Avesulzone

Uses

Avesulzone is used for the treatment of the following infections when caused by susceptible organisms: Respiratory Tract Infections, Peritonitis & Other Intra-abdominal Infections, Bacterial Septicemia, Skin and Skin Structures Infections, Pelvic Inflammatory Disease, Endometritis & Other Infections of the Female Genital Tract, Urinary Tract Infections, Enterococcal Infections etc.

Avesulzone is also used to associated treatment for these conditions: Bacterial Infections, Bloodstream Infections, Bone and Joint Infections, Intra-Abdominal Infections, Lower Respiratory Tract Infection (LRTI), Meningitis, Peritonitis, Postoperative Infections, Skin and Soft Tissue Infections, Upper Respiratory Tract Infection, Urinary Tract Infection, Genital tract infection

How Avesulzone works

Like all beta-lactam antibiotics, cefoperazone binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins.

Dosage

Avesulzone dosage

Sterile Avesulzone Sodium can be administered by IM or IV injection (following dilution).

Adult: 2 to 4 grams per day administered in equally divided doses every 12 hours. In severe infections or infections caused by less sensitive organisms, the total daily dose and/or frequency may be increased. Patients have been successfully treated with a total daily dosage of 6-12 grams divided into 2,3, or 4 administrations ranging from 1.5 to 4 grams per dose. When treating infections caused by Streptococcus pyogenes, therapy should be continued for at least 10 days

Avesulzone for intravenous or intramuscular use may be initially reconstituted with compatible solution. Solutions should be allowed to stand after reconstitution to allow any foaming to dissipate to permit visual inspection for complete solubilization. Vigorous and prolonged agitation may be necessary to solubilize Avesulzone in higher concentrations (above 333 mg Avesulzone/ml). The maximum solubility of Avesulzone is approximately 475 mg Avesulzone/ml of compatible diluent.

Side Effects

As with all Cephalosporins, hypersensitivity manifested by skin reactions (1 patient in 45), drug fever (1 in 260), or a change in Coombs' test (1 in 60) has been reported. These reactions are more likely to occur in patients with a history of allergies, particularly to Penicillin.

Toxicity

Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.

Precaution

Avesulzone is extensively excreted in bile. The serum half-life of Avesulzone is increased 2-4 fold in patients with hepatic disease and/or biliary obstruction. In general, total daily dosage above 4 gm should not be necessary in such patients. If higher dosages are used, serum concentrations should be monitored.

Food Interaction

• Avoid alcohol. Ingesting alcohol with cefoperazone may precipitate a disulfuram like reaction including symptoms such as flushing, tachycardia, sweating, and headache.

Avesulzone Alcohol interaction

[Moderate] GENERALLY AVOID:

Some cephalosporins may occasionally induce a disulfiram-like reaction when coadministered with alcohol.

The interaction has been reported for cefamandole, cefoperazone, cefotetan, and moxalactam.

These agents contain an N-methylthiotetrazole (NMTT) side chain that may inhibit aldehyde dehydrogenase (ALDH) similar to disulfiram.

Following ingestion of alcohol, inhibition of ALDH results in increased concentration of acetaldehyde, the accumulation of which produces an unpleasant physiologic response referred to as the 'disulfiram reaction'.

Symptoms include flushing, throbbing in head and neck, throbbing headache, respiratory difficulty, nausea, vomiting, sweating, thirst, chest pain, palpitation, dyspnea, hyperventilation, tachycardia, hypotension, syncope, weakness, vertigo, blurred vision, and confusion.

Severe reactions may result in respiratory depression, cardiovascular collapse, arrhythmias, myocardial infarction, acute congestive heart failure, unconsciousness, convulsions, and death.

Cefonicid contains a structurally similar side chain but did not produce elevations in blood acetaldehyde or a disulfiram reaction to ethanol in 15 healthy volunteers given single and multiple one gram doses of the drug.

Patients receiving cephalosporins with the NMTT side chain should avoid the concomitant use of alcohol and alcohol-containing products.

Avesulzone Hypertension interaction

[Moderate] Parenteral cefoperazone sodium contains approximately 34 mg (1.5 mEq) of sodium per each gram of cefoperazone activity.

The sodium content should be considered in patients with conditions that may require sodium restriction, such as congestive heart failure, hypertension, and fluid retention.

Avesulzone Drug Interaction

Unknown: aspirin, aspirin, albuterol / ipratropium, albuterol / ipratropium, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, glycerin, glycerin, acetaminophen, acetaminophen, valproic acid, valproic acid, thiamine, thiamine, cyanocobalamin, cyanocobalamin, riboflavin, riboflavin, pyridoxine, pyridoxine

Avesulzone Disease Interaction

Major: colitis, hypoprothrombinemiaModerate: renal/liver disease, sodium, dialysis, disulfiram-like reaction, liver disease

Half Life

The mean serum half-life is approximately 2.0 hours, independent of the route of administration.

Elimination Route

Avesulzone is excreted mainly in the bile.

Pregnancy & Breastfeeding use

Pregnancy Category B.This drug should be used during pregnancy only if clearly needed. Only low concentrations of Avesulzone is excreted in human milk. Although Avesulzone passes poorly into breast milk of nursing mothers, caution should be exercised when Avesulzone is administered to a nursing woman.

Contraindication

Avesulzone is contraindicated in patients with known allergy to the Cephalosporin-class of antibiotics.

Special Warning

Children use: Safety and effectiveness in children have not been established.

Geriatric use: Reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Storage Condition

Avesulzone is to be stored in a dry place, below 25°C and protected from light prior to reconstitution. The reconstituted solution may be stored for 24 hours if kept in room temperature (below 25°C).

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