Drug Interactions between Baycol and Locholest
This report displays the potential drug interactions for the following 2 drugs:
- Baycol (cerivastatin)
- Locholest (cholestyramine)
Interactions between your drugs
cholestyramine cerivastatin
Applies to: Locholest (cholestyramine) and Baycol (cerivastatin)
ADJUST DOSING INTERVAL: When administered concomitantly, cholestyramine decreases the bioavailability and peak plasma concentration of cerivastatin, most likely due to adsorption of the statin to the resin. In one study, the bioavailability was reduced by 21% and the peak plasma concentration by 41% under fasting conditions. Separating their administration times by 1 to 5 hours attenuated the effect, resulting in a reduction of 8% to 16% in the bioavailability, depending on length of time between the doses.
MANAGEMENT: If simultaneous therapy with both agents is desired, cerivastatin should be administered several hours after the bile acid binding resin.
References
- Smith HT, Jokubaitis LA, Troendle AJ, Hwang DS, Robinson WT "Pharmacokinetics of fluvastatin and specific drug interactions." Am J Hypertens 6 (1993): s375-82
- "Product Information. Baycol (cerivastatin)." Bayer PROD (2001):
- Muck W, Ritter W, Frey R, Wetzelsberger N, Lucker PW, Kuhlmann J "Influence of cholestyramine on the pharmacokinetics of cerivastatin." Int J Clin Pharmacol Ther 35 (1997): 1997
Drug and food interactions
cerivastatin food
Applies to: Baycol (cerivastatin)
GENERALLY AVOID: Coadministration with grapefruit juice may increase the plasma concentrations of atorvastatin. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. When a single 40 mg dose of atorvastatin was coadministered with 240 mL of grapefruit juice, atorvastatin peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 16% and 37%, respectively. Greater increases in Cmax (up to 71%) and/or AUC (up to 2.5 fold) have been reported with excessive consumption of grapefruit juice (>=750 mL to 1.2 liters per day). Clinically, high levels of HMG-CoA reductase inhibitory activity in plasma is associated with an increased risk of musculoskeletal toxicity. Myopathy manifested as muscle pain and/or weakness associated with grossly elevated creatine kinase exceeding ten times the upper limit of normal has been reported occasionally. Rhabdomyolysis has also occurred rarely, which may be accompanied by acute renal failure secondary to myoglobinuria and may result in death.
ADJUST DOSING INTERVAL: Fibres such as oat bran and pectin may diminish the pharmacologic effects of HMG-CoA reductase inhibitors by interfering with their absorption from the gastrointestinal tract.
MANAGEMENT: Patients receiving therapy with atorvastatin should limit their consumption of grapefruit juice to no more than 1 liter per day. Patients should be advised to promptly report any unexplained muscle pain, tenderness or weakness, particularly if accompanied by fever, malaise and/or dark colored urine. Therapy should be discontinued if creatine kinase is markedly elevated in the absence of strenuous exercise or if myopathy is otherwise suspected or diagnosed. In addition, patients should either refrain from the use of oat bran and pectin or, if concurrent use cannot be avoided, to separate the administration times by at least 2 to 4 hours.
References
- Richter WO, Jacob BG, Schwandt P "Interaction between fibre and lovastatin." Lancet 338 (1991): 706
- McMillan K "Considerations in the formulary selection of hydroxymethylglutaryl coenzyme a reductase inhibitors." Am J Health Syst Pharm 53 (1996): 2206-14
- "Product Information. Lipitor (atorvastatin)." Parke-Davis PROD (2001):
- Boberg M, Angerbauer R, Fey P, Kanhai WK, Karl W, Kern A, Ploschke J, Radtke M "Metabolism of cerivastatin by human liver microsomes in vitro. Characterization of primary metabolic pathways and of cytochrome P45 isozymes involved." Drug Metab Dispos 25 (1997): 321-31
- Bailey DG, Malcolm J, Arnold O, Spence JD "Grapefruit juice-drug interactions." Br J Clin Pharmacol 46 (1998): 101-10
- Lilja JJ, Kivisto KT, Neuvonen PJ "Grapefruit juice increases serum concentrations of atorvastatin and has no effect on pravastatin." Clin Pharmacol Ther 66 (1999): 118-27
- Neuvonen PJ, Backman JT, Niemi M "Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin." Clin Pharmacokinet 47 (2008): 463-74
cholestyramine food
Applies to: Locholest (cholestyramine)
ADJUST DOSING INTERVAL: Bile acid sequestrants and the phosphate binder, sevelamer, can decrease the absorption of fat-soluble vitamins A, D, E, and K. In non-clinical safety studies, rats administered colesevelam at doses greater than 30-fold the projected human clinical dose developed hemorrhage in association with vitamin K deficiency. In a crossover study involving healthy subjects, coadministration of sevelamer with calcitriol resulted in a significant reduction in bioavailability for calcitriol (calcitriol with sevelamer vs calcitriol alone: AUC 137 pg*h/mL vs 318 pg*h/mL and Cmax 40.1 pg/mL vs 49.7 pg/mL, respectively).
MANAGEMENT: Oral vitamin supplements should be administered at least 4 hours before colesevelam and either 1 hour before or 4 to 6 hours after other bile acid sequestrants and sevelamer.
References
- "Product Information. Rocaltrol (calcitriol)." Roche Laboratories PROD (2001):
- "Product Information. Welchol (colesevelam)." Daiichi Sankyo, Inc. PROD (2001):
- "Product Information. Fosamax Plus D (alendronate-cholecalciferol)." Merck & Co., Inc (2005):
- Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
- Cerner Multum, Inc. "Australian Product Information." O 0
- Peirce D, Hossack S, Poole L, et al. "The effect of sevelamer carbonate and lanthanum carbonate on the pharmacokinetics of oral calcitriol." Nephrol Dial Transplant 26 (2011): 1615-21
Therapeutic duplication warnings
No warnings were found for your selected drugs.
Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.
See also
Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
No interaction information available. |
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Check Interactions
To view an interaction report containing 4 (or more) medications, please sign in or create an account.
Save Interactions List
Sign in to your account to save this drug interaction list.