CAMTAXONE CEFTRIAXONE 1G+5ML LIDOCAINE+WATER FOR INJECTION.
Formula, Pharmacological properties, Indications, Contraindications, Warnings and precautions, Side effects / reverse effects, Drug interaction, Dosage and administration, Preparation of solutions, Storage conditions, How supplied, NAFDAC registration number and Manufacturer of Camtaxone Ceftriaxone Lidocaine Injection Medicine for Infections.
Each vial contains ceftriaxone sodium equivalent to 500mg-1g ceftriaxone.
Each diluents ampoule contains 2 or 3.5ml water for injection and also contains 20-35mg (1%) lidocaine hydrochloride for only intramuscular administration.
Each diluents ampoule Contains 5 or 10ml water for injection for intravenous administration.
Ceftriaxone, a third generation cephalosporin, has bactericidal activity and exerts this effect by inhibiting cell wall synthesis, Ceftriaxone has a high degree of stability against beta-lactamases, both penicillinases and cephalosporinases produced by gram-negative and gram-positive bacteria Enterobacter aerogenes, Enterobacter cloacea, Escherichia coli, Haemophilus influezae (including ampicillin-restistant strains). H. parainfluenzae, Klebsiella-species (including pneamoniae). Neisseria gonorrhea (including penicillinase and non-penicllinase producing strains), Neisseria meningitides, Proteus mirabilis, Proteus vulgaris, Morganella morganii and Serratia Marcescens are gram-negative microorganisms susceptible to ceftriaxone in vitro. Many strains of these microorganisms that are resistant to other antibiotics such as penicillins, cephalosporins, and aminoglycosides are susceptible to ceftriaxone sodium. Gram’s positive microorganisms susceptible to ceftriaxone sodium are staphylococcas aureus (including penicillinase-producing strains), Staphylococcus epidermidis) methicillin-resistant staphylococci are resistant to cephalosporins including ceftriaxone), Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus, agalactiae (group-B streptococcus pneumoniae. Most strains of enterococci and Streptococcus faecalis and group D streptococci are resistant. Ceftriaxone demonstrates in vitro activity against gram-negative aerobic organisms such as Citrobacter feundi, Citrobacter diversus, Providencia species, (including Providencia rettgeri), Salmonella species (including S.typhi) Shigella species and Actinobacter calcoacetious and anerobic organisms such as Bactericides species, Clostridium species (most strains of C. difficile are resistant); however the clinical significance is unknown. Ceftriaxone in rapidly and adequately distributed into body fluids and tissues following parenteral administration. In healthy voIunteers*** 500mg (or 1g) IV ceftriaxone administration produced mean plasma concentrations of 82mg (151mcg) -59mcg) (111mcg)-48mcg) and 37mcg (67mcg) at 0.5-1-2 and 4 hours, respectively. Following 500mg (or 1g) ceftriaxone IV dose, the mean concentration in bile was 581mcg/ml and in gallbladder wall 63.1mcg/ml at 1-2 hours.
**Aeromonas species, Alcaligenes species, Vibrio species (including V. cholerea), Yersinia species (including Y.enterocolitica).
***As a 30-min infusion.
Thirty-three to 67% of a ceftriaxone dose is excreted in urine and 40%-50% in bile as unchanged drug; a small amount is found in faeces as inactive metabolite. Ceftriaxone concentrations in urine (mcg/ml) are shown in the Table below:
|0-2 hours||2-4 hours||4-8 hours|
In healthy adult subjects, the elimination half-life of a 0.15g – 3g dose ceftriaxone ranges between 5.8-8.7 hours, volume of distribution is 5.78-13.5 L/kg. Plasma clearance is 0.58-1.45 L/hour and renal clearance is 0.32-0.73 L/hour.
Ceftriaxone is reversibly bound to plasma protein and the rate of binding decreases as the plasma concentration is increased (for example, while the binding rate at 25mcg/ml is 95%, it decreases to 300mcg/ml at 85%).
Ceftriaxone penetrates the inflamed meninges of infants and children. The average pharmacokinetic parameters of 50mg/kg and 75mg/kg IV ceftriaxone doses in pediatric patients with meningitis are shown in the Table below:
|Maximum plasma concentration (mcg/ml)||216||275|
|Elimination half-life (hours)||4.6||4.3|
|Plasma clearance (ml/hour/kg)||49||60|
|Volume of distribution (ml/kg)||338||373|
|CSF concentration-inflamed meninges (mcg/ml)||5.6||6.4|
|Time after dose (hour)||3.7 (±1.6)||3.3 (±1.4)|
Compared to that healthy adults the pharmacokinetics of ceftriaxone were not significantly altered in elderly subjects and in the patients with renal and hepatic impairment. Therefore, dosage adjustments are not necessary for these patients with ceftriaxone dosage up to 2g per day. Ceftriaxone is not removed from the plasma by hemodialysis. Therefore, in patient with severe renal impairment and undergoing hemodialysis, plasma ceftriaxone concentrations should be closely monitored and necessary dosage adjustment should be made in infants less than 8 days old and in patient over 75 years the average half-life is approximately 2 times longer.
