Cephapirin

423.468

423.46

244-466-5

89B59H32VN

DTXSID9022784

C61670

J - Antiinfectives for systemic use

177

-0.1

Solid

1.4021 (rough estimate)

>135°C (dec.)

1.51e-01 g/L

-20°C Freezer, Under Inert Atmosphere

6.98E-26mmHg at 25°C

Oral-rat LD50: 16356 mg/kg; Oral-Mouse LD50: 26088 mg/kg

Thermal decomposition emits toxic nitrogen oxides and sulfur oxide fumes

2.15None

2.15

183.5 Ų [M+H]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]|191.2 Ų [M+Na]+ [CCS Type: TW, Method: calibrated with Waters Major Mix]

Odorless or with a slight odor. /Cephapirin Sodium/

The warehouse is low-temperature, ventilated and dry

If frozen immediately after reconstitution with sterile water for injection, bacteriostatic water for injection, 0.9% sodium chloride injection, or 5% dextrose injection, solutions retain their potency for up to 60 days at -15 deg C (5 deg F). After thawing at room temperature, solutions retain their potency for 12 hours at room temperature or for 10 days if refrigerated at 4 deg C (39 deg F).

P261, P285, P304+P341, P342+P311, P501

H334

Tolerances are established for the residues of cephapirin in the milk and edible tissues of dairy cattle.

|Danger|H315 (97.56%): Causes skin irritation [Warning Skin corrosion/irritation]|P261, P264, P271, P272, P280, P285, P302+P352, P304+P340, P304+P341, P305+P351+P338, P312, P321, P332+P313, P333+P313, P337+P313, P342+P311, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 41 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H317 (14.63%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P261, P272, P280, P285, P302+P352, P304+P341, P321, P333+P313, P342+P311, P363, and P501|Aggregated GHS information provided by 41 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

practically nontoxic

Rats exposed via the oral route to cephapirin displayed low acute toxicity (LD50 = 14000 mg/kg). The most common adverse reactions are hypersensitivity reactions and alterations to liver function. Evidence of white blood cell disorders and anaemia were noted in some subjects.

PROBENECID & SULFINPYRAZONE COMPETE WITH URIC ACID @ RENAL TUBULE TRANSPORT SITES. URINARY EXCRETION OF OTHER WEAK ACIDS ALSO CAN BE AFFECTED BY THESE URICOSURIC AGENTS. ... CEPHALOSPORINS ... MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. /CEPHALOSPORINS/|The admixture of beta-lactam antibacterials (penicillins and cephalosporins) and aminoglycosides may result in substantial mutual inactivation. If they are administered concurrently, they should be administered in separate sites. Do not mix them in the same intravenous bag or bottle. /Cephalosporins/

These medications sould not be used when the following medical problem exists: Previous allergic reaction (anaphylaxis) to penicillins, penicillin derivatives penicillamine, or cephalosporins; Gastrointestinal disease, history of, especially ulcerative colitis, regional enteritis, or antibiotic-associated colitis (cephalosporins may cause pseudomembranous colitis); Hepatic function impairment (cefoperazone is primarily excreted in bile; may also cause elevated SGOT, SGPT, and alkaline phosphatase; it is recommended that patients with both severe liver disease and significant renal disease receive a reduced dosage of cefoperazone. /Cephalosporins/

Cephalosporins cross the placenta and are found in low concentrations in milk. /Cephalosporins/

Cephalosporins cross the placenta and are found in low concentrations in milk. /Cephalosporins/

For treatment of infections caused by susceptible bacteria.

Cephalosporins|Cephalosporins are still useful as alternatives to penicillins for a variety of infections in patients who can't tolerate penicillins. These include streptococcal and staphylococcal infections.|BACTERIA SUSCEPTIBLE TO CEPHALOTHIN /BOTH GRAM POSITIVE & GRAM-NEGATIVE MICROORGANISMS/ ARE SENSITIVE OVER APPROX SAME RANGE OF CONCN TO ... CEPHAPIRIN. ... CEPHAPIRIN IS SOMEWHAT MORE INHIBITORY THAN CEPHALOTHIN FOR GROUP-A STREP PYOGENES & PNEUMOCOCCUS.|CEPHAPIRIN IS ONE OF NEWEST SEMISYNTHETIC CEPHALOSPORINS. ... LIKE OTHER CEPHALOSPORINS, CEPHAPIRIN SHOULD BE RESERVED FOR THOSE INSTANCES IN WHICH ORGANISM IS SENSITIVE TO IT & PATIENT IS HYPERSENSITIVE TO PENICILLIN.|For more Therapeutic Uses (Complete) data for CEPHAPIRIN (10 total), please visit the HSDB record page.

