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LINEZOLID. The discovery and clinical development of effective antibiotics is most remarkable achievement over the past 60 years. Since the introduction of the sulphonamides in 1936, researchers have developed a range of antibiotic classes.

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Linezolid

LINEZOLID


Linezolid

  • The discovery and clinical development of effective antibiotics is most remarkable achievement over the past 60 years.

  • .

  • Since the introduction of the sulphonamides in 1936, researchers have developed a range of antibiotic classes.


Linezolid

  • Until recently, however all new antibiotics introduced over the past 35 years have been structural modifications of existing antibiotic classes.


Linezolid

  • The oxazolidinones represent the first truly new class of antibacterial agents.

  • Approved in 2000 by the US FDA.

  • .

  • Linezolid has a unique mechanism of antibacterial action.


Linezolid

  • .


Linezolid

  • Linezolid is the first of a new class of anti microbial agents, the Oxazolidinones, whose mechanism of action differs from that of existing agents.


Linezolid

  • Cross resistance to other antimicrobials is therefore less likely and has not been shown till date.

  • .

  • It is approved US FDA in adults (April 2000) and children (December 2002) for the treatment of Gram Positive bacteria.


Linezolid

  • It disrupts bacterial growth by inhibiting

  • the initiation process in protein synthesis.

  • It binds to a site on the bacterial 23s

  • ribosomal RNA of the 50s subunit,

  • preventing the formation of functional 70s

  • initiation complex which is an essential

  • component of the bacterial translation

  • process.


Linezolid

  • This site of inhibition process occurs

  • earlier in the initiation process than

  • other protein synthesis inhibitors

  • that interfere with the elongation

  • process.


Linezolid

  • Absorption: Well absorbed orally irrespective of timing of meal

  • .

  • Bioavailability: 100%


Linezolid

  • Half Life:

  • Preterm neonate < 1 week: 5.6 hrs.

  • Term neonate < 1 week: 3 hrs.

  • Term neonate > 1 week: 1.5 hrs.

  • Infants: 1.8 hrs

  • Children: 3 + 1.1 hrs

  • Adolescent: 4.1 hrs

  • .


Linezolid

  • Maximum Plasma concentration is reached

  • within 1 to 2 hrs.

  • .

  • Distributes readily to well perfused area


Linezolid

  • Metabolism: It is primarily metabolized by oxidation of the morphine ring which results in two inactive ring-opened carboxylic acid metabolites

  • .

  • A) aminoethoxyacetic acid

  • (B) hydroxyethyl glycine


Linezolid

  • Excretion: Non renal clearance accounts for about 65% of total clearance.

  • .

  • Approximately 30% of the dose appears in urine as Linezolid, 40% as metabolite B and 10% as metabolite A


Linezolid

  • Aerobic and facultative Gram positive

  • microorganisms

  • Enterococcus faecium (vancomycin

  • resistant strains only)

  • Staphylococcus aureus ( including

  • methicillin resistantstrain)

  • Streptococcus agalactiae

  • Streptococcus pneumoniae

  • ( penicillin susceptible strains only)

  • Strptococcus pyrogenes

  • .


Linezolid

  • Aerobic and facultative Gram positive microorganisms

Enterococcus faecalis (including vancomycin-resistan strains)

Enterococcus faecalis (vancomycin-susceptible strains)

Staphylococcus epidermidis (including methicillin- resistant strains)

Staphylococcus haemolyticus.

Streptococcus pneumoniae (penicillin-resistant strains)

Viridans group streptococci

  • .

  • Aerobic and facultative Gram-negative microorganisms

Pasteurella multocida


Linezolid

  • Vancomycin-Resistant Enterococcus faecium

  • infections, including cases with concurrent bacteremia

  • Nosocomial pneumonia caused by staphylococcus aureus

  • (methicillin susceptible and resistant strains), or

  • streptococcus pneumoniae (penicillin susceptible strains).

  • .

  • Combination therapy may be clinically indicated if the

  • documented or presumptive pathogens include

  • Gram- negative organisms.


Linezolid

  • Complicated skin and skin structure infections 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


Linezolid

  • Community-acquired pneumonia caused

  • by Streptococcus pneumoniae (penicillin-susceptible strains only),including cases with concurrent bacteremia, or staphylococcus aureus (methicillin-susceptible strains).

  • .


Linezolid

  • .


Linezolid

  • .


Linezolid

  • CBC, Hb & Platelet count: particularly in patients who are at increased risk for bleeding, patients with pre-existing thrombocytopenia or Myelosuppression or concomitant medications that decrease platelet count or function or produce bone marrow suppression and in patient requiring more than 2 weeks therapy.

  • .

  • Number and type of stools /day for diarrhea


Linezolid

  • Well tolerated by most patients.

  • Same in children & adults

  • The most common adverse effects are:

  • Myelosuppression (1 to 10%) including anemia, pancytopenia,

  • leucopenia & thrombocytopenia

  • Diarrhea (4 to 8%),

  • Headache, Insomnia, Dizziness (2 to 6%)

  • Nausea, vomiting (1 to 3.7%),

  • Altered taste or tongue discoloration (1 to 2%)

  • Transient elevation in liver function test (1 to 2%).

  • Pseudo membranous colitis


Linezolid

  • .


Linezolid

  • LINEZOLID is contraindicated for use in patients who have known hypersensitivity to Linezolid or any of the other product components.

  • .


Linezolid

  • No dose adjustment is recommended

  • .


Linezolid

  • No dose adjustment is recommended in case of mild & moderate hepatic insufficiency.

  • .


Linezolid

  • Ingestion of Tyramine containing foods

  • may cause hypertensive crisis.

  • .

  • Limit intake of Tyramine containing

  • foods to less than 100 mg/meal


Linezolid

  • Linezolid is not an inducer of

  • cytochrome p450 (CYP).

  • Therefore no CYP 450 induced

  • drug interactions are expected.

  • So the drugs like Warfarin and

  • Phenytoin can be given without

  • dose alteration.

  • .


Linezolid

  • Monoamine Oxidase inhibiter:

  • It is a reversible non selective inhibitor of monoamine oxidase. Therefore, it has potential for interaction with adrenergic and serotonergic agents such

  • as Tricyclic antidepressants, Detromethorpan and

  • Trazodone.

  • .


Linezolid

  • Store reconstituted preparation at room

  • temperature and use within 21 days.

  • Store infusion bag in over wrap until

  • ready to use. The yellow color of

  • infusion solution may intensify over

  • time without adversely affecting the

  • potency.

  • Store at room temperature & protect

  • from light.

  • Injection is compatible with D5, RL, NS


Linezolid

  • Avoid excessive amount of Tyramine

  • containing foods; Red wine, Aged

  • cheese, Smoked or pickled fish, Beef

  • or chicken liver, dried sausage, fava

  • or broad bean.

  • Notify in case of persistent or

  • worsening of symptoms of infection,

  • diarrhea, nausea or vomiting.

  • Complete course of therapy even if

  • symptoms improve.

  • .


Linezolid

  • -Injection: 200mg (100 ml)

  • 400mg (200 ml)

  • 600mg (300 ml)

  • Infuse over 30-120 mins. Do not infuse

  • with any other medication. Flush IV

  • line before & after infusion with

  • compatible solution.

  • - Suspension: Dry powder 20mg/ml

  • Gently invert bottle 3-5 times. Do not

  • shake.

  • - Tablet: 400mg, 600mg


Linezolid

  • Linospan (Cipla)

  • Linox (Unichem)

  • Lizolid (Integrace)

  • Lizomed (Aglomed)


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