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DrugsLevel 4 LocalisationS4INF · INJ · TAB · FCT · GRAEML

Linezolid

OxazolidinoneAntibacterial

Indications

These indications are based on manufacturer information for both originator and generic products. For product specific registered indications, please refer to product specific manufacturer information

Registered South African indications:

  • Vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteraemia
  • Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), or Streptococcus pneumoniae (including multi-drug resistant S. pneumoniae (MDRSP) strains)
  • Complicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes, or Streptococcus agalactiae
  • Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin -susceptible and -resistant strains) or Streptococcus pyogenes
  • Community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant S. pneumoniae (MDRSP) strains), including cases with concurrent bacteraemia, or Staphylococcus aureus (methicillin-susceptible and -resistant strains)

Linezolid has not been studied in the treatment of decubitus ulcers

Contraindications (ZA)

Registered South African contraindications

  • Hypersensitivity to the active ingredient or to any of its excipients
  • Pregnancy
  • Breastfeeding
  • Unless there are facilities available for close observation and monitoring of blood pressure, linezolid should not be administered to patients with the following:
    - Uncontrolled hypertension
    - Phaeochromocytoma
    - Carcinoid
    - Thyrotoxicosis (inj)
    - Hyperthyroidism (fct, tab, sus)
    - Bipolar depression
    - Schizoaffective disorder
    - Acute confusional states
    - Coadministration with serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), directly and indirectly acting sympathomimetic agents (including the adrenergic bronchodilators, pseudoephedrine and phenylpropanolamine), vasopressive agents (e.g. epinephrine, norepinephrine), dopaminergic agents (e.g. dopamine, dobutamine), pethidine or buspirone
  • Coadministration with any medicinal product which inhibits monoamine oxidases A or B (e.g. phenelzine, isocarboxazid, selegiline, moclobemide) or within 14 days of their use

Warnings & precautions

  • Severe renal impairment (CrCl<30ml/min)
    - Haemodialysis
  • Hepatic impairment (particularly in severe hepatic impairment)
  • Elderly
  • Porphyria
  • Males of childbearing potential
  • Pre-existing anaemia, granulocytopaenia or thrombocytopaenia
  • Prolonged use
  • Complicated skin and soft tissue infections with known or possible co-infection with Gram-negative organisms
  • A history of seizures or risk factors for seizures
  • Diabetic foot lesions
  • Decubitus or ischaemic lesions
  • Severe burns
  • Gangrene
  • Diabetes mellitus (inj)
  • Consuming large amounts of tyramine-rich foods
  • Patients currently taking or who have recently taken antimycobacterial medications for the treatment of tuberculosis
  • Coadministration with agents that may decrease haemoglobin levels, depress blood counts or adversely affect platelet count or function
  • Phenylketonuria (sus)
  • Sodium-controlled diet (sus, inj)
  • Conditions associated with glucose intolerance (inj)
  • Sensitivity to ethanol (alcohol) (sus)
  • Fructose intolerance (sus)
  • Glucose-galactose malabsorption  (sus)
  • Sucrase-isomaltase insufficiency (sus)
  • May impair ability to drive and operate machinery

Adult dosage

Forms avail. in SA and covered in this monograph: sus, tab, inj

Dosages below include:

  • South African Standard Treatment Guideline indications and dosages
  • South African Management of Rifampicin-Resistant Tuberculosis: A Clinical Reference Guide recommendations
  • South African registered indications and dosages
  • Indications and dosages registered in other jurisdictions

Infections caused by: Some Gram-positive aerobic organisms, such as Enterococcus faecalis (VRE), Enterococcus faecium* (S) and (VRE), Staphylococcus aureus* (MRSA), Coagulase negative staphylococci (R), Staphylococcus epidermidis, Streptococcus agalactiae*, Streptococcus pneumoniae*, Streptococcus pyogenes*, Group C streptococci, Group G streptococci; Some Gram-positive anaerobic organisms, such as Clostridium perfringens, Peptostreptococcus anaerobius, Peptostreptococcus species 

Specific dose for individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Standard Treatment Guideline indications and dosages

Hepatitis in those on ART and anti-tuberculosis therapy (Additional agents required)

