Zobactin
Zobactin Uses, Dosage, Side Effects, Food Interaction and all others data.
Semisynthetic, broad-spectrum, ampicillin derived ureidopenicillin antibiotic proposed for pseudomonas infections. It is also used in combination with other antibiotics.
Piperacillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Piperacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Piperacillin results from the inhibition of cell wall synthesis and is mediated through Piperacillin binding to penicillin binding proteins (PBPs). Piperacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.
Tazobactam is an antibiotic of the beta-lactamase inhibitor class that prevents the breakdown of other antibiotics by beta-lactamase enzyme producing organisms. It is combined with Piperacillin and Ceftolozane for the treatment of a variety of bacterial infections.
Piperacillin-tazobactam was initially approved by the FDA in 1994, and ceftolozane-tazobactam was approved by the FDA in 2014, providing wider antibacterial coverage for gram-negative infections. In June 2019, ceftolozane-tazobactam was approved by the FDA for treating hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia, which are significant causes of morbidity and mortality in hospitalized patients.
Tazobactam inhibits the action of bacterial beta-lactamase producing organisms, which are normally resistant to beta-lactam antibiotics. This augments the effects of antibiotics which would otherwise not be effective in treating certain infections. These antibiotics contain a beta-lactam ring in their chemical structure, which is destroyed by beta-lactam resistant organisms. When combined with other antibiotics, a variety of infections, including serious and life-threatening infections may be treated.
| Trade Name | Zobactin |
| Generic | Tazobactam + Piperacillin |
| Weight | 500mg |
| Type | Injection |
| Therapeutic Class | |
| Manufacturer | Glaxosmithkline |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Piperacillin is a penicillin antibiotic combined with tazobactam to treat piperacillin-resistant, piperacillin/tazobactam susceptible, β-lactamase generating strains of several bacteria.
For the treatment of polymicrobial infections.
Tazobactam is a beta lactamase inhibitor administered with antibiotics such as piperacillin and ceftolozane to prevent their degradation, resulting in increased efficacy.
Tazobactam is used in combination with piperacillin or ceftolozane to broaden the spectrum of piperacillin antibacterial action, treating susceptible infections. As with any other antibiotic, tazobactam should only be used for infections that are either proven or strongly suspected to be susceptible to the tazobactam containing drug.
Tazobactam-piperacillin
When combined with piperacillin, it is used to treat a variety of infections, including those caused by aerobic and facultative gram-positive and gram-negative bacteria, in addition to gram-positive and gram-negative anaerobes. Some examples of infections treated with piperacillin-tazobactam include cellulitis, diabetic foot infections, appendicitis, and postpartum endometritis infections. Certain gram-negative bacilli infections with beta-lactamase producing organisms cannot be treated with piperacillin-tazobactam, due to a gene mutation conferring antibiotic resistance.
Tazobactam-ceftolozane
Tazobactam-ceftolozane combined with metronidazole is used to treat complicated urinary tract infections (UTI) and complicated intra-abdominal infections, as well as ventilator-associated bacterial pneumonia and hospital-acquired bacterial pneumonia.. This combination increases efficacy against infections with gram-negative bacilli.
Zobactin is also used to associated treatment for these conditions: Animal bite, Complicated Appendicitis, Pelvic Inflammatory Disease (PID), Peritonitis, Postpartum Endometritis, Surgical Site Infections, Moderate Bacterial Infections, Moderate Community acquired pneumonia, Moderate Nosocomial pneumonia, Severe Bacterial Infections, Severe Nosocomial pneumonia, Uncomplicated skin and subcutaneous tissue bacterial infectionsAnimal bite, Cellulitis, Complicated Appendicitis, Cutaneous Abscess, Diabetic Foot Ulcers (DFU), Pelvic Inflammatory Disease (PID), Peritonitis, Pneumonia, Hospital-Acquired, Postpartum Endometritis, Surgical Site Infections, Ventilator-Associated Pneumonia (VAP), Complicated Bacterial Urinary Tract Infections, Complicated Pyelonephritis, Complicated intra-abdominal bacterial infections, Moderate Bacterial Infections, Moderate Community acquired pneumonia, Moderate Nosocomial pneumonia, Severe Bacterial Infections, Severe Nosocomial pneumonia, Uncomplicated skin and subcutaneous tissue bacterial infections
How Zobactin works
By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Piperacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Piperacillin interferes with an autolysin inhibitor.
