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What is ampicillin?

4 min read

First introduced in 1961, ampicillin was a groundbreaking "broad spectrum" penicillin that extended antimicrobial activity to include many gram-negative bacteria. So, what is ampicillin and how does this powerful antibiotic work to combat a variety of bacterial illnesses?

Quick Summary

A penicillin-type antibiotic, ampicillin treats various bacterial infections, including those affecting the respiratory, urinary, and gastrointestinal tracts. It works by inhibiting bacterial cell wall synthesis, leading to bacterial death, but is vulnerable to beta-lactamase enzymes.

Key Points

  • Broad-Spectrum Antibiotic: Ampicillin is a penicillin-class antibiotic effective against a wide range of gram-positive and gram-negative bacteria, representing a key advance over earlier penicillins.

  • Cell Wall Synthesis Inhibitor: Its mechanism of action is to bind to penicillin-binding proteins (PBPs), which inhibits bacterial cell wall synthesis and causes cell death.

  • Treats Diverse Infections: It is used to treat infections affecting the respiratory, urinary, and gastrointestinal tracts, as well as more serious conditions like meningitis and endocarditis.

  • Vulnerable to Resistance: Ampicillin can be inactivated by beta-lactamase enzymes produced by resistant bacteria, which is why it is often combined with beta-lactamase inhibitors.

  • Less Bioavailable Than Amoxicillin: Compared to amoxicillin, ampicillin has lower oral bioavailability, requires more frequent dosing, and is associated with a higher incidence of gastrointestinal side effects.

  • Administration Methods: Ampicillin is available for oral use (capsules, suspension) and for injection (intravenous or intramuscular) in hospital settings for severe infections.

  • Allergy Warning: It is contraindicated in patients with a penicillin allergy due to the risk of severe hypersensitivity reactions, including anaphylaxis.

In This Article

What is ampicillin?

  • Disclaimer: Information provided is for general knowledge and should not be taken as medical advice. Consult with a healthcare provider.

Ampicillin is a semi-synthetic, broad-spectrum antibiotic that belongs to the aminopenicillin subgroup of the penicillin family. Discovered in 1958 and introduced to the market in 1961, it was significant because it extended the antimicrobial coverage of penicillins beyond just gram-positive bacteria to include a variety of gram-negative organisms. Ampicillin is available in oral forms, like capsules and liquid suspensions, and injectable forms for intravenous (IV) or intramuscular (IM) administration.

The mechanism of action: How ampicillin works

As a beta-lactam antibiotic, ampicillin works by targeting the bacterial cell wall, which is essential for the survival of bacteria. The mechanism of action involves a key two-step process:

  1. Binding to Penicillin-Binding Proteins (PBPs): Ampicillin binds to and inactivates specific enzymes located on the inner membrane of the bacterial cell wall, known as penicillin-binding proteins (PBPs). These PBPs are crucial for the final stage of peptidoglycan synthesis, the main structural component of the cell wall.
  2. Inhibiting Cell Wall Synthesis: By inactivating PBPs, ampicillin disrupts the formation of the cell wall's peptidoglycan structure. This structural defect weakens the cell wall, eventually leading to bacterial cell lysis and death. This bactericidal action means it kills the bacteria rather than just stopping its growth.

Common uses and indications

Ampicillin is prescribed to treat a wide range of infections caused by susceptible bacteria. It is important to note that, like all antibiotics, it is ineffective against viral infections such as the common cold or flu.

Commonly treated infections include:

  • Respiratory Tract Infections: Infections of the throat, sinuses, and lungs, including pneumonia.
  • Urinary Tract Infections (UTIs): Caused by susceptible bacteria like E. coli and Proteus mirabilis.
  • Gastrointestinal Infections: Including those caused by Salmonella and Shigella species.
  • Meningitis: An infection of the membranes surrounding the brain and spinal cord.
  • Septicemia and Endocarditis: Severe infections of the bloodstream and heart lining, respectively.

Administration

Ampicillin can be administered through different routes, depending on the severity of the infection and patient needs. Oral administration must be done on an empty stomach to maximize absorption.

  • Oral (capsules or suspension): This route is typically used for less severe infections or as a follow-up after initial intravenous therapy. It is often taken multiple times a day on an empty stomach.
  • Intravenous (IV) or Intramuscular (IM): These routes are reserved for more severe infections or for patients who cannot take oral medication. Parenteral administration often serves as initial therapy for life-threatening conditions before transitioning to an oral form.

Ampicillin vs. Amoxicillin: A key comparison

Ampicillin and amoxicillin are both aminopenicillins with similar mechanisms of action and broad-spectrum activity. However, key differences exist, primarily in their oral absorption and bioavailability.

Feature Ampicillin Amoxicillin
Oral Absorption Less bioavailable; requires an empty stomach for better absorption. More completely and predictably absorbed, can be taken with or without food.
Dosing Frequency Typically dosed more frequently throughout the day. Typically dosed less frequently throughout the day, offering convenience.
Gastrointestinal Side Effects Higher incidence of diarrhea and other GI issues. Lower incidence of diarrhea and stomach upset.
Resistance Combination Often combined with sulbactam (e.g., Unasyn) for injectables to counteract bacterial resistance. Commonly combined with clavulanic acid (e.g., Augmentin) for oral use.

Potential side effects and warnings

Like all medications, ampicillin can cause side effects. Patients with a known allergy to penicillin should not take ampicillin due to the risk of severe, life-threatening anaphylactic reactions.

Common side effects

  • Diarrhea, nausea, and vomiting
  • Skin rash and itching
  • Loss of appetite and abdominal pain
  • Oral candidiasis (thrush)

Serious side effects

  • Severe Allergic Reaction (Anaphylaxis): Characterized by difficulty breathing, swelling, and hives.
  • Clostridioides difficile-Associated Diarrhea (CDAD): An overgrowth of harmful bacteria in the colon, which can range from mild diarrhea to severe colitis.
  • Blood Disorders: Rare but serious reactions, including anemia and low white blood cell count.
  • Seizures: A rare but possible side effect, particularly with high doses or in patients with kidney impairment.

The challenge of antibiotic resistance

Overuse and misuse of antibiotics like ampicillin have led to the development of drug-resistant bacteria. A primary mechanism of resistance is the production of beta-lactamase enzymes by bacteria, which inactivate ampicillin by cleaving its beta-lactam ring. This is why ampicillin is now often combined with a beta-lactamase inhibitor like sulbactam, especially for injectable formulations. Other resistance mechanisms include mutations that alter penicillin-binding proteins.

Conclusion

Ampicillin remains a historically significant and effective broad-spectrum antibiotic, particularly for its activity against a variety of gram-positive and gram-negative bacteria. Its utility in treating serious infections like meningitis, along with common infections of the respiratory and urinary tracts, is well-established. However, its use is more limited today compared to its more bioavailable counterpart, amoxicillin, especially in oral applications, due to increased resistance and a higher incidence of gastrointestinal side effects. Careful use and patient monitoring are crucial to maximize effectiveness and combat the ongoing threat of antibiotic resistance. For serious infections, it is often administered intravenously, sometimes in combination with other agents to overcome resistance.

Frequently Asked Questions

Oral ampicillin should be taken on an empty stomach, at least one hour before or two hours after a meal, with a full glass of water. It is typically prescribed to be taken multiple times a day.

No, ampicillin is an antibiotic and is only effective against bacterial infections. It will not work for viral infections such as the common cold or flu.

While both are aminopenicillins, amoxicillin is better absorbed orally, can be taken with or without food, and has a lower incidence of diarrhea compared to ampicillin. Amoxicillin is more widely prescribed for outpatient oral use.

Common side effects include nausea, vomiting, diarrhea, abdominal pain, and skin rash. Some patients may also experience oral thrush or a sore mouth.

Antibiotic resistance is when bacteria develop the ability to survive and grow despite being exposed to an antibiotic. Some bacteria have become resistant to ampicillin by producing beta-lactamase enzymes that inactivate the drug.

If a dose is missed, it should be taken as soon as remembered. If it is almost time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Double doses should not be taken.

Ampicillin is sometimes used during pregnancy for specific infections, such as Group B streptococcal infections. However, the use of any medication during pregnancy or breastfeeding should always be discussed with a healthcare provider.

The injectable form is used for moderately severe and severe infections, or for patients who are unable to take oral forms. It is commonly used in hospital settings.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.