  • Oral (tab, sus): 600mg, dly; Treatment duration: Stop at day 8 of rechallenge
    (STG, Adult 2023)

- If drug rechallenge is unsuccessful, rifampicin not tolerated (intensive phase)

  • Oral (tab, sus): 600mg, dly; Treatment duration: 2 months
    (STG, Adult 2023)

South African Management of Rifampicin-Resistant Tuberculosis: A Clinical Reference Guide recommendations

Rifampicin-resistant tuberculosis (RR-TB)
- Shorter regimen with Hb≥8g/dl at diagnosis or following transfusion 

  • Oral (tab, sus): Intensive phase: 10mg/kg, dly; Treatment duration: 2 months
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019) 

Shorter regimen should be continued in the following after review of line probe assay (LPA) and phenotypic drug susceptibility (DST) results whilst on shorter course:
- Isoniazid (INH) susceptible on LPA and phenotypic (300mg, dly)
- Only one INH mutation (not both) and both fluoroquinolone (FLQ) and injectable susceptible
- LPA inconclusive (send repeat specimen and continue short course). Consider switch to long course if no clinical improvement


- Basic longer regimen

  • ≥30kg: Oral (tab, sus): Intensive phase: 600mg, dly; Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months (only used in continuation phase if one of the standard 3 agents are not tolerated)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019) 

- Fluoroquinolone resistant RR-TB longer regimen

  • ≥30kg: Oral (tab, sus): Intensive phase: 600mg, dly; Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months (only used in continuation phase if selected as one of the 3-4 agents required, depending on tolerance)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019)

- Central nervous system RR-TB longer regimen

  • ≥30kg: Oral (tab, sus): Intensive phase: 600mg, dly; Treatment duration: 12 months; Continuation phase: Treatment duration: 6 months (if selected as 5th agent, depending on isoniazid (INH) mutation)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019)

Longer regimens: Treatment duration is 18 months but could be extended to 20 months per clinician discretion


Longer regimen initiation is applicable to the following upon Xpert or LPA reported as rifampicin resistant: 
- History of previous treatment with second-line drugs >1/12
- Complicated EPTB (meningitis, osteoarticular, pericarditis,
abdominal)
- Contact with XDR or pre-XDR
- Younger than 6 years
- Extensive disease on CXR


Long course is applicable to the following after review LPA and phenotypic DST results whilst on shorter course:
- Both INH (inhA and KatG) mutations
- Resistance to fluoroquinolone, injectable, bedaquiniline, linezolid or clofazimine
- LPA inconclusive (if no clinical improvement is realised in shorter course)


South African registered indications and dosages

Community-acquired pneumonia
- Including concurrent bacteraemia
Nosocomial pneumonia
- Including concurrent bacteraemia

  • Oral (tab, sus): 600mg, 12hrly; Treatment duration: 10-14 days
  • IV: 600mg, 12hrly, as an infusion over 30-120min; Treatment duration: 10-14 days

Skin and soft tissue infections
- Including concurrent bacteraemia

  • Oral (tab, sus): 400-600mg, 12hrly; Treatment duration: 10-14 days
  • IV: 600mg, 12hrly, as an infusion over 30-120min; Treatment duration: 10-14 days

Choice of regimen should depend on clinical severity


Enterococcal infections, including vancomycin-resistant infections
- Including concurrent bacteraemia

  • Oral (tab, sus): 600mg, 12hrly; Treatment duration: 14-28 days
  • IV: 600mg, 12hrly, as an infusion over 30-120min; Treatment duration: 14-28 days

Linezolid tablets, oral suspension or solution for infusion may be used as initial therapy. Patients who commence treatment on the parenteral formulation may be switched to either oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as linezolid has an oral bioavailability of approximately 100%


Indications and dosages registered in other jurisdictions

Nosocomial pneumonia
Community-acquired pneumonia

Complicated skin and soft tissue infections

  • Oral (tab, sus): 600mg, 12hrly; Treatment duration: 10-14 days
  • IV: 600mg, 12hrly, as an infusion over 30-120min; Treatment duration: 10-14 days

