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What-is-piperacillin

What are the side effects of piperacillin?

Posted on  March 10, 2021, Edited by Jason, Category  

What is piperacillin?

1. Definition

Piperacillin belongs to the fourth-generation penicillin. This type of drug is a semi-synthetic penicillin antibiotic. It has obvious antibacterial effect and can kill many kinds of bacteria, such as Proteus, Escherichia coli, Klebsiella and Enterobacter, a variety of anaerobic bacteria and Gram-negative bacteria. Piperacillin can not only treat respiratory infections caused by bacteria, but also has therapeutic effects on gynecological diseases, urinary tract infections, skin infections, and joint infections.

Piperacillin is mainly used by intravenous injection to kill bacteria and eliminate inflammation. For mild patients, the daily injection volume should not exceed 8 grams. For severe patients, the dose can be increased to 12 grams. During the patient's use of piperacillin, some patients will experience redness and swelling at the injection site and phlebitis. It is best to adjust the dosage and the speed of infusion when this happens.

2. Physical and chemical properties

This product is white crystalline powder; odorless; slightly hygroscopic. It is easily soluble in methanol, soluble in absolute ethanol or acetone, and slightly soluble in water.

3. Antibacterial spectrum

  • Sensitive bacteria: Pseudomonas aeruginosa, Escherichia coli, Proteus, Klebsiella pneumoniae, Neisseria gonorrhoeae, Salmonella that does not produce beta lactamase, Shigella, Bacteroides fragilis, intestines Coccus.
  • Insensitive bacteria: Aerobacter, Citrobacter, Providencia and Acinetobacter, Serratia, Enzyme-producing Haemophilus influenza.

4. Pharmacology

It is a semi-synthetic semicarbazide anti-pseudomonas penicillin. The effect on gram-positive bacteria is similar to that of ampicillin. It has a good antibacterial effect on enterococci, and also has a certain effect on some Bacteroides and Clostridia.

It has a strong effect on gram-negative bacteria. The antibacterial spectrum includes Neisseria gonorrhoeae, Escherichia coli, Proteus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Citrobacter, Enterobacter, Haemophilus, Salmonella, Shigella, some pseudomonas (except Pseudomonas aeruginosa), meningococcus, Yersinia.

This product is not resistant to enzymes. Piperacillin is not absorbed orally. Intramuscular injection of 2g, the serum drug concentration peaked at 0.5 hours, about 36μg/mL intravenous infusion of 4g within 30 minutes, immediate plasma concentration> 200μg/ml, 100μg/ml in 1 hour, t1/2 is about 1 hour. It is widely distributed in the body, and the surrounding organs can reach effective concentrations, and there are high concentrations in bile and prostate fluid. Piperacillin is mainly excreted by the kidneys, and 1/2~2/3 of the dose can be excreted in the urine within 12 hours.

5. Pharmacokinetics

This medicine cannot be absorbed orally. The peak blood concentration (Cmax) of normal people was 52.2 mg/L at 0.71 hours after intramuscular injection of the 1g drug, and the blood concentration at 6 hours was 1.3 mg/L. The blood concentration immediately after intravenous drip and intravenous bolus injection of the drug reached 58.0 mg/L and 142.1 mg/L, respectively, 0.5 mg/L and 0-6 mg/L in 6 hours. Give patients with severe renal impairment (endogenous creatinine clearance rate <5ml/L) intravenous drip 70mg/kg according to body weight within 30 minutes, and the blood concentration after 1 hour is about 350mg/L.

The serum protein binding rate of piperacillin is 17%-22%, the apparent volume of distribution (Vd) is 0.18-0.3L/kg, and the distribution half-life (t1/2β) is 11-20 minutes. It is well distributed and can reach a considerable concentration in the cerebrospinal fluid when the meninges are inflamed.

Piperacillin blood elimination half-life (t1/2β) for patients with normal renal function is 0.6-1.2 hours, and those with moderate or more renal insufficiency can be extended to 3.3-5.1 hours without being metabolized in the liver. Piperacillin is eliminated through the kidney (glomerular filtration and tubular secretion) and non-renal (mainly bile) pathways. After intravenous injection of 1g, 49%-68% of the dose is excreted in urine within 12 hours. 10%-20% of drugs with normal liver function are excreted by bile. Very few drugs are excreted through breast milk. Hemodialysis can clear 30%-50% of the dose in 4 hours. Oral probenecid 1g 1 hour before intramuscular injection can increase the peak blood concentration (Cmax) by 30% and prolong the blood elimination half-life (t1/2β) by 30%.

Piperacillin Uses

Piperacillin-Uses
Piperacillin-Uses

1. Indications

Infections caused by sensitive bacteria, such as sepsis, urinary tract infections, respiratory tract infections, biliary tract infections, abdominal cavity infections, pelvic infections and skin and soft tissue infections.

Used in conjunction with aminoglycoside drugs, it can treat infections in patients with neutropenia and immunodeficiency.

2. Uses

Piperacillin is suitable for sensitive Enterobacteriaceae bacteria, Pseudomonas aeruginosa, Acinetobacter sepsis, upper urinary tract and complicated urinary tract infections, respiratory tract infections, biliary tract infections, abdominal infections, pelvic infections, skin and soft tissues Infection etc. The combined application of piperacillin and aminoglycosides can also be used for infection in patients with neutropenia and immunodeficiency.

3. Dosage

  • Moderate infection: 4g/time, 2 times/day, intravenous injection.
  • Severe infection: 3~4g/time, 4 times/day, intravenous injection.
  • Children: 50~200 mg/kg/time, 2~4 times/day.
  • Pregnant women: The drug has not been found to be harmful to animal embryos, but please follow the doctor’s advice.
  • Breastfeeding women: The drug can be secreted through breast milk, and you should follow the doctor’s advice.

