Ceftriaxone Sodium is a salt of Ceftriaxone, which is a third-generation cephalosporin antibiotic. It works by inhibiting the action of penicillin-binding proteins (PBP) in the bacterial cell wall. This product is more effective against gram-negative bacteria than gram-positive ones. It can cross the blood-brain barrier to reach the central nervous system.
This antibiotic is mainly used to manage infections of the skin, lower respiratory tract, urinary tract, bone, and joints. It is also effective for pelvic inflammatory disease and meningitis.
What Is Ceftriaxone Sodium
Definition
It is a sodium salt of Ceftriaxone (beta-lactam), a third-generation cephalosporin. It is associated with the formation of biliary colic and sludge when used in higher doses.
Chemical & Physical Features
CAS Number: 74578-69-1
Molecular Formula: C18H16N8Na2O7S3
Weight: 598.6
Appearance: yellowish, crystalline powder
Structure
Brand Names
Rocephin®
Ceftriaxone Forms and Specifications
This product is available in the mentioned forms and specifications:
Ceftriaxone Sodium Injection
Ceftriaxone Tablet
Ceftriaxone Sodium Powder
Cefotaxime Vs Ceftriaxone
Both Ceftriaxone and Cefotaxime are third-generation cephalosporins that are effective against severe nosocomial gram-negative bacterial infections. They have similar resistance to beta-lactamases and antibacterial spectrum but differ in elimination half-life and serum protein-binding.
According to a few studies, serum protein binding may inhibit therapeutic efficacy by influencing drug distribution and antibacterial activity. So, the action of Ceftriaxone may have a limited in vitro activity than that of cefotaxime.
In a study on serious bacterial infections, the effectiveness of Ceftriaxone was 81%, while that of cefotaxime was 80%. Their safety and adverse effects were also similar.
This suggests that both the products are equally effective and safe for bacterial infections.
Mechanism of Action of Ceftriaxone Sodium
Ceftriaxone sodium works by combating the action of penicillin-binding proteins (PBP) in the bacterial cell wall. Inhibiting this action alters the cross-linkage of peptidoglycan chains, which is fundamental for bacterial cell wall rigidity and strength. All this weakens the cell wall, causing its lysis.
Besides, the product binds to endopeptidases, carboxypeptidases, and transpeptidases in the cell membrane of the bacteria. The mentioned enzymes help bacterial cell division and cell-wall synthesis. Binding with the enzymes prevents them from carrying out their action, resulting in bacterial cell death.
Unlike the first- and second-generation antibiotics, this product is more effective against gram-negative bacteria than gram-positive bacteria.
Ceftriaxone Sodium Manufacturing Process
Manufacturing of Ceftriaxone sodium involves the following steps:
Preparation of acid chloride in dichloromethane with the help of Phosphorous pentachloride
Dichloromethane is evaporated after the formation of acid chloride
Washing the residue with n-heptane
The final residue is dissolved in tetrahydrofuran
The resultant acid chloride is reacted with 7-ACT that gives Cephalosporanic acid
This is dissolved in tetrahydrofuran- water solvent system along with 2 N sodium hydroxide solution
Removal of tetrahydrofuran under vacuum along with acidification of the mass with sulfuric acid and filtration provides a crude residue of N-protected Ceftriaxone acid
Now, this is deprotected in an aqueous solution of thiourea at an ambient temperature and pH between 6.8 to 7.0, followed by overnight cooling
Ceftriaxone acid is formed by adjusting the pH to 2.0 with the help of formic acid
The resultant mass is filtered and dried
Lastly, this acid is converted to Ceftriaxone sodium using sodium-2- ethyl hexanoate solution in acetone-water
Ceftriaxone Sodium Uses
The product is a broad-spectrum third-generation antibiotic. It has a longer half-life as compared to other cephalosporins. It also has high penetrative action into the eyes, meninges, and inner ear.
Ceftriaxone sodium is a popular antibiotic due to its significant action against multidrug-resistant Enterobacteriaceae, the long half-life, and safe adverse effect profile. All this makes it possible to administer it twice daily or once, increasing its convenience.
It is effective against:
Infection of the female reproductive tract
Gonorrhea and chlamydia
Meningitis
Pneumonia
Infections of the ears, urinary tract, bones, abdomen, lungs, skin, blood, and joints
The product is also administered during some surgical procedures to prevent post-surgery infections.
It may also be used for sinusitis, genital sores, endocarditis, Lyme disease, relapsing fever, shigella, typhoid fever, salmonella, and Whipple's disease.
Doctors also prescribe this antibiotic in penicillin-allergic patients with upper respiratory tract or dental infection, especially in those with heart conditions.
Ceftriaxone Sodium Dosage
The usual dose is between 1 to 2 grams a day, not exceeding 4 grams.
The dose also varies depending on the disease condition:
Pneumonia, urinary tract infection, and abdominal infection: 1-2 g/day
Infections of the skin, bones, and joints: 2 g/day
Neutropenic patients with suspected infection and bacterial endocarditis and meningitis
Ceftriaxone Sodium Side Effects
Some common side effects include:
Rash
Nausea
Vomiting
Blood clots
Headache
Vaginal itching or discharge
Change in taste
Diarrhea
Upset stomach
Dizziness
Pain or swelling in your tongue
A lump where the medicine was injected
Sweating
Anemia
Flushing
Ceftriaxone Sodium API Price
The average price of Ceftriaxone Sodium in China is about $10/ kg.
Ceftriaxone Sodium Trihydrate API Manufacturers in China
Many reputed manufacturers and medical product suppliers offer Ceftriaxone Sodium in China. Some of them include:
Zhuhai United Laboratories Trading Company Ltd: t is a leading manufacturer of pharmaceutical products, especially antibiotics. It also possesses the most extensive semi-synthetic penicillin API in quantity. Their products have a significant in both export and domestic markets.
Taizhou Sunzone Pharmaceutical Limited: They are a professional supplier of pharmaceutical products for more than 20 years. Ceftriaxone Sodium is one of the leading products of the company.
Sinopharm Weiqida Pharmaceutical Co., Ltd: They are into the production, development, and sales of pharmaceutical products, mainly amino acid products and antibiotics.
Bulk Production
You can also buy Ceftriaxone Sodium in bulk from PharmaSources.com. It is a vertical e-commerce online destination with many quality global suppliers. PharmSources offers high-quality products to about 211 countries and regions. You can also compare products sold by various distributors and companies and thus make an informed decision.
FAQ
Is Ceftriaxone Sodium A Safe Antibiotic?
Yes, it is comparatively safe for use in most people with infections, and severe side effects are rare.
How Long Does It Take for Ceftriaxone Sodium to Start Working?
Usually, you will start feeling better in a few days after taking the product. If you fail to see the effect, it is best to consult your doctor.
What Kind of Bacteria Does Ceftriaxone Sodium Kill?
Ceftriaxone Sodium is highly effective against infections of the skin, respiratory tract, ears, throat, nose, and urinary tract.
Bacteria that are susceptible to the product are S. pyogenes, coagulase-negative staphylococci, S. pneumoniae, N. gonorrhea, H. influenzae, E. coli, P. mirabilis, M. catarrhalis, and B. burgdorferi.
References:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3327896/
https://pubmed.ncbi.nlm.nih.gov/2668428/
https://pubchem.ncbi.nlm.nih.gov/compound/Ceftriaxone-sodium#section=ATC-Code
https://www.medicines.org.uk/emc/product/1361/smpc#gref
https://go.drugbank.com/drugs/DB01212
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