Ampicillin trihydrate is a semisynthetic penicillin derived from the basic penicillin nucleus, 6-aminopenicillanic acid. Ampicillin is designated chemically as (2S, 5R, 6R)-6-[(8)-2-Amino-2-phenylacetamido]-3,3-dimethyl-t-oxo-4-thia-1- azabicyclo[3.2.0] heptane-2-carboxylic acid. The chemical formula is C₁₆H₁₉N₃O₄S·3H₂O and its molecular weight is 403.45.

This is the anhydrous form of ampicillin. It is prepared as the trihydrate form attached to 3 water (H2O) molecules.

PRINCIPEN Capsules (Ampicillin Capsules USP) for oral administration provide ampicillin trihydrate equivalent to 250 mg and 500 mg ampicillin.

Inactive ingredients: black iron oxide, gelatin, FD&C Blue #1, FD&C Red #3, FD&C Red #40, lactose monohydrate, silica gel, and titanium dioxide.

PRINCIPEN for Oral Suspension (Ampicillin for oral suspension USP) provide, after constitution, ampicillin trihydrate equivalent to 125 mg and 250 mg ampicillin per 5 mL.

Inactive ingredients: antifoam AF emulsion, Atmos 300, colloidal silicon dioxide, FD&C Red #40, lecithin, natural and artificial flavors, sucrose, sodium citrate, sodium benzoate, and vanillin.

Last updated on RxList: 1/29/2005

PRINCIPEN Capsules (Ampicillin Capsules) and PRINCIPEN for Oral Suspension (Ampicillin for Oral Suspension) are indicated in the treatment of infections caused by susceptible strains of the designated organism listed below;

Infections of the Genitourinary Tract Including Gonorrhea: E. coli, P. mirabilis, enterococci, Shigella, S. typhosa and other Salmonella, and nonpenicillinase-producing N. gononhoeae.

Infections of the Respiratory Tract: Nonpenicillinase-producing H. influenzae and staphylococci, and streptococci including streptococcus pneumoniae.

Infections of the Gastrointestinal Tract: Shigella, S. typhosa and other Salmonella, E. coli, P. mirabilis, and enterococci.

Meningitis: O. Meningitides.

Bacteriology studies to determine the causative organisms and their sensetivity to ampicillin should be performed. Therapy may be instituted prior to the results of susceptibility testing.

Adults and Children Weight Over 20 kg.

For genitourinary or gastrointestinal tract infections other than gonorrhea in men and women, the usual dose is 500 mg qid in equally spaced doses; severe or chronic infections may require larger doses.

For the treatment of gonerrhea in both men and women, a single oral dose of 3.5 grams of ampicillin administered simultaneously with 1 gram of probenecid is recommended. Physicians are cautioned to use no less than the above recommended dosage for the treatment of gonorrhea. Follow-up cultures should be obtained from the original site(s) of infection 7 to 14 days after therapy. In women, it is also desirable to obtain culture test-of-cure from both the endo-cervical and anal canals. Prolonged intensive therapy is needed for complications such as proshtitis and epididymitis. For respiratory tract infections, the usual dose is 250 mg qid in equally spaced doses.

Children Weighing 20 kg or Less

For genitourinary or gastrointestinal tract infections, the usual dose is 100 mg/kg/day total, qid in equally divided and spaced doses. For respiratory infections, the usual dose is 50 mg/kg/day total, in equally divided and spaced doses three to four times daily. Doses for children should not exceed doses recommended for adults,

All Patients, Irrespective of Age and Weight

Larger doses may be required for severe or chronic infections. Although ampicillin is resistant to degradation by gastric acid, it should be administered at least one half-hour before or two hours after meals for maximal absorption. Except for the single dose regimen for gonorrhea referred to above, therapy should be continued for a minimum of 48 to 72 hours after the patient becomes asymptomatic or evidence at bacterial eradication has been obtained. In infections caused by hemolytic strains of streptococci, a minimum of 10 days treatment is recommended to guard against the risk of rheumatic fever of glomerulonephritis (see PRECAUTIONS — Laboratory Tests). In the treatment of chronic urinary or gastrointestinal infections, frequent bacteriologic and clinical appraisal is necessary during therapy and may be necessary for several months afterwards. Stubborn infections may require treatment for several weeks. Smaller doses than those indicated above should not be used.

