Abstract
Food-drug interactions can be associated with alterations in the pharmacokinetic and pharmacodynamic profile of various drugs that may have clinical implications. The various phases in which food may interact with a coadministered drug are: (i) before and during gastrointestinal absorption; (ii) during distribution; (iii) during metabolism; and (iv) during elimination. Absorption and metabolism are the phases where food has most effect, and this review will focus on those areas. It will also review the variable and complex effects of antacids and metal ions on drug absorption.
Mechanisms related to food effects on drug absorption have been described under 5 categories: those causing decreased, delayed, increased or accelerated absorption, and those in which food has no significant effect. Among the major variables that interface between differential effects of food and postprandial bioavailability are: (i) the physicochemical characteristics and enantiomorphic composition of the drug; (ii) timing of meals in relation to time of drug administration; (iii) size and composition of meals (especially fat, protein and fibre); and (iv) dose size. However, the influence of food is largely a matter of the design of the pharmaceutical formulation. In addition, the mechanism of ‘food effect’ may involve physiological and sensory responses to food, such as changes in gastrointestinal milieu and gastric emptying rate, reflex action, and may also involve the site and route (either portal or lymphatic) of drug absorption.
Mixing drugs with fruit juice, such as grapefruit and orange juice, and acidic beverages, such as commercial soft drinks, may affect absorption because of decreases in gastric pH, which could offer a therapeutic advantage in certain clinical conditions, such as patients with HIV disease and cancer. The increased bioavailability caused by the concomitant intake of grapefruit juice results from the inhibition of intestinal cytochrome P450 (CYP) 3A4, but not hepatic CYP3A4 or colon CYP3A5, which probably involves the bioflavonoid naringenin and furanocoumarins.
Although there is a vast amount of literature, there is still no rational scientific basis to predict the effect of food for a particular chemical entity or a chemical class of therapeutic agents. A mechanistic understanding of the effects of food may serve as a key to the pharmacokinetic optimisation of patient therapy, both in outpatients and hospitalised patients of various age groups.
Similar content being viewed by others
References
Welling PG. Effects of food on drug absorption. Annu Rev Nutr 1996; 16: 383–415.
Piquette-Miller M, Jamali F. Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats. Biopharm Drug Dispos 1997; 18: 543–56.
Pao L-H, Zhou SY, Cook C, et al. Reduced systemic availability of an antiarrhythmic drug, bidisomide, with meal co-administration: relationship with region-dependent intestinal absorption. Pharm Res 1998; 15: 221–7.
Massarella JW, DeFeo TM, Brown AN, et al. The influence of food on the pharmacokinetics and ACE inhibition of cilazapril. Br J Clin Pharmacol 1989; 27 Suppl. 2: 205–9.
Rittig S, Jensen AR, Jensen KT, et al. Desmopressin tablet treatment: factors influencing gastrointestinal absorption. Scand J Urol Nephrol Suppl 1997; 183: 51–2.
Ritting S, Jensen AR, Jensen KT, et al. Effect of food intake on the pharmacokinetics and antidiuretic activity of oral desmopressin (DDAVP) in hydrated normal subjects. Clin Endocrinol 1998; 48: 235–41.
Kindler J, Ruegg PC, Neuray M, et al. Effect of food intake on plasma levels and antihypertensive response during maintenance therapy with endralazine. Eur J Clin Pharmacol 1987; 32: 367–72.
Clancy A, Locke-Haydon J, Cregeen RJ, et al. Effect of concomitant food intake on absorption kinetics of fenoldopam (SK&F 82526) in healthy volunteers. Eur J Clin Pharmacol 1987; 32: 103–6.
Paintaud G, Alvan G, Eckernas SA, et al. The influence of food intake on the effect of two controlled release formulations of furosemide. Biopharm Drug Dispos 1995; 16: 221–32.
McCrindle JL, Li Kam Wa TC, Barron W, et al. Effect of food on the absorption of frusemide and bumetanide in man. Br J Clin Pharmacol 1996; 42: 743–6.
Jackson SH, Shepherd AM, Ludden TM, et al. Effect of food on oral availability of apresoline and controlled release hydralazine in hypertensive patients. J Cardiovasc Pharmacol 1990; 16: 624–8.
Choi RL, Kochak GM, Reydel-Bax P, et al. Effects of food on the bioavailability of CGS 16617, an angiotensin converting enzyme inhibitor, in healthy subjects. J Clin Pharmacol 1988; 28: 848–52.
Ritter W, Wingender W, Hanisch M, et al. Food and muzolimine interaction [in German]. Z Kardiol 1985; 74 Suppl. 2: 145–8.
Buice RG, Subramanian VS, Duchin KL, et al. Bioequivalence of a highly variable drug: an experience with nadolol. Pharm Res 1996; 13: 1109–15.
Buice RG, Subramanian V, Lane E. Bioequivalence of two orally administered nicardipine products. Biopharm Drug Dispos 1996; 17: 471–80.
Wells TG, Sinaiko AR. Antihypertensive effect and pharmacokinetics of nitrendipine in children. J Pediatr 1991; 118: 638–43.
Lecocq B, Funck-Brentano C, Lecocq V, et al. Influence of food on the pharmacokinetics of perindopril and the time course of antgiotensin-converting enzyme inhibition in serum. Clin Pharmacol Ther 1990; 47: 397–402.
Morgan T. Clinical pharmacokinetics and pharmacodynamics of carvedilol. Clin Pharmacokinet 1994 May; 26: 335–46.
Kosoglou T, Kazierad DJ, Schentag JJ, et al. Effect of food on the oral bioavailability of isosorbide-5-mononitrate administered as an extended-release tablet. J Clin Pharmacol 1995; 35: 151–8.
Mazer N, Abisch E, Gfeller JC, et al. Intragastric behavior and absorption kinetics of a normal and ‘floating’ modified-release capsule of isradipine under fasted and fed conditions. J Pharm Sci 1988; 77: 647–57.
Reitberg DP, Love SJ, Quercia GT, et al. Effect of food on nifedipine pharmacokinetics. Clin Pharmacol Ther 1987; 42: 72–5.
Qato MK, Mohammed FA. Effect of food on the comparative bioavailability of two commercially available sustained-release tablet formulations containing nifedipine. STP Pharma Sci 1998; 8: 369–73.
Conway EL, Phillips PA, Drummer OH, et al. Influence of food on the bioavailability of a sustained-release verapamil preparation. J Pharm Sci 1990; 79: 228–31.
Bianchetti G, Bagheri H, Houin G, et al. Pharmacokinetics and bioavailability of diltiazem sustained-release: influence of food and time of administration. Fundam Clin Pharmacol 1995; 9: 197–201.
Wilson CG, Washington N, Greaves JL, et al. Predictive modeling of the behavior of a controlled release buflomedil HC1 formulation using scintigraphic and pharmacokinetic data. Int J Pharm 1991; 72: 79–86.
Sun JX, Cipriano A, Chan K, et al. Effect of food on the relative bioavailability of a hypolipidemic agent (CGP 43371) in healthy subjects. J Pharm Sci 1994; 83: 264–6.
Inskeep PB, Davis KM, Reed AE. Pharmacokinetics of the acyl coenzyme A: cholesterol acyl transferase inhibitor CP-105, 191 in dogs: the effect of food and sesame oil on systemic exposure following oral dosing. J Pharm Sci 1995; 84: 131–3.
Koytchev R, Alken RG, Mayer O, et al. Influence of food on the bioavailability and some pharmacokinetic parameters of diprafenone: a novel antiarrhythmic agent. Eur J Clin Pharmacol 1996; 50: 315–9.
Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am J Health Syst Pharm 1995; 52: 1639–45.
Rosillon D, Stockis A, Poli G, et al. Food effect on the oral bioavailability of manidipine: single dose, randomized, crossover study in healthy male subjects. Eur J Drug Metab Pharmacokinet 1998; 23: 197–202.
Balogh Nemes K, Horvath V, Grezal G, et al. Food interaction pharmacokinetic study of cordaflex 20 mg retard filmtablet in healthy volunteers. Int J Clin Pharmacol Ther 1998; 36: 263–9.
Abrahamsson B, Alpsten M, Bake B, et al. Drug absorption from nifedipine hydrophilic matrix extended-release (ER) tablet — comparison with an osmotic pump tablet and effect of food. J Control Rel 1998; 52: 301–10.
Ueno K, Kawashima S, Uemoto K, et al. Effect of food on nifedipine sustained-release preparation. DICP 1989; 23: 662–5.
Martinez MN, Pelsor FR, Shah VP, et al. Effect of dietary fat content on the bioavailability of a sustained release quinidine gluconate tablet. Biopharm Drug Dispos 1990; 11: 17–29.
Dessager JP. Clinical pharmacokinetics of ticlopidine. Clin Pharmacokinet 1994 May; 26: 347–55.
Deedwania PC, Cheitlin MD, Das SK, et al. Amlodipine once a day in stable angina: double-blind crossover comparison with placebo. Clin Cardiol 1993; 16: 599–602.
Radulovic LL, Cilla DD, Posvar EL, et al. Effect of food on the bioavailability of atorvastatin, an HMG-CoA reductase inhibitor. J Clin Pharmacol 1995; 35: 990–4.
Karam R, Marcello S, Brooks RR, et al. Azimilide dihydrochloride, a novel antiarrhythmic agent. Am J Cardiol 1998; 81 (6A): 40D–6D.
Mooradian AD. Digitalis. An update of clinical pharmacokinetics, therapeutic monitoring techniques and treatment recommendations. Clin Pharmacokinet 1988; 15: 165–79.
Du Souich P, Lery N, Lery L, et al. Influence of food on the bioavailability of diltiazem and two of its metabolites following the administration of conventional tablets and slow-release capsules. Biopharm Drug Dispos 1990; 11: 137–47.
Wilding IR, Hardy JG, Maccari M, et al. Scintigraphic and pharmacokinetic assessment of a multiparticulate sustained release formulation of diltiazem. Int J Pharm 1991; 76: 133–43.
Tenero D, Martin D, Ilson B, et al. Pharmacokinetics of intravenously and orally administered eprosartan in healthy males: absolute bioavailability and effect of food. Biopharm Drug Dispos 1998; 19: 351–6.
Abrahamsson B, Alpsten M, Hugosson M, et al. Absorption, gastrointestinal transit, and tablet erosion of felodipine extended-release (ER) tablets. Pharm Res 1993; 10: 709–14.
