Effect of food on nitrofurantoin absorption

Bates, Theodore R.; Sequeira, Joel; Tembo, V B S Aubrey

doi:10.1002/cpt1974161part163

Cited by 67 publications

(11 citation statements)

References 4 publications

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“…While the absorption of atenolol is reduced by food (Melander et aI., 1979b), and that of metoprolol and propranolol is increased (Melander et aI., 1977d), plasma concentrations of oxprenolol are unaffected by food whether it is taken as conventional or slow-release tablets (Dawes et a!., 1979). It is not clear whether this is due to the intrinsic properties of the compound, or to the different Reference Welling et al (1980) Melander et al (1977c) Levyet al (1975 Welling and ) Welling et al (1975b) Melander and Wahlin (1978) Tenconi et al (1977) Crounse (1961; Kabasakalian et al (1970) Melander et al (1977b Beerman and Groschinsky-Grind (1978b) Mantyla et al (1980) Jeppson and Sjogren (1975) Munst et al (1980) Ehrsson et al (1979) Melander et al (1977d) Bates et al (1974; Rosenberg and Bates (1976);Mannisto (1978). Melander (1979a) Jordan et al (1981) Melander et al (1977d) Ohnhaus (1980 Levy and Jusko (1966) Levy (1967) Kaumeier (1979); Kaumeier et al (1979) Hasegawa et al (1981 methodologies used in the various studies.…”

Section: Interactions Having No Effect On Drug Absorptionmentioning

confidence: 91%

Interactions Affecting Drug Absorption

Welling¹

1984

Clinical Pharmacokinetics

157

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The influence of drug-drug and drug-food interactions affecting the absorption of orally administered medication is reviewed. Drug-drug interactions can be classified in terms of indirect effects by one drug on gastrointestinal tract physiology influencing the absorption of other drugs, or direct interactions involving altered pH, adsorption, absorption, or chelation. Most, but not all, drug-drug interactions result in reduced or delayed systemic drug availability. Drug-food interactions may result in reduced, delayed, or increased systemic drug availability. The absorption of only a small number of drugs is unaffected by concomitant food intake. The degree of interaction and whether it positively or negatively affects drug absorption depends on a number of factors including the physical and chemical nature of the drug, the formulation, the type of meal, and the time interval between eating and dosing. Mechanisms of drug-food interactions are not well characterised. They clearly involve both direct and indirect factors in a similar fashion to drug-drug interactions, but indirect factors probably predominate. Reduced or delayed drug absorption is generally attributed, at least in part, to delayed stomach-emptying due to food. Increased absorption may also result from delayed stomach-emptying facilitating greater drug dissolution before it passes from the stomach into the small intestine. Increased bioavailability of some drugs, e.g. propranolol, metoprolol and labetalol, may be related to reduced presystemic clearance. The potential clinical implications of drug-drug and drug-food interactions must be taken into account with oral medications in order to minimise variations in systemic drug availability and hence in clinical efficacy.

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Section: Interactions Having No Effect On Drug Absorptionmentioning

confidence: 91%

Interactions Affecting Drug Absorption

Welling¹

1984

Clinical Pharmacokinetics

157

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“…Food intake can influence tablet disintegration, drug dissolution, the rate of gastric emptying, gastrointestinal secretion, and active transport of drugs (Melander, 1978(Melander, , 1981. Such mechanisms are probably responsible for the foodinduced enhancement of the bioavailability of dicoumarol 1hlin, 1978), phenytoin (Johansson et aI., 1983;Melander et aI., I 979a), hydrochlorothiazide (Beermann and GroschinskyGrind, 1978) and nitrofurantoin (Bates et al, 1974), as well as for the food-induced reduction of the bioavailability of isoniazid (Melander et aI., 1976), rifampicin (Acocella, 1978), atenolol (Melander et aI., 1979b) and captopril (Williams and Sugerman, 1982).…”

