Ampicillin: Indications, Uses, Dosage, Drugs Interactions, Side effects

2022-12-17 12:43:47 By : Mr. sdyuntai CN

Ampicillin is a Penicillin derivative belonging to Antibiotic / Antimicrobial agent.

Ampicillin is a penicillin derivative used for the treatment of a variety of infections caused by gram-positive and gram-negative bacteria as well as some anaerobes. Enrotril For Dogs

Ampicillin: Indications, Uses, Dosage, Drugs Interactions, Side effects

Ampicillin moderately well absorbed from the gastrointestinal tract. Ampicillin decreased absorption rate with food. Time to peak plasma concentration is approximately 1-2 hours (oral); approximately 1 hour (IM). Ampicillin is widely distributed throughout the body and can be found in ascitic, pleural, and joint fluids. Ampicillin crosses the placenta and enters breast milk (small amounts). It penetrates the CSF with inflamed meninges. The plasma protein binding is about 15-18%. It is metabolized into penicilloic acid. It is excreted via urine (approximately 90%, as unchanged drug within 24 hours); faeces. The Elimination half-life is about 1-1.8 hours.

Ampicillin shows common side effects like Diarrhea, nausea, vomiting, skin rash.

Ampicillin is available in the form of Oral Capsule, Oral suspension, and Injectable solution.

Ampicillin is available in India, US, Singapore, China, Spain, France, Russia, Malaysia, Canada, Italy, Japan, and Austria.

Ampicillin belongs to the Antibiotic / Antimicrobial agent acts as a Penicillinderivative.

By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, Ampicillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that Ampicillin interferes with an autolysin inhibitor.

The Data of onset of action of Ampicillin is not available.

The Ampicillin may remain in your body for 9 hours after oral administration.

The Tmax of Ampicillin is approximately 1-2 hours (oral); approximately 1 hour (IM).

Ampicillin is available in the form of Oral Capsule, Oral suspension, and Injectable solution.

Ampicillin capsule and suspension is taken orally, and Ampicillin injectable solution is given via intravenous or intramuscular route.

Ampicillin is an antibiotic. It is used for the treatment of bacterial infections that affects your lungs, nose, throat, urinary tract, stomach, and intestine, etc. It works by preventing the formation of the protective outer layer of the bacteria and kills them. This medication is effective only for the treatment of infections caused by bacteria and not viruses.

Ampicillin is a Penicillin derivative belonging to Antibiotic / Antimicrobial agent.

Ampicillin prevents bacterial cell wall synthesis by binding to 1 or more of the penicillin-binding proteins resulting in the inhibition of the final transpeptidation step of peptidoglycan synthesis in the bacterial cell walls.

Ampicillin is approved for use in the following clinical indications

Although not approved, there have been certain off-label indications. These include

Pathogen-directed therapy for Enterococcus spp.

IV: 2 g every 4 hours; use as part of an appropriate combination regimen in the setting of suspected endocarditis or critical illness. Duration of therapy is 7 to 14 days for uncomplicated infection (ie, fever resolution within 72 hours and absence of metastatic focus of infection or endovascular hardware). Some experts recommend a duration of 5 to 7 days for uncomplicated infection with rapid blood culture clearance (within 24 hours) and in the absence of metastatic infection.

Pathogen-directed therapy for Listeria monocytogenes

IV: 2 g every 4 hours; use in combination with gentamicin for nonpregnant patients. Duration should be individualized based on patient factors, source and extent of infection, and clinical response, but ampicillin is usually continued for at least 14 to 21 days.

Enterococcus faecalis, native or prosthetic valve (penicillin-susceptible)

IV: 2 g every 4 hours as part of an appropriate combination regimen (eg, with ceftriaxone or gentamicin). Duration is usually 6 weeks; for patients with native valve endocarditis and symptoms <3 months, the combination of ampicillin and gentamicin can be given for 4 weeks.

HACEK organisms, native or prosthetic valve (ampicillin-susceptible) (off-label use)

IV: 2 g every 4 hours for 4 weeks (native valve) or 6 weeks (prosthetic valve).

Viridans group streptococci and Streptococcus gallolyticus (Streptococcus bovis)

Native valve: Highly penicillin-susceptible (minimum inhibitory concentration [MIC] ≤0.12 mcg/mL)

IV: 2 g every 4 hours for 4 weeks.

Native valve: Relatively penicillin-resistant (MIC >0.12 to <0.5 mcg/mL)

IV: 2 g every 4 hours for 4 weeks in combination with gentamicin for the first 2 weeks.

Native valve: Penicillin-resistant (MIC ≥0.5 mcg/mL)

IV: 2 g every 4 hours in combination with gentamicin. The duration of this regimen is not well established; infectious diseases consultation recommended.

Prosthetic valve: Highly penicillin-susceptible (MIC ≤0.12 mcg/mL)

IV: 2 g every 4 hours for 6 weeks (with or without concomitant gentamicin for the first 2 weeks).

Prosthetic valve: Relatively penicillin-resistant (MIC >0.12 to <0.5 mcg/mL) or fully penicillin-resistant (MIC ≥0.5 mcg/mL)

IV: 2 g every 4 hours in combination with gentamicin for 6 weeks. For relatively resistant strains, some experts prefer a shorter duration of the gentamicin component (≥2 weeks).

IV: 2 g every 4 hours; for empiric therapy and for directed therapy for Enterococcus or Listeria, use as part of an appropriate combination regimen. Treatment duration is 7 to 21 days, depending on causative pathogen(s) and clinical response.

Acute uncomplicated or simple cystitis due to Enterococcus spp.

Oral: 500 mg every 6 hours for 5 to 7 days.

Acute pyelonephritis or other complicated urinary tract infection due to Enterococcus spp. (off label)

IV: 1 to 2 g every 4 to 6 hours; can give with an aminoglycoside for critical illness. Switch to an appropriate oral regimen once patient has improvement in symptoms. Duration of therapy depends on the antimicrobial chosen to complete the regimen and ranges from 5 to 14 days.

Endocarditis, prophylaxis (dental or invasive respiratory tract procedures) (alternative agent for patients unable to take oral therapy) (off-label use)

IM, IV: 2 g as a single dose 30 to 60 minutes before procedure; if inadvertently not given prior to the procedure, may be administered up to 2 hours after the procedure.

IV: 2 g every 4 hours as part of an appropriate combination regimen. Total duration of therapy (which may include transition to oral antibiotics) is 4 to 5 days following adequate source control.

Pathogen-directed therapy for penicillin-susceptible Enterococcus or Streptococcus spp.

IV: 2 g every 4 hours or 12 g as a continuous infusion every 24 hours, generally for ≥6 weeks. Shorter courses are appropriate if the affected bone is completely resected (eg, by amputation). For Enterococcus, some experts use with ceftriaxone in the setting of retained hardware.

IV: 2 g every 6 hours in combination with gentamicin. In females undergoing cesarean delivery, an anti-anaerobic agent should also be added. Continue regimen until vaginal delivery or for 1 dose after cesarean delivery.

IV: 2 g every 6 hours in combination with clindamycin and gentamicin; treat until patient is clinically improved (no fundal tenderness) and afebrile for 24 to 48 hours.

IV: 2 g every 6 hours in combination with clindamycin and gentamicin. After 24 to 48 hours of sustained clinical improvement, may transition to oral therapy to complete 14 days of treatment.

Intraperitoneal: 125 mg/L of dialysate with each exchange. Duration of therapy is ≥2 weeks for patients with adequate clinical response.

IV: 2 g every 4 hours or 12 g continuous infusion every 24 hours. Duration varies but is generally 4 to 6 weeks; for enterococcal infections, some experts use with ceftriaxone in the setting of retained hardware.

IV: 2 g as a single dose at onset of labor or prelabor rupture of membranes, then 1 g every 4 hours until delivery.

Oral: 50 to 100 mg/kg/day divided every 6 hours; maximum daily dose: 2,000 mg/day.

IM, IV: 50 to 200 mg/kg/day divided every 6 hours; maximum daily dose: 8 g/day; higher doses (300 to 400 mg/kg/day; maximum daily dose: 12 g/day) are recommended for some infections.

Infants >3 months, Children, and Adolescents:

Empiric treatment or S. pneumoniae (MICs for penicillin ≤2 mcg/mL) or H. influenzae (beta-lactamase negative) in fully immunized patients

IV: 150 to 200 mg/kg/day divided every 6 hours.

IV: 200 mg/kg/day divided every 6 hours.

S. pneumoniae (MICs for penicillin ≥4 mcg/mL)

IV: 300 to 400 mg/kg/day divided every 6 hours.

Children and Adolescents: IV: 200 to 300 mg/kg/day divided every 4 to 6 hours; maximum daily dose: 12 g/day; use in combination with other antibiotics for at least 4 weeks; some organisms may require longer duration.

Dental or oral procedures or respiratory tract procedures (eg, tonsillectomy, adenoidectomy)

Infants, Children, and Adolescents: IV, IM: 50 mg/kg within 30 to 60 minutes before procedure; maximum dose: 2,000 mg/dose. Intravenously (IV) administered antibiotics should be used for patients who are unable to tolerate or absorb oral medications.

Infants, Children, and Adolescents: IV: 200 mg/kg/day divided every 6 hours; maximum single dose: 2,000 mg; maximize doses if undrained abdominal abscesses.

Infants, Children, and Adolescents: IV: 300 to 400 mg/kg/day divided every 4 to 6 hours; maximum daily dose: 12 g/day.

Infants, Children, and Adolescents: Intraperitoneal: 125 mg per liter of dialysate for 2 weeks.

Infants, Children, and Adolescents: IV: 50 mg/kg within 60 minutes prior to surgical incision; may repeat in 2 hours if lengthy procedure or excessive blood loss; maximum dose: 2,000 mg/dose.

Ampicillin is available in various strengths as 250mg, 500mg and 125mg/5mL and 250mg/5mL.

Ampicillin is available in the form of Oral Capsule, Oral suspension, and Injectable solution.

If usual recommended dose is 1 to 2 g every 6 hours: 1 to 2 g every 6 hours

If usual recommended dose is 2 g every 4 hours: 2 g every 4 hours

If usual recommended dose is 1 to 2 g every 6 hours: 1 to 2 g every 8 hours

If usual recommended dose is 2 g every 4 hours: 2 g every 6 hours

If usual recommended dose is 1 to 2 g every 6 hours: 1 to 2 g every 12 hours

If usual recommended dose is 2 g every 4 hours: 2 g every 8 hours

If usual recommended dose is 1 to 2 g every 6 hours: 1 to 2 g every 24 hours

If usual recommended dose is 2 g every 4 hours: 2 g every 12 hours

Take on an empty stomach. Food decreases ampicillin absorption rate; may decrease ampicillin serum concentration. Management: Take at equal intervals around-the-clock, preferably on an empty stomach (30 minutes before or 2 hours after meals). Maintain adequate hydration, unless instructed to restrict fluid intake.

Ampicillin is contraindicated in patients with

Ampicillin is excreted in trace amounts in human milk. Therefore, caution should be exercised when ampicillin-class antibacterial are administered to a nursing woman.

Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.

Take on an empty stomach. Food decreases ampicillin absorption rate; may decrease ampicillin serum concentration. Management: Take at equal intervals around-the-clock, preferably on an empty stomach (30 minutes before or 2 hours after meals). Maintain adequate hydration, unless instructed to restrict fluid intake.

● Brain disease (penicillin-induced), glossalgia, seizure, sore mouth, Erythema multiforme, exfoliative dermatitis, skin rash, urticaria, Diarrhea, enterocolitis, glossitis, melanoglossia, nausea, oral candidiasis, pseudomembranous colitis, stomatitis, vomiting, Agranulocytosis, anemia, eosinophilia, hemolytic anemia, immune thrombocytopenia, leukopenia, Increased serum AST, Anaphylaxis, Serum sickness-like reaction, Stridor, Fever.

The common side effects of Ampicillin include the following

● Diarrhea, nausea, vomiting, skin rash.

● Itching, hives, difficulty breathing or swallowing, wheezing, severe diarrhea (watery or bloody stools) that may occur with or without fever and stomach cramps (may occur up to 2 months or more after your treatment), a return of fever, cough, sore throat, chills, and other signs of infection.

Reproduction studies have been performed in laboratory animals at doses several times the human dose and have revealed no evidence of adverse effects due to ampicillin. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Ampicillin is excreted in trace amounts in human milk. Therefore, caution should be exercised when ampicillin-class antibacterial are administered to a nursing woman.

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.

In case of over dosage, 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.

Ampicillin is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Ampicillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of Ampicillin results from the inhibition of cell wall synthesis and is mediated through Ampicillin binding to penicillin binding proteins (PBPs). Ampicillin is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

Ampicillin moderately well absorbed from the gastrointestinal tract. Ampicillin decreased absorption rate with food. Time to peak plasma concentration is approximately 1-2 hours (oral); approximately 1 hour (IM).

Ampicillin is widely distributed throughout the body and can be found in ascitic, pleural, and joint fluids. Ampicillin crosses the placenta and enters breast milk (small amounts). It penetrates the CSF with inflamed meninges. The plasma protein binding is about 15-18%.

It is metabolized into penicilloic acid. It is excreted via urine (approximately 90%, as unchanged drug within 24 hours); faeces. The Elimination half-life is about 1-1.8 hours.

1. Lockey E, Eaton BR, Compston N. Preliminary Bacteriological and Clinical Studies with Ampicillin (BRL 1341). Brit. J. Clin. Practice. 1962;16(1):13-7.

2. Kaplan JM, McCracken Jr GH, Horton LJ, Thomas ML, Davis N. Pharmacologic studies in neonates given large dosages of ampicillin. The Journal of pediatrics. 1974 Apr 1;84(4):571-7.

Ampicillin: Indications, Uses, Dosage, Drugs Interactions, Side effects

Gentamicin C1 3. Lode H. Role of sultamicillin and ampicillin/sulbactam in the treatment of upper and lower bacterial respiratory tract infections. International journal of antimicrobial agents. 2001 Sep 1;18(3):199-209.