Vachharajani NN, Shyu WC, Mantha S, et al. Lack of effect of food on the oral bioavailability of irbesartan in healthy male volunteers. J Clin Pharmacol 1998; 38: 433–6.
van den Berg G, van Steveninck F, Gubbens-Stibbe JM, et al. Influence of food on the bioavailability of metoprolol from an OROS system: a study in healthy volunteers. Eur J Clin Pharmacol 1990; 39: 315–6.
Rimoy GH, Idle JR, Bhaskar NK, et al. The influence of food on the pharmacokinetics of ‘biphasic’ nifedipine at steady state in normal subjects. Br J Clin Pharmacol 1989; 28: 612–5.
Armstrong J, Challenor VF, Macklin BS, et al. The influence of two types of meal on the pharmacokinetics of a modified-re-lease formulation of nifedipine (Adalat Retard). Eur J Clin Pharmacol 1997; 53: 141–3.
Holm V, Melander A, Wahlin-Boll E. Influence of food and age on nitrazepam kinetics. Drug Nutr Interact 1982; 1: 307–11.
Junginger HE, Verhoeven J, Danhof M. Oral controlled drug delivery systems based on microporous polymers. Drug Dev Ind Pharm 1989; 15: 1059–72.
Berdai D, Demotes-Mainard F, Philip F, et al. Influence of food and body weight on the pharmacokinetics of penticainide. Fundam Clin Pharmacol 1994; 8: 453–7.
Haegele KD, Hinze C, Joder-Ohlenbusch AM, et al. Effects of a standardized meal on the pharmacokinetics of the new cardiotonic agent piroximone. Arzneimittel Forschung 1991; 41: 1225–9.
Quion JA, Jones PH. Clinical pharmacokinetics of pravastatin. Clin Pharmacokinet 1994 Aug; 27 (2): 94–103.
Dahlström U, Graffner C, Johnsson U, et al. Pharmacokinetics of prenalterol after single and multiple administration of controlled release tablets to patients with congestive heart failure. Eur J Clin Pharmacol 1983; 24: 495–502.
Rocci ML, Mojaverian P, Davis RJ, et al. Food-induced gastric retention and absorption of sustained release procainamide. Clin Pharmacol Ther 1987; 42: 45–9.
Ferry JJ, Horvath AM, Sedman AJ, et al. Influence of food on the pharmacokinetics of quinapril and its active diacid metabolite, Cl-928. J Clin Pharmacol 1987; 27: 397–9.
Boberg M, Ahra H-J, Beckermann B, et al. Pharmacokinetics and metabolism of the new thromboxane A2 receptor antagonist ramatroban in animals. 1 st communication: absorption, concentrations in plasma, metabolism, and excretion after single administration to rats and dogs. Arzneimittel Forschung 1997; 47: 928–38.
Lee I-D, Hunt TL, Bradley CR, et al. Effects on the pharmacokinetics and pharmacodynamics in the elderly of coadministering ramipril with water, apple juice, and apple sauce. Pharm Res 1996; 13: 639–42.
Hashiguchi M, Ogata H, Maeda A, et al. No effect of high-protein food on the stereoselective bioavailability and pharmacokinetics of verapamil. J Clin Pharmacol 1996; 36: 1022–8.
Gupta SK, Yih BM, Atkinson L, et al. The effect of food, time of dosing, and body position on the pharmacokinetics and pharmacodynamics of verapamil and norverapamil. J Clin Pharmacol 1995; 35: 1083–93.
Gottfries J, Svenheden A, Alpsten M, et al. Gastrointestinal transit of amoxicillin modofied-release tablets and a placebo tablet including pharmacokinetic assessments of amoxicillin. Scand J Gastroenterol 1996; 31: 49–53.
Wan XX, Xia ZQ, Zhang L. Influence of food on bioavailability of ciprofloxacin. Chin J Hosp Pharm 1993; 13: 17–8.
Digenis GA, Sandefer EP, Parr AF, et al. Gastrointestinal behavior of orally administered radiolabeled erythromycin pellets in man as determined by gamma scintigraphy. J Clin Pharmacol 1990; 30: 621–31.
Randinitis EJ, Sedman AJ, Welling PG, et al. Effect of a high-fat meal on the bioavailability of a polymer-coated erythromycin particle tablet formulation. J Clin Pharmacol 1989; 29: 79–84.
Peloquin CA, Bulpitt AE, Jaresco GS, et al. Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids. Antimicrob Agents Chemother 1999; 43: 568–72.
Yeh KC, Deutsch PJ, Haddix H, et al. Single-dose pharmacokinetics of indinavir and the effect of food. Antimicrob Agents Chemother 1998; 42: 332–8.
Zent C, Smith P. Study of the effect of concomitant food on the bioavailability of rifampicin, isoniazid and pyrazinamide. Tuber Lung Dis 1995; 76: 109–13.
Van de Velde VJS, Van Peer AP, Heykants JJP, et al. Effect of food on the pharmacokinetics of a new hydroxypropyl-β-cyclodextrin formulation of itraconazole. Pharmacotherapy 1996; 16: 424–8.
Osman MA, Patel RB, Schuna A, et al. Reduction in oral penicillamine absorption by food, antacid and ferrous sulfate. Clin Pharmacol Ther 1983; 33: 465–70.
D’Angelo L, De Ponti F, Crema F, et al. Effect of food on the bioavailability of pidotimod in healthy volunteers. Arzneimittel Forschung 1994; 44: 1473–5.
Nazareno LA, Holazo AA, Limjuco R, et al. The effect of food on pharmacokinetics of zalcitabine in HIV-positive patients. Pharm Res 1995; 12: 1462–5.
Borin MT, Forbes KK, Hughes GS. The bioavailability of cefpodoxime proxetil tablets relative to an oral solution. Biopharm Drug Dispos 1995; 16: 295–302.
Kearns GL, Abdel-Rahman SM, Jacobs RF, et al. Cefpodoxime pharmacokinetics in children: effect of food. Pediatr Infect Dis J 1998; 17: 799–804.
Zimmermann T, Yeates RA, Albrecht M, et al. Influence of concomitant food intake on the gastrointestinal absorption of fluconazole and itraconazole in Japanese subjects. Int J Clin Pharmacol Res 1994; 14: 87–93.
Lelawongs P, Barone JA, Colaizzi JL, et al. Effect of food and gastric acidity on absorption of orally administered ketoconazole. Clin Pharm 1988; 7: 228–35.
Lee LJ, Hafkin B, Lee ID, et al. Effects of food and sucralfate on a single oral dose of 500 milligrams of levofloxacin in healthy subjects. Antimicrob Agents Chemother 1997; 41: 2196–200.
Granneman GR, Mukherjee D. Effect of food on the bioavailability of temafloxacin: a review of 3 studies. Clin Pharmacokinet 1992; 22 Suppl. 1: 48–56.
Awadzi K, Hero M, Opoku NO, et al. The chemotherapy of onchocerciasis XVII. A clinical evaluation of albendazole in patients with onchocerciasis: effects of food and pretreatment with ivermectin on drug response and pharmacokinetics. Trop Med Parasitai 1994; 45: 203–8.
Lange H, Eggers R, Bircher J. Increased systemic availability of albendazole when taken with a fatty meal. Eur J Clin Pharmacol 1988; 34: 315–7.
Dixon R, Pozniak AL, Watt HM, et al. Single-dose and steadystate pharmacokinetics of a novel microfluidized suspension of atovaquone in human immunodeficiency virus-seropositive patients. Antimicrob Agents Chemother 1996; 40: 556–60.
Emori H, Yamamoto K, Yokohama S, et al. Bioavailability of bropirimine 250 mg tablet in dogs: effect of food. J Pharm Pharmacol 1995; 47: 822–6.
Lode H, Fassbender M, Schaberg T, et al. Comparative pharmacokinetics of the new oral cephalosporins. Drugs 1994; 47 Suppl. 3: 10–9.
Hughes GS, Heald DL, Barker KB, et al. The effects of gastric pH and food on the pharmacokinetics of a new oral cephalosporin, cefpodoxime proxetil. Clin Pharmacol Ther 1989; 46: 674–85.
Borin MT, Driver MR, Forbes KK. Effect of timing of food on absorption of cefpodoxime proxetil. J Clin Pharmacol 1995; 35: 505–9.
Finn A, Straughn A, Meyer M, et al. Effect of dose and food on the bioavailability of cefuroxime axetil. Biopharm Drug Dispos 1987; 8: 519–26.
Chen RR, Lee TY, Hsieh WC. Effect of food on pharmacokinetics of cefuroxime axetil in Chinese subjects. JFormos Med Assoc 1992; 91: 1171–81.
Schaad-Lanyi Z, Dieterle W, Dubois JP, et al. Pharmacokinetics of clofazimine in healthy human volunteers. Int J Leprosy 1987; 55: 9–15.
Lavelle J, Follansbee S, Trapnell CB, et al. Effect of food on the relative bioavailability of oral ganciclovir. J Clin Pharmacol 1996; 36: 238–41.
Griffy KG. Pharmacokinetics of oral ganciclovir capsules in HIV-infected persons. AIDS 1996; 10 Suppl. 4: 3–6.
Khalafalla N, Elgholmy ZA, Khalil SA. Influence of high fat diet on GI absorption of griseofulvin tablets in man. Pharmazie 1981; 36: 692–3.
Humberstone AJ, Porter CJ, Charman WN. Physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine. J Pharm Sci 1996; 85: 525–9.
Milton KA, Edwards G, Ward SA, et al. Pharmacokinetics of halofantrine in man: effects of food and dose size. Br J Clin Pharmacol 1989; 28: 71–7.
Zimmermann T, Yeates RA, Laufen H, et al. Influence of concomitant food intake on the oral absorption of two triazole antifungal agents, itraconazole and fluconazole. Eur J Clin Pharmacol 1994; 46: 147–50.
Crevoisier C, Handschin J, Barre J, et al. Food increases the bioavailability of mefloquine. Eur J Clin Pharmacol 1997; 53: 135–9.
Quart BD, Chapman SK, Peterkin J, et al. Phase I safety, tolerance, pharmacokinetics and food effect studies of AG1343: a novel HIV protease inhibitor [abstract no. LB3]. 2nd National Conference on Human Retrovirus and Related Infections; 1995 Jan 29–Feb 2; Washington, DC.
