Linezolid 600 mg Tablet, Film Coated, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Oxazolidinone Antibacterial class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Linezolid is used to treat certain 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 will not work for colds, flu, and other viral 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.
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 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 M28OL1HH48
Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
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Hydroxypropyl cellulose is a plant-derived thickener and binder made from cellulose. In medicines, it helps hold tablet ingredients together, thickens liquids, and can form a coating on pills or capsules.
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Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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A plant-based thickener made from cellulose that helps control how quickly the medicine dissolves and releases its active ingredient. It also binds ingredients together and improves the tablet's texture and handling during manufacturing.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII B697894SGQ
Polyethylene glycol 400 is a clear, thick liquid made from petroleum-derived polymers. It acts as a solvent and humectant in medicines, helping dissolve active ingredients and retain moisture in the formulation.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII 7CV7WJK4UI
Sodium stearyl fumarate is a synthetic compound made from stearyl alcohol and fumaric acid. It acts as a lubricant and glidant in tablets and capsules, helping ingredients flow smoothly during manufacturing and preventing sticking.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
9 inactive ingredients listed in the exact product block matched to this NDC.
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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 each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $2.58 | $77.49 / 30 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Linezolid 600 mg 00904-6553-04 | Major | 1 tablet | $1.382 | AB | Availability likely | — |
| Linezolid 600 mg 60687-0309-21 | American | 1 tablet | $1.382 | AB | Availability likely | — |
| linezolid 600 mg 62135-0442-20 | Chartwell | 20 tablets | $1.382 | AB | Availability likely | — |
| Linezolid 600 mg 64980-0561-02 | Rising | 20 tablets | $1.382 | AB | Availability likely | — |
| Linezolid 600 mg 59762-1307-01 | Mylan | 20 tablets | $1.495 | — | Discontinued | — |
| Linezolid 600 mg 62332-0183-20 | Alembic | 20 tablets | $2.084 | AB | FDA listed | — |
| Zyvox 600 mg 00009-5138-02 | Pharmacia | 20 tablets | — | — | FDA listed | — |
| Linezolid 600 mg 31722-0749-01 | Camber | 100 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 33342-0352-11 | Macleods | 100 tablets | — | — | FDA listed | — |
| Linezolid 600 mgthis 46708-0183-30 | Alembic | 30 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 63629-8576-01 | Bryant | 20 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 67046-1576-03 | Coupler | 30 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 67877-0419-01 | Ascend | 100 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 70518-4034-00 | REMEDYREPACK | 20 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 71335-2565-01 | Bryant | 20 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 85766-0075-20 | Sportpharm | 20 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 43386-0022-02 | Lupin | 20 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 85766-0231-01 | Sportpharm | 100 tablets | — | AB | FDA listed | — |
| Linezolid 600 mg 50090-8044-00 | A-S | 20 tablets | — | AB | 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?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 46708-0183-20 | 20 TABLET, FILM COATED in 1 BOTTLE (46708-183-20) | 2015-12-22 | Active |
| 46708-0183-30 You're viewing this | 30 TABLET, FILM COATED in 1 BOTTLE (46708-183-30) | 2015-12-22 | Active |
| 46708-0183-31 | 100 TABLET, FILM COATED in 1 BOTTLE (46708-183-31) | 2015-12-22 | Active |
| 46708-0183-91 | 1000 TABLET, FILM COATED in 1 BOTTLE (46708-183-91) | 2015-12-22 | Active |
You're viewing one of 4 pack sizes for this product.
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🧭 About this NDC listing & data coverage
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| 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 | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Linezolid tablets are indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the specific conditions listed below. Linezolid tablets are 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) ]. Linezolid tablets are 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 (1.1); Complicated skin and skin structure infections, including diabetic foot infections, without concomitant osteomyelitis (1.2); Uncomplicated skin and skin structure infections (1.2); Vancomycin-resistant Enterococcus faecium infections (1.3) To reduce the development of drug-resistant bacteria and maintain the effectiveness of linezolid tablets and other antibacterial drugs, linezolid tablets should be used only to treat infections that are proven or strongly suspected to be caused by bacteria.
(1.4)
1.1Pneumonia Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant isolates) or Streptococcus pneumoniae [ see Clinical Studies (14) ]. Community-acquired pneumonia caused by Streptococcus pneumoniae , including cases with concurrent bacteremia, or Staphylococcus aureus (methicillin-susceptible isolates only) [ see Clinical Studies (14) ].
1.2Skin and Skin Structure Infections 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 has not been studied in the treatment of decubitus ulcers [ see Clinical Studies (14) ]. Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes [ see Clinical Studies (14) ].
1.3Vancomycin-resistant Enterococcus faecium Infections Vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia [ see Clinical Studies (14) ].
1.4Usage To reduce the development of drug-resistant bacteria and maintain the effectiveness of linezolid tablets and other antibacterial drugs, linezolid should be used only to treat 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.
