Cefalotin

First-generation cephalosporins (cefalotin, cefaloridin, cephalexin, cephapirin, cefa-zolin, cefadroxil, cephradine, and others) possess high biological activity with respect to staphylococci, streptococci, pneumococci, and many types of enterobacteria. 

Cefalotin Cefalotin, (6/ -frfl )-3-[(acetyloxy)methyl]-8-oxo-7-[(2-thienylacetyl) amino]-5-thia-l-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (32.1.2.1), is synthesized by direct interaction of 2-thienylacetic acid chloride with 7-aminocephalosporanic acid in the presence of sodium bicarbonate [70-74]. 

Cefalotin is used for bacterial infections of the lower respiratory tract, urinary tract, skin, soft tissues, bones and joints, sepsis, peritonitis, osteomyelitis, mastitis, infected wounds, and post-operational infections. Synonyms of this drag are ceflin, seffein, coaxin, and others. 

The second necessary fragment, 7-amino-3-(l-pyridinomethyl)cef-3-en-carbonic acid (32.1.2.80), is synthesized from cefalosporidin (32.1.2.79), a cephalosporin antibiotic that is used independently in medicine and which is synthesized in the form of an internal salt by reacting cefalotin (32.1.2.1) with pyridine to replace the acetoxyl group with a pyridine group. Initially treating cephaloridin with trimethylchlorosilane in the presence of dimethylaniline and then with phosphorous pentachloride, followed by a reaction with 1,... 

CH2OCOMe cefalotin (cephalothin) R2 group unstable to mammalian esterases generally superseded... 

F Cefalotine (Panpharma) Coaxin (Tobishi) Toricelocin (Torii)... 

In isolated cases, cefalotin (3) and cefaclor (4) have been suspected to cause hypersensitivity myocarditis. 

Autoimmune hemolytic anemia has rarely been reported with the older cephalosporins, including cefalexin (40), cefalotin (41,42), cefazolin (43), and cefaloridine (44). The main laboratory findings correspond to the drug adsorption mechanism classically found in benzylpenicil-lin-induced immune hemolysis. Antibodies cross-reacting with cefalotin and benzylpenicillin were found in both benzylpenicillin-induced and cefalotin-induced hemolysis (43,45) Cases have also been reported with cefamandole (46), cefalexin (47), ceftriaxone (48), cefotaxime (49,50), cefotetan (51,52) and ceftazidime (53). 

Thrombocytopenia has rarely been reported, always associated with cefalotin (83-85). In one case there were drug-dependent antibodies. In two other cases the role of drug-dependent antibodies was further evaluated. In one case the antibodies only reacted with platelets in the presence of exogenons cefotetan, but not with cefotetan-coated platelets (86). In another case associated with cefamandole, antibodies cross-reacted with two cephalosporins that had a thiomethyltetrazole gronp at position 3 but not with other cephalosporins (87). In an additional case, cefuroxime has been implicated (88). In abont one-third of cases with cephalosporin-indnced nentropenia, slight concomitant thrombocjdopenia has been found (73). 

Cefalotin can cause two types of renal disease in man (111) acute tubular necrosis, similar to that seen with cefaloridine, although less often and acute interstitial nephritis, often accompanied by a rash, fever, or eosino-phUia, resembling the same disorder as that caused by methicillin. 

In a retrospective study the frequency of systemic anaphylaxis to cefaloridine, cefalotin, or cefalexin was two out of 9388 patients (0.02%) without a history of penicillin allergy, and two out of 450 patients (0.4%) with a history of peniciUin allergy (152). In the first group, two of the 1983 patients treated with cefalotin accounted for the adverse event. 

Thrombophlebitis is a common reaction to the administration of cephalosporins into peripheral veins. The use of buffered solutions mitigated the reaction with cefalotin (192). Published trials have mainly compared older cephalosporins, but the overall results are still contradictory (193,194). Pain and inflammatory reactions after intramuscular injection are also common. Ceftriaxone is probably given more often intramuscularly now than any other cephalosporin. Its local tolerability does not differ from that of other compounds (195). 

Certain cephalosporins (cefoxitin, cefpirome, cefacetrile, cefaloglycin, cefaloridine, cefalotin) react with alkaline picrate solution, forming a chromogen with the same spectrum of absorbance as that formed by creatinine and alkaline picrate, producing falsely high serum... 

Reports of drug-induced thrombocytopenia have been systematically reviewed (78). Among the 98 different drugs described in 561 articles the following antibiotics were found with level I (definite) evidence co-trimoxa-zole, rifampicin, vancomycin, sulfisoxazole, cefalotin, piperacillin, methicillin, novobiocin. Drugs with level II (probable) evidence were oxytetracycline and ampicillin. 

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