Ceftriaxone sodium, Rich History, Uses, Side effects, Dosage & 30 brands in Pakistan

May 17, 2024
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Introduction

Ceftriaxone sodium is a semi-synthetic, broad-spectrum cephalosporin antibiotic used to treat bacterial infections. It is administered intravenously or intramuscularly and works by inhibiting the growth of bacteria, ultimately leading to their death. Effective against Gram-positive and Gram-negative bacteria, ceftriaxone sodium is commonly used to treat conditions such as pneumonia, meningitis, septicemia, and skin, soft tissues, and urinary tract infections.

History of Ceftriaxone Sodium

Ceftriaxone sodium, a third-generation cephalosporin antibiotic, has a rich history dating back to the 1980s. Its development marked a significant milestone in the fight against bacterial infections.

Early Beginnings

The first cephalosporin antibiotic, cephalosporin C, was discovered in 1948 by Italian scientist Giuseppe Brotzu.
In the 1960s and 1970s, researchers developed first- and second-generation cephalosporins, which showed improved efficacy against Gram-positive and Gram-negative bacteria.

Development of Ceftriaxone Sodium

In the 1980s, scientists at the Swiss pharmaceutical company Roche (now Hoffman-La Roche) began developing ceftriaxone sodium.
Led by a team of researchers, including Dr. Max Kuhn and Dr. Ernst Gubler, they synthesized and tested various compounds, ultimately leading to the creation of ceftriaxone sodium.
The new antibiotic showed exceptional broad-spectrum activity, stability, and a long half-life, making it an attractive option for treating severe bacterial infections.

Approval and Launch

Ceftriaxone sodium received approval from the US FDA in 1982 under the brand name Rocephin.
It was launched in the US market in 1984 and quickly gained popularity among healthcare professionals due to its efficacy and convenience of administration.

Impact and Legacy

Ceftriaxone sodium revolutionized the treatment of severe bacterial infections, including meningitis, septicemia, and pneumonia.
Its broad-spectrum activity and long half-life made it a preferred choice for many healthcare providers.
The success of ceftriaxone sodium paved the way for the development of subsequent generations of cephalosporin antibiotics.

Molecular Formula

The molecular formula of Ceftriaxone Sodium is C18H16N8Na2O7S3. This formula represents the specific arrangement and number of atoms of each element in a single molecule of Ceftriaxone Sodium.

Chemical Structure

Ceftriaxone Sodium is a β-lactam antibiotic, belonging to the cephalosporin class. Its chemical structure consists of a β-lactam ring fused to a six-membered thiazolidine ring. Attached to this structure are various functional groups, including an aminothiazole moiety and a carboxylate group.

Ceftriaxone Sodium Available Forms

Ceftriaxone sodium is a powerful antibiotic used to treat bacterial infections in various parts of the body. It is available in different forms to suit different administration methods. The main available form of ceftriaxone sodium is a powder that is used to prepare a solution for injection or infusion.

Mechanism of Action

Ceftriaxone Sodium is a broad-spectrum antibiotic belonging to the cephalosporin class. It works by inhibiting bacterial cell wall synthesis, leading to bactericidal activity against susceptible bacteria. Here’s how it works:

Inhibition of Cell Wall Synthesis

Like other β-lactam antibiotics, such as penicillins, cephalosporins, and carbapenems, Ceftriaxone Sodium targets the bacterial cell wall, which is essential for the structural integrity and survival of bacteria. Bacterial cell walls are composed of peptidoglycan, a mesh-like polymer that provides strength and rigidity to the cell membrane.

Binding to Penicillin-Binding Proteins (PBPs)

Ceftriaxone Sodium exerts its antibacterial effects by binding to penicillin-binding proteins (PBPs), which are enzymes involved in the final stages of bacterial cell wall synthesis. PBPs catalyze the cross-linking of peptidoglycan strands, a crucial step in cell wall formation. By binding to PBPs, Ceftriaxone interferes with this cross-linking process, inhibiting the formation of a functional cell wall.

Disruption of Cell Wall Integrity

As a result of PBP binding, the normal process of cell wall synthesis is disrupted. This leads to the weakening of the bacterial cell wall and the accumulation of abnormal cell wall structures.

Cell Lysis and Bacterial Death

The weakened cell wall is unable to withstand the internal osmotic pressure exerted by the bacterial cytoplasm, leading to cell lysis and bacterial death. Without an intact cell wall, bacteria lose their structural integrity and are unable to maintain their shape, ultimately leading to their destruction.

