Ceftriaxone Sodium 250mg/500mg/1g/2g: Full Prescription Information - pharmacyteach

Ceftriaxone
Injection

 

 

COMPOSITION:

 

Each vial of Ceftriaxone 250mg IM/IV contains: Sterile Powder of Ceftriaxone Sodium USP equivalent to Ceftriaxone 250mg

Each vial of Ceftriaxone 500mg IM/IV contains: Sterile Powder of Ceftriaxone Sodium USP equivalent to Ceftriaxone 500mg

Each vial of Ceftriaxone 1g IV contains: Sterile Powder of Ceftriaxone Sodium USP equivalent to Ceftriaxone 19

Each vial of Ceftriaxone 2g IV contains: Sterile Powder of Ceftriaxone Sodium USP equivalent to Ceftriaxone 29.

 Learn About: List of antibacterial drugs 

Brands/tread name

Oxidil injection,

Rocephin injection,

 

DESCRIPTION:

Ceftriaxone sodium is a semi-synthetic 3d 3rd-generation cephalosporin antibiotic, with high stability to β-lactamases, broad-spectrum activity, effectiveness, and convenience of long action. 

 

PHARMACOLOGY:

 

Pharmacodynamic properties:

The bactericidal activity of Ceftriaxone results from inhibition of bacterial cell wall synthesis. Ceftriaxone exerts in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Ceftriaxone is highly stable to most beta-lactamases, both penicillinases and cephalosporinases of gram-positive and gram-negative bacteria

 

Pharmacokinetic properties:

The pharmacokinetics of Ceftriaxone is non-linear, and all basic pharmacokinetic parameters except the elimination half-life are dose dependent if based on total drug concentrations

 

Absorption

The maximum plasma concentration after a single I.M. dose of 1g is about 81mg/L and is reached in 2-3 hours after administration. The area under the plasma concentration time curve after 1 M. administration is equivalent to that after IV. Administration of an equivalent dose, indicating 100% bioavailability of intramuscularly administered Ceftriaxone

 

Distribution

Ceftriaxone has shown excellent tissue and body fluid penetration after a dose of 1-2g, concentrations well above the minimal inhibitory concentrations of most pathogens responsible for infection are detectable for more than 24 hours in over 60 tissues or body fluids including lung, heart, biliary tract/liver, tonsil, middle ear and nasal mucosa, bone as well as cerebrospinal, pleural, prostatic and synovial fluids. On intravenous administration, Ceftriaxone diffuses rapidly into the interstitial fluids, where bactericidal concentrations against susceptible organisms are maintained for 24 hours

 

Protein binding

Ceftriaxone is reversibly bound to albumin, and the binding decreases with the increase in concentration, e.g., from 95% binding at plasma concentrations of <100mg/l to 85% binding at 300mg/l. Owing to the lower albumin content, the proportion of free Ceftriaxone in interstitial fluid is correspondingly higher than in plasma.

 

Penetration into particular tissues

Ceftriaxone penetrates into the inflamed meninges of neonates, infants and children: Ceftriaxone concentrations exceed 1.4 mg/l in the CSF 24 hours after I.V. injection of Ceftriaxone in doses of 50-100mg/kg (neonates and infants respectively). Peak concentration in CSF is reached about 4 hours after I.V. injection and gives an average value of 18mg/l. Mean CSF levels are 17% of plasma concentrations in patients with bacterial meningitis and 4% in patients with aseptic meningitis. In adult meningitis patients, administration of 50mg/kg leads within 2-24 hours to CSF concentrations several times higher than the minimum inhibitory concentrations required for the most common meningitis pathogens. Ceftriaxone crosses the placental barrier and is excreted in the breast milk at low concentrations

 

Metabolism

Ceftriaxone is not metabolized systemically, but is converted to inactive metabolites by the gut flora

 

Elimination

Total plasma clearance is 10- 22ml/min, Renal clearance is 5- 12ml/min. 50-60% of Ceftriaxone is excreted unchanged in the urine, while 40-50% is excreted unchanged in the bile. The elimination half-life in adults is about 8 hours

 Find creatinine clearance using an online creatinine clearance calculator. 

