Actions of Meropenem Auro Pharma in details
Pharmacology: Meropenem Auro Pharma is a carbapenem antibiotic for parenteral use, that is stable to human dehydropeptidase-1(DHP-1). It is structurally similar to imipenem.
Meropenem Auro Pharma exerts its bactericidal action by interfering with vital bacterial cell wall synthesis. The ease with which it penetrates bacterial cell walls, its high level of stability to all serine β-lactamases and its marked affinity for the penicillin-binding proteins (PBPs) explain the potent bactericidal action of Meropenem Auro Pharma against a broad spectrum of aerobic and anaerobic bacteria. Bactericidal concentrations are commonly the same as the minimum inhibitory concentrations (MICs).
Meropenem Auro Pharma is stable in susceptibility tests and these tests can be performed using normal routine methods. In vitro tests show that Meropenem Auro Pharma acts synergistically with various antibiotics. It has been demonstrated both in vitro and in vivo that Meropenem Auro Pharma has a post-antibiotic effect.
Meropenem Auro Pharma is usually active, in vitro and in clinical infections, against the following strains of bacteria as follows:
Gram-Positive Aerobes: Enterococcus faecalis, Staphylococcus aureus (penicillinase negative and positive), Staphylococci-coagulase negative including Staphylococcus epidermidis, Streptococci including Streptococcus pneumoniae, Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus mitis, Streptococcus milleri, Streptococcus sanguis, Streptococcus viridans.
Gram-Negative Aerobes: Acinetobacter anitratus, Citrobacter spp including Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae and other Enterobacter spp, Escherichia coli, Haemophilus influenzae (including β-lactamase positive strains), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Klebsiella pneumoniae and other Klebsiella spp, Morganella morganii, Proteus mirabilis, Serratia spp.
Anaerobic Bacteria: Bacteroides fragilis, Bacteroides thetaiotaomicron and other Bacteroides spp, Clostridium spp including C. perfringens, Eubacterium lentum, Fusobacterium spp, Mobiluncus curtisii, Peptostreptococcus spp, Peptococcus spp.
Some strains of Pseudomonas aeruginosa are susceptible to Meropenem Auro Pharma in vitro and in clinical infections.
Enterococcus faecium, Stenotrophomonas (Xanthomonas) maltophilia and methicillin-resistant Staphylococci have been found to be resistant to Meropenem Auro Pharma.
Pharmacokinetics: A 30-min IV infusion of a single dose of Meropenem Auro Pharma in normal volunteers resulted in peak plasma levels of approximately 11, 23, 49 and 115 mcg/mL following the 250-mg, 500-mg, 1-g and 2-g doses, respectively.
A 5-min IV bolus injection of Meropenem Auro Pharma in normal volunteers resulted in peak plasma levels of approximately 52 and 112 mcg/mL for the 500-mg and 1-g dose, respectively.
Intravenous infusions over 2, 3 and 5 min of a 1 g dose of Meropenem Auro Pharma were compared in a 3-way crossover trial. These durations of infusion resulted in peak plasma levels of 110, 91 and 94 mcg/mL, respectively.
After an IV dose of 500 mg, plasma levels of Meropenem Auro Pharma declined to values of ≤1 mcg/mL 6 hrs after administration.
When multiple doses are administered at 8-hourly intervals to subjects with normal renal function, accumulation of Meropenem Auro Pharma does not occur.
In subjects with normal renal function, Meropenem Auro Pharma's elimination t½ is approximately 1 hr.
Plasma protein-binding of Meropenem Auro Pharma is approximately 2%.
Approximately 70% of the IV administered dose is recovered as unchanged Meropenem Auro Pharma in the urine over 12 hrs, after which little further urinary excretion is detectable. Urinary concentrations of Meropenem Auro Pharma in excess of 10 mcg/mL are maintained for up to 5 hrs at the 500-mg dose. No accumulation of Meropenem Auro Pharma in plasma or urine was observed with regimens using 500 mg administered every 8 hrs or 1 g administered every 6 hrs in volunteers with normal renal function.
The only metabolite of Meropenem Auro Pharma is microbiologically inactive.
Meropenem Auro Pharma penetrates well into most body fluids and tissues including cerebrospinal fluid of patients with bacterial meningitis, achieving concentrations in excess of those required to inhibit most bacteria.
