Prednisone with Saiboku-To Interaction Details
Brand Names Associated with Prednisone
- Cortan®
- Deltasone®
- Orasone®
- Prednisone
- Prednisone Intensol
- Rayos®
- Sterapred®
- Sterapred® DS
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 05, 2023
Interaction Effect
Enhanced and prolonged effect of corticosteroids
Interaction Summary
Saiboku-To components glycyrrhetinic acid and glycyrrhizin inhibit the metabolism of corticosteroids, delaying their excretion and prolonging their activity. In healthy subjects, area under the curve (AUC) of prednisolone was increased and clearance of prednisolone was decreased with concomitant use of Saiboku-To and licorice component glycyrrhizin . Patients taking Saiboku-To and corticosteroids concomitantly should be monitored closely for corticosteroid excess.
Severity
Moderate
Onset
Delayed
Evidence
Probable
How To Manage Interaction
The dose of the corticosteroid may need to be reduced if saiboku-to is used consistently and the saiboku-to product contains a standard amount of active ingredients.
Mechanism Of Interaction
Inhibition of corticosteroid metabolism
Literature Reports
A) In an open, cross-over study of 9 subjects receiving a single oral dose of 10 mg prednisolone, Saiboku-To given three times daily for 3 days increased the area under the curve (AUC) of prednisolone from 0.92 milligrams/hour/liter (mg/hour/L) to 1.06 mg/hour/L (p less than 0.01). Clearance of prednisolone was reduced by Saiboku-To from 10.9 +/- 0.9 L/hour to 9.6 +/- 1.1 L/hour (p less than 0.01). Subjects were nonsmokers, and were not taking any medication known to influence glucocorticoid hepatic metabolism or pharmacokinetics. The Saiboku-To preparation provided glycyrrhizin 63.5 mg daily. AUC ratio of prednisone to prednisolone decreased significantly (p less than 0.01), indicating inhibition of 11-beta-hydroxysteroid dehydrogenase .
B) Pharmacokinetics of prednisolone were significantly affected when glycyrrhizin 200 mg was administered intravenously (IV) with prednisolone hemisuccinate 0.096 milligrams/kilogram (mg/kg) IV in 6 healthy men. Total prednisolone concentration was increased at 6 and 8 hours and free prednisolone concentration was increased at 4, 6, and 8 hours after the prednisolone hemisuccinate infusion (p less than 0.05). Area under the curve (AUC) of free prednisolone increased from 126 +/- 10 micrograms/liter/hour (mcg/L/hour) to 199 +/- 24 mcg/L/hour (p less than 0.05). Clearance of free prednisolone decreased from 0.22 +/- 0.02 L/kg/hour to 0.38 +/- 0.05 L/kg/hour (p less than 0.05). Proposed mechanisms for the alteration of prednisolone pharmacokinetics by glycyrrhizin or its metabolites were (1) inhibition of protein binding, (2) inhibition of hydrolysis of prednisolone hemisuccinate to prednisolone, and (3) inhibition or metabolism of free prednisolone .
C) Oral glycyrrhizin significantly altered pharmacokinetics of prednisolone in 6 healthy men. Glycyrrhizin was administered as four 50 mg doses prior to intravenous administration of prednisolone hemisuccinate 0.096 mg/kg. Total prednisolone concentration was increased at 6 and 8 hours, and free prednisolone concentration was increased at 4, 6, and 8 hours post-prednisolone infusion (p less than 0.05). AUC of both total and free prednisolone increased significantly (p less than 0.05). Clearance of both total and free prednisolone decreased significantly (p less than 0.05). Volume of distribution was not significantly altered, suggesting that oral glycyrrhizin increases prednisolone concentrations by inhibiting metabolism, not by affecting distribution .
D) In rats, glycyrrhizic acid and glycyrrhetinic acid inhibited 11 beta-dehydrogenase in a dose-dependent manner. Percent conversion of corticosterone to 11-dehydrocorticosterone was 51.7 +/- 1.5% in controls versus 43.2 +/- 2.3% (p less than 0.001) in rats receiving glycyrrhizic acid. While glycyrrhetinic acid inhibited the conversion in dose-dependent fashion, it required high concentrations to do so (0.0001 to 0.000001M) .
E) In male rats glycyrrhetinic acid 50 mg/100 grams body weight administered intramuscularly (IM) for 7 days, produced near complete inhibition of 5-beta reductase inhibition of cortisol (7.4 +/- 5.1%; p less than 0.001). Glycyrrhizin 50 mg/100 grams body weight was less effective, but still achieved statistical significance in 5-beta reductase inhibition of cortisol (75.0 +/- 4.4%; p less than 0.001) .
F) Glycyrrhizin has shown an enhancing effect on the immunosuppressive action of cortisone. In a study of immunized rats, glycyrrhizin administered as 15 mg/kg and 30 mg/kg suppressed the antibody titer to one-half and to one-fourth of the control, respectively. Glycyrrhizin had no effect on the antibody titer in adrenalectomized rats .
Prednisone Overview
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Prednisone is used alone or with other medications to treat the symptoms of low corticosteroid levels (lack of certain substances that are usually produced by the body and are needed for normal body functioning). Prednisone is also used to treat other conditions in patients with normal corticosteroid levels. These conditions include certain types of arthritis; severe allergic reactions; multiple sclerosis (a disease in which the nerves do not function properly); lupus (a disease in which the body attacks many of its own organs); and certain conditions that affect the lungs, skin, eyes, kidneys blood, thyroid, stomach, and intestines. Prednisone is also sometimes used to treat the symptoms of certain types of cancer. Prednisone is in a class of medications called corticosteroids. It works to treat patients with low levels of corticosteroids by replacing steroids that are normally produced naturally by the body. It works to treat other conditions by reducing swelling and redness and by changing the way the immune system works.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.