Linezolid 2 mg/mL Injection, Solution
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Oxazolidinone Antibacterial class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Linezolid injection is used to treat infections caused by bacteria. Linezolid is in a class of antibacterials called oxazolidinones. It works by stopping the growth of bacteria. Antibiotics such as linezolid injection will not kill viruses that can cause colds, flu, or other infections. Using antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.
Read the full MedlinePlus article ↗- Linezolid is reserved for infections caused by bacteria that are resistant to more common antibiotics — particularly MRSA (methicillin-resistant Staphylococcus aureus) and vancomyc...
- Why was I prescribed linezolid instead of a more common antibiotic?
- This is a really important question, and you're right to ask. Linezolid interacts with many antidepressants — especially SSRIs, tricyclics, and others that affect serotonin — and c...
- Can I take my antidepressant while I'm on linezolid?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Linezolid — tap one for details:
Linezolid may be associated with lower levels of 7 nutrients — worth a chat with your pharmacist, not a cause for alarm.
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
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UNII IY9XDZ35W2
Dextrose is a simple sugar derived from corn or other sources. It serves as a filler and sweetener in medicines to add bulk, improve taste, and help stabilize the medication's form.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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UNII 1Q73Q2JULR
Sodium citrate is a salt derived from citric acid. It works as a buffer to maintain the medicine's pH level and may also help improve taste or act as a preservative in the formulation.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
6 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $0.0159 | $47.70 / 3000 ml |
| Medicare drug plans payPart D · Q2 2026 | $0.1172 | $351.60 / 3000 ml |
| Medicare Part B allowsASP · J2020 | $2.268 / J2020 unit | — |
Where does this data come from?
🧾 Billing & reimbursement
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Zyvox 600 mg/300mL 00009-5140-04 | Pharmacia | 300 ml | — | AP | FDA listed | — |
| Zyvox 600 mg/300mL 00009-7807-02 | Pharmacia | 300 ml | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 00143-9534-10 | Hikma | 10 pouches | — | AP | FDA listed | — |
| Linezolid 2 mg/mL 00409-4883-01 | Hospira, | 10 pouches | — | — | Discontinued | — |
| Linezolid 600 mg/300mL 00781-3433-46 | Sandoz | 300 ml | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 55150-0242-51 | Eugia | 10 pouches | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 57664-0683-57 | Sun | 300 ml | — | AP | FDA listed | — |
| Linezolid 2 mg/mLthis 63323-0713-13 | Fresenius | 300 ml | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 65145-0181-10 | Caplin | 10 pouches | — | AP | FDA listed | — |
| Zyvox 600 mg/300mL 66298-5140-01 | Hp | 300 ml | — | AP | FDA listed | — |
| Linezolid 2 mg/mL 66298-7131-03 | Hp | 300 ml | — | AP | FDA listed | — |
| Zyvox 600 mg/300mL 66298-7807-01 | Hp | 300 ml | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 66794-0219-43 | Piramal | 300 ml | — | AP | FDA listed | — |
| Linezolid 600 mg/300mL 66794-0236-43 | Piramal | 300 ml | — | AP | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 63323-0713-13 You're viewing this | 10 BAG in 1 CASE (63323-713-13) / 300 mL in 1 BAG (63323-713-03) | 2015-06-22 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Linezolid injection is an oxazolidinone-class antibacterial indicated in adults and children for the treatment of the following infections caused by susceptible Gram-positive bacteria: Nosocomial pneumonia ( 1.1 ); Community-acquired pneumonia ( 1.2 ); Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis ( 1.3 ); Uncomplicated skin and skin structure infections ( 1.4 ); Vancomycin-resistant Enterococcus faecium infections. ( 1.5 ) Limitations of Use ( 1.6 ): Linezolid injection is not indicated for the treatment of Gram-negative infections.
The safety and efficacy of Linezolid injection formulations given for longer than 28 days have not been evaluated in controlled clinical trials. To reduce the development of drug-resistant bacteria and maintain the effectiveness of linezolid formulations and other antibacterial drugs, linezolid injection should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. ( 1.7 )
1.1Nosocomial Pneumonia Linezolid injection is indicated for the treatment of nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates) or Streptococcus pneumoniae [ see Clinical Studies ( 14 ) ].
