Bacampicillin is an oral prodrug belonging to the semisynthetic penicillin class of antibiotics. Bacampicillin is hydrolyzed in the body to Bacampicillin active metabolite, ampicillin. Bacampicillin exerts bactericidal action by inhibiting bacterial cell wall synthesis[1-2]. Bacampicillin is used in research related to infections caused by susceptible bacteria, such as respiratory tract infections, urinary tract infections, and skin and soft tissue infections[3-4].
In vitro, Caco-2 cells were incubated with Bacampicillin (0.2mM) for 5-10 minutes. The cellular uptake rate of Bacampicillin was significantly higher than that of Ampicillin. The transmembrane transport of Bacampicillin significantly increased as the pH of the culture medium was elevated[5].
In vivo, conventional female Swiss mice were orally treated with Bacampicillin (0-3mg/mouse/day) for 4 weeks starting from the 3rd week. The fecal microflora of the mice receiving Bacampicillin was almost unaffected. The interference of Bacampicillin with the normal protective intestinal flora was significantly less than that caused by ampicillin alone or its combination with clavulanic acid[6]. Fasted SPF rats were orally administered Bacampicillin (135mg/kg; single injection). Bacampicillin resulted in higher peak ampicillin concentration levels in the blood, kidneys, liver, and tissue fluid from subcutaneously implanted cages compared to treatment with an equimolar dose of ampicillin. In an experimental mouse infection model, when administered orally Bacampicillin (135mg/kg) 4 hours after infection with Haemophilus influenzae, Bacampicillin demonstrated higher anti-infective activity compared to ampicillin[7].
References:
[1] Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Bacampicillin. 2024 Sep 15.
[2] Scheife RT, Neu HC. Bacampicillin hydrochloride: chemistry, pharmacology, and clinical use. Pharmacotherapy. 1982 Nov-Dec;2(6):313-21.
[3] Neu HC. The pharmacokinetics of bacampicillin. Rev Infect Dis. 1981 Jan-Feb;3(1):110-6.
[4] Sum ZM, Sefton AM, Jepson AP, et al. Comparative pharmacokinetic study between lenampicillin, bacampicillin and amoxycillin. J Antimicrob Chemother. 1989 Jun;23(6):861-8.
[5] Oda M, Fujimoto K, Kobayashi M, et al. Bacampicillin uptake is shared with thiamine in Caco-2 cells. Biol Pharm Bull. 2007 Jul;30(7):1344-9.
[6] Hofstra W, Welling GW, Van der Waaij D. A comparative study of the effect of oral treatment with augmentin, amoxycillin and bacampicillin on the faecal flora in mice. Zentralbl Bakteriol Mikrobiol Hyg A. 1988 Jul;269(1):78-85.
[7] Bodin NO, Ekström B, Forsgren U, et al. Bacampicillin: a new orally well-absorbed derivative of ampicillin. Antimicrob Agents Chemother. 1975 Nov;8(5):518-25.
Bacampicillin是一种口服的前体药物，属于半合成青霉素类抗生素，在体内水解为活性代谢物氨苄西林，Bacampicillin通过抑制细菌细胞壁合成发挥杀菌作用[1-2]。Bacampicillin可用于敏感菌引起的呼吸道感染、泌尿系统感染和皮肤软组织感染等相关研究[3-4]。
在体外，Bacampicillin（0.2mM）孵育Caco-2细胞5-10min，Caco-2细胞对Bacampicillin的摄取率显著高于Ampicillin，Bacampicillin的跨膜转运在培养基pH值升高时显著增加[5]。
在体内，Bacampicillin（0-3mg/小鼠/天）口服处理常规雌性瑞士小鼠（从第3周开始持续4周），Bacampicillin的粪便菌群几乎未受影响，Bacampicillin对肠道正常保护性菌群的干扰远小于氨苄西林及其与克拉维酸的组合[6]。Bacampicillin（135mg/kg；单次）口服处理空腹SPF大鼠，Bacampicillin能使大鼠的血液、肾脏、肝脏以及皮下植入组织笼中的组织液获得更高浓度的氨苄西林峰值水平；在实验性小鼠感染模型中，在感染4小时后给药治疗流感嗜血杆菌感染时，口服给药Bacampicillin（135mg/kg），Bacampicillin显示出比氨苄西林更高的抗感染活性[7]。