Forlen Davipharm medicine for infection (2 blisters x 10 tablets)

Dosage form Box of 2 blisters x 10 tablets
Specifications Linezolid

Ingredient

Composition informationContent
Linezolid600mg

Uses

Indications

Linezolid is indicated that the following infections are indicated that including cases of suspected or defined blood infections or anaerobic bacteria or anaerobic bacteria (+) sensitive.

Clinical coordination treatment can be indicated in the case of pathogenic bacteria including Gram (-) bacteria strains.

Linezolid only works on Gram (+) bacteria. Linezolid has no activity on the strains of bacteria that cause gram disease (-). It is necessary to use a specific effect on Gram (-) bacteria in the case of identified or suspected infection with Gram (-) bacteria.

Hospital pneumonia.

Pneumonia is suffering from the community.

Skin and soft tissue infections.

Infections caused by Enterococcus including infections caused by Enterococcus Faecium and Faecalis resistant Vancomycin.

Pharmacokology

General characteristics

Linezolid is a synthetic antibiotic of the new antibiotic group Oxazolidinon.

In vitro, the drug works on Gram (+) aerobic bacteria, some gram (-) bacteria and anaerobic bacteria. Linezolid selectively inhibits bacterial protein synthesis process according to a special mechanism. Specifically, the drug is attached to a position on the ribosom of bacteria (23s of the subunit of 50s) and prevents the formation of a 70S starting complex that is an important component in the code of code.

Sensitivity

Only bacteria related to clinical indications are presented below:

Classification coagulase
streptococcus agalactiae*
streptococcus pneumoniae*
streptococcus pyogenes*
streptococci group C
streptococci group g Anaerobius
peptostreptococcus resistant bacteria:
haemophilus influenzae
moraxella catarrhalis
Neisseria species
enteracteriaceaeee
species species
species species species species species species species species species species Pseudomonas

* Clinical efficiency has been proven in sensitive bacterial strains related to the approved clinical indications.

pharmacokinetic

absorption

Linezolid is absorbed quickly and completely after drinking. The maximum plasma concentration is achieved within 2 hours after taking the drug. The absolute oral bioavailability of Linezolid (oral and intravenous use in double diagonal research) is completely (about 100%). The absorption of the drug does not affect the food and absorption of the same drink when using a film tablet.

Linezolid's cmax and cmin value in the plasma (average and [standard deviation]) in a stable state after intravenous injection of 600mg, 2 times/day have been defined by 15.1 [2.5] mg/l and 3.68 [2.68]).

In another study when orally orally, 600mg, 2 times/day, cmax and cmin of the drug in a stable state are determined, respectively, 21.2 [5.8] mg/l and 6.15 [2.94] mg/l.

Stable state of the drug is achieved on Monday after taking the drug.

Distribution

The volume of distribution is in an average stable state of about 40 - 50L in healthy adults, approximately the total volume of water in the body. About 31% of drugs are associated with plasma proteins. This link ratio does not depend on concentration.

Linezolid concentration is determined in many different biological translations on a small number of volunteers in studies after repeated dose. The ratio of linezolid in saliva and sweat compared to the corresponding plasma is 1.2/1.0 and 0.55/1.0. The linezolid ratio in the epithelium and alveolar cells compared to the corresponding plasma is 4.5/1.0 and 0.15/1.0, measured at the time of determining CMAX in plasma in a stable state.

The pharmacokinetic information on children's ventricular drainage - abdominal cavity shows the oscillation of the linezolid concentration in the cerebrospinal fluid after using a single dose or a repeated dose. The concentration of irregular treatment is achieved or maintained stably in the cerebrospinal fluid. Therefore, it is not recommended to use Linezolid according to experience in cases of central nervous system infections in children.

Metabolism

Linezolid is metabolized mainly through the oxidation of the morpholin ring to form two conductive carboxylic acid derivatives that open the main ring without active as amino acid acid acid (PNU-142300) and hydroxyethyl glycin (PNU-142586).

