Get the Flash Player to see this player.
Get the Flash Player to see this player.
Products
Ceftriaxone 1000mg
VN_bigPicture Ceftriaxone 1000 mg
Vial 1000 mg
Description
Ceftriaxone is a broad spectrum β – lactam antibiotic of third generation cephalosporin.
Clinical pharmacology
Ceftriaxone kills bacteria by interfering in the synthesis of the bacterial cell wall. Ceftriaxone binds with high affinity to penicillin binding proteins (PBP) in bacterial cytoplasmic membrane and by acylation of membrane-bound transpeptidase enzymes, prevent cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity.
Also cell division and growth are inhibited and elongation of susceptible bacteria and lysis frequently occur. Rapidly dividing bacteria are those most susceptible to the action of Ceftriaxone .
Antibacterial activity
Ceftriaxone has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria. , Aerobic gram-negative bacteria:acinetobacter calcoaceticus, enterobacter aerogenes, entrobacter cloacae,E.coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, klebsiella pneumoniae, moraxella catarrhalis, morganella morganii , neissera gonorrhoea, neisseria meningitidis, proteus mirabilis, proteus vulgaris, serratia marcscens
Aerobic gram-positive microorincluding penicillinase-producing strains of N.gonorrhoeae and most enterobacteriaceae (Citrobacter, E.coli Enterobacter, Klebsiella, Morganella, Proteus, Providencia, and Serratia species). Ceftriaxone is not as active against gram-positive cocci as are the first and second generation cephalosporins.
Pharmacokinetics
Oral absorption -----
Presystemic metabolism -----
Plasma half – life Range 6-9 h
Volume of distribution 0.15 l.kg -1
Plasma protein binding 95%
Indication
-1Lower respiratory tract infections.
-2Acute bacterial otitis media.
-3Skin and skin structure infections.
-4Urinary tract infections.
-5Uncomplicated gonorrhea(cervical/urethral and rectal)
-6Pelvic inflammatory disease (PID).
-7Bacteremia, septicemia.
-8Bacterial meningitis.
-9Bone and joint infections
-10Intra-abdominal infections
-11Prevention of postoperative infections.
Contraindication
Ceftriaxone is contraindicated in patients with known allergy to the cephalosporin class of antibiotics.
Precaution
• Before Ceftriaxone administration, previous hypersensitivity reactions to cephalosporins or penicillins must be determined because of cross hypersensitivity among β-lactams.
• Ceftriaxone should be used with caution when administered to hyperbilirubinemic neonates, specially premature neonates.
• Patients with impaired hepatic function do not generally require a reduction in dose. However, in patients with both impaired hepatic & renal function, the daily dose should not exceed 2 grams.
• Long-term therapy with Ceftriaxone may allow for the overgrowth of Candida albicans, resulting in oral candidiasis.
• Risk – benefit should be considered when history of bleeding disorders, gastrointestinal diseases, specially ulcerative colitis, regional enteritis, or antibiotic associated colitis exist. (Ceftriaxone may cause pseudomembranous colitis).
• Preoperative (preoperative, intraoperative, and post operative) prophylactic administration of Ceftriaxone usually should be discontinued within 24 hours following surgery.
Pregnancy
Pregnancy category B.
There are no adequate and well controlled studies in pregnant women. Therefore Ceftriaxone should be used during pregnancy only if clearly needed.
Breast feeding
Ceftriaxone is excreted in human milk in low concentrations. Caution should be exercised when it is administered to a nursing woman.
Dosage
The dosing and strengths of the dosage form available are expressed in terms of Ceftriaxone base. (Not the sodium salt).
Usual adult dose
• Uncomplicated gonorrhea, Intramuscular, 250 mg (base) as a single dose.
• Preoperative prophylaxis: Intravenous, 1 gram (base) one – half to two hours prior to the start of surgery.
• For all other infections: Intramuscular or intravenous, 1 to 2 grams (base) every 24 hours, or 500 mg to 1 gram every 12 hours.
Usual adult prescribing limits
4 grams (base) per day.
Usual pediatric dose
• Meningitis: intravenous or intramuscular, 100 mg (base) per kg of body weight, up to 4 grams, on the first day, then 100 mg per kg of body weight every 24 hours, or 50 mg per kg of body weight every 12 hours, up to 4 grams per day, for 7 to 14 days.
• Skin and soft tissue infections: intravenous or intramuscular, 50 to 75 mg (base) per kg of body weight every 24 hours, or 25 to 37.5 mg per kg of body weight every 12 hours up to 2 grams per day.
• For all other serious infections: intravenous or intramuscular 25 to 37.5 mg (base) per kg of body weight every 12 hours up to 2 grams per day.
• Otitis media; intramuscular, 50 mg (base)per kg of body weight, up to 1 gram, as a single dose.
Usual pediatric prescribing limits
4 grams per day for meningitis and 2 grams per day for all other infections.
Usual geriatric dose
• Dosing is the same as adult dose.
Usual geriatric prescribing limits
Dosing is the same as adult dose.
Note: Treatment with Ceftriaxone should be continued for 2 days after the sign and symptoms of infection have disappeared. The usual duration of therapy is 4 - 14 days but in complicated infections, longer therapy may be required.
