Drugs List

Therapeutic Indications

Uses

Community acquired pneumonia
Complicated skin and soft tissue infections
Nosocomial pneumonia

Nosocomial pneumonia or community acquired pneumonia caused by confirmed or suspected gram positive bacteria. Combination therapy will be necessary if a concomitant Gram negative pathogen is documented or suspected.

Complicated skin and soft tissue infections caused by confirmed gram positive bacteria. Combination therapy will be necessary if a concomitant Gram negative pathogen is documented or suspected.

Administration

For intravenous infusion, to be administered over a period of 30 to 120 minutes.

Contraindications

Within 2 weeks of discontinuing other MAOIs
Breastfeeding

Precautions and Warnings

Carcinoid
Children under 18 years
Elderly
Impaired glucose tolerance
Predisposition to seizures
Restricted sodium intake
Bipolar disorder
Confusional states
Diabetes mellitus
Hepatic impairment
History of seizures
Myelosuppression
Phaeochromocytoma
Pregnancy
Renal dialysis
Renal impairment - creatinine clearance below 30 ml/minute
Schizoaffective disorder
Thyrotoxicosis
Uncontrolled hypertension

Sodium content of formulation may be significant
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Contains glucose
Assess risk/benefit of treatment if symptoms of peripheral neuropathy occur
If visual disturbances occur, perform ophthalmic evaluation
Monitor blood counts in anaemia, leukopenia and thrombocytopenia
Monitor closely patients receiving > 10-14 days of treatment
Monitor closely patients receiving myelosuppressive drugs
Monitor closely patients with pre-existing myelosuppression
Monitor for development of lactic acidosis
Monitor for signs of superinfection with non-susceptible organisms
Monitor full blood counts weekly
When used with SSRIs, risk of Serotonin syndrome
Advise patient to report new visual problems and symptoms
Consider pseudomembranous colitis if patient presents with diarrhoea
Discontinue if myelosuppression occurs
Discontinue if serotonin syndrome develops
Discontinue if severe and persistent diarrhoea develops
Not recommended for use longer than 4 weeks
Advise patient against consuming large amounts of tyramine rich foods
Male: May cause infertility

Elderly patients may be at greater risk of experiencing blood dyscrasias than younger patients.

Thrombocytopenia may occur more commonly in patients with severe renal impairment, whether or not on dialysis.

Linezolid inhibits mitochondrial protein synthesis, which can cause lactic acidosis, anaemia and neuropathy. More commonly in treatments lasting longer than 28 days.

Microbiological tests and the prevalence of antibacterial agent resistance in Gram positive bacteria, should be considered before linezolid treatment.

In patients taking linezolid for longer than the recommended 28 days, their visual function should be monitored.

Sideroblastic anaemia has been reported in patients who had been treated with linezolid for more than 28 days. Most patients fully or partially recovered following discontinuation of linezolid.

Pregnancy and Lactation

Pregnancy

Use linezolid with caution in pregnancy.

At the time of writing there is limited data on the use of linezolid in pregnant women. It is not known if linezolid crosses the placenta, but the molecular weight is low enough that transfer to the foetus should be expected.

Studies in animals have shown reproductive toxicity and a potential risk for humans exists.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Linezolid is contraindicated during breastfeeding.

The molecular weight is low enough that excretion of linezolid should be expected. The effects of this on the breastfed infant are unknown. Limited data indicate that the maximum dose an infant would receive through breast milk would be much lower than the standard infant dose.

It is suggested that if linezolid is required by the mother, breastfeeding can be continued but the infant should be monitored for possible effects on the gastrointestinal tract.