Hydroxyethyl glycin metabolites (PNU-142586) are the main metabolites in the body and are said to form no participation of enzymes. Etho acetic amino acid metabolites (PNU-142300) are formed less. Some other non -active auxiliary changes have also been determined.

Elimination

In patients with normal kidney function or mild to moderate renal failure, Linezolid is excreted mainly through urine in a stable state in the form of PNU-142586 (40%), intact form (30%) and PNU-142300 (10%). The intact drugs are almost not found in the feces while about 6% and 3% of the dose corresponding to the PNU-142586 and PNU-142300 formats are detected in the feces. The average selling time of Linezolid is about 5 - 7 hours.

Linezolid's outer clearance accounts for about 65% of total clearance. A non -linear part of the clearance appears when increasing the linezolid dose. This may be because at higher concentrations, the lines of the kidney and the kidneys of the linezolid are lower. However, the difference in clearance is small and does not change the sale time.

Special patient population

Patients with renal failure

After using a single dose of 600mg, the concentration of two main metabolites in plasma increased by 7-8 times in patients with severe renal impairment (creatinine clearance

However, the area under the AUC curve of the intact drug does not increase. Although a small amount of the main metabolites of Linezolid is eliminated through dialysis, the concentration of the metabolites in plasma after the single dose of 600mg is still significantly higher than the observed concentration on normal kidney function patients or patients with mild to medium levels of renal impairment.

Over 24 patients with severe renal failure among them are required regular hemolysis, the peak concentration of two main metabolites in plasma after a few days of medication is about 10 times higher than the observation concentration of patients with normal renal function. Linezolid peak concentration in plasma is not affected.

The clinical significance of these observations has not been set up due to the limited current safety data of the drug (see Section 4.).

Patients with liver failure

The limited data shows that the pharmacokinetics of Linezolid, PNU-142300 and PNU-142586 do not change in patients with mild to moderate liver failure (group-Pul group A or B). Linezolid's pharmacokinetics parameters in patients with severe liver failure (group C) have not been evaluated. However, because Linezolid is metabolized through the path without enzyme, the liver function impairment will not significantly change the metabolism of the drug (see item 4.).

Children and teenagers (

On teenagers (12 to 17 years old), linezolid's pharmacokinetics similar to adults when taking a dose of 600mg. Therefore, the amount of medicine in the body in teenagers when taking 600mg of Linezolid, every 12 hours will be similar to adults when using the same dose level.

In children from 1 week to 12 years old, taking 10mg/kg every 8 hours will obtain the total amount of drugs in the same body in adults when taking 600mg 2 times a day.

In newborns under 1 week of age, the whole body of Linezolid (per kg of body weight) increases rapidly in the first week of age. Therefore, babies who use 10mg/ kg every 8 hours will have the total amount of drugs in the body will be the largest on the first day after taking the drug. However, this dose will not cause excessive accumulation of drugs in the first week after birth because the clearance increases rapidly in this period.

Elderly patients

Linezolid's

pharmacokinetics does not change significantly in patients aged 65 and over.

female patient

Women with Linezolid's distribution are slightly lower than that of men and the average clearance value decreases by about 20% corresponding to body weight. Linezolid concentration in plasma is higher in women, this is partly due to the difference in body weight.

However, the average selling time of Linezolid is negligible between women and men, the plasma drug concentration in women does not increase significantly in well -tolerated patients, so it is not necessary to adjust the dose.

Before taking Forlen Davipharm medicine for infection (2 blisters x 10 tablets)

How to use

Patients with initial treatment with injection linezolid can be switched to oral linezolid or oral delinquent without adjusting dose.

Dosage

Adults and teenagers (aged 12 years and older)

Hospital pneumonia, including cases where there is an infection

Use 600mg static or oral* every 12 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Pneumonia is suffering from the community, including cases where there is an infection

Use 600mg static or oral* every 12 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Skin and soft tissue infections, including cases with hemorrhage

Use 600mg static or oral* every 12 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Enterococcus infections, including vancomycin strains and cases that are accompanied by blood infections

Use 600mg static or oral* every 12 hours.

recommended treatment time (continuous number of days): 14 - 28 days.

