Ampicillin

Ampicillin capsules and powder for oral suspension should be stored in tight containers @ 15-30 °C. Following reconstitution, oral suspensions of either anhydrous ampicillin or ampicillin trihydrate should preferable be refrigerated @ 2-8 °C but are stable for 7 days @ room temperature or 14 days @ 2-8 °C.

Following reconstitution with sterile or bacteriostatic water for injection, ampicillin sodium solutions for IM or direct IV injection should be used within 1 hr after reconstitution and should not be frozen.

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

...AMPICILLIN...MIXED IN VITRO WITH GENTAMICIN.../FOR PROLONGED PERIODS/ CAUSE LOSS OF GENTAMICIN ANTIMICROBIAL ACTIVITY.

CONCURRENT ADMIN OF PENICILLIN & PROBENECID RESULTS IN HIGHER & MORE SUSTAINED SERUM ANTIBIOTIC LEVELS. /AMPICILLIN HAS BEEN SHOWN TO INTERACT IN SIMILAR MANNER/.

/GENTAMICIN/ RELATED DRUGS...KANAMYCIN, NEOMYCIN & TOBRAMYCIN MAY INTERACT...WITH CARBENICILLIN. /CARBENICILLIN/

LIMITED...DATA INDICATE THAT ASPIRIN, IN LARGE DOSES, INCR SERUM LEVEL & HALF-LIFE OF PENICILLIN WHEN...GIVEN CONCURRENTLY. ALTHOUGH CONCURRENT USE OF HIGH DOSES OF ASPIRIN HAS BEEN SUGGESTED TO INCR CLINICAL BENEFITS OF PENICILLIN, POSSIBLE TOXICITIES DUE TO HIGH-DOSE ASPIRIN ADMIN DISCOURAGE SUCH THERAPY. /PENICILLIN/

For more Interactions (Complete) data for AMPICILLIN (21 total), please visit the HSDB record page.

The rate of serum aminotransferase and alkaline phosphatase elevations during ampicillin therapy is not well defined. High dose, intravenous ampicillin has been associated with ALT elevations in 9% to 11% of patients, but a similar rate is often found in comparator arms and the elevations are generally transient and asymptomatic. Rare instances of idiosyncratic liver injury have been reported in persons receiving the aminopenicillins, but they are rarely listed in large case series or prospective databases on drug-induced liver injury. The incidence of clinically apparent liver injury is far lower with ampicillin than occurs with amoxicillin, occurring probably in less than 1 in 200,000 exposed persons. Cases are characterized by a short latency period of a few days to as long as six weeks. The onset of liver injury can occur after the antibiotic is stopped. The serum enzyme pattern associated with aminopenicillin liver injury has included a hepatocellular pattern with marked elevations in ALT and AST, and minimal elevations in alkaline phosphatase and rapid recovery after withdrawal. In addition, cholestatic forms of hepatic injury with marked alkaline phosphatase elevations (as also seen with penicillin-induced liver injury) have also been described, some of which have been associated with prolonged cholestasis and, rarely, with vanishing bile duct syndrome. The onset of hepatic injury may be accompanied by skin rash, toxic epidermal necrolysis, or Stevens Johnson syndrome. Autoantibodies are uncommon.

Skin Sensitizer - An agent that can induce an allergic reaction in the skin.

Serious Adverse Drug Reactions

The following link will take the user to the National Toxicology Program (NTP) Test Agent Search Results page, which tabulates all of the "Standard Toxicology & Carcinogenesis Studies", "Developmental Studies", and "Genetic Toxicity Studies" performed with this chemical. Clicking on the "Testing Status" link will take the user to the status (i.e., in review, in progress, in preparation, on test, completed, etc.) and results of all the studies that the NTP has done on this chemical. /Ampicillin trihydrate/ [http://ntp-apps.niehs.nih.gov/ntp_tox/index.cfm?fuseaction=ntpsearch.searchresults&searchterm=7177-48-2]

AGRANULOCYTOSIS WITH PERIPHERAL MONOCYTOSIS & BONE-MARROW HISTIOCYTOSIS HAS BEEN REPORTED FOLLOWING TREATMENT WITH AMPICILLIN.

Ampicillin has comparatively few adverse properties, permitting it to be used preferentially over other agents such as chloramphenicol or tetracyclines when a broad-spectrum antibacterial drug is desired. It has been used as treatment for urinary, respiratory, and GI infections and bacterial otitis. Since ampicillin is excreted in bile, it can be used to treat biliary tract infections. Superinfections caused by Enterobacter, Pseudomonas, or Candida have occurred during oral ampicillin therapy, necessitating a reduced dose or substitution of another antibacterial drug.

Ampicillin reportedly induces environmental or occupational asthma possibly by IgE mediation /from table/

GI side effects of ampicillin include diarrhea, nausea/vomiting, epigastric/abdominal pain, and stomatitis/glossitis /from table/

For more Human Toxicity Excerpts (Complete) data for AMPICILLIN (59 total), please visit the HSDB record page.

Ampicillin

Group 3: Not classifiable as to its carcinogenicity to humans

Volume 50: (1990) Pharmaceutical Drugs

1990

1989

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

ampicillin

DILI Positive

Oral

DOI:10.1016/j.drudis.2019.09.022

DEATH FROM RESP FAILURE WITH OR WITHOUT CONVULSIONS OCCURRED 6-18 HR AFTER SINGLE ORAL DOSES. ACUTE GASTROENTERITIS & CARDIOVASCULAR SHOCK WERE ASSOCIATED PHENOMENA. ...PATTERN...ALSO TRUE FOR GUINEA PIGS EXCEPT THAT LATE (1-2 WK) & GRADUALLY DEVELOPING TOXEMIA KILLED ALL SURVIVORS OF ACUTE RESPONSE. /PENICILLINS/

IN HAMSTERS...SOMEWHAT MORE TOXIC BY ORAL THAN BY SC ROUTE WHEN OBSERVED FOR 14 DAYS AFTER SINGLE DOSES. TOLERANCE DEVELOPED TO MULTIPLE DOSING. PERHAPS SENSITIVITY OF GUINEA PIGS IS RELATED TO EFFECTS ON INTESTINAL MICROFLORA. SC LD50 IN NEWBORN (LESS THAN 72 HR) RATS WAS 7-FOLD LOWER THAN LD50 IN ADULTS. /PENICILLINS/

Ampicillin may have an adverse effect on rabbits when administered orally. Rabbits that consumed 18.8 mg ampicillin/100 ml drinking water developed diarrhea and died within a month. Severe enteritis and renal tubular damage was thought to be related to an antibiotic-induced disturbance of intestinal bacterial equilibrium. The oral dose of ampicillin is approximately 12 mg/kg 4 times daily.

Ampicillin has been used in a variety of domestic animals at doses ranging from 2 to 50 mg/kg. Blood concentrations are dose dependent and the maintenance dose must be administered at 4- to 6-hour intervals. Although ampicillin disappears from the blood quite rapidly, it appears that tissue concentrations may be greater than blood concentrations for a significant therapeutic effect; eg, /it was/ reported that uterine tissue concentrations in the mare were 10-50% higher than serum. They recommended an IV dose of 11-16 mg ampicillin/kg at 4- to 8-hour intervals. Ampicillin has been used to treat bacterial infections in cattle. A dose of 4.5-11 mg/kg was administered parenterally once daily for 3 days. Clinical improvement was noted in 86% of the cases and adverse effect were noted in experimental tests.

For more Non-Human Toxicity Excerpts (Complete) data for AMPICILLIN (17 total), please visit the HSDB record page.

Evaluation: There is inadequate evidence for the carcinogenicity of ampicillin in humans. There is limited evidence for the carcinogenicity of ampicillin in experimental animals. Overall evaluation: Ampicillin is not classifiable as to its carcinogenicity to humans (Group 3).

