Disease relevance of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• Cephacetrile in the treatment of female pelvic inflammatory disease [1].
• Phlebitis occurred in 6 of the 53 patients (11%) who received intravenous cephacetrile and thrombosis was present in 3 (6%) [1].
• The pharmacokinetics of cephacetrile were studied after its administration as a single i.v. bolus injection of 15 mg/kg body weight to 11 patients with terminal renal inpairment undergoing haemodialysis for 6 h [2].
• Comparative evaluation of cephacetrile in experimentally induced bovine mastitis [3].
• Cephacetrile in the treatment of acute bacterial pneumonia [4].

High impact information on (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• The cephacetrile-related compounds Ro 25-4095 and Ro 25-4835 were hydrolyzed by all three beta-lactamases with catalytic efficiencies (relative to penicillin G) ranging from approximately 5 (TEM-1, AmpC) to approximately 25 (TEM-3) [5].
• Penicillin G minimum inhibitory concentration values showed significant differences when 6557-bp, 4361-bp, 2322-bp, or 2027-bp plasmids were present, and weak or no differences were observed for cephacetrile, rifamycin, and norfloxacin [6].
• The beta-lactam antibiotics carfecillin, cephapirin sodium, and cephacetrile sodium decreased phagocytosis 11.2, 12.8, and 23.8%, respectively [7].
• Pharmacokinetics of cephacetrile in patients undergoing haemodialysis [2].
• During haemodialysis sessions, the average pharmacokinetic parameters of cephacetrile determined at the dialyser input were: a = 5.03 h-1, beta = 0.458 h-1, K12 = 2.337 h-1, K21 = 1.996 h-1 K13 = 1.154 h-1, Vc = 5.5081, Vp = 6.4481, Vdss = 11.9561 [2].

Biological context of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• Clinical pharmacology of cephacetrile in ruminants [8].

Anatomical context of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• Studies on serum and cerebrospinal fluid levels of cephacetrile in neonates [9].
• Cephacetrile and desacetylcephacetrile did not enter erythrocytes [10].
• It appeared that after infusion of the microcapsulated preparations of cephacetrile and clindamycin, rates of drug release from the depot were equal to the rates of absorption of free drug from the udder [11].
• On the other hand, neither destruction of lysosomes nor cell lesion was found in rats treated with cephacetrile or cephalothin [12].

Associations of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid with other chemical compounds

• The persistence of chloramphenicol, cephacetrile, and clindamycin in the udders of dry cows was studied after drying-off therapy with salts of these antibiotics suspended in conventional oil bases [11].
• Biophotometric growth studies were conducted with clinical isolates of beta-lactamase-producing staphylococi in the presence and absence of cephradine, cephalexin, cefazolin and cephacetrile [13].

Gene context of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• Cephacetrile, on the other hand, showed clear reactions in 9 out of 15 subjects, in the form of elevated AAP activity in urine and in 6 of the cases membrane elimination was demonstrable immunologically [14].

Analytical, diagnostic and therapeutic context of (6S,7S)-3-(acetyloxymethyl)-7-(2-cyanoethanoylamino)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

• Pain was absent or mild in 86% of the patients who received cephacetrile by intramuscular injection [1].
• A patient on chronic intermittent hemodialysis at home showed signs of acute encephalopathy after an 8-day's treatment with a total dose of 78 g cephacetril (Celospor) [15].
• After intravenous injection of 1 gm of the antibiotic, the plasma clearance of cephacetrile was 407 ml/min., and its renal clearance 313 ml/min [16].
• The animals were divided into experimental groups, each treated subcutaneously with different amounts of cephacetrile (50, 100 and 500 mg/kg/die), control group receiving physiological solution [17].

References