Ampicillin

Ampicillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Ampicillin has been approved to relieve symptoms and also for the treatment and maintenance of Bloodstream infection, Endocarditis, prophylaxis, Endocarditis, treatment, Intra-abdominal infection, health care–associated, Meningitis, bacterial, Osteomyelitis and/or discitis, treatment, Pelvic infections, Peritonitis, treatment, Prosthetic joint infection, Streptococcus, maternal prophylaxis for prevention of neonatal disease, Urinary tract infection.

Ampicillin is a broad-spectrum penicillin antibiotic that is administered orally, intravenously, or intramuscularly. The drug is rapidly and well-absorbed after oral administration, with peak plasma concentrations achieved within 1 to 2 hours. The drug is widely distributed in body fluids and tissues, with high concentrations found in the bile, urine, and cerebrospinal fluid. Ampicillin is primarily eliminated through the kidneys via glomerular filtration and tubular secretion, with a half-life of approximately 1 hour in patients with normal kidney function. In patients with impaired kidney function, the half-life of ampicillin may be prolonged, necessitating dosage adjustments to avoid toxicity.

The common side effects which involve the use of Ampicillin are Diarrhea, Nausea, Vomiting, Skin rash or hives, Fever, Joint pain or swelling, Headache, Dizziness, Fatigue and Pain or redness at the injection site

Ampicillin is available in the form of Oral capsule, Oral suspension, Injectable solution , Powder for injection .

Ampicillin is approved in Germany, Japan, Malaysia, India, the U.S., U.K., and China.

Ampicillin belongs to the pharmacological class of Beta-Lactam Antibiotics.

Ampicillin is a beta-lactam antibiotic that works by inhibiting the growth of bacterial cell walls. It binds to penicillin-binding proteins (PBPs) in the bacterial cell wall, interfering with the cross-linking of peptidoglycan chains, ultimately leading to cell death.

Ampicillin has been approved to relieve symptoms and also for the treatment and maintenance of Bloodstream infection, Endocarditis, prophylaxis, Endocarditis, treatment, Intra-abdominal infection, health care–associated, Meningitis, bacterial, Osteomyelitis and/or discitis, treatment, Pelvic infections, Peritonitis, treatment, Prosthetic joint infection, Streptococcus, maternal prophylaxis for prevention of neonatal disease, Urinary tract infection.

The peak plasma concentration (Cmax) of ampicillin typically occurs within 1 to 2 hours after oral administration and within 15 to 30 minutes after intravenous administration. The onset of action of ampicillin is also rapid, with clinical effects observed within the first few hours of administration.

The duration of action of ampicillin varies depending on the condition being treated, the dose and frequency of administration, and the patient's individual factors such as kidney function. In general, the half-life of ampicillin in adults with normal kidney function is approximately 1 hour, and the drug is typically eliminated from the body within 6 to 8 hours.

Ampicillin is available in the form of Oral capsule, Oral suspension, Injectable solution , Powder for injection.

Ampicillin can be used in the following treatment:

• Bloodstream infection
• Endocarditis, prophylaxis
• Endocarditis, treatment
• Intra-abdominal infection, health care-associated
• Meningitis, bacterial
• Osteomyelitis and/or discitis, treatment
• Pelvic infections
• Peritonitis, treatment
• Prosthetic joint infection
• Streptococcus, maternal prophylaxis for prevention of neonatal disease
• Urinary tract infection

Ampicillin can help to relieve symptoms and also for the treatment and maintenance of Bloodstream infection, Endocarditis, prophylaxis, Endocarditis, treatment, Intra-abdominal infection, health care-associated, Meningitis, bacterial, Osteomyelitis and/or discitis, treatment, Pelvic infections, Peritonitis, treatment, Prosthetic joint infection, Streptococcus, maternal prophylaxis for prevention of neonatal disease, Urinary tract infection.

