From the Guidelines
Linezolid has nearly 100% oral bioavailability.
Key Points
- The oral bioavailability of linezolid is 100%, making it an effective option for treatment of various infections, including those caused by methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) 1.
- This high bioavailability means that the oral dose of linezolid is the same as the intravenous dose, simplifying treatment regimens 1.
- The excellent bioavailability of linezolid is also noted in the context of treating prosthetic joint infections, where it is listed among oral antibiotic regimens with excellent bioavailability 1.
- The high oral bioavailability of linezolid is consistent across different studies and guidelines, including those from the Infectious Diseases Society of America 1.
Clinical Implications
- The 100% oral bioavailability of linezolid allows for flexible treatment options, including oral administration, which can be particularly beneficial for patients who have difficulties with intravenous access or prefer oral medications 1.
- However, it's crucial to consider the potential for adverse effects, such as hematologic toxicity and neuropathies, especially with long-term use 1.
- Clinicians should be aware of the potential for drug interactions, including the risk of serotonin syndrome when linezolid is used concurrently with selective serotonin reuptake inhibitors 1.
From the FDA Drug Label
Linezolid is rapidly and extensively absorbed after oral dosing. ... The absolute bioavailability is approximately 100% The bioavailability of linezolid is approximately 100% 2.
From the Research
Bioavailability of Linezolid
- The bioavailability of linezolid is approximately 100% 3, 4, 5, indicating that the oral and intravenous formulations are equivalent in terms of absorption.
- A study found that the mean absolute bioavailability of linezolid tablets was 103% (+/-20%) when compared to an intravenous sterile solution 3.
- The presence of food or enteral feedings does not significantly affect the bioavailability of linezolid 3, 6.
- Linezolid can be administered orally or intravenously without changing the drug or dosage regimen, making it a convenient option for patients 4, 5.
Factors Affecting Bioavailability
- The absorption of linezolid is not significantly affected by the presence of a high-fat meal 3.
- Enteral feedings do not alter the bioavailability of linezolid 6.
- The bioavailability of linezolid is not affected by renal failure or other clinical conditions 7.
Clinical Implications
- The high bioavailability of linezolid makes it an effective option for the treatment of serious Gram-positive infections 4, 5.
- Linezolid can be used as an alternative to vancomycin in patients with impaired renal function or poor intravenous access 4.
- The oral formulation of linezolid can be used for step-down therapy from intravenous to oral administration 5.