Avesulzone

Avesulzone Uses, Dosage, Side Effects, Food Interaction and all others data.

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.

Avesulzone is a third generation cephalosporin antibiotic. Avesulzone exerts its bactericidal effect by inhibiting the bacterial cell wall synthesis

Trade Name Avesulzone
Availability Discontinued
Generic Cefoperazone
Cefoperazone Other Names Cefoperazone, Cefoperazono, Cefoperazonum
Related Drugs amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, Augmentin
Weight 1gm
Type Injection-IM
Formula C25H27N9O8S2
Weight Average: 645.67
Monoisotopic: 645.142401213
Protein binding

The degree of reversible protein binding varies with the serum concentration from 93% at 25 mcg/mL to 90% at 250 mcg/mL and 82% at 500 mcg/mL. Cefotetan is 88% plasma protein bound.

Groups Approved, Investigational
Therapeutic Class Third generation Cephalosporins
Manufacturer Aventek Pharma
Available Country Pakistan
Last Updated: September 19, 2023 at 7:00 am
Avesulzone
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.

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).

Innovators Monograph

You find simplified version here Avesulzone

Avesulzone contains Cefoperazone see full prescribing information from innovator Avesulzone Monograph, Avesulzone MSDS, Avesulzone FDA label

FAQ

What is Avesulzone used for?

Avesulzone is a cephalosporin antibiotic used to treat infections caused by bacteria.

How safe is Avesulzone?

The clinical efficacy and safety of Avesulzone-sulbactam were similar to those of alternative antibiotics in the treatment of intra-abdominal infections. Therefore, Avesulzone -sulbactam could be recommended as an effective and safe antibiotic for treating intra-abdominal infections.

How does Avesulzone work?

Avesulzone works by killing bacteria or preventing their growth. Avesulzone exerts its bactericidal effect by inhibiting the bacterial cell wall synthesis, and sulbactam acts as a beta-lactamase inhibitor, to increase the antibacterial activity of Avesulzone bagainst beta-lactamase-producing organisms.

What are the common side effects of Avesulzone?

Common side effects of Avesulzone include:

  • diarrhea,
  • nausea,
  • vomiting,
  • hypersensitivity skin reactions including rash, injection site reactions (pain, swelling, or redness), or.
  • reversible low white blood cell count (neutropenia).

Is Avesulzone safe during pregnancy?

Avesulzone has been assigned to pregnancy category B by the FDA. Animal studies failed to reveal evidence of fetal harm. There are no controlled data in human pregnancy. Avesulzone should only be given during pregnancy when need has been clearly established.

Is Avesulzone safe during breastfeeding?

Avesulzone is acceptable in nursing mothers.

Can I drink alcohol with Avesulzone?

Do not drink alcohol while you are taking Avesulzone. You may have unpleasant side effects such as fast heartbeats, warmth or redness under your skin, tingly feeling, nausea, and vomiting. Check your food and medicine labels to be sure these products do not contain alcohol.

Can I drink alcohol with Avesulzone?

Do not drink alcohol while you are taking Avesulzone. You may have unpleasant side effects such as fast heartbeats, warmth or redness under your skin, tingly feeling, nausea, and vomiting. Check your food and medicine labels to be sure these products do not contain alcohol.

How much Avesulzone can I take daily?

The usual adult daily dose of Avesulzone is 2 to 4 grams per day.

How often can I take Avesulzone?

Avesulzone administered in equally divided doses every 12 hours.

Can I take Avesulzone on an empty stomach?

Avesulzone is preferably taken with food to avoid an upset stomach.

What is the half life of Avesulzone sodium?

Avesulzone was 90% bound to serum proteins. The apparent volume of distribution was 10 to 13L. The half-life of the drug varied from 1.6 to 2.4 hours; serum clearance was between 75 and 96 ml/min.

What happen if I overdose on Avesulzone?

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Who should not take Avesulzone?

If you are allergic to barnd; any part of Avesulzone; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

What happen If I missed Avesulzone?

Missing one or two-dose of Avesulzone won't show any effect on your body. The skipped dose causes no problem.

Can I just stop taking Avesulzone?

Do not start, stop, or change the dose of any drug without checking with your doctor.

Can Avesulzone affect my kidneys?

Avesulzone promises to be an effective and safe broad-spectrum antibiotic for patients with all degrees of renal function impairment. A dosage schedule of 2 to 4 g daily will not lead to significant drug accumulation in the presence of severe renal failure.

Can Avesulzone affects my liver?

At usual dosages, adjustments are generally not necessary in either renal or hepatobiliary impairment.

*** Taking medicines without doctor's advice can cause long-term problems.
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