Actions of Ceftriaxone 1000mg in details
Antibacterial.
Pharmacology: Ceftriaxone 1000mg sodium is a β-lactam antibiotic from the 3rd generation cephalosporin group.
Ceftriaxone 1000mg is a broad-spectrum cephalosporin antibiotic resistant to β-lactamases. It is active against gram-positive aerobes (Staphylococcus metis, Streptococcus, Streptococcus pneumoniae), gram-negative aerobes (Borrelia burgdorferi, Branhamella catarrhalis, Citrobacter freundii, Citrobacter koseri, Enterobacter, Escherichia coli, Haemophilus influenzae, Klebsiella, Morganella morganii, Neisseria including N. meningitidis and N. gonorrheae, Proteus mirabilis, Proteus multocida, Proteus vulgaris, Providencia, Salmonella, Serratia, Shigella, Yersinia) and anaerobes (Clostridium perfringens, Fusobacterium, Peptostreptococcus, Prevotella).
Pharmacokinetics: Distribution: After IV infusion of a single dosage of 1 g, the maximum serum concentration is in average about 168 mg/L after 30 min. After IM injection of the same dosage, a serum peak of 80 mg/L is reached within 2 or 3 hrs.
The IM and IV routes are bioequivalent (similar areas under the curve). Ceftriaxone 1000mg administered by IM route has an absolute bioavailability near 100%. The distribution volume of Ceftriaxone 1000mg is 7-12 L. The diffusion of Ceftriaxone 1000mg is good in the interstitial liquid, the tissues and the organic liquids (especially the cerebrospinal fluid, bile, bones, bronchial secretions, infectious areas of the ENT sphere).
Protein-Binding: The binding of Ceftriaxone 1000mg to serum proteins (albumin) is reversible and saturable. It may vary from 80-95% in the range of therapeutic concentrations. As the albumin rate is lower, the proportion of free Ceftriaxone 1000mg in the interstitial liquid is consequently higher than in the plasma.
Metabolism: Ceftriaxone 1000mg is very poorly metabolized. The intestinal flora only transforms it to inactive metabolites.
Excretion: Ceftriaxone 1000mg is excreted by urinary and biliary routes. The total serum clearance is 10-22 mL/min. The renal clearance is 5-12 mL/min. Fifty to 60% of Ceftriaxone 1000mg is excreted as unchanged form in the urine whereas around 40-50% is excreted in the bile. In adults, the elimination t½ is about 8 hrs long.
Pharmacokinetics in Particular Clinical Conditions: In newborns, the quantity of Ceftriaxone 1000mg remaining in the urine corresponds to about 70% of the administered dosage.
In newborns <8 days, the average elimination t½ is generally 2 or 3 times higher than in young adults; it is shorter in newborns 3-12 months.
In children and newborns, after a single IM injection of 50 mg/kg, the peak serum concentration of Ceftriaxone 1000mg is reached after 5.4 hrs (192±135mg/L).
In children and newborns, after a single IM injection, the diffusion in the middle ear is good with rates higher than the MIC of main bacillus responsible for middle ear acute disease during at least 48 hrs. After a single injection of 50 mg/kg, the total concentration of Ceftriaxone 1000mg in the middle ear liquid is about 5 mg/L after 1.5 hrs (33±20 mg/L), after the 15th hr, stable on the 24th hr (35±12 mg/L) and is still about 19±7mg/L after 48 hrs.
In patients with renal or hepatic insufficiency, Ceftriaxone 1000mg pharmacokinetics is very much different and the elimination t½ is only very poorly increased. If only the renal function is concerned, then the Ceftriaxone 1000mg biliary elimination is increased. If only the hepatic function is concerned, the renal elimination is increased.
How should I take Ceftriaxone 1000mg?
A nurse or other trained health professional will give you Ceftriaxone 1000mg. Ceftriaxone 1000mg is given as a shot into one of your muscles or through a needle placed in one of your veins.
Ceftriaxone 1000mg administration
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Ceftriaxone 1000mg is injected into a muscle, or 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 fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.
Ceftriaxone 1000mg must be given slowly, and the IV infusion can take at least 30 minutes to complete.
You may need to mix Ceftriaxone 1000mg 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 medication. Use only the diluent your doctor has recommended.
After mixing your medicine, you will need to use it within a certain number of hours or days. This will depend on the diluent and how you store the mixture (at room temperature, in a refrigerator, or frozen). Carefully follow the mixing and storage instructions provided with your medicine. Ask your pharmacist if you have questions.
Do not mix Ceftriaxone 1000mg in the same injection with other antibiotics, or with any diluent that contains calcium, including a TPN (total parenteral nutrition) solution.
If you use other injectable medications, be sure to flush your intravenous catheter between injections of each medication.
Use this medicine 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. Ceftriaxone 1000mg will not treat a viral infection such as the common cold or flu.
This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Ceftriaxone 1000mg.
Store unmixed Ceftriaxone 1000mg powder at room temperature, away from moisture, heat, and light.
If your medicine was provided in a frozen form or was frozen after mixing, thaw it in a refrigerator or at room temperature. Do not warm in a microwave or boiling water. Use the medicine as soon as possible after thawing it. Do not refreeze.
Ceftriaxone 1000mg pharmacology
Average plasma concentrations of Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) above single dose values.
Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) concentrations in urine are high, as shown in Table 2.
TABLE 2. Urinary Concentrations of Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) dosages up to 2 g per day. Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) was markedly reduced, suggesting that plasma concentrations of Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) should be monitored in these patients to determine if dosage adjustments are necessary.
TABLE 4. Average Pharmacokinetic Parameters of Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium and dextrose injection ) results from inhibition of cell wall synthesis. Ceftriaxone 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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 1000mg (Ceftriaxone 1000mg sodium 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.
References
- 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).
- 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).
- 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).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
