Cefmetazole

Cefmetazole (78) is a cephamycin-inspired cephalosporin differing from the mainstream compounds in having an aliphatic amide moiety attached to C-7. Its antibacterial spectrum is similar to the second generation agent cefoxitin. The synthesis starts with 7-aminocephalosporan-... 

The structures of the drugs used as a small test set for the model are listed in Table 17.1. Loperamide and asimadoline are P-gp substrates terfenadine and ebastine are compounds that are rapidly metabolized alprazolam, dobazam, di-and mono-hydroxy-L66858 [11] are benzodiazepines testosterone and corticosterone are hormones and cefadroxyl, cefaclor, cephalotin and cefmetazole are cephalosporins [12]. Finally, peptides 1 to 10 are peptidomimetic drugs [13]. 

Cefmetazole Dosage Guidelines in Renal Function Impairment... 

Safety and efficacy of cefmetazole, cefoperazone, cephalexin, and cefotetan in... 

Urinary excretion is the major elimination path for most cephalosporins. When prescribing cephalosporins to patients with renal failure, practitioners must consider dose reduction or dose interval extension (Table 45.2). Renal tubular secretion contributes to the elimination of some cephalosporins, and an increase in cephalosporin plasma concentrations may occur when probenecid blocks renal tubular secretion of cephalosporins. Biliary elimination is important for some cephalosporins. Cefmetazole, cefoperazone (Cefobid), cefoxitin, and ceftriaxone achieve biliary concentrations greater than those in plasma. After parenteral administration of cefoperazone, 70% of the dose appears in the bile within 24 hours. Practitioners should decrease the dose of cefoperazone when prescribing for patients with hepatic failure or biliary obstruction. Metabolism is not a major elimination path for most cephalosporins. Cefotaxime is one of the few cephalosporins having an active metabolite, desacetyl cefotaxime. 

Cephalosporins that contain a methylthiotetrazole group (eg, cefamandole, cefmetazole, cefotetan, cefoperazone) frequently cause hypoprothrombinemia and bleeding disorders. Administration of vitamin Ki, 10 mg twice weekly, can prevent this. Drugs with the methylthiotetrazole ring can also cause severe disulfiram-like reactions consequently, alcohol and alcohol-containing medications must be avoided. 

Oral 250, 500 mg capsules 375, 500 mg extended-release tablets powder to reconstitute for 125, 187, 250, 375 mg/5 mL suspension Cefmetazole (Zefazone)... 

Recent studies describe the use of cyclic voltammetry in conjunction with controlled-potential coulometry to study the oxidative reaction mechanisms of benzofuran derivatives [115] and bamipine hydrochloride [116]. The use of fast-scan cyclic voltammetry and linear sweep voltammetry to study the reduction kinetic and thermodynamic parameters of cefazolin and cefmetazole has also been described [117]. Determinations of vitamins have been studied with voltammetric techniques, such as differential pulse voltammetry for vitamin D3 with a rotating glassy carbon electrode [118,119], and cyclic voltammetry and square-wave adsorptive stripping voltammetry for vitamin K3 (menadione) [120]. 

CyDs are known to be able to solubilize lipophilic drugs as well as lipophilic absorption enhancers, leading to the improvement of the enhancer s efficiency. There are some reports on the use of CyDs as a candidate for a coenhancer. For example, Yanagi et al. [35] reported that CyDs may promote the potency of absorption enhancers in rectum of rabbits. Inclusion complex of decanoic acid (CIO), an absorption enhancer, with a-CyD was prepared as an additive of cefmetazole sodium suppository and rectally administered to rabbits. Plasma concentration and area under the curve (AUC) of cefmetazole sodium after rectal administration of a suppository containing ClO-a-CyD complex to rabbits increased more significantly than those with no additive. 

Yanagi, H., et al. 1991. Effect of inclusion complexation of decanoic acid with a-cyclodextrin on rectal absorption of cefmetazole sodium suppository in rabbits. Yakugaku Zasshi 111 65. 

Nishihata, T., J.H. Rytting, and T. Higuchi. 1982. Enhanced rectal absorption of theophylline, lidocaine, cefmetazole, and levodopa by several adjuvants. J Pharm Sci 71 865. 

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