ROSACTAM 1500
-
Chemical Name:
Ceftriaxone + sulbactam Na -
Therapeutic Category:
Antimicrobial -
Pharmacologic Category:
Antibiotic, Cephalosporin (Third Generation) -
Pharmaceutical Form:
Vial -
Composition:
Ceftriaxone 1000 mg + sulbactam 500 mg
ROSACTAM
For Injection (Vial)
Ceftriaxone (Sodium) + Sulbactam (Sodium)
Broad Spectrum Antibiotic
1-MECHANISM OF ACTION:
The antibacterial effect of Ceftriaxone & Sulbactam is due to the inhibition of cell wall synthesis attained by Ceftriaxone. Sulbactam is a potent highly specific inhibitor of a wide variety of beta-lactamases produced by common gram-negative and gram-positive aerobes and anaerobes by forming a protein complex with beta-lactamases. Thus, the full potential of Ceftriaxone against Enterobacter and Pseudomonas species is restored by the addition of Sulbactam.
The combination of Sulbactam and Ceftriaxone is active against all organisms sensitive to Ceftriaxone. In addition it demonstrates synergistic activity in a variety of organisms.
2-MICROBIOLOGY:
Gram positive aerobes: Staphylococcus aureus (including penicillinase-producing strains), Staphylococcus epidermidis, Streptococcus pneumonia, Streptococcus pyogenes, Viridans group streptococci.
Gram negative aerobes: Acinetobacter calcoacetius, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenza, Haemophilus para-influenzae, Klebsiella oxytoca, Klebsiella pneumonia, Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitides, Proteus mirabilis, Proteus vulgaris, Serratia marcescens. It is also active against many strains of Pseudomonas aeruginosa.
Anaerobes: Clostridium species, Peptococcus species, Bacteroides species.
3-PHARMACOKINETCS:
Following intramuscular administration, peak serum concentration of Ceftriaxone & Sulbactam are seen between 15 minutes to 2 hours.
The maximum plasma concentration of Ceftriaxone after a single IM dose of 1500 mg is about 81 mcg/ml and is reached in 2-3 hours after the dose, while that of Sulbactam is 6-24 mcg/ml and reached approximately in 1 hour. Serum concentrations have shown to be proportional to the administered dose.
The bioavailability of IM administration is equivalent to that of IV administered Ceftriaxone & Sulbactam. Both Ceftriaxone & Sulbactam are widely distributed into body tissues and fluids. Ceftriaxone diffuses into the tissue fluid, where if it is given in the recommended dosage range, bactericidal concentrations lasting up to 24 hours. Ceftriaxone is reversibly bound to albumin and the binding decreases with the increase in concentration. Ceftriaxone crosses the palcenta and is distributed in the amoniotic fluid.
The total plasma clearance is 10-22 ml/min. The renal clearance is 5-12 ml/min. Approximately 75-85% of Sulbactam and 50-60% of Ceftriaxone is excreted unchanged in the urine, while the remaining dose is excreted in the bile.
The mean plasma elimination half-life of Ceftriaxone is approximately 8 hours.
The mean serum half life of Sulbactam is approximately 1 hour.
In infants aged less than eighty days and in elderly aged over 75 years, the average elimination half life is usually 2-3 times that in the young adult.
In patients with renal or hepatic dysfunction, the pharmacokinetics of Ceftriaxone are only minimally altered and the elimination half life is only slightly increased.
Patients, who are functionally anephric, show a significantly longer half life of Sulbactam.
Haemodialysis significantly alters the half life, total body clearance and volume of distribution of Sulbactam.
4-INDICATIONS:
ROSACTAM in indicated for the treatment of the following infections:
- Lower respiratory infections.
- Acute bacterial otitis media.
- Skin and skin structure infections.
- Urinary tract infections.
- Pelvic inflammatory Disease.
- Bacterial septicemia.
- Bone and joint infections.
- Intra-abdominal infections.
- Meningitis.
- Sexually transmitted diseases.
Surgical prophylaxis: The preoperative administration of ROSACTAM reduces the incidence of postoperative infections in patients undergoing surgical procedures.
5-CONTRAINDICATIONS:
Ceftriaxone & Sulbactam is contraindicated in patients with known allergy to penicillins or to Ceftriaxone & Sulbactam.
6-WARNINGS:
Serious hypersensitivity reactions have been reported in patients receiving beta-lactam therapy. These reactions are more likely to occur in individuals with a history of hypersensitivity reactions to multiple allergens. If an allergic reaction develops, the drug should be discontinued and appropriate therapy instituted.
Treatment with broad spectrum antibiotics alters the normal flora of the colon and may permit overgrowth of Clostridia, the primary cause of pseudomembraneus colitis. It is important to consider its diagnosis in patients who develop diarrhea in association with antibiotic use.