Linezolid solution for infusion, film-coated tablets or oral suspension may be used as initial therapy. Patients who commence treatment on the parenteral formulation may be switched to either oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as linezolid has an oral bioavailability of approximately 100%


The duration of treatment is dependent on the pathogen, the site of infection and its severity, and on the patient's clinical response

The recommendations for duration of therapy reflect those used in the clinical trials. Shorter treatment regimens may be suitable for some types of infection but have not been evaluated in clinical trials

The maximum treatment duration is 28 days. The safety and effectiveness of linezolid when administered for periods longer than 28 days have not been established


No increase in the recommended dosage or duration of treatment is required for infections associated with concurrent bacteraemia

Paediatric dosage

Paed. forms avail. in SA and covered in this monograph: sus, tab, inj

Paed. dosages below include:

  • South African Management of Rifampicin-Resistant Tuberculosis: A Clinical Reference Guide recommendations
  • South African registered indications and dosages

Infections caused by: Some Gram-positive aerobic organisms, such as Enterococcus faecalis (VRE), Enterococcus faecium* (S) and (VRE), Staphylococcus aureus* (MRSA), Coagulase negative staphylococci (R), Staphylococcus epidermidis, Streptococcus agalactiae*, Streptococcus pneumoniae*, Streptococcus pyogenes*, Group C streptococci, Group G streptococci; Some Gram-positive anaerobic organisms, such as Clostridium perfringens, Peptostreptococcus anaerobius, Peptostreptococcus species 

Specific dose for individual indications

Please note that the dosages below should be used in combination with regional guidelines, taking into account local antibiotic sensitivities

South African Management of Rifampicin-Resistant Tuberculosis: A Clinical Reference Guide recommendations

Rifampicin-resistant tuberculosis (RR-TB)
- Shorter regimen with Hb≥8g/dl at diagnosis or following transfusion 

Younger than 6 years

  • Excluded for use

6 years and older

  • <16kg: Oral (tab, sus): Intensive phase: 15mg/kg, dly; Treatment duration: 2 months
  • ≥16kg: Oral (tab, sus): Intensive phase: 10mg/kg, dly; Treatment duration: 2 months
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019) 

Shorter regimen should be continued in the following after review of line probe assay (LPA) and phenotypic drug susceptibility (DST) results whilst on shorter course:
- Isoniazid (INH) susceptible on LPA and phenotypic
- Only one INH mutation (not both) and both fluoroquinolone (FLQ) and injectable susceptible
- LPA inconclusive (send repeat specimen and continue short course). Consider switch to long course if no clinical improvement


- Basic longer regimen

Younger than 6 years

  • <16kg: Oral (sus): 15mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months
  • ≥16kg: Oral (sus): 10-12mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months

6 years and older

  • ≥30kg: Oral (tab, sus): 10mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months (only used in continuation phase if one of the standard 3 agents are not tolerated)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019) 

- Fluoroquinolone resistant RR-TB longer regimen

Younger than 6 years

  • <16kg: Oral (sus): 15mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months
  • ≥16kg: Oral (sus): 10-12mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months

6 years and older

  • ≥30kg: Oral (tab, sus): 10mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months (only used in continuation phase if selected as one of the 3-4 agents required)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019)

- Central nervous system RR-TB longer regimen

Younger than 6 years

  • <16kg: Oral (sus): 15mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months
  • ≥16kg: Oral (sus): 10-12mg/kg, dly; Intensive phase: Treatment duration: 6 months; Continuation phase: Treatment duration: 12 months

6 years and older

  • ≥30kg: Oral (tab, sus): 10mg/kg, dly; Intensive phase: Treatment duration: 12 months; Continuation phase: Treatment duration: 6 months (if selected as 5th agent, depending on isoniazid (INH) mutation)
    (Management of Rifampicin Resistant Tuberculosis, A Clinical Reference Guide 2019)

<3kg: Consult with experienced clinician


Longer regimen initiation is applicable to the following upon Xpert or LPA reported as rifampicin resistant: 
- History of previous treatment with second-line drugs >1/12
- Complicated EPTB (meningitis, osteoarticular, pericarditis, abdominal)
- Contact with XDR or pre-XDR
- Younger than 6 years
- Extensive disease on CXR