1.2Community-acquired Pneumonia Linezolid injection is indicated for the treatment of community-acquired pneumonia caused by Streptococcus pneumoniae , including cases with concurrent bacteremia, or Staphylococcus aureus (methicillin-susceptible isolates only) [ see Clinical Studies ( 14 ) ].
1.3Complicated Skin and Skin Structure Infections Linezolid injection is indicated for the treatment of complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis, caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus pyogenes , or Streptococcus agalactiae . Linezolid injection has not been studied in the treatment of decubitus ulcers [ see Clinical Studies ( 14 ) ].
1.4Uncomplicated Skin and Skin Structure Infections Linezolid injection is indicated for the treatment of uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes [ see Clinical Studies ( 14 ) ].
1.5Vancomycin-resistant Enterococcus faecium Infections Linezolid injection is indicated for the treatment of vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia [ see Clinical Studies ( 14 ) ].
1.6Limitations of Use Linezolid injection is not indicated for the treatment of Gram-negative infections. It is critical that specific Gram-negative therapy be initiated immediately if a concomitant Gram-negative pathogen is documented or suspected [ see Warnings and Precautions ( 5.4 ) ]. The safety and efficacy of Linezolid injection formulations given for longer than 28 days have not been evaluated in controlled clinical trials [ see Clinical Studies ( 14 ) ].
1.7Usage To reduce the development of drug-resistant bacteria and maintain the effectiveness of Linezolid injection and other antibacterial drugs, Linezolid injection should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Dosage, Route, and Frequency of Administration Infection Pediatric Patients (Birth through 11 years of Age) Adults and Adolescents (12 years and Older) Duration (days ) Nosocomial pneumonia 10 mg/kg intravenous or oral every 8 hours 600 mg intravenous or oral every 12 hours 10 to 14 Community-acquired pneumonia, including concurrent bacteremia Complicated skin and skin structure infections Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia 10 mg/kg intravenous or oral every 8 hours 600 mg intravenous or oral every 12 hours 14 to 28
2.1General Dosage and Administration The recommended dosage for Linezolid formulations for the treatment of infections is described in Table 1 . Table 1. Dosage Guidelines for Linezolid * Due to the designated pathogens [see Indications and Usage ( 1 )] † Neonates less than 7 days : Most pre-term neonates less than 7 days of age (gestational age less than 34 weeks) have lower systemic linezolid clearance values and larger AUC values than many full-term neonates and older infants.
These neonates should be initiated with a dosing regimen of 10 mg/kg every 12 hours. Consideration may be given to the use of 10 mg/kg every 8 hours regimen in neonates with a sub-optimal clinical response. All neonatal patients should receive 10 mg/kg every 8 hours by 7 days of life [see Use in Specific Populations ( 8.4 ) and Clinical Pharmacology ( 12.3 )] . ‡ Oral dosing using either Linezolid Tablets or Linezolid for Oral Suspension [see How Supplied/Storage and Handling ( 16 )] .
Infection* Dosage, Route and Frequency of Administration Recommended Duration of Treatment (consecutive days) Pediatric Patients † (Birth through 11 Years of Age) Adults and Adolescents (12 Years and Older) Nosocomial pneumonia 10 mg/kg intravenously or oral ‡ every 8 hours 600 mg intravenously or oral ‡ every 12 hours 10 to 14 Community-acquired pneumonia, including concurrent bacteremia Complicated skin and skin structure infections Vancomycin-resistant Enterococcus faecium infections , including concurrent bacteremia 10 mg/kg intravenously or oral ‡ every 8 hours 600 mg intravenously or oral ‡ every 12 hours 14 to 28 No dose adjustment is necessary when switching from intravenous to oral administration.
2.2Intravenous Administration Linezolid injection is supplied in single-dose, ready-to-use flexible plastic containers. Parenteral drug products should be inspected visually for particulate matter prior to administration. Check for minute leaks by firmly squeezing the bag.
If leaks are detected, discard the solution, as sterility may be impaired. Keep the infusion bags in the overwrap until ready to use. Store at room temperature.
Protect from freezing. Linezolid injection may exhibit a yellow color that can intensify over time without adversely affecting potency. Linezolid injection should be administered by intravenous infusion over a period of 30 to 120 minutes.
Do not use this intravenous flexible plastic container in series connections . Additives should not be introduced into this solution. If Linezolid injection is to be given concomitantly with another drug, each drug should be given separately in accordance with the recommended dosage and route of administration for each product.
