Cefuroxime Actions

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Actions of Cefuroxime in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacology: Pharmacodynamics: Cefuroxime is a cephalosporin antibiotic. All cephalosporins (β-lactam antibiotics) inhibit cell wall production and are selective inhibitors of peptidoglycan synthesis. The initial step in drug action consists of binding of the drug to cell receptors called the penicillin-binding proteins. After a β-lactam antibiotic has bound to these receptors, the transpeptidation reaction is inhibited and peptidoglycan synthesis is blocked. Bacterial lysis is the end result.

Pharmacokinetics: Cefuroxime 250/500: After oral administration, Cefuroxime axetil is slowly absorbed from the gastrointestinal tract, and rapidly hydrolysed in the intestinal mucosa and blood to release Cefuroxime into the circulation.

Optimum absorption occurs when it is administered shortly after a meal.

Peak serum levels of 5-8 mg/L for a 500-mg dose occur approximately 2-3 hrs after dosing when taken after food.

Post peak levels, the serum half-life is between 1 and 1.5 hrs. Protein-binding has been variously stated as 33-50% depending on the methodology used. Cefuroxime is not metabolised and is excreted by glomerular filtration and tubular secretion.

Concurrent administration of probenecid increases the area under the mean serum concentration-time curve (AUC) by 50%. Serum levels of Cefuroxime are reduced by dialysis.

Cefuroxime Injection: The serum half-life after either IM or IV administration is approximately 70 min. After IM injection, the peak serum level occurs after about 45 min.

Cefuroxime can be found in bone, synovial fluid and aqueous humor above the minimum inhibitory levels for common pathogens. The blood-brain barrier can be passed by Cefuroxime when the meninges are inflamed.

Cefuroxime is excreted approximately 50% by glomerular filtration and 50% through the renal tubules. Cefuroxime is almost completely recovered unchanged in the urine within 24 hrs, most being excreted within 6 hrs.

Microbiology: Cefuroxime 250/500: Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound, Cefuroxime. It is a well characterised and effective antibacterial agent which has bactericidal activity against a wide range of common pathogens, including β-lactamase producing strains. Cefuroxime has good stability to bacterial β-lactamase, and consequently is active against many ampicillin-resistant or amoxycillin-resistant strains.

The bactericidal action of Cefuroxime results from inhibition of cell wall synthesis by binding to essential target proteins.

How should I take Cefuroxime?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.

You may take Cefuroxime tablets with or without meals.

Cefuroxime oral suspension (liquid) must be taken with food.

Shake the oral liquid well just before you measure a dose. To be sure you get the correct dose, measure the liquid with a marked measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

If you switch from using the tablet form to using the oral suspension (liquid) form of Cefuroxime, you may not need to use the same exact dosage in number of milligrams. The medication may not be as effective unless you use the exact form and strength your doctor has prescribed.

Use this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before the infection is completely treated. Cefuroxime will not treat a viral infection such as the common cold or flu.

This medication can cause you to have false results with certain medical tests, including urine glucose (sugar) tests. Tell any doctor who treats you that you are using Cefuroxime.

Store Cefuroxime tablets at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.

Store Cefuroxime oral liquid in the refrigerator. Do not allow it to freeze. Throw away any unused medication that is older than 10 days.

Cefuroxime administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Oral suspension: Administer with food. Shake well before use.

Oral tablet: May administer with or without food. Swallow tablet whole (crushed tablet has strong, persistent, bitter taste).

IM: Inject deep IM into large muscle mass.

IV: Inject direct IV over 3 to 5 minutes. Infuse intermittent infusion over 15 to 30 minutes.

Cefuroxime pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Following IV doses of 750 mg and 1.5 g, serum concentrations were approximately 50 and 100 mcg/mL, respectively, at 15 minutes. Therapeutic serum concentrations of approximately 2 mcg/mL or more were maintained for 5.3 hours and 8 hours or more, respectively. There was no evidence of accumulation of Cefuroxime (Cefuroxime (Cefuroxime injection) injection) in the serum following IV administration of 1.5 g doses every 8 hours to normal volunteers. The serum half-life after IV injection is approximately 80 minutes.

Approximately 89% of a dose of Cefuroxime (Cefuroxime (Cefuroxime injection) injection) is excreted by the kidneys over an 8 hour period, resulting in high urinary concentrations.

Intravenous doses of 750 mg and 1.5 g produced urinary levels averaging 1,150 and 2,500 mcg/mL, respectively, during the first 8 hour period.

The concomitant oral administration of probenecid with Cefuroxime (Cefuroxime (Cefuroxime injection) injection) slows tubular secretion, decreases renal clearance by approximately 40%, increases the peak serum level by approximately 30%, and increases the serum half-life by approximately 30%. Cefuroxime (Cefuroxime (Cefuroxime injection) injection) is detectable in therapeutic concentrations in pleural fluid, joint fluid, bile, sputum, bone, cerebrospinal fluid (in patients with meningitis), and aqueous humor.

Cefuroxime (Cefuroxime (Cefuroxime injection) injection) is detectable in therapeutic concentrations in cerebrospinal fluid (CSF) of adults and pediatric patients with meningitis. The following table shows the concentrations of Cefuroxime (Cefuroxime (Cefuroxime injection) injection) achieved in cerebrospinal fluid during multiple dosing of patients with meningitis.

Table 1. Concentrations of Cefuroxime (Cefuroxime (Cefuroxime injection) injection) Achieved in Cerebrospinal Fluid During Multiple Dosing of Patients with Meningitis

Patients Dose Number of

Patients

Mean (Range) CFS

Cefuroxime (Cefuroxime (Cefuroxime injection) injection) Concentrations

(mcg/mL) Achieved Within

8 Hours Post Dose

Pediatric patients

(4 weeks to 6.5 years)

200 mg/kg/day, divided q 6 hours 5 6.6

(0.9-17.3)

Pediatric patients

(7 months to 9 years)

200 to 230 mg/kg/day, divided q 8 hours 6 8.3

(<2-22.5)

Adults 1.5 grams q 8 hours 2 5.2

(2.7-8.9)

Adults 1.5 grams q 6 hours 10 6.0

(1.5-13.5)

Cefuroxime (Cefuroxime (Cefuroxime injection) injection) is approximately 50% bound to serum protein.

Microbiology: Cefuroxime (Cefuroxime (Cefuroxime injection) injection) has in vitro activity against a wide range of gram-positive and gram-negative organisms, and it is highly stable in the presence of beta-lactamases of certain gram-negative bacteria. The bactericidal action of Cefuroxime (Cefuroxime (Cefuroxime injection) injection) results from inhibition of cell-wall synthesis.

Cefuroxime (Cefuroxime (Cefuroxime injection) injection) is usually active against the following organisms in vitro.

Aerobes, Gram-positive

Staphylococcus aureus

Staphylococcus epidermidis

Streptococcus pneumoniae, and

Streptococcus pyogenes (and other streptococci)

NOTE: Most strains of enterococci, e.g., Enterococcus faecalis (formerly Streptococcus faecalis), are resistant to Cefuroxime (Cefuroxime (Cefuroxime injection) injection). Methicillin-resistant staphylococci and Listeria monocytogenes are resistant to Cefuroxime (Cefuroxime (Cefuroxime injection) injection).

Aerobes, Gram-negative

Citrobacter spp.

Enterobacter spp.

Escherichia coli

Haemophilus influenzae (including ampicillin-resistant strains)

Haemophilus parainfluenzae

Klebsiella spp. (including Klebsiella pneumoniae)

Moraxella (Branhamella) catarrhalis (including ampicillin- and cephalothin-resistant strains)

Morganella morganii (formerly Proteus morganii)

Neisseria gonorrhoeae (including penicillinase- and non-penicillinase-producing strains)

Neisseria meningitidis

Proteus mirabilis

Providencia rettgeri (formerly Proteus rettgeri)

Salmonella spp., and Shigella spp.

NOTE: Some strains of Morganella morganii, Enterobacter cloacae, and Citrobacter spp. have been shown by in vitro tests to be resistant to Cefuroxime (Cefuroxime (Cefuroxime injection) injection) and other cephalosporins. Pseudomonas and Campylobacter spp., Acinetobacter calcoaceticus, and most strains of Serratia spp. and Proteus vulgaris are resistant to most first- and second-generation cephalosporins.

Anaerobes: Gram-positive and gram-negative cocci (including Peptococcus and Peptostreptococcus spp.), gram-positive bacilli (including Clostridium spp.), and gram-negative bacilli (including Bacteroides and Fusobacterium spp.).

NOTE: Clostridium difficile and most strains of Bacteroides fragilis are resistant to Cefuroxime (Cefuroxime (Cefuroxime injection) injection).

Susceptibility Tests

Diffusion Techniques

Quantitative methods that require measurement of zone diameters give an estimate of antibiotic susceptibility. One such standard procedure (broth, agar, microdilution) or equivalent with Cefuroxime (Cefuroxime (Cefuroxime injection) injection) powder. The MIC values obtained for bacterial isolates other than Haemophilus spp. and Neisseria gonorrhoeae should be interpreted according to the following criteria:

MIC (mcg/mL) Interpretation
≤ 8 (S) Susceptible
16 (MS) Moderately Susceptible
≥ 32 (R) Resistant

MIC values obtained for Haemophilus spp. should be interpreted according to the following criteria:

MIC (mcg/mL) Interpretation
≤ 4 (S) Susceptible
8 (I) Intermediate
≥ 16 (R) Resistant

MIC values obtained for Neisseria gonorrhoeae should be interpreted according to the following criteria:

MIC (mcg/mL) Interpretation
≤ 1 (S) Susceptible
2 (MS) Moderately Susceptible
≥ 4 (R) Resistant

As with standard diffusion techniques, dilution methods require the use of laboratory control organisms. Standard Cefuroxime (Cefuroxime (Cefuroxime injection) injection) powder should provide the following MIC values.

1. For organisms other than Haemophilus spp. and Neisseria gonorrhoeae:

Organism MIC (mcg/mL)
Staphylococcus aureus ATCC 29213 0.5-2.0
Escherichia coli ATCC 25922 2.0-8.0

2. For Haemophilus spp.:

Organism MIC (mcg/mL)
Haemophilus influenzae ATCC 49766 0.25-1.0

3. For Neisseria gonorrhoeae:

Organism MIC (mcg/mL)
Neisseria gonorrhoeae ATCC 49226 0.25-1.0
Staphylococcus aureus ATCC 29213 0.25-1.0

REFERENCES

1. National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Susceptibility Testing. Third Informational Supplement. NCCLS Document M100-S3, Vol. 11, No. 17, Villanova, PA: NCCLS; 1991.


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References

  1. NCIt. "Cefuroxime: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Cefuroxime 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 Cefuroxime. 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 reports

2 consumers reported administration

When best can I take Cefuroxime, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Cefuroxime should be taken After food. In any case, this may not be the right description on how you ought to take this Cefuroxime. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Cefuroxime can be taken.
Users%
After food1
50.0%
With a meal1
50.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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