Ampicillin (Systemic)

Introductory Information

Antibacterial; β-lactam antibiotic; aminopenicillin.1, 2, 8, 9

Class: 8:12.16.08 Aminopenicillins

Brands*: Principen®
*
also available generically

Generic Name: Ampicillin

CAS Number: 69-53-4
Chemical Name: [2S-[2α,5α,6β(S*)]]-6-[(Aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-
1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Molecular Formula: C16H19N3O4S
Investigational Drug Number: AY-6108, BRL 1341, NSC-528986
Synonym: Aminobenzylpenicillin, d(-)-α-Aminobenzylpenicillin, Ampicillin A

Generic Name: Ampicillin Sodium

CAS Number: 69-52-3
Chemical Name: [2S-[2α,5α,6β(S*)]]-6-[(Aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-
1-azabicyclo[3.2.0]heptane-2-carboxylic acid monosodium salt
Molecular Formula: C16H19N3O4S•Na
Synonym: Sodium Ampicillin

Generic Name: Ampicillin Trihydrate

CAS Number: 7177-48-2
Chemical Name: [2S-[2α,5α,6β(S*)]]-6-[(Aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-
1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate
Molecular Formula: C16H19N3O4S•3H2O
Synonym: Aminobenzylpenicillin Trihydrate, Ampicillin

Uses

Endocarditis

Treatment of enterococcal endocarditis;2, 4, 6, 7 used in conjunction with an aminoglycoside.4, 6, 7

Treatment of endocarditis caused by slow-growing fastidious gram-negative bacilli termed the

HACEK group (i.e., Haemophilus parainfluenzae, H. aphrophilus, Actinobacillus

actinomycetemcomitans, Cardiobacterium hominis, Eikenella corrodens, Kingella kingae).6, 7
Used in conjunction with gentamicin; consider that these infections may involve β-lacatamase-
producing bacteria resistant to ampicillin alone.6, 7
Treatment of endocarditis caused by susceptible staphylococci, streptococci, E. coli, P. mirabilis,
or Salmonella.2

Prevention of bacterial endocarditis in patients undergoing certain dental, oral, respiratory tract,

or esophageal procedures who have cardiac conditions that put them at moderate or high
risk.10 AHA recommends ampicillin as a drug of choice.10

Prevention of bacterial endocarditis in patients undergoing certain GU and GI (except

esophageal) procedures who have cardiac conditions that put them at moderate or high
risk. AHA recommends ampicillin as a drug of choice.10 Used alone in those at moderate risk
10

or in conjunction with gentamicin in those at high risk.10

Consult most recent AHA recommendations for specific information on which cardiac
conditions are associated with high or moderate risk of endocarditis and which procedures
require prophylaxis.10

Meningitis and Other CNS Infections

Treatment of meningitis caused by susceptible Neisseria meningitidis,2, 5 Streptococcus

agalactiae (group B streptococci),2, 5 Listeria monocytogenes,2, 4, 5 E. coli,2, 5 H. influenzae

,5 or S. pneumoniae .

Drug of choice for empiric treatment of neonatal S. agalactiae meningitis.5 An aminoglycoside

(IV gentamicin) used concomitantly until in vitro susceptibility testing is complete and a clinical
response obtained;5 treatment can then be changed to penicillin G.5

Drug of choice for L. monocytogenes meningitis;4, 5, 9 used alone or in conjunction with an

aminoglycoside (e.g., gentamicin).4, 5, 9

Penicillin G usually preferred for N. meningitidis meningitis and penicillin-susceptible S.

pneumoniae meningitis.5 For H. influenzae meningitis, cefotaxime, ceftriaxone, or, alternatively,
ampicillin in conjunction with chloramphenicol is recommended; ampicillin should not be used
alone (see Ampicillin-resistant Haemophilus influenzae under Cautions).5

Respiratory Tract Infections

Treatment of respiratory tract infections caused by susceptible Staphylococcus aureus (including

penicillinase-producing strains), Streptococcus (including S. pneumoniae), S. pyogenes (group A
β-hemolytic streptococci), or H. influenzae (nonpenicillinase-producing strains only).1, 2, 9

Generally should not be used for the treatment of streptococcal or staphylococcal infections
when a natural penicillin would be effective.4, 5, 8, 9 Should not be used alone for empiric
treatment of respiratory tract infections when ampicillin-resistant H. influenzae may be
involved.5, 9
Septicemia

Treatment of septicemia caused by susceptible staphylococci, streptococci, enterococci, E. coli,

P. mirabilis, or Salmonella.2, 9

Urinary Tract Infections (UTIs)

