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Product Name
:
AMPI
Chemical Name
:
Ampicillin (Sodium)
Therapeutic Category
:
Antimicrobial
Pharmacologic Category
:
Antibiotic, Penicillin
Pharmaceutical Form
:
Vial
Composition
:
Ampicillin (Sodium) 500mg / 1000mg / 2000mg
Dosing
 
Usual dosage range:
I.M., I.V.: 250-500 mg every 6 hours
Actinomycosis: I.V.: 50 mg/kg/day for 4-6 weeks then oral amoxicillin

Cholangitis (acute): I.V.: 2 g every 4 hours with gentamicin

Diverticulitis: I.M., I.V.: 2 g every 6 hours with metronidazole

Endocarditis:

Infective: I.V.: 12 g/day via continuous infusion or divided every 4 hours

Prophylaxis: Dental, oral, or respiratory tract procedures: I.M., I.V.: 2 g within 30-60 minutes prior to procedure in patients not allergic to penicillin and unable to take oral amoxicillin. Intramuscular injections should be avoided in patients who are receiving anticoagulant therapy. In these circumstances, orally administered regimens should be given whenever possible. Intravenously administered antibiotics should be used for patients who are unable to tolerate or absorb oral medications. Note: American Heart Association (AHA) guidelines now recommend prophylaxis only in patients undergoing invasive procedures and in whom underlying cardiac conditions may predispose to a higher risk of adverse outcomes should infection occur.

Prophylaxis in total joint replacement patient: I.M., I.V.: 2 g 1 hour prior to the procedure

Genitourinary and gastrointestinal tract procedures: I.M., I.V.:

High-risk patients: 2 g within 30 minutes prior to procedure, followed by ampicillin 1 g (or amoxicillin 1 g orally) 6 hours later; must be used in combination with gentamicin. Note: As of April 2007, routine prophylaxis for GI/GU procedures is no longer recommended by the AHA.

Moderate-risk patients: 2 g within 30 minutes prior to procedure

Group B strep prophylaxis (intrapartum): I.V.: 2 g initial dose, then 1 g every 4 hours until delivery

Listeria infections: I.V.: 2 g every 4 hours (consider addition of aminoglycoside)

Sepsis/meningitis: I.M., I.V.: 150-250 mg/kg/day divided every 3-4 hours (range: 6-12 g/day)

Urinary tract infections (Enterococcus suspected): I.V.: 1-2 g every 6 hours with gentamicin

Dosing: Pediatric

Usual dosage range: Infants and Children:

I.M., I.V.: 100-400 mg/kg/day in divided doses every 6 hours (maximum: 12 g/day)

Endocarditis prophylaxis: Infants and Children: I.M., I.V.:

Dental, oral, or respiratory tract procedures: 50 mg/kg within 30-60 minutes prior to procedure in patients not allergic to penicillin and unable to take oral amoxicillin. Intramuscular injections should be avoided in patients who are receiving anticoagulant therapy. In these circumstances, orally administered regimens should be given whenever possible. Intravenously administered antibiotics should be used for patients who are unable to tolerate or absorb oral medications.

Note: American Heart Association (AHA) guidelines now recommend prophylaxis only in patients undergoing invasive procedures and in whom underlying cardiac conditions may predispose to a higher risk of adverse outcomes should infection occur.

Genitourinary and gastrointestinal tract procedures:

High-risk patients: 50 mg/kg (maximum: 2 g) within 30 minutes prior to procedure, followed by ampicillin 25 mg/kg (or amoxicillin 25 mg/kg orally) 6 hours later; must be used in combination with gentamicin. Note: As of April 2007, routine prophylaxis for GI/GU procedures is no longer recommended by the AHA.

Moderate-risk patients: 50 mg/kg within 30 minutes prior to procedure.

Mild-to-moderate infections: Infants and Children:

I.M., I.V.: 100-150 mg/kg/day in divided doses every 6 hours (maximum: 2-4 g/day)

Severe infections/meningitis: Infants and Children: I.M., I.V.: 200-400 mg/kg/day in divided doses every 6 hours (maximum: 6-12 g/day)

Dosing: Geriatric

Administer usual adult dose unless renal function is markedly reduced.

Dosing: Renal Impairment
Clcr >50 mL/minute: Administer every 6 hours

Clcr 10-50 mL/minute: Administer every 6-12 hours

Clcr <10 mL/minute: Administer every 12-24 hours

Intermittent hemodialysis (IHD) (administer after hemodialysis on dialysis days): Dialyzable (20% to 50%): I.V.: 1-2 g every 12-24 hours (Heintz, 2009). Note: Dosing dependent on the assumption of 3 times/week, complete IHD sessions.

