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:

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3327896/

2. https://pubmed.ncbi.nlm.nih.gov/2668428/

3. https://pubchem.ncbi.nlm.nih.gov/compound/Ceftriaxone-sodium#section=ATC-Code

4. https://www.medicines.org.uk/emc/product/1361/smpc#gref

5. https://go.drugbank.com/drugs/DB01212