*Oral dose using Linezolid tablets or chaos.

*Adults with mild skin and soft tissue can be used 400mg of oral linezolid every 12 hours.

Children (from birth to 11 years old)

Hospital pneumonia, including cases where there is an infection

Use 10mg/10kg static or oral* 8 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Pneumonia is suffering from the community, including cases where there is an infection

Use 10mg/10kg static or oral* 8 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Skin and soft tissue infections, including cases with hemorrhage

Use 10mg/10kg static or oral* 8 hours.

recommended treatment time (continuous number of days): 10 - 14 days.

Enterococcus infections, including vancomycin strains and cases that are accompanied by blood infections

Use 10mg/10kg static or oral* every 8 hours.

recommended treatment time (continuous number of days): 14 - 28 days.

*Premature babies under 7 days of age (gestational age under 34 weeks) have a lower body clearance of Linezolid and the value under the AUC curve is much larger than that of a monthly and larger newborn babies. In the 7th day, the clearance of Linezolid and the AUC value is similar to that of a newborn and a bigger newborn.

*Oral dose used Linezolid tablet or translation.

Elderly patients

No dose adjustment.

Patients with impaired renal function

No dose adjustment.

Patients with severe renal impairment (eg Creatinine clearance

No need to adjust the dose. Due to clinical influence when exposed to two main metabolites of Linezolid at high concentrations (up to 10 times) in patients with severe renal impairment has not been determined, so be careful when using Linezolid for these patients and only use when expected benefits are superior to theoretical risks.

For patients with hemolysis, Linezolid should be used after the appraisal because of about 30% of the linezolid doses are eliminated within 3 hours of fertilizer. The main metabolites of Linezolid are partially eliminated during the appraisal process, but the concentration of these metabolites is still relatively high after the process of fertilization compared to patients with normal kidney function or patients with renal impairment at a mild to medium to medium.

Therefore, it is advisable to use Linezolid for patients with severe kidney impairment and use only when expected benefits surpasses theoretical risks.

So far, no experience in using Linezolid for patients with constant peritoneal jurisdoms (CAPD) or alternative treatments in case of kidney failure (in addition to hemolysis).

Patients with liver function impairment

No dose adjustment.

However, clinical data is still limited and Linezolid is recommended to be used only for these patients when the expected benefits are superior to theoretical risk.

What to do when more than 1 dose? Dialysis can eliminate 30% of the linezolid dose.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

Clinical trials

Side effects encountered in drug -related drugs in controlled clinical trials with a rate of at least 1% include:

Disorders on the digestive system: abdominal pain/abdominal distention, diarrhea, nausea, vomiting.

Infection: Monilia disease (Candida).

Testing: abnormal hematology tests, abnormal liver function tests.

Disorders on the nervous system: headache, taste change.

After the drug circulates in the market:

Disorders on blood and lymphatic systems: anemia, leukopenia, thrombocytopenia, all healing of healing blood.

Enjoy disorders: optic neuropathy sometimes progresses to loss of vision, which has been recorded in patients using Linezolid. This side effect is common in patients using Linezolid for a longer time than the maximum recommended time of 28 days.

Disorders on the immune system: Anaphylaxis.

Disorders of metabolism and nutrition: Lactic metabolic acidosis.

Disorders on the nervous system: peripheral neuropathy, convulsions.

Disorders on the skin and subcutaneous organization: rash, angioedema. Very few reports are recognized for bullous skin disorders described as Stevens-Johnson syndrome.

Disorders on the digestive system: Coloring blade, enamel changing is rarely recorded when using Linezolid. The discoloration may be lost when using specialized tooth detergents (exfoliating) in case the cause of discoloration is due to the use of Linezolid.