Peritoneal dialysis (PD): 250 mg every 12 hours

Continuous renal replacement therapy (CRRT) (Heintz, 2009): Drug clearance is highly dependent on the method of renal replacement, filter type, and flow rate. Appropriate dosing requires close monitoring of pharmacologic response, signs of adverse reactions due to drug accumulation, as well as drug concentrations in relation to target trough (if appropriate). The following are general recommendations only (based on dialysate flow/ultrafiltration rates of 1-2 L/hour and minimal residual renal function) and should not supersede clinical judgment:

CVVH: Loading dose of 2 g followed by 1-2 g every 8-12 hours
CVVHD: Loading dose of 2 g followed by 1-2 g every 8 hours

CVVHDF: Loading dose of 2 g followed by 1-2 g every 6-8 hours

Use
 

Treatment of susceptible bacterial infections (nonbeta-lactamase-producing organisms); treatment or prophylaxis of infective endocarditis; susceptible bacterial infections caused by streptococci, pneumococci, nonpenicillinase-producing staphylococci, Listeria, meningococci; some strains of H. influenzae, Salmonella, Shigella, E. coli, Enterobacter, and Klebsiella

Adverse Reactions
 
Frequency not defined.

Central nervous system: Fever, penicillin encephalopathy, seizure

Dermatologic: Erythema multiforme, exfoliative dermatitis, rash, urticaria

Note: 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 infection, Salmonella infection, lymphocytic leukemia, or patients that have hyperuricemia.

Gastrointestinal: Black hairy tongue, diarrhea, enterocolitis, glossitis, nausea, pseudomembranous colitis, sore mouth or tongue, stomatitis, vomiting, oral candidiasis

Hematologic: Agranulocytosis, anemia, hemolytic anemia, eosinophilia, leukopenia, thrombocytopenia purpura

Hepatic: AST increased
Renal: Interstitial nephritis (rare)
Respiratory: Laryngeal stridor
Miscellaneous: Anaphylaxis, serum sickness-like reaction
Contraindications
 

Hypersensitivity to ampicillin, any component of the formulation, or other penicillins

Warnings / Precautions Drug
 
Concerns related to adverse effects:

• Anaphylactoid/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Use with caution in asthmatic patients.

• Rash: Appearance of a rash should be carefully evaluated to differentiate a nonallergic ampicillin rash from a hypersensitivity reaction; rash occurs in 5% to 10% of children 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.

• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

• Infectious mononucleosis: A high percentage of patients with infectious mononucleosis have developed rash during therapy; ampicillin-class antibiotics not recommended in these patients.

• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.

Interactions
 

Allopurinol: May enhance the potential for allergic or hypersensitivity reactions to Ampicillin. Risk C: Monitor therapy

Atenolol: Ampicillin may decrease the bioavailability of Atenolol. Risk C: Monitor therapy

BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination

Chloroquine: May decrease the serum concentration of Ampicillin. Management: Choroquine prescribing information recommends separating administration of ampicillin and chloroquine by at least 2 hours to minimize any potential negative impact of chloroquine on ampicillin bioavailability. Risk D: Consider therapy modification

Fusidic Acid: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Lanthanum: May decrease the serum concentration of Ampicillin. Management: Administer oral ampicillin at least two hours before or after lanthanum. Risk D: Consider therapy modification

Methotrexate: Penicillins may decrease the excretion of Methotrexate. Risk C: Monitor therapy

Mycophenolate: Penicillins may decrease serum concentrations of the active metabolite(s) of Mycophenolate. This effect appears to be the result of impaired enterohepatic recirculation. Risk C: Monitor therapy

Probenecid: May increase the serum concentration of Penicillins. Risk C: Monitor therapy

Tetracycline Derivatives: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Pregnancy
 
B
Pregnancy Implications

Adverse events have not been observed in animal studies; therefore, ampicillin is classified as pregnancy category B. Ampicillin crosses the human placenta, providing detectable concentrations in the cord serum and amniotic fluid. Most studies have not identified a teratogenic potential for ampicillin use during pregnancy. Two possible associations (congenital heart disease and cleft palate) have been noted; each of these was observed in a single study, was not substantiated by other studies, and may have been chance associations. Ampicillin is recommended for use in pregnant women for the management of premature rupture of membranes. Ampicillin is considered an acceptable alternative to penicillin for the prevention of early-onset Group B Streptococcal (GBS) disease in newborns.

The volume of distribution of ampicillin is increased during pregnancy and the half-life is decreased. As a result, serum concentrations in pregnant patients are approximately 50% of those in nonpregnant patients receiving the same dose. Higher doses may be needed during pregnancy. Although oral absorption is not altered during pregnancy, oral ampicillin is poorly-absorbed during labor.

Lactation
 
Enters breast milk/use caution
Breast-Feeding Considerations

Ampicillin is excreted in breast milk. The manufacturer recommends that caution be exercised when administering ampicillin to nursing women. Due to the low concentrations in human milk, minimal toxicity would be expected in the nursing infant. Nondose-related effects could include modification of bowel flora and allergic sensitization.

Monitoring Parameters
 

With prolonged therapy, monitor renal, hepatic, and hematologic function periodically; observe signs and symptoms of anaphylaxis during first dose

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: Bile, blister, and tissue fluids; penetration into CSF occurs with inflamed meninges only, good only with inflammation (exceeds usual MICs)

Normal meninges: Nil; Inflamed meninges: 5% to 10%
Protein binding: 15% to 25%
Half-life elimination:
Children and Adults: 1-1.8 hours
Anuria/end-stage renal disease: 7-20 hours
Excretion: Urine (90% as unchanged drug) within 24 hours
 
   
 
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