Treatment of UTIs caused by susceptible enterococci, E. coli, or Proteus mirabilis.1, 2, 9

A drug of choice for enterococcal UTIs.4, 9 Because of high urinary concentrations, may be
effective when used alone,9 but consider that enterococci resistant to ampicillin have been
reported.4

Eikenella Infections

Treatment of infections caused by Eikenella corrodens ; drug of choice.4

Gonorrhea and Associated Infections

Previously used for treatment of acute uncomplicated gonorrhea (anogenital and urethral) caused
by susceptible Neisseria gonorrhoeae.1 Has been used for gonococcal urethritis.2 No longer
recommended for gonorrhea or gonococcal urethritis by CDC or other experts (high incidence of
penicillin-resistant strains).11

Listeria Infections

Treatment of infections caused by Listeria monocytogenes; used alone or in conjunction with an

aminoglycoside.5, 9

A drug of choice for Listeria infections occurring during pregnancy, granulomatosis

infantiseptica, sepsis, endocarditis, meningitis, and foodborne infections.4, 5, 9, 9 (See Meningitis
and Other CNS Infections under Uses.)

Pertussis

Has been used to treat and prevent secondary pulmonary infections in patients with pertussis

.9 Erythromycin generally considered drug of choice for treatment of catarrhal stage of

pertussis and to shorten the period of communicability of the disease.5, 9 Ampicillin, like most
other anti-infectives, does not shorten clinical course of pertussis.9

Typhoid Fever and Other Salmonella Infections

Alternative for treatment of typhoid fever (enteric fever) caused by susceptible Salmonella
typhi.2, 4, 5, 9 Drugs of choice are third generation cephalosporins (e.g., ceftriaxone, cefotaxime)
or fluoroquinolones (e.g., ciprofloxacin, ofloxacin);4 consider that multidrug-resistant strains of
S. typhi (strains resistant to ampicillin, amoxicillin, chloramphenicol, and/or co-trimoxazole)
reported with increasing frequency.5
Treatment of chronic carriers of S. typhi ; drugs of choice are fluoroquinolones (e.g.,
ciprofloxacin), ampicillin, or amoxicillin (with probenecid).5, 8, 9

Treatment of gastroenteritis caused by susceptible Salmonella.2, 4, 5

Long-term suppressive or maintenance therapy (secondary prophylaxis) in HIV-infected patients

to prevent recurrence of nontyphi Salmonella septicemia .

Shigella Infections

Treatment of GI infections caused by susceptible Shigella.1, 2, 5, 9

Anti-infectives generally indicated in addition to fluid and electrolyte replacement for severe
shigellosis.5, 9 Previously considered a drug of choice for shigellosis (especially in children),9 but
strains of S. flexneri and S. sonnei resistant to ampicillin reported with increasing frequency.9
Fluoroquinolones, ceftriaxone, or co-trimoxazole now considered drugs of choice for empiric
treatment,4, 5, 9 especially in areas where ampicillin-resistant strains of Shigella have been
reported.5, 9

Prevention of Perinatal Group B Streptococcal Disease

Prevention of early-onset neonatal group B streptococcal (GBS) disease .5

Intrapartum anti-infective prophylaxis to prevent early-onset neonatal GBS disease is

administered to women identified as GBS carriers during routine prenatal GBS screening
performed at 35-37 weeks during the current pregnancy and to women who have GBS
bacteriuria during the current pregnancy, a previous infant with invasive GBS disease, unknown
GBS status with delivery at <37 weeks gestation, amniotic membrane rupture for ≥18 hours, or
intrapartum temperature of ≥38°C.

When intrapartum GBS prophylaxis is indicated, IV penicillin G is the drug of choice. Although
IV ampicillin can be used, CDC and AAP state that penicillin G is preferred since it has a
narrower spectrum of activity and is less likely to select for antibiotic-resistant organisms.

Perioperative Prophylaxis

Has been used for perioperative prophylaxis in patients undergoing vaginal hysterectomy or
cesarean section. Cephalosporins (cefazolin, cefotetan, cefoxitin) usually drugs of choice for
perioperative prophylaxis in patients undergoing obstetric and gynecologic surgery.

Perioperative prophylaxis in patients undergoing biliary tract or intestinal surgery including

appendectomy . Cephalosporins (cefazolin, cefoxitin) usually drugs of choice.

Dosage and Administration

Administration

Administer orally,1 by slow IV injection or infusion,2 or by IM injection.2

Parenteral route used for treatment of moderately severe or severe infections.2 Oral route should
not be used for initial treatment of severe, life-threatening infections, but may be used as follow-
up after parenteral ampicillin.

