CEFOTAN

CEFOTAN- cefotetan disodium injection, solution
CEFOTAN- cefotetan disodium injection, powder, for solution
AstraZeneca Pharmaceuticals, LP

In GALAXY® Plastic Container (PL 2040)

To reduce the development of drug-resistant bacteria and maintain the effectiveness of CEFOTAN and other antibacterial drugs, CEFOTAN should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

DESCRIPTION

CEFOTAN (cefotetan disodium for injection) and CEFOTAN (cefotetan injection) in Galaxy® * plastic container (PL 2040) as cefotetan disodium are sterile, semisynthetic, broad-spectrum, beta-lactamase resistant, cephalosporin (cephamycin) antibiotics for parenteral administration. It is the disodium salt of [6R-(6α,7α)]-7-[[[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl]amino]-7-methoxy-3-[[(1-methyl-1H -tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Its molecular formula is

C17 H15 N7 Na2 O8 S4 with a molecular weight of 619.57.

Structural Formula

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CEFOTAN (cefotetan disodium for injection) is supplied in vials containing 80 mg (3.5 mEq) of sodium per gram of cefotetan activity. It is a white to pale yellow powder which is very soluble in water. Reconstituted solutions of CEFOTAN (cefotetan disodium for injection) are intended for intravenous and intramuscular administration. The solution varies from colorless to yellow depending on the concentration. The pH of freshly reconstituted solutions is usually between 4.5 to 6.5.

CEFOTAN in the ADD-Vantage Vial† is intended for intravenous use only after dilution with the appropriate volume of ADD-Vantage diluent solution.

CEFOTAN is available in two vial strengths. Each CEFOTAN 1 g vial contains cefotetan disodium equivalent to 1 g cefotetan activity. Each CEFOTAN 2 g vial contains cefotetan disodium equivalent to 2 g cefotetan activity.

CEFOTAN (cefotetan injection) in the Galaxy® plastic container (PL 2040) is a frozen, iso-osmotic, sterile, nonpyrogenic premixed 50 mL solution containing 1 g or 2 g cefotetan as sterile cefotetan disodium. Dextrose, USP has been added to adjust the osmolality to 300 mOsmol/kg (approximately 1.9 g and 1.1 g to the 1 g and 2 g dosages, respectively); sodium bicarbonate has been added to convert cefotetan free acid to the sodium salt. The pH has been adjusted between 4 and 6.5 with sodium bicarbonate and may have been adjusted with hydrochloric acid. CEFOTAN (cefotetan injection) in the Galaxy® plastic container (PL 2040) contains 80 mg (3.5 mEq) of sodium per gram of cefotetan activity. After thawing to room temperature, the solution is intended for intravenous use only.

This Galaxy® container is fabricated from a specially designed multilayer plastic (PL 2040). Solutions are in contact with the polyethylene layer of this container and can leach out certain chemical components of the plastic in very small amounts within the expiration dating period. The suitability of the plastic has been confirmed in tests in animals according to the USP biological tests for plastic containers as well as by tissue culture toxicity.

CLINICAL PHARMACOLOGY

High plasma levels of cefotetan are attained after intravenous and intramuscular administration of single doses to normal volunteers.

PLASMA CONCENTRATIONS AFTER 1 GRAM IV * OR IM DOSE
*
30-minute infusion

Mean Plasma Concentration (μg/mL)

Time After Injection

Route

15 min

30 min

1h

2h

4h

8h

12h

IV

92

158

103

72

42

18

9

IM

34

56

71

68

47

20

9

PLASMA CONCENTRATIONS AFTER 2 GRAM IV * OR IM DOSE
*
Injected over 3 minutes
Concentrations estimated from regression line

Mean Plasma Concentration (μg/mL)

Time After Injection

Route

5 min

10 min

1h

3h

5h

9h

12h

IV

237

223

135

74

48

22

12

IM

20

75

91

69

33

19

The plasma elimination half-life of cefotetan is 3 to 4.6 hours after either intravenous or intramuscular administration.

Repeated administration of CEFOTAN does not result in

accumulation of the drug in normal subjects.

Cefotetan is 88% plasma protein bound.

No active metabolites of cefotetan have been detected; however, small amounts (less than 7%) of cefotetan in plasma and urine may be converted to its tautomer, which has antimicrobial activity similar to the parent drug.

In normal patients, from 51% to 81% of an administered dose of CEFOTAN is excreted unchanged by the kidneys over a 24 hour period, which results in high and prolonged urinary concentrations. Following intravenous doses of 1 gram and 2 grams, urinary concentrations are highest during the first hour and reach concentrations of approximately 1700 and 3500 µg/mL respectively.

In volunteers with reduced renal function, the plasma half-life of cefotetan is prolonged. The mean terminal half-life increases with declining renal function, from approximately 4 hours in volunteers with normal renal function to about 10 hours in those with moderate renal impairment. There is a linear correlation between the systemic clearance of cefotetan and creatinine clearance. When renal function is impaired, a reduced dosing schedule based on creatinine clearance must be used. (see DOSAGE AND ADMINISTRATION).

In pharmacokinetics studies of eight elderly patients (greater than 65 years) with normal renal function and six healthy volunteers (aged 25 to 28 years), mean (± 1sd) Total Body Clearance (1.8(0.1) L/h vs. 1.8 (0.3) L/h) and mean Volume of Distribution (10.4(1.2) L vs. 10.3 (1.6)L) were similar following administration of a one gram intravenous bolus dose.

Therapeutic levels of cefotetan are achieved in many body tissues and fluids including:

skin

ureter

muscle

bladder

fat

maxillary sinus mucosa

myometrium

tonsil

endometrium

bile

cervix

peritoneal fluid

ovary

umbilical cord serum

kidney

amniotic fluid

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