Warnings

Contraindicated

Forlen drugs are contraindicated in the following cases:

  • Do not use Linezolid for patients with a history of hypersensitivity to Linezolid or any ingredients of the drug. This drug within 2 weeks before taking Linezolid.

    • Interactions are at risk of hypertension

    Except for patients who monitor the risk of hypertension, linezolid should not be used for untreated hypertension patients, patients with chromium skin tumors, thyroid poisoning or patients taking any drugs such as direct or indirect sympathetic drugs (for example: pseudoephedrin, phenylpropanolamine), vascular drugs) norepinephrin), dopaminergic drugs (for example: dopamine, dobutamin).

    Serotonin syndrome interactions

    Except for patients who are carefully monitored the signs or symptoms of serotonin syndrome, linezolid should not be used for patients with carcinoid syndrome and patients taking any of the following drugs: Serotonin recovery inhibitors, three-ring anti-depression drugs, 5-HT1 serotonin (Triptans), Meperine or bepire.

    Precautions when used

    Inhibition of bone marrow inhibitors (anemia, thrombocytopenia, leukopenia and all hemorrhage reduction) depending on the treatment time has been recorded in some patients using Linezolid. Blood formula should be monitored in patients at risk of increased bleeding, patients who have a history of marrow failure, patients who are taking simultaneously drugs may cause hemoglobin reduction or function or platelet or Linezolid patients for more than 2 weeks.

    Palm of fake colitis has been recorded with most antibacterial drugs, including Linezolid with severe seriousness from mild to life -threatening. diarrhea involved in Clostridium difficile (CDAD) has been recorded when using most antibacterial drugs, including linezolid, and may fluctuate from mild diarrhea to fatal colitis.

    Treatment with antibacterial drugs changes the normal chanting bacteria of the intestine leading to the excessive growth of C. different.

    c. Difficile produces toxins A and B related to the progression of CDAD diarrhea. The extremely strong toxin difficile strains are the cause of increased likelihood of disease and death, because these infections do not respond to antibiotic therapy and can lead to removal of the colon. Acute diarrhea caused by C. Difficile should be considered in patients with diarrhea after antibiotics, carefully assessing patients' history because CDAD has been recorded after more than 2 months after antibiotic use.

    Peripheral and optic neurological diseases have been recorded in Linezolid patients, mainly in patients who take the drug longer than the recommended time of 28 days.

    In the case of progressive visual neurological diseases, the patient has been treated for a longer period of time the maximum time is recommended.

    If symptoms of vision impairment appear, such as vision changes, changes when identifying colors, blurred vision or defects in the visual field, patients should see an eye exam immediately. The visual function should be monitored in all patients using Linezolid for a long time (greater than or equal to 3 months) and on patients with vision abnormal symptoms whether long or short linezolid treatment time. If peripheral and optic neurological diseases appear, continuing to use Linezolid should be considered effectively to bring superior to these risks.

    Lactic metabolic acidosis has been recorded in patients using Linezolid.

    Patients appear nausea or constant vomiting, acidosis for unknown causes or concentrations of bicarbonate decreases when taking Linezolid should be monitored immediately.

    Rarely cases of convulsions on patients treated with Linezolid. Most cases of patients with seizures have been recorded with a history of epilepsy or risk factors for epilepsy.

    Voluntary reports on serotonin syndrome related to simultaneous use of Linezolid with serotonergic drugs, including anti -depression drugs Serive inhibitor recovery Serotonin (SSRIs) have been recorded.

    When necessary to simultaneously use Linezolid and serotonergic drugs, patients should carefully monitor the signs and symptoms of serotonin syndrome such as cognitive disorders, high fever, increased reflexes and inability to coordinate. If the signs or symptoms occur, the doctor should consider stopping one or both medications. If you stop taking serotonergic drugs, the above symptoms may retreat.

    On healthy volunteers, simultaneous use of rifampin with Linezolid reduces 21% cmax and 32% of the area under the AUC curve of Linezolid. The clinical significance of this interaction is not well known.