Ampicillin is approved for use in the following clinical indications:

• Bloodstream infection
• Endocarditis, prophylaxis
• Endocarditis, treatment
• Intra-abdominal infection, health care-associated
• Meningitis, bacterial
• Osteomyelitis and/or discitis, treatment
• Pelvic infections
• Peritonitis, treatment
• Prosthetic joint infection
• Streptococcus, maternal prophylaxis for prevention of neonatal disease
• Urinary tract infection

• Bloodstream infection: Ampicillin is used to treat infections in the bloodstream caused by susceptible bacteria. The recommended dosage is 1 to 2 grams every 4 to 6 hours.
• Endocarditis prophylaxis: Ampicillin is used as a prophylaxis to prevent bacterial endocarditis in patients who are at risk of developing the condition. The recommended dosage is 2 grams given as a single dose for about 30 to 60 minutes before the procedure.
• Endocarditis treatment: Ampicillin is used to treat bacterial endocarditis, which is said to be an infection of the lining of the heart. The recommended dosage is 2 grams every 4 hours for 4 to 6 weeks.
• Intra-abdominal infection, healthcare-associated: Ampicillin is used to treat healthcare-associated intra-abdominal infections caused by susceptible bacteria. The recommended dosage is 1 to 2 grams every 6 hours.
• Meningitis, bacterial: Ampicillin is used to treat bacterial meningitis, which is said to be an infection of the membranes surrounding the brain and spinal cord. The recommended dosage is 2 grams every 4 hours.
• Osteomyelitis and/or discitis, treatment: Ampicillin is used to treat bone infections such as osteomyelitis and discitis caused by susceptible bacteria. The recommended dosage is 2 grams every 4 hours for 4 to 6 weeks.
• Pelvic infections: Ampicillin is used to treat pelvic infections such as pelvic inflammatory disease (PID) caused by susceptible bacteria. The recommended dosage is 2 grams every 6 hours.
• Peritonitis, treatment: Ampicillin is used to treat peritonitis, which is an infection of the lining of the abdominal cavity. The recommended dosage is 1 to 2 grams every 4 to 6 hours.
• Prosthetic joint infection: Ampicillin is used to treat infections of prosthetic joints caused by susceptible bacteria. The recommended dosage is 2 grams every 4 to 6 hours for 4 to 6 weeks.
• Streptococcus, maternal prophylaxis for prevention of neonatal disease: Ampicillin is used to prevent neonatal Group B Streptococcus (GBS) disease in infants born to mothers who carry GBS. The recommended dosage is 2 grams followed by 1 gram every 4 hours until delivery.
• Urinary tract infection: Ampicillin is used to treat urinary tract infections caused by susceptible bacteria. The recommended dosage is 250 to 500 mg every 6 hours or 500 mg to 1 gram every 8 hours.

• Oral capsules: Ampicillin capsules are available in strengths of 250mg and 500mg.
• Oral suspension: Ampicillin oral suspension is available in various strengths, including 125mg/5ml, 200mg/5ml, 250mg/5ml, and 400mg/5ml.
• Injectable solution: Ampicillin injectable solution is available in strengths of 125mg/ml, 250mg/ml, and 500mg/ml.
• Powder for injection is available in strengths of 125mg, 250mg, 500mg, 1g, and 2g.

Oral capsule, Oral suspension, Injectable solution, Powder for injection

• Dosage Adjustments in Kidney Patients:

Ampicillin dosing adjustments may be necessary in patients with renal impairment to prevent toxicity and ensure efficacy. The dose adjustment is based on the patient's estimated creatinine clearance (CrCl) using the Cockcroft-Gault equation. Here are some general guidelines for dosing adjustments in patients with renal impairment:

Mild to moderate renal impairment (CrCl 30-80 mL/min): No dosage adjustment is usually necessary, but close monitoring of the patient's clinical response and serum levels of ampicillin may be necessary.

Severe renal impairment (CrCl less than 30 mL/min): The dosing interval should be increased to 12-24 hours depending on the severity of the renal impairment. The dosage may also need to be reduced based on the severity of renal impairment. For example, a dose of 500 mg every 12 hours may be given to a patient with a CrCl of 10-20 mL/min.

End-stage renal disease (ESRD): Ampicillin may be removed by hemodialysis. Therefore, a dose of 500 mg to 1 g may be given after each dialysis session.

• Dosage Adjustments in Pediatric Patients:

Neonates and Infants: For neonates and infants up to 3 months of age, ampicillin is typically dosed at 50mg/kg/dose every 12 hours. The maximum daily dose should not exceed 400mg/kg/day.

Children and Adolescents: For children and adolescents older than 3 months of age, ampicillin is typically dosed at 100mg/kg/day divided into 4 equal doses. The maximum daily dose should not exceed 12g/day.

There are no specific dietary restrictions for patients receiving benzathine benzylpenicillin. Take ampicillin on an empty stomach: It is generally recommended to take ampicillin on an empty stomach, at least one hour before or two hours after a meal. This helps to maximize absorption of the medication. Consuming high-fat meals can decrease the absorption of ampicillin. Therefore, it is best to avoid high-fat meals while taking the medication. Calcium in dairy products can interfere with the absorption of ampicillin. Therefore, it is best to avoid consuming dairy products, such as milk or cheese, while taking ampicillin.

Ampicillin may be contraindicated under the following conditions:

• Allergy to penicillin: Patients with a known allergy to penicillin or cephalosporin antibiotics should not take Ampicillin.

The physician should closely monitor the patients as well as keep pharmacovigilance as follows:

Hypersensitivity reactions: Serious as well as occasionally fatal hypersensitivity reactions, including anaphylaxis, have been reported in patients receiving penicillin therapy. Patients with a history of penicillin hypersensitivity and/or hypersensitivity reactions to multiple allergens may be at higher risk. Before therapy with ampicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillin, cephalosporins or other allergens.

Clostridium difficile-associated diarrhea (CDAD): Clostridium difficile-associated diarrhea had been reported with use of nearly all antibacterial agents, which including ampicillin. It might range in severity from mild diarrhea to fatal colitis. Treatment with some antibacterial agents alters the normal flora of the colon leading to the overgrowth of C. difficile. Clostridium difficile-associated diarrhea must be considered in all patients who present with diarrhea following antibiotic use.

Interference with laboratory tests: Ampicillin may interfere with the results of certain laboratory tests, such as urinary glucose tests or Coombs' tests.

The alcohol consumption should be avoided while taking ampicillin, as it may increase the risk of side effects such as dizziness, headache, and stomach upset.

WHO and the FDA both state that ampicillin is excreted into breast milk in small amounts and is generally considered safe to use during breastfeeding.

Pregnancy Category B

WHO categorizes ampicillin as a category B medication, meaning that animal studies have not shown any evidence of harm to the fetus, but there are no adequate as well as well-controlled studies in pregnant women. The FDA categorizes ampicillin as a pregnancy category B medication as well, indicating that animal studies have shown no risk to the fetus, but there are no adequate or well-controlled studies in pregnant women.

Ampicillin can be taken with or without food. However, it is recommended to take ampicillin on an empty stomach, at least one hour before or two hours after a meal, for optimal absorption. Taking ampicillin with food may delay its absorption and reduce its effectiveness.

It is also important to avoid consuming certain foods and drinks while taking ampicillin. For example, taking ampicillin with dairy products or calcium-fortified foods or drinks, such as milk, yogurt, cheese, or orange juice, may reduce its absorption and effectiveness. Therefore, it is recommended to avoid consuming these products within 2 hours of taking ampicillin.

The adverse reactions related to Ampicillin can be categorized as follows:

Common

• Diarrhea
• Nausea and vomiting
• Skin rash
• Allergic reactions,( hives, itching, and difficulty breathing)
• Oral thrush
• Headache
• Dizziness
• Insomnia
• Vaginal yeast infection in women

Less common

• Abdominal pain
• Loss of appetite
• Indigestion
• Joint pain
• Fever
• Anemia
• Low white blood cell count, which can increase the risk of infection
• Kidney problems, such as acute interstitial nephritis

Rare

• Severe allergic reactions, such as anaphylaxis, which is a potentially life-threatening reaction which requires immediate medical attention
• Seizures or convulsions, which are more likely to occur in patients with a history of seizures or who are taking high doses of ampicillin
• Liver damage, which is rare but can occur in patients with preexisting liver disease or who are taking other medications that can damage the liver
• Stevens-Johnson syndrome or toxic epidermal necrolysis, which are severe skin reactions that can be life-threatening.

The clinically relevant drug interactions of Ampicillin are briefly summarized here:

• Probenecid: Probenecid is a medication used to treat gout and can also increase the levels of Ampicillin in the blood by reducing its excretion from the body. This can result in an increased risk of side effects from Ampicillin. Therefore, patients taking probenecid and Ampicillin should be closely monitored for adverse effects, and the dosage of Ampicillin may need to be adjusted.
• Methotrexate: Methotrexate is a medication used to treat cancer and certain autoimmune diseases, and Ampicillin can decrease its excretion from the body, leading to increased levels of methotrexate in the blood. This can increase the risk of methotrexate toxicity, such as bone marrow suppression and gastrointestinal toxicity. Patients taking both drugs should be closely monitored for adverse effects, and the dosage of methotrexate may need to be adjusted.
• Aminoglycosides: Aminoglycosides, such as gentamicin and tobramycin, are antibiotics that can be used to treat serious infections. Ampicillin can interact with aminoglycosides, leading to decreased effectiveness of both drugs. This is because Ampicillin can inactivate the aminoglycosides in the bloodstream. If a patient needs to take both drugs, their healthcare provider may need to adjust the dosages or choose an alternative antibiotic.
• Tetracyclines: Tetracyclines, such as doxycycline and minocycline, are antibiotics used to treat various infections. Ampicillin can interact with tetracycline antibiotics, leading to decreased effectiveness of both drugs. This is because Ampicillin can inactivate the tetracyclines in the bloodstream. Patients taking both drugs may need to be monitored closely for adverse effects, and the dosage of either drug may need to be adjusted.
• Oral contraceptives: Ampicillin can decrease the effectiveness of oral contraceptives, increasing the risk of unintended pregnancy. This is because Ampicillin can interfere with the absorption and metabolism of estrogen in the body. Women taking oral contraceptives and Ampicillin should use a backup method of contraception, such as condoms, during treatment with Ampicillin and for a few days afterward.
• Warfarin: Warfarin is a blood thinner used to prevent blood clots. Ampicillin can interact with warfarin, leading to an increased risk of bleeding. This is because Ampicillin can decrease the metabolism of warfarin in the liver, leading to increased levels of warfarin in the blood. Patients taking both drugs should be closely monitored for signs of bleeding, and the dosage of warfarin may need to be adjusted.
• Allopurinol: The concurrent administration of allopurinol with ampicillin has been associated with an increased risk of skin rashes. While the exact mechanism of this interaction is not fully understood, it is thought that the combination of the two drugs may lead to an accumulation of ampicillin in the body, which can increase the risk of skin rashes. It is also possible that the interaction may be related to hyperuricemia, a condition that is often treated with allopurinol.

The following are the side effects involving Ampicillin:

• Diarrhea
• Nausea and vomiting
• Skin rash
• Allergic reactions, (hives, itching, and difficulty breathing)
• Superinfection, which is a new infection that develops during or after treatment with antibiotics
• Oral thrush
• Headache
• Dizziness
• Insomnia
• Vaginal yeast infection in women

• Pregnancy

Category B

WHO categorizes ampicillin as a category B medication, meaning that animal studies have not shown any evidence of harm to the fetus, but there are no adequate or well-controlled studies in pregnant women. The FDA categorizes ampicillin as a pregnancy category B medication as well, indicating that animal studies have shown no risk to the fetus, but there are no adequate and well-controlled studies in pregnant women.

• Lactation: WHO and the FDA both state that ampicillin is excreted into breast milk in small amounts and is generally considered safe to use during breastfeeding.

• Pediatric: WHO and the FDA both state that ampicillin can be used in children, but dosage adjustments may be necessary based on the child's age and weight. The FDA states that the safety and effectiveness of ampicillin in pediatric patients below the age of 1 month has not been established.

• Geriatric: WHO and the FDA both state that ampicillin can be used in elderly patients, but dosage adjustments may be necessary based on the patient's renal function. Elderly patients may be more susceptible to side effects such as diarrhea and rash.

Physicians should be knowledgeable and vigilant about the treatment and identification of over dosage of Ampicillin.

Overdosing on ampicillin can lead to a range of symptoms and potential complications, including:

• Nausea and vomiting
• Diarrhea
• Abdominal pain and cramping
• Seizures
• Allergic reactions, such as hives, itching, and difficulty breathing
• Anaphylaxis, which is a severe and potentially life-threatening allergic reaction that requires immediate medical attention

Treatment for an ampicillin overdose typically involves supportive care and management of symptoms. In cases of severe overdose, hospitalization may be necessary. The following steps may be taken to manage an ampicillin overdose:

• Gastric lavage or pumping of the stomach to remove any remaining ampicillin from the digestive tract
• Activated charcoal administration to absorb any remaining ampicillin in the digestive tract
• Intravenous fluids to maintain hydration and electrolyte balance
• Close monitoring of vital signs, such as blood pressure, heart rate, and respiratory rate
• Treatment of any symptoms or complications that arise, such as seizures or anaphylaxis

Pharmacodynamics

Ampicillin is a beta-lactam antibiotic that works by inhibiting bacterial cell wall synthesis. Specifically, it binds to and inactivates the enzyme transpeptidase, which is involved in the cross-linking of peptidoglycan chains in bacterial cell walls. This leads to the weakening of the cell wall and eventual lysis of the bacterial cell.

Spectrum of activity: Ampicillin has a broad spectrum of activity against many Gram-positive and Gram-negative bacteria, including Streptococcus pneumoniae, Streptococcus pyogenes, Neisseria meningitidis, Haemophilus influenzae, Escherichia coli, and Proteus mirabilis, among others. However, ampicillin is less active against some bacteria that produce beta-lactamases, such as Staphylococcus aureus, and it is ineffective against some bacteria that lack cell walls, such as Mycoplasma and Chlamydia.

Pharmacokinetics

• Absorption: Ampicillin is rapidly absorbed after oral administration, with peak serum concentrations reached within 1-2 hours. The bioavailability of oral ampicillin is approximately 80-90%. The presence of food in the stomach does not significantly affect the absorption of ampicillin.

• Distribution: Ampicillin has a volume of distribution of approximately 0.2-0.3 L/kg in adults. It is widely distributed throughout the body, including into the cerebrospinal fluid, pleural fluid, and ascitic fluid. The protein binding of ampicillin is low, ranging from 15-25%.

• Metabolism: Ampicillin is not extensively metabolized in the liver. A small amount of the drug may be converted to inactive metabolites before being excreted from the body.

• Excretion: Ampicillin is primarily excreted unchanged in the urine, with up to 80% of a dose excreted within 6 hours of administration. The elimination half-life is approximately 1 hour in patients with normal renal function. In patients with impaired renal function, the elimination half-life is prolonged.

• https://www.drugs.com/drug-interactions/ampicillin.html
• https://www.everydayhealth.com/drugs/ampicillin#drug-interactions
• https://www.medbroadcast.com/drug/getdrug/teva-ampicillin
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