Kenzolin

Piperacillin sodium, tazobactam sodium.

Each vial contains: Piperacillin Sodium eq. to Piperacillin 4 g and Tazobactam Sodium eq. to Tazobactam 500 mg.

Pharmacology: Pharmacodynamics: Piperacillin is an antibiotic that has the ability to kill a wide variety of bacteria. It works by interfering with the formation of bacterial cell walls. It does this by preventing the bacteria from vital cross-links within their cell walls. These cross-links strengthen the cell walls and allow them to protect the bacteria from their environment. By interfering with the cross linking meshwork in the cell walls, piperacillin weakens them. The cell walls of bacteria are essential for their survival. They protect the bacteria from environment and keep unwanted substances from entering the cells. As piperacillin weakens the cell walls, it allows unwanted substances to enter the bacteria cells. This causes the cells to swell and eventually rupture, and kills the bacteria. Certain bacteria are resistant to penicillin-type antibiotics, because they have developed the ability to produce defensive chemicals. These chemicals are called beta-lactamases. They interfere with the structure of penicillin-type antibiotics and stop them from working. Tazobactam is a type of medicine known as beta-lactamase inhibitor. It is included in this medicine because it inhibits the action of the beta lactamases produced by certain bacteria. This prevents the bacteria from inactivating the piperacillin, and then leaves them susceptible to attack. Tazobactam therefore increases the range of bacteria that piperacillin can kill.
Pharmacokinetics: After the administration of single doses of piperacillin/tazobactam to subjects with renal impairment, the half life of piperacillin and tazobactam increases with decreasing creatinine clearance. At creatinine clearance below 20mL/min, the increase in half-life is twofold for piperacillin and fourfold for tazobactam compared to subjects with normal renal function. Piperacillin and tazobactam are widely distributed into tissues and body fluids including intestinal mucosa, gallbladder, lung, female reproductive tissues (uterus, ovary, and fallopian tube), interstitial fluid and bile.
Mean tissue concentrations are generally 50% to 100% of those in plasma. Distribution of piperacillin and tazobactam into cerebrospinal fluid is low in subjects with non-inflamed meninges, as with other penicillins. Piperacillin is metabolized to a minor microbiologically active desethyl metabolite. Tazobactam is metabolized to a single metabolite that lacks pharmacological and antibacterial activities. Both piperacillin and tazobactam are eliminated via the kidney by glomerular filtration and tubular secretion. Piperacillin is excreted rapidly as unchanged drug with 68% of the administered dose excreted in the urine. Tazobactam and its metabolite are eliminated primarily by renal excretion with 80% of the administered dose excreted as unchanged drug and the remainder as the single metabolite. Piperacillin, tazobactam and desethyl piperacillin are also secreted into the bile.

In adults and children over 12 years of age: Bacterial infections of the lungs and airways (chest or lower respiratory tract infections); Bacterial infections within the abdomen; Bacterial infections of the urinary tract; Bacterial infection of the skin; Bacterial infections of the blood (septicaemia or blood poisoning); Bacterial infections in people with low white blood cell (neutropenia) and hence decreased ability to fight infection (used in combination with an aminoglycosides antibiotic for this purpose).
In children under 12 years of age: Appendicitis complicated by a burst appendix, peritonitis and/or abscess formation.
In children aged 2 to 12 years: Bacterial infections in children with low white blood cell counts (neutropenia) and hence decreased ability to fight infection (used in combination with an aminoglycoside antibiotic for this purpose).

Piperacillin and Tazobactam for injection is administered by intravenous infusion over 30 minutes. The usual total daily dose of Piperacillin and Tazobactam for injection for adults is 3.375 g every six hours totaling 13.5 g (12 g piperacillin/1.5 g tazobactam). Or as prescribed by the physician.

Bleeding manifestations have occurred in some patients receiving beta lactam antibiotics, including piperacillin. These reactions have sometimes been associated with abnormalities of coagulation tests such as clotting time, platelet aggregation and prothrombin time, and are more likely to occur in patients with renal failure. If bleeding manifestations occur, piperacillin and tazobactam for injection should be discontinued and appropriate therapy instituted. The possibility of the emergence of resistant organisms that might cause superinfections should be kept in mind. If this occurs, appropriate measures should be taken. Piperacillin is excreted in low concentrations in human milk; tazobactam concentrations in human milk have not been studied. Caution should be exercised when piperacillin and tazobactam for injection is administered to a nursing woman.

Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding provided that the benefits to the mother outweigh the risks to the unborn baby. Always inform the doctor if the patient is pregnant or planning a pregnancy, before using any medicine. The safety of this medicine during pregnancy has not been established. The manufacturer recommends it should only be used in pregnant women if the expected benefit to the mother is greater than any possible risk to the developing fetus. Seek medical advice from the doctor. This medicine passes into breast milk in small amounts. The manufacturer recommends it should only be used in breast feeding mothers if the expected benefit to the mother is greater than any possible risk to the nursing infant. Seek medical advice from the doctor.

Piperacillin and tazobactam may cause adverse effects such as upset stomach, vomiting, unpleasant or abnormal taste, diarrhea, gas, headache, constipation, insomnia, rash, itching, skin swelling, shortness of breath, unusual bruising or bleeding.

Probenecid: Administered concomitantly with Piperacillin and Tazobactam for Injection prolongs the half-life of piperacillin by 21% and that of tazobactam by 71%.
Vancomycin: No pharmacokinetic interactions have been noted between Piperacillin and Tazobactam for injection and vancomycin.
Heparin: Coagulation parameters should be tested more frequently and monitored regularly during simultaneous administration of high doses of heparin, oral anticoagulants or other drugs that may affect the blood coagulation system or the thrombocyte function.
Vecuronium: Piperacillin when used concomitantly with vecuronium has been implicated in the prolongation of the neuromuscular blockage of vecuronium. Piperacillin and tazobactam could produce the same phenomenon if given along with vecuronium. Due to their similar mechanism of action, it is expected that the neuromuscular blockage produce by any of the non-depolarizing muscle relaxants could be prolonged in the presence of piperacillin.
Methotrexate: Limited data suggests that co-administration of methotrexate and piperacillin may reduce the clearance of methotrexate due to competition for renal secretion. The impact of tazobactam on the elimination of methotrexate has not been evaluated. If concurrent therapy is necessary, serum concentrations of methotrexate as well as the signs and symptoms of methotrexate toxicity should be frequently monitored.

Direction for Reconstitution: 2.25 g, 3.375 g and 4.5 g Piperacillin and Tazobactam for Injection should be reconstituted with 10 mL, 15 mL and 20 mL of Sterile Water for Injection respectively swirl until dissolved.
For conventional vials, reconstitute Piperacillin and Tazobactam for Injection per gram of piperacillin with 5 mL of compatible sterile water/diluents for reconstitution.
Shake well until dissolved. Discard any unused portion.

Store at temperatures not exceeding 30°C.
Protect from light.

Penicillins

J01CR05 - piperacillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

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