Linser

Linser Uses, Dosage, Side Effects, Food Interaction and all others data.

Linser is a synthetic, antibacterial agent belonging to a new class of antibiotics, the oxazolidinones, with in vitro activity against Gram positive aerobic bacteria, some Gram positive anaerobic bacteria and certain Gram negative bacteria. It selectively inhibits bacterial protein synthesis via a mechanism of action different from that of other antibacterial agents. Linser binds to the 23S ribosomal RNA of the 50S subunit of the bacterial ribosome 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 Linser to be bacteriostatic against enterococci and staphylococci. For streptococci, Linser was found to be bactericidal for the majority of strains.

Linser is an oxazolidinone antibacterial agent effective against most strains of aerobic Gram-positive bacteria and mycobacteria. It appears to be bacteriostatic against both staphylococci and enterococci and bactericidal against most isolates of streptococci. Linser has shown some in vitro activity against Gram-negative and anaerobic bacteria but is not considered efficacious against these organisms.

Linser is a reversible and non-selective inhibitor of monoamine oxidase (MAO) enzymes and can therefore contribute to the development of serotonin syndrome when administered alongside serotonergic agents such as selective serotonin re-uptake inhibitors (SSRIs) or tricyclic antidepressants (TCAs). Linser should not be used for the treatment of catheter-related bloodstream infections or catheter-site infections, as the risk of therapy appears to outweigh its benefits under these circumstances.

Trade Name Linser
Availability Prescription only
Generic Linezolid
Linezolid Other Names Linezolid, Linezolide, Linezolidum
Related Drugs amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, Augmentin
Type Infusion, Tablet
Formula C16H20FN3O4
Weight Average: 337.3461
Monoisotopic: 337.143784348
Protein binding

Plasma protein binding of linezolid is approximately 31% - primarily to serum albumin - and is concentration-dependent.

Groups Approved, Investigational
Therapeutic Class Oxazolidinones
Manufacturer Serene Lifescience
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Linser
Linser

Uses

Vancomycin-Resistant Enterococcus faecium infections including cases with concurrent bacteremia.

Nosocomial pneumonia caused by Staphylococcus aureus (methicillin-susceptible and -resistant strains) or Streptococcus pneumoniae (including multi-drug resistant strains). Combination therapy may be clinically used if the documented or presumptive pathogens include Gram-negative organism.

Complicated skin and skin structure infections, including diabetic foot infections (without concomitant osteomyelitis) caused by Staphylococcus aureus (methicillin-susceptible and ¬resistant strains), Streptococcus pyogenes, or Streptococcus agalactiae.

Uncomplicated skin and skin structure infections caused by Staphylococcus aureus (methicillin-susceptible only) or Streptococcus pyogenes.

Community-acquired pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains) including cases with concurrent bacteremia, or Staphylococcus aureus (methicillin-susceptible strains only)

Linser is also used to associated treatment for these conditions: Community Acquired Pneumonia (CAP) caused by Staphylococcus Aureus Infections, Community acquired pneumonia caused by Susceptible strains of Streptococcus pneumoniae, Complicated Skin and Skin Structure Infection caused by Staphylococcus Aureus Infections, Complicated Skin and Skin Structure Infection caused by Streptococcus Agalactiae Infection, Complicated Skin and Skin Structure Infection caused by Streptococcus Pyogenes Infection, Nosocomial Pneumonia caused by Staphylococcus Aureus Infections, Nosocomial Pneumonia caused by Streptococcus Pneumoniae Infections, Uncomplicated Skin and Skin Structure Infections caused by Staphylococcus Aureus Infections, Uncomplicated Skin and Skin Structure Infections caused by Streptococcus Pyogenes Infection, Vancomycin-resistant Enterococcus faecium infection

How Linser works

Linser exerts its antibacterial effects by interfering with bacterial protein translation. It 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 essential for bacterial reproduction, thereby preventing bacteria from dividing.

Point mutations in the bacterial 23S rRNA can lead to linezolid resistance, and the development of linezolid-resistant Enterococcus faecium and Staphylococcus aureus have been documented during its clinical use. As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.