Mild cases of colitis may respond to drug discontinuance alone. Moderate to serious cases should be managed with fluid, electrolyte and protein supplementation as indicated.
7-PRECAUTIONS:
Although transient elevations of BUN and serum creatinine have been observed, at the recommended dosages, the nephrotoxic potential of Ceftriaxone and Sulbactam is similar to that of the cephalosporins. Ceftriaxone is excreted via both biliary and renal excretion. Therefore patients with renal failure normally require no adjustment in dosage when usual doses of Ceftriaxone and Sulbactam are administered but concentrations of drug in the serum should be monitored periodically. If evidence of accumulation exists, dosage should be decreased accordingly.
Dosage adjustments should not be necessary in patients with hepatic dysfunction, however, in patients with both hepatic and significant renal disease, Ceftriaxone and Sulbactam should not exceed 3 g daily without close monitoring of serum concentrations.
Alterations in prothrombin time have occurred rarely in patients treated with Ceftriaxone and Sulbactam. Patients with impaired vitamin K stores may require monitoring of prothrombin time during treatment.
Ceftriaxone and Sulbactam should be prescribed with caution in individuals with a history of gastrointestinal disease especially colitis.
Pregnancy: Category B. This drug should be used during pregnancy only if clearly needed.
Nursing mothers: Low concentrations are excreted in human milk. Caution should be exercised when the product is administered to a nursing women.
Pediatric use: The product should not be administered to hyperbilirubinemic neonates, especially prematures.
8-DOSAGE & ADMINISTRATION:
ROSACTAM is to be administered intravenously or intramuscularly, after reconstitution with solvent.
RECONSTITUTION:
Reconstitute ROSACTAM with the solvent and agitate the vial gently until the powder dissolves completely. Though the reconstituted solution is stable for 24 hours at 25oC and up to 3 days under 2-8°C. It is advisable to use the solution immediately after reconstitution.
The following are the recommendation for diluting the solution:
| ROSACTAM 1500 mg | ROSACTAM 750 mg | ROSACTAM 375 mg | |
| Volume of solvent required to prepare the solution for IM use | 5 mL | 2.5 mL | 1 mL |
| Maximum final concentration in mg/ml Ceftriaxone/Sulbactam | 200 + 100 | 200 + 100 | 250 + 125 |
| Volume of solvent required to prepare the solution for IV use | 10 mL | 5 mL | 3 mL |
| Maximum final concentration in mg/ml Ceftriaxone/Sulbactam | 100 + 50 | 100 + 50 | 83.3 + 41.6 |
DOSAGE OF ROSACTAM:
Adults: The usual adult dose is 1.5 - 3grams given once a day or in equally divide doses twice daily depending upon the type and severity of infection. The total daily dose should not exceed 6 grams.
Dosage regimen should be adjusted in patients with marked decrease in renal function (creatinine clearance less than 30 mL/min) to compensate for the reduced clearance less than 15mL/min should receive a maximum dose of 500 mg Sulbactam every 12 hours.
Pediatric Patients: The usual pediatric dose is 375 to 750 mg given once a day or in equally divide doses twice daily.
For the treatment of serious miscellaneous infections other than meningitis, the recommended total daily dose is 75 mg to 100 mg/kg given in divided doses every 12 hours. The total daily dose should not exceed 3 grams. The usual duration of therapy is 7 to 14 days. Generally, therapy should be continued for at least 2 days after the signs and symptoms of the infection have disappeared.
The usual duration of therapy is 4 to 14 days in complicated infections, longer therapy may be required.
When treating infections caused by Streptococcus pyogenes, therapy should be continued for at least 10 days. No dosage adjustment is necessary in patients with impairment of renal or hepatic function.
9-OVERDOSAGE:
If acute over dosage occurs, supportive and symptomatic treatment should be initiated. Heamodialysis or peritoneal dialysis are infective in reducing Ceftriaxone concentration following over dosage.
10-PACKAGING & COMPOSITION:
-ROSACTAM 375 – For Injection: A pack of 1 or 100 vials. Each vial contains sterile Ceftriaxone sodium equivalent to Ceftriaxone 250 mg and Sulbactam sodium equivalent to Sulbactam 125mg.
- ROSACTAM 750 – For Injection: A pack of 1 or 100 Vials. Each vial contains sterile Ceftriaxone sodium equivalent to Ceftriaxone 500 mg and Sulbactam sodium equivalent to Sulbactam 250mg.
-ROSACTAM 1500 – For Injection: A Pack of 1 or 100 Vials. Each vial contains: Sterile Ceftriaxone sodium equivalent to Ceftriaxone 1000mg and Sulbactam sodium equivalent to Sulbactam 500mg.
11-STORAGE CONDITIONS:
Store ROSACTAM - For Injection at temperature below 25°C. Protect from light.
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