Cephapirine

Aminocephalosporanic acid Cefazolin sodium Ceftizoxime Cephacetriie sodium Cephalogiycin Cephaloridine Cephalothin sodium Cephapirin sodium 2-Amino-5-chlorobenzonitrile Ciorazepate dipotassium 2-Amino-5-chlorobenzophenone Chlordiazepoxide HCi Pinazepam Prazepam... 

Timolol maleate a-Bromoacetophenone Nomifensine maleate Bromoacetyl bromide Bromazepam Cephapirin sodium Clonazepam Flunitrazepam 5-Bromoacetyl salicylamide Labetalol HCI m-Bromoanisole Tramadol HCI p-Bromoanisole Cyclofenil Bromobenzene... 

First generation-cephalexin (Keflex), cefazolin (Ancef), cephapirin (Cefadyl) Second generation-cefaclor (Cedor), cefoxitin (Mefoxin), cefuroxime (Zinacef)... 

Pharmaeokinetie properties of the cephalosporins depend to a considerable extent on their ehemieal nature, e.g. the substituent R. The 3-acetoxymethyl compounds such as cephalothin, cephapirin and cephacetrile are converted in vivo by esterases to the antibaeterially less aetive 3-hydroxymethyl derivatives and are excreted partly as such. The rapid exeretion means that such cephalosporins have a short half-life in the body. Replaeement of the 3-acetoxymethyl group by a variety of groups has rendered other eephalosporins mueh less prone to esterase attack. For example, cephaloridine has an internally eompensated betaine group at position 3 (R ) and is metabolically stable. 

A more traditional cephalosporin analogue is cephapirin (22). It was made by reacting 7-aminocephalo-sporanic acid with bromoacetyl chloride to give amide 21. The halo group was displaced by 4-thiopyridine... 

Cephalosporin Ceftiofur and cephapirin Gastrointestinal upset, diarrhea, nausea and allergic reactions... 

OTC - cephapirin, erythromycin, novobiocin, oxytetracycline, penicillin, penicillin and novobiocin in combination, penicillin and dihydrostreptomycin in combination. 

Specialized antibiotic formulations have been developed for DCT, with physicochemical properties chosen to confer prolonged retention in the mammary secretions (21,, ). Ziv ( ) has summarized the desirable kinetic and other properties of such a product. The following antibiotic formulations are presently approved by the U.S. Center for Veterinary Medicine, FDA for infusion into the dry mammary gland erythromycin (300 mg), oxytetracycline-HCl (426 mg), benzathine cloxacillin (500 mg), cephapirin benzathine (300 mg), novobiocin (400 penicillin (200,000 lU) novobiocin (400 mg), penicil-... 

Tolerances for these compounds are generally O-.Ol ppm except for penicillin G in cattle (.05 ppm) and cephapirin in edible tissue (0.1 ppm) and milk (.02 ppm) (70). Many chromatographic methods have been described for determination of these compounds in clinical applications, but these methods are not sufficiently sensitive for residue analysis. The summary of methods in Table II includes one GLC (71), five TLC (72-76), and five HPLC methods (77-81). Four of the TLC methods use detection by bioautography. Three HPLC methods have been described for milk (77-79) and two for tissue (80,81). The HPLC methods described by Moats C7 ,80) and by Munns et al (77) are satisfactory for any penicillin with a neutral side-chain and this may be true with the procedure of Terada, et al. (81). The procedure of Terada and Sakabe (79) is also satisfactory for the aminopenicillin, amplclllin. The method of Munns et al (77) can also be used to detect the corresponding penicilloic acid metabolites. 

Ceph - Cephapirin Ox - oxacillin, Amp - ampicillin, BCD - Electron capture detection... 

Penicillins form several major metabolites which are excreted in the urine (83,84). These metabolites are usually inactive microbio-logically and they would not be detected by the usual microbiological tests. There are no analytical methods for these metabolites in tissues and, therefore, little is known as to their occurrence and persistence in tissues. There are no methods available for identifying residues of some commonly used B-lactam antibiotics including carbenicillin and ticarcillin. For cephapirin and ampicillin, except for one HPLC method for ampicillin in milk (79) only TLC procedures (72-74,76) with detection by bioautography are reported. 

Cefadroxi1, 440 Cefamandole, 441 Cefazolin, 442 cefoxitin, 435, 443 Cephalexin, 439 Cephamycin C, 442 Cephradine, 440 Cephapirin, 441 Cetophenicol, 46 Chioramphenicol, 28, 45 Chlordiazepoxide, 401 Chlormadinone acetate, 165 p-Chlorophenylalanine, 52 Chlorothiazide, 395 Chlorpromazine, 409 Cholinergic transmission, 71... 

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. 

Cephapirin Cephapirin, (6/ -franx)-3-[(acetyloxy)methyl]-8-oxo-7-[[(4-pyridinylthio) acetyl]amino]-5-thia-l-azabicyclo[4.2.0]oct-2-en-2-carboxylic acid (32.1.2.4), is synthesized by acylating 7-aminocephalosporanic acid with 4-pyridylthioacetic acid chloride (32.1.2.3), which is synthesized by reacting 4-chloropyridine with mercaptoacetic acid in the presence of a base, forming 4-pyridylthioacetic acid (32.1.22), and further transforming the resulting acid to the acid chloride by reacting it with phosphorous pentachloride. 

An alternative way of making cephapirin is the acylation of 7-aminocephalosporanic acid by bromoacetyl bromide, which gives a bromoacetyl derivative (32.1.2.5), and which is then reacted with 4-mercaptopyridine in the presence of triethylamine, forming the desired cephapirin (32.1.2.4) [75-78]. 

The spectrum of action and indications for use of cephapirin are the same as those of cephalothin. Synonyms of this drug are bristocef, cefarin, cefatrexyl, cefadil, and others. 

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