Azlocillin

Azlocillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Azlocillin has been approved to relieve symptoms and also for the treatment and maintenance of infections due to Pseudomonas aeruginosa, peritonitis, respiratory tract infections, septicemia, urinary tract Infection.

Azlocillin is not absorbed significantly in the Gastrointestinal tract. Azlocillin is widely distributed and crosses the placenta. Azlocillin is metabolized to a limited extent. About 50-70% of a dose of Azlocillin is excreted unchanged in the urine within 24 hr. Azlocillin is also excreted in the bile.

The common side effects involving the use of Azlocillin are fever, angioedema, joint pains, phlebitis, irritation at the site of injection, vomiting, diarrhea, headache, upset stomach, etc.

Azlocillin is available in the form of Intravenous.

Azlocillin is approved in the U.S., U.K., Germany, Japan, Malaysia, India, and China.

Azlocillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Azlocillin acts by binding to a specific penicillin-binding protein (PBPs) located inside the bacterial cell wall, Azlocillin is also said to inhibit the third as well as the last stage of bacterial cell wall synthesis. The cell lysis is then mediated by the bacterial cell wall autolytic enzymes, example autolysins. It is possible that the drug Azlocillin interferes with an autolysin inhibitor.

Azlocillin has been approved to relieve symptoms and also for the treatment and maintenance of infections due to Pseudomonas aeruginosa , peritonitis, respiratory tract infections, septicemia, and urinary tract Infection.

Azlocillin is available in the form of Intravenous.

Azlocillin can be used in the following treatment:

• Infections due to Pseudomonas aeruginosa
• Peritonitis
• Respiratory tract infections
• Septicaemia
• Urinary tract Infection

Azlocillin can help to relieve symptoms and also for the treatment and maintenance of infections due to Pseudomonas aeruginosa , peritonitis, respiratory tract infections, septicemia, and urinary tract Infections.

Azlocillin is approved for use in the following clinical indications:

• Infections due to Pseudomonas aeruginosa
• Peritonitis
• Respiratory tract infections
• Septicaemia
• Urinary tract Infection

Infections due to Pseudomonas aeruginosa, Peritonitis, Respiratory tract infections, Septicaemia, and Urinary tract:

Adult: 2 g every eight hr. Life-threatening infections: 5 g every 8 hr.

Child: Up to 14 yr: 75 mg/kg tid.

Azlocillin is available in the form of 500 mg, 1 g, 1.5 g , and 3g vials

Intravenous

• Dosage Adjustments in Kidney Patients:

CrCl 30 to 50 mL/min: increase the dosing interval to every 4 to 6 hours

CrCl between 10 to 30 mL/min: 2 g Intravenous every 8 hours

CrCl < 10 mL/min: 3 g Intravenous every 12 hours

• Dosage Adjustments in Pediatric Patients:

Infants 7 days-1 yr: 100 mg/kg tid. Neonates <7 days: 100 mg/kg bid. Premature infants: 50 mg/kg bid.

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

Multivitamins 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 Azlocillin administration is recommended.

Azlocillin may is contraindicated under the following conditions:

• Patients with known hypersensitivity to Penicillin and cephalosporins.
  

The physician should closely monitor the patients and keep pharmacovigilance as follows:

Sensitivity

Serious and occasionally fatal hypersensitivity (anaphylactoid) reactions have been reported in patients receiving penicillin. The reactions are more likely to occur in persons with a history of sensitivity to multiple allergens. Before therapy with Azlocillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins/ other allergens. If an allergic reaction occurs, the administration of Azlocillin should be discontinued and appropriate therapy instituted. The possibility of superinfections with mycotic or bacterial pathogens should be kept in mind during the therapy. If superinfections, usually involving Pseudomonas or Candida, or hypersensitivity reactions occur, the Azlocillin should be discontinued and/or appropriate therapy instituted.

