What are the contraindications to Linezolid (Oxazolidinone antibiotic)?

From the Guidelines

Linezolid is contraindicated in patients with hypersensitivity to the drug, those taking monoamine oxidase inhibitors, and in patients with uncontrolled hypertension, phaeochromocytoma, carcinoid tumor, thyrotoxicosis, bipolar depression, schizophrenia, or acute confusional states, as well as in breastfeeding women.

Contraindications

• Hypersensitivity to linezolid 1
• Concomitant use of monoamine oxidase inhibitors (eg, phenelzine, isocarboxazid, selegiline, moclobemide) or within 2 weeks of taking any such medicinal product 1
• Uncontrolled hypertension, phaeochromocytoma, carcinoid tumor, thyrotoxicosis, bipolar depression, schizophrenia, or acute confusional states 1
• Breast feeding 1 The use of linezolid requires careful consideration of its potential side effects, including cytopenias, peripheral neuropathy, optic neuritis, serotonin syndrome, and lactic acidosis 1. Additionally, monitoring for severe anemia is important, especially in patients with preexisting anemia 1.

From the FDA Drug Label

ZYVOX formulations are contraindicated for use in patients who have known hypersensitivity to linezolid or any of the other product components. Monoamine 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 Unless patients are monitored for potential increases in blood pressure, linezolid should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis and/or patients taking any of the following types of medications: directly and indirectly acting sympathomimetic agents (e.g., pseudoephedrine), vasopressive agents (e.g., epinephrine, norepinephrine), dopaminergic agents (e.g., dopamine, dobutamine) Unless patients are carefully observed for signs and/or symptoms of serotonin syndrome, 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 or buspirone

The contraindications to Linezolid are:

• Known hypersensitivity to linezolid or any of the other product components
• Use of monoamine oxidase inhibitors (MAOIs)
• Uncontrolled hypertension
• Pheochromocytoma
• Thyrotoxicosis
• Use of certain medications, including:
  • Directly and indirectly acting sympathomimetic agents
  • Vasopressive agents
  • Dopaminergic agents
• Carcinoid syndrome
• Use of certain medications, including:
  • Serotonin re-uptake inhibitors
  • Tricyclic antidepressants
  • Serotonin 5-HT1 receptor agonists (triptans)
  • Meperidine or buspirone 2

From the Research

Contraindications to Linezolid

The following are contraindications to Linezolid:

• Use in patients with uncontrolled hypertension, pheochromocytoma, carcinoid syndrome, or other conditions where an increase in blood pressure could be harmful 3, 4
• Use in patients taking monoamine oxidase inhibitors (MAOIs) or other medications that increase serotonin levels, due to the risk of serotonin syndrome 3, 5, 4
• Use in patients with a history of myelosuppression, neuropathies, or lactic acidosis, as linezolid may exacerbate these conditions 5
• Use in patients with untreated hyperthyroidism, as linezolid may increase the risk of thyroid storm 4

Special Considerations

The following are special considerations for the use of linezolid:

• Linezolid should be used with caution in patients with renal insufficiency or those receiving renal replacement therapy, as the drug may accumulate to toxic levels 6
• Linezolid should be used with caution in patients taking medications that interact with the cytochrome P450 enzyme system, although linezolid is not metabolized by this system 7
• Linezolid should be used with caution in patients with a history of seizures or other neurological disorders, as the drug may lower the seizure threshold 5

Warnings and Precautions

The following are warnings and precautions for the use of linezolid:

• Linezolid may cause thrombocytopenia, anemia, or other hematologic abnormalities, and patients should be monitored for these adverse effects 6, 7, 5
• Linezolid may cause neuropathy, and patients should be monitored for signs and symptoms of this condition 6, 5
• Linezolid may cause lactic acidosis, and patients should be monitored for signs and symptoms of this condition 5
• Linezolid may cause serotonin syndrome, and patients should be monitored for signs and symptoms of this condition 3, 5