Toxicology and carcinogenesis studies of ampicillin trihydrate (97-99% pure) were conducted by administering the chemical in corn oil by gavage to groups of 50 F344/N rats and 50 B6C3F1 mice of each sex, 5 days/wk for 103 wk. Male and female rats received doses of 0, 750, or 1,500 mg/kg, and male and female mice received doses of 0, 1,500 or 3,000 mg/kg. ... Under the conditions of these 2 yr gavage studies, there was equivocal evidence of carcinogenicity of ampicillin trihydrate for male F344/N rats as shown by increased incidences of pheochromocytomas of the adrenal medulla and marginally increased incidences of mononuclear cell leukemia. There was no evidence of carcinogenicity for female F344/N rats receiving 750 or 1,500 mg/kg or for male or female B6C3F1 mice receiving 1,500 or 3,000 mg/kg per day. Noneoplastic lesions of the forestomach were seen in male rats and male and female mice. /Ampicillin trihydrate/

Oral Dosage Form New Animal Drugs. Specifications and conditions of use for dogs and cats. /Ampicillin capsules/

Oral Dosage Form New Animal Drugs. Specifications and conditions of use for dogs. /Ampicillin trihydrate tablets/

Oral Dosage Form New Animal Drugs. Specifications and conditions of use for dogs and cats. /Ampicillin trihydrate capsules/

Oral Dosage Form New Animal Drugs. Specifications and conditions of use for dogs and cats. /Ampicillin trihydrate for oral suspension/

For more FDA Requirements (Complete) data for AMPICILLIN (11 total), please visit the HSDB record page.

Ampicillin is a broad-spectrum antibiotic. The clinical indications for ampicillin cover a variety of infections, including those of the respiratory and urinary tracts, gonorrhoea, meningitis, septicaemia and enteric infections.

MEDICATION

Use (kg; approx.) in Germany (2009): >10000

Impurities of ampicillin that occur during preparation of the product are D-(-)-alpha-phenylglycine and 6-aminopenicillanic acid. It has been reported that sodium ampicillin in aqueous solution undergoes a reaction to form oligomeric products.

(1978) 7.51X10+7 GRAMS (INCL SALTS)

(1979) 1.89X10+7 GRAMS (INCL SALTS)

(1977) 3.83X10+7 GRAMS (PRINCPL CUSTMS DISTS)

(1979) 2.25X10+7 GRAMS (PRINCPL CUSTMS DISTS)

(1977) 5.30X10+8 GRAMS

(1979) 4.53X10+8 GRAMS

ACYLATION OF 6-AMINOPENICILLANIC ACID WITH D-(-)-GLYCINE

DOYLE ET AL, US PATENT 2,985,648 (1961); EIDEM, BRITISH PATENT 902,703 (1962 TO BEECHAM); DOYLE ET AL, J CHEM SOC 1962, 1440; KAUFMANN, BAUER, US PATENT 3,079,307 (1963 TO BAYER); JOHNSON, WOLFE, & JOHNSON, HARDCASTLE, US PATENTS 3,140,282 & 3,157,640 (BOTH 1964 TO BRISTOL-MYERS)...

...GRANT, ALBURN, US PATENT 3,144,445 (1964 TO AM HOME PRODUCTS); DANE, DOCKNER, BER 98, 789 (1965). ... DL-FORM.../OF SODIUM SALT/ BRITISH PATENT 958,824 (1964 TO PFIZER).

Ampicillin is produced by the acylation of 6-aminopenicillanic acid with D-(-)-alpha-phenylglycine by either microbiological or chemical synthesis.

USP anhydrous ampicillin contains 900-1050 ug/mg ampicillin (calculated as the anhydrous base). Ampicillin is available in 125-, 200-, 250-, and 500-mg tablets that contain 90-120% labelled active ingredient, in 125-, 250-, and 500-mg capsules containing 90-120% labelled active ingredient, and as oral suspensions of 100, 125, and 250 mg/5 ml containing 90-120% of the labelled active ingredient and probenecid.

Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients

Veterinary Drug -> ANTIMICROBIAL_AGENT; Veterinary Drug -> -> JECFA Functional Classes

Pharmaceuticals -> Animal Drugs -> Approved in Taiwan

HAS BEEN USED CLINICALLY TO IMPROVE FERTILITY IN KENNEL BY TREATING STUD DOG TO ELIMINATE BACTERIAL CONTAMINATION OF SEMEN. ... IN US... NOT RECOMMENDED FOR USE IN FOOD PRODUCING ANIMALS EXCEPT SWINE. TOLERANCE OF 0.01 PPM FOR...RESIDUES IN UNCOOKED EDIBLE TISSUES OF SWINE IS PERMITTED...