Subscribe to RSS
DOI: 10.1055/s-0031-1296404
Antacid Use and Reduced Bioavailability of Oral Drugs
Case studies, overview and perspectivesPublication History
Publication Date:
13 December 2011 (online)
Abstract
A close scrutiny of deployment of the present day home medicines has shown increased indulgence of antacids as a household remedy. While such household interventions are considered innocuous, it could trigger potential drug-drug inter-action(s), if the subject is taking other prescription medicine(s). Examination of the literature indicated that co-administration of antacids may have the potential to cause therapy failures due to reduced oral bioavailability of several drugs. Additionally, fortified foods and beverages with mineral supplement may also have the potential to reduce the bioavailability of oral drugs.
On the basis of this review a number of drugs displayed reduced oral bioavailability in the presence of antacids. However, almost one third of the reviewed drugs showed a drastic bioavailability reduction (< 50%) warranting total avoidance of antacid ingestion in such drug uses. If antacid use is warranted, it needs to be carefully monitored in relation to the administration of the drug (either pre or post drug administration). It appeared that a safe window for antacid administration could be established especially for drugs that display moderate reduction of oral bioavailability. While possible mechanisms explaining the purported antacid-drug interaction are covered, additional perspectives with regard to assessment protocols for antacid-drug interaction are discussed.
-
Literature
- 1 Maton PN, Burton ME. Antacids revisited: review of their clinical pharmacology and recommended therapeutic use. Drugs. 1999; 57: 855-70
- 2 Martin PD, Schneck DW, Dane AL, Warwick MJ. The effect of a combination antacid containing aluminium hydroxise and magnesium hydroxide on rosuvastatin pharmacokinetics. Curr Med Res Opin. 2008; 24: 1231-5
- 3 Khosarvan R, Grabowski B, Wu IT, Joseph-Ridge N, Vernillet L. Effect of food or antacid on pharmacokinetics and pharmacodynamics of febuxostat in healthy subjects. Br J Clin Pharmacol. 2008; 65: 355-63
- 4 Schwartz JI, Agarwal NG, Kher UA, DeSmet M, Cavanaugh Jr. PF, Guillaume M et al Lack of effect of antacids on single-dose pharmacokinetics of etoricoxib. J Clin Pharmacol. 2007; 47: 1342-6
- 5 Krishna G, Kisicki JC, Olsen S, Grasela DM, Wang Z. Effect of an aluminium- and magnesium-containing antacid on the bioavailability of garenoxacin in healthy volunteers. Pharmacother. 2007; 27: 963-9
- 6 Nassr N, Lahu G, Hunnemeyer A, von Richter O, Knoerzer D, Reutter F et al Magnesium hydroxide/aluminium hydroxide-cotaining antacid does not affect the pharmacokinetics of the targeted phosphodiesterase 4 inhibitor roflumilast. J Clin Pharmacol. 2007; 47: 660-6
- 7 Kubitza D, Becka M, Zuehlsdorf M, Mueck W. Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59–7939 (rivaroxaban), an oral director Xa inhibitor, in healthy subjects. J Clin Pharmacol. 2006; 46: 549-58
- 8 Grunder G, Zysset-Aschmann Y, Vollenweider F, Maier T, Krahenbuhl S, Drewe I. Lack of pharmacokinetic interaction between linezolid and antacid in healthy volunteers. Antimicrob Agents Chemother. 2006; 50: 68-72
- 9 Lohitnavy M, Lohitnavy O, Thangkeattiyanon O, Srichai W. Reduced oral itraconazole bioavailability by antacid suspension. J Clin Pharm Ther. 2005; 30: 201-6
- 10 Ford SL, Wire MB, Lou Y, Baker KL, Stein DS. Ffect of antacids and ranitidine on the single-dose pharmacokinetics of fosamprenavir. Antimicrob Agents Chemother. 2005; 49: 467-9
- 11 Nix DE, Adam RD, Auclair B, Krueger TS, Godo PG, Peloquin CA. Pharmacokinetics and relative bioavailability of clofazimine in relation to food, orange juice and antacid. Tuberculosis. 2004; 84: 365-73