Oral Administration
Administer orally with a full glass of water 1 hour before or 2 hours after meals.1

IV Administration
Reconstitution
Reconstitute vials containing 125, 250, or 500 mg with 5 mL of sterile or bacteriostatic water for
injection.2 Alternatively, reconstitute vials containing 1 or 2 g with 7.4 or 14.8 mL, respectively,
of sterile or bacteriostatic water for injection.2

Rate of Administration
Solutions reconstituted from 125-, 250-, or 500-mg vials may be given by IV injection over a
period of 3-5 minutes.2 Solutions reconstituted from 1- or 2-g vials should be given IV over a
period of ≥10-15 minutes.2

For IV infusion, concentration and rate of administration should be adjusted so that the total dose
is administered before the drug is inactivated in the IV solution.2

IM Administration
Reconstitution
Reconstitute with sterile or bacteriostatic water for injection according to manufacturer's
directions to provide solutions containing 125 or 250 mg/mL.2

Dosage

Available as ampicillin trihydrate1 and ampicillin sodium2; dosage expressed in terms of

ampicillin.1, 2

Duration of therapy depends on type and severity of infection and should be determined by
clinical and bacteriologic response of the patient.1, 2 For most infections, therapy should be
continued for ≥48-72 hours after patient becomes asymptomatic or evidence of eradication of the
infection has been obtained.1, 2 More prolonged therapy may be necessary for some infections.1, 2

Pediatric Patients
General Pediatric Dosage
Oral: Children ≥1 month of age: AAP recommends 50-100 mg/kg daily given in 4 divided doses
for mild to moderate infections.5
AAP states oral route is inappropriate for severe infections.5

>IV or IM
Neonates <1 week of age: AAP recommends 25-50 mg/kg every 12 hours in those weighing ≤2
kg or 25-50 mg/kg every 8 hours in those weighing >2 kg.5
Neonates 1-4 weeks of age: AAP recommends 25-50 mg/kg every 12 hours for those weighing
<1.2 kg, 25-50 mg/kg every 8 hours for those weighing 1.2-2 kg, or 25-50 mg/kg every 6 hours
for those weighing >2 kg.5
Children ≥1 month of age: AAP recommends 100-150 mg/kg daily given in 4 divided doses for
mild to moderate infections or 200-400 mg/kg daily given in 4 divided doses for severe
infections.5

Endocarditis
>Treatment of Endocarditis Caused by Viridans Streptococci or S. bovis
IV: 300 mg/kg daily given in 4-6 divided doses for 4 weeks.7 Used in conjunction with IM or IV
gentamicin (3 mg daily given during the first 2 weeks).7

>Treatment of Enterococcal Endocarditis

IV: 300 mg/kg daily given in 4-6 divided doses for 4-6 weeks.7 Used in conjunction with IM or
IV gentamicin (3 mg daily given for 4-6 weeks).7

>Prevention of Bacterial Endocarditis in Patients Undergoing Certain Dental, Oral,

Respiratory Tract, or Esophageal Procedures

IV or IM: 50 mg/kg given 30 minutes prior to the procedure.10

>Prevention of Enterococcal Endocarditis in Patients Undergoing Certain Genitourinary or

GI (except Esophageal) Procedures

IV or IM: For moderate-risk patients, 50 mg/kg given 30 minutes prior to the procedure.10
For high-risk patients, 50 mg/kg (up to 2 g) as a single dose in conjunction with a single dose of
gentamicin (1.5 mg/kg) given 30 minutes prior to the procedure followed a dose of IM or IV
ampicillin (25 mg/kg) given 6 hours later or, alternatively, oral amoxicillin (25 mg/kg) given 6
hours later.10

GI Infections
Oral: Children weighing ≤20 kg: 100 mg/kg daily in 4 divided doses.1
Children weighing >20 kg: 500 mg 4 times daily.1 Severe or chronic infections may require
higher dosage.1

>IV or IM
Children weighing <40 kg: 50 mg/kg daily in divided doses every 6-8 hours.2
Children weighing ≥40 kg: 500 mg every 6 hours.2 Severe or chronic infections may require
higher dosage.1

Meningitis and Other CNS Infections

>Empiric Treatment of Meningitis
IV: Neonates and children <2 months of age: 100-300 mg/kg daily given in divided doses; used
in conjunction with IM gentamicin pending results of in vitro susceptibility tests.
Children 2 months to 12 years of age: 200-400 mg/kg daily given in divided doses every 4-6
hours; used in conjunction with IV chloramphenicol.
>Treatment of Meningitis Caused by S. agalactiae
IV: AAP recommends 200-300 mg/kg daily given in 3 divided for neonates ≤7 days of age or
300 mg/kg daily given in 4-6 divided doses for neonates >7 days of age.5

