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Indications/Uses
Treatment of infections due to penicillinase-producing staphylococci eg, skin and soft tissue infections and infections of the respiratory and genitourinary tracts.
Dosage/Direction for Use
Dosage: Usual Dose: Adults: 500 mg every 6 hrs.
Administration: Administer at least an hr before or 2 hrs after meals.
Administration: Administer at least an hr before or 2 hrs after meals.
Administration
Should be taken on an empty stomach: Take 1 hr before or 2 hr after meals.
Contraindications
History of hypersensitivity to any of the penicillins.
Do not use for the initial treatment of severe, life-threatening infections, including endocarditis, but may be used as follow-up therapy after parenteral penicillinase-resistant penicillin therapy.
Do not use for the treatment of meningitis.
Do not use for the initial treatment of severe, life-threatening infections, including endocarditis, but may be used as follow-up therapy after parenteral penicillinase-resistant penicillin therapy.
Do not use for the treatment of meningitis.
Warnings
Serious and occasionally fatal hypersensitivity (anaphylactic shock with collapse) reactions have occurred in patients receiving penicillin. The incidence of anaphylactic shock in all penicillin-treated patients is between 0.015 and 0.04%. Anaphylactic shock resulting in death has occurred in approximately 0.002% of patients treated. Although anaphylaxis is more frequent following parenteral administration, it has occurred in patients receiving oral penicillins.
When penicillin therapy is indicated, it should be initiated only after a comprehensive patient drug and allergy history has been obtained. Discontinue cloxacillin and give supportive treatment (ie, artificial maintenance of ventilation, pressor amines, antihistamines and corticosteroids) if an allergic reaction occurs.
When penicillin therapy is indicated, it should be initiated only after a comprehensive patient drug and allergy history has been obtained. Discontinue cloxacillin and give supportive treatment (ie, artificial maintenance of ventilation, pressor amines, antihistamines and corticosteroids) if an allergic reaction occurs.
Special Precautions
Cloxacillin shares the toxic potentials of the penicillins, including the risk of hypersensitivity reactions and the usual precautions of penicillin therapy should be observed. Prior to initiation of therapy with cloxacillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins. There is clinical and laboratory evidence of partial cross-allergenicity among penicillins and other β-lactam antibiotics including cephalosporins, cephamycins and 1-oxo-β-lactams.
Evaluate renal, hepatic and hematologic systems periodically during prolonged therapy with cloxacillin.
Prolonged use of penicillinase-resistant penicillins may result in overgrowth of nonsusceptible organisms, including fungi or gram-negative bacteria eg, Pseudomonas. Discontinue cloxacillin and institute appropriate measures if supra- or superinfection occurs.
Evaluate renal, hepatic and hematologic systems periodically during prolonged therapy with cloxacillin.
Prolonged use of penicillinase-resistant penicillins may result in overgrowth of nonsusceptible organisms, including fungi or gram-negative bacteria eg, Pseudomonas. Discontinue cloxacillin and institute appropriate measures if supra- or superinfection occurs.
Adverse Reactions
Hypersensitivity: Rash (morbilliform, maculopapular, urticarial or erythematous), fever, eosinophilia, pruritus and serum sickness-like reactions with fever, chills and myalgia. Eosinophilia reportedly occurs in 5-38% of patients receiving a penicillinase-resistant penicillin and fever or rash occurs in 2-6% of patients receiving one of these drugs. Rarely, anaphylaxis.
Gastrointestinal: Frequently, nausea, vomiting, epigastric distress, loose stools, diarrhea and flatulence. Rarely, antibiotic-associated pseudomembranous colitis.
Renal: Rarely, transient microscopic hematuria.
Hematologic: Rarely, eosinophilia, hemolytic anemia, transient neutropenia, leukopenia, granulocytopenia, thrombocytopenia and agranulocytosis.
Hepatic: Occasionally, transient elevations in serum concentrations of alkaline phosphatase, AST, ALT, bilirubin and LDH; these reactions are more common in infants. One case of intrahepatic cholestasis has been reported.
Gastrointestinal: Frequently, nausea, vomiting, epigastric distress, loose stools, diarrhea and flatulence. Rarely, antibiotic-associated pseudomembranous colitis.
Renal: Rarely, transient microscopic hematuria.
Hematologic: Rarely, eosinophilia, hemolytic anemia, transient neutropenia, leukopenia, granulocytopenia, thrombocytopenia and agranulocytosis.
Hepatic: Occasionally, transient elevations in serum concentrations of alkaline phosphatase, AST, ALT, bilirubin and LDH; these reactions are more common in infants. One case of intrahepatic cholestasis has been reported.
Drug Interactions
Penicillinase-resistant penicillins eg, cloxacillin are physically and/or chemically incompatible with aminoglycosides and can inactivate the drugs in vitro. If concomitant therapy is indicated, avoid in vitro mixing of penicillinase-resistant penicillins and aminoglycosides and administer drugs separately. Penicillinase-resistant penicillins can also inactivate aminoglycosides in vitro in serum samples obtained from patients receiving concomitant therapy with the drugs. This could adversely affect results of serum aminoglycoside assays performed on the serum samples.
