Cefobid

CEFOBID- cefoperazone powder, for solution
Roerig

PHARMACY BULK PACKAGE NOT FOR DIRECT INFUSION

DESCRIPTION

CEFOBID® (cefoperazone), formerly known as cefoperazone sodium, is a sterile, semisynthetic, broad-spectrum, parenteral cephalosporin antibiotic for intravenous or intramuscular administration. It is the sodium salt of 7-[(R)-2-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-2-(p -hydroxyphenyl)acetamido-3-[[(1-methyl-H -tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate. Its chemical formula is C25 H26 N9 NaO8 S2 with a molecular weight of 667.65. The structural formula is given below:

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CEFOBID contains 34 mg sodium (1.5 mEq) per gram. CEFOBID is a white powder which is freely soluble in water. The pH of a 25% (w/v) freshly reconstituted solution varies between 4.5–6.5 and the solution ranges from colorless to straw yellow depending on the concentration.

CEFOBID in crystalline form is supplied in vials equivalent to 1 g or 2 g of cefoperazone.

A pharmacy bulk package is a container of a sterile preparation for parenteral use that contains many single doses.

This Pharmacy Bulk Package is for use in a pharmacy admixture service; it provides many single doses of cefoperazone for addition to suitable parenteral fluids in the preparation of admixtures for intravenous infusion. (See DOSAGE AND ADMINISTRATION, and DIRECTIONS FOR PROPER USE OF PHARMACY BULK PACKAGE.)

CLINICAL PHARMACOLOGY

High serum and bile levels of CEFOBID are attained after a single dose of the drug. Table 1 demonstrates the serum concentrations of CEFOBID in normal volunteers following either a single 15-minute constant rate intravenous infusion of 1, 2, 3 or 4 grams of the drug, or a single intramuscular injection of 1 or 2 grams of the drug.

TABLE 1. Cefoperazone Serum Concentrations
Mean Serum Concentrations (mcg/mL)
Dose/Route 0* 0.5 hr 1 hr 2 hr 4 hr 8 hr 12 hr
*
Hours post-administration, with 0 time being the end of the infusion.
Values obtained 15 minutes post-injection.
1 g IV 153 114 73 38 16 4 0.5
2 g IV 252 153 114 70 32 8 2
3 g IV 340 210 142 89 41 9 2
4 g IV 506 325 251 161 71 19 6
1 g IM 32 52 65 57 33 7 1
2 g IM 40 69 93 97 58 14 4

The mean serum half-life of CEFOBID is approximately 2.0 hours, independent of the route of administration.

In vitro studies with human serum indicate that the degree of CEFOBID reversible protein binding varies with the serum concentration from 93% at 25 mcg/mL of CEFOBID to 90% at 250 mcg/mL and 82% at 500 mcg/mL.

CEFOBID achieves therapeutic concentrations in the following body tissues and fluids:

Tissue or Fluid Dose Concentration
Ascitic Fluid 2 g 64 mcg/mL
Cerebrospinal Fluid (in patients with inflamed meninges) 50 mg/kg 1.8 mcg/mL to 8.0 mcg/mL
Urine 2 g 3,286 mcg/mL
Sputum 3 g 6.0 mcg/mL
Endometrium 2 g 74 mcg/g
Myometrium 2 g 54 mcg/g
Palatine Tonsil 1 g 8 mcg/g
Sinus Mucous Membrane 1 g 8 mcg/g
Umbilical Cord Blood 1 g 25 mcg/mL
Amniotic Fluid 1 g 4.8 mcg/mL
Lung 1 g 28 mcg/g
Bone 2 g 40 mcg/g

CEFOBID is excreted mainly in the bile. Maximum bile concentrations are generally obtained between one and three hours following drug administration and exceed concurrent serum concentrations by up to 100 times. Reported biliary concentrations of CEFOBID range from 66 mcg/mL at 30 minutes to as high as 6000 mcg/mL at 3 hours after an intravenous bolus injection of 2 grams.

Following a single intramuscular or intravenous dose, the urinary recovery of CEFOBID over a 12-hour period averages 20–30%. No significant quantity of metabolites has been found in the urine. Urinary concentrations greater than 2200 mcg/mL have been obtained following a 15-minute infusion of a 2 g dose. After an IM injection of 2 g, peak urine concentrations of almost 1000 mcg/mL have been obtained, and therapeutic levels are maintained for 12 hours.

Repeated administration of CEFOBID at 12-hour intervals does not result in accumulation of the drug in normal subjects. Peak serum concentrations, areas under the curve (AUC’s), and serum half-lives in patients with severe renal insufficiency are not significantly different from those in normal volunteers. In patients with hepatic dysfunction, the serum half-life is prolonged and urinary excretion is increased. In patients with combined renal and hepatic insufficiencies, CEFOBID may accumulate in the serum.

CEFOBID has been used in pediatrics, but the safety and effectiveness in children have not been established. The half-life of CEFOBID in serum is 6–10 hours in low birth-weight neonates.

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