Respiratory Tract Infections

Oral: Children weighing ≤20 kg: 50 mg/kg daily in 3 or 4 divided doses.1
Children weighing >20 kg: 250 mg 4 times daily.1

>IV or IM
Children weighing <40 kg: 25-50 mg/kg daily in divided doses every 6-8 hours.2
Children weighing ≥40 kg: 250-500 mg every 6 hours.2

Septicemia
>IV or IM
150-200 mg/kg daily.2

Skin and Skin Structure Infections

>IV or IM
Children weighing <40 kg: 25-50 mg/kg daily in divided doses every 6-8 hours.2
Children weighing ≥40 kg: 250-500 mg every 6 hours.2

Urinary Tract Infections (UTIs)

Oral: Children weighing ≤20 kg: 100 mg/kg daily in 4 divided doses.1
Children weighing >20 kg: 500 mg 4 times daily.1 Severe or chronic infections may require
higher dosage.1

>IV or IM
Children weighing <40 kg: 50 mg/kg daily in divided doses every 6-8 hours.2
Children weighing ≥40 kg: 500 mg every 6 hours.2 Severe or chronic infections may require
higher dosage.1

Adults
Endocarditis
>Treatment of Enterococcal Endocarditis
IV: 12 g daily (by continuous IV infusion or in 6 equally divided IV doses) in conjunction with
IM or IV gentamicin (1 mg/kg every 8 hours).6 Treatment with both drugs generally should be
continued for 4-6 weeks, but patients who had symptoms of infection for >3 months before
treatment was initiated and patients with prosthetic heart valves require ≥6 weeks of therapy with
both drugs.6

>Treatment of Endocarditis Caused by HACEK group (i.e., H. parainfluenzae, H.

aphrophilus, A. actinomycetemcomitans, C. hominis, E. corrodens, K. kingae)

IV: 12 g daily (by continuous IV infusion or in 6 equally divided IV doses) in conjunction with
IM or IV gentamicin (1 mg/kg every 8 hours).6 Treatment with both drugs generally should be
continued for 4 weeks.6
>Prevention of Bacterial Endocarditis in Patients Undergoing Certain Dental, Oral,

Respiratory Tract, or Esophageal Procedures

IV or IM: 2 g as a single dose given 30 minutes prior to the procedure.10

>Prevention of Enterococcal Endocarditis in Patients Undergoing Certain GU or GI (except

Esophageal) Procedures
IV or IM: For moderate-risk patients, 2 g given 30 minutes prior to the procedure.10
For high-risk patients, 2 g as a single dose in conjunction with a single dose of gentamicin (1.5
mg/kg) given 30 minutes prior to the procedure followed by a dose of IM or IV ampicillin (1 g)
given 6 hours later or, alternatively, a dose of oral amoxicillin (1 g) given 6 hours later.10

GI Infections
Oral: 500 mg 4 times daily.1

>IV or IM
Adults weighing <40 kg: 50 mg/kg daily in divided doses every 6-8 hours.2
Adults weighing ≥40 kg: 500 mg every 6 hours.2

Meningitis and Other CNS Infections

>IV, then IM
150-200 mg/kg daily in divided doses every 3-4 hours.2 Use IV initially, may switch to IM after
3 days.2

Respiratory Tract Infections

Oral: 250 mg 4 times daily.1

>IV or IM
Adults weighing <40 kg: 25-50 mg/kg daily in divided doses every 6-8 hours.2
Adults weighing ≥40 kg: 250-500 mg every 6 hours.2

Septicemia
>IV or IM
150-200 mg/kg daily.2

Skin and Skin Structure Infections

>IV or IM
Adults weighing <40 kg: 25-50 mg/kg daily in divided doses every 6-8 hours.2
Adults weighing ≥40 kg: 250-500 mg every 6 hours.2

Urinary Tract Infections (UTIs)

Oral: 500 mg 4 times daily.1

>IV or IM
Adults weighing <40 kg: 50 mg/kg daily in divided doses every 6-8 hours.2
Adults weighing ≥40 kg: 500 mg every 6 hours.2
 Gonorrhea and Associated Infections
>Uncomplicated Gonorrhea
Oral: 3.5 g as a single dose (with 1 g of oral probenecid).1 No longer recommended for
gonorrhea by CDC or other experts.11

>Gonococcal Urethritis
IV or IM: 500 mg initially followed by 500 mg 8-12 hours later.2 No longer recommended by
CDC or other experts.11

Prevention of Perinatal Group B Streptococcal (GBS) Disease

>IV
An initial 2-g dose (at time of labor or rupture of membranes) followed by 1 g every 4 hours
until delivery.

Prescribing Limits

Pediatric Patients
Pediatric dosage should not exceed adult dosage.1

Special Populations

Renal Impairment
Dosage adjustments necessary in patients with renal impairment.9

Some clinicians suggest that adults with GFR 10-50 mL/minute receive the usual dose every 6-
12 hours and that adults with GFR <10 mL/minute receive the usual dose every 12-16 hours.
Alternatively, some clinicians suggest that modification of usual dosage is unnecessary in adults
with Clcr ≥ 30 mL/minute, but that adults with Clcr ≤10 mL/minute should receive the usual dose
every 8 hours.

Patients undergoing hemodialysis should receive a supplemental dose after each dialysis period.

Geriatric Patients
No dosage adjustments except those related to renal impairment. (See Renal Impairment under
Dosage and Administration.)

Cautions

Contraindications

• Known hypersensitivity to any penicillin.1, 2

Warnings/Precautions

Warnings
Superinfection/Clostridium difficile-associated Colitis
Possible emergence and overgrowth of nonsusceptible bacteria or fungi.1, 2 Discontinue and
institute appropriate therapy if superinfection occurs.1, 2

Treatment with anti-infectives may permit overgrowth of clostridia.1 Consider Clostridium

difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if
diarrhea develops and manage accordingly.1

Some mild cases of C. difficile-associated diarrhea and colitis may respond to discontinuance
alone.1 Manage moderate to severe cases with fluid, electrolyte, and protein supplementation;
appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) recommended if
colitis is severe.1

Sensitivity Reactions
Hypersensitivity Reactions
Serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, reported with
penicillins.1, 2, 9

Prior to initiation of therapy, make careful inquiry regarding previous hypersensitivity reactions
to penicillins, cephalosporins, or other drugs.1, 2 Partial cross-allergenicity occurs among
penicillins and other β-lactam antibiotics including cephalosporins and cephamycins.1, 2

If a severe hypersensitivity reaction occurs, discontinue immediately and institute appropriate

therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and
oxygen).1, 2

General Precautions
Selection and Use of Anti-infectives
To reduce development of drug-resistant bacteria and maintain effectiveness of ampicillin and
other antibacterials, use only for treatment or prevention of infections proven or strongly
suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro
susceptibility testing.1, 2 In the absence of such data, consider local epidemiology and
susceptibility patterns when selecting anti-infectives for empiric therapy.1, 2

Mononucleosis
Possible increased risk of rash in patients with mononucleosis; use in these patients not
recommended.

Ampicillin-resistant Haemophilus influenzae

Because of increasing prevalence of ampicillin-resistant H. influenzae,5 the drug should not be
used alone for empiric treatment of serious infections (e.g., meningitis, pneumonia) when H.
influenzae may be involved.5, 9

Laboratory Monitoring
Periodically assess organ system functions, including renal, hepatic, and hematopoietic, during
prolonged therapy.1, 2
Sodium Content
Powder for injection contains 2.9 mEq of sodium per g of ampicillin.2

Specific Populations
Pregnancy
Category B.1, 2

Lactation
Distributed into milk.1, 2, 9 Use with caution.1, 2

Pediatric Use
Renal clearance of ampicillin may be delayed in neonates and young infants because of
incompletely developed renal function.1, 9 Use lowest effective dosage.1

Renal Impairment
Dosage adjustments necessary in renal impairment.9 (See Renal Impairment under Dosage and
Administration.)

Common Adverse Effects

GI effects (diarrhea, nausea), rash.

