Ceftolozane
Ceftolozane Uses, Dosage, Side Effects, Food Interaction and all others data.
Ceftolozane is a semi-synthetic broad-spectrum fifth generation cephalosporin. It was approved by the FDA in 2014 for use in combination with Tazobactam for the treatment of serious infections, such as intra-abdominal infections and complicated urinary tract infections. The manufacturer of this drug is Cubist Pharmaceuticals. Most recently, in June 2019, ceftolozane-tazobactam was approved for the treatment of hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia.
Hospital-acquired pneumonia and ventilator-associated pneumonia are major causes of morbidity and mortality in hospitalized patients and the use of ceftolozane-tazobactam offers effective activity against various organisms causing these infections, such as Pseudomonas aeruginosa.
Ceftolozane exerts bactericidal activities against susceptible gram-negative and gram-positive infections by interfering with bacterial cell wall synthesis. When it is combined with tazobactam, it exerts further activity against beta-lactamase enzyme producing bacteria, which are normally resistant to beta-lactam antibiotics and interfere with infection treatment. The addition of tazobactam strengthens the therapeutic response to ceftolozane, giving it the ability to treat a broader range of bacterial infections and resistant organisms.
| Trade Name | Ceftolozane |
| Generic | Ceftolozane |
| Ceftolozane Other Names | Ceftolozane, ceftolozano |
| Type | |
| Formula | C23H30N12O8S2 |
| Weight | Average: 666.69 Monoisotopic: 666.175098322 |
| Protein binding | 16% to 21% bound to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ceftolozane is a cephalosporin antibiotic used to treat complicated intra-abdominal infections in combination with metronidazole, complicated urinary tract infections, and hospital-acquired pneumonia.
This drug is administered in combination with tazobactam for the treatment of complicated intra-abdominal infections (in combination with metronidazole) and complicated urinary tract infections, which may include pyelonephritis. Ceftolozane-tazobactam is also indicated in the treatment of bacterial ventilator-associated pneumonia and bacterial hospital-acquired pneumonia.
Ceftolozane is also used to associated treatment for these conditions: Hospital Acquired Bacterial Pneumonia, Ventilator Associated Bacterial Pneumonia, Complicated Bacterial Urinary Tract Infections, Complicated Pyelonephritis, Complicated intra-abdominal bacterial infections
How Ceftolozane works
Ceftolozane belongs to the cephalosporin class of antibacterial drugs. Ceftolozane exerts antibacterial effects, preventing the formation of cell walls that protect bacteria from injury and confer resistance to some antibiotics. Its antibacterial activity is also mediated through ceftolozane binding to penicillin-binding proteins (PBPs), which are required for peptidoglycan cross-linking for bacterial cell wall synthesis. As a result of cell wall synthesis inhibition, bacterial cells are killed, treating various infections. Ceftolozane has a particularly high affinity to the penicillin-binding proteins for Pseudomonas aeruginosa and Escherichia coli as well as Klebsiella pneumoniae and other enteric bacteria. In particular, a high affinity has been seen in vitro for penicillin-binding proteins 1b, 1c, 2, and 3 when compared to other antibiotics, ceftazidime and imipenem.
Toxicity
A note on nephrotoxicity
This drug is mainly excreted by the kidneys, and if administered to a patient with a creatinine clearance of less than 50 mL/min, may cause renal damage. Consult official product labeling for dosing adjustments in patients with renal impairment.
Overdose information
If an overdose occurs, discontinue the drug and follow this with supportive treatment. Dialysis may be used.
Use in pregnancy
Ceftolozane-tazobactam is a pregnancy category B drug, but human studies have not been performed to validate this in humans. At doses equivalent to 4-7 the standard dose administered in humans, no developmental abnormalities were seen. Since animal studies are not always predictive of drug response in humans, it is advisable to exercise caution if this drug is prescribed during pregnancy. The mother's clinical need should be assessed as well as possible risks to the fetus.
Use in lactation
Whether this drug is excreted in human breast milk is unknown. Caution is advised if this drug is administered during lactation, as many other drugs are known to be secreted into breast milk.
Carcinogenesis/mutagenesis
Formal studies have not been conducted in humans to assess mutagenicity or carcinogenicity. Studies in mice and rats did not reveal any mutagenic or carcinogenic potential, however, the potential risks resulting from long-term use have not been studied.
Food Interaction
No interactions found.Volume of Distribution
13.5 L Tissue distribution of ceftalozone-tazobactam is rapid and shows good penetration into the lung, rendering it an ideal treatment for bacterial pneumonia.
Elimination Route
The area under the curve (AUC) of ceftolozane-tazobactam after an injected dose of 1 g/0.5 g every 8 hours for 1 day was 172 mcg•h/mL. The Cmax (peak concentration) and AUC are dose-dependent. The Cmax on day one of the above dose of ceftolozane-tazobactam was 69.1 mcg/mL.
Half Life
2.77 hours on day 1 of treatment on a dose of 1 g/0.5 g every 8 hours. 3.12 hours on day 10 of treatment on a dose of 1 g/0.5 g every 8 hours.
Clearance
The renal clearance of was measured to be 3.41 – 6.69 L/h after a single dose of ceftolozane-tazobactam. Dose adjustments of this drug are required in patients with impaired renal function with a creatinine clearance of 50 mL/min or below. Consult official labeling for dosing adjustment guidelines.
Elimination Route
Ceftolozane is mainly excreted in the urine.
Innovators Monograph
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