Indications and uses:

Lower respiratory tract infection caused by Streptococcus pneumoniae, Staphylococcus aureus, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Escherichia coli, Enterobacter aerogenes, Proteus mirabilis, of Serratia marcescens

 

Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae (including β-lactamase producing strains) or Moraxella catarrhalis (including β-lactamase producing strains)

 

Skin and Skin Structure Infections caused by Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Viridans group streptococci, Escherichia coli, Enterobacter cloacae, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Morganella morganii, Pseudomonas aeruginosa, Serratia marcescens, Acinetobacter calcoaceticus, Bacteroides fragilis or Peptostreptococcus species Urinary Tract Infections (complicated and uncomplicated) caused by Escherichia coli, Proteus mirabilis, Proteus vulgaris, Morganetta morganii or Klebsiella pneumoniae Uncomplicated Gonorrhoea (cervical/urethral and rectal) caused by Neisseria gononhoeae, including both penicillinase and non-penicillinase producing strains, and pharyngeal gonorrhoea caused by non-penicillinase producing strains of Neisseria gonorrhoeae

 

Bacterial Septicemia caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae, or Klebsiella pneumoniae. Bone and Joint Infections caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, or Enterobacter species

 

Intra-abdominal Infections caused by Escherichia coli, Klebsiella pneumoniae, Bacteroides fragilis, Clostridium species (Note: most strains of Clostridium difficile are resistant) or Peptostreptococcus species

 

Meningitis caused by Haemophilus influenzae, Neisseria meningitidis, or Streptococcus pneumoniae. Ceftriaxone has also been used successfully in a limited number of cases of meningitis and shunt infection caused by Staphylococcus Epidermidis and Escherichia coli.

 

Surgical Prophylaxis for preoperative use (surgical prophylaxis), a single dose of 19% administered intravenously % to 2 hours before surgery is recommended. Note: Methicillin-resistant Staphylococci are resistant to cephalosporin, including Ceftriaxone. Most strains of Group D streptococci and enterococci, e.g., Enterococcus (Streptococcus) faecalis, are resistant.

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DOSAGE AND ADMINISTRATION:

 

Administration

Ceftriaxone may be administered intravenously or intramuscularly.

 General Instructions

Do not use diluents containing calcium, such as Ringer's solution or Hartmann's solution, to reconstitute Ceftriaxone vials or to further dilute a reconstituted vial for EV administration because a precipitate can form. Precipitation of Ceftriaxone-calcium can also occur when Ceftriaxone is mixed with calcium-containing solutions in the same IV Administration line. Ceftriaxone must not be administered simultaneously with calcium-containing IV solutions, including continuous calcium-containing infusions such as parenteral nutrition via a Y-site. However, in patients other than neonates, Ceftriaxone and calcium-containing solutions may be administered sequentially of one another if the infusion lines are thoroughly flushed between infusions with a compatible fluid.

 

There have been no reports of an interaction between Ceftriaxone and oral calcium-containing products or intersection between intramuscular Ceftriaxone and calcium containing products (I.V. or oral).

 

 Method of Administration

As a general rule, the solutions should be used immediately after preparation. Reconstituted solutions retain their physical and chemical stability for 6 hours al room temperature for 24 hours in the refrigerator at 2-8°C The solutions range in color from saffron yellow to amber, depending on the concentration and length of storage. The colonization of the solutions is of no significance for the efficacy or tolerance of the intramuscular injection drug

 

For IM injection, Ceftriaxone 250mg or 500mg is dissolved in 2ml and Ceftriaxone 10 in 3.5 mL of 15% lignocaine solution and injected well within the body of a relatively large muscle. No more than 1g should be injected at one site. The lignocaine solution should never be administered intravenously. Intravenous Injection

 

For IV injection, Ceftriaxone 250mg or 500mg is dissolved in 5 mL, Ceftriaxone 19 in 10ml and 2g in 20 mL sterile water for injection. The intravenous administration should be given over 2-4 minutes. Intravenous Infusion

 

The infusion should be given over at least 30 minutes. For IV infusion, 2g Ceftriaxone is dissolved in 40ml of one of the following calcium-free infusion solutions, sodium chloride 0.9%, sodium chloride 0.45% + dextrose 2.5%, dextrose 5%, dextrose 10% dextran 6% in dextrose 5%, hydroxyethyl starch 6-10%, water for injection. Ceftriaxone solutions should not be mixed with or piggy-backed into solutions containing other antimicrobial drugs or into diluent solutions other than those listed above, owing to possible incompatibility

 

Dosage:

Ceftriaxone may be administered by deep intramuscular injection, slow intravenous injection, or as a slow intravenous infusion after reconstitution of the solution according to the directions given below:

Dosage and mode of administration should be determined by the severity of the infection, susceptibility of the causative organism, and the patient's condition. Under most circumstances, a once-daily dose or, in the specified indications, a single dose will give satisfactory therapeutic results.

Standard dosage. Standard therapeutic dosage for adults and children (12 years and over) is 1g once daily; in severe cases or in infections caused by moderately sensitive organisms, the dosage may be raised to 4g once daily. Duration of therapy

The duration of therapy varies according to the course of the disease. As with antibiotic therapy in general, administration of Ceftriaxone should be continued for a minimum of 48-72 hours after the patient has become afebrile or evidence of bacterial eradication has been obtained. Combination therapy

In severe, life-threatening infections, the combination of Ceftriaxone sodium with aminoglycosides is indicated without awaiting the results of sensitivity tests. Because of physical incompatibility, the two drugs must be administered separately, not mixed in one syringe. Infections with Pseudomonas aeruginosa may require concomitant treatment

 

Special dosage instructions

Patients with Renal Impairment. In patients with impaired renal function, there is no need to reduce the dosage of Ceftriaxone provided liver function is intact. Only in cases of pre-terminal renal failure (creatinine clearance < 10 mL per minute) should the daily dosage be limited to 2g or less. In severe renal impairment accompanied by hepatic insufficiency, the plasma concentration of Ceftriaxone should be determined at regular intervals and the dosage adjusted. in patients undergoing dialysis, no additional supplementary dosing is required following the dialysis. Serum concentrations should be monitored, however, to determine whether dosage adjustments are necessary, since the elimination rate in these patients may be reduced. Patients with Hepatic Impairment. In patients with liver damage, there is no need for the dosage to be reduced, provided renal function is intact.

 

Elderly

These dosages do not require modification in elderly patients provided that renal and hepatic function is satisfactory.

Neonates, infants, and children up to 12 years

The following dosage schedules are recommended for once daily administration

Neonates (up to 14 days)

A daily dose of 20-50mg/kg body weight, not to exceed 50mg/kg

 

Infants and children (15 days to 12 years)

Standard therapeutic dosage: 20-80mg/kg body weight once daily. For children with body weights of 50kg or more, the usual adult dosage should be used. Doses of 50mg/kg or over should be given by slow intravenous infusion over at least 30 minutes

 

Acute, uncomplicated gonorrhea

A single dose of 250mg intramuscularly should be administered

 

Pri-operative prophylaxis

A single dose of 1-2g depending on the risk of infection of 30-90 minutes prior to surgery. In colorectal surgery, 2g should be given intramuscularly (dosages greater than 10 should be divided and injected at more than one site), or by slow intravenous infusion, in conjunction with a suitable agent against anaerobic bacteria

 

Use in special populations:

Pregnancy

Ceftriaxone crosses the placental barrier. Safety in human pregnancy has not been established. Reproductive studies in animals have shown no evidence of embryo toxicity, phototoxicity, teratogenicity, or adverse effects on male or female fertility, birth, or prenatal & postnatal development. in neonates, no embryo toxicity or teratogenicity has been observed. Nursing Mothers. Low concentrations of Ceftriaxone ars excreted in human milk, Caution should be exercised when Ceftriaxone is administered to a nursing woman or as directed by the physician.

 

CONTRAINDICATIONS:

Ceftriaxone is contraindicated in patients with known allergy to the cephalosporin class of antibiotics

 Read about:  Common Drug Interactions and Contraindications Every Doctor Should Know. 

WARNINGS AND PRECAUTIONS:

 

As with another cephalosporin, anaphylactic shock cannot be ruled out even if a thorough patient history is taken. Pseudomembranous colitis has been reported with nearly all antibacterial agents, including Ceftriaxone. Therefore, it is important to consider this diagnosis in patients who present with diarrhea after the administration of antibacterial agents. Superinfections with non-susceptible microorganisms may occur, as with other antibacterial agents. Shadows, which have been mistaken for gallstones, have been detected on sonograms of the gallbladder, usually following doses higher than the standard recommended dose. These shadows are, however, precipitates of calcium-Ceftriaxone, which disappear on completion or discontinuation of Ceftriaxone Therapy. Rarely have these findings been associated with symptoms. In symptomatic cases, conservative non-surgical management is recommended. Discontinuation of Ceftriaxone treatment in symptomatic cases should be at the discretion of the physician. Ceftriaxone must not be mixed or administered simultaneously with calcium-containing solutions or products, even via different infusion lines. Calcium-containing solutions or products must not be administered within 48 hrs. Of last administration of Ceftriaxone Cases of fatal reactions with calcium-Ceftriaxone precipitates in lung and kidneys in neonates and premature has been described. In some cases the infusion lines of administration of Ceftriaxone and calcium containing solutions differed. Cases of pancreatitis possibly of biliary obstruction etiology have been rarely reported in patients treated with Ceftriaxone Most patients presented with risk factors for biliary stasis and biliary sludge eg. Preceding major therapy, severe illness and total parenteral nutrition. A trigger or cofactor role of Ceftriaxone related biliary precipitation cannot be ruled out Safety and effectiveness of Ceftriaxone in neonates, infants and children have been established for the dosages described under dosage and administration. Studies have shown that Ceftriaxone, like some other cephalosporin can displace bilirubin from serum albumin. Therefore caution should be exercised when considering Ceftriaxone treatment in hyperbilirubinemic neonates. Ceftriaxone should not be used in neonates (especially premature) at risk of developing bilirubin encephalopathy. During prolonged treatment the blood should be checked at regular intervals as with other cephalosporins, anaphylactic reactions with fatal outcome have been reported, even if a patient is not known to be allergic or previously exposed.

