linezolid


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linezolid

 [lĭ-nez´o-lid]
a synthetic antibacterial of the oxazolidinone class, effective against gram-positive organisms; used for the treatment of community-acquired and nosocomial pneumonia, skin and soft tissue infections, and bacteremia, administered orally or intravenously.

linezolid

Zyvox, Zyvoxam (CA)

Pharmacologic class: Oxazolidinone

Therapeutic class: Anti-infective

Pregnancy risk category C

Action

Selectively binds to bacterial 23S ribosomal RNA of 50S subunit, preventing formation of essential component of bacterial protein synthesis. Bacteriostatic or bactericidal against gram-positive and some gram-negative bacteria.

Availability

Injection: 2 mg/ml

Powder for oral suspension: 100 mg/5 ml

Tablets: 400 mg, 600 mg

Indications and dosages

Vancomycin-resistant Enterococcus faecium infections

Adults and children ages 12 and older: 600 mg P.O. or I.V. infusion q 12 hours for 14 to 28 days

Children from birth to age 11: 10 mg/kg I.V. q 8 hours for 14 to 28 days

Nosocomial pneumonia; community-acquired pneumonia; complicated skin and skin-structure infections

Adults and children ages 12 and older: 600 mg P.O. or I.V. infusion q 12 hours for 10 to 14 days

Children from birth to age 11: 10 mg/kg P.O. or I.V. q 8 hours for 10 to 14 days

Uncomplicated skin and soft-tissue infections

Adults: 400 mg P.O. q 12 hours for 10 to 14 days

Adolescents: 600 mg P.O. or I.V. q 12 hours for 10 to 14 days

Children ages 5 to 11: 10 mg/kg P.O. or I.V. q 12 hours for 10 to 14 days

Children younger than age 5: 10 mg/kg P.O. or I.V. q 8 hours for 10 to 14 days

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• hepatic dysfunction, hypertension, hyperthyroidism, pheochromocytoma, bone marrow depression, pseudomembranous colitis

• phenylketonuria (oral suspension only)

• pregnant or breastfeeding patients.

Administration

• Give oral drug with or without food.

• For I.V. injection, use single-use, ready-to-use infusion bag. Check for particulate matter before giving. Infuse over 30 minutes to 2 hours.

• For I.V. infusion, mix with dextrose 5% in water, normal saline solution, or lactated Ringer's injection.

• Flush I.V. line before and after administering, to avoid incompatibilities.

Adverse reactions

CNS: anxiety, confusion, difficulty speaking, dizziness, hallucinations, lethargy, paresthesia, light-headedness, fatigue, drowsiness, headache, seizures

GI: nausea, vomiting, diarrhea, gastritis, anorexia, dry mouth, pseudomembranous colitis

Hematologic: thrombocytopenia

Skin: rash, photosensitivity, diaphoresis

Other: fever, fungal infections

Interactions

Drug-drug. Antiplatelet drugs (such as aspirin, dipyridamole, nonsteroidal anti-inflammatory drugs): increased bleeding risk

MAO inhibitors, pseudoephedrine: increased risk of hypertension and associated adverse effects

Serotonergics: serotonin syndrome

Drug-diagnostic tests. Prothrombin time: altered

Drug-food. Tyramine-containing foods and beverages (such as beer; Chianti and certain other red wines; aged cheese; bananas; aged, cured, or spoiled meats; salted herring and other dried fish; avocado; bean curd; red plums; soy sauce; spinach; tofu, tomatoes; yeast): hypertension

Patient monitoring

• Monitor neurologic status. Institute safety measures as needed to prevent injury.

• Check I.V. site for infiltration.

Watch for bleeding and signs and symptoms of other adverse reactions (especially pseudomembranous colitis).

• Monitor CBC, coagulation studies, and culture and sensitivity tests.

Patient teaching

• Tell patient he may take with or without food, but should avoid foods containing tyramine.

Tell patient to promptly report bleeding or severe diarrhea.

• Instruct patient to minimize adverse GI effects by eating small, frequent servings of healthy food.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.

linezolid

Infectious disease An oxazolidinone antimicrobial in trials for gram-positive bacteria, possibly for managing VRE. See Vancomycin-resistant enterococcus.
References in periodicals archive ?
Pretomanid in combination with bedaquiline and linezolid is approved for treating a limited and specific population of adult patients with extensively drug resistant, treatment-intolerant or nonresponsive multidrug resistant pulmonary TB.
Besiyerlerinin birine fusidik asid (10 [micro]g), linezolid (10 [micro]g), kinupristin/dalfopristin (15 [micro]g), kloramfenikol (30 [micro]g), rifampisin (5 [micro]g), siprofloksasin (5 [micro]g) ve levofloksasin (10 [micro]g) diskleri (Becton Dickinson, Sparks, MD, ABD) yerlestirilirken, digerine vankomisin Etest[R] (bioMerieux, Marcy l'Etoile, Fransa) seridi konularak plaklar 35[degrees]C'de bir gece inkubasyona birakilmistir.
Keywords: Coagulase negative Staphylococcus (CNS), Methicillin resistant S.hemolyticus (MRSH), Linezolid (LNZ) resistant, intensive care unit (ICU), Sepsis.
aureus isolates showed the highest resistance rate against penicillin (96%), while they were most sensitive to linezolid (95%), followed by clindamycin (94%), trimethoprim-sulfamethoxazole (89%), and erythromycin and ciprofloxacin (76% each).
The Infectious Diseases Society of America recommends vancomycin and linezolid as first-line drugs for the treatment of CA-MRSA infection.[5] In our case, vancomycin (1.0 g Q12 h) was initially used to treat the patient (weight, 60 kg) for 12 days.
Linezolid (LZD) was approved in 2000 for DR, gram-positive bacterial infections and also has shown good activity against Mycobacterium tuberculosis strains, including MDR-TB and XDR-TB strains, both in vitro and in animal studies (5, 6).
Results for antimicrobial resistance in major bacterial isolates revealed; In Pseudomonas resistance to Cephalosporins, polymxins, amino-glycosides, quinolones, penicillin and tetracycline was 66.7%, 55.6%, 55.6%, 66.7%, 66.7% and 88.9% respectively, while 100% strains were resistant to glycyclines, linezolid, vancomycin, macrolides and lincosamide.
Daptomycin, linezolid, and vancomycin are commonly used antibiotics for these indications (daptomycin is indicated for ABSSSI but not indicated for nosocomial pneumonia); however, increased selective pressure to these antibiotics has resulted in outbreaks of bacterial resistance to these antibiotics.
Linezolid has been shown to have promise in the treatment of nocardiosis even as monotherapy [7, 8].
The following antibiotics like penicillin, cloxacillin, erythromycin, azithromycin, amikacin, gentamicin, ciprofloxacin, gatifloxacin, tetracycline, cephalexin, cefuroxime, cefoperazone, linezolid and combination drug like piperacillin + tazobactam were used and the diameter of zone of inhibition was measured with the help of special scale provided by Hi-Media, Mumbai, India.
Similarly, linezolid is an effective drug for treating XDR TB, but side effects such as neurotoxicity and hematologic toxicity frequently occur (6).