Camtaxone ceftriaxone for injection is indicated for the treatment of serious infections listed below that are caused by organisms susceptible to ceftriaxone.
Lower respiratory tract infections: caused by Streptococcus pneumonia, Streptococcus species (excluding enterococci), staphylococcus aureus, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella species (including K. pneumoniae), Escherichia coli, E. aerogenes, Proteus mirabilis and Serratia marcescens.
Skin and skin structure infections: caused by staphylococcus aureus, Staphylococcus epidermidis, Streptococcus species (excluding enteroccocci), E. cloacae, Klebsiella species (including K. pneumonia), Proteus mirabilis and Pseudomonas aeruginosa.
Urinary tract Infections (Complicated and uncomplicated): caused by Escherichia coli, Proteus mirabilis, Proteus vulgaris, M. morganii and KlebsielIa species (including K. pneumonia) and cervical/rectal/urethral uncomplicated gonorrhea and pelvic inflammatory disease caused by penicillinase and non-penicillinase producing strains of Neisseria gonorrhea.
Bone and Joint infections: Caused by Staphylococcus aureus, Streptococcus pneumonia, Streptococcus species (excluding enterococci), Escherichia coli, Proteus mirabilis, Klebsiella pneumonia and enterobacter species.
Intra-abdominal infections: Caused by Escherichia coli and Klebsiella pneumoniae.
Bacterial Septicemia: Caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Haemophillia influenzae and Klebsiella pneumonia.
Meningitis: Caused by Haemophilus influenzae, Neisseria meningitidis and Streptococcus pneumoniae.
Ceftriaxone can be used as a prophylactic agent in cases such as vaginal/abdominal hysterectomy and coronary artery by-pass surgery where the incidence of pest operative infection risk is high.
Camtaxone ceftriaxone for injection should be used in patients with known sensitivity to ceftriaxone sodium and cephalosporins class of antibiotics. In patients with hypersensitivity to penicillins, the possibility of cross allergic reactions should be considered.
WARNINGS AND PRECAUTIONS
Before instituting therapy with Camtaxone ceftriaxone for injection, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to ceftriaxone sodium, cephalosporins and penicillin class of antibiotics or any other drug. In case of allergic reactions during therapy, treatment should be discontinued. Serious hypersensitivity reaction may require epinephrine treatment and other emergency measures.
During treatment with cephalosporins and other broad-spectrum antibiotics, pseudomembraneous colitis has been reported; these agents may also alter the normal flora of the colon and cause overgrowth of clostridium. Particularly, a toxin produced by Clostridium difficile is one primary cause of this type colitis. Therefore, this diagnosis should be considered in patients who develop diarrhea during therapy and necessary precautions should be taken. Usually discontinuation of drug therapy is sufficient; but in some cases electrolyte and protein supplementation and oral vancomycin treatment may be required.
Camtaxone ceftraxone for injection should be used with caution in patients with a history of gastrointestinal disease and colitis.
Symptomatic or asymptomatic gallbladder sludge may be observed during ceftriaxone therapy. Appropriate monitoring should be performed by abdominal ultrasonography and treatment should be discontinued. This condition is reversible and normalizes by discontinuation of therapy.
Sight elevation in BUN and serum creatinine levels maybe observed during ceftriaxone therapy. Serum should be monitored and drug accumulation should be prevented in patients with hepatic and renal dysfunction and in severe cases. Ceftriaxone dosage should not exceed total 2g daily without close monitoring of serum concentrations.
Prothrombin times may be prolonged during ceftriaxone treatment. Since vitamin K synthesis may be impaired or Vitamin K stores may be low in patient with chronic hepatic diseases or malnutrition, ceftriaxone therapy should be administered cautiously and vitamin K should be supplemented when required (10mg weekly).
Prolonged use of ceftriaxone may be associated with the development of super infection; appropriate therapy should be instituted.
In vitro studies have revealed that ceftriaxone, like other cephalosporin group of antibiotics, can displace bilirubin from serum albumin. Therefore, ceftriaxane should be administered with caution to hyperbilirubinemic neonates, especially prematures.
Ceftriaxone is found in human milk; nursing mothers should consider this. Although there were no evidence for mutagenicity or carcinogenicity, its safety in pregnant women has not been established.
Blood test should be performed regularly during ceftriaxone therapy.
SIDE EFFECTS / REVERSE EFFECTS
Camtaxone ceftriaxone for injection is generally well tolerated. The adverse reactions which were observed during ceftriaxone therapy and resolved following discontinuation of treatment, are as follows:
Location reaction: pain, induration or tenderness at the site of injection (1%) and very rarely phlebitis alter IV administration.
