Linezolid Macrolides
Macrolide
The macrolides are a class of natural products that consist of a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered. Macrolides belong to the polyketide class of natu…
Full Answer
What are the uses of linezolid?
Linezolid is used to treat different types of bacterial infections, such as pneumonia, skin infections, and infections that are resistant to other antibiotics. Linezolid may also be used for purposes not listed in this medication guide.
Is there a generic version of linezolid?
Linezolid is available as a generic medication. The main use of linezolid is the treatment of severe infections caused by aerobic Gram-positive bacteria that are resistant to other antibiotics; it should not be used against bacteria that are sensitive to drugs with a narrower spectrum of activity, such as penicillins and cephalosporins.
What is the PMID for linezolid (linezolid)?
PMID 19072714. ^ a b c Ament PW, Jamshed N, Horne JP (February 2002). "Linezolid: its role in the treatment of gram-positive, drug-resistant bacterial infections". American Family Physician. 65 (4): 663–70. ISSN 0002-838X. PMID 11871684. Archived from the original on 24 July 2008. ^ Buck ML (June 2003).
What is the mortality and morbidity associated with linezolid?
When data from all participants were pooled, the study found that 21.5% of those given linezolid died, compared to 16% of those not receiving it. The difference was found to be due to the inferiority of linezolid in the treatment of Gram-negative infections alone or mixed Gram-negative/Gram-positive infections.
What class of antibiotic is linezolid?
Linezolid is used to treat infections, including pneumonia, and infections of the skin . Linezolid is in a class of antibacterials called oxazolidinones. It works by stopping the growth of bacteria.
What are some common macrolides?
Macrolides are a class of antibiotic that includes erythromycin, roxithromycin, azithromycin and clarithromycin. They are useful in treating respiratory, skin, soft tissue, sexually transmitted, H.
Is azithromycin a linezolid?
Azithromycin+Linezolid is used in the treatment of bacterial infections. Azithromycin + Linezolid is a combination of two antibiotics: Azithromycin and Linezolid. It works by preventing synthesis of essential proteins required by bacteria to carry out vital functions.
What bacteria is sensitive to linezolid?
Several Gram-positive and Gram-negative anaerobic bacteria are susceptible to linezolid, including many strains of Clostridium difficile,14,15 Fusobacterium spp.,16 Prevotella spp.,17 and Bacteroides spp. Linezolid is active against some strains of Actinomyces spp.
Which antibiotics are macrolides?
Five macrolide antibiotics are currently available for use in the United States: erythromycin, clarithromycin, azithromycin, fidaxomicin and telithromycin, the latter being a related ketolide.
Who should not take macrolides?
Macrolides are contraindicated in patients who have had an allergic reaction to them.
Who should not take linezolid?
You should not use this medicine if you or your child have used an MAO inhibitor (MAOI), including isocarboxazid, phenelzine, Eldepryl®, Marplan®, Nardil®, or Parnate® within the past 14 days.
What drugs should not be taken with linezolid?
Before using linezolid, report the use of drugs that may increase the risk of extremely high blood pressure (hypertensive crisis) when combined with linezolid, including herbal products (such as ephedra/ma huang), allergy and cold products (including decongestants such as phenylephrine/pseudoephedrine), and stimulants ...
Is linezolid a broad spectrum antibiotic?
Linezolid, the first oxazolidinone to be approved for the clinical treatment of Gram-positive bacterial infections, displays a wide spectrum of in vitro activity against many important pathogens, including for instance methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci and penicillin- ...
Why is linezolid not good for bacteremia?
Although linezolid is an option for S. aureus bacteremia, it is not FDA approved and is often not the preferred agent due to its bacteriostatic activity and large volume of distribution.
What should I monitor while on linezolid?
Monitoring parameters include heart rate, blood pressure, blood glucose, weekly complete blood count (CBC), and visual function. Blood pressure requires close monitoring in patients with untreated hyperthyroidism.
Is linezolid the same as vancomycin?
The results of this study demonstrate that linezolid therapy is well tolerated, equivalent to vancomycin in treating CSSTIs, and superior to vancomycin in the treatment of CSSTIs due to MRSA. Skin and soft tissue infections (SSTIs) are a common cause of morbidity in both the community and the hospital.
Is doxycycline a macrolide?
Doxycycline and azithromycin are different types of antibiotics. Doxycycline is a tetracycline antibiotic and azithromycin is a macrolide antibiotic.
Is amoxicillin a macrolide?
Both medications are used to treat bacterial infections in adults and children. Azithromycin is in the macrolide category of antibiotics, while amoxicillin is in the beta-lactam/penicillin category.
Is clindamycin a macrolides?
Clindamycin is a macrolide antibiotic, which, when used as an antiprotozoan agent, is always combined with other therapies for the treatment of falciparum malaria, toxoplasmosis, and babesiosis.
Is ciprofloxacin a macrolide?
Zithromax Z-PAK (azithromycin) and Cipro (ciprofloxacin) are antibiotics used to treat susceptible bacterial infections. Zithromax and Cipro belong to different antibiotic classes. Zithromax is a macrolide antibiotic and Cipro is a quinolone antibiotic.
What is the role of Linezolid in bacterial synthesis?
It acts as an inhibitor of bacterial protein synthesis by blocking the formation of the 70S ribosomal initiation complex.
Is linezolid bacteriostatic or bactericidal?
Its activity is bacteriostatic against some species (e.g., enterococci) and bactericidal against others (e.g., pneumococci). The antibacterial spectrum of linezolid includes Gram-positive pathogens and some Gram-negative anaerobic species but not Gram-negative aerobes.
Is linezolid a weak MAO inhibitor?
Linezolid is a weak and reversible monoamine oxidase (MAO) inhibitor and although no increased frequency of adrenergic or serotonergic adverse events has been reported, it is recommended that linezolid is used with caution in patients treated with other MAO inhibitors.
What is the MIC of Linezolid?
Linezolid use may result in a suboptimal clinical response when treating organisms with a MIC (minimum inhibitory concentration ) of 4 mcg/ml or greater and warrants a complete ID re-assessment and change in drug therapy.
How long to infuse linezolid?
Administer linezolid IV infusion over 30 to 120 minutes. Do not mix or infuse with other medications. When using the same IV line for sequential infusion, flush the line with D5W, normal saline, or lactated Ringer's solution before and after infusing linezolid. The yellow color of the injection may intensify with time without affecting potency.
What is the first available oxazolidinone to inhibit bacterial protein synthesis by interfering with?
Linezolid is the first available oxazolidinone to inhibit bacterial protein synthesis by interfering with translation. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit, which prevents the formation of a functional 70S initiation complex.[4] This activity essentially inhibits protein production and prevents bacteria from multiplying.
How long after MAO inhibitors can you take phenelzine?
Do not use within two weeks of MAO inhibitors, e.g., phenelzine.
Does Linezolid work against MRSA?
Linezolid has activity against a broad range of antimicrobial susceptible and resistant gram-positive bacteria, including activity against MRSA with intermediate resistance to glycopeptides like vancomycin.
Is Linezolid a substitute for vancomycin?
Linezolid’s primary place in therapy is an alternative to vancomycin in inpatient settings. Vancomycin remains a standard treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection. However, vancomycin- resistant isolates of S. aureus have emerged, and there are increasing reports of vancomycin-resistant isolates worldwide. Alternative treatment agents merit consideration before using linezolid in outpatient settings, as inappropriate use has led to an increase in linezolid-resistant vancomycin-resistant enterococci. [1]
Is Linezolid an antibiotic?
