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Pronunciation |
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(pi
PER a sil
in) |
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U.S. Brand
Names |
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Pipracil® |
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Generic
Available |
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No |
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Synonyms |
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Piperacillin Sodium |
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Pharmacological Index |
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Antibiotic, Penicillin |
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Use |
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Treatment of susceptible infections such as septicemia, acute and chronic
respiratory tract infections, skin and soft tissue infections, and urinary tract
infections due to susceptible strains of Pseudomonas, Proteus,
and Escherichia coli and Enterobacter; active against some
streptococci and some anaerobic bacteria |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to piperacillin or any component or
penicillins |
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Warnings/Precautions |
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Dosage modification required in patients with impaired renal function;
history of seizure activity; use with caution in patients with a history of
beta-lactam allergy |
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Adverse
Reactions |
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Percentage unknown: Convulsions, confusion, drowsiness, fever, rash,
electrolyte imbalance, hemolytic anemia, positive Coombs' reaction, abnormal
platelet aggregation and prolonged PT (high doses), thrombophlebitis, myoclonus,
acute interstitial nephritis, hypersensitivity reactions, anaphylaxis,
Jarisch-Herxheimer reaction |
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Overdosage/Toxicology |
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Symptoms of penicillin overdose include neuromuscular hypersensitivity
(agitation, hallucinations, asterixis, encephalopathy, confusion, and seizures)
and electrolyte imbalance with potassium or sodium salts, especially in renal
failure
Hemodialysis may be helpful to aid in the removal of the drug from the blood,
otherwise most treatment is supportive or symptom directed |
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Drug
Interactions |
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Decreased effect: Tetracyclines may decrease penicillin effectiveness;
aminoglycosides physical
inactivation of
aminoglycosides in the presence of high concentrations of piperacillin and
potential toxicity in patients with mild to moderate renal dysfunction;
decreased efficacy of oral contraceptives is possible
Increased effect:
Probenecid may increase penicillin levels
Neuromuscular blockers may increase duration of blockade
Aminoglycosides
synergistic efficacy
Heparin with high-dose parenteral penicillins may result in increased risk of
bleeding |
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Stability |
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Reconstituted solution is stable (I.V. infusion) in NS or D5W for
24 hours at room temperature, 7 days when refrigerated or 4 weeks when frozen;
after freezing, thawed solution is stable for 24 hours at room temperature or 48
hours when refrigerated; 40 g bulk vial should not be frozen after
reconstitution; incompatible with aminoglycosides |
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Mechanism of
Action |
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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. |
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Pharmacodynamics/Kinetics |
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Absorption: I.M.: 70% to 80%
Distribution: Crosses the placenta; distributes into milk at low
concentrations
Protein binding: 22%
Half-life: Dose-dependent; prolonged with moderately severe renal or hepatic
impairment:
Neonates: 1-5 days: 3.6 hours; >6 days: 2.1-2.7 hours
Children: 1-6 months: 0.79 hour; 6 months to 12 years: 0.39-0.5 hour
Adults: 36-80 minutes
Time to peak serum concentration: I.M.: Within 30-50 minutes
Elimination: Principally in urine and partially in feces (via bile)
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Usual Dosage |
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Neonates: 100 mg/kg every 12 hours
Infants and Children: I.M., I.V.: 200-300 mg/kg/day in divided doses every
4-6 hours
Higher doses have been used in cystic fibrosis: 350-500 mg/kg/day in divided
doses every 4-6 hours
Adults: I.M., I.V.:
Moderate infections (urinary tract infections): 2-3 g/dose every 6-12 hours;
maximum: 2 g I.M./site
Serious infections: 3-4 g/dose every 4-6 hours; maximum: 24 g/24 hours
Uncomplicated gonorrhea: 2 g I.M. in a single dose accompanied by 1 g
probenecid 30 minutes prior to injection
Dosing adjustment in renal impairment: Adults: I.V.:
Clcr 20-40 mL/minute: Administer 3-4 g every 8 hours
Clcr <20 mL/minute: Administer 3-4 g every 12 hours
Moderately dialyzable (20% to 50%)
Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose
as for Clcr 10-50 mL/minute |
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Monitoring
Parameters |
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Observe for signs and symptoms for anaphylaxis during first
dose |
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Test
Interactions |
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May interfere with urinary glucose tests using cupric sulfate (Benedict's
solution, Clinitest®); may inactivate aminoglycosides
in vitro; false-positive urinary and serum proteins, positive Coombs' test
[direct] |
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Mental Health: Effects
on Mental Status |
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May cause drowsiness or confusion; penicillins reported to cause
apprehension, illusions, hallucinations, depersonalization, agitation,
encephalopathy, and insomnia |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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Prolonged use of penicillins may lead to development of oral
candidiasis |
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Patient
Information |
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This medication will be administered I.V. or I.M. Maintain adequate hydration
(2-3 L/day of fluids unless instructed to restrict fluid intake). If being
treated for sexually transmitted disease, partner will also need to be treated.
Small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may
reduce nausea or dry mouth. Important to maintain good oral and vaginal hygiene
to reduce incidence of opportunistic infection. Diabetics should use serum
glucose testing while on this medication. If diabetic, drug may cause false
tests with Clinitest® urine glucose monitoring; use of
glucose oxidase methods (Clinistix®) or serum glucose
monitoring is preferable. This drug may interfere with oral contraceptives; an
alternate form of birth control should be used. Report persistent diarrhea,
fever, chills, unhealed sores, bloody urine or stool, muscle pain, mouth sores,
or difficulty breathing. |
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Nursing
Implications |
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Administer one hour apart from aminoglycosides; extended spectrum includes
Pseudomonas aeruginosa; dosage modification required in patients with
impaired renal function; can be administered I.V. push over 3-5 minutes at a
maximum concentration of 200 mg/mL or I.V. intermittent infusion over 30-60
minutes at a final concentration less than or equal to 20 mg/mL
Monitor serum electrolytes, bleeding time especially in patients with renal
impairment, periodic tests of renal, hepatic and hematologic function
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Dosage Forms |
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Powder for injection, as sodium: 2 g, 3 g, 4 g, 40 g |
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References |
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Capellier G, Cornette C, Boillot A, et al,
"Removal of Piperacillin in Critically Ill Patients Undergoing Continuous Veno-Venous Hemofiltration,"
Crit Care Med, 1998, 26(1):88-91.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Keller E, Bohler J, Busse-Grawitz A, et al,
"Single Dose Kinetics of Piperacillin During Continuous Arteriovenous Hemodialysis in Intensive Care Patients,"
Clin Nephrol, 1995, 43(Suppl 1):S20-3.
Placzek M, Whitelaw A, Want S, et al,
"Piperacillin in Early Neonatal Infection," Arch Dis Child, 1983,
58(12):1006-9.
Prince AS and Neu HC,
"Use of Piperacillin, A Semisynthetic Penicillin, in the Therapy of Acute Exacerbations of Pulmonary Disease in Patients With Cystic Fibrosis,"
J Pediatr, 1980, 97(1):148-51.
Tan JS and File TM Jr, "Antipseudomonal Penicillins," Med Clin North
Am, 1995, 79(4):679-93.
Thirumoorthi MC, Asmar BI, Buckley JA, et al,
"Pharmacokinetics of Intravenously Administered Piperacillin in Preadolescent Children,"
J Pediatr, 1983, 102(6):941-6.
Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.
Yoshikawa TT, "Antimicrobial Therapy for the Elderly Patient," J Am
Geriatr Soc, 1990, 38(12):1353-72.
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