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Pronunciation |
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(mez
loe SIL
in) |
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U.S. Brand
Names |
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Mezlin® |
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Generic
Available |
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No |
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Synonyms |
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Mezlocillin Sodium |
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Pharmacological Index |
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Antibiotic, Penicillin |
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Use |
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Treatment of infections caused by susceptible gram-negative aerobic bacilli
( Klebsiella, Proteus, Escherichia coli,
Enterobacter, Pseudomonas aeruginosa, Serratia) involving
the skin and skin structure, bone and joint, respiratory tract, urinary tract,
gastrointestinal tract, as well as, septicemia |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to mezlocillin, any component, or
penicillins |
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Warnings/Precautions |
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If bleeding occurs during therapy, mezlocillin should be discontinued; dosage
modification required in patients with impaired renal function; use with caution
in patients with renal impairment or biliary obstruction, or history of allergy
to cephalosporins |
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Adverse
Reactions |
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1% to 10%: Gastrointestinal: Nausea, diarrhea
<1%: Fever, seizures, dizziness, headache, rash, exfoliative dermatitis,
hypokalemia, hypernatremia, vomiting, eosinophilia, leukopenia, neutropenia,
thrombocytopenia, agranulocytosis, hemolytic anemia, prolonged bleeding time,
positive Coombs' [direct], hepatotoxicity, elevated liver enzymes, hematuria,
elevated BUN/serum creatinine, interstitial nephritis, serum sickness-like
reactions |
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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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Aminoglycosides (synergy), probenecid (decreased clearance), vecuronium
(increased duration of neuromuscular blockade), heparin (increased risk of
bleeding); possible decrease in effectiveness of oral contraceptives;
bacteriostatic action of tetracycline may impair bactericidal effects of the
penicillins |
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Stability |
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Reconstituted solution is stable for 48 hours at room temperature and 7 days
when refrigerated; for I.V. infusion in NS or D5W solution is stable
for 48 hours at room temperature, 7 days when refrigerated or 28 days when
frozen; after freezing, thawed solution is stable for 48 hours at room
temperature or 7 days when refrigerated; if precipitation occurs under
refrigeration, warm in water bath (37°C) for 20 minutes
and shake well |
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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.: 63%
Distribution: Into bile, heart, peritoneal fluid, sputum, bone; does not
cross the blood-brain barrier well unless meninges are inflamed; crosses the
placenta; distributes into breast milk at low concentrations
Protein binding: 30%
Metabolism: Minimal
Half-life: Dose dependent:
Neonates: <7 days: 3.7-4.4 hours; >7 days: 2.5 hours
Children 2-19 years: 0.9 hour
Adults: 50-70 minutes, increased in renal impairment
Time to peak serum concentration:
I.M.: 45-90 minutes after administration
I.V. infusion: Within 5 minutes
Elimination: Principally as unchanged drug in urine, also excreted via bile
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Usual Dosage |
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I.M., I.V.:
less than or equal to 7 days, less than or equal to 2000 g: 75 mg/kg every
12 hours
less than or equal to 7 days, >2000 g: Same as above
>7 days, less than or equal to 2000 g: 75 mg/kg every 8 hours
>7 days, >2000 g: 75 mg/kg every 6 hours
Children: 300 mg/kg/day divided every 4-6 hours; maximum: 24 g/day
Adults: Usual: 3-4 g every 4-6 hours
Uncomplicated urinary tract infection: 1.5-2 g every 6 hours
Serious infections: 200-300 mg/kg/day in 4-6 divided doses
Dosing interval in renal impairment:
Clcr 10-30 mL/minute: Administer every 6-8 hours
Clcr <10 mL/minute: Administer every 8 hours
Hemodialysis: Moderately dialyzable (20% to 50%)
Dosing adjustment in hepatic impairment: Reduce dose by 50%
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Monitoring
Parameters |
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Observe for signs and symptoms of anaphylaxis during first
dose |
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Test
Interactions |
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False-positive direct Coombs'; false-positive urinary or serum protein; may
inactivate aminoglycosides in vitro |
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Mental Health: Effects
on Mental Status |
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May cause dizziness; 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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May cause leukopenia; use caution with clozapine and
carbamazepine |
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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 can only be administered by infusion or injection. Maintain
adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid
intake). Small frequent meals, frequent mouth care, and adequate fluids may
reduce incidence of nausea or vomiting. 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 difficulty breathing, acute
diarrhea, systemic rash, fever, white plaques in mouth, or mouth sores.
Breast-feeding precautions: Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Administer at least 1 hour prior to aminoglycosides |
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Dosage Forms |
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Powder for injection, as sodium: 1 g, 2 g, 3 g, 4 g, 20
g |
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References |
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Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Meyers BR, Mendelson MH, Srulevitch-Chin E, et al,
"Pharmacokinetic Properties of Mezlocillin in Ambulatory Elderly Subjects," J
Clin Pharmacol, 1987, 27(9):678-81.
Odio C, Threlkeld N, Thomas ML, et al,
"Pharmacokinetic Properties of Mezlocillin in Newborn Infants," Antimicrob
Agents Chemother, 1984, 25(5):556-9.
Prober CG, Stevenson DK, and Benitz WE,
"The Use of Antibiotics in Neonates Weighing Less Than 1200 Grams," Pediatr
Infect Dis J, 1990, 9(2):111-21.
Rohde B, Werner U, Hickstein H, et al,
"Pharmacokinetics of Mezlocillin and Sulbactam Under Continuous Veno-Venous Hemodialysis (CVVHD) in Intensive Care Patients With Acute Renal Failure,"
Eur J Clin Pharmacol, 1997, 53(2):111-5.
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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