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ampicillin (Principen, Omnipen, Amcill, Polycillin, Polycillin-N, D-cillin, J-cillin, Marcillin, Rancillin Totacillin-N)
Tradenames: Principen, Omnipen. 3rd generation penicillin.
Indications:
1) infections caused by susceptible gram positive bacteria & gram negative bacteria, including
- intra-abdominal infection
- gastrointestinal infection
- gastroenteritis, enterocolitis
- cholangitis
- acute otitis media,
- endocarditis
- upper respiratory tract infection
- acute sinusitis
- pharyngitis
- epiglottitis
- lower respiratory tract infection
- pneumonia
- urogenital infections
- skin or soft tissue infections
2) treatment of choice (generally in combination with gentamicin) for treatment of serious enterococcal infections
3) treatment of meningitis caused by Listeria monocytogenes
4) empiric treatment of fever of unknown origin [6]
5) prophylaxis for bacterial endocarditis [6]
6) prophylaxis for perioperative infection, including
- gastrointestinal surgery
- hysterectomy
- cesarean section [6]
7) bacterial infections associated with necrosis [6]
Dosage:
- 1-2 g IV/IM every 4-6 hours.
- 250-500 mg PO QID.
Pediatrics: 50-200 mg/kg/day divided QID.
Tabs: 250 & 500 mg.
Elixir: 125 & 250 mg/5 mL.
Dosage adjustment in renal failure:
creatinine clearance dose
> 30 mL/min 1-2 g every 4-6 hours
10-30 mL/min 1-2 g every 6 hours
< 10 mL/min* 1-2 g every 8 hours
* dose after hemodialysis
Pharmacokinetics:
1) CSF levels are 11-65% of serum levels with meningeal inflammation
2) elimination 1/2life 1 hour (7-20 hours ESRD)
Antimicrobial activity:
Gram positive:
- Streptococcus sp
- Enterococcus sp
- Listeria
Gram negative:
- Neisseria meningitidis
- Salmonella
- Shigella
- Proteus
- Campylobacter fetus [6]
- Haemophilus
- Haemophilus influenzae
- Haemophilus parainfluenzae
- Yersinia pseudotuberculosis
- Escherichia coli [6]
Anaerobes:
- Peptostreptococcus
- Clostridium species
Adverse effects:
1) common (> 10%)
a) rash
- distingush non-allergic rash from hypersensitivity reaction
- incidence higher in patients with viral infections (CMV, EBV)* Salmonella, lymphocytic leukemia (ALL)*, hyperuricemia, diarrhea, vomiting, oral candidiasis
- duration of rash is independent of whether ampicillin is discontinued or not [5]
- no risk of allergic reaction on re-exposure to ampicillin after underlying condition has resolved
b) urticarial rash in infectious mononucleosis
2) less common (1-10%)
a) severe abdominal or stomach cramps
b) diarrhea
3) uncommon (< 1%)
a) blood dyscrasias (rare)
b) seizures (rare)
* maculopapular rash assoicated with use of intravenous ampicillin in patients with CMV, EBV, or ALL is not a drug allergy & the duration of the rash is independent of whether or not ampicillin is continued [5]
Drug interactions:
1) coadministration of allopurinol increases the frequency of rash
2) ampicillin decreases atenolol absorption
3) probenecid increases 1/2life of ampicillin
Mechanism of action: inhibition of bacterial cell wall synthesis
Interactions
drug interactions
Related
Enterococcus
Listeria
General
3rd generation penicillin (aminopenicillin)
Properties
MISC-INFO: elimination route KIDNEY
1/2life 1-2 HOURS
elimination by hemodialysis +
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Harrison's Principles of Internal Medicine, 13th ed.
Companion Handbook. Isselbacher et al (eds),
McGraw-Hill Inc. NY, 1995, pg 161
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Medical Knowledge Self Assessment Program (MKSAP) 14,
American College of Physicians, Philadelphia 2006
- Medical Knowledge Self Assessment Program (MKSAP) 19
Board Basics. An Enhancement to MKSAP19.
American College of Physicians, Philadelphia 2022
- Deprecated Reference
Component-of
ampicillin sulbactam (Unasyn)