PRINCIPEN Capsules (Ampicillin Capsules USP):

250 mg/capsule: Size 2 capsule with a light gray body and scarlet cap. Printed in black ink with BRISTOL 7902 on both body and cap.

bottles of 100 NDC 0003-0122-50
bottles of 500 NDC 0003-0122-60
Unimatic, unit dose packs of 100 NDC 0003-0122-51

500 mg/capsule: Size 0 capsule with a light gray body and scarlet cap. Printed in black ink with BRISTOL 7093 on both body and cap.

bottles of 100 NDC 0003-0134-50
bottles of 500 NDC 0003-0134-60
Unimatic, unit dose packs of 100 NDC 0003-0134-51

PRINCIPEN for Oral Suspension (Ampicillin for Oral Suspension USP):

Ampicilin 125: When constituted as directed on the container label, a pleasant fruit-flavored suspension containing: 125 mg per 6 mL, In bottle sizes for preparation of

100 mL NDC 0003-0969-09
150 mL NDC 0003-0969-52
200 mL NOC 0003-0969-61

Ampicilin 260: When constituted as directed on the container label, a pleasant fruit-flavored suspension containing: 250 mg per 5 mL, In bottle sizes for preparation of

100 mL NDC 0003-0972-52
200 mL NDC 0003-0972-61

Storage

Capsules: Store at room temperature; avoid excessive heat; keep tightly closed.

Ampicilin for oral suspension: Store at room temperature; after constitution, discard unused portion after 7 days if kept at room temperature or after 14 days if refrigerated; keep bottles tightly closed.

For Rx only

Last updated on RxList: 1/29/2005

As with other penicillins, it may be expected that untoward reactions will be essentially limited to sensitivity phenomena. They are more likely to occur in individuals who have previously demonstrated hypersensitivity to penicillin and in those with a history of allergy, asthma, hay fever, or urticaria.

The following adverse reactions have been reported as associated with the use of ampicillin:

Gastrointestinal: glositis, stamatitis, nausea, vomiting, enterocolitis, pseudomembranous colitis, and diarrhea. These reactions are usually associated with oral dosage forms of the drugs.

Hypersensitivity Reactions: An erythematous, mildly pruritic, maculopapular skin rash has been reported fairly frequently. The rash, which usually does not develop within the first week of therapy, may cover the entire body including the soles, palms, and oral mucosa. The eruption usually disappears in three to seven days.

Other hypersensitivity reactions that have been reported are: skin rash, pruritus, urticaria, erythema multiforme, and an occasional case of exfoliative dermatitis. Anaphylaxis is the most serious reaction experienced and has usually been associated with the parenteral dosage form of the drug

Note: Urticaria, other skin rashes, and serum sickness-like reactions may be controlled by antihistamines, and if necessary, systemic corticosteroids. Whenever such reactions occur, ampicillin should be discontinued unless, in the opinion of the physician, the condition being treated is life-threatening, and amenable only to ampicillin therapy. Serious anaphylactoid reactions require emergency measures (see WARNINGS).

Liver: Moderate elevation in serum glutamic oxalaacetic transaminase (SGOT) has been noted, but the significance of this finding is unknown.

Hemic and Lymphatic Systems: Anemia, thrombocytopenia, thrombocytopenic purpura, eosinophilia, leukapenia, and agranulacytosis have been reported during therapy with penicillins. These reactions are usually reversible on discontinuation of therapy and are believed to be hypersensitivity phenomena.