Studies in children have shown that the pharmacokinetics of Meropenem Auro Pharma in children is essentially similar to those in adults. The elimination t½ for Meropenem Auro Pharma was approximately 1.5 hrs in children <2 years.
The pharmacokinetics is linear over the dose range of 10-40 mg/kg.
Pharmacokinetic studies in patients with renal insufficiency have shown the plasma clearance of Meropenem Auro Pharma correlates with creatinine clearance. Dosage adjustments are necessary in subjects with renal impairment.
Pharmacokinetic studies in the elderly have shown a reduction in plasma clearance of Meropenem Auro Pharma which correlated with age-associated reduction in creatinine clearance.
Pharmacokinetic studies in patients with liver disease have shown no effects of liver disease on the pharmacokinetics of Meropenem Auro Pharma.
How should I take Meropenem Auro Pharma?
Meropenem Auro Pharma is injected into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.
Meropenem Auro Pharma is usually given every 8 hours. Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.
Meropenem Auro Pharma must be mixed with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medicine.
Do not mix other injectable medications in the same IV bag or tubing used to given your Meropenem Auro Pharma injection.
Use a disposable needle and syringe only once. Follow any state or local laws about throwing away used needles and syringes. Use a puncture-proof "sharps" disposal container (ask your pharmacist where to get one and how to throw it away). Keep this container out of the reach of children and pets.
Use Meropenem Auro Pharma for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Meropenem Auro Pharma will not treat a viral infection such as the common cold or flu.
If you use this medication long-term, you may need frequent medical tests at your doctor's office.
Store unopened vials of Meropenem Auro Pharma at cool room temperature away from moisture and heat.
After mixing your medicine, you will need to use it within a certain number of hours. This will depend on the diluent and how you store the mixture (at cool room temperature, or in a refrigerator). Carefully follow the mixing and storage instructions provided with your medicine. Ask your pharmacist if you have questions.
Meropenem Auro Pharma administration
Meropenem Auro Pharma will be administered as an intravenous (into a vein) injection by a healthcare provider.
If you are using Meropenem Auro Pharma at home, your healthcare provider will give you detailed instructions regarding preparation, administration, and storage of the medication.
It is important to take Meropenem Auro Pharma regularly to get the most benefit.
Take all of the Meropenem Auro Pharma that has been prescribed for you, even if you begin to feel better. Your symptoms may start to improve before the infection is completely treated.
Your doctor may want you to have blood tests or other medical evaluations during treatment with Meropenem Auro Pharma to monitor progress and side effects.
Meropenem Auro Pharma pharmacology
Mechanism Of Action
Meropenem Auro Pharma is an antibacterial drug.
Pharmacokinetics
Plasma Concentrations
At the end of a 30-minute intravenous infusion of a single dose of Meropenem Auro Pharma I.V. in healthy volunteers, mean peak plasma concentrations of Meropenem Auro Pharma are approximately 23 mcg/mL (range 14-26) for the 500 mg dose and 49 mcg/mL (range 39-58) for the 1 gram dose. A 5-minute intravenous bolus injection of Meropenem Auro Pharma I.V. in healthy volunteers results in mean peak plasma concentrations of approximately 45 mcg/mL (range 18-65) for the 500 mg dose and 112 mcg/mL (range 83-140) for the 1 gram dose.
Following intravenous doses of 500 mg, mean plasma concentrations of Meropenem Auro Pharma usually decline to approximately 1 mcg/mL at 6 hours after administration.
No accumulation of Meropenem Auro Pharma in plasma was observed with regimens using 500 mg administered every 8 hours or 1 gram administered every 6 hours in healthy volunteers with normal renal function.
Distribution
The plasma protein binding of Meropenem Auro Pharma is approximately 2%.
Meropenem Auro Pharma penetrates well into most body fluids and tissues including cerebrospinal fluid, achieving concentrations matching or exceeding those required to inhibit most susceptible bacteria. After a single intravenous dose of Meropenem Auro Pharma I.V., the highest mean concentrations of Meropenem Auro Pharma were found in tissues and fluids at 1 hour (0.5 hours to 1.5 hours) after the start of infusion, except where indicated in the tissues and fluids listed in the table below.
