Linezolid and Tedizolid
Linezolid and tedizolid are oxazolidinone antibiotics (see Lincosamides, Oxazolidinones, and Streptogramins).
Linezolid is an oxazolidinone antibiotic that has activity against the following:
Linezolid is contraindicated in patients with a prior allergic reaction to it.
Other contraindications include having risk factors for serotonin syndrome or hypertension.
Linezolid is a reversible, nonselective monamine oxidase inhibitor (MAOI); MAO inhibition causes levels of the neurotransmitter serotonin to increase. Thus, linezolid has the potential for causing serotonin syndrome (a hyperserotonergic state characterized by mental status changes, neurologic abnormalities, and autonomic instability—see also Serotonin Syndrome) when it is used in patients with either of the following: .
Endocrinologically active carcinoid tumors (see Overview of Carcinoid Tumors)
Use of drugs with serotonergic activity
Such drugs include SSRIs, MAOIs (eg, phenelzine, isocarboxazid), tricyclic antidepressants, serotonin 1B,1D receptor agonists (triptans), meperidine, bupropion, and buspirone. Patients who are taking such drugs and urgently need linezolid may be treated if the benefit is thought to outweigh the risk and if they
Linezolid is not been studied in patients with carcinoid syndrome; it should be used only if patients are closely monitored for symptoms and signs of serotonin syndrome.
Linezolid should not be given to the following patients unless they are monitored for potential increases in BP:
Adverse effects include
Reversible myelosuppression, including thrombocytopenia, leukopenia, and anemia, occurs in about 3% of patients, usually when therapy is used > 2 wk. Consequently, CBC is monitored weekly, especially when therapy lasts > 2 wk.
Peripheral and optic neuropathy may occur with prolonged use, and patients taking long-term linezolid therapy should be closely monitored for these disorders.
Tedizolid is an oxazolidinone antibiotic with a spectrum of activity similar to that of linezolid, although it may have activity against some linezolid-resistant gram-positive cocci.
In clinical trials, risk of serotonin syndrome and thrombocytopenia was lower with tedizolid than with linezolid. Tedizolid can cause significant neutropenia and its use is not recommended in patients with neutrophil counts of < 1000 cell/mm3.