linezolid

General

Pronunciation
li-NEZ-o-lid [Pronunciation]

Trade Name(s)

• Zyvox

Pregnancy Category
Category C

Ther. class.
anti-infectives

Pharm. class.
oxazolidinones

Indications

Treatment of:

» Infections caused by vancomycin-resistant Enterococcus faecium ,

» Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains),

» Complicated skin/skin structure infections caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes or Streptococcus agalactiae (including diabetic foot infections),

» Uncomplicated skin/skin structure infections caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains), Streptococcus pyogenes ,

» Community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains) or Staphylococcus aureus (methicillin-susceptible strains only).

Action

Inhibits bacterial protein synthesis at the level of the 23S ribosome of the 50S subunit.

Therapeutic Effect(s):
Bactericidal action against streptococci; bacteriostatic action against enterococci and staphylococci.

Pharmacokinetics

Absorption: Rapidly and extensively (100%) absorbed following oral administration.

Distribution: Readily distributes to well-perfused tissues.

Metabolism and Excretion: 65% metabolized, mostly by the liver; 30% excreted unchanged by the kidneys.

Half-life: 6.4 hr.

TIME/ACTION PROFILE

ROUTE	ONSET	PEAK	DURATION
PO	rapid	1–2 hr	12 hr
IV	rapid	end of infusion	12 hr

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;

• Phenylketonuria (suspension contains aspartame);

• Uncontrolled HTN, pheochromocytoma, thyrotoxicosis, or concurrent use of sympathomimetic agents, vasopressors, or dopaminergic agents (↑ risk of hypertensive response);

• Concurrent or recent (<2 wk) use of monoamine oxidase (MAO) inhibitors (↑ risk of hypertensive response);

• Carcinoid syndrome or concurrent use of SSRIs, TCAs, triptans, meperidine, or buspirone (↑ risk of serotonin syndrome).

Use Cautiously in:

• Thrombocytopenia, concurrent use of antiplatelet agents or bleeding diathesis (platelet counts should be monitored more frequently);

• OB: Safety not established; use only if maternal benefit outweighs potential risk to fetus;

• Lactation: Lactation.

Adverse Reactions/Side Effects

CV: headache, insomnia.

EENT: teeth discoloration, tongue discoloration.

GI: PSEUDOMEMBRANOUS COLITIS, diarrhea, ↑ liver enzymes, nausea, taste alteration, vomiting.

F and E: lactic acidosis.

Hemat: thrombocytopenia.

Neuro: optic neuropathy, peripheral neuropathy.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

• ↑ risk of hypertensive response with MAO inhibitors , sympathomimetics (e.g., pseudoephedrine ), vasopressors (e.g., epinephrine , norepinephrine ), and dopaminergic agents (e.g., dopamine , dobutamine ); concurrent or recent use should be avoided.

• ↑ risk of serotonin syndrome with SSRIs , TCAs , 5–HT1 agonists , meperidine , or buspirone ; concurrent use should be avoided.

• Rifampin , carbamazepine , phenytoin , and phenobarbital may ↓ levels.

Drug-Food
Because of monoamine oxidase inhibitory properties, consumption of large amounts of foods or beverages containing tyramine should be avoided (↑ risk of pressor response. See Food Sources for Specific Nutrients).

Route/Dosage

Vancomycin-Resistant Enterococcus faecium Infections

• 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)..

Pneumonia, Complicated Skin/Skin Structure Infections

• 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)..

Uncomplicated Skin/Skin Structure Infections

• 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)..

Availability

• Oral suspension: (orange): 20 mg/mL

• Tablets: 400 mg, 600 mg

» Cost: 600 mg $2,213.46/30.

• Premixed infusion: 200 mg/100 mL, 400 mg/200 mL, 600 mg/300 mL

Assessment

• Assess for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and during therapy.

• Obtain specimens for culture and sensitivity prior to initiating therapy. First dose may be given before receiving.

• May cause lactic acidosis. Notify health care professional if recurrent nausea and vomiting, unexplained acidosis or low bicarbonate levels occur.

• Monitor visual function in patients receiving linezolid for ≥3 mo or who report visual symptoms (changes in acuity or color vision, blurred vision, visual field defect) regardless of length of therapy. If optic neuropathy occurs therapy should be reconsidered.

• Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of pseudomembranous colitis. May begin up to several weeks following cessation of therapy.

Lab Test Considerations

• May cause bone marrow suppression, anemia, leukopenia, pancytopenia. Monitor CBC and platelet count weekly, especially in patients at risk for increased bleeding, having pre-existing bone marrow suppression, receiving concurrent medications that may cause myelosuppression, or requiring >2 weeks of therapy. Discontinue therapy if bone marrow suppression occurs or worsens.

» May cause ↑ AST, ALT, LDH, alkaline phosphatase and BUN.

Potential Nursing Diagnoses

• Risk for infection (Indications)

• Diarrhea (Adverse Reaction)

Implementation

• Dose adjustment is not necessary when switching from IV to oral dose.

