Temocillin
Encyclopedia
Temocillin is a β-lactamase
resistant penicillin
introduced by Beecham
, marketed by Eumedica Pharmaceuticals as Negaban primarily for the treatment of multiresistant Gram negative bacteria.
It is a carboxypenicillin
.
resistant penicillin
. It is not active against Gram positive bacteria or bacteria with altered penicillin-binding proteins.
It is normally active against Moraxella catarrhalis
, Brucella abortus, Burkholderia cepacia, Citrobacter
species, Escherichia coli
, Haemophilus influenzae
, Klebsiella pneumoniae
, Pasteurella multocida
, Proteus mirabilis
, Salmonella typhimurium and Yersinia enterocolitica
. It is also active against some Enterobacter
species, Morganella morganii
, and Serratia
species. Temocillin has no useful activity against Gram positive organisms, Acinetobacter
species, or Pseudomonas aeruginosa
.
Its primary use is against Enterobacteriaceae
, and in particular against strains producing extended spectrum β-lactamase or AmpC β-lactamase
.
Temocillin may be given to patients with impaired renal function. No adjustment needs to be made to the dose in mild to moderate renal impairment (creatinine clearance greater than 30ml/min). The manufacturer does not recommend using reduced doses, instead they recommend increasing the duration between doses. In severe renal impairment when it is 10 to 30, the dose is 1g in 24 hours; when less than 10, the dose is 1g every 48 hours. Temocillin is cleared by haemodialysis, which means that in dialysis patients, the dose should be given after dialysis.
There is no licensed oral preparation of temocillin.
infection. As with any other penicillin, convulsions can occur if very high doses are given.
Beta-lactamase
Beta-lactamases are enzymes produced by some bacteria and are responsible for their resistance to beta-lactam antibiotics like penicillins, cephamycins, and carbapenems . These antibiotics have a common element in their molecular structure: a four-atom ring known as a beta-lactam...
resistant penicillin
Penicillin
Penicillin is a group of antibiotics derived from Penicillium fungi. They include penicillin G, procaine penicillin, benzathine penicillin, and penicillin V....
introduced by Beecham
Beecham (pharmaceutical company)
Beecham was a British pharmaceutical company. It was once a constituent of the FTSE 100 Index. Beecham, after having merged with SmithKline Beckman, merged with GlaxoWellcome to become GlaxoSmithKline .-History:...
, marketed by Eumedica Pharmaceuticals as Negaban primarily for the treatment of multiresistant Gram negative bacteria.
It is a carboxypenicillin
Carboxypenicillin
The carboxypenicillins are a group of antibiotics. They belong to the penicillin family and comprise the members carbenicillin and ticarcillin.- Chemical structure :...
.
Pharmacology
Temocillin is a β-lactamaseBeta-lactamase
Beta-lactamases are enzymes produced by some bacteria and are responsible for their resistance to beta-lactam antibiotics like penicillins, cephamycins, and carbapenems . These antibiotics have a common element in their molecular structure: a four-atom ring known as a beta-lactam...
resistant penicillin
Penicillin
Penicillin is a group of antibiotics derived from Penicillium fungi. They include penicillin G, procaine penicillin, benzathine penicillin, and penicillin V....
. It is not active against Gram positive bacteria or bacteria with altered penicillin-binding proteins.
It is normally active against Moraxella catarrhalis
Moraxella catarrhalis
Moraxella catarrhalis is a fastidious, nonmotile, Gram-negative, aerobic, oxidase-positive diplococcus that can cause infections of the respiratory system, middle ear, eye, central nervous system and joints of humans.-History:...
, Brucella abortus, Burkholderia cepacia, Citrobacter
Citrobacter
Citrobacter is a genus of Gram-negative coliform bacteria in the Enterobacteriaceae family.The species C. amalonaticus, C. koseri, and C. freundii use solely citrate as a carbon source...
species, Escherichia coli
Escherichia coli
Escherichia coli is a Gram-negative, rod-shaped bacterium that is commonly found in the lower intestine of warm-blooded organisms . Most E. coli strains are harmless, but some serotypes can cause serious food poisoning in humans, and are occasionally responsible for product recalls...
, Haemophilus influenzae
Haemophilus influenzae
Haemophilus influenzae, formerly called Pfeiffer's bacillus or Bacillus influenzae, Gram-negative, rod-shaped bacterium first described in 1892 by Richard Pfeiffer during an influenza pandemic. A member of the Pasteurellaceae family, it is generally aerobic, but can grow as a facultative anaerobe. H...
, Klebsiella pneumoniae
Klebsiella pneumoniae
Klebsiella pneumoniae is a Gram-negative, non-motile, encapsulated, lactose fermenting, facultative anaerobic, rod shaped bacterium found in the normal flora of the mouth, skin, and intestines....