SINCE ... CEPHAPIRIN ... ADMIN AS ... SODIUM SALTS, CARE SHOULD BE EXERCISED IN USE OF LARGE DOSES IN PERSONS WITH IMPAIRED CAPACITY TO EXCRETE THIS CATION. ... SUPRAINFECTIONS, USUALLY DUE TO GRAM NEGATIVE BACTERIA, MAY OCCUR WHEN THESE ANTIBIOTICS ARE EMPLOYED.|TYPICAL DOSAGE SCHEDULES ... FOR MOST OF CEPHALOSPORINS MUST BE MODIFIED FOR PATIENTS WITH IMPAIRED RENAL FUNCTION. /CEPHALOSPORINS/|... HYPERSENSITIVITY REACTIONS TO CEPHALOSPORINS IS HIGHER IN PATIENTS WHO HAVE SHOWN ALLERGIC MANIFESTATIONS FOLLOWING ADMIN OF PENICILLIN. THIS APPEARS TO BE RELATED TO SENSITIZATION TO BETA-LACTAM RING COMMON TO BOTH THESE DRUGS. /CEPHALOSPORINS/|... ENTEROCOCCAL ENDOCARDITIS CANNOT BE CURED WITH CEPHALOSPORIN EVEN WHEN ... GIVEN CONCURRENTLY WITH GENTAMICIN OR STREPTOMYCIN. ... ENTEROBACTER (AEROBACTER) INFECTIONS ARE, AS A RULE, RESISTANT TO THESE CMPD. /CEPHALOSPORINS/|For more Drug Warnings (Complete) data for CEPHAPIRIN (10 total), please visit the HSDB record page.

Cephapirin is a first-generation cephalosporin that has a wide spectrum of activity against gram-positive and gram-negative organisms. Cephapirin is more resistant to beta-lactamases than are the penicillins and so is effective against staphylococci, with the exception of methicillin-resistant staphylococci.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

... PENETRATION OF CEPHALOSPORINS INTO /CEREBROSPINAL FLUID/ IS POOR. /CEPHALOSPORINS/|CLOSE TO 50% OF CEPHAPIRIN IS BOUND TO PLASMA PROTEIN. HALF-LIFE ... IN NORMAL INDIVIDUALS IS ABOUT 40 MIN & IS DEPENDENT ON RENAL FUNCTION. SIGNIFICANT AMT ... PRESENT IN BLOOD IS REMOVED BY HEMODIALYSIS. ... EXCRETED MAINLY BY KIDNEY; ONLY 1% PRESENT IN BILE.|... /CEPHAPIRIN/ NOT ABSORBED FROM GI TRACT. IM INJECTION OF 0.5 G OF CEPHAPIRIN PRODUCES MAX PLASMA CONCN OF ABOUT 10 UG/ML @ 45 MIN; 1 G ABOUT 16 UG/ML. PLASMA CONCN ... EFFECTIVE AGAINST MANY SENSITIVE MICROORGANISMS ARE STILL DETECTABLE 6 HR AFTER SINGLE IM DOSE OF 1 G.|ABOUT 30% OF IM DOSE OF CEPHAPIRIN IS EXCRETED IN URINE IN EACH OF 1ST 2 HR PERIODS AFTER INJECTION.|For more Absorption, Distribution and Excretion (Complete) data for CEPHAPIRIN (8 total), please visit the HSDB record page.

Major metabolite detected is desacetylcephapirin.|MAJOR METABOLITE OF CEPHAPIRIN IS DEACETYLCEPHAPIRIN, WHICH IS ABOUT ONE HALF OF ANTIMICROBIAL ACTIVITY OF PARENT CMPD; 20% OF ANTIBIOTIC ACTIVITY IN PLASMA IS DUE TO DEACETYLATED CMPD.|Cephapirin is partially metabolized in the plasma, liver and kidneys to diacetyl cephapirin, which has about 50% of the antibacterial activity of the parent cmpd. ... Up to 20% of the antibiotic activity in serum is due to the desacetyl metabolite.