Susceptibility/Resistance Development of Drug-Resistant Bacteria

Prescribing Azlocillin in the absence of a proven or strongly suspected bacterial infection which is unlikely to provide benefit to the patient and risks the development of drug-resistant bacteria.

Usage of alcohol should be avoided while on Azlocillin medication, as alcohol can worsen the effects of any underlying disease condition, including conditions such as dizziness, blurred vision, etc.

It was found that at therapeutic doses of Azlocillin, no effects on breastfed newborns/infants are anticipated. Azlocillin can be used during breastfeeding.

Category B

The clinical data on pregnant women, which is more than 1000 pregnancy outcomes, indicates that there is no malformation nor feto/neonatal toxicity of Azlocillin. Azlocillin can be used in pregnancy if clinically needed.

A reduced sodium diet has been recommended in the patients being treated with Azlocillin.

The adverse reactions related to Azlocillin can be categorized as follows:

• Pain at the injection site
• Phlebitis
• Electrolyte disturbances
• Dose-dependent coagulation defect
• Purpura and hemorrhage
• Hypersensitivity reactions, including urticaria
• Fever
• Joint pains
• Rashes
• angioedema
• Serum sickness-like reactions
• Hemolytic anemia
• Interstitial nephritis
• Neutropenia
• Thrombocytopenia
• CNS toxicity, including convulsions
• Diarrhea
• Antibiotic-associated colitis
• Anaphylaxis.

The clinically relevant drug interactions of Azlocillin are briefly summarized here:

• Simultaneous administration of the drug probenecid reduces the excretion of penicillins and hence increases the blood level of the antibiotic.
• The bactericidal effect of penicillins can be hindered by concurrent administration of products with bacteriostatic effects, for instance, erythromycin and tetracyclines.

The following are the side effects involving Azlocillin:

• Pregnancy

Category B

The clinical data on pregnant women, which is more than 1000 pregnancy outcomes, indicates that there is no malformation nor feto/neonatal toxicity of Azlocillin. Azlocillin can be used in pregnancy if clinically needed.

• Lactation

It was found that at therapeutic doses of Azlocillin, no effects on breastfed newborns/infants are anticipated. Azlocillin can be used during breastfeeding. Although it is advised that caution be exercised when administering Azlocillin to patients who are breastfeeding, penicillins are considered compatible with breastfeeding when used in the usual recommended doses.

Physicians should be knowledgeable as well as vigilant about the treatment and identification of the over dosage of Azlocillin.

There is no experience of over dosage with Azlocillin (Azlocillin hydrochloride) tablets. However, excessive doses of Azlocillin are likely to induce nausea, vomiting, abdominal pain, and diarrhea.

Pharmacodynamics

Similar to mezlocillin and also piperacillin, Azlocillin is an acyl ampicillin that exhibits an extended spectrum of activity and in vitro potency that is greater than that of carboxy penicillins. Azlocillin is said to be shown to be effective against a broad spectrum of bacteria, which including Pseudomonas aeruginosa and enterococci.

Pharmacokinetics

• Absorption: Not absorbed significantly in the Gastrointestinal tract.

• Distribution: Protein binding: 20-46%. Widely distributed and crosses the placenta.

• Metabolism: Metabolized to a limited extent.

• Excretion: About 50-70% of a dose is excreted unchanged in the urine within 24 hr. Also excreted in the bile. Plasma half-life: About 1 hr. Removed by hemodialysis.

• https://www.mims.com/philippines/drug/info/azlocillin?mtype=generic
• https://go.drugbank.com/drugs/DB01061
• http://www.antimicrobe.org/drugpopup/azlocillin.htm
• https://www.govinfo.gov/app/details/CFR-1996-title21-vol5/CFR-1996-title21-vol5-sec440-201
• https://drugs.ncats.io/substance/DWV1EFW947
• https://drugs.ncats.io/substance/DWV1EFW947
• https://www.rxwiki.com/azlocillin
• https://www.nature.com/articles/s41598-020-59600-4