Cephaloridine

415.482

415.06600

200-052-6

LVZ1VC61HB

DTXSID9022782

C76594

CRYSTALS|WHITE TO OFF-WHITE, CRYSTALLINE POWDER

J - Antiinfectives for systemic use

147

-1.70 at pH = 2

1.3230 (rough estimate)

184°C

No data

In water, >2.0X10+4 at 21 deg C

2-8°C

LD50 mice, rats (g/kg): >15, 2.5-4 orally; in monkeys (g/kg): >0.2 i.m. (Atkinson)

D +47.7° (c = 1.25 in water)

AQ SOLN ARE SLIGHTLY ACID (PH 4.5-5)

EXPOSURE TO SUNLIGHT CAUSES DISCOLORATION|Aqueous solutions (20% w/v) are stable for four weeks at 4 °C in the dark.

42/43

22-36/37-45

Xn

AQ SOLN (20% WT/VOL) ARE STABLE FOR 4 WK @ 4 DEG C IN DARK

P261, P272, P280, P302+P352, P321, P333+P313, P363, P501

H317

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

WHO; Environmental Health Criteria 119: Principles and Methods for the Assessment of Nephrotoxicity Associated with Exposure to Chemicals (1991)

|Warning|H317 (100%): May cause an allergic skin reaction [Warning Sensitization, Skin]|P261, P272, P280, P302+P352, P321, P333+P313, P363, and P501|Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory.

NON-IONIC, ANIONIC, & ZWITTERIONIC SURFACTANTS INDUCED RAPIDLY REVERSIBLE HYPER-ABSORPTIVE STATE IN THOMAS CANINE FUNDIC POUCH FOR CEPHALORIDINE...BLOOD LEVELS...MANY TIMES GREATER THAN VALUES IN CONTROLS.|CEPHALORIDINE SEEMS TO HAVE GREATEST POTENTIAL FOR NEPHROTOXICITY.../IT SHOULD NOT/ BE USED WITH GENTAMICIN /OR OTHER AMINOGLYCOSIDES, AMIKACIN, NEOMYCIN, PAROMOMYCIN & TOBRAMYCIN/ UNLESS LIFE-THREATENING CONDITION EXISTS /MAY INCR NEPHROTOXICITY/.|CEPHALORIDINE NEPHROTOXICITY IS ENHANCED BY CONCURRENT FUROSEMIDE ADMIN. SUCH THERAPY SHOULD BE AVOIDED IN PATIENTS WHO HAVE EVEN MILD PREEXISTING RENAL DISEASE.|...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION OF...WEAK ACIDS COULD RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/|Groups of ten male rats were treated with a high challenge dose of cephaloridine (3750 mg/kg), with methylprednisolone (100 mg/kg) or with cephaloridine and methylprednisolone by single sc injection. A control group received the injection vehicles only. Urine was collected from all animals daily over 18-hr collection periods, up to 96 hr after treatment. Blood was collected at 24, 48, 72 and 96 hr after treatment. At necropsy, kidneys were weighed, processed and examined histopathologically. Results show that methylprednisolone significantly ameliorated the nephrotoxicity of the challenge dose of cephaloridine. Cephaloridine-only treated rats had severe toxic nephrosis characterized by acute tubular necrosis, and elevated blood urea and creatinine. by contrast, the majority of cephaloridine plus methylprednisolone treated rats had only a slight or moderate toxic nephrosis, and had lower blood urea and creatinine levels compared with rats treated with cephaloridine only, indicating preservation of kidney function. Interestingly, rats treated with cephaloridine and methylprednisolone had higher urinary enzymes ... as well as protein and glucose, compared with rats treated with cephaloridine only. this is taken to indicate that rats treated with cephaloridine only had such marked kidney damage and necrosis that the population of cells able to produce these marker enzymes was significantly and rapidly depleted, but the protection afforded by methylprednisolone allowed cephaloridine plus methylprednisolone treated rats to sustain urinary enzyme output. Effects on urinary glucose and other parameters ... demonstrate interactions between glucocorticoid pharmacology and cephaloridine nephrotoxicity.

