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Cephapirin
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(sef a PYE rin)

U.S. Brand Names
Cefadyl®

Generic Available

No


Synonyms
Cephapirin Sodium

Pharmacological Index

Antibiotic, Cephalosporin (First Generation)


Use

Treatment of infections when caused by susceptible strains in respiratory, genitourinary, gastrointestinal, skin and soft tissue, bone and joint infections, septicemia; treatment of susceptible gram-positive bacilli and cocci (never enterococcus); some gram-negative bacilli including E. coli, Proteus, and Klebsiella may be susceptible


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cephapirin sodium, any component, or cephalosporins


Warnings/Precautions

Modify dosage in patients with severe renal impairment, prolonged use may result in superinfection; use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, urticaria); may cause antibiotic-associated colitis or colitis secondary to C. difficile


Adverse Reactions

1% to 10%: Gastrointestinal: Diarrhea

<1%: CNS irritation, seizures, fever, rash, urticaria, leukopenia, thrombocytopenia, increased transaminases

Other reactions with cephalosporins include anaphylaxis, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, dizziness, fever, headache, encephalopathy, asterixis, neuromuscular excitability, seizures, nausea, vomiting, pseudomembranous colitis, decreased hemoglobin, agranulocytosis, pancytopenia, aplastic anemia, hemolytic anemia, interstitial nephritis, toxic nephropathy, pain at injection site, vaginitis, angioedema, cholestasis, hemorrhage, prolonged PT, serum-sickness reactions, superinfection


Overdosage/Toxicology

Symptoms of overdose include neuromuscular hypersensitivity, convulsions especially with renal insufficiency; many beta-lactam antibiotics have the potential to cause neuromuscular hyperirritability or seizures

Hemodialysis may be helpful to aid in the removal of the drug from the blood, otherwise most treatment is supportive or symptom directed


Drug Interactions

Increased effect: High-dose probenecid decreases clearance

Increased toxicity: Aminoglycosides increase nephrotoxic potential


Stability

Reconstituted solution is stable for 24 hours at room temperature and 10 days when refrigerated; for I.V. infusion in NS or D5W solution is stable for 24 hours at room temperature, 10 days when refrigerated or 14 days when frozen; after freezing, thawed solution is stable for 12 hours at room temperature or 10 days when refrigerated


Mechanism of Action

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.


Pharmacodynamics/Kinetics

Distribution: Widely distributed into most body tissues and fluids including gallbladder, liver, kidneys, bone, sputum, bile, and pleural and synovial fluids; CSF penetration is poor; crosses the placenta and small amounts appear in breast milk

Protein binding: 22% to 25%

Metabolism: Partially in the liver, kidney, and plasma to metabolites (50% active)

Half-life: 36-60 minutes

Time to peak serum concentration: I.M.: Within 30 minutes

Elimination: 60% to 85% excreted as unchanged drug in urine


Usual Dosage

I.M., I.V.:

Adults: 500 mg to 1 g every 6 hours up to 12 g/day

Perioperative prophylaxis: 1-2 g 30 minutes to 1 hour prior to surgery and every 6 hours as needed for 24 hours following

Dosing interval in renal impairment:

Clcr 10-50 mL/minute: Administer every 6-8 hours

Clcr <10 mL/minute: Administer every 12 hours

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Administer 1 g every 8 hours


Monitoring Parameters

Observe for signs and symptoms of anaphylaxis during first dose


Test Interactions

Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution), false-positive serum or urine creatinine with Jaffé reaction, false-positive urinary proteins and steroids


Mental Health: Effects on Mental Status

May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins


Mental Health: Effects on Psychiatric Treatment

May rarely cause neutropenia; use caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

This drug is administered I.M. or I.V. Drink 2-3 L fluid/day. If diarrhea occurs, yogurt or buttermilk may help. May cause false-positive test with Clinitest®; use another form of testing. May interfere with oral contraceptives; additional contraceptive measures are necessary. Report severe, unresolved diarrhea; vaginal itching or drainage; sores in mouth; blood, pus, or mucus in stool or urine; easy bleeding or bruising; unusual fever or chills; rash; or respiratory difficulty. Breast-feeding precautions: Consult prescriber if breast-feeding.


Nursing Implications

Do not admix with aminoglycosides in same bottle/bag; obtain specimens for culture and sensitivity prior to administration of first dose


Dosage Forms

Powder for injection, as sodium: 500 mg, 1 g, 2 g, 4 g, 20 g


References

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Khan AJ and Pryles CV, "Clinical and Pharmacological Evaluation of Cephapirin Sodium (BL-P-1322) in Infants and Children (Cephapirin in Pediatric Patients)," Curr Ther Res Clin Exp, 1973, 15(4):198-204.


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