Pharmaceuticals API List 4 >>
CAS NO. 62893-19-0 (Base)
EINECS NO. 263-749-4(Base)
MOL WT. 667.65
ANTIBOITICS / CEPHALOSPORINS /
PHYSICAL AND CHEMICAL PROPERTIES
PHYSICAL STATE White to slightly yellowish crystalline powder
SOLUBILITY IN WATER Freely soluble (practically insoluble in ether)
pH 4.5 - 6.5
STABILITY Stable under ordinary conditions.
GENERAL DESCRIPTION & APPLICATIONS
Cephalosporin: any of a group of broad-spectrum derived from species of
fungi of the genus Cephalosporium and are related to the penicillins in both
structure and mode of action but relatively penicillinase-resistant
antibiotics. These antibiotics have low toxicity for the host, considering
their broad antibacterial spectrum. They have the active nucleus of beta-lactam
ring which results in a variety of antibacterial and pharmacologic
characteristics when modified mainly by substitution at 3 and 7 positions.
Their antibacterial activities result from the inhibition of mucopeptide
synthesis in the cell wall.
They are widely used to treat gonorrhea, meningitis, pneumococcal,
staphylococcal and streptococcal infections. The cephalosporin class of
antibiotics is usually divided into generations by their antimicrobial
properties. Three generations of cephalosporins are recognized and the
fourth has been grouped.
Each newer generation of cephalosporins has broader range of activity
against gram-negative organisms but a narrower range of activity against
gram-positive organisms than the preceding generation. The newer agents have
much longer half-lives resulting in the decrease of dosing frequency.
Accordingly, the third-generation cephalosporins can penetrate into tissues
well, and thus antibiotic levels are good in various body fluids.
Second-generation cephalosporins have broader spectrums of activity against
gram negative coverage but less active against gram-positive organisms than
first-generation agents. T
Cefoperazone sodium is a semi-synthetic 3rd generation cephalosporin
effective against a wide range of aerobic and anaerobic gram-positive and
gram-negative bacteria. It is a white to pale yellow crystalline powder;
soluble in water, methanol; slightly soluble in dehydrated alcohol;
insoluble in acetone, ethyl acetate, ether. Chemical designation is
[4.2.0]oct-2-ene-2-carboxylic acid, monosodium salt.
Chemistry - A third generation cephalosporin, cefoperazone sodium contains
a piperazine side chain giving it antipseudomonal activity. It occurs as
white, crystalline powder and is freely soluble in water and poorly soluble
in alcohol. At room temperature, cefoperazone sodium has a maximum
solubility in compatible IV solutions of 475 mg/ml (at concentrations >333
mg/ml vigorous and prolonged shaking may be required). Reconstituted
solutions of the drug have a pH from 4.5 - 6.5. One gram contains 1.5 mEq of
Storage/Stability/Compatibility - The sterile powder for injection should be
stored at temperatures less than 25°C and protected from light. Once
reconstituted, solutions do not need to be protected from light.
Uses/Indications - Cefoperazone is used to treat serious infections,
particularly against susceptible Enterobacteriaceae not susceptible to other
less expensive agents or when aminoglycosides are not indicated (due to
their potential toxicity).
Adverse Effects/Warnings - Cefoperazone is a relatively safe agent. Rarely,
hypersensitivity reactions could potentially occur in animals. Because of
its thiomethyltetrazole side-chain it may also rarely cause
hypoprothrombinemia. Diarrhea secondary to changes in gut flora have been