Long course is applicable to the following after review of LPA and phenotypic DST results whilst on shorter course:
- Both INH (inhA and KatG) mutations
- Resistance to fluoroquinolone, injectable, bedaquiniline, linezolid or clofazimine
- LPA inconclusive (if no clinical improvement is realised in shorter course)


Longer regimens: The duration of therapy in children under the age of 6 years should depend upon the site and severity of disease: children with non-severe disease can be treated for 9-15 months while children with severe disease will require 12-18 months of therapy depending on their clinical progress. Treatment duration for children 6 years and older is 18 months but could be extended to 20 months per clinician discretion


South African registered indications and dosages

Community-acquired pneumonia
- Including concurrent bacteraemia
Nosocomial pneumonia
- Including concurrent bacteraemia
Skin and soft tissue infections
- Including concurrent bacteraemia

  • Oral (tab, sus): 10mg/kg, 8hrly; Treatment duration: 10-14 days
  • IV: 10mg/kg, 8hrly, as an infusion over 30-120min; Treatment duration: 10-14 days

Enterococcal infections, including vancomycin-resistant infections

  • Oral (tab, sus): 10mg/kg, 8hrly; Treatment duration: 14-28 days
  • IV: 10mg/kg, 8hrly, as an infusion over 30-120min; Treatment duration: 14-28 days

Pre-term neonates <7 days of age (gestational age <34 weeks) have lower systemic linezolid clearance values and larger AUC values than many full-term neonates and older infants. By day 7 of age, linezolid clearance and AUC values are similar to those of full-term neonates and older infants


According to international manufacturer recommendations, the safety and efficacy of linezolid in children <18 years old has not been established. No recommendation on a posology can be made

Special populations

Pregnancy

  • Contraindicated
  • Safety has not been demonstrated in pregnancy

Breastfeeding

  • Contraindicated
  • Animal data suggest that linezolid and its metabolites may pass into breast milk and, accordingly, breastfeeding should be discontinued prior to and throughout administration

Fertility

  • Linezolid reversibly decreased fertility and induced abnormal sperm morphology in adult male rats at exposure levels approximately equal to those expected in humans; possible effects of linezolid on the human male reproductive system are not known 

Renal Impairment

  • Mild to moderate (CrCl ≥30ml/min): No dose adjustment recommended
  • Severe (CrCl <30ml/min) and haemodialysis: Caution; no dose adjustment recommended
    Due to the unknown clinical significance of higher exposure (up to 10-fold) to the two primary metabolites of linezolid in patients with severe renal insufficiency, linezolid should be used with special caution in these patients and only when the anticipated benefit is considered to outweigh the theoretical risk
    As approximately 30% of a linezolid dose is removed during 3 hours of haemodialysis, linezolid should be given after dialysis in patients receiving such treatment. The primary metabolites of linezolid are removed to some extent by haemodialysis, but the concentrations of these metabolites are still considerably higher following dialysis than those observed in patients with normal renal function or mild to moderate renal insufficiency
    Therefore, linezolid should be used with special caution in patients with severe renal insufficiency who are undergoing dialysis and only when the anticipated benefit is considered to outweigh the theoretical risk
    To date, there is no experience of linezolid administration to patients undergoing continuous ambulatory peritoneal dialysis (CAPD) or alternative treatments for renal failure (other than haemodialysis)

Hepatic Impairment

  • Caution; no dose adjustment recommended
    There are limited clinical data and it is recommended that linezolid should be used in patients with hepatic impairment only when the anticipated benefit is considered to outweigh the theoretical risk

Elderly

Porphyria Information

  • Probably not porphyrinogenic (PNP)
    Nausea, vomiting and diarrhoea are reported very common side effects of linezolid that may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake

Drugs in Sport

  • Permitted - No warnings

Adverse reactions

Central Nervous System Disorders 

  • Insomnia
  • Headache
  • Dizziness
  • Convulsions
  • Hypoaesthesia
  • Paraesthesia
  • Serotonin syndrome
    - Confusion
    - Delirium
    - Restlessness
    - Tremors
    - Blushing
    - Diaphoresis
    - Hyperpyrexia
    - Cognitive dysfunction
    - Incoordination
  • Peripheral neuropathy
  • Fatigue