• PO: May be administered with or without food.

» Before using oral solution gently invert 3–5 times to mix; do not shake. Store at room temperature.

IV Adminstration:

• pH:
4.8.

• Intermittent Infusion:

Diluent: Premixed infusions are already diluted and ready to use. Solution is yellowish in color which may intensify over time without affecting its potency.
Concentration: 2 mg/mL.

• Rate:
Infuse over 30–120 minutes. Flush line before and after infusion.

• Y-Site Compatibility:

» acyclovir

» alfentanil

» allopurinol

» amifostine

» amikacin

» aminophylline

» amiodarone

» amphotericin B lipid complex

» amphotericin B liposome

» ampicillin

» ampicillin/sulbactam

» anidulafungin

» atracurium

» aztreonam

» bivalirudin

» bleomycin

» bumetanide

» buprenorphine

» busulfan

» butorphanol

» calcium chloride

» calcium gluconate

» carboplatin

» carmustine

» caspofungin

» cefazolin

» cefepime

» cefotaxime

» cefoxitin

» ceftazidime

.

» ceftriaxone

» cefuroxime

» chloramphenicol

» ciprofloxacin

» cisatracurium

» cisplatin

» clindamycin

» cyclophosphamide

» cyclosporine

» cytarabine

» dactinomycin

» daptomycin

» dexamethasone sodium phosphate

» dexmedetomidine

» dexrazoxane

» digoxin

» diltiazem

» diphenhydramine

» dobutamine

» docetaxel

» dolasetron

» dopamine

» doripenem

» doxacurium

» doxorubicin

» doxycycline

» droperidol

» enalaprilat

» ephedrine

» epinephrine

» epirubicin

» eptifibatide

» ertapenem

» esmolol

» etoposide

» etoposide phosphate

» famotidine

» fenoldopam

» fentanyl

» fluconazole

» fludarabine

» fluorouracil

» foscarnet

» fosphenytoin

» furosemide

» ganciclovir

» gemcitabine

» gentamicin

» glycopyrrolate

» granisetron

» haloperidol

» heparin

» hydralazine

» hydrocortisone

» hydromorphone

» idarubicin

» ifosfamide

» imipenem/cilastatin

.

» insulin

» irinotecan

» isoproterenol

» ketorolac

» labetalol

» leucovorin

» levofloxacin

» lidocaine

» lorazepam

» magnesium sulfate

» mannitol

» mechlorethamine

» melphalan

» meperidine

» meropenem

» mesna

» metaraminol

» methotrexate

» methyldopate

» methylprednisolone

» metoclopramide

» metoprolol

» metronidazole

» midazolam

» milrinone

» mitoxantrone

» morphine

» mycophenolate

» nafcillin

» nalbuphine

» naloxone

» nesiritide

» nicardipine

» nitroglycerin

» nitroprusside

» norepinephrine

» octreotide

» ondansetron

» oxaliplatin

» oxytocin

» paclitaxel

» palonosetron

» pamidronate

» pancuronium

» pemetrexed

» pentazocine

» pentobarbital

» phenobarbital

» phentolamine

» phenylephrine

» piperacillin/tazobactam

» potassium acetate

» potassium chloride

» potassium phosphates

» procainamide

» prochlorperazine

» promethazine

» propranolol

» quinupristin/dalfopristin

» ranitidine

» remifentanil

» rocuronium

» sodium acetate

» sodium bicarbonate

» sodium phosphates

» streptozocin

» succinylcholine

» sufentanil

» tacrolimus

» teniposide

» theophylline

» thiotepa

» ticarcillin/clavulanate

» tigecycline

» tirofiban

» tobramycin

» trimethoprim/sulfamethoxazole

» vancomycin

» vasopressin

» vecuronium

» verapamil

» vincristine

» vinorelbine

» voriconazole

» zidovudine

» zolendronic acid

• Y-Site Incompatibility:

» amphotericin B colloidal

» chlorpromazine

» dantrolene

» diazepam

» pantoprazole

» pentamidine

» phenytoin

» thiopental

Patient/Family Teaching

• Advise patients taking oral linezolid to take as directed, for full course of therapy, even if feeling better. Take missed doses as soon as remembered unless almost time for next dose; do not double dose.

• Instruct patient to avoid large quantities of foods or beverages containing tyramine (See Food Sources for Specific Nutrients). May cause hypertensive response.

• Instruct patient to notify health care professional if patient has a history of hypertension and before patient takes other Rx, OTC, or herbal products, especially cold remedies, decongestants, or antidepressants.

• Instruct patient to notify health care professional immediately if diarrhea, abdominal cramping, fever, or bloody stools occur and not to treat with antidiarrheals without consulting health care professionals.

• Advise patient to notify health care professional if no improvement is seen in a few days.

Evaluation/Desired Outcomes

Resolution of signs and symptoms of infection. Length of time for complete resolution depends on organism and site of infection.