Section: Influence Of Food Intake On Absorption Of Drugsmentioning

confidence: 97%

Influence of Food Intake on Presystemic Clearance of Drugs

Melander

McLean

1983

Clinical Pharmacokinetics

109

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Many drugs have a low degree of oral bioavailability even though their gastrointestinal absorption is complete. This is because they undergo extensive presystemic metabolic transformation during the first passage of the drug through the gastrointestinal mucosa and the liver. In addition to effects on the absorption of some drugs, food intake has been found to influence the bioavailability of drugs with extensive presystemic metabolic clearance. Extensive presystemic clearance occurs commonly with compounds that are lipophilic bases, e.g. propranolol and amitriptyline, but rarely if ever with lipophilic acids, e.g. salicylic acid and penicillin, except for esters of such acids, e.g. acetylsalicylic acid (aspirin) and pivampicillin. While presystemic clearance of (esterified) acidic drugs is unaffected by food, concurrent food intake markedly reduces presystemic clearance, and thus enhances bioavailability, of several lipophilic bases. Among these are propranolol, metoprolol, labetalol, dixyrazine and hydralazine, which are presystemically metabolised by hydroxylation, glucuronidation and acetylation enzymes systems. In contrast, the bioavailability of lipophilic bases which undergo presystemic dealkylation (amitriptyline, codeine, dextropropoxyphene, prazosin, zimelidine) is unaffected by concurrent food intake. Food intake reduces presystemic clearance of hydralazine and propranolol when these drugs are administered in conventional rapid-release tablets but not when they are given in slow-release formulations. Likewise, coadministration of hydralazine reduces presystemic clearance of rapid-release but not slow-release propranolol. These and other observations favour the view that food may reduce presystemic clearance of (certain) lipophilic basic drugs via transient, complex effects on splanchnic-hepatic blood flow and/or shunt processes, and that the extent of this effect is influenced by the rate of drug delivery to the liver. In addition, these findings refute the notion that the reduced presystemic clearance results from (long-lasting) hepatic enzyme inhibition by some nutrient. On the other hand, repeated intake of specific nutrients (protein) and food contaminants (benzpyrene) can enhance presystemic drug clearance by enzyme induction. Thus, food may exert a dual effect on presystemic drug clearance. A complete evaluation of the influence of food on presystemic drug clearance necessitates bioavailability studies carried out following both single and repeated meals, including different kinds of food prepared by various cooking methods. The influence of food on the presystemic clearance of drugs is most likely to be clinically relevant with drugs having narrow therapeutic margins and/or steep dose-response curves.

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“…The mechanisms causing increased absorption of certain drugs have been rationalized, but not proven, in most cases (Welling, 1977). One explanation suggested for increased absorption is that delayed stomach emptying permits more drug to dissolve in the stomach before it passes into the optimal absorption environment of the small intestine (Bates et al, 1974).…”

Section: Introductionmentioning

confidence: 99%

Influence of food and reduced gastric acidity on the bioavailability of bacampicillin and cefuroxime axetil.

Sommers¹,

Wyk²,

Moncrieff³

et al. 1984

Brit J Clinical Pharma

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1 The present study was designed to investigate the effect of food and of a raised intragastric pH on the bioavailability of two prodrug P-lactam, antibiotics, namely bacampicillin and cefuroxime axetil. 2 Six healthy volunteers participated in an intraindividual comparison of absorption of (a) prodrug, (b) breakfast, followed by prodrug, (c) breakfast, ranitidine and sodium bicarbonate followed by prodrug, and (d) ranitidine and sodium bicarbonate, followed by prodrug. All volunteers were dosed with both bacampicillin and cefuroxime axetil under the above regimens. The drug-free periods between trials were 7 days. 3 Blood samples were obtained before and 20, 40, 60, 90, 120, 150, 180, 210 min and 4, 5, 6, 8 and 10 h after administration. The urine was collected for a period of 10 h after dosing with the antibiotic. An estimation of the relative bioavailability of the drugs under the various regimens was made by comparing the average areas under the serum concentration time curves and also the amounts recovered in the urine.4 Both food and reduced gastric acidity decreased the bioavailability of bacampicillin (as ampicillin) and these variables had an additive lowering effect on the AUC and percentage urinary recovery. Possibly this ester becomes partially hydrolyzed prior to absorption on raising the intragastric pH. Adsorption onto food components or complexing with proteins may also play a role in the reduced bioavailability of bacampicillin in the presence of food. 5 In contrast, the absorption of the cefuroxime ester was enhanced postprandially. This may be rationalized in terms of delayed gastric emptying and gastrointestinal transit which allows more complete dissolution or prolonged residence at the most favourable site of absorption in the intestine. However, the raising of the intragastric pH by the concomittant administration of ranitidine and sodium bicarbonate, reduced the enhanced postprandial absorption. Possibly the good absorption of cefuroxime axetil requires a sufficient low gastric pH to allow the drug to dissolve in the gastric juices.

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Effect of food on nitrofurantoin absorption

Cited by 67 publications

References 4 publications

Interactions Affecting Drug Absorption

Interactions Affecting Drug Absorption

Influence of Food Intake on Presystemic Clearance of Drugs

Influence of food and reduced gastric acidity on the bioavailability of bacampicillin and cefuroxime axetil.

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