Hypersensitivity reaction: rash (1.7%) and less frequently pruritis, fever and chills.
Hematologic reaction: eosinopilia (6%), thrombocytosis (5.1%), leucopoenia (2.1%) and less frequently anemia, lymphopenia, thrombocytopenia and prolongation of the prothrombin time.
Gastrointestinal tract: diarrhea or loose stools, nausea, vomiting, stomatitis and glossitis. Rarely headaches and dizziness, nomiliasis or vaginitis, diaphoresis, flushing, gall bladder sludge, anaphylactic, or anaphylactoid reactions have been reported. Pseudomembranous colitis and abnormalities were reported less frequently.
IN CASE OF AN UNESPECTED EFFECT, CONSULT YOUR PHYSICIAN.
There are no published data on the interaction of ceftriaxone with any other drug.
DOSAGE AND ADMINISTRATION
After reconstitution Camtaxone ceftriaxone injection cab be administered intravenously or intramuscularly. The usual adult dose is 1-2g. This dose can be given once a day or in equally divided doses twice a day every 12 hours depending on the type and severity of the infection. The total daily dose should never exceed 4 grams.
For the treatment of serious miscellaneous infection in children, other than meningitis, the recommended daily dose is 50mg-75mg/kg: this should be equally divided in 2 doses and given every 12 hours. Total daily dose should not exceed 2 grams since the enzymatic mechanism is not fully developed in 1-2 weeks old infants, 25mg-50mg/kg daily doses should be administered and the total daily dose should not exceed 50mg/kg.
Camtaxone ceftriaxone for injection therapy should be continued for at least two days after the signs and symptoms of infection have disappeared. The usual duration of therapy is 4-14 days and in complicated infections longer therapy may be required.
In the treatment of meningitis, a dose of 100gm/kg Camtaxone ceftriaxone injection given in equal divided 2 doses every 12 hours is recommended. A loading dose of 150mg/kg can be administered initially. Daily dose should not exceed 4 grams.
For the treatment of uncomplicated gonorrhea, a single intramuscular dose of 250mg should be administered.
For surgical prophylaxis, a single 1g administered 1/2 to 2 hours before surgery is recommended. In streptococcus pyogenes infections therapy should be continued for at least 10 days.
Adjustment in dosage should be made in patients undergoing dialysis as well as those with hepatic and renal dysfunction.
In elderly patient, the same dosage scheduled is used as in adult.
In clinical trials, a synergistic effect is observed between ceftriaxone and aminoglycosides. A combination therapy can be considered in the treatment of severe and life-threatening infection, particularly those caused by Pseudomonas aeruginosa.
However due to physical incompatibility between these two agents, they should be administered separately.
Preparation of solution
For intravenous or intramuscular administration, the vial should be reconstituted with the diluents and shaken vigorously; particle matter and the color should be monitored. The color of solution ranges from light yellow to amber depending on the concentration, diluents used and storage conditions. These factors do not affect the activity and the tolerance of the active ingredient. For intramuscular administration 0.5g Camtaxone ceftriaxone for injection is diluted with 2ml and 1g Camtaxone ceftriaxone for injection with 3.5ml lidocaine containing diluents and injected deeply into a gluteal muscle.
Lidocaine containing diluents should never be injected into a blood vessel.
For intravenous injection Camtaxone ceftriaxone 0.5g Camtaxone ceftriaxone for injection is diluted with 2ml and 1g Camtaxone ceftriaxone with 10ml water for injection and directly injected intravenously in 2 – 4 minutes.
For intravenous infusion, Camtaxone ceftriaxone for injection is reconstituted as above and further diluted with an appropriate calcium-free IV diluents (0.9% sodium chloride, 0.45% sodium chloride +2.5% dextrose, 5% and 10% dextrose, 5% laevulose, 6% dextran in dextrose or water for injection); it is infused over a period of 30 minutes.
The fresh prepared solutions for Camtaxone ceftriaxone injection are physically and chemically stable at room temperature and remain stable at 5oC for 24 hours. However, it is recommended that solutions are administered shortly after reconstitution.
Keep out of reach of children.
Pharmaceutical dosage forms (one vial with one diluents ampoule)
Camtaxone ceftriaxone 500mg IM injection
Camtaxone ceftriaxone 1g IM injection
Camtaxone ceftriaxone 500mg IV injection
Camtaxone ceftriaxone 1g IV injection
NAFDAC REG NO.: A4-7940
MANUFACTURED IN CHINA BY
SHANDONG XIER KANGTAI PHARMACEUTICAL CO., LTD.
PRIVATE ECONOMY GARDEN, XINYAN TOWN,
YANZHOU, JINING CITY, SHANDONG CHINA
MARK PHARMACEUTICALS LIMITED