Bactericidal Activity

Ceftriaxone Sodium exhibits bactericidal activity, meaning that it directly kills susceptible bacteria rather than merely inhibiting their growth. By disrupting cell wall synthesis, it effectively targets a wide range of Gram-positive and Gram-negative bacteria, including those responsible for serious infections such as pneumonia, meningitis, sepsis, and intra-abdominal infections.

Broad Spectrum

Ceftriaxone Sodium has a broad spectrum of activity against many bacteria, including Streptococcus pneumoniae, Haemophilus influenzae, Neisseria gonorrhoeae, Escherichia coli, Salmonella spp., Shigella spp., and many others. This broad spectrum of activity makes it a valuable antibiotic for the treatment of various bacterial infections.

Overall, Ceftriaxone Sodium’s mechanism of action involves disrupting bacterial cell wall synthesis, leading to cell lysis and bacterial death, and it is effective against a wide range of Gram-positive and Gram-negative bacteria.

Ceftriaxone Sodium uses

Ceftriaxone Sodium is a versatile antibiotic used to treat a wide range of bacterial infections due to its broad-spectrum activity. Here are some common uses of Ceftriaxone Sodium:

Lower Respiratory Tract Infections: Ceftriaxone Sodium is used to treat bacterial pneumonia, including community-acquired pneumonia and hospital-acquired pneumonia.
Urinary Tract Infections (UTIs): It is effective against UTIs caused by susceptible bacteria, including complicated urinary tract infections and pyelonephritis.
Skin and Soft Tissue Infections: Ceftriaxone Sodium is also used to treat cellulitis, abscesses, wound infections, and other skin and soft tissue infections.
Intra-abdominal Infections: It is used as part of the treatment regimen for intra-abdominal infections, including peritonitis, cholecystitis, and intra-abdominal abscesses.
Sexually Transmitted Infections (STIs): Ceftriaxone Sodium is the first-line treatment for gonorrhea, often administered in combination with another antibiotic to cover for concurrent chlamydial infection.
Bacterial Meningitis: Ceftriaxone Sodium is one of the first-line antibiotics used for the empirical treatment of bacterial meningitis in adults and children, including meningitis caused by Streptococcus pneumonia, Neisseria meningitidis, and Haemophilus influenza-type b.
Bone and Joint Infections: It is also used to treat bacterial osteomyelitis and septic arthritis.
Endocarditis Prophylaxis: Ceftriaxone Sodium is sometimes used for prophylaxis against infective endocarditis in certain high-risk individuals undergoing dental or surgical procedures.
Lyme Disease: In certain cases, Ceftriaxone Sodium is used in the treatment of Lyme disease.
Salmonella and Shigella Infections: Ceftriaxone Sodium is effective against Salmonella and Shigella infections, including typhoid fever and shigellosis.
Septicemia: It is used in the treatment of septicemia, and bloodstream infections caused by susceptible bacteria.
Empirical Antibiotic Therapy: Ceftriaxone Sodium is also used as empirical therapy in hospitalized patients with suspected bacterial infections pending culture and susceptibility results.

Ceftriaxone Sodium uses in Urdu

سیف ٹرائیکسون سوڈیم ایک ورسٹائل اینٹی بائیوٹک ہے جو اس کی وائڈ سپیکٹرم کی سرگرمی کی وجہ سے مختلف بیماریوں کے علاج میں استعمال ہوتا ہے۔ یہاں کچھ عام استعمالات کو درج ذیل طریقے سے بیان کیا گیا ہے

نچلے تنفسی نظامی انفیکشن: سیف ٹرائیکسون سوڈیم کا استعمال بیمار پنومونیا، جو کہ مجتمعہ حاصل پنومونیا اور ہسپتال میں حاصل پنومونیا شامل ہے، کے علاج میں کیا جاتا ہے۔

مثانی نظامی انفیکشن (یو ٹی آئیز): یہ مثانی نظامی انفیکشن جیسے کہ پیچیدہ مثانی نظامی انفیکشن اور پیلونیفرائٹس کے علاج میں موثر ہے۔

جلد اور نرم انسجامات کی انفیکشنات: سیف ٹرائیکسون سوڈیم سیلیولائٹس، ایبسس، زخمی انفیکشنات اور دیگر جلد اور نرم انسجامی انفیکشنات کے علاج میں استعمال کیا جا سکتا ہے۔

اندری ایبڈومنل انفیکشنز: یہ پیٹ کے اندری انفیکشنات، جیسے کہ پیریٹونائٹس، کولیسٹائٹس، اور اندری ایبڈومنل ایبسیسز کے علاج کے حصے کے طور پر استعمال ہوتا ہے۔

