LINEZOLID

LINEZOLID
(lin-e-zo'lid)
Zyvox, Zyvoxam 
Classifications: antibiotic, oxazolidinone;
Therapeutic: antibiotic

Pregnancy Category: C

Availability

400 mg, 600 mg tablets; 100 mg/5 mL suspension; 200 mg, 400 mg, 600 mg injection

Action

Synthetic antibiotic that binds to a site on the bacterial 23S ribosomal RNA of the bacteria which prevents the bacterial RNA translation process, thus preventing the bacteria from further growth.

Therapeutic Effect

Bacteriostatic against enterococci and staphylococci, and bactericidal against streptococci. Is bacteriocidal against gram-positive, gram-negative, and anaerobic bacteria.

Uses

Treatment of vancomycin-resistant Enterococcus faecium (VREF), nosocomial pneumonia, complicated and uncomplicated skin and skin structure infections, community-acquired pneumonia due to susceptible gram-positive organisms.

Contraindications

Hypersensitivity to linezolid, pregnancy (category C), lactation.

Cautious Use

Lactation, history of thrombocytopenia, thrombocytopenia; patients on MAOI, or serotonin reuptake inhibitors, or adrenergic agents, active alcoholism, anemia, bleeding, bone marrow suppression, cardiac arrhythmias, cardiac disease, cerebrovascular disease, chemotherapy, coagulopathy, colitis, diarrhea, hypertension, hyperthyroidism, leukopenia, MI, radiographic contrast administration, spinal anesthesia, surgery, hypertension; phenylketonuria; carcinoid syndrome.

Route & Dosage

Vancomycin-Resistant Enterococcus faecium
Adult/Adolescent (>12 y): PO/IV 600 mg q12h x 14–28 d
Child (2–11 y): PO/IV 10 mg/kg q8h x 14–28 d

Nosocomial or Community-Acquired Pneumonia, Complicated Skin Infections
Adult/Adolescent (>12 y): PO/IV 600 mg q12h x 10–14 d
Child (5–11 y): PO/IV 10 mg/kg q8h x 10–14 d

Uncomplicated Skin Infections
Adult: PO 400 mg q12h x 10–14 d
Adolescent: PO 600 mg q12h x 10–14 d
Child: PO <5 y, 10 mg/kg q8h x 10–14 d; 5–11 y, 10 mg/kg q12h x 10–14 d

Administration

Note: No dosage adjustment is necessary when switching from IV to oral administration.

Oral
  • Reconstitute suspension by adding 123 mL distilled water in two portions; after adding first half, shake to wet all of the powder, then add second half of water and shake vigorously to produce a uniform suspension with a concentration of 100 mg/5 mL.
  • Before each use, mix suspension by inverting bottle 3–5 times, but DO NOT SHAKE. Discard unused suspension after 21 d.
Intravenous

PREPARE: Intermittent: IV solution is supplied in a single-use, ready-to-use infusion bag. Remove from protective wrap immediately prior to use. Check for minute leaks by firmly squeezing bag. Discard if leaks are detected.  

ADMINISTER: Intermittent: Do not use infusion bag in a series connection. Give over 30–120 min. If IV line is used to infuse other drugs, flush before and after with D5W, NS, or LR.  

INCOMPATIBILITIES Solution/additive: Ceftriaxone, erythromycin, trimethoprim-sulfamethoxazole. Y-site: Amphotericin B, ceftriaxone, chlorpromazine, diazepam, pentamidine, phenytoin.

  • Store at 25° C (77° F) preferred; 15°–30° C (59°–86° F) permitted. Protect from light and keep bottles tightly closed.

Adverse Effects (≥1%)

Body as a Whole: Fever. GI: Diarrhea, nausea, vomiting, constipation, taste alteration, abnormal LFTs, tongue discoloration. Hematologic: Thrombocytopenia, leukopenia. CNS: Headache, insomnia, dizziness. Skin: Rash. Urogenital: Vaginal moniliasis.

Interactions

Drug: mao inhibitors may cause hypertensive crisis; pseudoephedrine may cause elevated BP; may cause serotonin syndrome with selective serotonin reuptake inhibitors. Food: Tyramine-containing food may cause elevated BP. Herbal: Ginseng, ephedra, ma huang may lead to elevated BP, headache, nervousness.

Pharmacokinetics

Absorption: Rapidly or extensively absorbed, 100% bioavailable. Peak: 1–2 h PO. Distribution: 31% protein bound. Metabolism: By oxidation. Elimination: Primarily in urine. Half-Life: 6–7 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for signs and symptoms in individuals with a history of seizure activity or conditions that make them prone to seizures. If a seizure occurs, discontinue the drug and report to the physician immediately.
  • Monitor for S&S of: Bleeding; hypertension; or pseudomembranous colitis that begins with diarrhea.
  • Lab tests: C&S before initiating therapy and during therapy as indicated; drug may be started pending results. Monitor complete blood count, including platelet count and Hgb & Hct, in those at risk for bleeding or with >2 wk of linezolid therapy.

Patient & Family Education

  • Report any of the following to physician promptly: Onset of diarrhea; easy bruising or bleeding of any type; or S&S of superinfection (see Appendix F), S&S of seizure activity.
  • Avoid foods and beverages high in tyramine (e.g., aged, fermented, pickled, or smoked foods, and beverages). Limit tyramine intake to <100 mg per meal (see Information for Patients provided by the manufacturer).
  • Do not take OTC cold remedies or decongestants without consulting physician.
  • Note for phenylketonurics: Each 5 mL oral suspension contains 20 mg phenylalanine.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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