Other: Other adverse reactions that have been reported with the use at ampicillin are laryngeal stride and high fever. An occasional patient may complain of sore mouth or tongue as with any oral penicillin preparation.

When administered concurrently, the following drugs may interact with ampicillin.

Allopurinol: Increased possibility of skin rash, particularly in hyperuricemic patients may occur.

Bacteriostatic Antibiotics: Chloramphenicol, erythromycins, sulfonamides, or tetracyclines may interfere with the bactericidal effect of penicillins. This has been demonstrated in view, however, the clinical significance of this interaction is not well documented.

Oral Contraceptives: May be less effective and increased breakthrough bleeding may occur.

Probenecid: May decrease renal tubular secretion of ampicillin resulting in increased blood levels and/or ampicillin toxicity.

Drug/Laboratory Test Interaction

After treatment with ampicillin, a false-positive reaction for glucose in the urine may occur with copper sulfate tests (Benedict's solution, Fehling's solution, or Clinitest tablets) but not with enzyme based tests such as Clinistix and Glucose Enzymatic Test Strip USP.

Last updated on RxList: 1/29/2005

Serious and occasional fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy. Although anaphylaxis is more frequent following parenteral administration, it has occurred in patients on oral penicillins. These reactions are more apt to occur in individuals with a history at penicillin hypersensitivity and/or a history of sensitivity to multiple allergens. There have been well documented reports of individuals with a history of penicillin hypersensitivity who have experienced severe hypersensitivity reactions when treated with cephalosporins. Before initiating therapy with any penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, and other allergens. If an allergic reaction occurs, the drug should be discontinued and appropriate therapy instituted. Serious anaphylactoid reactions require immediate emergency treatment with epinephrine. Oxygen, intravenous steroids, and airway management, including intubation, should also be administered as indicated.

Pseudomembranous colitis has been reported with nearly all antibacterial agents, including ampicillin, and may range in severity from mild to life-threatening. Therefore, it is important to consider this diagnosis in patients who present with diarrhea subsequent to the administration of antibacterial agents. Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of clostridia. Studies indicate that a toxin produced by clostridium difficile, is one primary cause of "antibiotic-associated colitis". After the diagnosis of pseudomembranous colitis has bean established, therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation and treatment with an antibacterial drug clinically effective against C. difficile colitis.

General

Prolonged use of antibiotics may promote the overgrowth of nonsusceptible organisms, including fungi. Should superinfection occur, appropriate measures should be taken. Patients with gonorrhea who also have syphilis should be given additional appropriate parenteral penicillin treatment. Treatment with ampicillin does not preclude the need for surgical procedures, particularly in staphylococcal infections.

Laboratory Tests

In prolonged therapy, and particularly with high dosage regimens, periodic evaluation of the renal, hepatic, and hematopoietic systems is recommended.

In streptococcal infections, therapy must be sufficient to eliminate the organism (10 days minimum); otherwise the sequelae of streptococcal disease may occur. Cultures should be taken following completion of treatment to determine whether streptococci have been eradicated.

Cases of gonococcal infection with a suspected lesion of syphilis should have darkfield examinations ruling out syphilis before receiving ampicillin. Patients who do not have suspected lesions of syphilis and are treated with ampicillin should have a follow- up serologic test for syphilis each month for four months to detect syphilis that may have been masked from treatment for gonorrhea.

Drug Interactions

See DRUG INTERACTIONS section.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term studies in animals have not been performed to evaluate carcinogenesis, mutagenesis, or impairment of fertility in males or females.

Pregnancy

Teratogenic Eftects: Category B: Reproduction studies in animals have revealed no evidence of impaired fertility or harm to the fetus due to penicillin. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, penicillin should be used during pregnancy only if clearly needed.

