Effects of aluminum and magnesium antacids and ranitidine on the absorption of ciprofloxacin

Abstract

The effect of an antacid (Maalox) and ranitidine administration on the absorption of ciprofloxacin was evaluated in healthy male volunteers who were enrolled in three separate studies. Each study was designed at a three- or four-period crossover and included the administration of 750 mg ciprofloxacin alone as a control treatment. Treatments that were evaluated included the administration of ciprofloxacin 5 to 10 minutes, 2 hours, 4 hours, and 6 hours after a single 30 ml dose of antacid; the administration of antacid 2 hours after ciprofloxacin was given; and the administration of ciprofloxacin 2 hours after a 200 mg ranitidine tablet. Administration of antacid within 4 hours before ciprofloxacin dose resulted in a significant decrease in ciprofloxacin absorption (p less than 0.05). Percentages of relative bioavailability compared with control values were 15.1%, 23.2%, and 70% for the 5 to 10 minute, 2 hour, and 4 hour antacid pretreatments, respectively. Administration of antacid 6 hours before or 2 hours after the ciprofloxacin dose did not affect absorption. Ranitidine did not alter ciprofloxacin absorption. Antacids that contain magnesium and aluminum salts may reduce the absorption of ciprofloxacin. The extent of this interaction appears to increase as the time between administration of the two drugs decreases. Ranitidine is suggested as an alternative to antacids for patients receiving treatment with ciprofloxacin.

Effect of <i>Carica papaya</i> (Linn) aqueous leaf extract on pharmacokinetic profile of ciprofloxacin in rabbits

“…Ciprofloxacin is usually well absorbed but in the presence of agents containing some cations, its absorption is impaired [4,17,18]. The leaf of C. Papaya, as demonstrated in this study, contains some cations like Mg, Ca, Na, K, Fe, Cu, Zn and Mn (Table 2); and is line with the work of [19][20][21]; with this, the result of our pharmacokinetic study was not unexpected.…”

“…There are convincing reports that the impairment of the absorption of ciprofloxacin by metal cations is as a result of the formation of a water soluble, non-absorbable metal chelate complex with the 3-carboxyl and 4 keto oxygen groups of the ciprofloxacin molecule which are in close proximity [23,24] thus resulting in very low lipophilicity leading to poor permeation through the gut wall [1,6,17]. The presence of cations in the leaves of C. papaya may be sufficient in impairing the absorption of ciprofloxacin.…”

Effects of magnesium-aluminum hydroxide and calcium carbonate antacids on bioavailability of ofloxacin

“…This phenomenon has been reported to be due to the formation of insoluble chelates in the gastrointestinal tract (5)(6)(7)(9)(10)(11)(12). Although the majority of these interaction studies have investigated the quinolone ciprofloxacin, four reports have suggested the existence of a similar interaction between antacids and ofloxacin (7,12 This study was designed to rigorously characterize the interaction potential between ofloxacin and two commonly used antacid preparations: (i) magnesium-aluminum hydroxide (Maalox; Rorer Pharmaceutical Corp., Fort Washington, Pa.) and (ii) calcium carbonate (Titralac; 3M Riker, St. Paul, Minn.).…”

Norfloxacin interaction with antacids and minerals.

“…Therefore, the 50-90% reductions in urinary excretion of norfloxacin observed in this study following concurrent ingestion of several preparations containing metal ions may be associated with a decreased efficacy of norfloxacin in the treatment of urinary tract and systemic infections. The bioavailability of other quinolone antimicrobials has been shown to be less when they are ingested with antacid or mineral preparations (Kara et al, 1991;Nix et al, 1989b) and binding of metal ions contained in these preparations to the 4 keto and 3 carboxyl groups of quinolones is likely to be responsible Polk et al, 1989). As these chemical groups are common to additional quinolone antimicrobials it is probable that metal ions will have a similar effect on their bioavailability.…”

“…A variety of pharmaceuticals containing metal ions have been shown to interfere with the absorption of another quinolone antimicrobial, ciprofloxacin (Kara et al, 1991;Nix et al, 1989b;Polk et al, 1989). It has also been reported that aluminium containing preparations alone or with magnesium interfere with norfloxacin bioavailability possibly because of the formation of non-absorbable norfloxacin-metal ion complexes (Nix et al, 1989a).…”