Interactions

Specific Drugs and Laboratory Tests

Drug or Test Interaction Comments

Unclear whether potentiation of rash is
caused by allopurinol or hyperuricemia
present in these patients
Possible increased incidence of
Allopurinol Clinical importance has not been
rash
determined; some clinicians suggest that
concomitant use of the drugs should be
avoided if possible
In vitro evidence of synergistic
antibacterial effects against
enterococci; used to therapeutic
advantage in treatment of
Aminoglycosides endocarditis and other severe
enterococcal infections
Potential in vitro and in vivo
inactivation of
aminoglycosidesHID
Chloramphenicol In vitro evidence of antagonism Clinical importance unclear
Hormonal Possible decreased efficacy of Some clinicians suggest that a
contraceptives estrogen-containing oral supplemental method of contraception be
 contraceptives and increased used in patients receiving oral
incidence of breakthrough contraceptives and ampicillin
bleeding concomitantly, other clinicians state that
most women taking oral contraceptives
probably do not need to use alternative
contraceptive precautions while receiving
ampicillin
Possible decreased renal clearance
of methotrexate with penicillins;
Methotrexate possible increased methotrexate Monitor closely if used concomitantly
concentrations and hematologic
and GI toxicity
Decreased renal tubular secretion
of ampicillin; increased and
Probenecid
prolonged ampicillin
concentrations may occur9
Synergistic bactericidal effect
Sulbactam against many strains of β-
lactamase-producing bacteria
Sulfonamides In vitro evidence of antagonism1 Clinical importance unclear1
Possible false-positive reactions
Use glucose tests based on enzymatic
in urine glucose tests using
Tests for glucose glucose oxidase reactions (e.g., Clinistix®,
Clinitest®, Benedict's solution, or
Tes-Tape®)1 2
Fehling's solution1, 2
Possible falsely increased serum
uric acid concentrations when
copper-chelate method is used;
Tests for uric acid
phosphotungstate and uricase
methods appear to be unaffected
by the ampicillin

Pharmacokinetics

Absorption

Bioavailability
30-55% of an oral dose absorbed from the GI tract in fasting adults; peak serum concentrations
attained within 1-2 hours.9

Following IM administration, peak serum concentrations generally attained more quickly and are
higher than following equivalent oral doses.9

Rapid IV administration results in peak serum concentrations immediately after completion of

the infusion; serum concentrations may still be detectable 6 hours later.
Food
Food generally decreases rate and extent of absorption.9

Distribution

Extent
Distributed into ascitic, synovial, and pleural fluids. Also distributed into liver, bile,9 lungs,
gallbladder, prostate, muscle, middle ear effusions, bronchial secretions, sputum, maxillary sinus
secretions, tonsils, saliva, sweat, and tears.

Distributed into CSF in concentrations 11-65% of simultaneous serum concentrations; highest

CSF concentrations occur 3-7 hours after an IV dose.

Readily crosses the placenta.9 Distributed into milk in low concentrations.

Plasma Protein Binding

15-25%.1, 2, 9

Protein binding is lower in neonates than in children or adults; ampicillin reportedly 8-12%
bound to serum proteins in neonates.

Elimination

Metabolism
Partially metabolized by hydrolysis of the β-lactam ring to penicilloic acid which is
microbiologically inactive.9

Elimination Route
Eliminated in urine by renal tubular secretion and to a lesser extent by glomerular filtration.9
Small amounts also excreted in feces and bile.9

In adults with normal renal function, approximately 20-64% of a single oral dose9 excreted
unchanged in urine within 6-8 hours. Approximately 60-70% of a single IM dose or 73-90% of a
single IV dose excreted unchanged in urine.

Half-life
0.7-1.5 hours in adults with normal renal function.9

Half-life is 4 hours in neonates 2-7 days of age, 2.8 hours in neonates 8-14 days of age, and 1.7
hours in neonates 15-30 days of age.9

Special Populations
Serum concentrations higher and more prolonged in premature or full-term neonates <6 days of
age than in full-term neonates ≥6 days of age.

Renal clearance decreased in geriatric patients because of diminished tubular secretory ability;
serum concentrations may be higher and half-life prolonged. In those 67-76 years of age, half-
life ranges from 1.4-6.2 hours.
Serum concentrations are higher and half-life prolonged in patients with impaired renal function.
Half-life may range from 7.4-21 hours in patients with Clcr <10 mL/minute9

Stability

Storage

Oral
Capsules
Tight container at 15-30°C; avoid excessive heat.1

For Suspension
Tight container at 15-30°C.1 After reconstitution, discard after 7 days if stored at room
temperature or after 14 days if refrigerated.1

Parenteral
Powder for Injection or Infusion
Solutions for IM injection or IV injection or infusion should be used within 1 hour after
reconstitution and should not be frozen.2

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral
Solution CompatibilityHID

Compatible
Isolyte M or P with dextrose 5%
Incompatible
Amino acids 4.25%, dextrose 25%
Dextran 40 10% in sodium chloride 0.9%
Dextran 40 10% in dextrose 5% in water
Dextran 70 6% in sodium chloride 0.9%
Dextran 70 6% in dextrose 5% in water
Dextrose 5% in sodium chloride 0.9%
Dextrose 5 or 10% in water
Fat emulsion 10%, IV
Fructose 5.25%
Hetastarch 6%
Invert sugar 7.5% with electrolytes
Invert sugar 10% in water
Ringer's injection, lactated
Sodium bicarbonate 1.4%
Sodium lactate (1/6) M
Variable
Ringer's injection
Sodium chloride 0.9%