جنسی طریقے سے منتقل ہونے والی انفیکشنز (ایس ٹی آئیز): سیف ٹرائیکسون سوڈیم گونوریا کے لیے پہلی لائن کا علاج ہے، جو کہ عموماً دوسرے اینٹی بائیوٹک کے ساتھ ملا کر ایک ساتھ استعمال کیا جاتا ہے تاکہ دوسری بکٹیریائی انفیکشن بھی کور کیا جا سکے۔

بیکٹیریا میننجیٹس: سیف ٹرائیکسون سوڈیم بچوں اور بڑوں میں بیکٹیریا میننجیٹس کے تشخیصی علاج کے لئے استعمال ہوتا ہے، جو کہ سٹریپٹوکوکس پنیومونیئے، نائیسیریا میننجٹیڈس، اور ہیموفیلس انفلونزا تائپ بی کیو سے پیدا ہونے والی میننجیٹس کی علاج کے لئے استعمال ہوتا ہے۔

ہڈی اور جوڑوں کی انفیکشنز: یہ بیکٹیریاکے بون اور جوڑوں کی انفیکشن کے علاج میں استعمال کیا جاتا ہے۔

انڈوکارڈائٹس کی پیشگوئی: سیف ٹرائیکسون سوڈیم کو کچھ خاص افراد میں جس کی میں اندوکارڈائٹس کے خلاف پیشگوئی کے لئے استعمال کیا جاتا ہے، جو دندانوں یا جراحی اعمال کے دوران دندانہ چرھانے یا جراحتی اعمال ک

Dosage and Administration

Ceftriaxone Sodium Dosage for Treating Bacterial Infections

The optimal dosage of ceftriaxone sodium for treating bacterial infections depends on several factors, including the severity of the infection, the patient’s age and weight, renal function, and the susceptibility of the causative organism. Here are general dosage guidelines for various indications:

Community-Acquired Pneumonia (CAP)

Adults: The typical dosage is 1 to 2 grams once daily, administered intravenously or intramuscularly. Severe cases may require higher doses.
Pediatric Patients: The recommended dosage is 50 to 100 mg/kg once daily, not to exceed 4 grams per day. Pediatric dosages are typically administered intravenously.

Urinary Tract Infections (UTIs)

Adults: A dosage of 1 to 2 grams once daily is often sufficient. In complicated UTIs or pyelonephritis, higher doses may be required.
Pediatric Patients: The dosage is generally 50 to 100 mg/kg once daily, not to exceed 4 grams per day, administered intravenously.

Meningitis

Adults and Pediatric Patients: For the treatment of bacterial meningitis, ceftriaxone is typically administered in high doses of 2 to 4 grams every 12 hours. Dosages may vary based on the causative organism and the patient’s age.

Intra-abdominal Infections

Adults: The recommended dosage is 1 to 2 grams once daily, administered intravenously or intramuscularly. In severe cases, higher doses may be necessary.
Pediatric Patients: Dosages typically range from 50 to 100 mg/kg once daily, not to exceed 4 grams per day, administered intravenously.

Septicemia/Bacteremia

Adults: A dosage of 1 to 2 grams once daily is commonly used. Higher doses may be required in severe cases.
Pediatric Patients: Dosages range from 50 to 100 mg/kg once daily, not to exceed 4 grams per day, administered intravenously.

Gonorrhea

Adults: The recommended dosage is a single intramuscular injection of 250 mg for uncomplicated gonorrhea. For dual therapy with azithromycin, a single dose of ceftriaxone 250 mg plus azithromycin 1 gram orally is recommended.

Side effects

Ceftriaxone Sodium, like other antibiotics, can cause side effects. Here are some possible side effects to be aware of:

Common side effects

Pain, swelling, or redness at the injection site
Allergic reactions, such as rash, itching, or hives
Diarrhea or stomach cramps
Vomiting
Headache
Dizziness or drowsiness
Fever
Chills

Less common side effects

Blood disorders, such as anemia, low white blood cell count, or low platelet count
Kidney problems, such as increased creatinine or kidney failure
Seizures or convulsions
Yellowing of the skin and eyes (jaundice)
Easy bruising or bleeding
Shortness of breath or wheezing
Swelling of the face, lips, tongue, or throat

Rare but serious side effects

Anaphylaxis (a severe allergic reaction)
Stevens-Johnson syndrome (a life-threatening skin and mucous membrane disorder)
Toxic epidermal necrolysis (a life-threatening skin condition)
Blood clotting disorders
Pseudomembranous colitis (a serious gut infection)
Cardiac arrest or heart failure

Ceftriaxone sodium during pregnancy

The use of ceftriaxone sodium during pregnancy is generally considered safe and necessary to treat serious bacterial infections that pose risks to both the mother and the fetus. However, like all medications, it should be used with caution and only when the potential benefits outweigh the potential risks.