Cardiovascular Disorders 

  • Arrhythmia
    - Tachycardia
  • Hypertension
  • Transient ischaemic attacks
  • Phlebitis
  • Thrombophlebitis

Gastrointestinal Disorders 

  • Antibiotic-associated colitis
    - Pseudomembranous colitis
  • Oral candidiasis
  • Nausea and vomiting
  • Diarrhoea
  • Loose stools
  • Localised or general abdominal pain
  • Constipation
  • Pancreatitis
  • Gastritis
  • Dry mouth
  • Dyspepsia
  • Glossitis
  • Stomatitis
  • Superficial tooth discolouration
  • Tongue discolouration or disorder

Hepatobiliary Disorders 

  • Abnormal hepatic function tests
    - Increased aspartate aminotransferase
    - Increased alanine aminotransferase
    - Increased alkaline phosphatase
  • Increased total bilirubin

Genitourinary Disorders 

  • Increased blood urea nitrogen
  • Renal failure
  • Increased creatinine
  • Polyuria
  • Vulvovaginal disorder
  • Vaginal candidiasis
  • Vaginitis

Endocrine and Metabolic Disorders 

  • Hyponatraemia
  • Lactic acidosis
    - Recurrent nausea or vomiting
    - Abdominal pain
    - Low bicarbonate level
    - Hyperventilation
  • Increased thirst
  • Increased or decreased sodium
  • Increased or decreased calcium
  • Increased or decreased non-fasting glucose
  • Increased or decreased chloride
  • Increased lactate dehydrogenase
  • Increased creatine kinase
  • Increased lipase
  • Increased amylase
  • Decreased total protein
  • Decreased albumin
  • Increased or decreased potassium
  • Increased or decreased bicarbonate
  • Increased or decreased chloride

Skin and Subcutaneous Tissue Disorders 

  • Pruritus
  • Rash
  • Urticaria
  • Dermatitis
  • Diaphoresis
  • Bullous disorders
    - Stevens-Johnson syndrome
    - Toxic epidermal necrolysis
  • Angioedema
  • Alopecia
  • injection site pain (inj)

Immune, Blood and Lymphatic System Disorders 

  • Candidiasis
  • Fungal infections
  • Anaemia
    - Sideroblastic anaemia
  • Leucopenia
  • Neutropenia
  • Thrombocytopenia
  • Eosinophilia
  • Pancytopenia
  • Increased eosinophils
  • Decreased haemoglobin
  • Decreased haematocrit  
  • Decreased red blood cell count
  • Increased or decreased platelet count
  • Increased or decreased white blood cell counts
  • Increased reticulocyte count
  • Increased or decreased neutrophils
  • Myelosuppression
  • Anaphylaxis
  • Fever
  • Chills

Sensory Disorders 

  • Blurred vision
  • Taste perversion
    - Metallic taste
  • Visual field defects
  • Changes in visual field defect
  • Optic neuropathy
  • Optic neuritis
  • Loss of vision
  • Changes in visual acuity
  • Changes in colour vision
  • Tinnitus

Others

  • Localised pain

Interactions

  • Monoamine oxidase inhibitors
  • Phenelzine
  • Isocarboxazid
  • Selegiline
  • Moclobemide
  • Adrenergic bronchodilators
  • Pseudoephedrine
  • Phenylpropanolamine hydrochloride
  • Vasopressive agents
  • Dopaminergic agents
  • Dopamine
  • Dobutamine
  • Pethidine
  • Buspirone
  • Dextromethorphan 
  • Antidepressants
  • Tricyclic antidepressants
  • Serotonergic agents
  • Selective serotonin reuptake inhibitors
  • Serotonin 5-HT1 receptor agonists (triptans)
  • Sympathomimetic agents
  • Agents that decrease haemoglobin levels
  • Agents that depress blood counts
  • Agents that affect platelet count or function
  • Rifampicin
  • Warfarin

Other interactions

  • Food and beverages with a high tyramine content (in excessive amounts)
    - Mature cheese
    - Yeast extracts
    - Undistilled alcoholic beverages
    - Fermented soya bean products, such as soy sauce

