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Cefetamet Sale

(Synonyms: 盐酸头孢他美,Ro 15-8074; Deacetoxycefotaxime) 目录号 : GC63974

Cefetamet 是一种头孢类抗生素。Cefetamet 具有研究上、下社区获得性呼吸道感染的潜力。

Cefetamet Chemical Structure

Cas No.:65052-63-3

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5 mg
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10 mg
¥495.00
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25 mg
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50 mg
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100 mg
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产品描述

Cefetamet is a cephalosporin antibiotic. Cefetamet has the potential for the research of both upper and lower community-acquired respiratory tract infections[1].

[1]. Bryson HM, et al. Cefetamet pivoxil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1993;45(4):589-621.

Chemical Properties

Cas No. 65052-63-3 SDF Download SDF
别名 盐酸头孢他美,Ro 15-8074; Deacetoxycefotaxime
分子式 C14H15N5O5S2 分子量 397.43
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1 mM 2.5162 mL 12.5808 mL 25.1617 mL
5 mM 0.5032 mL 2.5162 mL 5.0323 mL
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Research Update

Cefetamet pivoxil clinical pharmacokinetics

Clin Pharmacokinet 1993 Sep;25(3):172-88.PMID:8222459DOI:10.2165/00003088-199325030-00002.

Cefetamet pivoxil is an orally absorbed prodrug ester of the microbiologically active cephalosporin, Cefetamet. The prodrug ester is completely hydrolysed to the active compound Cefetamet on its first pass through the gut wall, the liver or both. Cefetamet is classified as a third generation cephalosporin with excellent activity against streptococci, Enterobacteriaceae, Neisseria and Haemophilus species. It has enhanced stability against beta-lactamases compared with penicillins and first and second generation cephalosporins. The antibacterial spectrum is comparable with that of cefotaxime except for its poor activity against staphylococci. Following a 20-minute zero-order intravenous infusion, Cefetamet had a rapid distribution phase followed by a monoexponential decline. The average pharmacokinetic parameters from 152 healthy volunteers were: total body clearance 136 ml/min (8.16 L/h); renal clearance 119 ml/min (7.14 L/h); nonrenal clearance 17 ml/min (1.02 L/h); volume of distribution at steady-state 0.29 L/kg; terminal elimination half-life 2.2 hours; 88% of the dose recovered in the urine. Cefetamet is not extensively bound to plasma proteins. Consequently, these data indicate that Cefetamet is predominantly eliminated unchanged by the kidney via glomerular filtration with possibly a minor component of tubular secretion. Cefetamet has a relatively small apparent volume of distribution consistent with that of other beta-lactam antibiotics. Results following ascending intravenous doses of Cefetamet in healthy young male volunteers demonstrated that the pharmacokinetics of intravenous Cefetamet are independent of the dose. The absolute bioavailability of Cefetamet tablets following oral Cefetamet pivoxil administration is enhanced by the presence of food. Under fed conditions, 50 to 60% of the final oral dose is absorbed into the systemic circulation. This food effect is observed when Cefetamet pivoxil is administered within 1 hour of a meal. Food also produces a slight delay in the time to reach peak plasma concentrations of this drug. Changes in fluid volume intake with Cefetamet pivoxil administration have no effect on the bioavailability of this drug. Similar absorption characteristics have been observed for all of the tablet dosage formulations studied during clinical development. The absolute bioavailability of the final syrup dosage formulation was between 38 and 47%. Little improvement in the bioavailability of this preparation has been observed with food. The absorption and disposition of Cefetamet in human subpopulations [i.e. children, elderly (< 75 years of age), renal impairment, liver disease and patients taking concomitant drugs] have been studied extensively. Only impaired renal function appears to significantly alter the elimination of this drug.(ABSTRACT TRUNCATED AT 400 WORDS)

Cefetamet pivoxil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use

Drugs 1993 Apr;45(4):589-621.PMID:7684677DOI:10.2165/00003495-199345040-00009.

Cefetamet pivoxil is an oral third-generation cephalosporin which is hydrolysed to form the active agent, Cefetamet. Cefetamet has excellent in vitro activity against the major respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci; it is active against beta-lactamase-producing strains of H. influenzae and M. catarrhalis, but has poor activity against penicillin-resistant S. pneumoniae. Cefetamet has marked activity against Neisseria gonorrhoeae and possesses a broad spectrum of activity against Enterobacteriaceae. Both staphylococci and Pseudomonas spp. are resistant to Cefetamet. Cefetamet pivoxil has been investigated in the treatment of both upper and lower community-acquired respiratory tract infections and has demonstrated equivalent efficacy to a number of more established agents, namely cefaclor, amoxicillin and cefixime. In patients with group A beta-haemolytic streptococcal pharyngotonsillitis, a 7-day course of Cefetamet pivoxil was as effective as a 10-day course of the standard agent, phenoxymethylpenicillin, in this indication. In complicated urinary tract infections, Cefetamet pivoxil showed similar efficacy to cefadroxil, cefaclor and cefuroxime axetil. Cefetamet pivoxil was effective in the treatment of otitis media, pneumonia, pharyngotonsillitis and urinary tract infections in children. Preliminary data indicate that single dose Cefetamet pivoxil can effectively eradicate N. gonorrhoeae from both men and women. Cefetamet pivoxil has a tolerability profile similar to that of other oral cephalosporins, with gastrointestinal effects being the most commonly reported adverse events. To date, no symptoms of carnitine deficiency have been reported with Cefetamet pivoxil. Cefetamet pivoxil offers effective alternative oral therapy for outpatient treatment of community-acquired respiratory tract infections, with the advantage of improved activity against H. influenzae and increased beta-lactamase stability. However, its use in areas with a high incidence of penicillin-resistant S. pneumoniae is likely to be limited. Cefetamet pivoxil is also effective in the treatment of urinary tract infections, although further trials are required to define any comparative advantages over other oral agents.

Comparative clinical efficacy of Cefetamet pivoxil in lower respiratory tract infection

Drugs 1994;47 Suppl 3:35-42.PMID:7518765DOI:10.2165/00003495-199400473-00007.

Cefetamet pivoxil, because of its activity against respiratory pathogens and its pharmacokinetic behaviour, is expected to have clinical efficacy in the treatment of lower respiratory tract infection (LRTI). This paper presents an overview of clinical trials conducted worldwide to investigate the efficacy and tolerability of Cefetamet pivoxil in the treatment of adults and children with LRTI. A total of 626 adult patients, the majority of whom presented with exacerbations of chronic bronchitis (n = 500), received oral Cefetamet pivoxil 500 or 1000mg twice daily for 5 to 10 days (n = 351) or a standard comparator agent (n = 275). The comparator agents were amoxicillin (750mg 3 or 4 times daily, or 1000mg twice daily), amoxicillin/clavulanic acid (625mg 3 times daily), or cefaclor (250 or 500mg 3 times daily) administered for 5 to 12 days. A satisfactory clinical outcome (cure + improvement) was achieved in 79 to 94% of evaluable patients. In 336 children, 240 received Cefetamet pivoxil at 2 dosage levels (10 or 20 mg/kg twice daily) for 7 to 12 days and 96 received the standard comparator, cefaclor (10 mg/kg 3 times daily). Cefetamet pivoxil was clinically effective at both dosages, and did not differ significantly compared with cefaclor (clinical cure rates of 97 to 99% with Cefetamet pivoxil and 96% with cefaclor). A separate analysis of 305 patients with community-acquired pneumonia showed clinical successes in 80 to 100% of adults, 75 to 78% of elderly patients, and 98% of children treated with Cefetamet pivoxil.(ABSTRACT TRUNCATED AT 250 WORDS)

Cefetamet pivoxil in the treatment of pharyngitis/tonsillitis in children and adults

Drugs 1994;47 Suppl 3:27-33; discussion 34.PMID:7518764DOI:10.2165/00003495-199400473-00006.

Between 15 and 35% of pharyngeal infections are attributable to Group A beta-haemolytic streptococci. Streptococcal pharyngitis is one of the most common infections in adolescents and children. A specific diagnosis of pharyngitis can be obtained only by isolating organisms in culture. The current treatment of choice for streptococcal pharyngitis/tonsillitis is a 10-day course of phenoxymethylpenicillin (penicillin V); however, unresolved problems concerning the use of penicillin include the timing of therapy, appropriate therapy for treatment failures, chronic carriers and those with frequent recurrences. In addition, failure rates of 10 to 35% have been reported with oral phenoxymethylpenicillin. Effective treatment alternatives in this indication include oral cephalosporin agents or penicillin/beta-lactamase inhibitor combinations. The oral cephalosporins offer the advantage of an improved pharmacokinetic profile, once- or twice-daily administration, a shorter (7-day) regimen, and a low incidence of adverse effects, although these advantages must be balanced against the broad spectrum of these agents (broader than is necessary) and their cost. Clinical trials conducted with Cefetamet pivoxil, a new oral third generation cephalosporin, in both adults and children with pharyngitis/tonsillitis indicate that this agent offers an effective alternative for phenoxymethylpenicillin in this indication.

Pharmacokinetics of oral Cefetamet pivoxil (Ro 15-8075) and intravenous Cefetamet (Ro 15-8074) in humans: a review

Curr Med Res Opin 1989;11(7):432-41.PMID:2673663DOI:10.1185/03007998909115930.

Cefetamet pivoxil belongs to the class of orally absorbed pro-drug esters which are hydrolyzed to the active compound (Cefetamet) on their first pass through the gut wall and/or the liver. The intravenously administered Cefetamet is eliminated predominantly unchanged in the urine by glomerular filtration. Systemic and renal clearance values for Cefetamet were 140 and 130 ml/min, respectively. The plasma protein binding is 22%, whereby the only binding protein is albumin. The steady state volume of distribution (0.29 l/kg) corresponds roughly to the extracellular water space which is consistent with other low protein-bound cephalosporins. In general, after intravenous doses, Cefetamet follows the kinetic behaviour of a cephalosporin with low protein binding, limited non-renal clearance, and renal clearance that is predominantly due to glomerular filtration, e.g. ceftizoxime, ceftazidime. After oral administration, Cefetamet pivoxil shows a significant food effect (F = 41% vs 51%). Hence, Cefetamet pivoxil is recommended to be taken after food. The food effect, however, is not of such a magnitude that it will be of clinical consequence when this recommendation is not followed. The food effect is not related to a change in gastric pH because antacids and ranitidine do not affect the absorption of Cefetamet pivoxil, although in approximately 20% of the subjects absorption of the drug is delayed. The elimination of Cefetamet is directly proportional to renal function. In patients with varying degrees of renal insufficiencies, dosage should be decreased accordingly. Age has no effect on the bioavailability of Cefetamet pivoxil. However, the clearance of Cefetamet is higher in children and lower in the elderly.