Oxacillin

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

Oxacillin has been approved to relieve symptoms and also for the treatment and maintenance of bloodstream infection, endocarditis treatment, meningitis, bacteria, osteomyelitis and disciti, pneumonia, prosthetic joint infection, and skin and soft tissue infection.

Oxacillin Sodium is rapidly excreted in the form of unchanged drug in the urine by glomerular filtration as well as active tubular secretion.

The common side effects involving the use of Oxacillin are diarrhea, nausea, dizziness, oral thrush, vomiting, headache, and vaginal yeast infection.

Oxacillin is available in the form of Intramuscular and Intravenous Injections.

Oxacillin is available in the U.S., European Union, India, China, and Canada.

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

Oxacillin binds to and inhibits penicillin-binding proteins (PBPs). Oxacillin binds to specific penicillin-binding proteins (PBPs), which are located inside the bacterial cell wall. Oxacillin 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.

Oxacillin has been approved to relieve symptoms and also for the treatment and maintenance of bloodstream infection, endocarditis, treatment, meningitis, bacteria, osteomyelitis and/or disciti , pneumonia, prosthetic joint infection, skin, and soft tissue infection.

The duration of action of Oxacillin is 6-8 hours.

Oxacillin is available in the form of Intramuscular and Intravenous Injections.

Oxacillin can be used in the following treatment:

• Bloodstream infection
• Endocarditis, treatment
• Meningitis, bacterial
• Osteomyelitis and/or discitis
• Pneumonia
• Prosthetic joint infection
• Skin and soft tissue infection

Oxacillin is approved for use in the following clinical indications:

• Bloodstream infection
• Endocarditis, treatment
• Meningitis, bacterial
• Osteomyelitis and/or discitis
• Pneumonia
• Prosthetic joint infection
• Skin and soft tissue infection

Intramuscular or Intravenous Injection: To be administered by a registered medical practitioner.

Bloodstream infection

Pathogen-directed therapy for methicillin-susceptible staphylococci (off label):Intravenous: 2 g every 4 hours; treat uncomplicated bacteremia for ≥14 days starting from the day of first negatIntravenouse blood culture

Endocarditis, treatment

Pathogen-directed therapy for methicillin-susceptible staphylococci (off-label):

NatIntravenouse valve: Intravenous: 12 g/day in 4 or 6 divided doses (i.e., 2 g every 4 hours or 3 g every 6 hours) for six weeks.

Prosthetic valve: Intravenous: 12 g/day in 6 divided doses (i.e., 2 g every 4 hours) for ≥ six weeks; use with rifampin for the entire duration of therapy and gentamicin for first two weeks

Meningitis, bacterial

Pathogen-directed therapy for methicillin-susceptible staphylococci (off-label): Intravenous: 2 g every 4 hours; consider the addition of rifampin if the organism is susceptible and prosthetic material is present. The treatment duration is 10 to 14 days.

Osteomyelitis and/or discitis

Pathogen-directed therapy for methicillin-susceptible staphylococci (off-label): Intravenous: 1.5 to 2 g every 4 to 6 hours or via continuous infusion for ≥6 weeks

Pneumonia

Pathogen-directed therapy for methicillin-susceptible S. aureus (off-label): Intravenous: 2 g every 4 hours. The minimum duration is generally five days for community-acquired pneumonia and seven days for hospital-acquired or ventilator-associated pneumonia.

Prosthetic joint infection

Pathogen-directed therapy for methicillin-susceptible staphylococci (off-label): Intravenous: 1.5 to 2 g every 4 to 6 hours; duration ranges from 2 to 6 weeks depending on prosthesis management,

Skin and soft tissue infection

Cellulitis (nonpurulent) in patients without risk for methicillin-resistant S. aureus: Intravenous: 1 to 2 g every 4 hours. The total duration of therapy is ≥5 days.

Necrotizing infection due to methicillin-susceptible S. aureus (MSSA) (off-label): Intravenous: 1 to 2 g every 4 hours; continue until further debridement is not necessary

Surgical site incisional infection (trunk or extremity, not involving axilla or perineum) (off-label): Intravenous: 2 g every 6 hours; duration is dependent upon severity.

Intramuscular and Intravenous Injection

• Dosage Adjustments in Kidney Patients

The renal dosing recommendations are based on the best available evidence and clinical expertise.

CrCl ≥10 mL/minute: No dosage adjustment is necessary.

CrCl <10 mL/minute: No specific dosage adjustment is recommended

• Dosage Adjustments in Pediatric Patients

Infants, Children, and Adolescents: Intravenous, I.M.: 100 to 200 mg/kg/day in dIntravenousided doses every 4 to 6 hours and maximum daily dose: 12 g/day

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

Multi 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 Oxacillin administration is recommended.

Oxacillin may is contraindicated under the following conditions:

• Patients with known hypersensitivity to penicillin.

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

Serious and occasionally fatal hypersensitivity(anaphylactic) reactions had been reported in patients receIntravenousing therapy with penicillin. These reactions are more likely to occur in persons with a history of sensitIntravenousity to multiple allergens. Cross-sensitIntravenousity of patients to penicillin and cephalosporins has been reported. Before initiating therapy with Oxacillin for Injection, careful inquiry should be made concerning previous hypersensitIntravenousity reactions to penicillin, cephalosporins, and other allergens. If an allergic reaction occurs, the antibiotic should be discontinued. The usual agents (antihistamines, pressor amines, and corticosteroids) should be readily available.