Discard unused portion. If the same intravenous line is used for sequential infusion of several drugs, the line should be flushed before and after infusion of Linezolid injection with an infusion solution compatible with Linezolid injection and with any other drug(s) administered via this common line.
2.3Compatibilities Compatible intravenous solutions include 0.9% Sodium Chloride Injection, USP, 5% Dextrose Injection, USP, and Lactated Ringer's Injection, USP.
2.4Incompatibilities Physical incompatibilities resulted when Linezolid injection was combined with the following drugs during simulated Y-site administration: amphotericin B, chlorpromazine HCl, diazepam, pentamidine isothionate, er…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Linezolid injection: 600 mg/300 mL (2 mg per mL) linezolid single-dose, ready-to-use flexible plastic container in a foil laminate overwrap. The flexible plastic container and port are latex-free. Injection: 600 mg/300 mL (2 mg per mL) linezolid. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Known hypersensitivity to linezolid or any of the other product components. ( 4.1 ) Patients taking any monoamine oxidase inhibitors (MAOI) or within two weeks of taking an MAOI. ( 4.2 )
4.1Hypersensitivity Linezolid injection is contraindicated for use in patients who have known hypersensitivity to linezolid or any of the other product components.
4.2Monoamine Oxidase Inhibitors Linezolid should not be used in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g., phenelzine, isocarboxazid) or within two weeks of taking any such medicinal product.
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Myelosuppression: Monitor complete blood counts weekly. Thrombocytopenia has been reported more often in patients with severe renal and in patients with moderate to severe hepatic impairment. Consider discontinuation in patients who develop or have worsening myelosuppression.
( 5.1 ) Peripheral and Optic Neuropathy: Reported primarily in patients treated for longer than 28 days. If patients experience symptoms of visual impairment, prompt ophthalmic evaluation is recommended. ( 5.2 ) Serotonin Syndrome: Monitor patients taking serotonergic agents, including antidepressants and opioids, for signs of serotonin syndrome.
Patients taking serotonergic antidepressants should receive Linezolid injection only if no other therapies are available. Discontinue serotonergic antidepressants and monitor patients for signs and symptoms of both serotonin syndrome and antidepressant discontinuation. ( 5.3 ) A mortality imbalance was seen in an investigational study in linezolid- treated patients with catheter-related bloodstream infections.
( 5.4 ) Clostridioides difficile- Associated Diarrhea: Evaluate if diarrhea occurs. ( 5.5 ) Potential interactions producing elevation of blood pressure: monitor blood pressure. ( 5.6 ) Hypoglycemia: Postmarketing cases of symptomatic hypoglycemia have been reported in patients with diabetes mellitus receiving insulin or oral hypoglycemic agents.
( 5.9 ) Hyponatremia and/or Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH): Monitor serum sodium levels regularly in patients at risk of hyponatremia and/or SIADH. ( 5.10 )
5.1Myelosuppression Myelosuppression (including anemia, leukopenia, pancytopenia, and thrombocytopenia) has been reported in patients receiving linezolid. In cases where the outcome is known, when linezolid was discontinued, the affected hematologic parameters have risen toward pretreatment levels. Thrombocytopenia has been reported more often in patients with severe renal impairment, whether or not on dialysis, and in patients with moderate to severe hepatic impairment.
Complete blood counts should be monitored weekly in patients who receive linezolid, particularly in those who receive linezolid for longer than two weeks, those with pre-existing myelosuppression, those with severe renal impairment or moderate to severe hepatic impairment, those receiving concomitant drugs that produce bone marrow suppression, or those with a chronic infection who have received previous or concomitant antibacterial drug therapy. Discontinuation of therapy with linezolid should be considered in patients who develop or have worsening myelosuppression [ see Adverse Reactions ( 6.2 ) ].
5.2Peripheral and Optic Neuropathy Peripheral and optic neuropathies have been reported in patients treated with Linezolid injection, primarily in those patients treated for longer than the maximum recommended duration of 28 days. In cases of optic neuropathy that progressed to loss of vision, patients were treated for extended periods beyond the maximum recommended duration. Visual blurring has been reported in some patients treated with linezolid for less than 28 days.
Peripheral and optic neuropathy has also been reported in children. If patients experience symptoms of visual impairment, such as changes in visual acuity, changes in color vision, blurred vision, or visual field defect, prompt ophthalmic evaluation is recommended. Visual function should be monitored in all patients taking linezolid for extended periods (≥ 3 months) and in all patients reporting new visual symptoms regardless of length of therapy with linezolid.