Animal data suggest that linezolid and its metabolites may pass into animal milk.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal pain
Abnormal liver function tests
Abnormal serum sodium levels
Alopecia
Anaemia
Anaphylaxis
Angioedema
Arrhythmias
Blood glucose disturbances
Blurred vision
Bullous reactions
Candidiasis
Changes in blood chemistry
Chills
Colour vision deficiencies
Constipation
Convulsions
Creatine kinase increased
Decrease in haemoglobin and haematocrit
Decrease in plasma calcium
Decreased serum albumin
Decreased total serum protein
Dermatitis
Diaphoresis
Diarrhoea/loose stools
Dizziness
Dry mouth
Dyspepsia
Elevated amylase levels
Elevated serum lipase
Eosinophilia
Fatigue
Fever
Fluctuating serum potassium levels
Fungal infection
Gastritis
Glossitis
Headache
Hypertension
Hypoaesthesia
Hyponatraemia
Increase in alkaline phosphatase
Increase in blood urea nitrogen
Increase in lactate dehydrogenase
Increase in plasma calcium
Increase in serum ALT/AST
Increased platelet count
Increased thirst
Increases in eosinophils
Insomnia
Lactic acidosis
Leucopenia
Local pain
Local pain (injection site)
Loss of vision
Metallic taste
Myelosuppression
Nausea
Neutropenia
Optic neuritis
Optic neuropathy
Pancreatitis
Pancytopenia
Paraesthesia
Peripheral neuropathy
Phlebitis
Polyuria
Pruritus
Pseudomembranous colitis
Raised neutrophil count
Rash
Reduced neutrophil count
Reduced platelet count
Renal failure
Reticulocytosis
Serotonin syndrome
Serum bilirubin increased
Serum creatinine increased
Sideroblastic anaemia
Stevens-Johnson syndrome
Stomatitis
Superficial tooth discolouration
Taste disturbances
Thrombocytopenia
Thrombophlebitis
Tinnitus
Tongue discolouration
Toxic epidermal necrolysis
Transient ischaemic attack
Urticaria
Vaginitis
Visual field defects
Vomiting
Vulvovaginal disorders
White blood cell count decreased
White blood cell count raised

Presentation

Parenteral formulations of linezolid.

Drugs List

Therapeutic Indications

Uses

Community acquired pneumonia
Complicated skin and soft tissue infections
Nosocomial pneumonia

Nosocomial pneumonia or community acquired pneumonia caused by confirmed or suspected gram positive bacteria. Combination therapy will be necessary if a concomitant Gram negative pathogen is documented or suspected.

Complicated skin and soft tissue infections caused by confirmed gram positive bacteria. Combination therapy will be necessary if a concomitant Gram negative pathogen is documented or suspected.

Dosage

Adults

Children

Neonates

Additional Dosage Information

Administration

For intravenous infusion, to be administered over a period of 30 to 120 minutes.

Contraindications

Within 2 weeks of discontinuing other MAOIs
Breastfeeding

Precautions and Warnings

Carcinoid
Children under 18 years
Elderly
Impaired glucose tolerance
Predisposition to seizures
Restricted sodium intake
Bipolar disorder
Confusional states
Diabetes mellitus
Hepatic impairment
History of seizures
Myelosuppression
Phaeochromocytoma
Pregnancy
Renal dialysis
Renal impairment - creatinine clearance below 30 ml/minute
Schizoaffective disorder
Thyrotoxicosis
Uncontrolled hypertension

Sodium content of formulation may be significant
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Contains glucose
Assess risk/benefit of treatment if symptoms of peripheral neuropathy occur
If visual disturbances occur, perform ophthalmic evaluation
Monitor blood counts in anaemia, leukopenia and thrombocytopenia
Monitor closely patients receiving > 10-14 days of treatment
Monitor closely patients receiving myelosuppressive drugs
Monitor closely patients with pre-existing myelosuppression
Monitor for development of lactic acidosis
Monitor for signs of superinfection with non-susceptible organisms
Monitor full blood counts weekly
When used with SSRIs, risk of Serotonin syndrome
Advise patient to report new visual problems and symptoms
Consider pseudomembranous colitis if patient presents with diarrhoea
Discontinue if myelosuppression occurs
Discontinue if serotonin syndrome develops
Discontinue if severe and persistent diarrhoea develops
Not recommended for use longer than 4 weeks
Advise patient against consuming large amounts of tyramine rich foods
Male: May cause infertility

Elderly patients may be at greater risk of experiencing blood dyscrasias than younger patients.

