Ampicillin

Pronunciation

(am pi SIL in)

U.S. Brand Names

Principen®

Synonyms

Aminobenzylpenicillin; Ampicillin Sodium; Ampicillin Trihydrate

Generic Available

Yes

Canadian Brand Names

Apo-Ampi®; Novo-Ampicillin; Nu-Ampi

Use

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

Use - Dental

I.V. or I.M. administration for the prevention of bacterial endocarditis in patients unable to take oral amoxicillin

Pregnancy Risk Factor

Pregnancy Implications

Teratogenic effects were not observed in animal studies. Ampicillin crosses the human placenta.

Lactation

Enters breast milk/use caution

Contraindications

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

Warnings/Precautions

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.

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

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

Symptoms of penicillin overdose include neuromuscular hypersensitivity (eg, agitation, hallucinations, asterixis, encephalopathy, confusion, and seizures). Electrolyte imbalance may occur if the preparation contains potassium or sodium salts, especially in renal failure. Hemodialysis may be helpful to aid in removal of the drug from blood; otherwise, treatment is supportive or symptom-directed.

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

Food: Food decreases ampicillin absorption rate; may decrease ampicillin serum concentration.

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

Incompatible in D5W, D5NS, D10W, fat emulsion 10%, hetastarch 6%, LR; variable compatibility (consult detailed reference) in NS

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

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

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

Administer around-the-clock to promote less variation in peak and trough serum levels.

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

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

Test Interactions

May interfere with urinary glucose tests using cupric sulfate (Benedict's solution, Clinitest®); may inactivate aminoglycosides in vitro

Dietary Considerations

Take on an empty stomach 1 hour before or 2 hours after meals.

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

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. 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. If you have diabetes, drug may cause false test results with Clinitest® urine glucose monitoring; use of another type of glucose monitoring is preferable. May cause nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or diarrhea (buttermilk, boiled milk, or yogurt may help). Report immediately any rash; swelling of face, tongue, mouth, or throat; or chest tightness. Report if condition being treated worsens or does not improve by the time prescription is completed.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Oral candidiasis.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

Large I.V. doses may rarely produce encephalopathy; penicillins have been reported to cause apprehension, illusions, agitation, insomnia, depersonalization, and encephalopathy

Mental Health: Effects on Psychiatric Treatment

Rarely may cause bone marrow suppression; use caution with clozapine and carbamazepine

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)

References

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.