If peripheral or optic neuropathy occurs, the continued use of linezolid in these patients should be weighed against the potential risks.
5.3Serotonin Syndrome Spontaneous reports of serotonin syndrome including fatal cases associated with the co-administration of Linezolid injection and serotonergic agents, including antidepressants such as selective serotonin…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Most common adverse reactions (>5% of adult and/or pediatric patients treated with linezolid) include: diarrhea, vomiting, headache, nausea, and anemia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Fresenius Kabi USA, LLC at 1-800-551-7176 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adults The safety of Linezolid formulations was evaluated in 2,046 adult patients enrolled in seven Phase 3 comparator-controlled clinical trials, who were treated for up to 28 days. Of the patients treated for uncomplicated skin and skin structure infections (uSSSIs), 25.4% of Linezolid-treated and 19.6% of comparator-treated patients experienced at least one drug-related adverse event.
For all other indications, 20.4% of Linezolid-treated and 14.3% of comparator-treated patients experienced at least one drug-related adverse event. Table 2 shows the incidence of all-causality, treatment-emergent adverse reactions reported in at least 1% of adult patients in these trials by dose of Linezolid. Table 2.
Incidence (%) of Treatment–Emergent Adverse Reactions Occurring in >1% of Adult Patients Treated with Linezolid in Comparator-Controlled Clinical Trials * Comparators included cefpodoxime proxetil 200 mg by mouth every 12 hours; ceftriaxone 1 g intravenously every 12 hours; dicloxacillin 500 mg by mouth every 6 hours; oxacillin 2 g intravenously every 6 hours; vancomycin 1 g intravenously every 12 hours. ADVERSE REACTIONS Uncomplicated Skin and Skin Structure Infections All Other Indications Linezolid 400 mg by mouth every 12 hours (n=548) Clarithromycin 250 mg by mouth every 12 hours (n=537) Linezolid 600 mg every 12 hours (n=1,498) All Other Comparators* (n=1,464) Headache 8.8 8.4 5.7
4.4Diarrhea 8.2 6.1 8.3
6.4Nausea 5.1 4.5 6.6
4.6Vomiting 2.0 1.5 4.3
2.3Dizziness 2.6 3.0 1.8
1.5Rash 1.1 1.1 2.3
2.6Anemia 0.4 0 2.1
1.4Taste alteration 1.8 2.0 1.0
0.3Vaginal moniliasis 1.8 1.3 1.1
0.5Oral moniliasis 0.5 0 1.7
1.0Abnormal liver function tests 0.4 0.2 1.6
0.8Fungal infection 1.5 0.2 0.3
0.2Tongue discoloration 1.3 0 0.3 0 Localized abdominal pain 1.3 0.6 1.2
0.8Generalized abdominal pain 0.9 0.4 1.2
1.0Of the patients treated for uSSSIs, 3.5% of Linezolid-treated and 2.4% of comparator-treated patients discontinued treatment due to drug-related adverse events. For all other indications, discontinuations due to drug-related adverse events occurred in 2.1% of Linezolid-treated and 1.7% of comparator-treated patients. The most common reported drug-related adverse events leading to discontinuation of treatment were nausea, headache, diarrhea, and vomiting.
Pediatric Patients The safety of Linezolid formulations was evaluated in 215 pediatric patients ranging in age from birth through 11 years, and in 248 pediatric patients aged 5 through 17 years (146 of these 248 were age 5 through 11 and 102 were age 12 to 17). These patients were enrolled in two Phase 3 comparator-controlled clinical trials and were treated for up to 28 days. In the study of hospitalized pediatric patients (birth through 11 years) with Gram-positive infections, who were randomized 2 to 1 (linezolid: vancomycin), mortality was 6.0% (13/215) in the linezolid arm and 3.0% (3/101) in the vancomycin arm.
However, given the severe underlying illness in the patient population, no causality could be established. Of the pediatric patients treated for uSSSIs, 19.2% of Linezolid-treated and 14.1% of comparator-treated patients experienced at least one drug-related adverse event. For all other indications, 18.8% of Linezolid-treated and 34.3% of comparator-treated patients experienced at least one drug-related adverse event.