Dosage

Linser dosage

Patients who commence treatment on the parenteral formulation may be switched to either oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as Linser has an oral bioavailability of approximately 100%. The injection should be administered over a period of 30 to 120 minutes. The film coated tablets or oral suspension may be taken with or without food.Adults and Adolescents (12 Years and Older):

  • Complicated skin and skin structure infections & Community-acquired pneumonia, including concurrent bacteremia: 600 mg IV or oral b.i.d. for 10 to 14 days.
  • Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia: 600 mg IV or oral b.i.d. for 14-28

For Pediatric Patients (Birth through 11 Years of Age):

  • Complicated skin and skin structure infections & Community-acquired pneumonia, including concurrent bacteremia: 600 mg IV or oral b.i.d. for 10 to 14 days.
  • Vancomycin-resistant Enterococcus faecium infections, including concurrent bacteremia: 600 mg IV or oral b.i.d.for 14-28.

Neonates <7 days: Most pre-term neonates <7 days of age (gestational age <34 weeks) have lower systemic linezolid clearance values and larger AUC values than many full-term neonates and older infants. These neonates should be initiated with a dosing regimen of 10 mg/kg every 12 hours. Consideration may be given to the use of 10 mg/kg in every eight hours regimen in neonates with a sub-optimal clinical response. All neonatal patients should receive 10 mg/kg t.i.d. by 7 days of life.

Intravenous Administration: Linser IV Injection is supplied in single-use, ready-to-use infusion bags. Parenteral drug products should be inspected visually for particulate matter prior to administration. Minute leaks should be checked by firmly squeezing the bag. If leaks are detected, the solution should be discarded, as sterility may be impaired. Linser IV Injection should be administered by intravenous infusion over a period of 30 to 120 minutes. The intravenous infusion bag should not be used in series connections. Additives should not be introduced into this solution. The infusion bag should be stored at room temperature and protected from freezing. Linser IV Injection may exhibit a yellow color that can intensify over time without adversely affecting potency.

Patients who commence treatment on the parenteral formulation may be switched to either oral presentation when clinically indicated. In such circumstances, no dose adjustment is required as Linser has an oral bioavailability of approximately 100%.

The injection should be administered over a period of 30 to 120 minutes. The film coated tablets or oral suspension may be taken with or without food.

Reconstitution of Oral Suspension: Shake the bottle to loosen powder. Add 75 ml (with the help of given cup) of boiled & cooled water to the dry mixture in the bottle. For ease of preparation add water to the bottle in two portions. Shake well after each addition until all the powder is in suspension. Shake the suspension well before use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool & dry place. Use within 21 days after reconstitution.

Side Effects

Most of the adverse events reported with Linser were mild to moderate in intensity. The most common adverse events in patients treated with Linser were diarrhea, headache and nausea. Other adverse included oral moniliasis, vaginal moniliasis, hypertension, dyspepsia, localized abdominal pain, pruritus, and tongue discoloration.

Toxicity

Clinical signs of overdosage observed in rats were decreased activity and ataxia (2000 mg/kg/day) and in dogs were vomiting and tremors (3000 mg/kg/day). Treatment of overdose should involve symptomatic and supportive measures and may include hemodialysis if clinically necessary.

Precaution

Patients who develop recurrent nausea or vomiting, unexplained acidosis, or low bicarbonate level while receiving Linser should receive immediate medical evaluation. Where administration of Linser and concomitant serotonergic agents is clinically appropriate, patients should be closely observed for signs and symptoms of serotonin syndrome such as cognitive dysfunction, hyperpyrexia, hyper reflexia and incoordination. If signs or symptoms occur physicians should consider discontinuation of either one or both agents. If the concomitant serotonergic agent is withdrawn, discontinuation symptoms can be observed. If patients experience symptoms of visual impairment, such as changes in visual acuity, changes in color vision, blurred vision, or visual field defect, prompt ophthalmic evaluation is recommended. Convulsions have been reported in patients when treated with Linser. In some of these cases, a history of seizures or risk factors for seizures was reported.

Interaction

Monoamine Oxidase Inhibition: Linser is a reversible, nonselective inhibitor of monoamine oxidase. Therefore, Linser has the potential for interaction with adrenergic and serotonergic agents.

Adrenergic Agents: Some individuals receiving Linser may experience a reversible enhancement of the pressor response to indirect-acting sympathomimetic agents, vasopressor or dopaminergic agents. Initial doses of adrenergic agents, such as dopamine or epinephrine, should be reduced and titrated to achieve the desired response.

Serotonergic Agents: Physicians should be alert to the possible signs and symptoms of serotonergic syndrome in patients receiving concomitant Linser and serotonergic agents.

Food Interaction

  • Avoid tyramine-containing foods and supplements. Avoid food containing high amounts of tyramine (>100mg). Tyramine-containing foods include cheese, red wine, fava beans, pickled foods, cured foods, and alcoholic beverages.
  • Take with or without food. Co-administration with food does not significantly alter the pharmacokinetics of linezolid.

[Major] CONTRAINDICATED: Foods that contain large amounts of tyramine may precipitate a hypertensive crisis in patients treated with monoamine oxidase inhibitors (MAOIs).

The mechanism is inhibition of MAO-A, the enzyme responsible for metabolizing exogenous amines such as tyramine in the gut and preventing them from being absorbed intact.

Once absorbed, tyramine is metabolized to octopamine, a substance that is believed to displace norepinephrine from storage granules.



GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of MAOIs.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: In general, patients treated with MAOIs or other agents that possess MAOI activity (e.g., furazolidone, linezolid, procarbazine) should avoid consumption of products that contain large amounts of amines and protein foods in which aging or breakdown of protein is used to increase flavor.

These foods include cheese (particularly strong, aged or processed cheeses), sour cream, wine (particularly red wine), champagne, beer, pickled herring, anchovies, caviar, shrimp paste, liver (particularly chicken liver), dry sausage, salamis, figs, raisins, bananas, avocados, chocolate, soy sauce, bean curd, sauerkraut, yogurt, papaya products, meat tenderizers, fava bean pods, protein extracts, yeast extracts, and dietary supplements.

Caffeine may also precipitate hypertensive crisis so its intake should be minimized as well.

At least 14 days should elapse following discontinuation of MAOI therapy before these foods may be consumed.

Specially designed reference materials and dietary consultation are recommended so that an appropriate and safe diet can be planned.

Patients should be advised to promptly seek medical attention if they experience potential signs and symptoms of a hypertensive crisis such as severe headache, visual disturbances, difficulty thinking, stupor or coma, seizures, chest pain, unexplained nausea or vomiting, and stroke-like symptoms.

Patients should also be counseled not to use MAOIs with alcohol, and to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them.

Linser Hypertension interaction

[Moderate] Linser should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis and

Caution and close monitoring are recommended when prescribing this agent to these patients.

Volume of Distribution

At steady-state, the volume of distribution of linezolid in healthy adults is approximately 40-50 liters.

Elimination Route

Linser is extensively absorbed following oral administration and has an absolute bioavailability of approximately 100%. Maximum plasma concentrations are reached within approximately 1 to 2 hours after dosing (Tmax) and range from 8.1-12.9 mcg/mL after single doses and 11.0-21.2 mcg/mL after multiple dosing.

The absorption of orally administered linezolid is not significantly affected by co-administration with food and it may therefore be given without regard to the timing of meals.

Half Life

The elimination half-life is estimated to be between 5 and 7 hours.

Clearance

Total clearance of linezolid is estimated to be 100-200 mL/min, the majority of which appears to be non-renal. Mean renal clearance is approximately 40 mL/min, which suggests net tubular reabsorption, while non-renal clearance is estimated to account for roughly 65% of total clearance, or 70-150 mL/min on average. Variability in linezolid clearance is high, particularly for non-renal clearance.

Elimination Route

Urinary excretion is the primary means by which linezolid and its metabolic products are excreted. Following the administration of a radiolabeled dose of linezolid under steady-state conditions, approximately 84% of radioactivity was recovered in the urine, of which approximately 30% is unchanged parent drug, 40% is the hydroxyethyl glycine metabolite, and 10% is the aminoethoxyacetic acid metabolite. Fecal elimination is comparatively minor, with no parent drug observed in feces and only 6% and 3% of an administered dose found in the feces as the hydroxyethyl glycine metabolite and the aminoethoxyacetic acid metabolite, respectively.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Linser should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether Linser is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Linser is administered to a nursing woman.

Contraindication

Linser formulations are contraindicated for use in patients who have known hypersensitivity to Linser or any of the other product components. Linser should not be used in patients taking any medicinal product which inhibits monoamine oxidases A or B (e.g. phenelzine, isocarboxazid) or within two weeks of taking any such medicinal product. Linser should not be administered to patients with uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, carcinoid syndrome and/or patients taking directly and indirectly acting sympathomimetic agents (e.g. pseudoephedrine), vasopressive agents (e.g. epinephrine, norepinephrine), dopaminergic agents (e.g. dopamine, dobutamine), serotonin re-uptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists (triptans), meperidine or buspirone.

Acute Overdose

No cases of overdose have been reported. Symptomatic and supportive care is advised together with maintenance of glomerular filtration. Approximately 30% of a Linser dose is removed during 3 hours of haemodialysis. No data are available for the removal of Linser by peritoneal dialysis or haemoperfusion.

Storage Condition

Should be stored at room temperature 25° C, away from light and moisture.

Innovators Monograph

You find simplified version here Linser

Linser contains Linezolid see full prescribing information from innovator Linser Monograph, Linser MSDS, Linser FDA label

FAQ

What is Linser used for?

Linser is used to treat different types of bacterial infections, such as pneumonia, skin infections, and infections that are resistant to other antibiotics.

How safe is Linser?

When given for short periods Linser is a relatively safe antibiotic. It can be used in people of all ages and in people with liver disease or poor kidney function.

How does Linser work?

Linser disrupts bacterial growth by inhibiting the initiation process of protein synthesis a mechanism of action that is unique to this class of drugs.

What are the common side effects of Linser?

Common side effects of Linser are include:

  • diarrhea
  • vomiting
  • headache
  • red blood cell deficiency
  • low blood platelet count
  • nausea
  • abdominal pain
  • loose stools
  • increased white blood cells
  • itching, other than application site
  • spinning sensation

Is Linser safe during pregnancy?

Linser should be used during pregnancy only if clearly needed and the benefit outweighs the risk to the fetus.

Is Linser safe during breastfeeding?

Linser is excreted into breastmilk in concentration likely to be effective against staphylococcal strains found in mastitis.

Can I drink alcohol with Linser?

You should avoid the use of alcohol while being treated with Linser, as alcohol may increase some of the nervous system side effects such as dizziness, drowsiness, and difficulty concentrating.

Can I drive after taking Linser?

Linser may make you feel dizzy or experience problems with your vision. If this happens, do not drive or operate any machinery. Remember that if you are unwell your ability to drive or operate machinery may be affected.

How should Linser be taken?

Linser is usually taken with or without food twice a day (every 12 hours) for 10 to 28 days.

How long does Linser stay in my system?

The elimination half-life of Linser is 5-7 hours, and twice-daily administration of 400-600 mg provides steady-state concentrations in the therapeutic range. 

Is Linser hard on the kidneys?

Linser elimination is not affected by renal function, and no dosage adjustment is warranted for patients with renal impairment.

Does Linser affect blood pressure?

When taken with certain foods or drinks,Linser can cause an increase in blood pressure.

How long can I be on Linser?

The Linser safety population included 24 patients receiving Linser for a median of 80.5 days.

Can Linser cause anemia?

Linser has been associated with anemia and thrombocytopenia.

Is Linser toxic?

Linser toxicity is associated with significant morbidity and mortality.

Can Linser be taken empty stomach?

Take Linser by mouth with a glass of water. Follow the directions on the prescription label. Take with food or on an empty stomach.

Who should not take Linser?

Do not take Linser if you are allergic to Linser or any ingredients contained in this drug.Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Can you stop taking Linser?

Do not stop taking Linser without talking to your doctor. If you stop taking Linser too soon or if you skip doses, your infection may not be completely treated and the bacteria may become resistant to antibiotics.

What happens if I miss a dose?

Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention.If linezolid is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

*** Taking medicines without doctor's advice can cause long-term problems.
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