The safety and efficacy of linezolid tablets given for longer than 28 days have not been evaluated in controlled clinical trials.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Dosage, Route, and Frequency of Administration Infection Pediatric Patients Adults and Adolescents Duration (days) Nosocomial pneumonia 10 mg/kg oral every 8 hours 600 mg 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 oral every 8 hours 600 mg oral every 12 hours 14 to 28 Uncomplicated skin and skin structure infections less than 5 yrs: 10 mg/kg oral every 8 hours 5 to 11 yrs: 10 mg/kg oral every 12 hours Adults: 400 mg oral every 12 hours Adolescents: 600 mg oral every 12 hours 10 to 14
2.1General Dosage and Administration The recommended dosage for linezolid tablets for the treatment of infections is described in Table 1. Table 1. Dosage Guidelines for Linezolid Tablets Infection* Dosage and Route 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 oral ‡ every 8 hours 600 mg 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 oral ‡ every 8 hours 600 mg oral ‡ every 12 hours 14 to 28 Uncomplicated skin and skin structure infections less than 5 yrs: 10 mg/kg oral ‡ every 8 hours 5 to 11 yrs: 10 mg/kg oral ‡ every 12 hours Adults: 400 mg oral ‡ every 12 hours Adolescents: 600 mg oral ‡ every 12 hours 10 to 14 * 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 linezolid tablets [ see How Supplied/Storage and Handling (16) ].
No dose adjustment is necessary when switching from intravenous to oral administration.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMSAND STRENGTHS Linezolid tablets 600 mg are available as “White to off white, oval shaped, film-coated tablets debossed with “L340” on one side and plain on the other side. · Tablet: 600 mg linezolid
⛔ 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 tablets are 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. 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: Patients taking serotonergic antidepressants should receive linezolid 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) · Clostridium 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)
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. 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 receiving concomitant drugs that produce bone marrow suppression, or those with a chronic infection who have received previous or concomitant antibiotic therapy.
Discontinuation of therapy with linezolid should be considered in patients who develop or have worsening myelosuppression .
5.2Peripheral and Optic Neuropathy Peripheral and optic neuropathies have been reported in patients treated with linezolid, 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 and serotonergic agents, including antidepressants such as selective serotonin reuptake inhibitors (SSRIs), have been reported. Unless clinically appropriate and patients are carefully observed for signs and/or symptoms of serotonin syndrome or neuroleptic malignant syndrome-like (NMS-like) reactions, linezolid should not be administered to patients with carcinoid syndrome and/or patients taking any of the following medications: serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), meperidine, bupropion, or buspirone [ see Drug Interactions (7) and Clinical Pharmacology (12.3) ].
In some cases, a patient already receiving a serotonergic antidepressant or buspirone may require urgent treatment with linezolid. If alternatives to linezolid are not available and the potential benefits…
🤒 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 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 was evaluated in 2046 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 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=1498) All Other Comparators* (n=1464) 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 1.5 4.3
2.3Dizziness 2.6 3 1.8
1.5Rash 1.1 1.1 2.3
2.6Anemia 0.4 0 2.1
1.4Taste alteration 1.8 2 1
0.3Vaginal moniliasis 1.8 1.3 1.1
0.5Oral moniliasis 0.5 0 1.7 1 Abnormal 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 * 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. Of 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 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% (13/215) in the linezolid arm and 3% (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-causality, treatment-emergent adverse reactions reported in more than 1% of pediatric pat…
🔄 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 Teratogenic Effects – Pregnancy Category C Linezolid was not teratogenic in mice, rats, or rabbits at exposure levels 6.5-fold (in mice), equivalent to (in rats), or 0.06-fold (in rabbits) the expected human exposure level, based on AUCs. However, embryo and fetal toxicities were seen ( see Non-teratogenic Effects ). There are no adequate and well-controlled studies in pregnant women.
Linezolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Non-teratogenic Effects In mice, embryo and fetal toxicities were seen only at doses that caused maternal toxicity (clinical signs and reduced body weight gain). A dose of 450 mg/kg/day (6.5-fold the estimated human exposure level 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.
In rats, mild fetal toxicity was observed at 15 and 50 mg/kg/day (exposure levels 0.22-fold 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. Slight 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 a dose of 15 mg/kg/day (0.06-fold the estimated human exposure based on AUCs). 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, 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.
8.3Nursing Mothers Linezolid and its metabolites are excreted in the milk of lactating rats. Concentrations in milk were similar to those in maternal plasma. It is not known whether linezolid is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when linezolid is administered to a nursing woman.