Table 3 shows the incidence of all-…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Monoamine oxidase inhibitors and potential for interaction with adrenergic and serotonergic agents. ( 4.2 , 5.3 , 5.6 , 7 , 12.3 )
7.1Monoamine Oxidase Inhibitors Linezolid is a reversible, nonselective inhibitor of monoamine oxidase [ see Contraindications ( 4.2 ) and Clinical Pharmacology ( 12.3 ) ].
7.2Adrenergic and Serotonergic Agents Linezolid has the potential for interaction with adrenergic and serotonergic agents [ see Warnings and Precautions ( 5.3 , 5.6 ) and Clinical Pharmacology ( 12.3 ) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Available data from published and postmarketing case reports with linezolid use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. When administered during organogenesis, linezolid did not cause malformations in mice, rats, or rabbits at maternal exposure levels approximately 6.5 times (mice), equivalent to (rats), or 0.06 times (rabbits) the clinical therapeutic exposure, based on AUCs. However, embryo-fetal lethality was observed in mice at 6.5 times the estimated human exposure.
When female rats were dosed during organogenesis through lactation, postnatal survival of pups was decreased at doses approximately equivalent to the estimated human exposure based on AUCs ( see Data ). The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data In mice, embryo-fetal toxicities were observed only at doses that caused maternal toxicity (clinical signs and reduced body weight gain). An oral dose of 450 mg/kg/day given from Gestation Day (GD) 6-16 (6.5 times the estimated human exposure based on AUCs) correlated with increased postimplantational embryo death, including total litter loss, decreased fetal body weights, and an increased incidence of costal cartilage fusion.
Neither maternal nor embryo-fetal toxicities were observed at doses up to 150 mg/kg/day. Fetal malformations were not observed. In rats, fetal toxicity was observed at 15 and 50 mg/kg/day administered orally from GD 6-17 (exposures 0.22 times to approximately equivalent to the estimated human exposure, respectively, based on AUCs).
The effects consisted of decreased fetal body weights and reduced ossification of sternebrae, a finding often seen in association with decreased fetal body weights. Fetal malformations were not observed. Maternal toxicity, in the form of reduced body weight gain, was seen at 50 mg/kg/day.
In rabbits, reduced fetal body weight occurred only in the presence of maternal toxicity (clinical signs, reduced body weight gain and food consumption) when administered at an oral dose of 15 mg/kg/day given from GD 6-20 (0.06 times the estimated human exposure based on AUCs). Fetal malformations were not observed. When female rats were treated with 50 mg/kg/day (approximately equivalent to the estimated human exposure based on AUCs) of linezolid during pregnancy and lactation (GD 6 through Lactation Day 20), survival of pups was decreased on postnatal days 1 to 4.
Male and female pups permitted to mature to reproductive age, when mated, showed an increase in preimplantation loss.
8.2Lactation Risk Summary Linezolid is present in breast milk. Based on data from available published case reports, the daily dose of linezolid that the infant would receive from breast milk would be approximately 6% to 9% of the recommended therapeutic infant dose (10 mg/kg every 8 hours). There is no information on the effects of linezolid on the breastfed infant; however, diarrhea and vomiting were the most common adverse reactions reported in clinical trials in infants receiving linezolid therapeutically [ see Adverse Reactions ( 6.1 ) ] and (see Clinical Considerations).
There is no information on the effects of linezolid on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for linezolid and any potential adverse effects on the breastfed child from linezolid or from the underlying maternal condition. Clinical Considerations Advise lactating women to monitor a breastfed infant for diarrhea and vomiting.
8.3 Females and Males of Reproductive P…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Available data from published and postmarketing case reports with linezolid use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. When administered during organogenesis, linezolid did not cause malformations in mice, rats, or rabbits at maternal exposure levels approximately 6.5 times (mice), equivalent to (rats), or 0.06 times (rabbits) the clinical therapeutic exposure, based on AUCs. However, embryo-fetal lethality was observed in mice at 6.5 times the estimated human exposure.
When female rats were dosed during organogenesis through lactation, postnatal survival of pups was decreased at doses approximately equivalent to the estimated human exposure based on AUCs ( see Data ). The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data In mice, embryo-fetal toxicities were observed only at doses that caused maternal toxicity (clinical signs and reduced body weight gain). An oral dose of 450 mg/kg/day given from Gestation Day (GD) 6-16 (6.5 times the estimated human exposure based on AUCs) correlated with increased postimplantational embryo death, including total litter loss, decreased fetal body weights, and an increased incidence of costal cartilage fusion.