Table 1: Meropenem Auro Pharma Concentrations in Selected Tissues (Highest Concentrations Reported)
| Tissue | Intravenous Dose (gram) | Number of Samples | Mean [μg/mL ormcg/ (gram)]* | Range [μg/mL or mcg/ (gram)] |
| Endometrium | 0.5 | 7 | 4.2 | 1.7-10.2 |
| Myometrium | 0.5 | 15 | 3.8 | 0.4-8.1 |
| Ovary | 0.5 | 8 | 2.8 | 0.8-4.8 |
| Cervix | 0.5 | 2 | 7 | 5.4-8.5 |
| Fallopian tube | 0.5 | 9 | 1.7 | 0.3-3.4 |
| Skin | 0.5 | 22 | 3.3 | 0.5-12.6 |
| Interstitial fluidt | 0.5 | 9 | 5.5 | 3.2-8.6 |
| Skin | 1 | 10 | 5.3 | 1.3-16.7 |
| Interstitial fluidt | 1 | 5 | 26.3 | 20.9-37.4 |
| Colon | 1 | 2 | 2.6 | 2.5-2.7 |
| Bile | 1 | 7 | 14.6 (3 hours) | 4-25.7 |
| Gall bladder | 1 | 1 | — | 3.9 |
| Peritoneal fluid | 1 | 9 | 30.2 | 7.4-54.6 |
| Lung | 1 | 2 | 4.8 (2 hours) | 1.4-8.2 |
| Bronchial mucosa | 1 | 7 | 4.5 | 1.3-11.1 |
| Muscle | 1 | 2 | 6.1 (2 hours) | 5.3-6.9 |
| Fascia | 1 | 9 | 8.8 | 1.5-20 |
| Heart valves | 1 | 7 | 9.7 | 6.4-12.1 |
| Myocardium | 1 | 10 | 15.5 | 5.2-25.5 |
| CSF (inflamed) | 20 mg/kg‡ | 8 | 1.1 (2 hours) | 0.2-2.8 |
| 40 mg/kg§ | 5 | 3.3 (3 hours) | 0.9-6.5 | |
| CSF (uninflamed) | 1 | 4 | 0.2 (2 hours) | 0.1-0.3 |
| *at 1 hour unless otherwise noted †obtained from blister fluid ‡in pediatric patients of age 5 months to 8 years §in pediatric patients of age 1 month to 15 years |
Metabolism
There is one metabolite of Meropenem Auro Pharma that is microbiologically inactive.
Excretion
In subjects with normal renal function, the elimination half-life of Meropenem Auro Pharma is approximately 1 hour.
Meropenem Auro Pharma is primarily excreted unchanged by the kidneys. Approximately 70% (50% – 75%) of the dose is excreted unchanged within 12 hours. A further 28% is recovered as the microbiologically inactive metabolite. Fecal elimination represents only approximately 2% of the dose. The measured renal clearance and the effect of probenecid show that Meropenem Auro Pharma undergoes both filtration and tubular secretion.
Urinary concentrations of Meropenem Auro Pharma in excess of 10 mcg/mL are maintained for up to 5 hours after a 500 mg dose.
Specific Populations
Renal Impairment
Pharmacokinetic studies with Meropenem Auro Pharma I.V. in patients with renal impairment have shown that the plasma clearance of Meropenem Auro Pharma correlates with creatinine clearance. Dosage adjustments are necessary in subjects with renal impairment (creatinine clearance 50 mL/min or less).
Meropenem Auro Pharma I.V. is hemodialyzable. However, there is no information on the usefulness of hemodialysis to treat overdosage.
Hepatic Impairment
A pharmacokinetic study with Meropenem Auro Pharma I.V. in patients with hepatic impairment has shown no effects of liver disease on the pharmacokinetics of Meropenem Auro Pharma.
Geriatric Patients
A pharmacokinetic study with Meropenem Auro Pharma I.V. in elderly patients with renal impairment showed a reduction in plasma clearance of Meropenem Auro Pharma that correlates with age-associated reduction in creatinine clearance.
Pediatric Patients
The pharmacokinetics of Meropenem Auro Pharma for injection I.V., in pediatric patients 2 years of age or older, are similar to those in adults. The elimination half-life for Meropenem Auro Pharma was approximately 1.5 hours in pediatric patients of age 3 months to 2 years.