Tazocin

1. Ingredients

Tazocin is a compound preparation, and its components are piperacillin sodium and tazobactam sodium (based on piperacillin and tazobactam, the ratio of the labeled amount is 8:1); the excipients are: ethylenediaminetetraacetic acid Disodium (EDTA), citric acid, sodium bicarbonate and water for injection.

2. Indications

Tazocin (piperacillin sodium and tazobactam sodium for injection), its indication is systemic and local bacteria caused by detected or suspected sensitive bacteria.

  • Lower respiratory tract infection.
  • Urinary tract infection (mixed infection or single bacterial infection).
  • Infection in the abdominal cavity.
  • Skin and soft tissue infections.
  • Bacterial sepsis.
  • Gynecological infections.
  • Used in combination with aminoglycoside drugs for bacterial infections in patients suffering from neutropenia.
  • Bone and joint infections.
  • Mixed infections of multiple bacteria; Piperacillin/Tazobactam is suitable for the treatment of mixed infections of multiple bacteria, including the aerobic and anaerobic bacteria at the suspected infection site (intraperitoneal cavity, skin and soft tissue, upper and lower respiratory tract, gynecology).

3. Matters needing attention

Piperacillin contains a total of 64mg (2.79mEq) of sodium per gram of piperacillin, which can cause an increase in the patient's total sodium intake. This should be taken into consideration when patients who need to limit salt intake. Hypokalemia can occur in patients with low potassium reserves or taking drugs that can reduce blood potassium levels (treated with cytotoxic drugs or diuretics). Therefore, it is recommended that such patients regularly measure blood electrolyte levels.

Like other semi-synthetic penicillins, the use of piperacillin can increase the incidence of fever and rash in patients with cystic fibrosis.

Some patients treated with β-lactam antibiotics (including piperacillin) may have bleeding manifestations. These reactions are often related to abnormal blood coagulation tests (such as clotting time, platelet aggregation and prothrombin time), and are more common in patients with renal failure. If there are signs of bleeding, antibiotic treatment (piperacillin/tazobactam for injection) should be discontinued, and corresponding treatment measures should be taken.

It should be noted that drug-resistant strains may appear during treatment, causing double infection. If this happens, corresponding measures should be taken.

Piperacillin side effects

Piperacillin-side-effects
Piperacillin-side-effects

1. Adverse Reactions

  • Allergic reactions: Allergic reactions to penicillin drugs are common, including various types of rashes such as urticaria, leukopenia, interstitial nephritis, asthma attacks, and serotype reactions. In severe cases, such as anaphylactic shock, occasionally; once anaphylactic shock happens, it must be rescued on the spot: keeping the airway open, inhaling oxygen, and giving adrenaline, glucocorticoid and other treatment measures.
  • Local symptoms: pain at the local injection site, thrombophlebitis, etc.
  • Gastrointestinal symptoms: diarrhea, loose stools, nausea, vomiting, etc.; pseudomembranous enteritis is rare.
  • Some patients may have cholestatic jaundice.
  • Central nervous system symptoms: headache, dizziness and fatigue.
  • When large doses are used for patients with impaired renal function, penicillin encephalopathy occurs due to the increased concentration of cerebrospinal fluid, so the dose should be adjusted.

2. Piperacillin Interactions

  • Probenecid blocks the excretion of piperacillin, and the blood concentration increases, so that the effect is maintained long.
  • Combined with aminoglycosides, it has a synergistic antibacterial effect on sensitive strains of Pseudomonas aeruginosa, Serratia, Klebsiella, other Enterobacter and Staphylococcus.
  • Combined with anticoagulants such as heparin, it increases the risk of bleeding. When combined with thrombolytic drugs, severe bleeding can occur.
  • Cefoxitin: It can antagonize the antibacterial effect of this medicine on Pseudomonas aeruginosa, Serratia, Proteus, and Enterobacter.
  • Amikacin, gentamicin, tobramycin, and other aminoglycoside drugs: have synergistic bactericidal effects against Pseudomonas aeruginosa, Serratia, Klebsiella, Indole-positive Proteus, Providencia Bacteria, other Enterobacter, and Staphylococcus sensitive strains.
  • Thrombolytics: severe bleeding can occur.
  • Gentamicin: no synergistic effect on Enterococcus faecalis.

3. Warnings

  • Use with caution if you have a history of bleeding, ulcerative colitis, Crohn's disease or pseudomembranous colitis.
  • You should check liver and kidney function if you take this drug for a long time.
  • People who are allergic to one penicillin may be allergic to other penicillin drugs; those who are allergic to cephalosporins, griseofulvin or penicillamine may also be allergic to this drug.
  • People with history of allergy, bleeding, ulcerative colitis, Crohn's disease or antibiotic-related enteritis should use it with caution.
  • This drug can cause bleeding in a few patients, especially those with renal insufficiency. If it occurs, the drug should be discontinued in time and given appropriate treatment; dose for patients with impaired renal function should be appropriately reduced.
  • The application of this drug can cause direct antiglobulin (Coombs) test to be positive, blood urea nitrogen and serum creatinine can also increase, hypernatremia, hypokalemia, serum aminotransferase and serum Increased lactate dehydrogenase and serum bilirubin can increase.
  • Do not add this medicine to sodium bicarbonate solution intravenously.
  • The safe dose for children under 12 years of age has not been formally determined.

Conclusion

Piperacillin belongs to the class of penicillin antibiotics and has a good effect on sepsis, urinary tract infections and respiratory tract infections. The side effects of piperacillin are similar to those of other penicillin antibiotics.     

Piperacillin belongs to beta lactams. BALLYA provides a betalactam test to tell you if there are beta lactams residues in dairy products you eat every day.

References

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