Monitoring

None routine. Specific cases may require

  • Full blood count
  • Peripheral sensory and visual function
  • Serum bicarbonate
  • Lactic acid
  • Blood pressure
  • Visual function

Additional observations

  • Haematopoietic and neuropathic adverse events

Prescribing points

Injection 600mg/300ml, Tablet 600mg - EML (Tertiary)


Paediatric administration instructions

  • Child-friendly formulations of the medications should be used whenever possible. If these are not available, then extemporaneous preparations will be needed
  • The table below is from the Management of Rifampicin-Resistant Tuberculosis: A Clinical Reference Guide (Department of Health: South Africa, November 2019)

Weight 20mg/ml suspension 600mg tablet
<3kg Consult with an experienced clinician for children <4kg
3-3.9kg
4-4.9kg 70mg (3.5ml) 60mg (Crush 1 tab and mix in 10ml water. Administer 1ml. Discard rest)
5-6.9kg 80mg (4ml) 90mg (Crush 1 tab and mix in 10ml water. Administer 1.5ml. Discard rest)
7-9.9kg 120mg (6ml) 120mg
(Crush 1 tab and mix in 10ml water. Administer 2ml. Discard rest)
10-15.9kg 160-200mg (8-10ml) 150-180mg
(Crush 1 tab and mix in 10ml water. Administer 2.5-3.5ml. Discard rest)
16-23.9kg 160-220mg (8-11ml) 180-210 mg (Crush 1 tab and mix in 10ml
water. Administer 3-3.5ml. Discard rest)
24-30kg No information available 300mg
(Break 1 tab in half and swallow, or crush and mix in small amount of water)
>30kg Refer to adult dosing

Administration directions

  • IV infusion: Solution supplied as ready-to-use infusion bags, to be administered over 30-120mins
  • Linezolid solution for infusion is compatible with the following solutions:
    - Glucose 5% (50mg/ml) solution for infusion
    - Sodium chloride 0.9% (9mg/ml) solution for infusion
    - Ringer-lactate solution for injection (Hartmann's solution for injection)
  • Additives should not be introduced into this solution. If linezolid is to be given concomitantly with other drugs, each drug should be given separately in accordance with its own directions for use. Similarly, if the same intravenous line is to be used for sequential infusion of several drugs, the line should be flushed prior to and following linezolid administration with a compatible infusion solution
  • Reconstitution of granules: Loosen the granules and reconstitute using 123ml water in two approximately equal aliquots to produce 150ml oral suspension. The suspension should be vigorously shaken between each addition of water

Mechanism of action

Linezolid is a synthetic, antibacterial agent that belongs to a new class of antimicrobials, the oxazolidinones. Linezolid selectively inhibits bacterial protein synthesis via a unique mechanism of action. Specifically, it binds to a site on the bacterial ribosome (23S of the 50S subunit) and prevents the formation of a functional 70S initiation complex which is an essential component of the translation process.

Spectrum of activity: Some Gram-positive aerobic organisms, such as Enterococcus faecalis (VRE), Enterococcus faecium* (S) and (VRE), Staphylococcus aureus* (MRSA), Coagulase negative staphylococci (R), Staphylococcus epidermidis (R), Streptococcus agalactiae*, Streptococcus pneumoniae*, Streptococcus pyogenes*, Group C streptococci, Group G streptococci; Some Gram-positive anaerobic organisms, such as Clostridium perfringens, Peptostreptococcus anaerobius,Peptostreptococcus species 

*Clinical efficacy has been demonstrated for susceptible isolates in approved clinical indications

 

Dosage forms

  • Infusion
  • Injection
  • Tablet
  • Film-coated tablet
  • Granules

Formulation

Tablet 600mg

  • Aklid fct (Akacia)
  • Linezolid Hetero (Hetero)
  • Linezolid Teva fct (Teva Pharma) 
  • Linezolid Specpharm (Specpharm)
  • Linokem (Alkem Laboratories)
  • Voxwin (Zentiva)
  • Zenilid 600mg (Glenmark Pharmaceuticals)
  • Zenoxpar 600mg (Accord Healthcare)
  • Zyvoxid (Pfizer) originator