Labor and Delivery

Oral ampicillin-class antibiotics are poorly absorbed during labor. Studies in guinea pigs showed that intravenous administration of ampicillin slightly decreased the uterine tone and frequency of contractians, but moderately increased the height and duration of contractions. However, it is not known whether use of these drugs in humans during labor or delivery has immediate or delayed adverse effects on the fetus, prolongs the duration of labor, or increases the likelihood that forceps delivery or other obstetrical intervention or resuscitation of the newborn will be necessary.

Nursing Mothers

Ampicillin-class antibiotics are excreted in milk. Ampicillin used by nursing mothers may lead to sensitization of infants; therefore, a decision should be made whether to discontinue nursing or to discontinue ampicillin, taking into account the importance of the drug to the mother.

Pediatric Use

Penicillins are excreted primarily unchanged by the kidney, therefore, the incompletely developed renal functioning neonates and young infants will delay the excretion of penicillin. Administration to neonates and young infants should be limited to the lowest dosage compatible with an effective therapeutic regimen (see DOSAGE AND ADMINISTRATION).

Last updated on RxList: 1/29/2005

In case of overdosage, discontinue medication, treat symptomatically and institute supportive measures as required. In patients with renal function impairment, ampicillin-class antibiotics can be removed by hemodialysis but not by peritoneal dialysis.

A history of a previous hypersensitivity reaction to any of the penicillins is a contraindication. Ampicillin is also contraindicated in infections caused by penicillinase-producing organisms.

Last updated on RxList: 1/29/2005

Ampicillin is bactericidal at low concentrations and is clinically effective not only against the gram-positive organisms usually susceptible to penicillin G but also against a variety of gram-negative organisms. It is stable in the presence of gastric acid and is well absorbed from the gastrointestinal tract. It diffuses readily into most body tissues and fluids; however, penetration into the cerebrospinal fluid and brain occurs only with meningeal inflammation. Ampicillin is excreted largely unchanged in the urine; its excretion can be delayed by concurrent administration of probenecid which inhibits the renal tubular secretion of ampicillin. In blood serum, ampicillin is the least bound of all the penicillins; an average of about 20 percent of the drug is bound to plasma proteins as compared to 60 to 90 percent of the other penicillins. The administration of 500 mg dose of ampicillin capsules results in an average peak blood serum level of approximately 3.0 mcg/mL; the average peak serum level for the same dose of ampicillin for oral suspension is approximately 3.4 mcg/mL.

Microbiology

While in vitro studies have demonstrated the susceptibility of most strains of the following organisms, clinical efficacy for infections other than those included in the INDICATIONS AND USAGE section has not been documented.

Gram-Positive: strains of alpha- and beta-hemolytic streptococci, Streptococcus pneumoniae, those strains of staphylococci, which do not produce penicillinase, Clostridium sp., Bacillus anthracis, Corynebacterium xeroses, and most strains of enteracocci.

Gram-Negative: Hemophilus influenzae; Neisseria gonorrhoae and N. Meningitides; Proteus mirabilis, and many strains of Salmonella (including S. typhosa), Shigella, and Escherichia coli.

Note: Ampicillin is inactivated by penicillinase and therefore is ineffective against penicillinase-producing organisms including certain strains at staphylococci, Pseudomonas aeruginosa, P. Vulgaris, Klebsiella pneumoniae, Enterobacter aerogenes, and some strains of E. coli. Ampicillin is not active against Rickettsia, Mycoplasma, and "large viruses" (Miyagawanella).

Testing for Susceptibility: The invading organism should be cultured and its susceptibility demonstrated as a guide to therapy. If the Kirby-Bauer method of disc susceptibility is used, a 10 mcg ampicillin disc should be used to determine the relative in vitro susceptibility.

Last updated on RxList: 1/29/2005

1. The patient should inform the physician of any history of sensitivity to allergens, including previous hypersensitivity reactions to penicillins and cephalosporins (see WARNINGS).

2. The patient should discontinue ampicillin and contact the physician immediately if any side effect occurs (see WARNINGS).