Abdel-Rahman SM, Kearns GL. Single-dose pharmacokinetics of pleconaril (VP 63843) oral solution and effect of food. Antimicrob Agents Chemother 1998; 42: 2706–9.
Saathoff A, Lode H, Hampel B, et al. Pharmacokinetics of FCE 22891, a new oral penem. Antimicrob Agents Chemother 1990; 34: 1001–6.
Muirhead GJ, Shaw T, Williams PEO, et al. Pharmacokinetics of the HIV-proteinase inhibitor, Ro 318959, after single and multiple oral doses in healthy volunteers [abstract]. Br J Clin Pharmacol 1992; 34: 170P.
Kenyon CJ, Brown F, McClelland GR, et al. The use of pharmacoscintigraphy to elucidate food effects observed with a novel protease inhibitor. Pharm Res 1998; 15: 417–22.
Nedelman J, Cramer JA, Robbins B, et al. The effect of food on the pharmacokinetics of multiple-dose terbinafine in young and elderly healthy subjects. Biopharm Drug Dispos 1997; 18: 127–38.
Lecaillon JB, Godbillon J, Campestrini J, et al. Effect of food on the bioavailability of triclabendazole in patients with fascioliasis. Br J Clin Pharmacol 1998; 45: 601–4.
Cundy KC, Sue IL, Visor GC, et al. Oral formulations of adefovir dipivoxil: in vitro dissolution and in vivo bioavailability in dogs. J Pharm Sci 1997; 86: 1334–8.
Dien TK, de Vries PJ, Khanh NX, et al. Effect of food intake on pharmacokinetics of oral artemisinin in healthy Vietnamese subjects. Antimicrob Agents Chemother 1997; 41: 1069–72.
Foulds G, Luke DR, Teng R, et al. The absence of an effect of food on the bioavailability of azithromycin administered as tablets, sachet or suspension. J Antimicrob Chemother 1996; 37 Suppl. C: 37–44.
Faulkner RD, Bohaychuk W, Haynes JD, et al. The pharmacokinetics of cefixime in the fasted and fed state. Eur J Clin Pharmacol 1988; 34: 525–8.
Barriere SL. Pharmacology and pharmacokinetics of cefprozil. Clin Infect Dis 1992; 14 Suppl. 2: 184–8.
Umemura K, Ikeda Y, Kondo K, et al. Safety and pharmacokinetics of CS-834, a new oralcarbapenem antibiotic, in healthy volunteers. Antimicrob Agents Chemother 1997; 41: 2664–9.
Rao N, Eller M, Arumugham T, et al. The effect of food on the relative bioavailability of deflazacort. Eur J Drug Metab Pharmacokinet 1996; 21: 241–5.
Lehto P, Kivisto KT. Effects of milk and food on the absorption of enoxacin. Br J Clin Pharmacol 1995; 39: 194–6.
Nielsen P, Gyrd-Hansen N. Bioavailability of enrofloxacin after oral administration to fed and fasted pigs. Pharmacol Toxicol 1997; 80: 246–50.
Bertino Jr JS, Nafziger AN, Wong M, et al. Effect of a fat- and calcium-rich breakfast on pharmacokinetics of fleroxacin administered in single and multiple doses. Antimicrob Agents Chemother 1994; 38: 499–503.
Lepore AM, Bonardi G, Maggi GC. Influence of food on the absorption of flurithromycin in man. Int J Clin Pharmacol Res 1988; 8: 253–7.
Efthymiopoulos C, Bramer SL, Maroli A. Effect of food and gastric pH on the bioavailability of grepafloxacin. Clin Pharmacokinet 1997; 33 Suppl. 1: 18–24.
Angel JB, Hussey EK, Hall ST, et al. Pharmacokinetics of 3TC (GR-109714X) administered with and without food to HIV-infected patients. Drug Invest 1993; 6: 70–4.
Washington N, Lamont G, Wilson CG, et al. The effect of high and low fat meals on the absorption of rifampicin from the gastrointestinal tract in volunteer subjects. Int J Pharm 1994; 108: 125–32.
Hsu A, Granneman GR, Bertz RJ. Ritonavir: clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 1998 Oct; 35: 275–91.
Kaul S, Christofalo B, Raymond RH, et al. Effect of food on the bioavailability of stavudine in subjects with human immunodeficiency virus infection. Antimicrob Agents Chemother 1998; 42: 2295–8.
Eller MG, Walker BJ, Yuh L, et al. Absence of food effects on the pharmacokinetics of terfenadine. Biopharm Drug Dispos 1992; 13: 171–7.
Teng R, Dogolo LC, Willavize SA, et al. Oral bioavailability of trovafloxacin with and without food in healthy volunteers. J Antimicrob Chemother 1997; 39 Suppl. B: 87–92.
Peck RW, Wootton R, Wiggs R, et al. Effect of food and gender on the pharmacokinetics of tucaresol in healthy volunteers. Br J Clin Pharmacol 1998; 46: 83–6.
Marathe PH, Greene DS, Lee JS, et al. Assessment of effect of food, gender, and intra-subject variability in the pharmacokinetics of avitriptan. Biopharm Drug Dispos 1998; 19: 153–7.
Marathe PH, Sandefer EP, Kollia GE, et al. In vivo evaluation of the absorption and gastrointestinal transit of avitriptan in fed and fasted subjects using gamma scintigraphy. J Pharmacokinet Biopharm 1998; 26: 1–20.
Bjornsson TD, Troetel WM, Imbimbo BR Effect of food on the absorption of eptastigmine. Eur J Clin Pharmacol 1998; 54: 243–7.
Contin M, Riva R, Martinelli P, et al. Effect of meal timing on the kinetic-dynamic profile of levodopa/carbidopa controlled release in parkinsonian patients. Eur J Clin Pharmacol 1998; 54: 303–8.
Welty DF, Siedlik PH, Posvar EL, et al. The temporal effect of food on tacrine bioavailability. J Clin Pharmacol 1994; 34: 985–8.
Fleishaker JC, Phillips JP, Lau HS. Effect of food on the bioavailability of adinazolam from a sustained release formulation: effect of meal timing and lack of dose dumping. Biopharm Drug Dispos 1990; 11: 715–27.
Drewe J, Mazer N, Abisch E, et al. Differential effect of food on kinetics of bromocriptine in a modified release capsule and a conventional formulation. Eur J Clin Pharmacol 1988; 35: 535–41.
Lippert C, Keung A, Arumugham T, et al. The effect of food on the bioavailability of dolasetron mesylate tablets. Biopharm Drug Dispos 1998; 19: 17–9.
Schoerlin MP, Mayersohn M, Hoevels B, et al. Effect of food intake on the relative bioavailability of moclobemide (Ro 11-1163). J Neural Transm Suppl 1988; 26: 115–21.
Takahashi H, Ogata H, Nagai N, et al. Variability in absorption lag time of pyridoxal phosphate under fasting and pre- and postmeal conditions. Biopharm Drug Dispos 1994; 15: 505–17.
Cheng H, Polvino WJ, Sciberras D, et al. Pharmacokinetics and food interaction of MK-462 in healthy males. Biopharm Drug Dispos 1996; 17: 17–24.
Dresse A, Rosen JM, Brems H, et al. Influence of food on tianeptine and its main metabolite kinetics. J Clin Pharmacol 1988; 28: 1115–9.
Troy SM, Parker VP, Hicks DR, et al. Pharmacokinetics and effect of food on the bioavailability of orally administered venlafaxine. J Clin Pharmacol 1997; 37: 954–61.
Dingemanse J, Kleinbloesem CH, Crevoisier C, et al. Pharmacokinetic studies with a dual-release formulation of levodopa, a novel principle in the treatment of Parkinson’s disease. Eur Neurol 1998; 39: 119–24.
Lukkari E, Castren-Kortekangas P, Juhakoski A, et al. Effect of food on the bioavailability of oxybutynin from a controlled release tablet. Eur J Clin Pharmacol 1996; 50: 221–3.
Lubowskil T, Bertino JS, Shin IS, et al. Effect of food on the oral absorption of a generic carbamazepine [abstract]. American Society of Hospital Pharmacists Midyear Clinical Meeting: 1989 Dec 3–7; Atlanta. CR-10.
Liedholm H, Liden A, Kroon L, et al. Pharmacokinetics of dixyrazine: low bioavailability, improved by food intake. Drug Nutr Interact 1985; 3: 87–92.
Drake J, Kirkpatrick CT, Aliyar CA, et al. Effect of food on the comparative pharmacokinetics of modified-release morphine tablet formulations: Oramorph SR and MST Continus. Br J Clin Pharmacol 1996; 41: 417–20.
Gourlay GK, Plummer JL, Cherry DA, et al. The reproducibility of bioavailability of oral morphine from solution under fed and fasted conditions. J Pain Symptom Manage 1991; 6: 431–6.
Bozigian HP, Pritchard JF, Gooding AE, et al. Ondansetron absorption in adults: effect of dosage form, food, and antacids. JPharm Sci 1994; 83: 1011–3.
Cardot J-M, Lecaillon J-B, Czendlik C, et al. The influence of food on the disposition of the antiepileptic rufinamide in healthy volunteers. Biopharm Drug Dispos 1998; 19: 259–62.
Mahmood I. Clinical pharmacokinetics and pharmacodynamics of selegiline. Clin Pharmacokinet 1997 Aug; 33: 91–102.
Ingwersen SH, Mant TG, Larsen JJ. Food intake increases the relative oral bioavailability of vanoxerine. Br J Clin Pharmacol 1993; 35: 308–10.
Hamelin BA, Allard S, Laplante L, et al. The effect of timing of a standard meal on the pharmacokinetics and pharmacodynamics of the novel atypical antipsychotic agent ziprasidone. Pharmacotherapy 1998; 18: 9–15.
Aaes-Jorgensen T, Liedholm H, Melander A. Influence of food intake on the bioavailability of zuclopenthixol. Drug Nun-Interact 1987; 5: 157–60.
Eller MG, Della-Coletta AA. Absence of effect of food on alprazolam absorption from sustained release tablets. Biopharm Drug Dispos 1990; 11: 31–7.
Peterson GM, McLean S, Millingen KS. Food does not affect the bioavailability of baclofen. Med J Aust 1985; 142: 689–90.
Srinivas NR, Shyu WC, Lee J, et al. Lack of effect of food on the steady state pharmacokinetics of BMS-181101, an antidepressant, in healthy subjects. Biopharm Drug Dispos 1997; 18: 585–93.
