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Pronunciation |
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(am
pi SIL
in) |
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U.S. Brand
Names |
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Marcillin®; Omnipen®;
Omnipen®-N; Polycillin-N®; Principen®;
Totacillin®; Totacillin®-N |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Ampicin® Sodium; Apo®-Ampi
Trihydrate; Jaa Amp® Trihydrate; Nu-Ampi Trihydrate; Pro-Ampi®
Trihydrate; Taro-Ampicillin®
Trihydrate |
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Synonyms |
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Aminobenzylpenicillin; Ampicillin Sodium; Ampicillin Trihydrate |
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Pharmacological Index |
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Antibiotic, Penicillin |
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Use |
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Dental: Alternate antibiotic for the prevention of bacterial endocarditis in
patients undergoing dental procedures. It is used in those patients unable to
take oral medications
Medical: Treatment of susceptible bacterial infections
(nonbeta-lactamase-producing organisms); susceptible bacterial infections caused
by streptococci, pneumococci, nonpenicillinase-producing staphylococci,
Listeria, meningococci; some strains of H. influenzae,
Salmonella, Shigella, E. coli, Enterobacter, and
Klebsiella |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Known hypersensitivity to ampicillin or other
penicillins |
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Warnings/Precautions |
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Dosage adjustment may be necessary in patients with renal impairment; a low
incidence of cross-allergy with other beta-lactams exists; high percentage of
patients with infectious mononucleosis have developed rash during therapy with
ampicillin. Appearance of a rash should be carefully evaluated to differentiate
a nonallergic ampicillin rash from a hypersensitivity reaction. Ampicillin rash
occurs in 5% to 10% of children receiving ampicillin and is a generalized dull
red, maculopapular rash, generally appearing 3-14 days after the start of
therapy. It normally begins on the trunk and spreads over most of the body. It
may be most intense at pressure areas, elbows, and knees. |
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Adverse
Reactions |
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>10%: Local: Pain at injection site
1% to 10%:
Dermatologic: Rash (appearance of a rash should be carefully evaluated to
differentiate, if possible; nonallergic ampicillin rash from hypersensitivity
reaction; incidence is higher in patients with viral infections,
Salmonella infections, lymphocytic leukemia, or patients that have
hyperuricemia)
Gastrointestinal: Diarrhea, vomiting, oral candidiasis, abdominal cramps
Miscellaneous: Allergic reaction (includes serum sickness, urticaria,
angioedema, bronchospasm, hypotension, etc)
<1%: Penicillin encephalopathy, seizures (with large I.V. doses or
patients with renal dysfunction), anemia, hemolytic anemia, thrombocytopenia,
thrombocytopenic purpura, eosinophilia, leukopenia, granulocytopenia, decreased
lymphocytes, interstitial nephritis (rare) |
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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: Efficacy of oral contraceptives may be reduced
Increased effect: Disulfiram, probenecid may increase penicillin levels,
increased effect of anticoagulants
Increased toxicity: Allopurinol theoretically has an additive potential for
amoxicillin (ampicillin) rash |
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Stability |
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Oral suspension is stable for 7 days at room temperature or for 14 days under
refrigeration; solutions for I.M. or direct I.V. should be used within 1 hour;
solutions for I.V. infusion will be inactivated by dextrose at room temperature;
if dextrose-containing solutions are to be used, the resultant solution will
only be stable for 2 hours versus 8 hours in the 0.9% sodium chloride injection.
D5W has limited stability.
