Busulfan Injection and Ketobemidone: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Ketobemidone
No brand names on recordBusulfan Injection
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
An increase in busulfan and ketobemidone plasma levels
Interaction Deep Dive
The use of ketobemidone during high-dose busulfan therapy is not recommended without drug monitoring. High plasma levels of busulfan may result and these are correlated with a higher risk of drug-related toxicity. Dosage adjustment of busulfan and ketobemidone during concomitant therapy may result in decreased drug-related toxicity and transplantation-related mortality1.
Why it happens (mechanism)
Unknown
Literature reports
1 report — tap to read
a) A case report describes a possible interaction between ketobemidone and busulfan. Ketobemidone was administered to a 33-year old patient with acute myeloid leukemia for a rectal fissure. The patient's myeloablative regimen before bone marrow transplantation consisted of busulfan (1mg/kg) followed by cyclophosphamide (60 mg/kg intravenous for 2 days). The area under the concentration-time curve (AUC) of busulfan was elevated (7,352 ng h/ml) compared to the mean AUC of busulfan (5,500 ng h/ml). The minimum (trough) concentration after the second and third dose was also increased (between 750 ng/ml to 1,000 ng/ml; normal mean minimum concentration 600 ng/ml). Liver enzymes were elevated within the first two days of therapy. The dose of busulfan was reduced to 0.7 mg/kg and busulfan and ketobemidone levels remained elevated. Ketobemidone dose was reduced (100 mg/day) which resulted in a subsequent decrease in the mean minimum concentration of busulfan and a normalization of liver enzymes. An increase in busulfan concentrations occurred after an increase in ketobemidone dose to 500 mg/day. No further episodes of toxicity were experienced 1.
Common questions
Can I take Busulfan Injection and Ketobemidone together?
An increase in busulfan and ketobemidone plasma levels Always confirm with your pharmacist or prescriber before making any change.
How serious is the Busulfan Injection and Ketobemidone interaction?
It is rated moderate. Can be significant — usually manageable with monitoring.
How quickly could this interaction happen?
The documented onset is "delayed". Effects tend to build up gradually over days to weeks.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Busulfan Injection or Ketobemidone need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there anything you'd monitor while I'm on both?
References (1)
- Hassan M, Svensson J, Nilsson C, et al: Ketobemidone may alter busulfan pharmacokinetics during high-dose therapy. Ther Drug Monit 2000; 22:383-385. DOI
Keep reading about Ketobemidone
Keep reading about Busulfan Injection
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