Drug Compatibility

>Admixture CompatibilityHID
Compatible
Cefotiam HCl
Clindamycin phosphate
Erythromycin lactobionate
Floxacillin sodium
Furosemide
Incompatible
Amikacin sulfate
Chlorpromazine HCl
Dopamine HCl
Gentamicin sulfate
Hydralazine HCl
Prochlorperazine mesylate
Variable
Aztreonam
Cefepime HCl
Cimetidine HCl
Heparin sodium
Hydrocortisone sodium succinate
Metronidazole
Metronidazole HCl with sodium bicarbonate
Ranitidine HCl
Sodium bicarbonate
Verapamil HCl

>Y-Site CompatibilityHID
Compatible
Acyclovir sodium
Amifostine
Anidulafungin
Aztreonam
Bivalirudin
Cyclophosphamide
Dexmedetomidine HCl
Docetaxel
Doxapram HCl
Doxorubicin HCl liposome injection
Enalaprilat
Esmolol HCl
Etoposide phosphate
Famotidine
Filgrastim
Fludarabine phosphate
Foscarnet sodium
Gemcitabine HCl
Granisetron HCl
Heparin sodium
Heparin sodium with hydrocortisone sodium succinate
Hetastarch in lactated electrolyte injection (Hextend)
Labetalol HCl
Levofloxacin
Linezolid
Magnesium sulfate
Melphalan HCl
Meperidine HCl
Milrinone acetate
Morphine sulfate
Multivitamins
Ofloxacin
Pantoprazole sodium
Pemetrexed disodium
Perphenazine
Phytonadione
Potassium chloride
Propofol
Remifentanil HCl
Tacrolimus
Teniposide
 Theophylline
Thiotepa
Vitamin B complex with C
Incompatible
Amphotericin B cholesteryl sulfate complex
Epinephrine HCl
Fenoldopam mesylate
Fluconazole
Hydralazine HCl
Lansoprazole
Midazolam HCl
Nicardipine HCl
Ondansetron HCl
Sargramostim
Verapamil HCl
Vinorelbine tartrate
Variable
Calcium gluconate
Diltiazem HCl
Hetastarch in sodium chloride 0.9%
Hydromorphone HCl
Vancomycin HCl

Actions and Spectrum

• Based on spectrum of activity, classified as an aminopenicillin.8, 9 Aminopenicillins have

enhanced activity against gram-negative bacteria compared with natural and penicillinase-
resistant penicillins.8, 9
• Usually bactericidal.1, 2
• Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall
synthesis.1, 2
• Spectrum of activity includes many gram-positive and -negative aerobes and some anaerobes.1, 9,
12

• Gram-positive aerobes: active in vitro and in clinical infections against Staphylococcus (β-
lactamase-negative strains only), Streptococcus pneumoniae, other Streptococcus (α- and β-
hemolytic strains only), and Enterococcus faecalis.1, 9, 12 Also active against Corynebacteriun
and Listeria monocytogenes.1, 9, 12
• Gram-negative aerobes: active in vitro and in clinical infections against H. influenzae, N.
gonorrhoeae, E. coli, Proteus mirabilis, Salmonella, and Shigella.1, 9, 12 Also active in vitro
against Bordetella pertussis, Eikenella corrodens, and Neisseria meningitidis.9 Inactive against
Citrobacter, Enterobacter, Klebsiella, Providencia, and Serratia.9, 12
• Gram-positive and gram-negative bacteria that produce β-lactamases, including β-lactamase-
producing S. aureus and E. faecalis, are resistant.9, 12
• Complete cross-resistance generally occurs between ampicillin and amoxicillin.

Advice to Patients

• Advise patients that antibacterials (including ampicillin) should only be used to treat bacterial
infections and not used to treat viral infections (e.g., the common cold).
• Importance of completing the entire prescribed course of treatment, even if feeling better after a
few days.
• Advise patients that skipping doses or not completing the full course of therapy may decrease
effectiveness and increase the likelihood that bacteria will develop resistance and will not be
treatable with ampicillin or other antibacterials in the future.
• Importance of taking oral ampicillin with a full glass of water 1 hour before or 2 hours after a
meal.1
• Importance of discontinuing therapy and informing clinician if an allergic reaction occurs.1
• Importance of informing clinician of existing or contemplated concomitant therapy, including
prescription and OTC drugs.1
• Importance of women informing clinicians if they are or plan to become pregnant or plan to
breast-feed.1
• Importance of advising patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in
some individuals; consult specific product labeling for details.