- 12 Courtney R, Radwanski E, Lim J, Laughlin M. Pharmacokinetics of posaconazole coadministered with antacid in fasting or nonfasting healthy men. Antimicrob Agents Chemother. 2004; 48: 804-8
- 13 Pletz MW, Petzold P, Allen A, Burkhardt O, Lode H. Effect of calcium carbonate on bioavailability of orally administered gemifloxacin. Antimicrob Agents Chemother. 2003; 47: 2158-60
- 14 Allen A, Vousden M, Porter A, Lewis A. Effect of maalox on the bioavailability of oral gamifloxacin healthy volunteers. Chemother. 1999; 45: 504-11
- 15 Stass H, Bottcher MF, Ochmann K. Evaluation of the influence of antacids and H2 antagonists on the absorption of moxifloxacin after oral administration of a 400 mg dose to healthy volunteers. Clin Pharmacokin. 2001; 40: 39-48
- 16 Snell P, Oo C, Dorr A, Barrett J. Lack of pharmacokinetic interaction between the oral anti-influenza neuraminidase inhibitor prodrug oseltamivir and antacids. Br J Clin Pharmacol. 2002; 54: 372-7
- 17 Auclair B, Nix DE, Adam RD, James GT, Peloquin CA. Pharmacokinetics of ethionamide administered under fasting conditions or with orange juice, food, or antacids. Antimicrob Agents Chemother. 2001; 45: 810-4
- 18 Peloquin CA, Namdar R, Dodge AA, Nix DE. Pharmacokinetics of isoniazid under fasting conditions, with food, and with antacids. Int J Tuberc Lung Dis. 1999; 3: 703-10
- 19 McEwen J, Strauch G, Perles P, Pritchard G, Moreland TE, Necciari J et al Clopidogrel bioavailability: absence of influence of food or antacids. Semin Thromb Hemost. 1999; 25: 47-50
- 20 Lober S, Ziege S, Rau M, Schreiber G, Mignot A, Koeppe P et al Pharmacokinetics of gatifloxacin and interaction with an antacid containing aluminium and magnesium. Antimicrob Agents Chemother. 1999; 43: 1067-71
- 21 Radwanski E, Nomeir A, Cutler D, Affirme M, Lin CC. Pharmacokinetic drug interaction study: administration of Ceftibuten concurrently with the antacid Mylanta double strength liquid or with ranitidine. Am J Ther. 1998; 5: 67-72
- 22 Johnson RD, Dorr MB, Talbot GH, Caile G. Effect of Maalox on the oral absorption of Sparfloxacin. Clin Ther. 1998; 20: 1149-58
- 23 Aideloje SO, Onveji CO, Ugwu NC. Altered pharmacokinetics of halofantrine by an antacid, magnesium carbonate. Eur J Pharm Biopharm. 1998; 46: 299-303
- 24 McEwen J, De Luca M, Casini A, Gich I, Barbanoi MJ, Tost D et al The effect of food and an antacid on the bioavailability of dexketoprofen trometamol. J Clin Pharmacol. 1998; 38: 41S-45S
- 25 Minami R, Nakamura C, Inotsume N, Nakano M. Effects of aluminium hydroxide and famotidine of tsufloxacin in healthy volunteers. Antimicrob Agents Chemother. 1998; 42: 453-5
- 26 Wallace AW, Victory JM, Amsden GW. Lack of bioequiva-lence of gatifloxacin when coadministered with calcium-fortified orange juice in healthy volunteers. J Clin Pharmacol. 43: 92-6
- 27 Neuhofel AL, Wilton JH, Victory JM, Hejmanowski LG, Amsden GW. Lack of bioequivalence of ciprofloxacin when administered with calcium-fortified orange juice: a new twist on an old interaction. J Clin Pharmacol. 2002; 42: 461-6
- 28 Neuvonen PJ, Kivisto KT. Enhancement of drug absorption by antacids. Clin Pharmacokinet. 1994; 27: 120-8
- 29 Tuderman V, Klinge E, Lind H. In vitro evaluations of antacid suspensions marketed in Finland. Acta Pharma Fenn. 1982; 91: 153-73
- 30 Neuvonen PJ, Kivisto KT. Effect of magnesium hydroxide on the absorption of tolfenamic and mefenamic acids. Eur J Clin Pharmacol. 1988; 35: 495-501
- 31 Arayne MS, Sultana N, Hussain F. Interactions between ciprofloxacin and antacids-dissolution and adsorption studies. Drug Metabol Drug Interact. 2005; 21: 117-29