Effect of Sucralfate on Phenytoin Bioavailability

Hall, Thomas G.; Cuddy, Paul G.; Glass, Cynthia J.; Melethil, Srikumaran

doi:10.1177/106002808602000726

Cited by 17 publications

(4 citation statements)

References 20 publications

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“…Coadministration of the following drugs with sucralfate results in a substantially decreased bioavailability of single doses of the drug: ciprofloxacin, theophylline, tetracycline, doxycycline, minocycline, phenytoin, and digoxin . The bioavailability of digoxin, tetracycline, doxycycline, and phenytoin was not decreased when they were given 2 hours before sucralfate.…”

Section: Mechanism Of Action Biological Targets Efficacy Adverse Ementioning

confidence: 99%

ACVIM consensus statement: Support for rational administration of gastrointestinal protectants to dogs and cats

Marks

Kook

Papich

et al. 2018

Veterinary Internal Medicne

102

177

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The gastrointestinal (GI) mucosal barrier is continuously exposed to noxious toxins, reactive oxygen species, microbes, and drugs, leading to the development of inflammatory, erosive, and ultimately ulcerative lesions. This report offers a consensus opinion on the rational administration of GI protectants to dogs and cats, with an emphasis on proton pump inhibitors (PPIs), histamine type‐2 receptor antagonists (H2RAs), misoprostol, and sucralfate. These medications decrease gastric acidity or promote mucosal protective mechanisms, transforming the management of dyspepsia, peptic ulceration, and gastroesophageal reflux disease. In contrast to guidelines that have been established in people for the optimal treatment of gastroduodenal ulcers and gastroesophageal reflux disease, effective clinical dosages of antisecretory drugs have not been well established in the dog and cat to date. Similar to the situation in human medicine, practice of inappropriate prescription of acid suppressants is also commonplace in veterinary medicine. This report challenges the dogma and clinical practice of administering GI protectants for the routine management of gastritis, pancreatitis, hepatic disease, and renal disease in dogs and cats lacking additional risk factors for ulceration or concerns for GI bleeding. Judicious use of acid suppressants is warranted considering recent studies that have documented adverse effects of long‐term supplementation of PPIs in people and animals.

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Section: Mechanism Of Action Biological Targets Efficacy Adverse Ementioning

confidence: 99%

ACVIM consensus statement: Support for rational administration of gastrointestinal protectants to dogs and cats

Marks

Kook

Papich

et al. 2018

Veterinary Internal Medicne

102

177

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“…Several reports have demonstrated the pharmacokinetic drug interaction of sucralfate with chemically diversified classes of drugs. [6][7][8][9][10][11][12] In most of these cases, absorption of the concomitant drug was hindered either by chelation or adsorption of the drug to sucralfate. The objective of the present study is to investigate whether sucralfate pretreatment has any effect on the oral absorption and pharmacokinetics of rosiglitazone.…”

mentioning

confidence: 99%

Lack of Effect of Sucralfate on the Absorption and Pharmacokinetics of Rosiglitazone

Rao

Mullangi

Katneni

et al. 2002

The Journal of Clinical Pharma

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The aim of the present study was to investigate the effect of sucralfate pretreatment on the pharmacokinetics of rosiglitazone following a single oral dose in healthy male volunteers. After an over night fast, and according to a randomized schedule, each volunteer (n = 9) received a single oral dose of rosiglitazone 8 mg (Avandia tablets, 4 mg x 2) with or without pretreatment of sucralfate 2 g (Recolfate tablets, 1 g x 2) in an open-label crossover study with a 2-week washout period. Plasma samples were collected over a period of 24 hours at regular intervals. Safety assessment included monitoring of the vital signs, blood parameters, and ECG. No statistically significant differences (p > 0.05) were observed for any of the calculated rosiglitazone pharmacokinetic parameters in the two treatment groups. The mean parameters, AUC0-infinity and Cmax, following rosiglitazone administration alone were 3825.02 ng x h/ml and 664.47 ng/ml, respectively, and for rosiglitazone administered after pretreatment with sucralfate were 4848.19 ng x h/ml and 624.88 ng/ml, respectively. The t(max) for rosiglitazone alone and for rosiglitazone after sucralfate treatments was 1.11 and 1.67 hours, respectively. The mean elimination half-life for rosiglitazone and rosiglitazone after sucralfate treatment was 4.35 and 4.51 hours, respectively. Fraction of rosiglitazone absorbed was calculated by the Wagner-Nelson method, and no statistically significant difference (p > 0.05) was observed for the two treatments. Since sucralfate pretreatment did not show any significant difference in the pharmacokinetics of rosiglitazone, no dose adjustment is warranted for rosiglitazone when it is administered with sucralfate.

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“…Administration of this agent has been shown to lower concentrations of norfloxacin and phenytoin, but neither prednisone nor erythromycin, in plasma (8,11,16,18). Since sucralfate has not been reported to alter gastric acidity, these interactions are thought to result from binding of the affected drug to either the aluminum or sulfated sucrose moiety and not from changes in gastric pH (15,17).…”

mentioning

confidence: 99%

Effects of ranitidine and sucralfate on ketoconazole bioavailability

Piscitelli

Goss

Wilton

et al. 1991

Antimicrob Agents Chemother

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Ketoconazole is an oral imidazole antifungal agent useful in the treatment of opportunistic fungal infections. Gastrointestinal absorption of this agent is variable and dependent on the presence of gastric acid. This study compared the effects of concomitant sucralfate administration with ranitidine administration on the pharmacokinetic disposition of a 400-mg ketoconazole dose. Six healthy male volunteers were randomized to receive 400 mg of ketoconazole alone, 1.0 g of sucralfate concomitantly with a 400-mg ketoconazole dose, or ranitidine, administered 2 h prior to a 400-mg ketoconazole dose to titrate to a gastric pH of 6. All subjects received all three regimens in crossover fashion. Gastric pH was measured continuously for 4 h after ketoconazole administration in all subjects by using a Heidelberg radiotelemetry pH capsule. Relative ketoconazole bioavailability was compared between treatments. With sucralfate, five of six subjects demonstrated a decrease in the peak drug concentration in serum as well as an increase in the time to peak concentration, indicating a delay in ketoconazole absorption. The mean area under the concentration-time curve from 0 to 12 h for ketoconazole following gastric alkalinization was significantly different from that of either ketoconazole alone or ketoconazole with sucralfate (P < 0.01). Continuous gastric pH monitoring allowed correlation between the decrease in ketoconazole bioavailability observed with ranitidine and the increase in gastric pH. The apparent decrease in ketoconazole bioavailability observed with sucralfate appears to be caused by an alternative mechanism since a change in gastric pH was not observed. On the basis of these findings, separating the administration of ketoconazole and sucralfate should be considered to decrease the potential for interaction of sucralfate on ketoconazole bioavailability.

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Effect of Sucralfate on Phenytoin Bioavailability

Cited by 17 publications

References 20 publications

ACVIM consensus statement: Support for rational administration of gastrointestinal protectants to dogs and cats

ACVIM consensus statement: Support for rational administration of gastrointestinal protectants to dogs and cats

Lack of Effect of Sucralfate on the Absorption and Pharmacokinetics of Rosiglitazone

Effects of ranitidine and sucralfate on ketoconazole bioavailability

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