When the concentration of antibiotic is less than the MIC (minimum inhibitory concentration) of 0.70 μg/mL at pH 7.4 and pH 5.5, cefradine (0~8 μg/mL; 12 hours) can quickly boost bacterial viability [4].

Cefradine (25 mg/kg; subcutaneous; 11 days) lowers bacterial density and counts in abscesses [4].

Animal/Disease Models: Non-diabetic mice
Doses: 25 mg/kg
Route of Administration: Sc; 11 days
Experimental Results: diminished bacterial density and counts in abscesses.

Absorption, Distribution and Excretion
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.

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

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Limited information indicates cephradine produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. cephradine is acceptable in nursing mothers.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Interactions
...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.

[1]. Pharmacokinetics of cephradine administered intravenously and orally to young and elderly subjects. J Clin Pharmacol. 1990;30(10):893-899.

[2]. Intravenous use of cephradine and cefazolin against serious infections. Antimicrob Agents Chemother. 1979;15(1):119-122.

[3]. Cefradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of T-LAK cell-originated protein kinase. Oncotarget. 2016;7(17):24633-24645.

[4]. In Vitro and In Vivo Antimicrobial Activity of Antibiotic-Conjugated Carriers with Rapid pH-Responsive Release Kinetics. Adv Healthc Mater. 2019;8(14):e1900247.

Cephradine is a first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton. It has a role as an antibacterial drug. It is a cephalosporin and a beta-lactam antibiotic allergen.
A semi-synthetic cephalosporin antibiotic.
Cephradine anhydrous is a Cephalosporin Antibacterial.
Cephradine is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity. Cephradine binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Cephradine Anhydrous is the anhydrous form of cephradine, a semisynthetic, broad-spectrum, first-generation cephalosporin with antibacterial activity. Cephradine binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
A semi-synthetic cephalosporin antibiotic.

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Mechanism of Action
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/

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Therapeutic Uses
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.

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Drug Warnings
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.

C16H19N3O4S

349.4

349.109

38821-53-3

Cephradine monohydrate;75975-70-1

38103

White to light yellow solid powder

1.5±0.1 g/cm3

693.1±55.0 °C at 760 mmHg

140-142ºC

373.0±31.5 °C

0.0±4.7 mmHg at 25°C

1.684

0.98

3

6

4

24

697

3

CC1=C(N2[C@@H]([C@@H](C2=O)NC(=O)[C@@H](C3=CCC=CC3)N)SC1)C(=O)O

RDLPVSKMFDYCOR-UEKVPHQBSA-N

InChI=1S/C16H19N3O4S/c1-8-7-24-15-11(14(21)19(15)12(8)16(22)23)18-13(20)10(17)9-5-3-2-4-6-9/h2-3,6,10-11,15H,4-5,7,17H2,1H3,(H,18,20)(H,22,23)/t10-,11-,15-/m1/s1

(6R,7R)-7-[[(2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Anspor; Alpharma Brand of Cephradine; Cephradine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~8.33 mg/mL (~23.84 mM)
DMSO : ≥ 3.6 mg/mL (~10.30 mM)

Solubility in Formulation 1: 4.55 mg/mL (13.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

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 (Please use freshly prepared in vivo formulations for optimal results.)