Antibiotic-associated pseudomembranous colitis has been reported with nearly all antibacterial agents, including Oxacillin, and may range in severity from mild to life-threatening. It is important to consider this diagnosis if significant diarrhea or colitis occurs during therapy. Mild cases usually respond to the drug discontinuation alone. However, in moderate to severe cases, management with fluids as well as electrolytes, protein supplementation, and treatment with an oral antibacterial drug effective against Clostridium difficile (e.g., oral vancomycin) should be considered.

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

Caution should be exercised when Oxacillin for Injection is administered to nursing mothers. It is excreted in low concentrations in milk.

Category B

Although reproduction studies in mice and rats performed at doses up to 4 times the human dose have shown no evidence of impaired fertility or harm to the fetus, the safety of Oxacillin for Injection use in pregnant women has not been determined. Because animal reproduction studies aren't always predictive of human response, oxacillin should be used during pregnancy only if clearly needed. It has been found to cross the placenta in rats.

No sufficient scientific evidence is traceable regarding the use and safety of Oxacillin in concurrent use with any particular food.

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

Common

• Diarrhea
• Nausea
• Abdominal pain
• Erythema
• Exanthema
• Rash
• Vulvovaginal mycotic infection
• Headache
• Taste perversion

Rare

• Vomiting
• Urticaria
• Pruritus
• Convulsion
• Dizziness
• Hyperkinesia
• Crystalluria
• Interstitial nephritis
• Anaphylaxis
• Serum sickness-like reaction

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

• Simultaneous administration of probenecid reduces the excretion of penicillin and hence increases the blood level of the antibiotic.
• Tetracycline, a bacteriostatic antibiotic, may antagonize the bactericidal effect of Oxacillin, and concurrent use of these drugs should be avoided.

The following are the side effects involving Oxacillin:

• Muscle
• Nausea
• Vomiting
• Stomach pain
• Vaginal itching or discharge
• Headache
• Swollen/black/"hairy" tongue or thrush

Pregnancy

• Category B

Although reproduction studies in mice and rats performed at doses up to 4 times the human dose have shown no evidence of impaired fertility or harm to the fetus, the safety of Oxacillin for Injection use in pregnant women has not been determined. Because animal reproduction studies are not always predictive of human response, oxacillin should be used during pregnancy only if clearly needed. It has been found to cross the placenta in rats.

• Lactation

Caution should be exercised when Oxacillin for Injection is administered to nursing mothers. It is excreted in low concentrations in milk.

• Pediatric

Because of incompletely developed renal function in pediatric patients, Oxacillin may not be completely excreted, with abnormally high blood levels resulting. Frequent blood levels are advisable in this group, with dosage adjustments when necessary. All pediatric patients treated with penicillin should be monitored closely for clinical and laboratory evidence of toxic or adverse effects. Safety and effectIntravenouseness in pediatric patients have not been established.

• Geriatric

Clinical studies of Oxacillin injection did not include a sufficient number of subjects who were aged 65 and over to determine whether they respond differently from the younger subjects. Other reported clinical experience had not identified differences in responses between the older and younger patients. In general, dose selection for an older patient should be done cautiously usually starting at the low end of the dosing range, reflecting the greater frequency of decreased renal, hepatic, or cardiac function and of concomitant disease or other drug therapy.

Physicians should be knowledgeable and vigilant about the treatment and identification of overdosage of Oxacillin.

Signs or symptoms include gastrointestinal reactions, metabolic reactions such as nausea, vomiting, etc., urogenital reactions, black hairy tongue, etc.

If signs or symptoms occur, discontinue the use of Oxacillin, it is advised to treat symptomatically and institute appropriate supportive measures.

Pharmacodynamics

Oxacillin has in vitro actIntravenousity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Oxacillin results from the inhibition of cell wall synthesis and is mediated through Oxacillin binding to penicillin-binding proteins (PBPs). Oxacillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases, and extended-spectrum beta-lactamases.

Pharmacokinetics

• Absorption

N.A.

• Volume of distribution

N.A.

• Metabolism

N.A.

• Route of elimination

Oxacillin Sodium is rapidly excreted as an unchanged drug in the urine by glomerular filtration and active tubular secretion.

• Van der Auwera P, Klastersky J, Thys JP, Meunier-Carpentier F, Legrand JC.Double-blind, placebo-controlled study of Oxacillin combined with rifampin in the treatment of staphylococcal infections.Antimicrob Agents Chemother. 1985 Oct;28(4):467-72. doi: 10.1128/AAC.28.4.467.
• P Van der Auwera, F Meunier-Carpentier, J Klastersky.Clinical study of combination therapy with Oxacillin and rifampin for staphylococcal infections.Rev Infect Dis 1983 Jul-Aug;5 Suppl 3:S515-22. doi: 10.1093/clinids/5.supplement_3.s515.

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/050640s017lbl.pdf
• https://www.drugs.com/sfx/oxacillin-side-effects.html
• https://go.drugbank.com/drugs/DB00713
• https://pubchem.ncbi.nlm.nih.gov/compound/Oxacillin