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Brand Name :
Zyvox
Synonyms :
linezolid
Class :
Oxazolidinones
Brand Name :
Zyvox
Synonyms :
linezolid
Class :
Oxazolidinones
Dosage Forms & Strengths Â
Solution Â
2mg/mLÂ Â
Suspension Â
100mg/5mL Â
Tablet  Â
600mg Â
Indicated for Tuberculosis drug-resistant :
600
mg
Orally or IV
daily
as part of an appropriate combination regimen including pyridoxine; reduction in dose 300-450 mg once daily or 600 mg for patients who develop toxicity, 3-4 times per week may be used.
600 mg oral/IV 2 times daily 10-14 days
Dosage Forms & Strengths Â
Solution Â
2mg/mLÂ Â
Suspension Â
100mg/5mL Â
Tablet  Â
600mg Â
Indicated for Tuberculosis drug-resistant :
600 mg Oral/IV daily as part of an appropriate combination regimen including pyridoxine; reduction in dose to 300 to 450 mg once daily or 600 mg for patients who develop toxicity, 3 to 4 times per week may be used.
600 mg oral/IV 2 times daily 10-14 days
Refer to adult dosingÂ
may increase the hypertension effect
may increase the hypertension effect
may increase the hypertension effect
may increase the hypertension effect
may increase the hypertension effect
It may enhance the effects when combined with epinephrine by pharmacodynamic synergism
It may increase the hypertensive effect when combined with Sympathomimetics
It may increase the hypertensive effect when combined with Sympathomimetics
linezolid: they may increase the CNS depressant effect of CNS Depressants
linezolid: they may increase the CNS depressant effect of CNS Depressants
linezolid: they may increase the CNS depressant effect of CNS Depressants
linezolid: they may increase the CNS depressant effect of CNS Depressants
linezolid: they may increase the CNS depressant effect of CNS Depressants
linezolid: they may increase the hypertensive effect of Alpha2-Agonists
linezolid: they may increase the hypertensive effect of Alpha2-Agonists
linezolid: they may increase the hypertensive effect of Alpha2-Agonists
linezolid: they may increase the hypertensive effect of Alpha2-Agonists
linezolid: they may increase the hypertensive effect of Alpha2-Agonists
may increase the hypertension effect of sympathomimetic drugs
may increase the hypertensive effects of sympathomimetics
may increase the antihypertensive effect of sympathomimetics
may increase the hypertensive effect of sympathomimetics
the effects of caffeine may be enhanced with linezolid such as risk of hypertension
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
May have an increased serotonergic effect when combined with Serotonin/Norepinephrine Reuptake Inhibitors
may have an increased serotonergic effect when combined with linezolid
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the toxicity of SSRIs
it increases the toxicity of SSRIs
it increases the toxicity of SSRIs
it increases the toxicity of SSRIs
it increases the toxicity of SSRIs
Could potentially amplify the serotonergic effect of l-tryptophan
it increases the toxicity of diphenoxylate through an unknown mechanism
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of SSRIs
it increases the effect of Norepinephrine Reuptake Inhibitors
it increases the effect of SSRIs
it increases the effect of Norepinephrine Reuptake Inhibitors
linezolid may enhance the serotonergic effect of MAO inhibitors
linezolid may enhance the serotonergic effect of MAO inhibitors
linezolid may enhance the serotonergic effect of MAO inhibitors
linezolid may enhance the serotonergic effect of MAO inhibitors
linezolid may enhance the serotonergic effect of MAO inhibitors
linezolid may enhance the serotonergic effect of tricyclic antidepressants
when both drugs are combined, there may be an increased risk or severity of adverse effects  
It may enhance the risk of adverse effects when combined with oxazolidinones
It may enhance the risk of adverse effects when combined with oxazolidinones
It may enhance the risk of adverse effects when combined with oxazolidinones
It may enhance the risk of adverse effects when combined with oxazolidinones
It may enhance the risk of adverse effects when combined with oxazolidinones
may have a decrease in excretion when combined with linezolid
Actions and Spectrum:Â
Linezolid is an antibiotic that is effective against a wide range of gram-positive bacteria. It works by inhibiting the synthesis of proteins in bacterial cells, disrupting their ability to grow and multiply.Â
The specific actions of linezolid include inhibiting the formation of the bacterial ribosome, which is necessary for the synthesis of proteins. It also inhibits the initiation of protein synthesis by binding to the bacterial ribosome and blocking the transfer of amino acids from tRNA to the growing peptide chain.Â
The spectrum of linezolid includes a wide range of gram-positive bacteria, including staphylococci, streptococci, and enterococci. It is commonly used to treat infections caused by these bacteria, including pneumonia, skin and soft tissue infections, and infections in the bone and joint.Â
Frequency Defined Â
>10% Â
Diarrhea  Â
1-10% Â
Nausea (5.1-6.6%) Â
Headache (5.7-8.8%) Â
Abnormal LFTs (0.4-1.6%) Â
Rash (1.1-2.3%) Â
Diarrhea (8.2-8.3%) Â
Oral moniliasis (0.5-1.7%) Â
Fungal infection (0.3-1.5%) Â
Vaginal moniliasis (1.1-1.8%) Â
Vomiting (2-4.3%) Â
Localized abdominal pain (1.2-1.3%) Â
Dizziness (1.8-2.6%) Â
Taste alteration (1-1.8%) Â
 Â
Contraindication/Caution:
There are several contraindications and cautions for the use of linezolid:Â
 Â
Pregnancy warnings:    Â
AU TGA pregnancy category: B3
