Linezolid

Mechanism :

Linezolid is a synthetic antibacterial agent of the oxazolidinone class of antibiotics. It has in vitro activity against aerobic Gram-positive bacteria, certain Gram-negative bacteria and anaerobic microorganisms. It selectively inhibits bacterial protein synthesis through binding to sites on the bacterial ribosome and prevents the formation of a functional 70S-initiation complex. Specifically, linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process. The results of time-kill studies have shown linezolid to be bacteriostatic against enterococci and staphylococci. For streptococci, linezolid was found to be bactericidal for the majority of strains. Linezolid is also a reversible, nonselective inhibitor of monoamine oxidase. Therefore, linezolid has the potential for interaction with adrenergic and serotonergic agents.

Indication :

• Vancomycin-resistant Enterococcus faecium (VRE)
• VRSA infections
• Multidrug resistant tuberculosis (MDR TB)

Contraindications :

Hypersensitivity to drug/class/component, Avoid high tyramine-content foods.

Caution if myelosuppression, thrombocytopenia, uncontrolled HTN, pheochromocytoma, carcinoid syndrome, thyrotoxicosis, PKU (phenylalanine-containing forms), severe hepatic impairment or renal impairment, seizure history or seizure risk, use >28 days, Colitis history.

Dosing :

Adverse Effect :

Common Reactions: Diarrhea, vomiting, headache, nausea, anemia, thrombocytopenia, rash, hypertension, pseudomembranous colitis.

Severe Reactions: superinfection, Clostridium difficile associated diarrhea, anemia,

leukopenia, pancytopenia, thrombocytopenia, lactic acidosis, peripheral neuropathy, optic neuropathy, vision loss, serotonin syndrome, anaphylaxis Stevens-Johnson syndrome, seizures.

Interaction :

Contraindicated:
Amitriptyline, Amoxapine, BCG live intravesical, Bupropion, Buspirone, Citalopram, Clomipramine, Desipramine, Desvenlafaxine, Doxepin, Duloxetine, Escitalopram, Fluoxetine, Fluvoxamine, Imipramine, Isocarboxazid, Levomilnacipran, Milnacipran, Mirtazapine, Nefazodone, Nortriptyline, Paroxetine, Phenelzine, Procarbazine, Protriptyline, Selegiline Transdermal, Sertraline, Tetrabenazine, Tranylcypromine, Trazodone, Trimipramine, Venlafaxine, Vilazodone, Vortioxetine.
Avoid/Use Alternative:
Albuterol, Albuterol inhaled, Alfentanil, Amphetamine, Apraclonidine ophthalmic, Arformoterol inhaled, Atomoxetine, Benzphetamine, Brimonidine ophthalmic, Caffeine, Carbamazepine, Clonidine, Cocaine topical, Cyclobenzaprine, Dexmethylphenidate, Dextroamphetamine, Dextromethorphan, Diethylpropion, Dobutamine, Dopamine, Entacapone, Ephedra, Ephedrine, Epinephrine, Epinephrine inhaled, Ethanol, Fentanyl, Formoterol inhaled, Green Tea, Guanabenz, Guanfacine, Guarana, Indacaterol inhaled, Isometheptene, Isoproterenol, Levalbuterol inhaled, Levodopa, Lisdexamfetamine, Lorcaserin, Maprotiline, Meperidine, Metaproterenol, Methadone, Methamphetamine, Methyldopa, Methylene Blue, Methylphenidate, Metoclopramide, Naphazoline ophthalmic, Norepinephrine, Oxcarbazepine, Oxymetazoline nasal, Oxymetazoline ophthalmic, Pamabrom, Phendimetrazine, Phentermine, Phenylephrine, Phenylephrine Injection, Phenylephrine Nasal, Phenylephrine Ophthalmic, Phenylephrine Rectal, Pirbuterol inhaled, Pseudoephedrine, Remifentanil, Reserpine, Rizatriptan, Salmeterol inhaled, Sibutramine, St. John's Wort, Sufentanil, Sumatriptan, Tapentadol, Terbutaline, Tetrahydrozoline ophthalmic, Tolcapone, Tramadol, Typhoid vaccine Live, Yohimbe, Yohimbine, Zolmitriptan.

Renal Dose :

Hepatic Dose :