Enhancement of drug absorption by antacids. An unrecognised drug interaction.
Antacids are widely used for many disorders. The potential of antacids to interact with other concomitantly ingested drugs is well recognised. These interactions usually result in reduced or delayed absorption of the affected drug. However, this is not always the case. In contrast to aluminium hydroxide, magnesium hydroxide and sodium bicarbonate can enhance the absorption of some drugs. For example, magnesium hydroxide can increase the rate and sometimes even the extent of absorption of certain nonsteroidal anti-inflammatory drugs (e.g. tolfenamic acid, mefenamic acid and ibuprofen), sulphonylurea antidiabetic agents [e.g. glipizide, glibenclamide (glyburide) and tolbutamide] and the oral anticoagulant dicoumarol (bishydroxycoumarin). These weakly acidic drugs are nonionised at gastric pH, but are sparingly water soluble. Elevation of the gastric pH by administration of magnesium hydroxide or sodium bicarbonate increases the solubility and absorption of such sparingly water soluble agents. Chelate formation may be involved in the increased absorption of dicoumarol by magnesium hydroxide. In combination antacids containing both aluminium hydroxide and magnesium hydroxide, the absorption enhancing effect of magnesium hydroxide seems to be counterbalanced by the opposing effects of aluminium hydroxide. The clinical significance of increased drug absorption is not clear. However, accelerated and enhanced absorption of analgesic drugs may be beneficial when rapid pain relief is desired. In contrast, an unexpectedly increased hypoglycaemic or anticoagulant effect may be potentially dangerous. Therefore, a knowledge of the potential effect of antacids on the absorption of other drugs is clinically important.
Department of Clinical Pharmacology, University of Helsinki, Finland.
P J
PJ
Neuvonen
K T
KT
Kivistö
D000042:Absorption; D000863:Antacids / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics; D000925:Anticoagulants / Q000493:pharmacokinetics; D004357:Drug Synergism; D006801:Humans; D010599:Pharmacokinetics; D013453:Sulfonylurea Compounds / Q000493:pharmacokinetics
D000863:Antacids; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000925:Anticoagulants; D013453:Sulfonylurea Compounds