EIGHT HEALTHY ADULTS RECEIVED 1 G, IV AND IM. BIOLOGICAL HALF-LIFE OF CEPHAPIRIN WAS 43 MIN. ABSORPTION HALF-LIFE OF CEPHAPIRIN FROM IM ADMIN WAS 1.25 HR.|IV SODIUM CEPHAPIRIN SHOWED BIEXPONENTIAL DISPOSITION CHARACTERISTICS IN SERUM & SUBCHONDRAL BONE, REACHING DISTRIBUTION EQUIL WITHIN 20 MIN. RAPIDLY ELIMINATED, WITH BETA HALF-LIFE OF ABOUT 0.3 HR & BODY CLEARANCE OF 400 ML/MIN.|Serum half-life is 0.6 hr /From table/

The bactericidal activity of cephapirin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).|... VERY RESISTANT TO ACTION OF PENICILLINASE, FOR WHICH IT IS BOTH COMPETITIVE & NONCOMPETITIVE INHIBITOR ... IT DOES NOT SUPPRESS BREAKDOWN OF PENICILLIN G BY STAPHYLOCOCCAL PENICILLINASE. CEPHALOSPORIN C & ITS SEMISYNTHETIC CONGENERS INDUCE SYNTH OF PENICILLINASE BY B CEREUS & STAPH AUREUS. /CEPHALOSPORIN C/|... ENZYME ACTING SPECIFICALLY ON CEPHALOSPORIN C TO DESTROY ITS ANTIBACTERIAL ACTIVITY. THIS SUBSTANCE, CEPHALOSPORINASE IS ALSO BETA-LACTAMASE. MOST PREPN OF ENZYME ALSO EXHIBIT PENICILLINASE ACTIVITY, & SOME MICROORGANISMS PRODUCE ONE BETA-LACTAMASE THAT ACTS ON BOTH PENICILLIN & CEPHALOSPORINS. /CEPHALOSPORIN C/|Bactericidal; action depends on ability to reach and bind pencillin-binding proteins located in bacterial cytoplasmic membranes; cephalosporins inhibit bacterial septum and cell wall synthesis, probably by acylation of membrane-bound transpeptidase enzymes. This prevents cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity. Also, cell division and growth are inhibited, and lysis and elongation of susceptible bacteria frequently occur. Rapidly dividing bacteria are those most susceptible to the action of cephalosporins. /Cephalosporins/

... ADVERSE REACTIONS ... INCL LOCAL PAIN, INDURATION, STERILE ABSCESS, OR TISSUE SLOUGH AFTER IM INJECTION ... . /IV INFUSION/ IS CONSIDERABLY LESS IRRITATING THAN CEPHALOTHIN TO BLOOD VESSELS ... . REACTIONS ... DURING TREATMENT ARE TRANSIENT ELEVATIONS OF SERUM TRANSAMINASES & ALKALINE PHOSPHATASE, HALLUCINATIONS, NYSTAGMUS ... .|A positive Coombs' reaction appears frequently in patients who receive large doses of a cephalosporin. Hemolysis is not usually associated with this phenomenon, although it has been reported. Cephalosporins have produced rare instances of bone-marrow depression, characterized by granulocytopenia. The cephalosporins have /also/ been implicated as potentially nephrotoxic agents. /Cephalosporins/|TRANSIENT NEUTROPENIA HAS BEEN OBSERVED BETWEEN 10TH & 20TH DAYS OF THERAPY. /SEMISYNTHETIC CEPHALOSPORINS/|... MILD HYPERSENSITIVITY, MANIFESTED MOST FREQUENTLY AS ... LEUKOPENIA, ... TRANSIENT INCR IN SGOT, SGPT, ... BILIRUBIN, & BUN LEVELS. ... FALSE-POSITIVE REACTIONS FOR URINE GLUCOSE MAY BE OBSERVED ... OVERGROWTH OF NONSUSCEPTIBLE ORGANISMS CAN OCCUR AFTER PROLONGED USE.|For more Human Toxicity Excerpts (Complete) data for CEPHAPIRIN (12 total), please visit the HSDB record page.

BL P 1322

Cefadyl sodium is available in 500 mg, 1g, 2g, 4g, 20g, for IM and IV injection. /Cefadyl sodium/

UV SPECTROPHOTOMETRIC METHOD FOR QUANTITATIVE DETERMINATION OF CEPHAPIRIN SODIUM IN BULK & IN FINISHED DOSAGE FORMS IS PRESENTED.|IMPROVED HYDROXYLAMINE COLORIMETRIC DETERMINATION IS DESCRIBED FOR CEPHALOSPORINS INCL CEPHAPIRIN, OFFERING ADEQUATE SENSITIVITY, STABLE TEST & BLANK SOLN, & GOOD PRECISION.|LIQUID CHROMATOGRAPHY ANALYSIS WITH ULTRAVIOLET DETECTOR FOR THE DETERMINATION OF CEPHAPIRIN.|Protein is hydrolyzed under vacuum with 4.2 N sodium hydroxide. After pH adjustment and clarification, tryptophan is separated by ion exchange chromatography with measurement of ninhydrin chromophore or by reverse phase liquid chromatography with ultraviolet detection in foods and food and feed ingredients.

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