The pharmacokinetics of Meropenem Auro Pharma in patients less than 3 months of age receiving combination antibacterial drug therapy are given below.
Table 2: Meropenem Auro Pharma Pharmacokinetic Parameters in Patients Les s Than 3 Months of Age*
| GA less than 32 weeks PNA less than 2 weeks (20mg/kg every 12 hours) | GA less than 32 weeks PNA 2 weeks or older (20mg/kg every 8 hours) | GA 32 weeks or older PNA less than 2 weeks (20mg/kg every 8 hours) | GA 32 weeks or older PNA 2 weeks or older (30mg/kg every 8 hours) | Overall | |
| CL (L/h/kg) | 0.089 | 0.122 | 0.135 | 0.202 | 0.119 |
| V (L/kg) | 0.489 | 0.467 | 0.463 | 0.451 | 0.468 |
| AUC0-24 (mcg-h/mL) | 448 | 491 | 445 | 444 | 467 |
| Cmax (mcg/mL) | 44.3 | 46.5 | 44.9 | 61 | 46.9 |
| Cmin (mcg/mL) | 5.36 | 6.65 | 4.84 | 2.1 | 5.65 |
| T½ (h) | 3.82 | 2.68 | 2.33 | 1.58 | 2.68 |
| *Values are derived from a population pharmacokinetic analysis of sparse data |
Drug Interactions
Probenecid competes with Meropenem Auro Pharma for active tubular secretion and thus inhibits the renal excretion of Meropenem Auro Pharma. Following administration of probenecid with Meropenem Auro Pharma, the mean systemic exposure increased 56% and the mean elimination half-life increased 38%. Co-administration of probenecid with Meropenem Auro Pharma is not recommended.
Microbiology
Mechanism Of Action
The bactericidal activity of Meropenem Auro Pharma results from the inhibition of cell wall synthesis. Meropenem Auro Pharma readily penetrates the cell wall of most Gram-positive and Gram-negative bacteria to reach penicillin-binding-protein (PBP) targets. Its strongest affinities are toward PBPs 2, 3 and 4 of Escherichia coli and Pseudomonas aeruginosa; and PBPs 1, 2 and 4 of Staphylococcus aureus. Bactericidal concentrations (defined as a 3 log reduction in cell counts within 12 hours to 24 hours) are typically 1-2 times the bacteriostatic concentrations of Meropenem Auro Pharma, with the exception of Listeria monocytogenes, against which lethal activity is not observed.
Meropenem Auro Pharma has significant stability to hydrolysis by β-lactamases, both penicillinases and cephalosporinases produced by Gram-positive and Gram-negative bacteria.
Meropenem Auro Pharma should not be used to treat methicillin-resistant Staphylococcus aureus (MRSA) or methicillin-resistant Staphylococcus epidermidis (MRSE).
Mechanism Of Resistance
There are several mechanisms of resistance to carbapenems: 1) decreased permeability of the outer membrane of Gram-negative bacteria (due to diminished production of porins) causing reduced bacterial uptake, 2) reduced affinity of the target PBPs, 3) increased expression of efflux pump components, and 4) production of antibacterial drug-destroying enzymes (carbapenemases, metallo-β-lactamases). Localized clusters of infections due to carbapenem-resistant bacteria have been reported in some regions.
Cross-Resistance
Cross-resistance is sometimes observed with isolates resistant to other carbapenems.
Interactions With Other Antibacterial Drugs
In vitro tests show Meropenem Auro Pharma to act synergistically with aminoglycoside antibacterials against some isolates of Pseudomonas aeruginosa.
Spectrum Of Activity
Meropenem Auro Pharma has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections as described.
Gram-positive Bacteria
Enterococcus faecalis (vancomycin-susceptible isolates only)
Staphylococcus aureus (methicillin-susceptible isolates only)
Streptococcus agalactiae
Streptococcus pneumoniae (penicillin-susceptible isolates only)
Streptococcus pyogenes
Viridans group streptococci
Gram-negative Bacteria
Escherichia coli
Haemophilus influenzae
Klebsiella pneumoniae
Neisseria meningitidis
Pseudomonas aeruginosa
Proteus mirabilis
Anaerobic Bacteria
Bacteroides fragilis
Bacteroides thetaiotaomicron
Peptostreptococcus species
The following in vitro data are available, but their clinical significance is unknown. At least 90% of the following bacteria have exhibited in vitro minimum inhibitory concentrations (MICs) less than or equal to the susceptible breakpoints for Meropenem Auro Pharma. However, the safety and effectiveness of Meropenem Auro Pharma in treating clinical infections due to these bacteria have not been established in adequate and wellcontrolled trials.
Gram-positive Bacteria
Staphylococcus epidermidis (methicillin-susceptible isolates only)
Gram-negative Bacteria
Aeromonas hydrophila
Campylobacter jejuni
Citrobacter koseri (formerly diversus)
Citrobacter freundii
Enterobacter cloacae
Hafnia alvei
Klebsiella oxytoca
Moraxella catarrhalis
Morganella morganii
Pasteurella multocida
Proteus vulgaris
Serratia marcescens
Anaerobic Bacteria
Bacteroides distasonis
Bacteroides ovatus
Bacteroides uniformis
Bacteroides ureolyticus
Bacteroides vulgatus
Clostridium difficile
Clostridium perfringens
Eubacterium lentum
Fusobacterium species
Prevotella bivia
Prevotella intermedia
Prevotella melaninogenica
Porphyromonas asaccharolytica
Propionibacterium acnes
Susceptibility Test Methods
When available, the clinical microbiology laboratory should provide cumulative results of in vitro susceptibility test results for antimicrobial drugs used in local hospitals and practice areas to the physician as periodic reports that describe the susceptibility profile of nosocomial and communityacquired pathogens. These reports should aid the physician in selecting the most effective antimicrobial.
Dilution Techniques
Quantitative methods are used to determine antimicrobial minimum inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized test method. Standardized procedures are based on a dilution method (broth or agar) The MIC values obtained should be interpreted according to the criteria provided in Table 3.
Table 3: Susceptibility Interpretive Criteria for Meropenem Auro Pharma
| Pathogen | Minimum Inhibitory Concentrations (mcg/mL) | Disk Diffusion (zone diameters in mm) | ||||||
| S | I | R | S | I | R | |||
| Enterobacteriaceae | ≤ 1 | 2 | ≥ 4 | ≥ 23 | 20-22 | ≤ 19 | ||
| Pseudomonas aeruginosa* | ≤ 2 | 4 | ≥ 8 | ≥ 19 | 16-18 | ≤ 15 | ||
| Haemophilus influenzae† | ≤ 0.5 | — | — | ≥ 20 | — | — | ||
| Neisseria meningitidis† | ≤ 0.25 | — | — | ≥ 30 | — | — | ||
| Streptococcus pneumoniae‡§ | ≤ 0.25 | 0.5 | ≥ 1 | — | — | — | ||
| Streptococcus agalactiae and Streptococcus pyogenest†¶§ | ≤ 0.5 | — | — | — | — | — | ||
| Anaerobes# | ≤ 4 | 8 | ≥ 16 | — | — | — | ||
| S = Susceptible, I = Intermediate, R = Resistant No interpretative criteria have been established for testing enterococci. Susceptibility of staphylococci to Meropenem Auro Pharma may be deduced from testing penicillin and either cefoxitin or oxacillin. *The interpretive criteria for P. aeruginosa are based upon the dosing of 1g every 8 hours. †The current absence of data on resistant isolates precludes defining any category other than “Susceptible”. If isolates yield MIC results other than susceptible, they should be submitted to a reference laboratory for additional testing. ‡For nonmeningitis isolates of S. pneumoniae a penicillin MIC of ≤ 0.06 mcg/mL or oxacillin zone ≥ 20 mm can predict susceptibility to Meropenem Auro Pharma. MIC testing should be performed on isolates that do not test as susceptible by either of these methods, and on all meningitis S. pneumoniae isolates. §Reliable disk diffusion tests for Meropenem Auro Pharma do not yet exist for testing streptococci.
sponsored
References
ReviewsThe results of a survey conducted on ndrugs.com for Meropenem Auro Pharma are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Meropenem Auro Pharma. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reportsConsumer reported administrationNo survey data has been collected yetConsumer reviews
Information checked by Dr. Sachin Kumar, MD Pharmacology More about Meropenem Auro PharmaClinician Information
|
