Pronunciation:

(am pi SIL in)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Use - Dental:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

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

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

Overdosage/Toxicology:

Drug Interactions:

Allopurinol: Theoretically has an additive potential for ampicillin/amoxicillin rash

Aminoglycosides: May be synergistic against selected organisms

Methotrexate: Penicillins may increase the exposure to methotrexate during concurrent therapy; monitor.

Oral contraceptives: Anecdotal reports suggesting decreased contraceptive efficacy with penicillins have been refuted by more rigorous scientific and clinical data.

Probenecid, disulfiram: May increase levels of penicillins (ampicillin)

Warfarin: Effects of warfarin may be increased

Ethanol/Nutrition/Herb Interactions:

Stability:

Oral: Oral suspension is stable for 7 days at room temperature or for 14 days under refrigeration.

I.V.:

Minimum volume: Concentration should not exceed 30 mg/mL due to concentration-dependent stability restrictions.

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) is 8 hours.

Stability of parenteral admixture in NS at refrigeration temperature (4°C) is 2 days.

Standard diluent: 500 mg/50 mL NS; 1 g/50 mL NS; 2 g/100 mL NS

Compatibility:

Y-site administration: Compatible: Acyclovir, amifostine, aztreonam, clarithromycin, cyclophosphamide, docetaxel, doxorubicin liposome, enalaprilat, esmolol, etoposide, famotidine, filgrastim, fludarabine, foscarnet, gatifloxacin, gemcitabine, granisetron, heparin, heparin with hydrocortisone sodium succinate, insulin (regular), labetalol, levofloxacin, linezolid, magnesium sulfate, melphalan, meperidine, morphine, multivitamins, ofloxacin, perphenazine, phytonadione, potassium chloride, propofol, remifentanil, tacrolimus, teniposide, theophylline, thiotepa, tolazoline, vitamin B complex with C. Incompatible: Amphotericin B cholesteryl sulfate complex, epinephrine, fluconazole, hydralazine, midazolam, ondansetron, sargramostim, verapamil, vinorelbine. Variable (consult detailed reference): Calcium gluconate, cisatracurium, diltiazem, hetastarch, hydromorphone, vancomycin

Compatibility in syringe: Compatible: Chloramphenicol, colistimethate, diatrizoate meglumine 52%, diatrizoate sodium 8%, diatrizoate sodium 60%, heparin, iohexol, iopamidol, iothalamate meglumine 60%, ioxaglate meglumine 39.3%, ioxaglate 19.6%, procaine. Incompatible: Erythromycin lactobionate, gentamicin, hydromorphone, kanamycin, lincomycin, metoclopramide. Variable (consult detailed reference): Lidocaine, polymyxin B sulfate, streptomycin

Compatibility when admixed: Compatible: Clindamycin, erythromycin lactobionate, floxacillin, furosemide. Incompatible: Amikacin, chlorpromazine, dopamine, gentamicin, hydralazine, prochlorperazine. Variable (consult detailed reference): Aztreonam, cefepime, cimetidine, heparin, hydrocortisone sodium succinate, metronidazole, metronidazole with sodium bicarbonate, ranitidine, sodium bicarbonate, verapamil

Mechanism of Action:

Pharmacodynamics/Kinetics:

Absorption: Oral: 50%

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

Time to peak: Oral: Within 1-2 hours

Excretion: Urine (~90% as unchanged drug) within 24 hours

Dosage:

Infants and Children:

Mild-to-moderate infections:

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

Oral: 50-100 mg/kg/day in doses divided every 6 hours (maximum: 2-4 g/day)

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

Endocarditis prophylaxis: I.M., I.V.:

Dental, oral, respiratory tract, or esophageal procedures: 50 mg/kg within 30 minutes prior to procedure in patients unable to take oral amoxicillin

Genitourinary and gastrointestinal tract (except esophageal) 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.

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

Adults:

Susceptible infections:

Oral: 250-500 mg every 6 hours

I.M., I.V.: 250-500 mg every 6 hours

Sepsis/meningitis: I.M., I.V.: 150-250 mg/kg/24 hours divided every 3-4 hours (range: 6-12 g/day)

Endocarditis prophylaxis: I.M., I.V.:

Dental, oral, respiratory tract, or esophageal procedures: 2 g within 30 minutes prior to procedure in patients unable to take oral amoxicillin

Genitourinary and gastrointestinal tract (except esophageal) procedures:

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

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

Dosing interval in 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

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 effects: Dose as for Clcr 10-50 mL/minute; ~50 mg of ampicillin per liter of filtrate is removed

Administration:

Oral: Administer on an empty stomach (ie, 1 hour prior to, or 2 hours after meals) to increase total absorption.

I.V.: Administer over 3-5 minutes (125-500 mg) or over 10-15 minutes (1-2 g). More rapid infusion may cause seizures. Ampicillin and gentamicin should not be mixed in the same I.V. tubing or administered concurrently.

Monitoring Parameters:

Test Interactions:

Dietary Considerations:

Sodium content of 5 mL suspension (250 mg/5 mL): 10 mg (0.4 mEq)

Sodium content of 1 g: 66.7 mg (3 mEq)

Patient Education:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Capsule (Principen®): 250 mg, 500 mg

Injection, powder for reconstitution, as sodium: 125 mg, 250 mg, 500 mg, 1 g, 2 g, 10 g

Powder for oral suspension (Principen®): 125 mg/5 mL (100 mL, 200 mL); 250 mg/5 mL (100 mL, 200 mL)

International Brand Names: