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ceftriaxone for injection, USP | Ceftriaxone

05:17 EDT 27th August 2014 | BioPortfolio

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IMAGE ceftriaxone-str.jpg

The elimination of ceftriaxone is not altered when ceftriaxone is coadministered with probenecid.

Table 1  Ceftriaxone Plasma Concentrations After Single Dose Administration
* IV doses were infused at a constant rate over 30 minutes.
ND = Not determined.
 Dose/Route
         Average Plasma Concentrations (mcg/mL)
 
    0.5 hr   
    1 hr   
    2 hr   
   4 hr   
   6 hr   
   8 hr   
   12 hr   
   16 hr   
   24 hr   
0.5 g IV*
0.5 g IM
    250 mg/mL
0.5 g IM
    350 mg/mL
    1 g IV*
    1 g IM
    2 g IV*
      82   
    
      22   
 
      20   
     151   
      40   
     257   
     59   
 
     33   
 
     32   
    111   
     68   
    192   
     48    
 
     38   
 
     38   
     88   
     76   
    154   
     37   
 
     35   
 
     34
     67   
     68   
    117   
     29   
 
     30   
 
     31   
     53   
     56   
     89   
     23   
 
     26   
 
     24   
     43   
     44   
     74   
     15   
 
     16   
 
     16   
     28   
     29   
     46   
     10   
 
    ND   
 
    ND   
     18   
    ND   
     31   
     5   
 
     5   
 
     5   
     9   
    ND   
     15   
Table 2  Urinary Concentrations of Ceftriaxone After Single Dose Administration
ND = Not determined.
Dose/Route
        Average Urinary Concentrations (mcg/mL)
 
0-2 hr
2-4 hr
4-8 hr
8-12 hr
12-24 hr
24-48 hr
0.5 g IV
0.5 g IM
1 g IV
1 g IM
2 g IV
 526
 115
 995
 504
2692
 366
 425
 855
 628
1976
 142
 308
 293
 418
 757
   87
   127
   147
   237
   274
    70
    96
   132
   ND
   198
    15
    28
    32
   ND
    40
Table 3 Average Pharmacokinetic Parameters of Ceftriaxone in Pediatric Patients With Meningitis
 
50 mg/kg IV
 75 mg/kg IV
Maximum Plasma Concentrations (mcg/mL)
Elimination Half-life (hr)
Plasma Clearance (mL/hr/kg)
Volume of Distribution (mL/kg)
CSF Concentration—inflamed meninges (mcg/mL)
    Range (mcg/mL)
    Time after dose (hr)
        216
        4.6
        49
        338
        5.6
    1.3-18.5
  3.7 (± 1.6)
        275
        4.3
        60
        373
        6.4
    1.3-44
  3.3 (± 1.4)
Table 4.  Average Pharmacokinetic Parameters of Ceftriaxone in Humans
* Creatinine clearance.
Subject Group
Elimination
  Half-Life
     (hr)
  Plasma
Clearance
  (L/hr)
 Volume of
Distribution
       (L)
Healthy Subjects
Elderly Subjects (mean age, 70.5 yr)
Patients With Renal Impairment
    Hemodialysis Patients (0-5 mL/min)*
    Severe (5-15 mL/min)
    Moderate (16-30 mL/min)
    Mild (31-60 mL/min)
Patients With Liver Disease
    5.8-8.7
      8.9
 
      14.7
      15.7
      11.4
      12.4
       8.8
  0.58-1.45
      0.83
 
      0.65
      0.56
      0.72
       0.7
       1.1
    5.8-13.5
      10.7
 
      13.7
      12.5
      11.8
      13.3
      13.6
MIC (mcg/mL)
Interpretation
        ≤8
      16-32
        ≥64
(S) Susceptible
(I) Intermediate
(R) Resistant
MIC (mcg/mL)
Interpretation
        ≤2
(S) Susceptible
MIC (mcg/mL)
Interpretation
        ≤0.25
(S) Susceptible
MIC (mcg/mL)
Interpretation
        ≤0.5
          1
        ≥2
(S) Susceptible
(I) Intermediate
(R) Resistant
Microorganism
ATCC ® #
MIC (mcg/mL)
Escherichia coli
Staphylococcus aureus
Pseudomonas aeruginosa
Haemophilus influenzae
Neisseria gonorrhoeae
Streptococcus pneumoniae
  25922
  29213
  27853
  49247
  49226
  49619
    0.03 – 0.12
         1 – 8*
         8 – 32
    0.06 – 0.25
  0.004 – 0.015
    0.03 – 0.12
Zone Diameter (mm)
Interpretation
           ≥21
          14-20
           ≤13
(S) Susceptible
(I) Intermediate
(R) Resistant
Zone Diameter (mm)
Interpretation
           ≥26  (S) Susceptible
Zone Diameter (mm)
Interpretation
           ≥35  (S) Susceptible
Zone Diameter (mm)
Interpretation
        ≥27
      25 – 26
        ≤24
(S) Susceptible
(I) Intermediate
(R) Resistant
Microorganism
ATCC ® #
Zone Diameter
Ranges (mm)
Escherichia coli
Staphylococcus aureus
Pseudomonas aeruginosa
Haemophilus influenzae
Neisseria gonorrhoeae
Streptococcus pneumoniae
  25922
  25923
  27853
  49247
  49226
  49619
      29 – 35
      22 – 28
      17 – 23
      31 – 39
      39 – 51
      30 – 35
MIC (mcg/mL)
Interpretation
        ≤16
          32
        ≥64
(S) Susceptible
(I) Intermediate
(R) Resistant
Method
Microorganism
ATCC ® #
MIC (mcg/mL)
  Agar