Stability of parenteral admixture in NS at room temperature
(25°C): 8 hours
Stability of parenteral admixture in NS at refrigeration temperature
(4°C): 2 days
Standard diluent: 500 mg/50 mL NS; 1 g/50 mL NS; 2 g/100 mL NS
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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: Oral: 50%
Distribution: Distributes into bile; penetration into CSF occurs with
inflamed meninges only, good only with inflammation (exceeds usual MICs)
Normal meninges: Nil
Inflamed meninges: 5-10
Protein binding: 15% to 25%
Half-life:
Neonates: 2-7 days: 4 hours; 8-14 days: 2.8 hours; 15-30 days: 1.7 hours
Children and Adults: 1-1.8 hours
Anuria/end-stage renal disease: 7-20 hours
Time to peak: Oral: Within 1-2 hours
Elimination: ~90% of the drug excreted unchanged in the urine within 24 hours
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Usual Dosage |
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Neonates: I.M., I.V.:
Postnatal age less than or equal to 7 days:
less than or equal to 2000 g: Meningitis: 50 mg/kg/dose every 12 hours;
other infections: 25 mg/kg/dose every 12 hours
>2000 g: Meningitis: 50 mg/kg/dose every 8 hours; other infections: 25
mg/kg/dose every 8 hours
Postnatal age >7 days:
<1200 g: Meningitis: 50 mg/kg/dose every 12 hours; other infections: 25
mg/kg/dose every 12 hours
1200-2000 g: Meningitis: 50 mg/kg/dose every 8 hours; other infections: 25
mg/kg/dose every 8 hours
>2000 g: Meningitis: 50 mg/kg/dose every 6 hours; other infections: 25
mg/kg/dose every 6 hours
Infants and Children: I.M., I.V.: 100-400 mg/kg/day in doses divided every
4-6 hours
Meningitis: 200 mg/kg/day in doses divided every 4-6 hours; maximum dose: 12
g/day
Children: Oral: 50-100 mg/kg/day in doses divided every 6 hours; maximum
dose: 2-3 g/day
Adults:
Oral: 250-500 mg every 6 hours
I.M.: 500 mg to 1.5 g every 4-6 hours
I.V.: 500 mg to 3 g every 4-6 hours; maximum dose: 12 g/day
Sepsis/meningitis: 150-250 mg/kg/24 hours divided every 3-4 hours
Dosing interval in renal impairment:
Clcr 30-50 mL/minute: Administer every 6-8 hours
Clcr 10-30 mL/minute: Administer every 8-12 hours
Clcr <10 mL/minute: Administer every 12 hours
Hemodialysis: Moderately dialyzable (20% to 50%); administer dose after
dialysis
Peritoneal dialysis: Moderately dialyzable (20% to 50%)
Administer 250 mg every 12 hours
Continuous arteriovenous or venovenous hemofiltration (CAVH) effects: Dose as
for Clcr 10-50 mL/minute; ~50 mg of ampicillin per liter of filtrate
is removed |
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Dietary
Considerations |
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Food: Decreases drug absorption rate; decreases drug serum concentration.
Take on an empty stomach 1 hour before or 2 hours after
meals. |
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Monitoring
Parameters |
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With prolonged therapy monitor renal, hepatic, and hematologic function
periodically; observe signs and symptoms of 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 |
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Mental Health: Effects
on Mental Status |
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Large I.V. doses may rarely produce encephalopathy; penicillins have been
reported to cause apprehension, illusions, agitation, insomnia,
depersonalization, and encephalopathy |
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Mental Health:
Effects on Psychiatric
Treatment |
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Rarely may cause bone marrow suppression; 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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Take entire prescription, even if you are feeling better. Take at equal
intervals around-the-clock; preferably on an empty stomach with a full glass of
water (1 hour before or 2 hours after meals). Maintain adequate hydration (2-3
L/day of fluids unless instructed to restrict fluid intake). You may experience
nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges,
or chewing gum may help). 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 rash; unusual diarrhea; unusual
vaginal discharge, itching, burning, or pain; mouth sores; unresolved vomiting
or constipation; fever or chills; unusual bruising or bleeding; or if condition
being treated worsens or does not improve by the time prescription is
completed. |
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Nursing
Implications |
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Ampicillin and gentamicin should not be mixed in the same I.V. tubing or
administered concurrently |
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Dosage Forms |
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Capsule, as anhydrous: 250 mg, 500 mg
Capsule, as trihydrate: 250 mg, 500 mg
Powder for injection, as sodium: 125 mg, 250 mg, 500 mg, 1 g, 2 g, 10 g
Powder for oral suspension, as trihydrate: 125 mg/5 mL (5 mL unit dose, 80
mL, 100 mL, 150 mL, 200 mL); 250 mg/5 mL (5 mL unit dose, 80 mL, 100 mL, 150 mL,
200 mL); 500 mg/5 mL (5 mL unit dose, 100 mL)
Powder for oral suspension, drops, as trihydrate: 100 mg/mL (20 mL)
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References |
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Boguniewicz M and Leung DY,
"Hypersensitivity Reactions to Antibiotics Commonly Used in Children,"
Pediatr Infect Dis J, 1995, 14(3):221-31.
Brown RD, Campoli-Richards DM,
"Antimicrobial Therapy in Neonates, Infants, and Children," Clin
Pharmacokinet, 1989, 17(Suppl 1):105-15.
Dajani AS, Taubert KA, Wilson W, et al,
"Prevention of Bacterial Endocarditis Recommendations by the American Heart Association,"
JAMA 1997, 277(22):1794-801.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Tenenbein M, Cohen S, and Sitar DS,
"Whole Bowel Irrigation as a Decontamination Procedure After Acute Drug Overdose,"
Arch Intern Med, 1987, 147(5):905-7.
Triggs EJ, Johnson JM, and Learoyd B,
"Absorption and Disposition of Ampicillin in the Elderly," Eur J Clin
Pharmacol, 1980, 18(2):195-8.
Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.
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