Infusion (per 100ml) 200mg

  • Zyvoxid (Pfizer) originator

Injection (per 300ml) 600mg

  • Linezolid 600mg/300ml Aspen (Pharmacare Limited)
  • Linezolid Fresenius (Fresenius Kabi)
  • Linzai (Pharma Dynamics)
  • Zenilid IV 600mg/300ml (Glenmark Pharmaceuticals)
  • Zyvoxid (Pfizer) originator
  • Voxwin IV (Sanofi Aventis)

Granules (per ml) 20mg

  • Zyvoxid (Pfizer) originator

References

1. SAMF_12th Edition_Page 305 2. SmPC: Linezolid 600 mg film-coated tablets, Pfizer Limited: Last updated on eMC: 26 Feb 2018; Downloaded online; 26 Nov 2018 https://www.medicines.org.uk/emc/medicine/31358 3. SmPC: Linezolid 2mg/ml solution for infusion, Pfizer Limited: Last updated on eMC: 26 Feb 2018; Downloaded online; 26 Nov 2018 https://www.medicines.org.uk/emc/medicine/31359 4. PI: Zyvoxid 400 mg & 600 mg Tablets; 200 mg/100 ml & 600 mg/300 ml Solution for Infusion; 20 mg/ml Granules for Suspension, Pfizer. Date of publication: 02 March 2012 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 5.https://webedition.sanfordguide.com/sanford-guide-online/drug-information/antibacterial-agents/oxazolidinones/linezolid-zyvox 6. U2D: Linezolid: Drug information; Uptodate; Downloaded online: 14 May 2021 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 7. NAPOS The Drug Database for Acute Porphyria: Linezolid; Accessed online; 26 Nov 2018 [http://www.drugs-porphyria.org/languages/UnitedKingdom/s3.php?l=gbr&atc_code=J01XX08] 8. South African Institute for Drug-Free Sport: Zyvoxid; Accessed online; 2 Nov 2018 [http://www.drugfreesport.org.za/online-medication-check/ 9. SmPC: Zyvox 600 mg Film-Coated Tablets, Pfizer Limited: Last updated 17 Sept 2018; updated 15 April 2020, [https://www.medicines.org.uk/emc/product/1688/smpc/print] 10. Dr Irhuma. Updates for linezolid [https://trello.com/c/rMS5bjHg/321-list-of-hot-monographs-1]. Dated 19 November 2019. Updated 15 April 2020. 11. SmPC: Zyvox 100 mg/5 ml Granules for Oral Suspension, Pfizer Limited: Last updated 17 Jan 2020; Downloaded online 6 May 2021 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 12. SmPC: Linezolid 2mg/ml Solution for Infusion, Panpharma UK Ltd: Last updated 19 Feb 2020; Downloaded online 6 May 2021 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 13. SmPC: Linezolid 600 mg Film-coated Tablets, Sandoz: Last updated 29 Sep 2020; Downloaded online 6 May 2021 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 14. Sanford Guide: Linezolid; Downloaded online 6 May 2021 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 15. Department of Health: South Africa. Management of Rifampicin-Resistant Tuberculosis, November 2019 [https://drive.google.com/drive/folders/1yshRZ-L9J8oky2JklnBxP4Z8odPZNsUf] 16. Standard Treatment Guidelines and Essential Medicines List for South Africa Hospital Level, Aduls, 2023 Edition; Chapter 10: HIV AND AIDS; South African Department of Health [https://drive.google.com/drive/folders/1fcCkwtBdIRbCbfVZysrZIxSHNNee8iVY] 17. PI - LINEZOLID 600 mg/300 mL FRESENIUS solution for infusion, Fresenius Kabi South Africa (Pty) Ltd - DATE OF REVISION OF THE TEXT 23 July 2024 Downloaded online 16 October 2025 [https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2024/08/pi_linezolid-600mg-300ml-fresenius_July2024.pdf] 18. PI - ZYVOXID® all dosage forms, Pfizer Laboratories (Pty) Ltd - DATE OF REVISION OF THE TEXT 24 February 2023 Downloaded online 16 Oct 2025 [https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2024/11/pi-approved-24Feb2023.pdf] 19. PI - LIDONIT film coated tablets, Pharma Dynamics (Pty) Ltd - DATE OF REVISION OF THE TEXT 05 January 2023 Downloaded online 16 Oct 2025 [https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2023/02/pi-noref-post-reg-clin-approved05012023.pdf]

