Ceftriaxone Actions

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Actions of Ceftriaxone 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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Ceftriaxone works by inhibiting the mucopeptide synthesis in the bacterial cell wall. The beta-lactam moiety of Ceftriaxone binds to carboxypeptidases, endopeptidases, and transpeptidases in the bacterial cytoplasmic membrane. These enzymes are involved in cell-wall synthesis and cell division. By binding to these enzymes, Ceftriaxone results in the formation of of defective cell walls and cell death.

How should I take Ceftriaxone?

A nurse or other trained health professional will give you Ceftriaxone. Ceftriaxone is given as a shot into one of your muscles or through a needle placed in one of your veins.

Ceftriaxone 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.

IM: Inject deep IM into large muscle mass; a concentration of 250 mg/mL or 350 mg/mL is recommended for all vial sizes except the 250 mg size (250 mg/mL is suggested); can be diluted with 1:1 water or 1% lidocaine for IM administration only.

IV: Infuse as an intermittent infusion over 30 minutes. IV push administration over 1 to 4 minutes has been reported (concentration: 100 mg/mL), primarily in patients outside the hospital setting (Baumgartner 1983; Garrelts 1988; Poole 1999), although a 2 g dose administered IV push over 5 minutes resulted in tachycardia, restlessness, diaphoresis, and palpitations in one patient (Lossos 1994). Do not coadminister with calcium-containing solutions.

Ceftriaxone 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.
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Average plasma concentrations of Ceftriaxone (Ceftriaxone and dextrose injection ) following a single 30-minute intravenous (IV) infusion of a 0.5,1 or 2 g dose in healthy subjects are presented in Table 1.

TABLE 1. Ceftriaxone (Ceftriaxone and dextrose injection ) Plasma Concentrations After Single Dose Administration

Dose/Route Average Plasma Concentrations (µ/mL)
0.5 hr 1 hr 2hr 4hr 6hr 8hr 12hr 16 hr 24 hr
0.5 g IV* 82 59 48 37 29 23 15 10 5
1 g IV* 151 111 88 67 53 43 28 18 9
2 g IV* 257 192 154 117 89 74 46 31 15
*IV doses were infused at a constant rate over 30 minutes.

Multiple IV doses ranging from 0.5 to 2 g at 12- to 24-hour intervals resulted in 15% to 36% accumulation of Ceftriaxone (Ceftriaxone and dextrose injection ) above single dose values.

Ceftriaxone (Ceftriaxone and dextrose injection ) concentrations in urine are high, as shown in Table 2.

TABLE 2. Urinary Concentrations of Ceftriaxone (Ceftriaxone and dextrose injection ) After Single Dose Administration

Dose/Route Average Urinary Concentrations (µ/mL)
0-2 hr 2-4 hr 4-8 hr 8-12 hr 12-24 hr 24-48 hr
0.5 g IV 526 366 142 87 70 15
1 g IV 995 855 293 147 132 32
2g lV 2692 1976 757 274 198 40

Thirty-three percent to 67% of a Ceftriaxone (Ceftriaxone and dextrose injection ) dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds. After a 1 g IV dose, average concentrations of Ceftriaxone (Ceftriaxone and dextrose injection ), determined from 1 to 3 hours after dosing, were 581 µg/mL in the gallbladder bile, 788 µglml in the common duct bile, 898 µg/mL in the cystic duct bile, 78.2 µg/g in the gallbladder wall and 62.1 µg/mL in the concurrent plasma.

Over a 0.15 to 3 g dose range in healthy adult subjects, the values of elimination half-life ranged from 5.8 to 8.7 hours; apparent volume of distribution from 5.78 to 13.5 L; plasma clearance from 0.58 to 1.45 L/hour; and renal clearance from 0.32 to 0.73 L/hour. Ceftriaxone (Ceftriaxone and dextrose injection ) is reversibly bound to human plasma proteins, and the binding decreased from a value of 95% bound at plasma concentrations of < 25 µg/mL to a value of 85% bound at 300 µg/mL. Ceftriaxone (Ceftriaxone and dextrose injection ) crosses the blood placenta barrier.

The average values of maximum plasma concentration, elimination half-life, plasma clearance and volume of distribution after a 50 mg/kg IV dose and after a 75 mg/kg IV dose in pediatric patients suffering from bacterial meningitis are shown in Table 3. Ceftriaxone (Ceftriaxone and dextrose injection ) penetrated the inflamed meninges of infants and pediatric patients; CSF concentrations after a 50 mg/kg IV dose and after a 75 mg/kg IV dose are also shown in Table 3.

TABLE 3. Average Pharmacokinetic Parameters of Ceftriaxone (Ceftriaxone and dextrose injection ) in Pediatric Patients With Meningitis

50 mg/kg IV 75 mg/kq IV
Maximum Plasma Concentrations (µg/mL) 216 275
Elimination Half-life (hr) 4.6 4.3
Plasma Clearance (mL/hr/kg) 49 60
Volume of Distribution (mL/kg) 338 373
CSF Concentration — inflamed meninges (µg/mL) 5.6 6.4
Range (µ/mL) 1.3-18.5 1.3-44
Time after dose (hr) 3.7 (±1.6) 3.3 (±1.4)

Compared to that in healthy adult subjects, the pharmacokinetics of Ceftriaxone (Ceftriaxone and dextrose injection ) were only minimally altered in elderly subjects and in patients with renal impairment or hepatic dysfunction (Table 4); therefore, dosage adjustments are not necessary for these patients with Ceftriaxone (Ceftriaxone and dextrose injection ) dosages up to 2 g per day. Ceftriaxone (Ceftriaxone and dextrose injection ) was not removed to any significant extent from the plasma by hemodialysis. In 6 of 26 dialysis patients, the elimination rate of Ceftriaxone (Ceftriaxone and dextrose injection ) was markedly reduced, suggesting that plasma concentrations of Ceftriaxone (Ceftriaxone and dextrose injection ) should be monitored in these patients to determine if dosage adjustments are necessary.

TABLE 4. Average Pharmacokinetic Parameters of Ceftriaxone (Ceftriaxone and dextrose injection ) in Humans

Subject Group Elimination

Half-Life

(hr)

Plasma

Clearance

(L/hr)

Volume of

Distribution

(L)

Healthy Subjects 5.8-8.7 0.58-1.45 5.8-13.5
Elderly Subjects (mean age, 70.5 yr) 8.9 0.83 10.7
Patients with Renal Impairment
Hemodialysis Patients (0-5 mL/min)* 14.7 0.65 13.7
Severe (5-15 mL/min) 15.7 0.56 12.5
Moderate (16-30 mL/min) 11.4 0.72 11.8
Mild (31-60 mL/min) 12.4 0.70 13.3
Patients With Liver Disease 8.8 1.1 13.6
*Creatinine clearance.

Microbiology

The bactericidal activity of Ceftriaxone (Ceftriaxone and dextrose injection ) results from inhibition of cell wall synthesis. Ceftriaxone (Ceftriaxone and dextrose injection ) has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria.

Ceftriaxone (Ceftriaxone and dextrose injection ) has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections described in the INDICATIONS AND USAGE section.

Aerobic gram-negative microorganisms

Acinetobacter calcoaceticus

Enterobacter aerogenes

Enterobacter cloacae

Escherichia coli

Haemophilus influenzae (including ampicillin-resistant and beta-lactamase producing strains)

Haemophilus parainfluenzae

Klebsiella oxytoca

Klebsiella pneumoniae

Moraxella catarrhalis (including beta-lactamase producing strains)

Morganella morganii

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

Neisseria meningitidis

Proteus mirabilis

Proteus vulgaris

Serratia marcescens

Ceftriaxone (Ceftriaxone and dextrose injection ) is also active against many strains of Pseudomonas aeruginosa.

NOTE: Many strains of the above organisms that are multiply resistant to other antibiotics, e.g., penicillins, cephalosporins, and aminoglycosides, are susceptible to Ceftriaxone (Ceftriaxone and dextrose injection ).

Aerobic gram-positive microorganisms

Staphylococcus aureus (including penicillinase-producing strains)

Staphylococcus epidermidis

Streptococcus pneumoniae

Streptococcus pyogenes

Viridans group streptococci

NOTE: Methicillin-resistant staphylococci are resistant to cephalosporins, including Ceftriaxone (Ceftriaxone and dextrose injection ). Most strains of Group D streptococci and enterococci, e.g., Enterococcus (Streptococcus) faecalis, are resistant.

Anaerobic microorganisms

Bacteroides fragilis

Clostridium species

Peptostreptococcus species

NOTE: Most strains of Clostridium difficile are resistant.

The following in vitro data are available, but their clinical significance is unknown. Ceftriaxone (Ceftriaxone and dextrose injection ) exhibits in vitro minimal inhibitory concentrations (MICs) of ≤ 8 µg/mL or less against most strains of the following microorganisms, however, the safety and effectiveness of Ceftriaxone (Ceftriaxone and dextrose injection ) in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.

Aerobic gram-negative microorganisms

Citrobacter diversus

Citrobacterfreundii

Providencia species (including Providencia rertgeri)

Salmonella species (including Salmonella typhi)

Shigella species

Aerobic gram-positive microorganisms

Streptococcus agalactiae

Anaerobic microorganisms

Prevotella (Bacteroides) bivius

Porphyromonas (Bacteroides) melaninogenicus

Susceptibility Tests

Dilution Techniques

Quantitative methods are used to determine antimicrobial minimal inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized procedure. testing method:

Method Microoraanism ATCC®# MIC (µq/mL)
Agar Bacteroides fragilis 25285 32-128
Bacteroides thetaiotaomicron 29741 64-256
Broth Bacteroides thetaiotaomicron 29741 32-128

REFERENCES

1. National Committee for Clinical Laboratory Standards, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically; Approved Standard-Fifth Edition. NCCLS document M7-A5 (ISBN 1-56238-309-9). NCCLS, Wayne, PA 19087-1898,2000.

2. National Committee for Clinical Laboratory Standards, Supplemental Tables. NCCLS document M100-S10(M7) (ISBN 1-56238-309-9). NCCLS, Wayne, PA 19087-1898,2000.

3. National Committee fof'Clinical Laboratory Standards, Performance Standards for Antimicrobial Disk Susceptibility Teste; Approved Standard-Seventh Edition. NCCLS document M2-A7 (ISBN 1-56238-393-0). NCCLS, Wayne, PA 19087-1898,2000.

4. National Committee for Clinical Laboratory Standards, Methods for Antimicrobial Susceptibility Testing of Anaerobic Bacterial; Approved Standard-Fourth Edition. NCCLS document M11-A4 (ISBN 1-56238-210-1). NCCLS, Wayne, PA 19087-1898,1997.


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References

  1. DailyMed. "CEFTRIAXONE SODIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Ceftriaxone: 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).
  3. EPA DSStox. "Ceftriaxone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Ceftriaxone 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 Ceftriaxone. 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

1 consumer reported administration

When best can I take Ceftriaxone, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Ceftriaxone should be taken After food. In any case, this may not be the right description on how you ought to take this Ceftriaxone. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Ceftriaxone can be taken.
Users%
After food1
100.0%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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