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Inhibitory effects of antibiotics on platelet aggregation in vitro
H Kariyazono1, K Nakamura, T Shinkawa
1Department of Hospital Pharmacy, Faculty of Medicine, Kagoshima University, Japan.
Abstract:
1. We evaluated in vitro inhibitory effects of six types of antibiotic, aztreonam (AZT), cefamandole (CMD), cefmetazole (CMZ), cefotiam (CTM), flomoxef (FMOX) and latamoxef (LMOX), on platelet aggregation, using healthy volunteers' blood. Four types--FMOX, LMOX, CTM and CMD--inhibited, in concentration of 2500 micrograms/ml, the secondary aggregation induced by 3.0 microM adenosine diphosphate (ADP), and also inhibited the aggregation induced by 0.5 micrograms/mi collagen. AZT in the same concentration, did not inhibit the aggregation induced by collagen, and it inhibited only ADP-induced aggregation. CMZ, in the same concentration, inhibited neither of the two aggregations. 2. The inhibitory effects of the antibiotics on collagen-induced aggregation were dependent on the concentration of respective antibiotics. When classified by the strength of inhibitory action, LMOX and FMOX were strong, followed by CTM and CMD. The action of AZT and CMZ was weak. In particular, LMOX showed a 32% inhibitory effect at concentration of 50 micrograms/ml, a level near the blood concentration obtained with clinical usual dose. 3. No relationship was observed between inhibitory effects of antibiotics on ADP- or collagen-induced aggregation and the presence or absence of carboxyl group and/or N-methyltetrazolethiol group in the chemical structure.
Insights
Certain antibiotics, including flomoxef (FMOX) and latamoxef (LMOX), significantly inhibit platelet aggregation. These findings are crucial for understanding potential bleeding risks associated with antibiotic use in patients.
Area of Science:
- Pharmacology
- Hematology
- Microbiology
Background:
- Antibiotics are widely used, and their potential side effects on hemostasis require thorough investigation.
- Platelet aggregation is a critical process in blood clotting, and its inhibition can lead to bleeding complications.
Purpose of the Study:
- To evaluate the in vitro inhibitory effects of six different antibiotics on platelet aggregation.
- To compare the potency of various antibiotics in inhibiting platelet aggregation induced by adenosine diphosphate (ADP) and collagen.
Main Methods:
- In vitro assessment of antibiotic effects on platelet aggregation using blood from healthy volunteers.
- Testing concentrations of 2500 micrograms/ml and 50 micrograms/ml for antibiotics like aztreonam (AZT), cefamandole (CMD), cefmetazole (CMZ), cefotiam (CTM), flomoxef (FMOX), and latamoxef (LMOX).
- Platelet aggregation was induced using adenosine diphosphate (ADP) and collagen.
Main Results:
- Flomoxef (FMOX), latamoxef (LMOX), cefotiam (CTM), and cefamandole (CMD) inhibited secondary ADP-induced and collagen-induced platelet aggregation at 2500 micrograms/ml.
- Aztreonam (AZT) inhibited only ADP-induced aggregation, while cefmetazole (CMZ) showed no significant inhibitory effect.
- Latamoxef (LMOX) demonstrated a notable 32% inhibition at 50 micrograms/ml, a concentration relevant to clinical blood levels.
Conclusions:
- Antibiotics like FMOX and LMOX possess significant in vitro inhibitory effects on platelet aggregation.
- The degree of inhibition varies among antibiotic classes and is concentration-dependent.
- No correlation was found between the chemical structure of the antibiotics and their inhibitory effects on platelet aggregation.