Kopitar Z, Vrhovac B, Povšiè L, et al. The effect of food and metoclopramide on the pharmacokinetics and side effects of bromocriptine. Eur J Drug Metab Pharmacokinet 1991; 16: 177–81.
Persiani S, Rocchetti M, Pacciarini MA, et al. The effect of food on cabergoline pharmacokinetics and tolerability in healthy volunteers. Biopharm Drug Dispos 1996; 17: 443–55.
Retzow A, Schurer M, Schulz HU. Influence of food on the bioavailability of a carbamazepine slow-release formulation. Int J Clin Pharmacol Ther 1997; 35: 557–60.
Cenraud B, Guyot M, Levy RH, et al. No effect of food intake on clobazam absorption. Br J Clin Pharmacol 1983; 16: 728–30.
Van Harten J, Van Bemmel P, Dobrinska MR, et al. Bioavailability of fluvoxamine given with and withoutfood. Biopharm Drug Dispos 1991; 12: 571–6.
Gidal BE, Maly MM, Kowalski JW, et al. Gabapentin absorption: effect of mixing with foods of varying macronutrient composition. Ann Pharmacother 1998; 32: 405–9.
Benetello P, Fuflanut M, Fortunato M, et al. Oral gabapentin disposition in patients with epilepsy after a high-protein meal. Epilepsia 1997; 38: 1140–2.
Sainati SM, Hubbard JW, Chi E, et al. Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol 1995; 35: 713–20.
Umemura K, Konda K, Ikeda Y, et al. Pharmacokinetics and safety of JTP-4819, a novel specific orally active prolyl endopeptidase inhibitor, in healthy male volunteers. Br J Clin Pharmacol 1997; 43: 613–8.
Malcolm SL, Allen JG, Bird H, et al. Single-dose pharmacokinetics of Madospar HBS in patients and effect of food and antacid on the absorption of Madopar HBS in volunteers. Eur Neurol 1987; 27 Suppl. 1: 28–35.
Kaiko RF, Lazarus H, Cronin C, et al. Controlled-release morphine bioavailability (MS Contin tablets) in the presence and absence of food. Hosp J 1990; 6: 17–30.
Kaiko RF. The effect of food intake on the pharmacokinetics of sustained-release morphine sulfate capsules. Clin Ther 1997; 19: 296–303.
Dockens RC, Greene DS, Barbhaiya RH. The lack effect of food on the bioavailability of nefazodone tablets. Biopharm Drug Dispos 1996; 17: 135–43.
Benziger DP, Kaiko RF, Miotto JB, et al. Differential effects of food on the bioavailability of controlled-release oxycodone tablets and immediate-release oxycodone solution. J Pharm Sci 1996; 85: 407–10.
Nemeroff CB. Paroxetine: an overview of the efficacy and safety of a new selective serotonin reuptake inhibitor in the treatment of depression. J Clin Psychopharmacol 1993; 13 (6 Suppl.): 10S–7S.
Dostert P, Benedetti MS, Poggesi I. Review of the pharmacokinetics and metabolism of reboxetine, a selective noradren-aline reuptake inhibitor. Eur Neuropsychopharmacol 1997; 7 Suppl. 1: 23–35.
Brefel C, Thalamas C, Rayet S, et al. Effect of food on the pharmacokinetics of ropinirole in parkinsonian patients. Br J Clin Pharmacol 1998; 45: 412–5.
Wong SL, Linnen P, Mack R, et al. Effects of food, antacids, and dosage form on the pharmacokinetics and relative bioavailability of sertindole in healthy volunteers. Biopharm Drug Dispos 1997; 18: 533–41.
Ronfeld RA, Wilner KD, Baris BA. Sertraline. Chronopharmacokinetics and the effect of coadministration with food. Clin Pharmacokinet 1997; 32 Suppl. 1: 50–5.
Hutchinson DR. Modified release tizanidine: a review. J Int Med Res 1989; 17: 565–73.
Doose DR, Walker SA, Gisclon LG, et al. Single-dose pharmacokinetics and effect of food on the bioavailability of topiramate, a novel antiepileptic drug. J Clin Pharmacol 1996; 36: 884–91.
Kirsten R, Nelson K, Molz KH, et al. Influence of food intake on the bioavailability of urapidil in healthy volunteers. Int J Clin Pharmacol Ther Toxicol 1989; 27: 298–301.
Retzow A, Vens-Cappell B, Wangemann M. Influence of food on the pharmacokinetics of a new multiple unit sustained release sodium valproate formulation. Arzneimittel Forschung 1997; 47: 1347–50.
Puri SK, Hsu RS, Ho I, et al. The effect of food on the bioavailability of velnacrine (HP 029) in healthy elderly men: a potential Alzheimer agent. J Clin Pharmacol 1989; 29: 956–60.
Rey E, Pons G, Olive G. Vigabatrin: clinical pharmacokinetics. Clin Pharmacokinet 1992 Oct; 23: 267–78.
Seaber EJ, Peck RW, Smith DA, et al. The absolute bioavailability and effect of food on the pharmacokinetics of zolmitriptan in healthy volunteers. Br J Clin Pharmacol 1998; 46: 433–9.
Birkett DJ, Lines DR, Kneebone GM, et al. Effects of time of dose in relation to food on the bioavailability of Theo-Dur Sprinkle at steady state in asthmatic children. Clin Pharmacol Ther 1989; 45: 305–11.
Fujimura A, Shiga T, Kumagai Y, et al. Effect of food intake on pharmacokinetics and effects of a new thromboxane A2 receptor antagonist, S-1452. Eur J Clin Pharmacol 1996; 50: 311–4.
Uematsu T, Nagashima S, Inaba H, et al. Pharmacokinetic and pharmacodynamic profiles of CS-518, a selective, long-lasting thromboxane synthase inhibitor, after single and multiple oral administration to healthy volunteers. J Clin Pharmacol 1994; 34: 41–7.
Spangler DL, Lutz CN, Tinkelman D. The effect of diet on the efficacy onset and duration of action of procaterol hydrochloride tablets. Ann Allergy 1987; 58: 59–62.
Hussey EK, Donn KH, Powell JR, et al. Albuterol extended-release products: effect of food on the pharmacokinetics of single oral doses of Volmax® and Proventil® Repetabs® in healthy male volunteers. J Clin Pharmacol 1991; 31: 561–4.
Delhotal-Landes B, Flouvat B, Boutin MS, et al. Influence of food on the absorption of theophylline administered in the form of sustained release tablet and microgranules. Biopharm Drug Dispos 1988; 9: 19–29.
Schoors DF, De Smet M, Reiss T, et al. Single-dose pharmacokinetics, safety and tolerability of MK-0476, a new leukotriene D4-receptor antagonist, in healthy volunteers. Br J Clin Pharmacol 1995; 40: 277–80.
Edsbäcker S, Wollmer P, Nilsson Å, et al. Pharmacokinetics and gastrointestinal transit of budesonide controlled ileal release (CIR) capsules [abstract]. Gastroenterology 1993; 104 Suppl.: A695.
Cvetkovic S, Edsbäcker S, Wollmer P, et al. Food does not alter site of absorption of budesonide from controlled ileal release capsules [abstract]. Gut 1995; 37 Suppl. 2: A51.
Schran HF, Petryk L, Chang CT, et al. The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations. J Clin Pharmacol 1996; 36: 911–22.
Nomeir AA, Mojaverian P, Kosoglou T, et al. Influence of food on the oral bioavailability of loratadine and pseudoephedrine from extended-release tablets in healthy volunteers. J Clin Pharmacol 1996; 36: 923–30.
Lee DA, Taylor GM, Walker JG, et al. The effect of food and tablet formulation on plasma prednisolone levels following administration of enteric-coated tablets. Br J Clin Pharmacol 1979; 7: 523–8.
Chao ST, Prather D, Pinson D, et al. Effect of food on bioavailability of pseudoephedrine and brompheniramine administered from a gastrointestinal therapeutic system. J Pharm Sci 1991; 80: 432–5.
Pabst G, Weber W, Muller M, et al. Study on the influence of food on the absorption of theophylline from a controlled-release preparation. Arzneimittel Forschung 1994; 44: 333–7.
Gonzalez MA, Straughan AB. Effect of meals and dosage-form modification on theophylline bioavailability from a 24-hour sustained-release delivery system. Clin Ther 1994; 16: 804–14.
Ürmös I, Grézal Gy, Balogh Nemes K, et al. Food interaction study of a new theophylline (Egifilin) 200 and 400 mg retard tablet in healthy volunteers. Int J Clin Pharmacol Ther 1997; 35: 65–70.
Awni WM, Cavanaugh JH, Witt G, et al. Effect of food on the pharmacokinetics of zileuton. Clin Pharmacokinet 1995; 29 Suppl. 2: 62–6.
Reigner B, Verweij J, Dirix L, et al. Effect of food on the pharmacokinetics of capecitabine and its metabolites following oral administration in cancer patients. Clin Cancer Res 1998; 4: 941–8.
Gunnarsson PO, Davidsson T, Andersson SB, et al. Impairment of estramustine phosphate absorption by concurrent intake of milk and food. Eur J Clin Pharmacol 1990; 38: 189–93.
Riccardi R, Balis FM, Ferrara P, et al. Influence of food intake on bioavailability of oral 6-mercaptopurine in children with acute lymphoblastic leukemia. Pediatr Hematol Oncol 1986; 3: 319–24.
Dupuis LL, Koren G, Silverman ED, et al. Influence of food on the bioavailability of oral methotrexate in children. J Rheumatol 1995; 22: 1570–3.
Rowinsky EK, Lucas VS, Hsieh AL, et al. The effects of food and divided dosing on the bioavailability of oral vinorelbine. Cancer Chemother Pharmacol 1996; 39: 9–16.
Sioufi A, Sandrenan N, Godbillon J, et al. Comparative bioavailability of letrozole under fed and fasting conditions in 12 healthy subjects after a 2.5mg single oral administration. Biopharm Drug Dispos 1997; 18: 489–97.
Mueller EA, Kovarik JM, Van Bree JB, et al. Influence of a fat-rich meal on the pharmacokinetics of a new oral formulation of cyclosporine in a crossover comparison with the market formulation. Pharm Res 1994; 11: 151–5.
Doose DR, Minn FL, Stellar S, et al. Effects of meals and meal composition on the bioavailability of fenretinide. J Clin Pharmacol 1992; 32: 1089–95.
Cockshott ID, Oliver SD, Young JJ, et al. The effect of food on the pharmacokinetics of the bicalutamide (‘Casodex’) enantiomers. Biopharm Drug Dispos 1997; 18: 499–507.
Steiner JF. Clinical pharmacokinetics and pharmacodynamics of finasteride. Clin Pharmacokinet 1996 Jan; 30: 16–27.
Hamilton RA, Kremer JM. The effects of food on methotrexate absorption. J Rheumatol 1995; 22: 630–2.
Bannwarth B, Pehourcq F, Schaeverbeke T, et al. Clinical pharmacokinetics of low-dose pulse methotrexate in rheumatoid arthritis. Clin Pharmacokinet 1996 Mar; 30: 194–210.
Oguey D, Kölliker F, Gerber NJ, et al. Effect of food on the bioavailability of low-dose methotrexate in patients with rheumatoid arthritis. Arthritis Rheum 1992; 35: 611–4.
Kozloski GD, De Vito JM, Kisicki JC, et al. The effect of food on the absorption of methotrexate sodium tablets in healthy volunteers. Arthritis Rheum 1992; 35: 761–4.
Kaniwa N, Ogata H, Aoyagi N, et al. The bioavailabilies of aspirin from an aspirin aluminum and an aspirin tablet and the effects of food and aluminum hydroxide gel. J Pharmacobiodyn 1981; 4: 860–4.
Forbes JA, Sandberg RA, Bood-Bjorklund L. The effect of food on bromfenac, naproxen sodium and acetaminophen in postoperative pain after orthopedic surgery. Pharmacotherapy 1998; 18: 492–503.
Caille G, du Souich P, Besner JG, et al. Effects of food and sucralfate on the pharmacokinetics of naproxen and ketoprofen in humans. Am J Med 1989; 86 (6A): 38–44.
Chaikin P, Marriott TB, Simon D, et al. Comparative bioavailability of suprofen after coadministration with food or milk. J Clin Pharmacol 1988; 28: 1132–5.
Mojaverian P, Rocci ML, Conner DP, et al. Effect of food on the absorption of enteric coated aspirin: correlation with gastric residence time. Clin Pharmacol Ther 1987; 41: 11–7.
Poli A, Moreno RA, Ribeiro W, et al. Influence of gastric acid secretion blockade and food intake on the bioavailability of a potassium diclofenac suspension in healthy male volunteers. Int J Clin Pharmacol Ther 1996; 34: 76–9.
Zmeili S, Hasan M, Najib N, et al. Bioavailability and pharmacokinetic properties of 2 sustained-release formulations of diclofenac sodium, Voltaren vs Inflaban: effect of food on inflaban bioavailability. Int J Clin Pharmacol Ther 1996; 34: 564–70.
Aoyagi N, Kaniwa N, Ogata H. Effects of food on bioavailability of two indomethacin capsules containing different sizes of particles. Chem Pharm Bull 1990; 38: 1338–40.
Coates PE, Mesure R. Pharmacokinetics of tenidap sodium administered with food or antacid in healthy volunteers. Br J Clin Pharmacol 1995; 39 Suppl. 1: 17–9.
Day RO, Lam S, Pauli P, et al. Effect of food and various antacids on the absorption of tenoxicam. Br J Clin Pharmacol 1987; 24: 323–8.
Pargal A, Kelkar MG, Nayak PJ. The effect of food on the bioavailability of ibuprofen and flurbiprofen from sustained release formulations. Biopharm Drug Dispos 1996; 17: 511–9.
von Schrader HW, Buscher G, Dierdorf D, et al. Nabumetone: a novel anti-inflammatory drug. The influence of food, milk, antacids, and analgesics on bioavailability of single oral doses. Int J Clin Pharmacol Ther Toxicol 1983; 21: 311–21.
George S, Dauwe K, McBurney A, et al. The influence of food intake on the bioavailability of timegadine, a novel non-steroidal anti-inflammatory drug. Br J Clin Pharmacol 1983; 15: 495–8.
McEwen J, De Luca M, Casini A, et al. The effect of food and an antacid on the bioavailability of dexketoprofen trometamol. J Clin Pharmacol 1998; 38 Suppl.: 41–5.
Flusser D, Zylber-Katz E, Granit L, et al. Influence of food on the pharmacokinetics of dipyrone. Eur J Clin Pharmacol 1988; 34: 105–7.
Benet LZ. Pharmacokinetics of sustained-release etodolac. Rheumatol Int 1993; 13 (2 Suppl.): 3S–5S.
Kraml M, Cosyns L, Hicks DR, et al. Bioavailability studies with etodolac in dogs and man. Biopharm Drug Dispos 1984; 5: 63–74.
Stoltz M, Arumugham T, Lippert C, et al. Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16455A). Biopharm Drug Dispos 1997; 18: 645–8.
Borin MT, Khare S, Beihn RM, et al. Effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy. Pharm Res 1990; 7: 304–7.
Skinhøj A, Bechgaard H, Chasseaud LF, et al. The influence of food and repeated dosing on the bioavailability of indomethacin from a multiple-units controlled release formulation. Int J Clin Pharmacol Ther Toxicol 1984; 22: 557–61.
Tiirck D, Busch U, Heinzel G, et al. Effect of food on the pharmacokinetics of meloxicam after oral administration. Clin Drug Invest 1995; 9: 270–6.
Marzo A, Dal Bo L, Wool C, et al. Bioavailability, food effect and tolerability of S-naproxenbetainate sodium salt monohydrate in steady state. Arzneimittel Forschung 1998; 48: 935–40.
Kenyon CJ, Hooper G, Tierney D, et al. The effect of food on the gastrointestinal transit and systemic absorption of naproxen from a novel sustained release formulation. J Control Rel 1995; 34: 31–6.
Norlander B, Gotthard R, Strom M. Pharmacokinetics of a 5-aminosalicylic acid enteric-coated tablet and suppository dosage form. Aliment Pharmacol Ther 1989; 3: 333–42.
Karim A, Rozek LF, Smith ME, et al. Effects of food and antacid on oral absorption of misoprostol, a synthetic prostaglandin E1 analog. J Clin Pharmacol 1989; 29: 439–43.
Huang SM, Marriott TB, Weintraub HS, et al. The effect of food or milk on the bioavailability of etintidine in healthy subjects. Int J Clin Pharmacol Ther Toxicol 1988; 26: 113–7.
Lin JH, Chremos AN, Kanovsky SM, et al. Effects of antacids and food on absorption of famotidine. Br J Clin Pharmacol 1987; 24: 551–3.
Hardy JG, Harvey WJ, Sparrow RA, et al. Localization of drug release sites from an oral sustained-release formulation of 5-ASA (Pentasa™) in the gastrointestinal tract using gamma scintigraphy. J Clin Pharmacol 1993; 33: 712–8.
De Mey C, Meineke I. Prandial and diurnal effects on the absorption of orally administered enteric coated 5-aminosalicylic acid (5-ASA). Br J Clin Pharmacol 1992; 33: 179–82.
Huber R, Hartmann M, Bliesath H, et al. Pharmacokinetics of pantoprazole in man. Int J Clin Pharmacol Ther 1996; 34 (1 Suppl.): 7S–16S.
Yasuda S, Ohnishi A, Ogawa T, et al. Pharmacokinetic properties of E 3810, a new proton pump inhibitor, in healthy male volunteers. Int J Clin Pharmacol Ther 1994; 32: 466–73.
Tse FL, Labbadia D, Habucky K, et al. Effect of food on the bioavailability of SDZ DJN 608, an oral hypoglycemic agent, from a tablet and a liquid-filled capsule in the dog. Pharm Res 1996; 13: 440–4.
Gleiter CH, Schug BS, Hermann R, et al. Influence of food intake on the bioavailability of thioctic acid enantiomers. Eur J Clin Pharmacol 1996; 50: 513–4.
Lau DT-W, Kalafsky G, Tse FLS. The effect of food on the absorption of 14C-SDZ FOX 988, an antidiabetic agent, in healthy human volunteers. Biopharm Drug Dispos 1995; 16: 191–200.
Young MA, Lettis S, Eastmond R. Improvement in the gastrointestinal absorption of troglitazone when taken with, or shortly after, food. Br J Clin Pharmacol 1998; 45: 31–5.
Rosskamp R, Wernicke-Panten K, Draeger E. Clinical profile of the novel sulphonylurea glimepiride. Diabetes Res Clin Pract 1996; 31 Suppl.: 33–42.
Saffar F, Aiache JM, Andre P. Influence of food on the disposition of the antidiabetic drug metformin in diabetic patients at steadystate. Methods Find Exp Clin Pharmacol 1995; 17: 483–7.
Okuno A, Taguchi T, Inyaku F, et al. Pharmacokinetics of propylthiouracil in children and adolescents with Graves disease after a single oral dose. Pediatr Pharmacol 1983; 3: 43–7.
McNamara PJ, Jewell RC, Jensen BK, et al. Food increases the bioavailability of acitretin. J Clin Pharmacol 1988; 28: 1051–5.
Uematsu T, Nagashima S, Niwa M, et al. Effect of dietary fat content on oral bioavailability of menatetrenone in humans. J Pharm Sci 1996; 85: 1012–6.
Simon JA, Robinson DE, Andrews MC, et al. The absorption of oral micronized progesterone: the effect of food, dose proportionality, and comparison with intramuscular progesterone. Fertil Steril 1993; 60: 26–33.
Trautner K. Influence of food on relative bioavailability of fluoride in man from Na2FPO3-containing tablets for the treatment of osteoporosis. Int J Clin Pharmacol Ther Toxicol 1989; 27: 242–9.
Bullingham R, Shah J, Goldblum R, et al. Effects of food and antacid on the pharmacokinetics of single doses of mycophenolate mofetil in rheumatoid arthritis patients. Br J Clin Pharmacol 1996; 41: 513–6.
Lennernas H, Fager G. Pharmacodynamics and pharmacokinetics of the HMG-CoA reductase inhibitors. Clin Pharmacokinet 1997 May; 32: 403–25.
Nyberg L, Kennedy BM. Pharmacokinetics of terbutaline given in slow-release tablets. Eur J Respir Dis 1984; 65 Suppl. 134: 119–39.
Hoon TJ, McCollam PL, Beckman KJ, et al. Impact of food on the pharmacokinetics and electrocardiographic effects of sustained release verapamil in normal subjects. Am J Cardiol 1992; 70: 1072–6.
Welling PG. Effects of food on drug absorption. Pharmacol Ther 1989; 43: 425–41.
Reppas C, Eleftheriou G, Macheras P, et al. Effect of elevated viscosity in the upper gastrointestinal tract on drug absorption in dogs. Eur J Pharm Sci 1998; 6: 131–9.
Wilson CG, Washington N. Small intestine: transit and absorption of drugs. In: Rubinstein MH, editor. Physiological pharmaceutics: biological barriers to drug absorption. Chichester: Ellis Horwood, 1989: 71–90.
Greenwood DE. Small intestinal pH and buffer capacity: implications for dissolution of ionizable compounds [Ph.D thesis]. Michigan: The University of Michigan, 1994.
Barnwell SG, Laudanski T, Dwyer M, et al. Reduced bioavailability of atenolol in man: the role of bile acids. Int J Pharm 1993; 89: 245–50.
Yamaguchi T, Ikeda C, Sekine Y Intestinal absorption of a β-adrenergic blocking agent Nadolol: II. Mechanism of the inhibitory effect on the intestinal absorption of nadolol by sodium cholate in rats. Chem Pharm Bull 1986; 34: 3836–43.
Yamaguchi T, Oida T, Ikeda C. Intestinal absorption of a β-adrenergic blocking agent nadolol: III. Nuclear magnetic resonance spectroscopic study on nadolol-sodium cholate micellar complex and intestinal absorption of nadolol derivatives in rats. Chem Pharm Bull 1986; 34: 4259–64.
Dressman JB, Berardi RR, Dermentzoglou LC, et al. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm Res 1990; 7: 756–61.
Dongowski G, Neubert R, Haase H, et al. Interactions between food components and drugs: part 4. Influence of pectins and bile salts on propranolol absorption. Int J Pharm 1996; 144: 233–9.
Lindholm A, Henricsson S, Dahlqvist R. The effect of food and bile acid administration on the relative bioavailability of cyclosporin. Br J Clin Pharmacol 1990; 29: 541–8.
Charman WN, Porter CJ, Mithani S, et al. Physicochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci 1997; 86: 269–82.
Barry M, Gibbons S, Back D, et al. Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations. Clin Pharmacokinet 1997 Mar; 32: 194–209.
Tam YK. Individual variation in first-pass metabolism. Clin Pharmacokinet 1993 Oct; 25: 300–28.
Drug-nutrient interaction. In: Basu TK, editor. Drug-food interaction. New York: Croom Helm, 1988: 107–14.
Mao CC, Jacobson ED. Intestinal absorption and blood flow. Am J Clin Nutr 1970; 23: 820–3.
McLean AJ, McNamara PJ, DuSouich P, et al. Food, splanchnic blood flow, and bioavailability of drugs subject to first-pass metabolism. Clin Pharmacol Ther 1978; 24: 5–10.
McLean AJ, Isbister C, Bobik A, et al. Reduction of first-pass hepatic clearance of propranolol by food. Clin Pharmacol Ther 1981; 30: 31–4.
Power JM, Morgan DJ, McLean AJ. Effects of sensory (teasing) exposure to food on oral propranolol bioavailability. Biopharm Drug Dispos 1995; 16: 579–89.
Gidal BE, Maly MM, Budde J, et al. Effect of a high-protein meal on gabapentin pharmacokinetics. Epilepsy Res 1996; 23: 71–6.
Jonkman JH. Food interactions with sustained-release theophylline preparations: areview. Clin Pharmacokinet 1989 Mar; 16: 162–79.
Alderman DA. A review of cellulose ethers in hydrophilic matrices for oral controlled-release dosage forms. Int J Pharm Tech Prod Manufact 1984; 5: 1–9.
Shameem M, Katori LN, Aoyagi N, et al. Oral solid controlled release dosage forms: role of GI-mechanical destructive forces and colonic release in drug absorption under fasted and fed conditions in humans. Pharm Res 1995; 12: 1049–54.
Katori N, Ma W-S, Aoyagi N, et al. Effect of destructive force on drug release from multiple unit controlled release dosage forms in humans. Pharm Res 1996; 13: 1541–6.
Sako K, Mizumoto T, Kajiyama A, et al. Influence of physical factors in gastrointestinal tract on acetaminophen release from controlled-release tablets in fasted dogs. Int J Pharm 1996; 137: 225–32.
Aoki S, Ando H, Ishii M, et al. Evaluation of the correlation between in vivo and in vitro release. Effect of the force of contraction and food on drug release. Biol Pharm Bull 1994; 17: 291–5.
Hooper WD, Dickinson RG, Eadie MJ. Effect of food on absorption of lomefloxacin. Antimicrob Agents Chemother 1990; 34: 1797–9.
Sorgel F, Kinzig M. Phannacokinetics of gyrase inhibitors: part 1. Basic chemistry and gastrointestinal disposition. Am J Med 1993; 94 Suppl. 3A: 44–55.
Kottke MK, Stetsko G, Rosenbaum SE, et al. Problems encountered by the elderly in the use of conventional dosage forms. J Geriatr Drug Ther 1990; 5: 77–92.
Shinkuma D, Hamaguchi T, Kobayashi M, et al. Effects of food intake on the bioavailability of sulpiride from AEA film-coated tablet having a pH-dependent dissolution characteristics in normal or drug-induced achlorhydric subjects. Int J Clin Pharmacol Ther Toxicol 1991; 29: 303–9.
Shionoiri H. Pharmacokinetic drug interactions with ACE inhibitors. Clin Pharmacokinet 1993 Jul; 25: 20–58.
McBurney A, Farrow PR, Ward JW. Effects of food on the bioavailability of sustained-release pinacidil in humans. J Phann Sci 1988; 77: 68–9.
TenHoor CN, Bakatselou V, Dressman J. Solubility of mefenamic acid under simulated fed- and fasted-state conditions. Phann Res 1991; 8: 1203–5.
Luner PE, Babu SR, Radebaugh GW. The effects of bile salts and lipids on the physicochemical behavior of gemfibrozil. Phann Res 1994; 11: 1755–60.
Williams L, Davis JA, Lowenthal DT. The influence of food on the absorption and metabolism of drugs. Med Clin North Am 1993; 77: 815–29.
Prescott LF, Yoovathaworn K, Makarananda K, et al. Impaired absorption of paracetamol in vegetarians. Br J Clin Pharmacol 1993; 36: 237–40.
Yamaguchi T, Ikeda C, Sekine Y Intestinal absorption of a β-adrenergic blocking agent nadolol: I. Comparison of absorption behavior of nadolol with those of other β-blocking agents in the rats. Chem Pharm Bull 1986; 24: 3362–9.
Siemon D, de Vries JX, Stotzer F, et al. Fasting and postprandial disposition of R-(−)- and S-(+)- ibuprofen following oral administration of racemic drug in healthy individuals. Eur J Med Res 1997; 2: 215–9.
Waldman SA, Morganroth J. Effects of food on the bioequivalence of different verapamil sustained-release fonnulations. J Clin Phannacol 1995; 35: 163–9.
Holmes DG, Kutz K. Bioequivalence of a slow-release and a non-retard formulation of isradipine. Am J Hypertens 1993; 6 Suppl.: 70–3.
Hosny EA, El-Sayed YM, Al-Meshal MA, et al. Effect of food on bioavailability of bioadhesive-containing indomethacin tablets in dogs. Int J Pharm 1994; 112: 87–91.
Schall R, Muller FR, Muller FO, et al. Bioequivalence of controlled release calcium antagonists. Clin Phannacokinet 1997 Jan; 32: 75–89.
Melander A, McLean A. Influence of food intake on presystemic clearance of drugs. Clin Pharmacokinet 1983; 8: 286–96.
Follonier N, Doelker E. Biopharmaceutical comparison of oral multiple-unit and single-unit sustained-release dosage fonns. STPPhanna Sci 1992; 2: 141–58.
Hoener B-A, Benet LZ. Factors influencing drug absorption and drug availability. In: Banker GS, Rhodes CT, editors. Modern phannaceutics. New York: Marcel Dekker, Inc., 1990: 143–80.
Massarella JW, Blumenthal HP, Silvestri T, et al. Effect of food on cibenzoline bioavailability. Eur J Phannacol 1986; 30: 367–9.
Dunselman PH, Edgar B. Felodipine clinical phannacokinetics. Clin Phannacokinet 1991; 21: 418–30.
Lundahl J, Regardh CG, Edgar B, et al. Relationship between time of intake of grapefruit juice and its effect on phannacokinetics and phannacodynamics of felodipine in healthy subjects. Eur J Clin Pharmacol 1995; 49: 61–7.
Tam YK, Kneer J, Dubach UC, et al. Effect of timing of food and fluid volume on cefetamet pivoxil absorption in healthy nonnal volunteers. Antimicrob Agents Chemother 1990; 34: 1556–9.
Melander A, Liedholm H, McLean A. Concomitant food intake does enhance the bioavailability and effect of hydralazine. Clin Phannacol Ther 1985; 38: 475–6.
Gertz BJ, Holland SD, Kline WF, et al. Clinical phannacology of alendronate sodium. Osteoporosis Int 1993; 3 Suppl. 3: 13–6.
Samanta A, Jones GR, Burden AC, et al. Improved effect of tolbutamide when given before food in patients on long-term therapy. Br J Clin Pharmacol 1984; 18: 647–8.
Antal EJ, Gillespie WR, Phillips JP, et al. The effect of food on the bioavailability and pharmacodynamics of tolbutamide in diabetic patients. Eur J Clin Pharmacol 1982; 22: 459–62.
Hartshorn EA. Food and drug interactions. J Am Diet Assoc 1977; 70: 15–9.
Shively CA, Simons RJ, Passananti GT, et al. Dietary patterns and diurnal variations in aminopyrine disposition. Clin Pharmacol Ther 1981; 29: 65–73.
Lau DT, Kalafsky G, Aun RL, et al. The effect of the fat content of food on the pharmacokinetics and pharmacodynamics of SDZ FOX 988, an antidiabetic agent, in the dog. Biopharm Drug Dispos 1995; 16: 137–50.
Pan HY, DeVault AR, Brescia D, et al. Effect of food on pravastatin pharmacokinetics and pharmacodynamics. Int J Clin Pharmacol Ther Toxicol 1993; 31: 291–4.
