Treatment of vancomycin-resistant Enterococcus faecium , including cases with concurrent bacteremia; treatment of nosocomial pneumonia, complicated and uncomplicated skin and skin structure infections (including diabetic foot infections without concomitant osteomyelitis), and community-acquired pneumonia caused by susceptible strains of specific organisms.
|•||PO, IV (Adults): 600 mg every 12 hr for 14–28 days.|
|•||PO, IV (Children birth-11 yr): (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).|
|•||PO, IV (Adults): 600 mg every 12 hr for 10–14 days.|
|•||PO, IV (Children birth-11 yr): 10 mg/kg every 8 hr for 10–14 days (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).|
|•||PO (Adults): 400 mg q 12 hr for 10–14 days .|
|•||PO, IV (Children 5-11 yr): 10 mg/kg every 12 hr for 10–14 days.|
|•||PO, IV (Children < 5 yr): 10 mg/kg every 8 hr for 10–14 days (in the first week of life, pre-term neonates may initially receive 10 mg/kg every 12 hr).|
|•||Inhibits bacterial protein synthesis at the level of the 23S ribosome of the 50S subunit.|
|•||Bactericidal action against streptococci; bacteriostatic action against enterococci and staphylococci.|
Concomitant use or use within 14 days of any medicinal product that inhibits MAO-A or MAO-B; hypersensitivity to linezolid or any of the other product components.
Unless carefully observed for potential increases in BP, use is contraindicated in patients with uncontrolled hypertension, pheochromocytoma, and/or thyrotoxicosis; use is also contraindicated in patients with carcinoid syndrome or in patients taking directly and indirectly acting sympathomimetic agents, vasopressive agents, dopaminergic agents, serotonin reuptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists, meperidine, or buspirone, unless carefully observed for signs and/or symptoms of serotonin syndrome.
CNS: Headache (7%); convulsions, insomnia (3%); dizziness (2%); vertigo (1%); peripheral neuropathy (postmarketing).
DERM: Rash (7%); skin disorder (2%); bullous skin disorders (postmarketing).
EENT: Pharyngitis (3%); optic neuropathy sometimes progressing to vision loss (postmarketing).
GI: Diarrhea (11%); vomiting (9%); nausea (6%); altered taste, constipation, generalized and localized abdominal pain, GI bleeding, loose stools (2%); oral moniliasis, tongue discoloration (1%).
GU: Vaginal moniliasis (2%).
HEMA: Anemia (6%); thrombocytopenia (5%); thrombocythemia (3%); eosinophilia (1%); leukopenia, pancytopenia (postmarketing).
LABTESTABS: Abnormal Hgb (16%); abnormal platelets (13%); abnormal WBC (12%); abnormal ALT (10%); abnormal neutrophils, abnormal total bilirubin (6%); abnormal AST (5%); abnormal alkaline phosphatase, abnormal lipase (4%); abnormal amylase, BUN, creatinine, and LDH (2%).
LOCAL: Injection- or catheter-site reactions (3%).
METAB: Hypokalemia (3%); generalized edema (2%); lactic acidosis (postmarketing).
RESP: Upper respiratory tract infection (4%); dyspnea, pneumonia (3%); apnea, cough (2%).
OTHER: Fever (14%); sepsis (8%); trauma (3%); fungal infections, localized pain (2%); anaphylaxis, angioedema, serotonin syndrome, superficial tooth discoloration, tongue discoloration (postmarketing).
Linezolid is a reversible, nonselective MAOI. Apraclonidine is contraindicated in patients receiving MAOIs. The risk of hypertension may be increased. Do not coadminister linezolid and apraclonidine within 14 days of each other.
Risk of serious or fatal reactions, including hyperthermia and rapid fluctuations in vital signs, may be increased. Coadministration of linezolid and atomoxetine within 14 days of each other is contraindicated.
Beta-2 agonists (eg, albuterol)
Coadministration of linezolid and beta-2 agonists may result in adverse CV effects characterized by hypertension. Use caution when administering linezolid with or within 14 days of beta-2 agonists. Monitor for potential increases in BP with coadministration of these agents.
Bupropion, cyclobenzaprine, methylphenidate
The risk of hypertensive crisis is increased. Do not coadminister these agents and linezolid within 14 days of each other.
Buspirone, meperidine, selective 5-HT1 receptor agonists (eg, sumatriptan), serotonin reuptake inhibitors (eg, fluoxetine, paroxetine, sertraline, venlafaxine), tricyclic antidepressants (eg, amitriptyline)
Unless patients are carefully observed for signs and symptoms of serotonin syndrome, do not coadminister linezolid with these agents. Serotonin syndrome requires immediate medical attention, including withdrawal of the serotonergic agent and supportive care.
Catechol-O-methyl-transferase inhibitors (eg, entacapone)
Coadministration of linezolid and catechol-O-methyl-transferase (COMT) inhibitors may result in inhibition of the majority of pathways responsible for normal catecholamine metabolism. Excessive sympathetic stimulation may result. Use of linezolid with COMT inhibitors is not recommended.
Dopaminergic agents (eg, dobutamine, dopamine), sympathomimetic agents (eg, pseudoephedrine), vasopressive agents (eg, epinephrine, norepinephrine)
Unless patients are monitored for increases in BP, do not coadminister linezolid with dopaminergic agents.
Use of linezolid with ginseng may produce unexpected toxic effects (eg, headache, manic-like symptoms). Avoid concomitant use of linezolid and ginseng.
Linezolid may increase the pharmacologic and toxic effects (flushing, headache, and hypertension) of levodopa. Hypertensive crisis may occur. Avoid coadministration of levodopa and linezolid. If inadvertently given and hypertension occurs, administer phentolamine.
MAOIs (eg, phenelzine)
Linezolid is a reversible, nonselective MAOI; do not coadminister with any medicinal product that inhibits MAO-A or MAO-B or within 2 wk of administering such products.
A severe reaction potentially involving the respiratory, cardiac, and central nervous systems may occur shortly after administering propoxyphene to patients receiving linezolid. Because of the potential seriousness of the consequences, use propoxyphene with caution in patients receiving linezolid.
Rifamycins (eg, rifampin)
Linezolid Cmax and AUC (exposure) may be reduced, decreasing the pharmacologic effects. Monitor the response of the patient and adjust therapy as needed.
The risk of serotonin syndrome may be increased. Serotonergic effects of these agents may be additive. MAOIs are contraindicated in patients receiving sibutramine.
The combination of linezolid and tetrabenazine may produce severe unexpected toxicity (eg, behavioral changes, confusion, restlessness). Coadministration of linezolid and tetrabenazine is contraindicated.
The risk of serotonin syndrome may be increased. Serotonergic effects of these agents may be additive. Carefully monitor patients for adverse reactions, including signs and symptoms of serotonin syndrome. Serotonin syndrome requires immediate medical attention, including withdrawal of the serotonergic agent and supportive care.
Therapeutic Classification: anti-infectives
Pharmacologic Classification: oxazolidinones
Absorption: Rapidly and extensively (100%) absorbed following oral administration.
Distribution: Readily distributes to well-perfused tissues.
Metabolism/Excretion: 65% metabolized, mostly by the liver; 30% excreted unchanged by the kidneys.
Half-life: 6.4 hr.
|ORAL||RAPID||1-2 HOUR||12 HOUR|
|INTRAVENOUS||RAPID||END OF INFUSION||12 HOUR|