Safety Profile: Ceftriaxone belongs to the FDA pregnancy category B, indicating that animal reproduction studies have not demonstrated a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. While there is limited human data available, extensive clinical experience with ceftriaxone use during pregnancy has not shown an increased risk of birth defects or adverse pregnancy outcomes.

Treatment of Infections: In pregnant women, ceftriaxone may be prescribed to treat serious bacterial infections such as pneumonia, urinary tract infections, intra-abdominal infections, and bacterial meningitis. These infections, if left untreated, can lead to complications that may adversely affect maternal and fetal health.

Syphilis Treatment: Ceftriaxone is also commonly used as part of the treatment regimen for syphilis in pregnant women. It is the preferred antibiotic for this purpose due to its efficacy in treating syphilis and its ability to cross the placental barrier to reach the fetus.

Precautions and Warnings

Ceftriaxone Sodium is a powerful antibiotic used to treat a variety of bacterial infections. Like any medication, it comes with its own set of precautions and warnings. Here are some important precautions and warnings to be aware of:

Allergic Reactions: Patients should be monitored closely for signs of allergic reactions, including rash, itching, swelling, dizziness, or difficulty breathing. Immediate medical attention is necessary if any of these symptoms occur.

Severe Diarrhea: Ceftriaxone Sodium can disrupt the natural balance of bacteria in the gut, leading to severe diarrhea. If diarrhea occurs and persists, patients should contact their healthcare provider as this may be a sign of a more serious condition called Clostridium difficile-associated diarrhea.

Biliary Sludge and Calculi: Ceftriaxone Sodium can cause precipitation of ceftriaxone calcium salt in the gallbladder, leading to the formation of biliary sludge, which may progress to biliary calculi. This is more common in pediatric patients. Monitoring is recommended, especially in those receiving prolonged therapy.

Thrombophlebitis: Ceftriaxone Sodium can cause thrombophlebitis at the site of intravenous infusion, particularly in elderly patients or those with limited venous access. Rotation of infusion sites and proper dilution of the drug are recommended to minimize the risk.

Hypersensitivity Reactions: Serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, have been reported with cephalosporin antibiotics. Patients with a history of hypersensitivity to cephalosporins should be closely monitored during therapy.

Renal Impairment: Ceftriaxone Sodium should be used with caution in patients with renal impairment, as it is primarily excreted via the kidneys. Dosage adjustment may be necessary in these patients to prevent accumulation and potential toxicity.

Hematologic Effects: Ceftriaxone Sodium can affect blood clotting parameters, leading to thrombocytopenia or coagulation disorders. Patients should be monitored for signs of bleeding or bruising, especially if they have pre-existing coagulation disorders.

Superinfection: Prolonged use of Ceftriaxone Sodium may result in the overgrowth of non-susceptible organisms, leading to superinfection. If new infections occur during therapy, appropriate measures should be taken.

Neurotoxicity: Rarely, Ceftriaxone Sodium has been associated with neurotoxicity, particularly in patients with renal impairment, preterm infants, or those receiving high doses. Symptoms may include altered mental status, seizures, and/or coma.

Disulfiram-like Reaction: Ceftriaxone Sodium contains a small amount of ethanol. In patients who cannot tolerate even small amounts of alcohol, a disulfiram-like reaction (flushing, headache, nausea, vomiting) may occur if alcohol is consumed while on therapy.

Drugs interaction

Ceftriaxone Sodium, like other antibiotics, can interact with various drugs, potentially altering their efficacy or increasing the risk of adverse effects. Here are some notable interactions:

Calcium-containing Products: Ceftriaxone Sodium should not be mixed or co-administered with calcium-containing products (e.g., calcium-containing intravenous solutions or oral calcium supplements) in neonates due to the risk of precipitation and formation of ceftriaxone-calcium precipitates, which can lead to fatal outcomes.
Anticoagulants (e.g., Warfarin): Ceftriaxone Sodium may potentiate the effects of anticoagulants by interfering with vitamin K metabolism or displacing protein-bound warfarin. Close monitoring of prothrombin time (PT) or international normalized ratio (INR) is recommended when ceftriaxone is administered concomitantly with anticoagulants.
Probenecid: Concomitant use of probenecid may increase and prolong the serum levels of ceftriaxone by inhibiting its renal tubular secretion. This interaction may result in enhanced antibiotic activity and a prolonged half-life of ceftriaxone. Dosage adjustments may be necessary.
Aminoglycosides: Concurrent administration of ceftriaxone with aminoglycosides (e.g., gentamicin, amikacin) may increase the risk of nephrotoxicity and ototoxicity. Caution is advised, and renal function should be closely monitored when these drugs are used together.
Oral Contraceptives: Ceftriaxone Sodium may reduce the efficacy of hormonal contraceptives (e.g., birth control pills) by altering gut flora and impairing enterohepatic circulation of estrogen. Additional non-hormonal contraceptive methods should be considered during antibiotic therapy and for several weeks thereafter.
Loop Diuretics (e.g., Furosemide): Ceftriaxone Sodium, when administered with loop diuretics, may increase the risk of nephrotoxicity, particularly in patients with pre-existing renal impairment. Renal function should be monitored closely, especially in elderly patients.
NSAIDs (Nonsteroidal Anti-inflammatory Drugs): Concurrent use of NSAIDs with ceftriaxone may increase the risk of nephrotoxicity and gastrointestinal irritation. Patients should be monitored for signs of renal dysfunction, such as elevated serum creatinine levels and decreased urine output.
Vancomycin: When used concurrently, ceftriaxone may enhance the nephrotoxic effects of vancomycin. Renal function should be closely monitored, especially in patients with pre-existing renal impairment.

Ceftriaxone sodium brands in Pakistan

In Pakistan, Ceftriaxone Sodium is available under various brand names. Here are some common brands of Ceftriaxone Sodium formulations that are found in the Pakistani market:

Ceftrex – Getz Pharma

Ceftiax – PharmEvo Pharma

Rocephin – Roche Pharma

Cefaxone – Beximco Pharmaceuticals Ltd.

Cefix – Hilton Pharma

Ceftria – Atco Laboratories Ltd.

Ceftum – GlaxoSmithKline (GSK)

Cefzim – Pfizer Pharma

Cefaxin – SK+F Pharmaceuticals

Ceftri – Sami Pharmaceuticals Pvt Ltd.

Ceftron – Highnoon Laboratories Ltd.

Cefriax – Efroze Chemical Industries Pvt Ltd.

Cefatox – Biocare Pharmaceuticals

Cefzon – Zonex Pharmaceuticals

Cefmax – Platinum Pharmaceuticals Pvt Ltd.

Cefazone – Searle Company Limited

Cefxon – Ferozsons Laboratories Ltd.

Ceftrone – Novartis Pharma

Tricef – Hilton Pharma

Cefaxon – Sami Pharmaceuticals Pvt Ltd.

Cefixime – Martin Dow Pharmaceuticals

Cefteral – Martin Dow Pharmaceuticals

Ceftriforce – Pharmevo

Cefspid – Pharmevo

Cefzole – Globe Pharmaceuticals Ltd.

Cefthro – Medicaids Pakistan Pvt Ltd.

Ceftam – Getz Pharma

Ceftral – Obsurge Biotech Ltd.

Cef-3 – Themis Pharmaceuticals

Brands available in other countries

Certainly! Ceftriaxone Sodium is a widely used antibiotic, and it is available under various brand names in different countries around the world. Here are some additional brands of Ceftriaxone Sodium available in other countries:

Cefaxona: This brand is available in some Spanish-speaking countries, including Spain and parts of Latin America.

Ceftriax: This brand is available in some European countries, such as Germany and Switzerland.

Fortum: Fortum is a brand of Ceftriaxone Sodium available in several European countries, including Sweden, Norway, Denmark, and Finland.

Tricef: Tricef is also available in Bangladesh, in addition to being available in Pakistan.

Rotexmedica Ceftriaxone: This brand is available in Germany.

Ceftriaxon-Teva: This brand is available in some European countries where Teva Pharmaceuticals operates.

Ceftriaxone Medochemie: This brand is available in various countries where Medochemie operates, including Cyprus, Greece, and other European and international markets.

Ceftriaxone Sandoz: This brand is available in some countries where Sandoz operates, including parts of Europe and other international markets.

Ceftriaxone Teva: This brand is available in some countries where Teva Pharmaceuticals operates.

Ceftriaxone Fresenius Kabi: This brand is available in various countries where Fresenius Kabi operates, including parts of Europe, Asia, and other international markets.

These are just a few examples of Ceftriaxone Sodium brands available in other countries.