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Mezlocillin
Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Mezlocillin belongs to the pharmacological class of Beta-Lactam Antibiotics.
Mezlocillin has been approved to relieve symptoms and also for the treatment and maintenance of susceptible infections, respiratory tract infections, abdominal infections, skin, and soft tissue infections, pelvic infections, bacterial endocarditis, peritonitis, septicemia, biliary tract infections, prophylaxis of infection during surgery, uncomplicated gonorrhea, uncomplicated urinary tract infections.
Mezlocillin is not absorbed in the GIT Tract, but it is absorbed Intramuscularly or Intravenously into the bloodstream with then bioavailability for 45-90 minutes. Mezlocillin is widely distributed in body tissues and fluids; crosses the placenta. The excretion of Mezlocillin is via urine by glomerular filtration and tubular secretion, which is about 55% of the total dose, as an unchanged drug.
The common side effects involving the use of Mezlocillin are diarrhea, nausea, dizziness, oral thrush, vomiting, headache, fever, irritation at the site of injection, anemia, etc
Mezlocillin is available in the form of Intramuscular and Intravenous solutions.
Mezlocillin is available in the U.S., Italy, Germany, Austria, France, Israel, and Brazil.
Mezlocillin belongs to the pharmacological class of Beta-Lactam Antibiotics.
Mezlocillin binds to and inhibits penicillin-binding proteins (PBPs). Mezlocillin binds to specific penicillin-binding proteins (PBPs), which are located inside the bacterial cell wall. Mezlocillin is said to inhibit the third and last stage of bacterial cell wall synthesis. Hence, the Cell lysis is then mediated by the bacterial cell wall autolytic enzymes such as autolysins.
Mezlocillin has been approved to relieve symptoms and also for the treatment and maintenance of susceptible infections, respiratory tract infections, abdominal infections, skin, and soft tissue infections, pelvic infections, bacterial endocarditis, peritonitis, septicemia, biliary tract infections, prophylaxis of infection during surgery, uncomplicated gonorrhea, uncomplicated urinary tract infections.
The mezlocillin achieved a Cmax of 263 mcg/ml and a Half-life of 0.8 hours.
Mezlocillin is available in the form of Intramuscular and Intravenous.
Mezlocillin can be used in the following treatment:
- Susceptible infections, Respiratory tract infections, Abdominal infections, skin, and soft tissue infections, Pelvic infections, Bacterial endocarditis, Peritonitis, Septicaemia, Biliary tract infections
- Prophylaxis of infection during surgery
- Uncomplicated gonorrhea
- Uncomplicated urinary tract infections
Mezlocillin can help to relieve symptoms and also for the treatment and maintenance of susceptible infections, respiratory tract infections, abdominal infections, skin, and soft tissue infections, pelvic infections, bacterial endocarditis, peritonitis, septicemia, biliary tract infections, prophylaxis of infection during surgery, uncomplicated gonorrhea, uncomplicated urinary tract infections.
Mezlocillin is approved for use in the following clinical indications:
- Susceptible infections, Respiratory tract infections, Abdominal infections, skin, and soft tissue infections, Pelvic infections, Bacterial endocarditis, Peritonitis, Septicaemia, Biliary tract infections
- Prophylaxis of disease during surgery
- Uncomplicated gonorrhea
- Uncomplicated urinary tract infections
Intramuscular or Intravenous: To be administered by the registered medical practitioner.
Susceptible infections, Respiratory tract infections, Abdominal infections, skin, and soft tissue infections, Pelvic infections, Bacterial endocarditis, Peritonitis, Septicaemia, Biliary tract infections
Severe infections: 200-300 mg/kg/day in divided doses. Life-threatening infections: Up to 350 mg/kg/day. Max: 24 g/day.
Prophylaxis of infection during surgery
Adult: 4 g preoperatively, followed by two further doses every 6 hr.
Uncomplicated gonorrhea
Adult: 1-2 g Intramuscular or Intravenous as a single dose. Probenecid 1 g may be given orally at the same time or up to 30 min before the injection.
Uncomplicated urinary tract infections
Adult: 1.5-2 g Intramuscular or Intravenous every 6 hr.
Intramuscular and Intravenous.
- Dosage Adjustments in Kidney Patients:
CrCl < 10 mL/min: Uncomplicated UTI: 1.5 g Intravenous every 8 hours.
Complicated UTI: 1.5 g Intravenous every 8 hours.
Severe systemic infection: 2 g Intravenous every 8 hours.
Life-threatening infection: 2 g Intravenous every 6 hours.
CrCl 10 to 30 mL/min: Uncomplicated UTI: 1.5 g Intravenous every 8 hours.
Complicated UTI: 1.5 g Intravenous every 6 hours.
Severe systemic infection: 3 g Intravenous every 8 hours.
Life-threatening infection: 3 g Intravenous every 6 hours.
- Dosage Adjustments in Hepatic Impairment Patients:
No dosage adjustments are needed for hepatic Impairment.
- Dosage Adjustments in Pediatric Patients:
Less than one week: 75 mg/kg q12h
More than one week and Less than a month: 75 mg/kg q6-8 hrs
More than and Less than 12 yrs: 50-75 mg/kg q4h.
Avoid high-acid foods like citrus fruits and juices like orange and grapefruit, soda, and chocolates.
Alcohol intake might lead to nausea, vomiting, and headache
Mult Intravenous Vitamins and antacids contain minerals, primarily magnesium, calcium, aluminum, iron, or zinc, which bind to the antibiotic and refrain it from working. Spacing them at least for 2 hours after Mezlocillin administration is recommended.
Mezlocillin may is contraindicated under the following conditions:
- Patients with known hypersensitivity to penicillins.
The adverse reactions related to Mezlocillin can be categorized as follows:
- Loss of appetite
- Inflammation of kidney
- Absence of urine
- Protein in urine
- Blood/pus in the urine
- Skin scar
- Itchy eyes.
- Nausea
- Vomiting
- Abdominal cramps
- Diarrhea
- Rectal bleeding
- Flatulence
- Inflammation of intestine
- Elevated Blood Urea Nitrogen
- Jaundice and inflammation of the liver
- Pain at the site of injection
- Anemia
- Elevated liver enzyme levels
- Reduced mineral and uric acid levels in blood
- Vaginal inflammation
- Fever
- Blood clots
- Vein irritation
- Inflammation and compression of spinal nerve
The clinically relevant drug interactions of Mezlocillin are briefly summarized here:
- Probenecid may inhibit renal excretion of mezlocillin. Monitor blood coagulation parameters when used with high-dose heparin and other anticoagulants.
The following are the side effects involving Mezlocillin:
- Loss of appetite
- Inflammation of kidney
- Absence of urine
- Protein in urine
- Blood/pus in the urine
- Skin scar
- Itchy eyes.
- Nausea
- Vomiting
- Abdominal cramps
- Diarrhea
- Rectal bleeding
- Flatulence
- Inflammation of intestine
- Elevated Blood Urea Nitrogen
- Jaundice and inflammation of the liver
- Pain at the site of injection
- Anemia
- Elevated liver enzyme levels
- Reduced mineral and uric acid levels in blood
- Vaginal inflammation
- Fever
- Blood clots
- Vein irritation
- Inflammation and compression of spinal nerve
Pregnancy
Category B: No evidence of risk in humans but studies inadequate.
Physicians should be knowledgeable and vigilant about the treatment and identification of overdosage of Mezlocillin.
Some over dosage side effects include Rash, fever, chills, and peeling skin.
Pharmacodynamics
Mezlocillin, a broad-spectrum ureidopenicillin, blocks the final cross-linking stage of peptidoglycan production through binding and inactivation of transpeptidases, thus inhibiting bacterial cell wall synthesis. It is active against a wide range of gram-negative organisms but is less active against P. aeruginosa compared to azlocillin or piperacillin.
Pharmacokinetics
- Absorption: Not significantly absorbed from the Gastrointestinal tract. Well absorbed after Intramuscular injection, with peak plasma concentrations in 45-90 min.
- Distribution: Protein-binding: 16-42%. Widely distributed in body tissues and fluids, crosses the placenta, and is distributed into breast milk (in small amounts). Minimal diffusion into Cerebrospinal Fluid.
- Metabolism: Limited.
- Excretion: Via urine by glomerular filtration and tubular secretion (about 55% of the total dose, as unchanged drug); via bile (up to 30%). Half-life: Approximately 1 hour; slightly prolonged in neonates; up to 6 hr in patients with renal Impairment.
- Kurz R. [Experience with the combination mezlocillin/oxacillin in severe bacterial infections in a children's surgical ward (author's transl)].Arzneimittelforschung. 1979;29(12a):2014-7.
- https://pubchem.ncbi.nlm.nih.gov/compound/Mezlocillin
- https://www.sciencedirect.com/topics/agricultural-and-biological-sciences/mezlocillin
- https://www.drugs.com/sfx/mezlocillin-side-effects.html
- http://www.antimicrobe.org/drugpopup/Mezlocillin.pdf
- http://www.antimicrobe.org/drugpopup/mezlocillin.htm
- https://www.mims.com/philippines/drug/info/mezlocillin?mtype=generic
- https://www.medindia.net/drugs/medication-side-effects/mezlocillin_sodium.htm
- https://go.drugbank.com/drugs/DB00948