Linezolid is a synthetic oxazolidinone antimicrobial drug. It is indicated for gram-positive infections and approved for the treatment of bacterial pneumonia, skin and skin structure infections, and VRE infections, including infections complicated by bacteremia. Linezolid does not have approval for the treatment of gram-negative infections, catheter-related bloodstream infections, or catheter site infections.
What is linezolid?
Linezolid is an antibiotic that fights bacteria in the body. Linezolid is also an MAO (monoamine oxidase) inhibitor.
How to take Linezolid?
Linezolid tablets or liquid can be taken with or without food. Gently mix the oral suspension (liquid) by turning the bottle upside down 3 to 5 times. Do not shake. Measure a dose with the supplied syringe or a dose-measuring device (not a kitchen spoon). Linezolid injection is given in a vein.
What should I avoid while using linezolid?
Avoid taking anti-diarrhea medicine without first asking your doctor. Diarrhea may be a sign of a new infection.
What other drugs will affect linezolid?
Tell your doctor about all other medicines you use. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here.
What is MAO inhibitor?
MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, tranylcypromine, and others. Tell your doctor if you also take stimulant medicine, opioid medicine, herbal products, or medicine for depression, mental illness, Parkinson's disease, migraine headaches, serious infections, or prevention of nausea and vomiting.
Where is Linezolid given?
Linezolid injection is given in a vein.
Can linezolid cause serotonin?
An interaction with linezolid could cause a serious condition called serotonin syndrome. Tell your doctor if you have ever had: high blood pressure; a thyroid disorder; a carcinoid tumor; bone marrow suppression or a weak immune system; kidney or liver disease; pheochromocytoma (adrenal gland tumor); diabetes;
What is macrolide antibiotic?
The macrolide antibiotics erythromycin, clarithromycin, and roxithromycin have proven to be an effective long-term treatment for the idiopathic , Asian-prevalent lung disease diffuse panbronchiolitis (DPB).
What is macrolide used for?
Antibiotic macrolides are used to treat infections caused by Gram-positive bacteria (e. g., Streptococcus pneumoniae) and limited Gram-negative bacteria (e.g., Bordetella pertussis, Haemophilus influenzae ), and some respiratory tract and soft-tissue infections. The antimicrobial spectrum of macrolides is slightly wider than that of penicillin, and, therefore, macrolides are a common substitute for patients with a penicillin allergy. Beta-hemolytic streptococci, pneumococci, staphylococci, and enterococci are usually susceptible to macrolides. Unlike penicillin, macrolides have been shown to be effective against Legionella pneumophila, mycoplasma, mycobacteria, some rickettsia, and chlamydia .
What is the name of the ring in erythromycin?
Erythromycin. The macrolide ring is the lactone (cyclic ester) at upper left. The macrolides are a class of natural products that consist of a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered.
How does bacterial resistance to macrolides occur?
The primary means of bacterial resistance to macrolides occurs by post-transcriptional methylation of the 23S bacterial ribosomal RNA. This acquired resistance can be either plasmid -mediated or chromosomal, i.e., through mutation, and results in cross-resistance to macrolides, lincosamides, and streptogramins (an MLS-resistant phenotype).
How old can a horse be to take macrolide?
It can be used in horses less than one year old, but care must be taken that other horses (such as a foal's mother) do not come in contact with the macrolide treatment. Macrolides can be administered in a variety of ways that include tablets, capsules, suspensions, injectings and topically.
When was the first macrolide discovered?
The first macrolide discovered was erythromycin, which was first used in 1952 . Erythromycin was widely used as a substitute to penicillin in cases where patients were allergic to penicillin or had penicillin-resistant illnesses. Later macrolides developed, including azithromycin and clarithromycin, stemmed from chemically modifying erythromycin;
What is the mechanism of action of macrolides?
The mechanism of action of macrolides is inhibition of bacterial protein biosynthesis, and they are thought to do this by preventing peptidyltransferase from adding the growing peptide attached to tRNA to the next amino acid (similarly to chloramphenicol) as well as inhibi ting bacterial ribosomal translation.