  Broth
Bacteroides fragilis
Bacteroides thetaiotaomicron
Bacteroides thetaiotaomicron
  25285
  29741
  29741
    32 – 128
    64 – 256
    32 – 128

Intravenous Administration: Ceftriaxone for injection should be administered intravenously by infusion over a period of 30 minutes. Concentrations between 10 mg/mL and 40 mg/mL are recommended; however, lower concentrations may be used if desired. Reconstitute vials with an appropriate IV diluent (see Compatibility and Stability ). 

After reconstitution, each 1 mL of solution contains approximately 100 mg equivalent of ceftriaxone. Withdraw entire contents and dilute to the desired concentration with the appropriate IV diluent. 

Vial Dosage Size
Amount of Diluent to be Added
250 mg/mL
350 mg/mL
        250 mg
        500 mg
            1 g
            2 g
        0.9 mL
        1.8 mL
        3.6 mL
        7.2 mL
            —
          1 mL
       2.1 mL
       4.2 mL
Vial Dosage Size
Amount of Diluent to be Added
        250 mg
        500 mg
            1 g
            2 g
                      2.4 mL
                      4.8 mL
                      9.6 mL
                    19.2 mL
 
 
Storage
   Diluent

Concentration 
   mg/mL

Room Temp. 
   (25°C)

Refrigerated 
   (4°C)
   Sterile Water for Injection

      100
   250, 350

   2 days
   24 hours

  10 days
   3 days
   0.9% Sodium Chloride Solution   

      100
   250, 350

   2 days
    24 hours

   10 days
   3 days
   5% Dextrose Solution

      100
   250, 350

   2 days
    24 hours

   10 days
   3 days

   Bacteriostatic Water + 
   0.9%Benzyl Alcohol

      100
   250, 350

   24 hours
   24 hours

    10 days
   3 days

   1% Lidocaine Solution 
   (without epinephrine)

      100
   250, 350

   24 hours
   24 hours

   10 days
   3 days
* Data available for 10 to 40 mg/mL concentration in this diluent is PVC containers only.
 
Storage
   Diluent
Room Temp. (25°C)
Refrigerated (4°C)
   Sterile Water
2 days
10 days
   0.9% Sodium Chloride Solution
2 days
10 days
   5% Dextrose Solution
2 days
10 days
   10% Dextrose Solution
2 days
10 days
   5% Dextrose + 0.9% Sodium Chloride Solution*   
2 days
Incompatible
   5% Dextrose + 0.45% Sodium Chloride Solution   
2 days
Incompatible
Clinical Efficacy in Evaluable Population
Study Day
 Ceftriaxone
Single Dose
     Comparator –
     10 Days of
    Oral Therapy
         95%
  Confidence
     Interval
      Statistical
      Outcome
Study 1 – U.S.
         14
 
         28
 
74% (220/296)

58% (167/288)
Amoxicillin/clavulanate
        82% (247/302) 

        67% (200/297)
 
(-14.4%, -0.5%)

(-17.5%, -1.2%)
 
Ceftriaxone is lower
   than control at
      study day
      14 and 28.
Study 2 – U.S.5
         14
 
         28
 
54% (113/210)

35% (73/206)
         TMP-SMZ
        60% (124/206) 

        45% (93/205)
 
(-16.4%, 3.6%)

(-19.9%, 0%)
 
    Ceftriaxone is
    equivalent to
control at study day
       14 and 28.
 
Study Day
13-15
Study Day
30+2
Organism
No.
Analyzed
No. Erad.
(%)
No.
Analyzed
No. Erad. (%)
Streptococcus pneumoniae
38
32 (84)
35
25 (71)
Haemophilus influenzae
33
28 (85)
31
22 (71)
Moraxella catarrhalis
15
12 (80)
15
9 (60)

Distributed by Pfizer Labs Division of Pfizer Inc, NY, NY 10017

Code No.: 78/MD/AP/96/F/B/R

IMAGE ceftriaxone-fig1.jpgIMAGE ceftriaxone-fig2.jpgIMAGE ceftriaxone-fig3.jpgIMAGE ceftriaxone-fig4.jpgIMAGE ceftriaxone-fig5.jpgIMAGE ceftriaxone-fig6.jpgIMAGE ceftriaxone-fig7.jpgIMAGE ceftriaxone-fig8.jpgIMAGE ceftriaxone-fig9.jpgIMAGE ceftriaxone-fig10.jpgIMAGE ceftriaxone-fig11.jpgIMAGE ceftriaxone-fig12.jpg

Manufacturer

Pfizer Laboratories, Division of Pfizer Inc

Active Ingredients

Source

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