Brands & products

25 products · stale NAPPI snapshot · refreshed 5/29/2026 · 158 days old

infusionGeneric· 10 products

from R1.17/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Elturin Iv600 mg/300ml300S4R3511.65R1.17R406.653009089001
Linezolid fresenius solution for infusio600 mg/300ml300S4R3560.30R1.19R409.30722770002
Linobact Iv600 mg/300ml300S4R4039.68R1.35R435.363008467001
Zenilid Iv 600 Mg/300 Ml600 mg/300ml300S4R469.41R1.56R154.343004431001
Linezolid fresenius solution for infusio600 mg/300ml300S4R469.46R1.56R154.36722770001
Linezolid 600Mg/300Ml Aspen600 mg/300ml300S4R531.03R1.77R162.583004296001
Voxwin Iv600 mg/300ml300S4R699.96R2.33R187.443004929001
Linzai Iv600 mg/300ml300S4R6978.91R2.33R595.18722439001
Zyvoxid 300ml600 mg/300ml300S4R9031.68R3.01R706.79898507008
Zyvoxid 200Mg/100Ml200 mg/100ml100S4R3162.54R3.16R387.67708873002

suspensionGeneric· 1 product

from R48.92/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Zyvoxid20 mg/ml150S4R7338.38R48.92R614.72700466003

FctGeneric· 4 products

from R82.71/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Lidonit600 mg30S4R2481.29R82.71R350.633009420001
Lidohet 600 mg10S4R1485.59R148.56R296.493009572001
Zenoxpar 600Mg600 mg10S4R1505.05R150.50R297.553003818001
Linezolid Lhc 600600 mg10S4R3187.49R318.75R389.033003719001

tabletGeneric· 8 products

from R150.50/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Linezolid teva600 mg10S4R1505.05R150.50R297.55722714001
Elturin 600600 mg10S4R1523.28R152.33R298.543005593001
Linokem600 mg10S4R1676.73R167.67R306.883003772001
Zenilid 600 Mg600 mg10S4R1934.09R193.41R320.873002381001
Aklid600 mg10S4R2699.10R269.91R362.47723836001
Voxwin (was Linezolid hetero)600 mg30S4R19594.76R653.16R1281.15721141002
Zyvoxid600 mg10S4R8370.56R837.06R670.85700464007
Linezolid specpharm600 mg10S4R8370.72R837.07R670.86721512001

injectionGeneric· 1 product

from R266.21/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Zyvoxid 200Mg/100Ml200 mg/100ml1S4R266.21R266.21R98.44708873001

MlsGeneric· 1 product

from R668.36/unit
ProductStrengthPackSchedSEPUnitDisp feeNAPPI
Acetic acid600 mg10S4R6683.63R668.36R579.12721171001
Trade names (12)
  • Aklid
  • Linezolid Aspen
  • Linezolid Fresenius
  • Linezolid Hetero
  • Linezolid Specpharm
  • Linokem
  • Linzai
  • Voxwin
  • Voxwin IV
  • Zenilid
  • Zenoxpar
  • Zyvoxid

Medical aid coverage

data not yet integrated
Discovery Health
not yet integrated
  • Comprehensive Series—
  • Executive Plan—
  • KeyCare Series—
  • Priority Series—
  • Saver Series—

Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.

Bonitas Medical Fund
not yet integrated
  • BonClassic—
  • BonComprehensive—
  • BonEssential—
  • BonFit Select—
  • BonSave—
  • BonStart—

Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.

GEMS — Government Employees Medical Scheme
not yet integrated
  • Beryl—
  • Emerald—
  • Onyx—
  • Ruby—
  • Sapphire—
  • Tanzanite One—

Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.

POLMED — Police Medical Aid Scheme
not yet integrated
  • Aquarium Option—
  • Efficiency Option—
  • Marine Option—

Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.

Interacts with 28 known drugs

Check against other drugs →

Cited in 19 documents

NeoHealth® ID 14700 · updated 10/16/2025