Neither maternal nor embryo-fetal toxicities were observed at doses up to 150 mg/kg/day. Fetal malformations were not observed. In rats, fetal toxicity was observed at 15 and 50 mg/kg/day administered orally from GD 6-17 (exposures 0.22 times to approximately equivalent to the estimated human exposure, respectively, based on AUCs).
The effects consisted of decreased fetal body weights and reduced ossification of sternebrae, a finding often seen in association with decreased fetal body weights. Fetal malformations were not observed. Maternal toxicity, in the form of reduced body weight gain, was seen at 50 mg/kg/day.
In rabbits, reduced fetal body weight occurred only in the presence of maternal toxicity (clinical signs, reduced body weight gain and food consumption) when administered at an oral dose of 15 mg/kg/day given from GD 6-20 (0.06 times the estimated human exposure based on AUCs). Fetal malformations were not observed. When female rats were treated with 50 mg/kg/day (approximately equivalent to the estimated human exposure based on AUCs) of linezolid during pregnancy and lactation (GD 6 through Lactation Day 20), survival of pups was decreased on postnatal days 1 to 4.
Male and female pups permitted to mature to reproductive age, when mated, showed an increase in preimplantation loss.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of Linezolid injection for the treatment of pediatric patients with the following infections are supported by evidence from adequate and well-controlled studies in adults, pharmacokinetic data in pediatric patients, and additional data from a comparator-controlled study of Gram-positive infections in pediatric patients ranging in age from birth through 11 years [ see Indications and Usage ( 1 ), Clinical Pharmacology ( 12.3 ) and Clinical Studies ( 14 ) ]: nosocomial pneumonia complicated skin and skin structure infections community-acquired pneumonia (also supported by evidence from an uncontrolled study in patients ranging in age from 8 months through 12 years) vancomycin-resistant Enterococcus faecium infections The safety and effectiveness of Linezolid injection for the treatment of pediatric patients with the following infection have been established in a comparator-controlled study in pediatric patients ranging in age from 5 through 17 years [ see Clinical Studies ( 14 ) ]: uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible strains only) or Streptococcus pyogenes Pharmacokinetic information generated in pediatric patients with ventriculoperitoneal shunts showed variable cerebrospinal fluid (CSF) linezolid concentrations following single and multiple dosing of linezolid; therapeutic concentrations were not consistently achieved or maintained in the CSF.
Therefore, the use of linezolid for the empiric treatment of pediatric patients with central nervous system infections is not recommended. The pharmacokinetics of linezolid have been evaluated in pediatric patients from birth to 17 years of age. In general, weight-based clearance of linezolid gradually decreases with increasing age of pediatric patients.
However, in preterm (gestational age < 34 weeks) neonates < 7 days of age, linezolid clearance is often lower than in full-term neonates < 7 days of age. Consequently, preterm neonates < 7 days of age may need an alternative linezolid dosing regimen of 10 mg/kg every 12 hours [see Dosage and Administration ( 2.1 ) and Clinical Pharmacology ( 12.3 )]. In limited clinical experience, 5 out of 6 (83%) pediatric patients with infections due to Gram-positive pathogens with minimum inhibitory concentrations (MICs) of 4 mcg/mL treated with Linezolid had clinical cures.
However, pediatric patients exhibit wider variability in linezolid clearance and systemic exposure (AUC) compared with adults. In pediatric patients with a sub-optimal clinical response, particularly those with pathogens with MIC of 4 mcg/mL, lower systemic exposure, site and severity of infection, and the underlying medical condition should be considered when assessing clinical response [ see Clinical Pharmacology ( 12.3 ) and Dosage and Administration ( 2 ) ].
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 2,046 patients treated with Linezolid in Phase 3 comparator-controlled clinical trials, 589 (29%) were 65 years or older and 253 (12%) were 75 years or older. No overall differences in safety or effectiveness were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE In the event of overdosage, supportive care is advised, with maintenance of glomerular filtration. Hemodialysis may facilitate more rapid elimination of linezolid. In a Phase 1 clinical trial, approximately 30% of a dose of linezolid was removed during a 3-hour hemodialysis session beginning 3 hours after the dose of linezolid was administered.
Data are not available for removal of linezolid with peritoneal dialysis or hemoperfusion. Clinical signs of acute toxicity in animals were decreased activity and ataxia in rats and vomiting and tremors in dogs treated with 3,000 mg/kg/day and 2,000 mg/kg/day, respectively.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Linezolid injection is an antibacterial drug [ see Microbiology ( 12.4 ) ].
12.2Pharmacodynamics In a randomized, positive- and placebo-controlled crossover thorough QT study, 40 healthy subjects were administered a single Linezolid injection 600 mg dose via a 1 hour IV infusion, a single Linezolid injection 1,200 mg dose via a 1 hour IV infusion, placebo, and a single oral dose of positive control. At both the 600 mg and 1,200 mg Linezolid injection doses, no significant effect on QTc interval was detected at peak plasma concentration or at any other time.
12.3Pharmacokinetics The mean pharmacokinetic parameters of linezolid in adults after single and multiple oral and intravenous doses are summarized in Table 8 . Plasma concentrations of linezolid at steady-state after oral doses of 600 mg given every 12 hours are shown in Figure 1 . Table 8.
Mean (Standard Deviation) Pharmacokinetic Parameters of Linezolid in Adults * AUC for single dose = AUC 0- ∞ ; for multiple dose = AUC 0- τ † Data dose-normalized from 375 mg ‡ Data dose-normalized from 625 mg, intravenous dose was given as 0.5-hour infusion. C max = Maximum plasma concentration; C min = Minimum plasma concentration; T max = Time to C max ; AUC = Area under concentration-time curve; t 1/2 = Elimination half-life; CL = Systemic clearance Dose of Linezolid C max mcg/mL C min mcg/mL T max hrs AUC* mcg•h/mL t 1/2 hrs CL mL/min 400 mg tablet single dose † every 12 hours 8.10 (1.83) 11.00 (4.37) --- 3.08 (2.25) 1.52 (1.01) 1.12 (0.47) 55.10 (25.00) 73.40 (33.50) 5.20 (1.50) 4.69 (1.70) 146 (67) 110 (49) 600 mg tablet single dose every 12 hours 12.70 (3.96) 21.20 (5.78) --- 6.15 (2.94) 1.28 (0.66) 1.03 (0.62) 91.40 (39.30) 138.00 (42.10) 4.26 (1.65) 5.40 (2.06) 127 (48) 80 (29) 600 mg IV injection ‡ single dose every 12 hours 12.90 (1.60) 15.10 (2.52) --- 3.68 (2.36) 0.50 (0.10) 0.51 (0.03) 80.20 (33.30) 89.70 (31.00) 4.40 (2.40) 4.80 (1.70) 138 (39) 123 (40) 600 mg oral suspension single dose 11.00 (2.76) --- 0.97 (0.88) 80.80 (35.10) 4.60 (1.71) 141 (45) Figure 1.
Plasma Concentrations of Linezolid in Adults at Steady-State Following Oral Dosing Every 12 Hours (Mean ± Standard Deviation, n=16) Figure 1 Absorption Linezolid is extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%. Therefore, linezolid may be given orally or intravenously without dose adjustment.
Linezolid may be administered without regard to the timing of meals. The time to reach the maximum concentration is delayed from 1.5 hours to 2.2 hours and C max is decreased by about 17% when high fat food is given with linezolid. However, the total exposure measured as AUC 0- ∞ is similar under both conditions.
Distribution Animal and human pharmacokinetic studies have demonstrated that linezolid readily distributes to well-perfused tissues. The plasma protein binding of linezolid is approximately 31% and is concentration-independent. The volume of distribution of linezolid at steady-state averaged 40 to 50 liters in healthy adult volunteers.
Linezolid concentrations have been determined in various fluids from a limited number of subjects in Phase 1 volunteer studies following multiple dosing of linezolid. The ratio of linezolid in saliva relative to plasma was 1.2 to 1 and the ratio of linezolid in sweat relative to plasma was 0.55 to 1. Metabolism Linezolid is primarily metabolized by oxidation of the morpholine ring, which results in two inactive ring-opened carboxylic acid metabolites: the aminoethoxyacetic acid metabolite (A), and the hydroxyethyl glycine metabolite (B).
Formation of metabolite A is presumed to be formed via an enzymatic pathway whereas metabolite B is mediated by a non-enzymatic chemical oxidation mechanism in vitro. In vitro studies have demonstrated that linezolid is minimally metabolized and may be mediated by human c…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Linezolid injection is an antibacterial drug [ see Microbiology ( 12.4 ) ].