8.4Pediatric Use The safety and effectiveness of linezolid 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 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 evalu…
🤰 Pregnancy ▾
8.1Pregnancy Teratogenic Effects – Pregnancy Category C Linezolid was not teratogenic in mice, rats, or rabbits at exposure levels 6.5-fold (in mice), equivalent to (in rats), or 0.06-fold (in rabbits) the expected human exposure level, based on AUCs. However, embryo and fetal toxicities were seen ( see Non-teratogenic Effects ). There are no adequate and well-controlled studies in pregnant women.
Linezolid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Non-teratogenic Effects In mice, embryo and fetal toxicities were seen only at doses that caused maternal toxicity (clinical signs and reduced body weight gain). A dose of 450 mg/kg/day (6.5-fold the estimated human exposure level 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.
In rats, mild fetal toxicity was observed at 15 and 50 mg/kg/day (exposure levels 0.22-fold 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. Slight 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 a dose of 15 mg/kg/day (0.06-fold the estimated human exposure based on AUCs). 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, 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 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 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 2046 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 3000 mg/kg/day and 2000 mg/kg/day, respectively.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Linezolid 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 600 mg dose via a 1 hour IV infusion, a single linezolid 1200 mg dose via a 1 hour IV infusion, placebo, and a single oral dose of positive control. At both the 600 mg and 1200 mg linezolid 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 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 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 † 8.1 (1.83) -- 1.52 (1.01) 55.1 (25) 5.2 (1.5) 146 (67) every 12 hours 11 (4.37) 3.08 (2.25) 1.12 (0.47) 73.4 (33.5) 4.69 (1.7) 110 (49) 600 mg tablet single dose 12.7 (3.96) -- 1.28 (0.66) 91.4 (39.3) 4.26 (1.65) 127 (48) every 12 hours 21.2 (5.78) 6.15 (2.94) 1.03 (0.62) 138 (42.1) 5.4 (2.06) 80 (29) * AUC for single dose = AUC 0-∞; for multiple dose = AUC 0-τ; † Data dose-normalized from 375 mg 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 F igure 1.
Plasma Concentrations of Linezolid in Adults at Steady-State Following Oral Dosing Every 12 Hours (Mean ± Standard Deviation, n=16) 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 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 cytochrome P450. However, the metabolic pathway of linezolid is not fully understood.
Excretion Nonrenal clearance accounts for approximately 65% of the total clearance of linezolid. Under steady-state conditions, approximately 30% of the dose appears in the urine as linezolid, 40% as metabolite B, and 10% as metabolite A. The mean renal clearance of linezolid is 40 mL/min which suggests net tubular reabsorption.
Virtually no linezolid appears in the feces, while approximately…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Linezolid is an antibacterial drug [see Microbiology ( 12.4) ].
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING
16.2Tablets Linezolid tablets 600 mg are available as “White to off white, oval shaped, film-coated tablets debossed with “L340” on one side and plain on the other side. 20 tablets in HDPE bottle NDC 46708-183-20 30 tablets in HDPE bottle NDC 46708-183-30 100 tablets in HDPE bottle NDC 46708-183-31 1000 tablets in HDPE bottle NDC 46708-183-91
16.4Storage and Handling Store at 25ºC (77ºF); excursions permitted to 15 to 30°C (59 to 86°F) [see USP Controlled Room Temperature]. Protect from light. Keep bottles tightly closed to protect from moisture.
📋 Description ▾
11 DESCRIPTION Linezolid tablets contain linezolid, which is a synthetic antibacterial agent of the oxazolidinone class. The chemical name for linezolid is (S)-N-[[3-[3-Fluoro-4-(4morpholinyl)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 tablets for oral administration contain 600 mg linezolid as film-coated compressed tablets. Inactive ingredients are microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, colloidal silicon dioxide, sodium stearyl fumarate, croscarmellose sodium, hypromellose, titanium dioxide and polyethylene glycol. The sodium (Na + ) content is 2.92 mg per 600-mg tablet (0.1 mEq per tablet).
Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Patients should be counseled that antibacterial drugs including linezolid should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When linezolid 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. Patients should be advised that: • Linezolid may be taken with or without food. • They should inform their physician if they have a history of hypertension. • Large quantities of foods or beverages with high tyramine content should be avoided while taking linezolid.
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. •They should inform their physician if taking medications containing pseudoephedrine HCl or phenylpropanolamine HCl, such as cold remedies and decongestants. •They should inform their physician if taking serotonin re-uptake inhibitors or other antidepressants. •They should inform their physician if they experience changes in vision. •They should inform their physician if they have a history of seizures. •Diarrhea is a common problem caused by antibiotics, which usually ends when the antibiotic is discontinued.
Sometimes after starting treatment with antibiotics, 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 antibiotic. If this occurs, patients should contact their physician as soon as possible. •Inform patient, particularly those with diabetes mellitus that 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.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. Manufactured by: Alembic Pharmaceuticals Limited (Formulation Division), Village Panelav, P.
O. Tajpura, Near Baska, Taluka-Halol, Panchmahal, Gujarat, India. Revised: 07/2017