Cephradine

349.41

349.40

254-137-8

9YA6SX5S4D

DTXSID4022785

C76181

WHITE, CRYSTALLINE POWDER; POLYMORPHIC

J - Antiinfectives for systemic use

2941905400

138

0.4

Solid

1.5±0.1 g/cm3

140 °C

898℃

>110°(230°F)

1.684

soluble in water;1 M NH4OH: soluble 50mg/mL

Store at 0-5°C

PKA1 ABOUT 2.6, PKA2 ABOUT 7.3

MP 140-142 °C (DECOMP);PK1 = 2.63, PK2 = 7.57 /CEPHRADINE MONOHYDRATE/|SMALL, COLORLESS CRYSTALS /CEPHRADINE MONOHYDRATE/|Soluble in propylene glycol, slightly soluble in acetone, ethanol. Insoluble in ether, chloroform, benzene, hexane /Cephradine monohydrate/

NONH for all modes of transport

1

36/37/38-42/43-20/21/22

26-36-45-36/37-22

XI0336000

Xi,Xn

ACID STABLE

P261-P280-P284-P304 + P340-P305 + P351 + P338-P342 + P311

H315-H317-H319-H334-H335

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).

|Danger|H315 (100%): 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 42 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

...PARAMETERS OF RENAL FUNCTION...SHOULD BE MONITORED...WHEN...CEPHALOSPORIN & POLYPEPTIDE ANTIBIOTICS ARE USED CONCURRENTLY. /CEPHALOSPORINS/|URINARY EXCRETION OF...WEAK ACIDS...CAN BE AFFECTED BY THESE URICOSURIC AGENTS. THUS...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF PROBENECID OR SULFINPYRAZONE. /CEPHALOSPORINS/|CONCURRENT AS WELL AS INDIVIDUAL USE OF GENTAMICIN & CEPHALOTHIN MAY INCR NEPHROTOXICITY & ACUTE RENAL FAILURE. ... NEITHER IT NOR OTHER CEPHALOSPORINS USED PARENTERALLY SUCH AS CEPHRADINE, SHOULD BE USED WITH GENTAMICIN UNLESS LIFE-THREATENING CONDITION EXISTS.|Acetaldehyde, at concentrations occurring in vivo was found to avidly react in vitro with several clinically relevant drugs. The greatest reactivity was observed for the hydrazine and hydrazide-containing drugs, hydralazine and isoniazid, respectively. Substantial reactivity was also evidenced for the amine-containing penicillins cyclacillin and ampicillin and for the cephalosporins cephalexin, cephradroxyl and cephradine. However, the virtual lack of reactivity of the amine-containing penicillanic and cephalosporanic acids reveals a major role of the acyl groups of these antibiotics in their reactivity towards acetaldehyde. The presence of moieties which increase the electron density of the amine group appears to favor the molecule reactivity. Amongst several phenylethylallines tested, dopamine and noradrenaline were the most active in forming adducts with acetaldehyde. It is suggested that in vitro binding of acetaldehyde to the above-mentioned drugs could lead in vivo to decreased drug bioavailability, and conceivably the adducts formed may mediate some of the side effects associated with simultaneous drug and alcohol ingestion.|For more Interactions (Complete) data for CEPHRADINE (9 total), please visit the HSDB record page.

Cephalosporins|Cephradine /is/ indicated in the treatment of bacterial urinary tract infections caused by susceptible organisms. /Included in US product labeling/|Cephradine /is/ indicated in the treatment of bacterial pharyngitis caused by susceptible organisms. /Included in US product labeling/|Cephradine /is/ indicated in the treatment of skin and soft tissue infections caused by susceptible organisms. /Included in US product labeling/|For more Therapeutic Uses (Complete) data for CEPHRADINE (18 total), please visit the HSDB record page.

Cephalosporins should be used with caution in patients with a history of GI disease, particularly colitis. Because antibiotic-associated pseudomembranous colitis has been reported with the use of cephalosporins, it should be considered in the differential diagnosis of patients who develop diarrhea during or following therapy with the drugs. /Cephalosporins/|Prolonged use of a cephalosporin may result in the overgrowth of nonsusceptible organisms, especially Enterobacter, Pseudomonas, enterococci, or Candida. If superinfection occurs, appropriate therapy should be instituted. /Cephalosporins/|Other adverse effects reported with cephalosporin therapy include chest pain, pleural effusion, dyspnea or respiratory distress, cough, and rhinitis. Increased or decreased serum glucose concentration also has been reported. /Cephalosporins/|The most frequent adverse reactions to orally administered cephalosporins are nausea, vomiting, and diarrhea. These effects are usually mild and transient, but rarely may be severe enough to require discontinuance of the drug. Other adverse GI effects which have occurred with some of the oral cephalosporins include abdominal pain, tenesmus, epigastric pain/dyspepsia, decreased appetite/anorexia, glossitis, flatulence, candidiasis (eg, oral thrush), taste alteration, decreased salivation, and heartburn. Adverse GI effects can also occur with IM or IV cephalosporins. /Cephalosporins/|For more Drug Warnings (Complete) data for CEPHRADINE (9 total), please visit the HSDB record page.