International Brand Names

Acmecilin® (BD); Acupillin® (ZA); Alfasalin Enjektabl® (TR); Alfasilin Enjektabl® [inj.] (TR); Alfasilin Kapsül® (TR); Alfasilin Oral Suspansiyon® (TR); Alfasilin Tablet® (TR); Alphacin® (AU); Alpovex® (AR); Ambezetal® (BR); Amblosin® (BD); Amcillin® (ID, TH); Amfipen® (IE); Amilin® (TH); Amipenix® [caps.] (JP); Ampecu® (EC); Ampexin® (BD); Ampi® (BE, ID); Ampibex® (EC); Ampi-bis® (AR); Ampi-bis® [inj.] (AR); Ampicher® (EC); Ampicil® (BR); Ampicilina® (AR, BR, CL, EC, RO); Ampicilina Biocrom® (AR); Ampicilina Biocrom® [inj.] (AR); Ampicilina CBA® (AR); Ampicilina CBA® [inj.] (AR); Ampicilina Drawer® (AR); Ampicilina Etyc® (CO); Ampicilina Fada® (AR); Ampicilina Fecofar® (AR); Ampicilina Forte® (RO); Ampicilina Genfar® (EC); Ampicilina Ges® (ES); Ampicilina Ingram® (AR); Ampicilina Ingram® [inj.] (AR); Ampicilina L.CH.® (CL); Ampicilina Llorente® (ES); Ampicilina Medipharma® (AR); Ampicilina MK® (CO, CR, DO, GT, HN, PA, SV); Ampicilina MK® [inj.] (CO); Ampicilina Richet® (AR); Ampicilina Richet® [inj.] (AR); Ampicilina Rigo® (AR); Ampicilina Rigo® [inj.] (AR); Ampicilina Sintesina® (AR); Ampicilina Sintesina® [inj.] (AR); Ampicilina Trihidrat® (RO); Ampicilin® (HR, SI, YU); Ampicillina Biopharma® (IT); Ampicillina® (IT); Ampicillina Sodica® (IT); Ampicillin® (BG, CZ, GB, HU, ID, IL, PL, RO, RU); Ampicilline-Eurogenerics® (LU); Ampicilline® (RO); Ampicillin-Fresenius Vials® (ZA); Ampicillin-ratiopharm® (DE); Ampicillin Stada® (DE); Ampicillin Vana® (AT); Ampicillin Vepidan® (DK); Ampicin® (BD); Ampicler® (AR); Ampicyn® (AU, TH); Ampidar® (HK, JO, KW, LB, MT, MY, RO); Ampifar® (BR); Ampifarma® (DO); Ampigen Simple® (AR); Ampi GNO® (AR); Ampigrand® (AR); Ampigrand® [inj.] (AR); Ampilan® (EC); Ampil® (EC); Ampilin® (HK, IN, SG, TH); Ampilisa® [inj.] (IT); Ampilisa® (IT); Ampillin® (TH); Ampilux® (IT); Ampimax® (ZA); Ampipen® (IN, ZA); Ampiplus® (ES); Ampiplus Simplex® (CY, EG, IT, JO, KW, LB, MA, MT, SY); Ampirex® (BD); Ampisina® (BD, RO, TR); Ampisina® [inj.] (TR); Ampitenk® (AR); Ampitenk® [inj.] (AR); Ampitotal® (BR); Ampitrex® (DO); Ampixen® (AR); Amplacilina® (BR); Amplacilina® [inj.] (BR); Amplital® [inj.] (IT); Amplital® (IT); Amplitor® (BR); Amplivacil® (RO); Amplizer® (IT); Amplofen® (BR); Amplotal® (BR); Ampra MH® (TH); Amprexyl® (TH); Amprialen® (AR); Amprialen® [inj.] (AR); Ampro® (TH); Amsapen® (MX); Anglopen® (MX); Antibiopen® [caps./liqu.oral] (ES); Antibiopen® [inj.] (ES); A-Pen® (FI); Apo-Ampi® (CA, CZ); Arcocillin® [caps.] (ID); Austrapen® [caps./liqu.oral] (AU); Austrapen® [inj.] (AU); Avlocillin® (BD); Bacterinil® (BR); Bactilina® (AR); Bactosone® (ES); Be-Ampicil® (ZA); Benzotal® (BR); Binotal® (BR, CO, DE, EC, ID, MX); Biocilin® (IN); Biopenam® (ID); Biopensyn® (ID); Bipencil® (BR); Bremcillin® (ID); Britapen® (ES); Britapen® [inj.] (ES); Brodacillin® (ID); Campicilin® (IN); Cetacillin® (ID); Champicin® (BD); Clonamp® (IE); Copharcilin® (CH); Corsacillin® (ID); Dancillin® (ID); Decilina® (AR); Deripen® (EC); Dhacillin® (HK, SG); Dibacilina® (MX); Doktacillin® (DK, SE); Duplocin® (BD); Durapen® (BR); Ephicilin® (RO); Epicocillin® (RO); Eracillin® (TH); Exactum® (EC); Ficillin® (BD); Flamicina® [inj.] (MX); Flamicina® [tabs] (MX); Fortapen® (BE); Fortapen® [caps./liqu.oral] (BE); Fortapen® [inj.] (BE); G-Ampicillin® (BD); Gobemicina® (ES); Gobemicina® [inj.] (ES); Gobemicina retard® (ES); Gonocilin® (BR); Gramcilina® (BR); Grampenil® (AR); Grampenil® [inj.] (AR); H-Ambiotico® (CO); H.G. Ampicilin® (EC); Hiperbiotico® (PT); Histopen® (AR); Hostes simple® (AR); Huma-Ampicillin® (HU); Ibimicyn® (IT); Ikacillin® (ID); Ikapen® (IL); Julphapen® (EC); Kalpicin® (ID); Kamocillin® (BD); Kemocil® (ID); Kinabiot® (AR); Lampicin® (MX); Libracilina® (EC); Marovilina® (MX); Maxicilina INY® (ES); Medicillin® (BD); Navacillin® (BD); Navamox® (BD); Negopen® (TR); Novapen® (IE); Novencil® (EC); Novo-Ampicillin (CA, RO); Nu-Ampi (CA); Nuvapen® [inj.] (ES); Optacilin® (BR); Oracipen® (ID); Pamecil® (CY, HK, SG); Pamecil® [inj.] (RO); Parenzyme Ampicillina® (BR); Parpicillin® (ID); Pen-A® (BD); Penbiotic® (ID); Penbisin Injektabl® (TR); Penbritin® (BE, GB, HK, HR, ID, IE, KW, LU, MX, TH, ZA); Penbritin® [inj.] (BE, GB, ID, IE, KW); Pencotrex® (TH); Penglobe® (AT); Penibrin® [caps./liqu.oral] (IL); Penibrin® [inj.] (IL, RO); Penodil® (CY, HK); Penrite® (ZA); Penstabil® (CZ, HU); Pentrexyl® (BE, BG, CZ, DK, HU, IL, IT, LU, MX, NL, NO, RO, YU); Pentrexyl® [caps./liqu.oral] (BE, CN, HU, MX, TH); Petercillin Injection® (ZA); Petercillin® (ZA); Phapin® (ID); Poenbiotico® (AR); Polypen® (ID); Primacillin® (ID); Primapen® (ID); Probenzima® (BR); Ranamp® (ZA); Retarpen® (ES); Rimacillin® (GB); Rolab-Ampicillin® (ZA); Roscillin® (IN, RU); Rottacillin® (RO); Sanangin® (AR); Sanpicillin® (ID); Semicillin® (HU); Servicillin® [oral] (HK); Seskasilin Kapsül® (TR); Seskasilin Oral Süsp.® (TR); Siampicil® (TH); Silina® (TR); Sinaplin® [caps, syrup] (MX); Sinaplin® [inj.] (MX); Sinaplin® [tabs] (MX); Spectracil® (ZA); Standacillin® (CY, ID, JO, KW, LB, RO, RU, SG); Standacillin® [inj.] (AT, HU); Sumapen® (TH); Synthocilin® (IN); Synthocilin® [inj.] (IN); Tandrexin® (BR); Theracilline® (HK); Totapen® (FR); Totapen® [inj.] (FR); Trifacilina® (AR); Trimicro® (AR); Ultracillin® (BG, JO, KW, LB, MA, MY, SY); Ultrapen® (ID); Ultrapenil® (ES); Uniao Ampicilina® (BR); Urobiotic® (BR); Vacillin® (TH); Viccilin® (ID); Viccillin® (TH); Vidopen® (IE); Vidopen® [liqu.oral-sir.] (IE); Vitapen® (IL); Welticilina® (AR); Xepacillin® (ID); Xeracil® (ZA)

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