Tazobactam broadens the spectrum of piperacillin and ceftolozane by making them effective against organisms that express beta-lactamase and would normally degrade them. This occurs through the irreversible inhibition of beta-lactamase enzymes. In addition, tazobactam may bind covalently to plasmid-mediated and chromosome-mediated beta-lactamase enzymes. Tazobactam is predominantly effective against the OHIO-1, SHV-1, and TEM groups of beta-lactamases, but may also inhibit other beta-lactamases.
Tazobactam shows little antibacterial activity by itself, and for this reason, is generally not administered alone.
Toxicity
Overdose
Post-marketing reports have been made of overdose cases with piperacillin/tazobactam. Nausea, vomiting, and diarrhea are frequent manifestations of an overdose. Neuromuscular excitability or seizures may also occur with high intravenous doses or renal failure. There is no specific antidote. Provide supportive measures in case of an overdose. Anticonvulsive agents may be indicated when neuromuscular excitability or seizures occur. If anaphylaxis occurs, traditional measures should be taken to manage hypersensitivity (for example, adrenaline, antihistamines, corticosteroids, and oxygen/airway maintenance). Similar measures should be taken after a ceftolozane-tazobactam overdose. Hemodialysis can be used to remove the drug from the circulation .
A note on nephrotoxicity
Cases of life-threatening nephrotoxicity have been seen in critically ill patients receiving piperacillin-tazobactam. Alternative therapy and/or renal monitoring should be considered in critically ill patients.
Carcinogenesis/Mutagenesis
Tazobactam tested negative for genotoxic effects in the Ames assay, an after in vitro chromosomal aberration and point mutation assay in the Chinese hamster, an various other assays.
Use in pregnancy
Tazobactam has been found cross the placenta in rats. No data on human studies are available, however, rat studies have shown no teratogenetic effects at doses 6-14 times the equivalent maximum recommended human dose.
Use in lactation
There are no data on the presence of tazobactam in human breastmilk. No data are currently available on the effects of tazobactam on the infant, or how it affects milk production. Use clinical judgement and consider the maternal need for the drug and the benefits of breastfeeding the infant before administration during lactation. Small concentrations of piperacillin-tazobactam have been found in the breastmilk and can lead to hypersensitivity in a breastfeeding infant. In some cases, breastfeeding may have to be discontinued temporarily.
Volume of Distribution
- 101 mL/kg [intravenous administration of 50 mg/kg (5-minute infusion) in neonates]
18.2 L when given with piperacillin
13.5-18.2 L when given with ceftolozane
Piperacillin-tazobactam is widely distributed in body tissues and fluids. These may include but are not limited to the intestine, gallbladder, lung, female reproductive organs, and the bile. Meningeal distribution of piperacillin-tazobactam increases with inflammation, but is otherwise low.
Elimination Route
Not absorbed following oral administration.
Tazobactam is coadministered with piperacillin or ceftolozane, pharmacokinetic information will be provided for these combinations.
Piperacillin-tazobactam
Peak plasma concentrations occur immediately after the completion of intravenous infusion. Following several doses of piperacillin-tazobactam infusions every 6 hours, peak concentrations were similar to those that were measured after the initial dose.
Ceftolozane-piperacillin
AUC: 24.4-25 mcg•h/mL
Peak concentrations are reached on day 1 after the first dose and range from 18 to 18.4 mcg/mL.
Half Life
36-72 minutes
Piperacillin-tazobactam
After a single dose in healthy volunteers, the plasma half-life of piperacillin and tazobactam was in the range of 0.7 to 1.2 hours.
Ceftolozane-tazobactam
0.91-1.03 hours
Clearance
- 32 - 41 mL/min/1.73 m2
- 124 - 160 mL/min/1.73 m2 [older pediatric patients]
Because tazobactam is cleared by the kidneys and is a substrate of the transporters OAT1 and OAT3, inhibitors of these transporters should be avoided to ensure efficacy. Dosage adjustments of piperacillin-tazobactam and ceftolozane-tazobactam must be made for patients with impaired renal clearance.
The mean clearance rate of tazobactam was found to be 48.3-83.6 mL/min in patients admitted to the intensive care unit who were given renal replacement therapy and receiving intravenous piperacillin-tazobactam.
The clearance of tazobactam is dependent on renal function, as determined by renal clearance.
Elimination Route
As with other penicillins, PIPRACIL is eliminated primarily by glomerular filtration and tubular secretion; it is excreted rapidly as unchanged drug in high concentrations in the urine. Because PIPRACIL is excreted by the biliary route as well as by the renal route, it can be used safely in appropriate dosage in patients with severely restricted kidney function.
Tazobactam and its metabolite are mainly eliminated by the kidneys with about 80% of the administered dose eliminated as unchanged drug. The remaining drug is excreted as a single metabolite.
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