Gai MN, Isla A, Andonaegui MT, et al. Evaluation of the effect of 3 different diets on the bioavailability of 2 sustained release theophylline matrix tablets. Int J Clin Pharmacol Ther 1997; 35: 565–71.
Smith HT, Jokubaitis LA, Troendle AJ, et al. Pharmacokinetics of fluvastatin and specific drug interactions. Am J Hypertens 1993; 6 Suppl.: 375–82.
Hunt JN, Stubbs DF. The volume and energy content of meals as determinants of gastric emptying. J Physiol 1975; 245: 209–25.
Zhi J, Rakhit A, Patel IH. Effects of dietary fat on drug absorption. Clin Pharmacol Ther 1995; 58: 487–91.
Richter WO, Jacob BG, Schwandt P. Interaction between fiber and lovastatin [letter]. Lancet 1991; 338: 706.
Davidson MH, Dugan LD, Burns JH, et al. The hypocholesterolemic effects of β-glucan in oatmeal and oat bran. JAMA 1991; 265: 1833–9.
Bell LP, Hectorn KJ, Reynolds H, et al. Cholesterol-lowering effects of soluble-fiber cereals as part of a prudent diet for patients with mild to moderate hypercholesterolemia. Am J Clin Nutr 1990; 52: 1020–6.
Liel Y, Harman-Boehm I, Shany S. Evidence for a clinically important adverse effect of fiber-enriched diet on the bioavailability of levothyroxine in adult hypothyroid patients. J Clin Endocrinol Metab 1996; 81: 857–9.
Huupponen R, Seppala P, Iisalo E. Effect of guar gum, a fibre preparation, on digoxin and penicillin absorption in man. Eur J Clin Pharmacol 1984; 26: 279–81.
Gin H, Orgerie MB, Aubertin J. The influence of Guar gum on absorption of metformin from the gut in healthy volunteers. Horm Metab Res 1989; 21: 81–3.
Huupponen R, Karhuvaara S, Seppala P. Effect of guar gum on glipizide absorption in man. Eur J Clin Pharmacol 1985; 28: 717–9.
Montani A, Vimercati ME. Control of glucose and lipid metabolism by gel-forming fiber in diabetes: medium term effects of guar-gum. In: Piemonte G, Tagliaro F, Marigo M, et al., editors. Developments in analytical methods in pharmaceutical, biomédical, and forensic sciences. New York: Plenum Press, 1987: 315–9.
Vahouny GV, Kritchevsky D, editors. Dietary fiber, basic and clinical aspects. New York: Plenum Press, 1986.
Kritchevsky D, Bonfield C, editors. Dietary fiber in health and disease. St Paul (MN): Eagan Press, 1995.
Tew BY, Xu X, Wang HJ, et al. A diet high in wheat fiber decreases the bioavailability of soybean isoflavones in a single meal fed to women. J Nutr 1996; 126: 871–7.
Lin Y-J, Weidler DJ, Garg DC, et al. Effects of solid food on blood levels of alcohol in man. Res Commun Chem Pathol Pharmacol 1976; 13: 713–22.
Shinkuma D, Hamaguchi T, Kobayashi M, et al. Effect of food intake and meal size on the bioavailability of sulpiride in two dosage forms. Int JClin Pharmacol Ther Toxicol 1990; 28: 440–2.
Nievel JG, Havard CWH, Mitchell P, et al. Effect of meal size and composition on the bioavailability of ketoprofen (Oruvail). Xenobiotica 1987; 17: 487–92.
Wills RJ. Influence of food on the bioavailability of trimoprostil: an overview. J Clin Pharmacol 1984; 24: 194–201.
Lecaillon JB, Dubois JP, Soula G, et al. The influence of food on the pharmacokinetics of CGP6140 (amocarzine) after oral administration of a 1200mg single dose to patients with onchocerciasis. Br J Clin Pharmacol 1990; 30: 629–33.
Al-Gohary OMN, Hosny EA. Effect of antacid megaldrate oral suspension on in-vitro and in-vivo availability of indomethacin in dogs. Pharm Acta Helv 1997; 72: 81–6.
Ismail FA, Khalafallah N, Khalil SA. Adsorption of ketoprofen and bumadizone calcium on aluminum containing antacids and its effect on ketoprofen bioavailability in man. Int J Pharm 1987; 34: 189–96.
Fann WE, Davis JM, Janowsky DS, et al. Chlorpromazine: effects of antacids on its gastrointestinal absorption. J Clin Pharmacol 1973; 13: 388–90.
Nix DE, Wilton JH, Ronald B, et al. Inhibition of norfloxacin absorption by antacids. Antimicrob Agents Chemother 1990; 34: 432–5.
Lucarotti RL, Colaizzi JL, Barry H III, et al. Enhanced pseudoephedrine absorption by concurrent administration of aluminum hydroxide gel in humans. J Pharm Sci 1972; 61: 903–5.
Hurwitz A, Sheehan MB. The effects of antacids on the absorption of orally administered pentobarbital in the rat. J Pharmacol Exp Ther 1971; 179: 124–31.
Neuvonen PJ, Kivisto KT. Enhancement of drug absorption by antacids: an unrecognized drug interaction. Clin Pharmacokinet 1994 Aug; 27: 120–8.
Tett SE. Clinical pharmacokinetics of slow-acting antirheumatic drugs. Clin Pharmacokinet 1993 Nov; 25: 392–407.
Lehto P, Kivisto KT. Different effects of products containing metal ions on the absorption of lomefloxacin. Clin Pharmacol Ther 1994; 56: 477–82.
Lehto P, Kivisto KT, Neuvonen PJ. The effect of ferrous sulfate on the absorption of norfloxacin, ciprofloxacin and ofloxacin. Br J Clin Pharmacol 1994; 37: 82–5.
Brouwers JR, Van der Kam HJ, Sijtsma J, et al. Decreased ciprofloxacin absorption with concomitant administration of ferrous fumarate. Pharm Weekbl Sci 1990; 12: 182–3.
Brown DD, Juhl RP. Decreased bioavailability of digoxin due to antacids and kaolin-pectin. N Engl J Med 1976; 295: 1034–7.
Khalil SAH, Mortada LM, El-Khawas M. Decreased bioavailability of ampicillin and amoxicillin in presence of kaolin. Int J Pharm 1984; 19: 233–8.
Moustafa MA, Gouda MW, Tariq M. Decreased bioavailability of propranolol due to interactions with adsorbents, antacids and antidiarrheal mixtures. Int J Pharm 1986; 30: 225–8.
Molokhia AM, Al-Rahman S. Effect of concomitant oral administration of some adsorbing drugs on the bioavailability of metronidazole. Drug Dev Ind Pharm 1987; 13: 1229–37.
Moustafa MA, Al-Shora HI, Gaber M, et al. Decreased bioavailability of quinidine sulfate due to interactions with adsorbent antacids and antidiarrheal mixtures. Int J Pharm 1987; 34: 207–11.
Moustafa MA, Babhair SA, Kouta HI. Decreased bioavailability of some antipsychotic phenothiazines due to interactions with adsorbent antacid and antidiarrheal mixtures. Int J Pharm 1987; 36: 185–9.
Gouda MW. Effect of an antidiarrheal mixture on the bioavail-ability of tetracycline. Int J Pharm 1993; 89: 75–7.
Al-Gohary OMN. In-vitro adsorption of mebeverine hydrochloride onto kaolin and its relationship to pharmacological effects of the drug in vivo. Pharm Acta Helv 1997; 72: 11–21.
Jung H, Peregrina AA, Rodriquez JM, et al. The influence of coffee with milk and tea with milk on the bioavailability of tetracycline. Biopharm Drug Dispos 1997; 18: 459–63.
Minami R, Inotsume N, Nakano M, et al. Effect of milk on absorption of norfloxacin in healthy volunteers. J Clin Pharmacol 1993; 33: 1238–40.
Neuvonen PJ, Kivisto KT, Lehto P. Interference of dairy products with the absorption of ciprofloxacin. Clin Pharmacol Ther 1991; 50: 498–502.
Leahy DE, Lynch J, Finney RE, et al. Estimation of sieving coefficients of convective absorption of drugs in perfused rat jejunum. J Pharmacokinet Biopharm 1994; 22: 411–29.
Liguori A, Hughes JR, Grass JA. Absorption and subjective effects of caffeine from coffee, cola and capsules. Pharmacol Biochem Behav 1997; 58: 721–6.
Mumford GK, Benowitz NL, Evans SM, et al. Absorption rate of methylxanthines following capsules, cola and chocolate. Eur J Clin Pharmacol 1996; 51: 319–25.
Chvasta TE, Cooke AR. Emptying and absorption of caffeine from the human stomach. Gastroenterology 1971; 61: 838–43.
Bonati M, Latini R, Galletti F, et al. Caffeine disposition after oral doses. Clin Pharmacol Ther 1982; 32: 98–106.
Disler PB, Lynch SR, Torrence JD, et al. The mechanism of the inhibition of iron absorption by tea. S Afr J Med Sci 1975; 40: 109–16.
Tea and iron. Lipton® Tea and Health Information. Englewood Cliffs (NJ), Lipton, 1998.
Tukker JJ, Sitsen JM, Gusdorf CF. Bioavailability of paracetamol after oral administration to healthy volunteers. Influence of caffeine on rate and extent of absorption. Pharm Weekbl Sci 1986; 8: 239–43.
Monks TJ, Caldwell J, Smith RL. Influence of methylxanthine-containing foods on theophylline metabolism and kinetics. Clin Pharmacol Ther 1979; 26: 513–24.
Rubinstein E, Hauge C, Sommer P, et al. Oesophageal and gastric potential difference and pH in healthy volunteers following intake of coca-cola, red wine, and alcohol. Pharmacol Toxicol 1993; 72: 61–5.
Lange D, Pavao JH, Wu J, et al. Effect of a cola beverage on the bioavailability of itraconazole in the presence of H2 blockers. J Clin Pharmacol 1997; 37: 535–40.
Jaruratanasirikul S, Kleepkaew A. Influence of an acidic beverage (Coca-Cola) on the absorption of itraconazole. Eur J Clin Pharmacol 1997; 52: 235–7.
Chin TW, Loeb M, Fong IW. Effects of an acidic beverage (Coca-Cola) on absorption of ketoconazole. Antimicrob Agents Chemother 1995; 39: 1671–5.