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.1Injection Linezolid injection is available in a single-dose, ready-to-use flexible plastic container in a foil laminate overwrap. The flexible plastic container and port are latex-free. The flexible plastic container is available as follows: Product No . Unit of Sale Strength Each 713013 NDC 63323-713-13 Package of 10 free flex ® bags 600 mg per 300 mL (2 mg per mL) NDC 63323-713-03 One 300 mL free flex ® Bag
16.4Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light. It is recommended that the infusion bags be kept in the overwrap until ready to use. Protect infusion bags from freezing. The container closure is not made with natural rubber latex. Non-PVC, Non-DEHP, Sterile.
📦 Storage and Handling ▾
16.4Storage and Handling Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light. It is recommended that the infusion bags be kept in the overwrap until ready to use. Protect infusion bags from freezing. The container closure is not made with natural rubber latex. Non-PVC, Non-DEHP, Sterile.
📋 Description ▾
11 DESCRIPTION Linezolid injection contains linezolid, which is a synthetic antibacterial agent of the oxazolidinone class. The chemical name for linezolid is (S)-N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl] methyl]-acetamide. The empirical formula is C 16 H 20 FN 3 O 4 .
Its molecular weight is 337.35, and its chemical structure is represented below: Linezolid injection is supplied as a ready-to-use sterile isotonic solution for intravenous infusion. Each mL contains 2 mg of linezolid. Inactive ingredients are dextrose monohydrate 50.24 mg/mL in an aqueous vehicle for intravenous administration, sodium citrate dihydrate 1.64 mg/mL, and citric acid anhydrous 0.85 mg/mL.
Sodium hydroxide NF and/or hydrochloric acid NF are used to adjust the pH. The sodium (Na+ ) content is 0.38 mg/mL (5 mEq/300 mL bag). Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Peripheral and Optic Neuropathy Advise patients to inform their physician if they experience changes in vision while taking Linezolid injection [ see Warnings and Precautions ( 5.2 ) ]. Serotonin Syndrome Advise patients to inform their physician if taking serotonergic agents, including serotonin re-uptake inhibitors or other antidepressants and opioids [ see Warnings and Precautions ( 5.3 ) ]. Potential Interactions Producing Elevation of Blood Pressure Advise patients to inform their physician if they have a history of hypertension.
Advise patients to avoid large quantities of foods or beverages with high tyramine content while taking Linezolid injection. Foods high in tyramine content include those that may have undergone protein changes by aging, fermentation, pickling, or smoking to improve flavor, such as aged cheeses, fermented or air-dried meats, sauerkraut, soy sauce, tap beers, and red wines. The tyramine content of any protein-rich food may be increased if stored for long periods or improperly refrigerated.
Advise patients to inform their physician if taking medications containing pseudoephedrine HCl or phenylpropanolamine HCl, such as cold remedies and decongestants [ see Warnings and Precautions ( 5.6 ) ]. Lactic Acidosis Advise patients to inform their physician if they experience repeated episodes of nausea or vomiting while receiving Linezolid injection [ see Warnings and Precautions ( 5.7 ) ]. Convulsions Advise patients to inform their physician if they have a history of seizures or convulsions [ see Warnings and Precautions ( 5.8 ) ].
Hypoglycemia Advise patients to inform their physician if they have diabetes mellitus. Hypoglycemic reactions, such as diaphoresis and tremulousness, along with low blood glucose measurements may occur when treated with linezolid. If such reactions occur, patients should contact a physician or other health professional for proper treatment [ see Warnings and Precautions ( 5.9 ) ].
Hyponatremia and/or SIADH Advise patients at risk for hyponatremia to inform their physician if they experience signs and symptoms of hyponatremia and/or SIADH, including confusion, somnolence, generalized weakness, and respiratory distress [ see Warnings and Precautions ( 5.10 ) ]. Antibacterial Resistance Patients should be counseled that antibacterial drugs including Linezolid injection should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold).
When Linezolid injection is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Linezolid or other antibacterial drugs in the future. Diarrhea Diarrhea is a common problem caused by antibacterial drugs, which usually ends when the antibacterial drug is discontinued.
Sometimes after starting treatment with antibacterial drugs, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibacterial drug. If this occurs, patients should contact their physician as soon as possible [ see Warnings and Precautions ( 5.5 ) ]. Infertility Advise male patients that Linezolid may reversibly impair fertility [ see Use in Specific Populations ( 8.3 ) ].
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