Laboratory Test Interactions: Studies using cloxacillin indicate that cloxacillin causes false-positive or falsely elevated results in turbidimetric methods for urinary and serum proteins that use sulfosalicylic acid or trichloroacetic acid.
Laboratory Test Interactions: Studies using cloxacillin indicate that cloxacillin causes false-positive or falsely elevated results in turbidimetric methods for urinary and serum proteins that use sulfosalicylic acid or trichloroacetic acid.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacology: Mechanism of Action: Cloxacillin is an acid- and penicillinase-resistant isoxazolylpenicillin bactericidal antibiotic. It resists the action of bacterial penicillinase because the steric hindrance offered by its acyl side chain prevents penicillinase from attacking and opening the β-lactam ring, whose integrity is necessary for antibacterial activity.
Cloxacillin exerts its bactericidal activity by interfering with the synthesis of the bacterial cell wall. It binds to penicillin-binding proteins responsible for the synthesis of peptidoglycan, a heteropolymeric structure that gives the cell wall its mechanical stability. The final stage of peptidoglycan synthesis involves the completion of the cross-linking with the terminal glycine residue of the pentaglycine bridge linking to the 4th residue of the pentapeptide. The transpeptidase that performs this step is inhibited by penicillins. The bacterial cell wall, thus weakened, leads to swelling and rupture of the microorganism resulting in bacterial death.
Microbiology: Spectrum of Activity: Cloxacillin is active against many penicillinase-producing strains of Staphylococcus aureus, Streptococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae and Streptococcus viridans. It is also active against gram-positive bacilli but not against Streptococcus faecalis.
Pharmacokinetics: Cloxacillin is resistant to inactivation in the presence of acidic gastric secretions and is rapidly but incompletely absorbed from the GIT.
Cloxacillin is distributed into the liver, kidneys, synovial, pleural and ascitic fluids, bone and bile. In a child with septic arthritis who received oral 500 mg every 6 hrs, cloxacillin concentrations in serum and in synovial fluids were 7.7 and 3.8 mcg/mL, respectively, in samples obtained 2 hrs after a dose.
Like other penicillins, only minimal concentrations of cloxacillin are attained in cerebrospinal fluid.
Cloxacillin is 90-96% bound to serum proteins.
Cloxacillin is partially metabolized to active and inactive metabolites. Cloxacillin is also hydroxylated to a small extent to a microbiologically active metabolite which appears to be as active as cloxacillin.
Cloxacillin and its metabolites are rapidly excreted in urine mainly by tubular secretion and glomerular filtration. It is also partly excreted in feces via biliary elimination.
Cloxacillin's serum half-life is slightly prolonged in patients with impaired renal function and ranges from 0.8-2.3 hrs in patients with severe renal impairment.
Cloxacillin is only minimally removed by hemodialysis or peritoneal dialysis.
Cloxacillin exerts its bactericidal activity by interfering with the synthesis of the bacterial cell wall. It binds to penicillin-binding proteins responsible for the synthesis of peptidoglycan, a heteropolymeric structure that gives the cell wall its mechanical stability. The final stage of peptidoglycan synthesis involves the completion of the cross-linking with the terminal glycine residue of the pentaglycine bridge linking to the 4th residue of the pentapeptide. The transpeptidase that performs this step is inhibited by penicillins. The bacterial cell wall, thus weakened, leads to swelling and rupture of the microorganism resulting in bacterial death.
Microbiology: Spectrum of Activity: Cloxacillin is active against many penicillinase-producing strains of Staphylococcus aureus, Streptococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae and Streptococcus viridans. It is also active against gram-positive bacilli but not against Streptococcus faecalis.
Pharmacokinetics: Cloxacillin is resistant to inactivation in the presence of acidic gastric secretions and is rapidly but incompletely absorbed from the GIT.
Cloxacillin is distributed into the liver, kidneys, synovial, pleural and ascitic fluids, bone and bile. In a child with septic arthritis who received oral 500 mg every 6 hrs, cloxacillin concentrations in serum and in synovial fluids were 7.7 and 3.8 mcg/mL, respectively, in samples obtained 2 hrs after a dose.
Like other penicillins, only minimal concentrations of cloxacillin are attained in cerebrospinal fluid.
Cloxacillin is 90-96% bound to serum proteins.
Cloxacillin is partially metabolized to active and inactive metabolites. Cloxacillin is also hydroxylated to a small extent to a microbiologically active metabolite which appears to be as active as cloxacillin.
Cloxacillin and its metabolites are rapidly excreted in urine mainly by tubular secretion and glomerular filtration. It is also partly excreted in feces via biliary elimination.
Cloxacillin's serum half-life is slightly prolonged in patients with impaired renal function and ranges from 0.8-2.3 hrs in patients with severe renal impairment.
Cloxacillin is only minimally removed by hemodialysis or peritoneal dialysis.
MedsGo Class
Penicillins
Features
Brand
RiteMed
Full Details
Dosage Strength
250mg / 5ml
Drug Ingredients
- Cloxacillin
Drug Packaging
Powder for Oral Solution 60ml
Generic Name
Cloxacillin Sodium
Dosage Form
Powder for Oral Solution
Registration Number
DRP-4124-01
Drug Classification
Prescription Drug (RX)