US FDA pregnancy category: C
Lactation:  Â
Excreted into human milk is known Â
Pregnancy Categories:        Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    Â
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    Â
Category N: There is no data available for the drug under this categoryÂ
Pharmacology:
Linezolid inhibits the synthesis of proteins in bacterial cells by inhibiting a specific enzyme called ribosomal RNA synthase. This disrupts the ability of bacteria to grow and multiply, leading to their death. Â
Pharmacodynamics:Â
The pharmacodynamics of linezolid are complex and involve several mechanisms of action. Linezolid binds to a specific site on the bacterial ribosome, which is the cellular structure responsible for synthesizing proteins. This binding prevents the ribosome from adding amino acids to the growing protein chain, effectively inhibiting protein synthesis. Linezolid has a bacteriostatic effect, meaning it stops the growth of bacteria rather than killing them outright. However, it can also have a bactericidal effect, meaning it can kill bacteria, especially at higher concentrations or when used in combination with other antibiotics.Â
Linezolid has a broad spectrum of activity and is effective against a wide range of gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). It is also active against some gram-negative bacteria, although its activity against these bacteria is generally less potent. Linezolid has a long half-life, meaning it remains in the body for a long time after it is taken. It is generally well-tolerated and has a low potential for causing adverse effects. However, long-term use of linezolid can lead to the development of resistance in some bacteria. To minimize the risk of resistance, it is important to use linezolid only when it is necessary and to follow the recommended dosing and treatment duration.Â
Pharmacokinetics: Â
Linezolid is a synthetic antibiotic that is administered orally or intravenously.Â
Absorption Â
It is well absorbed after oral administration, with bioavailability ranging from 85-100%. Â
Distribution Â
It has a volume of distribution of approximately 58 L/kg and is highly protein bound (99%).Â
Metabolism Â
Linezolid is metabolized in the liver by the cytochrome P450 (CYP) enzyme system, with the majority being metabolized by CYP3A4. Â
Elimination and excretionÂ
It has a half-life of approximately 5 hours. It is excreted primarily through the urine, with approximately 80% being excreted unchanged.Â
Linezolid has a linear pharmacokinetic profile, meaning that the concentration of the drug in the body is proportional to the dose administered. It has a steady-state concentration after multiple doses, and its pharmacokinetics are not affected by age, gender, or liver or kidney function. However, the pharmacokinetics of linezolid may be altered in patients with renal impairment, requiring dose adjustments.Â
Administration:
linezolid is typically administered as an IV infusion over a period of 30-120 minutes. Â
It is supplied as a single-use, ready-to-use infusion bag that should be inspected for particulate matter and leaks before use. The reconstituted suspension should be used within 21 days.Â
When preparing to administer linezolid, it is important to consider its compatibility with other medications. linezolid may be incompatible with certain drugs when added together in the same IV infusion. For example, it may be incompatible with kanamycin, phenytoin, ceftriaxone, and erythromycin lactobionate when added as an additive, and with ampicillin when mixed in the same syringe. When administered through the same Y-site as other medications, linezolid may be incompatible with drugs such as amphotericin B, chlorpromazine, diazepam, pentamidine, and phenytoin.Â
linezolid should be stored at a temperature of 25°C (77°F) and protected from light. The infusion bags should be kept in overwrap until ready to use and protected from freezing.Â
It is important to follow the specific guidelines for the administration, compatibility, and storage of linezolid as directed by a healthcare provider or pharmacist.Â
Â
Patient information leafletÂ
Generic Name: linezolid Â
Why do we use linezolid?Â
linezolid is an antibiotic that is used to treat bacterial infections, particularly infections caused by Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pneumoniae. It is often used to treat infections that are resistant to other antibiotics, including methicillin-resistant Staphylococcus aureus (MRSA).Â
linezolid works by inhibiting the production of proteins in bacteria, which is essential for their growth and survival. By inhibiting protein synthesis, linezolid can kill the bacteria and clear the infection.Â
linezolid is typically used in the treatment of serious bacterial infections, including skin infections, pneumonia, and infections of the bone and joints. It is also sometimes used in the treatment of tuberculosis (TB), particularly in cases of multidrug-resistant TB (MDR-TB).Â
In TB treatment, linezolid is often used in combination with other TB medications, such as bedaquiline and pretomanid, as part of a treatment regimen called the BPaL regimen. This combination has been shown to be effective in the treatment of MDR-TB, though it is important to be aware of the potential side effects and adverse reactions associated with the use of linezolid, including myelosuppression, peripheral and optic neuropathy, and lactic acidosis.Â
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