Ampicillin (Trihydrate)
Routes Dosage Forms Strengths Brand Names Manufacturer
Oral Capsules 250 mg (of ampicillin)* Principen® Sandoz
500 mg (of ampicillin)* Principen® Sandoz
For suspension 125 mg (of ampicillin) per 5 mL* Principen® Sandoz
250 mg (of ampicillin) per 5 mL* Principen® Sandoz
* available from one or more manufacturer, distributor, and/or repackager by generic
(nonproprietary) name

Ampicillin Sodium
Routes Dosage Forms Strengths Brand Names Manufacturer
Ampicillin Sodium for
Parenteral For injection 125 mg (of ampicillin) Sandoz
Injection
Ampicillin Sodium for
250 mg (of ampicillin) Sandoz
Injection
 Ampicillin Sodium for
500 mg (of ampicillin) Sandoz
Injection
Ampicillin Sodium for
1 g (of ampicillin) Sandoz
Injection
Ampicillin Sodium for
2 g (of ampicillin) Sandoz
Injection
10 g (of ampicillin) Ampicillin Sodium for
Sandoz
pharmacy bulk package Injection
For injection, for Ampicillin Sodium
1 g (of ampicillin) Sandoz
IV infusion ADD-Vantage®
Ampicillin Sodium
2 g (of ampicillin) Sandoz
ADD-Vantage®

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing
information was updated 03/2011. For the most current and up-to-date pricing information,
please visit www.drugstore.com. Actual costs to patients will vary depending on the use of
specific retail or mail-order locations and health insurance copays.

Ampicillin 250MG Capsules (SANDOZ): 30/$12.99 or 90/$17.97

Ampicillin 500MG Capsules (SANDOZ): 100/$44.98 or 200/$86.64

Use is not currently included in the labeling approved by the US Food and Drug
Administration.

References

1. Apothecon. Principen® (ampicillin) capsules and powder for oral suspension prescribing
information. Princeton, NJ; 1997 Mar.

2. Apothecon. Sterile ampicillin sodium, USP for intramuscular or intravenous injection prescribing
information. Princeton, NJ; 1996 May.

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of
Health-System Pharmacists; 2007:141-58.

4. Anon. The choice of antibacterial drugs. Med Lett Drugs Ther. 2001; 43:69-78. [PubMed
11518876]

5. Committee on Infectious Diseases, American Academy of Pediatrics. Red book: 2000 report of
the Committee on Infectious Diseases. 25th ed. Elk Grove Village, IL: American Academy of
Pediatrics; 2000.
6. Wilson WR, Karchmer AW, Dajani AS et al and the Committee on Rheumatic Fever et al.
Antibiotic treatment of adults with infective endocarditis due to streptococci, enterococci,
staphylococci, and HACEK microorganisms. JAMA. 1995; 274:1706-13. [IDIS 356429]
[PubMed 7474277]

7. Ferrieri P, Gewitz MH, Gerber MA et al and the Committee on Rheumatic Fever et al. Unique
features of infective endocarditis in childhood. Circulation. 2002; 105:2115-27. [IDIS 481470]
[PubMed 11980694]

8. Chambers HF. Penicillins. In: Mandell GL, Bennett JE, Dolin R, eds. Mandell, Douglas, and
Bennett's principles and practice of infectious diseases. 5th ed. New York: Churchill
Livingstone; 2000: 261-74.

9. Kucers A, Crowe S, Grayson ML et al, eds. The use of antibiotics. A clinical review of
antibacterial, antifungal, and antiviral drugs. 5th ed. Jordan Hill, Oxford: Butterworth-
Heinemann; 1997: 108-33,209-19.

10. Dajani AS, Taubert KA, Wilson W et al. Prevention of bacterial endocarditis: recommendations
by the American Heart Association. JAMA. 1997; 277:1794-801. [IDIS 385878] [PubMed
9178793]

11. Centers for Disease Control and Prevention. Sexually transmitted diseases treatment guidelines
2002. MMWR Morb Mortal Wkly Rep. 2002; 51(No. RR-6):1-78. [Fulltext MMWR]

12. AHFS Drug Information 2004. McEvoy GK, ed. Aminopenicillins General Statement.
Bethesda, MD: American Society of Health-System Pharmacists; 2004:293-308.