Administration
To prepare solution for intramuscular use
• 2mL of sterile water for injection, 0.9% sodium chloride injection, 5% dextrose injection, bacteriostatic water for injection (with 0.9% benzyl alcohol), or 1% lidocaine hydrochloride injection, should be added to each 500 mg vial, or 3.5 mL of diluent to 1 gram vial) to provide a concentration of approximately 250 mg/mL.
• To reduce the volume of intramuscular injection a solution of 350 mg/mL could be prepared by adding 1 mL of diluent to each 500 mg vial or 2.1 mL diluent to each 1 gram vial. The 350 mg/mL solution is bioequivalent to a 250 mg/mL solution.
• Intramuscular injection should be administered deeply.
To prepare solution for intravenous use
• 5mL of sterile water for injection, 5% or 10% dextrose solution or 0.9% sodium chloride, should be added to each 500 mg vial or 10 mL of diluent to each 1 gram vial, to provide a concentration of approximately 100 mg/mL.
• Intravenous injection should be administered over 2-4 minutes.
To prepare solution for intravenous infusion
• The reconstituted solution for intravenous use could be further diluted to 50 or 100 mL with an appropriate diluent.
• Intravenous infusion should be administered over a period of 30 minutes.
Patient consultation
• Continue medicine for full time of treatment.
• If you missed a dose, take as soon as possible, don’t take if almost time for next dose and don’t double doses.
• If there wasn’t improvement of symptoms within few days, check with your physician.
• Store the medicine properly.
Warning
• Avoid using if there are particles inside after reconstitution.
• As a general rule, the solution should be used immediately after preparation.
• Use of diluents containing benzyl alcohol is not recommended for preparation of medications for use in neonates. A fatal toxic syndrome consisting of metabolic acidosis, CNS depression, respiratory problems, renal failure, hypotension and possible seizures and intracranial hemorrhages has been associated with this use.
Interaction
• The admixture of Ceftriaxone with other medications, including pentamidine isethionate or with labetalol hydrochloride is not recommended.
• The admixture of Ceftriaxone and aminoglycosides may result in substantial mutual inactivation.
If they are administrated concurrently, they should be administrated in separate sites. Do not mix them in the same intravenous bags or bottles.
• The admixture of Ceftriaxone and vancomycin and fluconazole are physically incompatible. When concomitantly administering Ceftriaxone by intermittent intravenous infusion, it is recommended that they be given sequentially, with thorough flushing of the intravenous lines (with one of the compatible fluids) between administrations.
• Caution should be exercised while using other medications specially alcohol, anticoagulants, heparin, other platelet aggregation inhibitors or thrombolytic agents concurrently with Ceftriaxone .
Laboratory value alteration
• A positive Coombs reaction appears frequently in patients who receive large doses of Ceftriaxone.
• Ceftriaxone may prolong prothrombin time.
• Administration of Ceftriaxone may change the following physiology/laboratory test values: Alanine aminotransferase (ALT [SGPT]), alkaline phosphatase, Aspartate aminotransferase (AST [SGOT]), Lactate dehydrogenase (LDH), Serum bilirubin, Blood urea nitrogen (BUN), Serum Creatinine, Complete blood count (CBC), and Platelet count.
Adverse reactions
Those indicating need for medical attention
• Incidence less frequent or rare Hypoprothrombinemia (unusual bleeding or bruising), pseudomembranous colitis (abdominal or stomach cramps and pain, abdominal tenderness. Severe watery and bloody diarrhea, fever).
• Allergic reactions, specifically anaphylaxis, Erythema multiform or Stevens Johnson syndrome (blistering, peeling or loosening of skin and mucous membranes, which may involves the eyes or the other organ systems) hearing loss, hemolytic anemia, immune, drug – induced (unusual tiredness or weakness, yellowing of the eyes or skin), hypersensitivity reactions, renal dysfunction, serum sickness-like reactions, seizures, thrombophlebitis.
Biliary “sludge” or pseudolithiasis (anorexia, epigasteric pain, nausea and vomiting) more likely when administered by intravenous bolus over 3 to 5 minutes.
Those indicating need for medical attention only if they continue or are bothersome.
• Incidence more frequent.
Gastrointestinal reactions (abdominal cramps, mild diarrhea, nausea or vomiting) headache, oral candidiasis (sore mouth or tongue), vaginal candidiasis (vaginal itching and discharge).
Overdose
In the case of overdosage, drug concentration would not be reduced by hemodialysis or peritoneal dialysis. There is no specific antidote. Treatment of overdosage should be symptomatic.
Storage and stability condition
• Prior to reconstitution store below 25˚C, Protect from light.
• After reconstitution for intramuscular use, solution is storable for 24 hours in room temperature (25°C) and 3 days in refrigerator (4°C).
• After reconstitution for intravenous use, solution is storable for 2 days in room temperature (25°C) and 10 days in refrigerator (4°C).
• The color of solutions ranges from light yellow to amber, depending on the length of time of storage, concentration and diluent used.
Packaging
Each vial containes: 500 or 1000 mg of Ceftriaxone, (as sodium).
Boxes of 20 vials.
Date of revision: November 8, 2008
© Copyright 2008 - daanapharmac.com | Powered By : [ PersianTools ]