (iv) simvastatin + pomelo juice. Plasma concentrations of simvastatin and simvastatin acid were analyzed using LC-MS/MS. Hepatic CYP3a2 activity was evaluated using midazolam hydroxylation assay. The expressions of hepatic and intestinal Mdr1a, Mdr1b and Slc21a5 were measured using the real-time RT-PCR. Results: Oral administration of pomelo juice for 7 days altered pharmacokinetic profiles of simvastatin and its primary active metabolite, simvastatin acid, in rats. Real-time RT-PCR analysis revealed that pomelo juice significantly suppressed the expression of intestinal Mdr1a and Mdr1b and hepatic Slc21a5. Rat hepatic CYP3a2 catalytic activity was also inhibited following pomelo juice administration. Conclusion: The results of this study suggested that there was a risk of potential drug interaction associated with inhibition of drug transporters and CYP3A caused by pomelo juice.

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Section: Discussionsupporting

confidence: 51%

Section: Discussionmentioning

confidence: 99%

Effect of Pomelo Juice on the Pharmacokinetics of Simvastatin, CYP3A2 Activity and Mdr1a, Mdr1b and Slc21a5 Expressions in Rats

et al. 2019

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“…11 The health consequences of these interactions were widely reported in both case reports and clinical studies. [12][13][14][15][16][17][18][19][20] Patients taking anticancer, cardiovascular and immunosuppressant medications were predominantly affected by these interactions. 21 With the lack of awareness in identifying and reporting these reactions among the public and healthcare professionals, this risk could be amplified.…”

Section: Strengths and Limitations Of This Studymentioning

confidence: 99%

“…Moreover, due to the common use of these products in patients with comorbidities, interactions with prescription and OTC medications are possible, leading to a decrease in the effectiveness of pharmacological treatments or toxic manifestations 11. The health consequences of these interactions were widely reported in both case reports and clinical studies 12–20. Patients taking anticancer, cardiovascular and immunosuppressant medications were predominantly affected by these interactions 21.…”

Section: Introductionmentioning

confidence: 99%

Herbal supplements in Jordan: a cross-sectional survey of pharmacists’ perspectives and knowledge

Jalil¹,

Naser

Prieto

et al. 2022

BMJ Open

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ObjectivesPharmacists are ideal partners for engaging with the needs and expectations of patients. They can play a vital role by providing information and supplying herbal medicines. In some community settings, pharmacists are also the main first point of care. This study explored Jordanian community pharmacists’ perspectives and knowledge of herbal medicines available in pharmacies.DesignA cross-sectional study using an online survey was developed, and it was distributed via social media platforms. The one-way analysis of variance (ANOVA) test was used to compare the mean knowledge scores between different demographic groups. Multiple linear regression analysis was used to identify predictors of herbal medicines knowledge.SettingJordanian community pharmacies.Participants401 Jordanian community pharmacists.ResultsHerbal supplements are sold in practically all pharmacies (98.5%). Slimming aids (14.7%), followed by sexual and sports enhancements (14%) and maintaining general health (12.1%) were most requested by Jordanian customers. While supplements for maintaining general health (12%), followed by slimming aids (11.4%) and skin conditions (9.3%) were most recommended by Jordanian pharmacists. 63.1% were not aware of potential herb–drug interactions, 95.6% did not receive complaints from customers about herbal medicines and 41.2% would not report adverse reactions to the national pharmacovigilance services. The mean knowledge score for knowledge of use, regulation, adverse reactions, and drug interactions was 3.7 (SD: 0.7), 3.5 (SD: 0.8), 3.6 (SD: 0.8), and 3.6 (SD: 0.8) (out of 5), respectively. ANOVA test showed that total pharmacists’ knowledge scores significantly differed based on the length of time practising pharmacy (p<0.05).ConclusionThis study highlights some key concerns relating to recommendations, awareness and reporting of herbal medicines among Jordanian community pharmacists. Pharmacists need enhanced education to provide objective and evidence-based information on the benefits–risks of herbal medicines. Future studies need to be carried out to confirm whether our findings are transferable to other Middle Eastern countries.

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“…Anlamlert et al investigated the effect of pomelo pulp on the pharmacokinetics of cyclosporine in healthy Thai volunteers who received 250 g of pomelo pulp or 250 ml of water 1 h before drug administration and once again 10 min following drug administration. Coadministration of pomelo pulp increased the mean AUC and C max values of cyclosporine by 28.8% and 36.1%, respectively [ 70 ]. These pharmacokinetic changes were in close agreement with the results derived from the study of pomelo juice–cyclosporine interaction in healthy volunteers [ 42 ], suggesting that the active components in pomelo pulp are sufficient to increase oral bioavailability of cyclosporine.…”

Section: Discussionmentioning

confidence: 99%

Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review

Chen

Zhou

Fabriaga

et al. 2018

Journal of Food and Drug Analysis

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This review addressed drug interactions precipitated by fruit juices other than grapefruit juice based on randomized controlled trials (RCTs). Literature was identified by searching PubMed, Cochrane Library, Scopus and Web of Science till December 30 2017. Among 46 finally included RCTs, six RCTs simply addressed pharmacodynamic interactions and 33 RCTs studied pharmacokinetic interactions, whereas seven RCTs investigated both pharmacokinetic and pharmacodynamic interactions. Twenty-two juice-drug combinations showed potential clinical relevance. The beneficial combinations included orange juice-ferrous fumarate, lemon juice-Tc-tetrofosmin, pomegranate juice-intravenous iron during hemodialysis, cranberry juice-triple therapy medications for H. pylori, blueberry juice-etanercept, lime juice-antimalarials, and wheat grass juice-chemotherapy. The potential adverse interactions included decreased drug bioavailability (apple juice-fexofenadine, atenolol, aliskiren; orange juice-aliskiren, atenolol, celiprolol, montelukast, fluoroquinolones, alendronate; pomelo juice-sildenafil; grape juice-cyclosporine), increased bioavailability (Seville orange juice-felodipine, pomelo juice-cyclosporine, orange-aluminum containing antacids). Unlike furanocoumarin-rich grapefruit juice which could primarily precipitate drug interactions by strong inhibition of cytochrome P450 3A4 isoenzyme and P-glycoprotein and thus cause deadly outcomes due to co-ingestion with some medications, other fruit juices did not precipitate severely detrimental food-drug interaction despite of sporadic case reports. The extent of a juice-drug interaction may be associated with volume of drinking juice, fruit varieties, type of fruit, time between juice drinking and drug intake, genetic polymorphism in the enzymes or transporters and anthropometric variables. Pharmacists and health professionals should properly screen for and educate patients about potential adverse juice-drug interactions and help minimize their occurrence. Much attention should be paid to adolescents and the elderly who ingest medications with drinking fruit juices or consume fresh fruits during drug treatment. Meanwhile, more researches in this interesting issue should be conducted.

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Pomelo enhances cyclosporine bioavailability in healthy male thai volunteers

Cited by 12 publications

References 37 publications

Effect of Pomelo Juice on the Pharmacokinetics of Simvastatin, CYP3A2 Activity and Mdr1a, Mdr1b and Slc21a5 Expressions in Rats

Effect of Pomelo Juice on the Pharmacokinetics of Simvastatin, CYP3A2 Activity and Mdr1a, Mdr1b and Slc21a5 Expressions in Rats

Herbal supplements in Jordan: a cross-sectional survey of pharmacists’ perspectives and knowledge

Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review

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