Thrombocytopenia may occur more commonly in patients with severe renal impairment, whether or not on dialysis.

Linezolid inhibits mitochondrial protein synthesis, which can cause lactic acidosis, anaemia and neuropathy. More commonly in treatments lasting longer than 28 days.

Microbiological tests and the prevalence of antibacterial agent resistance in Gram positive bacteria, should be considered before linezolid treatment.

In patients taking linezolid for longer than the recommended 28 days, their visual function should be monitored.

Sideroblastic anaemia has been reported in patients who had been treated with linezolid for more than 28 days. Most patients fully or partially recovered following discontinuation of linezolid.

Pregnancy and Lactation

Pregnancy

Use linezolid with caution in pregnancy.

At the time of writing there is limited data on the use of linezolid in pregnant women. It is not known if linezolid crosses the placenta, but the molecular weight is low enough that transfer to the foetus should be expected.

Studies in animals have shown reproductive toxicity and a potential risk for humans exists.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14-17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Linezolid is contraindicated during breastfeeding.

The molecular weight is low enough that excretion of linezolid should be expected. The effects of this on the breastfed infant are unknown. Limited data indicate that the maximum dose an infant would receive through breast milk would be much lower than the standard infant dose.

It is suggested that if linezolid is required by the mother, breastfeeding can be continued but the infant should be monitored for possible effects on the gastrointestinal tract.

Animal data suggest that linezolid and its metabolites may pass into animal milk.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Abdominal pain
Abnormal liver function tests
Abnormal serum sodium levels
Alopecia
Anaemia
Anaphylaxis
Angioedema
Arrhythmias
Blood glucose disturbances
Blurred vision
Bullous reactions
Candidiasis
Changes in blood chemistry
Chills
Colour vision deficiencies
Constipation
Convulsions
Creatine kinase increased
Decrease in haemoglobin and haematocrit
Decrease in plasma calcium
Decreased serum albumin
Decreased total serum protein
Dermatitis
Diaphoresis
Diarrhoea/loose stools
Dizziness
Dry mouth
Dyspepsia
Elevated amylase levels
Elevated serum lipase
Eosinophilia
Fatigue
Fever
Fluctuating serum potassium levels
Fungal infection
Gastritis
Glossitis
Headache
Hypertension
Hypoaesthesia
Hyponatraemia
Increase in alkaline phosphatase
Increase in blood urea nitrogen
Increase in lactate dehydrogenase
Increase in plasma calcium
Increase in serum ALT/AST
Increased platelet count
Increased thirst
Increases in eosinophils
Insomnia
Lactic acidosis
Leucopenia
Local pain
Local pain (injection site)
Loss of vision
Metallic taste
Myelosuppression
Nausea
Neutropenia
Optic neuritis
Optic neuropathy
Pancreatitis
Pancytopenia
Paraesthesia
Peripheral neuropathy
Phlebitis
Polyuria
Pruritus
Pseudomembranous colitis
Raised neutrophil count
Rash
Reduced neutrophil count
Reduced platelet count
Renal failure
Reticulocytosis
Serotonin syndrome
Serum bilirubin increased
Serum creatinine increased
Sideroblastic anaemia
Stevens-Johnson syndrome
Stomatitis
Superficial tooth discolouration
Taste disturbances
Thrombocytopenia
Thrombophlebitis
Tinnitus
Tongue discolouration
Toxic epidermal necrolysis
Transient ischaemic attack
Urticaria
Vaginitis
Visual field defects
Vomiting
Vulvovaginal disorders
White blood cell count decreased
White blood cell count raised

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: December 2018

Reference Sources

Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.

Summary of Product Characteristics: Zyvox 2mg/ml solution for infusion. Pharmacia Ltd. Revised January 2017.
Summary of Product Characteristics: Linezolid 2mg/ml solution for infusion, B. Braun Melsungen AG. Revised February 2017.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 19 December 2018.

US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Linezolid Last revised: 3rd December 2018
Last accessed: 18th December 2018.