, Pasteurella multocida
Pasteurella multocida
Pasteurella multocida is a Gram-negative, non-motile coccobacillus that is penicillin-sensitive and belongs to the Pasteurellaceae family . It can cause avian cholera in birds and a zoonotic infection in humans, which typically is a result of bites or scratches from domestic pets...
, Proteus mirabilis
Proteus mirabilis
Proteus mirabilis is a Gram-negative, facultatively anaerobic, rod shaped bacterium. It shows swarming motility, and urease activity. P. mirabilis causes 90% of all Proteus infections in humans.-Diagnosis:...
, Salmonella typhimurium and Yersinia enterocolitica
Yersinia enterocolitica
Yersinia enterocolitica is a species of gram-negative coccobacillus-shaped bacterium, belonging to the family Enterobacteriaceae. Yersinia enterocolitica infection causes the disease yersiniosis, which is a zoonotic disease occurring in humans as well as a wide array of animals such as cattle,...
. It is also active against some Enterobacter
Enterobacter
Enterobacter is a genus of common Gram-negative, facultatively-anaerobic, rod-shaped bacteria of the family Enterobacteriaceae. Several strains of the these bacteria are pathogenic and cause opportunistic infections in immunocompromised hosts and in those who are on mechanical ventilation...
species, Morganella morganii
Morganella morganii
Morganella morganii is a species of Gram-negative bacillus bacteria. It is oxidase-negative and conducts anaerobic respiration. It causes a disease known as Summer Diarrhea....
, and Serratia
Serratia
Serratia is a genus of Gram-negative, facultatively anaerobic, rod-shaped bacteria of the Enterobacteriaceae family. The most common species in the genus, S. marcescens, is normally the only pathogen and usually causes nosocomial infections. However, rare strains of S. plymuthica, S. liquefaciens,...
species. Temocillin has no useful activity against Gram positive organisms, Acinetobacter
Acinetobacter
Acinetobacter [asz−in−ée−toe–back−ter] is a genus of Gram-negative bacteria belonging to the Gammaproteobacteria. Acinetobacter species are non-motile and oxidase-negative, and occur in pairs under magnification....
species, or Pseudomonas aeruginosa
Pseudomonas aeruginosa
Pseudomonas aeruginosa is a common bacterium that can cause disease in animals, including humans. It is found in soil, water, skin flora, and most man-made environments throughout the world. It thrives not only in normal atmospheres, but also in hypoxic atmospheres, and has, thus, colonized many...
.
Its primary use is against Enterobacteriaceae
Enterobacteriaceae
The Enterobacteriaceae is a large family of bacteria that includes many of the more familiar pathogens, such as Salmonella, Escherichia coli, Yersinia pestis, Klebsiella and Shigella. This family is the only representative in the order Enterobacteriales of the class Gammaproteobacteria in the...
, and in particular against strains producing extended spectrum β-lactamase or AmpC β-lactamase
Beta-lactamase
Beta-lactamases are enzymes produced by some bacteria and are responsible for their resistance to beta-lactam antibiotics like penicillins, cephamycins, and carbapenems . These antibiotics have a common element in their molecular structure: a four-atom ring known as a beta-lactam...
.
Dosage
The common dosage is 2g intravenously every 12 hours. There are good theoretical reasons for giving Temocillin as a continuous intravenous infusion in severe disease: a single loading dose of 2g is given intravenously followed by a 4g infusion over 24 hours. Temocillin for intravenous injection is diluted in 20ml of sterile water; it is diluted in less than 2.7ml of sterile water when being prepared for intramuscular injection; the continuous infusion is diluted in 48ml of sterile water for ease of administration (1ml per half hour). To reduce pain, the intramuscular injection may be made up using sterile 1% lignocaine instead of sterile water.Temocillin may be given to patients with impaired renal function. No adjustment needs to be made to the dose in mild to moderate renal impairment (creatinine clearance greater than 30ml/min). The manufacturer does not recommend using reduced doses, instead they recommend increasing the duration between doses. In severe renal impairment when it is 10 to 30, the dose is 1g in 24 hours; when less than 10, the dose is 1g every 48 hours. Temocillin is cleared by haemodialysis, which means that in dialysis patients, the dose should be given after dialysis.
There is no licensed oral preparation of temocillin.
Adverse effects
The undesirable effects of temocillin are those of any β-lactam antibiotic. In particular, Temocillin has been associated with angioedema and anaphylaxis in penicillin allergic patients. Animal studies have not shown any induction of Clostridium difficileClostridium difficile
Clostridium difficile , also known as "CDF/cdf", or "C...
infection. As with any other penicillin, convulsions can occur if very high doses are given.