    Linezolid does not have clinical effects against Gram (-) bacteria and is not indicated in the treatment of Gram (-) infections. If suspected or sure to be infected at the same time, Gram (-) bacteria strains, should be treated with specific effects on Gram (-) bacteria.

    Be cautious when using Linezolid in patients with high risk of life -threatening body infections, such as infections related to central venous catheter placement in special care units. Linezolid is not prescribed treatment for patients with hematoma related to catheter placement.

    Clinical trial on hemorrhage infections related to catheter placement caused by gram (+) bacteria

    A random group of clinical clinical trials, opened labels, which have been conducted in adult patients with catheter -related catheter infections caused by gram bacteria (+) compares linezolid (600mg every 12 hours, intravenous/oral injection) with Vancomycin 1g intravenous intravenously every 12 hours or Oxacillin 2g intravenously every 6 hours and then switch to dicloxacillin 500mg every 6 or drinking time from 7 to 7 times 28 days.

    The mortality rate in this study was 78/363 (21.5%) in patients using Linezolid and 58/363 (16.0%) in the control group. Based on the logical regression analysis results, the risk ratio is estimated at 1,426 [95% trust range ranging from 0.970 to 2,098].

    Although the causal relationship has not been established, this observed imbalance appears mainly in patients using Linezolid with infections caused by gram bacteria (-), or suffered from mixed infections caused by gram (+) and gram (-) bacteria or not identified the pathogenic bacteria at the time before antibiotic use.

    Patients randomly divided into the Linezolid group only infected with gram (+) bacteria before using antibiotics, including small subgroups patients with blood infections caused by gram bacteria (+) with similar survival rates

    The ability to drive or operate machinery

    The effect of Linezolid on driving and operating machinery has not been systematically evaluated.

    Pregnancy and nursing mothers

    Pregnant women

    Studies on the effects of Linezolid on the reproductive system performed on mice and rats do not show the effect of fetal defects. The mild toxicity on the fetus is only observed on the mouse at the level of toxicity to the mother mouse.

    In mice, the toxicity on the fetus is shown by the effect of reducing the weight of the fetal and reducing the process of bone burning sternum (often accompanied by a decrease in body weight).

    Reducing the survival and developmental rate of the mice that appeared on rats. When pairing, in these mice also see the signs of increasing the loss of the nesting of the egg recovery and depending on the dose.

    There are no full -controlled studies conducted in pregnant women. Therefore, linezolid should only be used during pregnancy when the benefits bring out the risk of being harmful to the fetus. Linezolid reduces fertility on male rats.

    breastfeeding women

    Linezolid excreted through breast milk in the mice is experimenting. It is unknown whether the Linezolid is excreted through breast milk. Therefore, it is necessary to be cautious when using Linezolid for breastfeeding women.

    Medicinal interaction

    Linezolid is a non -selective inhibitor of weak and recovered monoamine oxidase. Therefore, some patients using Linezolid may have a mild hypertension recovery caused by pseudoephedrin hydrochloride or phenylpropanolamine hydrochloride. The initial dose of adrenergic drugs should be reduced such as dopamine and dopamine owners, and the dose detection to achieve the desired effect.

    Voluntary reports on serotonin syndrome when using Linezolid and serotonergic drugs are simultaneously recorded.

    Antibiotics: Linezolid's pharmacokinetics are not changed when used simultaneously with aztreonam or gentamicin. The effect of rifampin on linezolid's pharmacokinetics parameters is studied over 16 healthy volunteers, using Linezolid 600mg twice a day for 2.5 days with or not accompanied by rifampin 600mg once a day for 8 days. Rifampin reduces CMAX and AUC of Linezolid an average of 21% [90%, 15 - 270 and 32% reliability [90%, 27 - 37] respectively. The mechanism of this interaction and its meaning is unknown.

    Storage

    In a dry place, avoid light, the temperature does not exceed 30 degrees C.

    Expiry date: 36 months from the date of production.

    Other drugs

    Disclaimer

    Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

    The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

    count views

    Popular Keywords