 

ADVERSE EFFECTS:

Ceftriaxone is generally well tolerated; the most common adverse reactions associated with Ceftriaxone are changes in white blood cell counts, local reactions at the site of administration, rash, and diarrhea. Like all medicines, this medicine, with Ceftriaxone.

 

·        Incidence of adverse effects greater than 15%

·        Eosinophilia (0%) Thrombocytosis (5.1%)

·        Elevations in liver enzymes (3.1-3.3%)

·        Diarrhea (2.7%)

·        Leukopenia (2.1%)

·        Elevation in BUN (1.2%)

·        Local reactions-pain, tenderness, imitation (1%)

·        Rash (1.7%)

 

Some less frequently reported adverse events (Incidence < 1%) include phlebitis, itchiness, fever, chills, nausea, vomiting, elevations of bilirubin, elevations in creatinine, headache, and dizziness. Ceftriaxone may precipitate in bile, causing biliary sludge, biliary pseudolithiasis, and gallstones, especially in children. Hypoprothrombinaemia and bleeding are specific side effects. Hemolysis is reported. It has also been reported to cause post-renal failure in children. Like other antibiotics, Ceftriaxone can be used in Clostridium difficile-associated diarrhea, ranging from mild diarrhea to fatal colitis.

 

Severe allergic reactions (Not known, frequency cannot be estimated from the available data)

The signs may include:

·        Sudden swelling of the face, throat, lips, or mouth. This can make it difficult to breathe or swallow

·        Sudden swelling of the hands, feet, and ankles

·        Severe skin rashes (Not known, frequency cannot be estimated from the available data)

·        Exanthema

·        Allergic dermatitis

·        Urticaria

·        Acute generalized exanthematous pustulosis (AGEP)

 

Severe cutaneous adverse reactions (Erythema multiforme, Stevens-Johnson syndrome or Lyell's syndrome/toxic epidermal necrolysis)

 

OVERDOSAGE:

In the case of over dosage, drug concentration would not be reduced by hemodialysis or peritoneal dialysis. There is no specific antidote; Treatment of over dosage should be symptomatic

 

STABILITY:

See expiry on the pack

 

AVAILABILITY:

Ceftriaxone 250mg IV injection:

Contains a vial with dry substance equivalent to 250mg Ceftriaxone sodium and 1 ampoule of 5ml sterile water for injection

 

Ceftriaxone 250mg IM injection

Contains a vial with dry substance equivalent to 250mg Ceftriaxone sodium and 1 ampoule of 2ml 1% lidocaine injection

 

Ceftriaxone 500mg IV injection:

Contains a vial with dry substance equivalent to 500ing Ceftriaxone sodium and 1 ampoule of 5ml sterile water for injection

 

Ceftriaxone 500mg IM injection:

Contains a vial with dry substance equivalent to 500mg Ceftriaxone sodium and 1 ampoule of 2ml 1% lidocaine injection

 

Ceftriaxone 1g IV injection:

Contains a vial with dry substance equivalent to 1g Ceftriaxone sodium and 1g ampoule of 10ml sterile water for injection

 

Ceftriaxone 2g IV injection

Contains a vial with dry substance equivalent to 2g Ceftriaxone sodium and 2 ampoules of 10 ml sterile water for injection

 

INSTRUCTIONS:

Keep out of reach of children. Avoid exposure to heat, light and humidity Store between 15 and to 30°C. Improper storage may deteriorate the medicine.

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