Effects of bile salts on the lovastatin pharmacokinetics following oral administration to rats

Kim, Kyung‐Hee; Yoon, Inkyung; Chun, In‐Koo; Lee, Nayoung; Kim, Taekrho; Gwak, Hye Sun

doi:10.3109/10717544.2010.512024

Cited by 27 publications

(15 citation statements)

References 21 publications

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“…Not only does bile salt malabsorption lead to choleretic diarrhea, but the enterohepatic circulation of bile salts also influences medication absorption. Drugs that are excreted in bile and have the duration of their action enhanced by enterohepatic circulation or are disrupted by bile salt malabsorption 13 include mycophenolic acid, 14 warfarin, 13 digoxin, 15 oral contraceptives, cyclosporine, 16 – 18 tacrolimus, 18 and the statins 19 . Bioavailability and effects of these drugs may be decreased by the lack of normal absorption of bile in the terminal ileum.…”

Section: Surgical Modificationsmentioning

confidence: 99%

“…Since this diverts the fecal stream at least 100 cm above the terminal ileum, it can be thought of as either a proximal ileostomy or a distal jejeunostomy and may produce the bile salt malabsorption seen with patients with short gut. This predictably leads to malabsorption of drugs such as mycophenolic acid, 14 warfarin, 13 digoxin, 15 oral contraceptives, cyclosporine, 16 – 18 tacrolimus, 18 and the statins 19 . Although the loop ileostomy is temporary, the consequences of malabsorption of these agents can be long term and anticipated.…”

Section: Surgical Modificationsmentioning

confidence: 99%

“…Drugs that are excreted in bile and have the duration of their action enhanced by enterohepatic circulation or are disrupted by bile salt malabsorption 13 include mycophenolic acid, 14 warfarin, 13 digoxin, 15 oral contraceptives, cyclosporine, [16][17][18] tacrolimus, 18 and the statins. 19 Bioavailability and effects of these drugs may be decreased by the lack of normal absorption of bile in the terminal ileum. Instead of recycling and resecreting in the bile, these bile salts are excreted in feces, limiting bioavailability and decreasing the duration they are available for therapeutic effect.…”

Section: Small Intestinal Resectionsmentioning

confidence: 99%

“…This predictably leads to malabsorption of drugs such as mycophenolic acid, 14 warfarin, 13 digoxin, 15 oral contraceptives, cyclosporine, [16][17][18] tacrolimus, 18 and the statins. 19 Although the loop ileostomy is temporary, the consequences of malabsorption of these agents can be long term and anticipated. For subtotal colonic resection, no modification of pharmacologic dosing may be necessary.…”

Section: Colonic Resectionsmentioning

confidence: 99%

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Consequences of Gastrointestinal Surgery on Drug Absorption

2013

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Gastrointestinal (GI) surgery associated with resection or bypass can affect the absorption and kinetics of certain drugs. The goal of this article is 3-fold: (1) highlight the physiologic changes associated with selected GI surgeries (specifically gastric, small intestine, and colon), (2) review the implications for drug and nutrient absorption, and (3) suggest modifications of the pharmacologic agents, dosing regimens, and routes of delivery. Few large trials are available to use as references, but there is a wealth of individual reports and small series. Understanding the predictable challenges of drug administration in these patients will improve care.

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Section: Surgical Modificationsmentioning

confidence: 99%

Section: Surgical Modificationsmentioning

confidence: 99%

Section: Small Intestinal Resectionsmentioning

confidence: 99%

Section: Colonic Resectionsmentioning

confidence: 99%

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Consequences of Gastrointestinal Surgery on Drug Absorption

2013

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“…Serum bile acid concentrations may be increased in RYGB patients [21]. Certain medications such as lovastatin and pravastatin have shown increased absorption with increasing concentrations of bile acids [22,23]. However, bile acids are not in high concentrations in the alimentary limb so the overall effect is unclear.…”

Section: Pharmacokinetic Changes After Bariatric Surgerymentioning

confidence: 99%

Pharmacokinetic Changes Secondary to Roux en Y Gastric Bypass

Giuliano¹

2012

Adv Pharmacoepidem Drug Safety

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Objective: To review the influence of Roux-en-Y gastric bypass (RYGB) on pharmacokinetic parameters of medications.Data sources: PubMed was searched from inception to September 2012 to identify studies. Search terms included bariatric surgery, gastric bypass, Roux-en-Y, pharmacokinetic, and absorption. Studies included for this review were limited to English language studies published in full.Data synthesis: Obesity is a major health care concern and is on the rise. This has led to an increasing number of bariatric surgeries. Such procedures may have profound effects on pharmacokinetic parameters of many medications depending on the extent of surgical changes that are made. Surgical procedures such as RYGB are most likely to affect medication absorption. Factors that may affect medication absorption in RYGB patients include changes in intestinal or gastric pH, surface area, intestinal metabolism and transport mechanisms. Published studies have been primarily conducted in RYGB patients and have shown varied effect on overall absorption of medications.Conclusions: RYGB may have profound effects on medication absorption. Predicting absorption is difficult due to interplay of several factors including, changes in intestinal surface area, intestinal metabolism, efflux pumps, active transporters and gastrointestinal pH. Future studies are needed, particularly studies evaluating medications that have a low bioavailability and are commonly used in the bariatric surgery population.

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