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

Over 90 percent of the drug is excreted unchanged in the urine within six hours.|CEPHRADINE IS ALMOST COMPLETELY ABSORBED AFTER ORAL ADMIN; IN PRESENCE OF FOOD, ABSORPTION IS SLOWED BUT NOT DECR. ORAL DOSES OF 250 & 500 MG YIELD PEAK PLASMA LEVELS OF ABOUT 9 & 16.5 UG/ML, WITHIN 40 MIN FROM EMPTY STOMACH. ABSORPTION BY IM ROUTE IS CONSIDERABLY SLOWER.|AFTER SINGLE ORAL ADMIN, CEPHRADINE WAS ABSORBED RAPIDLY FROM GI TRACT & PEAK SERUM CONCN ACHIEVED WITHIN 1 HR. 75-100% OF DOSE EXCRETED UNCHANGED IN URINE IN FIRST 6 HOURS.|SIX SUBJECTS RECEIVED 1 G EACH OF CEPHRADINE (I) & CEPHALEXIN (II) EVERY 4 HR FOR 7 DOSES & 5 RECEIVED 2 G EVERY 6 HR FOR 5 DOSES. PEAK SERUM LEVELS FOR I & II WERE 29 & 35 UG/ML, RESPECTIVELY, FOLLOWING 1 G & 45-50 UG/ML FOLLOWING 2 G.|Cephalosporins are primarily excreted by the kidney ... . /Cephalosporins/|For more Absorption, Distribution and Excretion (Complete) data for CEPHRADINE (18 total), please visit the HSDB record page.

Cephradine is not metabolized and, after rapid absorption from the gastrointestinal tract, is excreted unchanged in the urine.

Cefradine is a first generation cephalosporin antibiotic with a spectrum of activity similar to Cefalexin. Cefradine, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Cefradine interferes with an autolysin inhibitor.|Cephalosporins and cephamycins inhibit bacterial cell wall synthesis in a manner similar to that of penicillin. /Cephalosporins/|The first generation cephalosporins ... have activity against gram positive bacteria and relatively modest activity against gram negative microorganisms. /Cephalosporins/

THROMBOPHLEBITIS HAS OCCURRED DURING IV INFUSION, MOST FREQUENTLY WHEN CEPHRADINE IS GIVEN FOR LONG PERIODS IN HIGH CONCN BY INFUSION INTO SAME VEIN.|Total body water increases in pregnancy and while the uterus, placenta, fetus, and amniotic fluid constitute part of this increase, the largest component is in the extracellular water. Fat stores also increase and thus the distribution volumes of all drugs expand, but the major effect is seen in polar drugs which are confined to the extracellular space. Cardiac output and renal function also increase and elimination of polar drugs is accelerated. In contrast, the elimination of lipophilic drugs may be retarded, and the effect on intermediate drugs is variable. Polar drugs cross the placenta slowly and accumulate in amniotic fluid and therefore in the fetal gut lumen. Lipophilic drugs cross the placenta rapidly and their transplacental distribution is dependent on relative maternal and fetal affinity: this is determined largely by protein binding on either side of the placenta. The fetus and neonate dispose of all drugs less rapidly than adults, the most efficient elimination processes being sulfate conjugation and renal excretion.|We report the case of a 15-year-old girl who developed high fever, syncope, abdominal pain, nausea and vomiting, myalgia, pharyngitis, and a desquamating rash eight days after a diagnostic peritoneal lavage. The diagnostic peritoneal lavage wound was erythematous and tender. Incision of the site yielded 10 ml of exudate that cultured Staphylococcus aureus. The patient was treated with a first-generation cephalosporin and recovered without sequelae. To our knowledge, this is the first reported case of toxic shock syndrome following diagnostic peritoneal lavage.

Anspor

19). MODIFIED IODOMETRIC & UV SPECTROPHOTOMETRIC METHODS DEVELOPED FOR DOSAGE FORM ANALYSIS.|NMR METHOD FOR DETERMINATION OF CEPHALEXIN IN CEPHRADINE BULK POWDERS, CAPSULES & SUSPENSION FORMULATIONS IS PRESENTED.

COMPARISON OF NEW FLUOROMETRIC METHOD & STANDARD MICROBIOLOGICAL BIOASSAY FOR DETERMINATION OF CEPHRADINE IN PLASMA.|SIMPLE, RAPID & REPRODUCIBLE FLUOROMETRIC ASSAY IN AQ SOLN & PLASMA INVOLVING ADDN OF FORMALDEHYDE WHICH CATALYZES FORMATION OF FLUORESCENT DERIVATIVES ON HYDROLYSIS IS DESCRIBED.|A rapid, simple, and accurate spectrophotometric method was developed and used for the analysis of cephalexin or cephradine in the urine of volunteers who ingested the drugs.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients