Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

Olajumoke A Olateju1, Chinedum P Babalola1,2, Olujide O Olubiyi3

  • 1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.

Insights

Quinine and chloroquine enhance ampicillin’s antibacterial effectiveness against common co-infections. This study investigated drug interactions, finding additive effects that may improve treatment outcomes for bacterial and malaria co-infections.

Area of Science:

  • Microbiology
  • Pharmacology
  • Infectious Diseases

Background:

  • Bacterial and malaria co-infections are prevalent in malaria-endemic regions.
  • Co-administration of antibiotics and antimalarials is clinically necessary.
  • Anecdotal reports suggest interactions between penicillins and antimalarials, but mechanisms are unclear.

Purpose of the Study:

  • To investigate the in vitro interaction between ampicillin and two quinoline antimalarials (chloroquine, quinine).
  • To determine the effect of these antimalarials on ampicillin's antibacterial activity.
  • To assess the impact of drug combinations on bacterial cell integrity.

Main Methods:

  • Antimicrobial interaction testing: paper strip diffusion, modified disc diffusion, and checkerboard assays.
  • Evaluation of ampicillin-antimalarial combinations against Gram-positive and Gram-negative bacteria.
  • Measurement of potassium ion release to assess bacterial cell integrity.

Main Results:

  • Antimalarials showed minimal intrinsic antibacterial activity, except quinine at high concentrations (bactericidal).
  • Chloroquine and quinine significantly enhanced ampicillin's inhibitory effect, increasing inhibition zones.
  • Interactions were predominantly additive, with Fractional Inhibitory Concentration Indices between 0.5 and 1.

Conclusions:

  • Quinine and chloroquine potentiate the antibacterial activity of ampicillin.
  • These findings have significant implications for the combined clinical use of ampicillin and antimalarials.
  • Further research into ampicillin-antimalarial interactions may optimize treatment strategies for co-infections.

Related Concept Videos

Combined Effects of Drugs: Synergism01:27

Combined Effects of Drugs: Synergism

Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
5.3K
Antimicrobial Proteins01:23

Antimicrobial Proteins

Antimicrobial proteins are important components of the immune system. They aid the body in combating pathogens by either killing them directly or hindering their replication processes. Four main types of antimicrobial substances are interferons, the complement system, iron-binding proteins, and antimicrobial proteins.
Interferons
Interferons (IFNs) are proteins produced by lymphocytes, macrophages, and fibroblasts infected with viruses. While IFNs cannot prevent viruses from entering and...
11.4K
Cholinergic Antagonists: Pharmacokinetics01:24

Cholinergic Antagonists: Pharmacokinetics

Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
635
Gene Regulation in Microbial Communities: Quorum Sensing01:28

Gene Regulation in Microbial Communities: Quorum Sensing

Quorum sensing is a mechanism of bacterial communication that enables coordinated gene expression in response to changes in population density. This facilitates collective behaviors that enhance survival, resource acquisition, and ecological adaptation. This process relies on small signaling molecules called autoinducers that accumulate as bacterial populations grow. When a critical threshold concentration of autoinducers is reached, bacterial cells collectively modify gene expression,...
178
Antimicrobial Effectiveness01:28

Antimicrobial Effectiveness

The effectiveness of antimicrobial agents depends on various factors influencing their ability to eliminate microbial populations. Larger microbial populations require more time for complete eradication, emphasizing the importance of population size analysis when evaluating antimicrobial efficacy.Microbial resistance to antimicrobial agents varies significantly. Highly resilient microorganisms include endospores, gram-negative bacteria, and non-enveloped viruses, while prions are exceptionally...
670
Cholinergic Antagonists: Pharmacological Actions01:28

Cholinergic Antagonists: Pharmacological Actions

Antimuscarinic drugs block muscarinic receptors in multiple systems, including the gut, eye, smooth muscles, respiratory tract, cardiovascular, and central nervous systems. They produce similar effects with varying selectivity depending on the specific agent and tissue. Here are the key pharmacological actions of antimuscarinics:
Gastrointestinal Effects: Antimuscarinics reduce gut contractions, increase gastric emptying, and slow intestinal transit. They partly inhibit gastric acid secretion...
1.3K