LD50 MOUSE ORAL GREATER THAN 15 G/KG|LD50 MONKEY INTRAMUSCULAR GREATER THAN 0.2 G/KG

Cephalosporins|GENERAL RANGE OF ACTIVITY & ANTIBACTERIAL SPECTRUM OF CEPHALORIDINE CLOSELY APPROX THAT OF CEPHALOTHIN, ALTHOUGH SOME STRAINS OF E COLI MAY BE SOMEWHAT MORE SENSITIVE TO FORMER. IT ALSO APPEARS TO BE MORE ACTIVE THAN CEPHALOTHIN AGAINST CL PERFRINGENS (WELCHII). MYCOBACTERIUM FORTUITUM IS SENSITIVE TO CEPHALORIDINE...|CEPHALORIDINE...GIVEN PARENTERALLY & SUBCONJUNCTIVALLY TO TREAT INTRAOCULAR INFECTIONS & MAY BE ADMIN TOPICALLY & SUBCONJUNCTIVALLY TO TREAT CORNEAL ULCERS.|CEPHALORIDINE IS EFFECTIVE IN THERAPY OF BRONCHITIS DUE TO H INFLUENZAE, BUT OTHER AGENTS OFTEN PRODUCE BETTER RESULTS, THIS DRUG HAS ALSO BEEN FOUND USEFUL WHEN EMPLOYED AS AEROSOL IN PATIENT WITH PURULENT BRONCHITIS.|For more Therapeutic Uses (Complete) data for CEPHALORIDINE (10 total), please visit the HSDB record page.

CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH; SINGLE DOSE OF 1 G IM YIELDS DETECTABLE CONCN FOR AS LONG AS 4 DAYS. ...CEPHALORIDINE SHOULD NOT BE GIVEN TO SUCH PATIENTS, SINCE IT IS NEPHROTOXIC.|WHILE CEPHALORIDINE PRODUCES LESS IRRITATION /THAN CEPHALOTHIN/, ITS NEPHROTOXICITY OUTWEIGHS THIS ADVANTAGE.|IN 48-HR HUMAN INFANTS...CEPHALORIDINE...HAVE VERY LONG PLASMA T/2, & TOXIC CONCN ARE REACHED WHEN DOSES ARE LOWERED CONSIDERABLY.|CEPHALORIDINE IS INJECTED EITHER IM OR IV. ... SINCE OTHER, LESS TOXIC CEPHALOSPORINS ARE AVAIL, THERE IS NO REASON TO RECOMMEND THIS PREPN.|For more Drug Warnings (Complete) data for CEPHALORIDINE (7 total), please visit the HSDB record page.

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

Renal.|.../CEPHALORIDINE/ POORLY ABSORBED FROM GI TRACT. PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED; 10 TO 20% OF PLASMA CEPHALORIDINE IS BOUND TO PROTEIN.|IM INJECTIONS OF 0.5 & 1 G YIELD PEAK PLASMA CONCN OF 15 & 30 UG/ML, RESPECTIVELY. APPROX 75% OF GIVEN DOSE IS EXCRETED IN URINE, MAINLY BY GLOMERULAR FILTRATION. CEPHALORIDINE ACCUM IN BLOOD OF PATIENTS WITH DECR RENAL FUNCTION, & IN AZOTEMIC PATIENTS PLASMA CONCN ARE VERY HIGH...|PLACENTAL DRUG TRANSFER- CEPHALORIDINE: TIME TO APPEAR IN FETUS 30 MIN; TIME TO FETAL/MATERNAL CONCN EQUIL 5 HR. /FROM TABLE/|.../CEPHALORIDINE/ READILY PENETRATE NORMAL EYE FOLLOWING SYSTEMIC OR SUBCONJUNCTIVAL ADMIN...|...CEPHALORIDINE...SHOWN...TO PENETRATE INTO BONE TO VERY LIMITED EXTENT AFTER SC OR ORAL DOSES TO RATS. RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER DOSING.

.../CEPHALORIDINE/ PEAK PLASMA CONCN ARE REACHED ABOUT 30 MIN AFTER DRUG IS INJECTED... WHILE ITS T/2 (60 TO 90 MIN)...ONLY SMALL AMT ARE DETECTABLE AFTER 8 HR.|/IN RATS/ RATIOS OF BONE TO SERUM CONCN AVG...1:7 FOR CEPHALORIDINE...DURING 0.25-4 HR AFTER /ORAL OR SC/ DOSING. DESPITE DIFFERENCES IN CONCN, T/2 IN BONE & SERUM WERE SIMILAR.

CEPHALOTHIN & ITS CONGENERS INHIBIT BACTERIAL CELL-WALL SYNTHESIS IN MANNER SIMILAR TO THAT OF PENICILLIN. /CEPHALOSPORINS/|Cephaloglycin and cephaloridine are acutely toxic to the proximal renal tubule, in part because of their cellular uptake by a contraluminal anionic secretory carrier and in part through their intracellular attack on the mitochondrial transport and oxidation of tricarboxylic acid (TCA) cycle anionic substrates. Preliminary studies with cephaloglycin have provided evidence of a role of fatty acid (FA) metabolism in its nephrotoxicity, and work with cephaloridine has shown it to be a potent inhibitor of renal tubular cell and mitochondrial carnitine (Carn) transport.

ADMIN OF PROBENECID CAN AMELIORATE NEPHROTOXICITY OF CEPHALORIDINE.|PERITONEAL DIALYSIS OR HEMODIALYSIS SIGNIFICANTLY REDUCES PLASMA CONCN OF /CEPHALORIDINE/...

...CASE HAS BEEN REPORTED IN WHICH TREATMENT WITH THIS DRUG /CEPHALORIDINE/ IN EXTREMELY ILL 18-YR-OLD GIRL WITH STAPHYLOCOCCUS SEPTICEMIA WAS ASSOCIATED WITH ACUTE RENAL FAILURE & BLINDNESS, WITH MUCH PAPILLEDEMA & PIGMENTATION IN PERIPHERY OF FUNDI. RETINAL VESSELS WERE SAID TO BE NORMAL.|CEPHALORIDINE OCCASIONALLY CAUSES ALLERGY, MANIFESTED BY PRURITUS, URTICARIA, VARIOUS SKIN RASHES, FEVER, EOSINOPHILIA, OR ANAPHYLAXIS. ...MAY CAUSE NAUSEA & VOMITING. ... NEUROTOXICITY, SUCH AS TWITCHING, MYOCLONUS, & COMA, ALSO OCCURS WITH LARGE DOSES.|CEPHALORIDINE IS NEPHROTOXIC. RENAL INJURY DUE TO THIS DRUG OCCURS MOST OFTEN WITH ADMIN OF 6 G OR MORE/DAY. CLINICAL PICTURE THAT DEVELOPS HAS ALL FEATURES OF ACUTE TUBULAR NECROSIS. MECHANISM OF THIS REACTION IS UNKNOWN.|LARGE DOSES OF CEPHALORIDINE RESULT IN HIGH INCIDENCE OF GRANULAR CASTS IN URINE.|For more Human Toxicity Excerpts (Complete) data for CEPHALORIDINE (10 total), please visit the HSDB record page.

Cefaloridine

ESSENTIALLY 100% AS AN ANTIBIOTIC

CEPHALOSPORINS ARE INCOMPATIBLE WITH ERYTHROMYCIN & TETRACYCLINES IN PARENTERAL MIXTURES. /CEPHALOSPORINS, FROM TABLE/|Because of its renal toxicity and the development of newer and more active synthetic cephalosporins, cephaloridine's use is declining.|This agent in no longer available in the US.