3. Ampicillin should be taken with a full glass (8 oz) of water, one-half hour before or two hours after meals.

4. Diabetic patients should consult with the physician before changing diet or dosage of diabetes medication (see PRECAUTIONS — Drug/Laboratory Test Interactions).

Last updated on RxList: 1/29/2005

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

AMPICILLIN - ORAL

(AM-pi-SIL-in)

COMMON BRAND NAME(S): Principen

USES: Ampicillin is used to treat a wide variety of bacterial infections. It is a penicillin-type antibiotic. It works by stopping the growth of bacteria.

This antibiotic treats only bacterial infections. It will not work for viral infections (e.g., common cold, flu). Unnecessary use or overuse of any antibiotic can lead to its decreased effectiveness.

HOW TO USE: Take this medication by mouth usually 4 times a day (every 6 hours), or as directed by your doctor. Take ampicillin on an empty stomach (1 hour before or 2 hours after a meal) with a full glass of water. Drink plenty of fluids while using this medication unless your doctor tells you otherwise.

The dosage is based on your medical condition and response to therapy.

Antibiotics work best when the amount of medicine in your body is kept at a constant level. Therefore, take this drug at evenly spaced intervals.

Continue to take this medication until the full-prescribed amount is finished even if symptoms disappear after a few days. Stopping the medication too early may allow bacteria to continue to grow, which may result in a relapse of the infection.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: Nausea, vomiting, diarrhea, or mouth/tongue sores may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these rare but very serious side effects occur: dark urine, persistent nausea or vomiting, stomach/abdominal pain, yellowing eyes or skin, easy bruising or bleeding, persistent sore throat or fever.

This medication may rarely cause a severe intestinal condition (pseudomembranous colitis) due to a type of resistant bacteria. This condition may occur during treatment or weeks to months after treatment has stopped. Do not use anti-diarrhea products or narcotic pain medications if you have any of the following symptoms because these products may make them worse. Tell your doctor immediately if you develop: persistent diarrhea, abdominal or stomach pain/cramping, blood/mucus in your stool.

Use of this medication for prolonged or repeated periods may result in oral thrush or a new vaginal yeast infection (oral or vaginal fungal infection). Contact your doctor if you notice white patches in your mouth, a change in vaginal discharge or other new symptoms.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

Ampicillin can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Therefore, seek immediate medical attention if you develop any rash.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking ampicillin, tell your doctor or pharmacist if you are allergic to it; or to penicillin or cephalosporin antibiotics; or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, a certain type of viral infection (infectious mononucleosis).

Kidney function declines as you grow older. This medication is removed by the kidneys. Therefore, elderly people may be more sensitive to this drug.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

Ampicillin passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: allopurinol, live bacterial vaccines, methotrexate, tetracyclines.

Before taking ampicillin, tell your doctor or pharmacist if you are also taking probenecid. Probenecid slows down the removal of ampicillin from your body, resulting in higher levels of this antibiotic in your bloodstream. For certain types of difficult-to-treat infections, your doctor may prescribe these 2 medications together in order to achieve this effect. Consult your doctor or pharmacist for more details.

This medication may decrease the effectiveness of combination-type birth control pills. This can result in pregnancy. You may need to use an additional form of reliable birth control while using this medication. Consult your doctor or pharmacist for details.

Ampicillin may cause false positive results with certain diabetic urine testing products (cupric sulfate-type). This drug may also affect the results of certain lab tests. Make sure laboratory personnel and your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose may include: severe vomiting, persistent diarrhea, unusual change in the amount of urine, or seizures.

NOTES: Do not share this medication with others.

This medication has been prescribed for your current condition only. Do not use it later for another infection unless told to do so by your doctor. A different medication may be necessary in those cases.

With prolonged treatment, laboratory and/or medical tests (e.g., kidney and liver function, complete blood counts) should be performed periodically to monitor your progress or check for side effects. Consult the doctor for more details.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C), away from excessive heat and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.