Lange D, Pavao JH, Jacqmin P, et al. The effect of coadministration of a cola beverage on the bioavailability of itraconazole in patients with acquired immunodeficiency syndrome. Curr Ther Res Clin Exp 1997; 58: 202–12.
Houston JB, Levy G. Effect of buffered carbohydrate solutions (Coca-Cola and Emetrol) on bioavailability of riboflavin in man [abstract no. 36]. 17 National Meeting of the Academy of Pharmaceutical Sciences; 1974 Nov 10–14; New Orleans, 128.
de Vries EG, Meyer C, Strubbe M, et al. Influence of various beverages on urine acid output. Cancer Res 1986; 41: 430–2.
Hunt JN, Knox MT. The slowing of gastric emptying by nine acids. J Physiol 1969; 201: 161–79.
Gilbert RM. Caffeine as a drug of abuse. In: Gibbins RJ, Israel Y, Kalant H, et al., editors. Recent advances in alcohol and drug problems. New York: Wiley, 1976: 49–176.
Fundamentals of clinical pharmacokinetics. In: Wagner JG, editor. Effect of normal and pathologic physiology on pharmacokinetics. Hamilton (IL): Drug Intelligence Publications, Inc., 1975: 359–95.
Diet and drug interactions. In: Roe DA, editor. Effects of food, nutrients, and nutritional status on drug disposition. New York: Van Nostrand Reinhold, 1989: 11–28.
Anderson KE. Influences of diet and nutrition on clinical pharmacokinetics. Clin Pharmacokinet 1988; 14: 325–46.
Krishnaswamy K. Drug metabolism and pharmacokinetics in malnourished children. Clin Pharmacokinet 1989; 17 Suppl. 1: 68–88.
Walter-Sack I, Klotz U. Influence of diet and nutritional status on drug metabolism. Clin Pharmacokinet 1996 Jul; 31: 47–64.
Williams L, Hill Jr DP, Davis JA, et al. The influence of food on the absorption and metabolism of drugs: an update. Eur J Drug Metab Pharmacokinet 1996; 21: 201–11.
Wilkinson GR. The effect of diet, aging and disease-states on presystemic elimination and oral drug bioavailability in humans. Adv Drug Del Rev 1997; 27: 129–59.
Josefsson M, Zackrisson AL, Ahlner J. Effect of grapefruit juice on the pharmacokinetics of amlodipine in healthy volunteers. Eur J Clin Pharmacol 1996; 51: 189–93.
Lilja JJ, Kivisto KT, Backman JT, et al. Grapefruit juice substantially increases plasma concentrations of buspirone. Clin Pharmacol Ther 1998; 64: 655–60.
Garg SK, Kumar N, Bhargava VK, et al. Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy. Clin Pharmacol Ther 1998; 64: 286–8.
Yee GC, Stanley DL, Pessa LJ, et al. Effect of grapefruit juice on blood cyclosporin concentration. Lancet 1995; 345: 955–6.
Ducharme MP, Warbasse LH, Edwards DJ. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 1995; 57: 485–91.
Ducharme MP, Provenzano R, Dehoorne-Smith M, et al. Trough concentrations of cyclosporine in blood following administration with grapefruit juice. Br J Clin Pharmacol 1993; 36: 457–9.
Ozdemir M, Aktan Y, Boydag BS, et al. Interaction between grapefruit juice and diazepam in humans. Eur J Drug Metab Pharmacokinet 1998; 23: 55–9.
Weber A, Jager R, Borner A. Can grapefruit juice influence ethinylestradiol bioavailability? Contraception 1996; 53: 41–7.
Bailey DG, Spence JD, Munoz C, et al. Interaction of citrus juices with felodipine and nifedipine. Lancet 1991; 337: 268–9.
Lundahl J, Regardh CG, Edgar B, et al. Effects of grapefruit juice ingestion — pharmacokinetic and haemodynamics of intravenously and orally administered felodipine in healthy men. Eur J Clin Pharmacol 1997; 52: 139–45.
Edgar B, Bailey D, Bergstrand R, et al. Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics of felodipine, and its potential clinical relevance. Eur J Clin Pharmacol 1992; 42: 313–7.
Bailey DG, Bend JR, Arnold JMO, et al. Erythromycin-felodipine interaction: magnitude, mechanism, and comparison with grapefruit juice. Clin Pharmacol Ther 1996; 60: 25–33.
Lundahl JU, Regardh CG, Edgar B, et al. The interaction effect of grapefruit juice is maximal after the first glass. Eur J Clin Pharmacol 1998; 54: 75–81.
Bailey DG, Arnold JM, Bend JR, et al. Grapefruit juice-felodipine interaction: reproducibility and characterization with the extended release drug formulation. Br J Clin Pharmacol 1995; 40: 135–40.
Kantola T, Kivisto KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998; 63: 397–402.
Kupferschmidt HH, Ha HR, Ziegler WH, et al. Interaction between grapefruit juice and midazolam in humans. Clin Pharmacol Ther 1995; 58: 20–8.
Sigusch H, Hippius M, Henschel L, et al. Influence of grapefruit juice on the pharmacokinetics of a slow release nifedipine formulation. Pharmazie 1994; 49: 522–4.
Grundy JS, Eliot LA, Kulmatycki KM, et al. Grapefruit juice and orange juice effects on the bioavailability of nifedipine in the rat. Biopharm Drug Dispos 1998; 19: 175–83.
Fuhr U, Maier-Bruggemann A, Blume H, et al. Grapefruit juice increases oral nimodipine bioavailability. Int J Clin Pharmacol Ther 1998; 36: 126–32.
Bailey DG, Arnold JM, Strong HA, et al. Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther 1993; 54: 589–94.
Soons PA, Vogels BAPM, Roosemalen MCM, et al. Grapefruit juice and cimetidine inhibit stereoselective metabolism of nitrendipine in humans. Clin Pharmacol Ther 1991; 50: 394–403.
Hashimoto K, Shirafuji T, Sekino H, et al. Interaction of citrus juices with pranidipine, a new 1,4-dihydropyridine calcium antagonist, in healthy subjects. Eur J Clin Pharmacol 1998; 54: 753–60.
Kupferschmidt HH, Fattinger KE, Ha HR, et al. Grapefruit juice enhances the bioavailability of the protease HIV inhibitor saquinavir in man. Br J Clin Pharmacol 1998; 45: 355–9.
Lilja JJ, Kivisto KT, Neuvonen PJ. Grapefruit juice-simvastatin interaction: effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors. Clin Pharmacol Ther 1998; 64: 477–83.
Benton RE, Honig PK, Zamani K, et al. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin Pharmacol Ther 1996; 59: 383–8.
Rau SE, Bend JR, Arnold MO, et al. Grapefruit juice-terfenadine single-dose interaction: magnitude, mechanism, and relevance. Clin Pharmacol Ther 1997; 61: 401–9.
Honig PK, Wortham DC, Lazarev A, et al. Grapefruit juice alters the systemic bioavailability and cardiac repolarization of terfenadine in poor metabolizers of terfenadine. J Clin Pharmacol 1996; 36: 345–51.
Clifford CP, Adams DA, Murray S, et al. The cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice. Eur J Clin Pharmacol 1997; 52: 311–5.
Hukkinen SK, Varhe A, Olkolla KT, et al. Plasma concentrations of triazolam are increased by concomitant ingestion of grapefruit juice. Clin Pharmacol Ther 1995; 58: 127–31.
Cheng KL, Nafziger AN, Peloquin CA, et al. Effect of grapefruit juice on clarithromycin pharmacokinetics. Antimicrob Agents Chemother 1998; 42: 927–9.
Sigusch H, Henschel L, Kraul H, et al. Lack of effect of grapefruit juice on diltiazem bioavailability in normal subjects. Pharmazie 1994; 49: 675–9.
Min DI, Ku Y-M, Geraets DR, et al. Effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of quinidine in healthy volunteers. J Clin Pharmacol 1996; 36: 469–76.
Fuhr U, Maier A, Keller A, et al. Lacking effect of grapefruit juice on theophylline pharmacokinetics. Int J Clin Pharmacol Ther 1995; 33: 311–4.
Zaidenstein R, Dishi V, Gips M, et al. The effect of grapefruit juice on the pharmacokinetics of orally administered verapamil. Eur J Clin Pharmacol 1998; 54: 337–40.
Chan WK, Nguyen LT, Miller VP, et al. Mechanism-based in-activation of human cytochrome P450 3 A4 by grapefruit juice and red wine. Life Sci 1998; 62: 135–42.
Runkel M, Bourian M, Tegtmeier M, et al. The character of inhibition of the metabolism of 1,2-benzopyrone (coumarin) by grapefruit juice in human. Eur J Clin Pharmacol 1997; 53: 265–9.
Bailey DG, Arnold JMO, Munoz C, et al. Grapefruit juice-felodipine interaction: mechanism, predictability, and effect of naringin. Clin Pharmacol Ther 1993; 53: 637–42.
Rashid J, McKinstry C, Renwick AG, et al. Quercetin, an in vitro inhibitor of CYP3A, does not contribute to the interaction between nifedipine and grapefruit juice. Br J Clin Pharmacol 1993; 36: 460–3.
Edwards DJ, Bernier SM. Naringin and naringenin are not the primary CYP3A inhibitors in grapefruit juice. Life Sci 1996; 59: 1025–30.
Guengerich FP, Kim D. In vitro inhibition of dihydropyridine oxidation and aflatoxin B1 activation in human liver microsomes by naringenin and other flavonoids. Carcinogenesis 1990; 11: 2275–9.
Miniscalco A, Lundahl J, Regardh CG, et al. Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavonoids found in grapefruit juice. J Pharmacol Exp Ther 1992; 261: 1195–9.
Edwards DJ, Bellevue III FH, Woster PM. Identification of 6′,7′-dihydroxybergamottin, a cytochrome P450 inhibitor, in grapefruit juice. Drug Metab Dispos 1996; 24: 1287–90.
Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, et al. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents. Decreased enterocyte concentration and mechanism-based inactivation by furanocoumarins. Drug Metab Dispos 1997; 25: 1228–33.
Fukuda K, Ohta T, Yamazoe Y Grapefruit component interacting with rat and human P450 CYP3A: possible involvement of non-flavonoid components in drug interaction. Biol Pharm Bull 1997; 20: 560–4.
Ameer B, Weintraub RA. Drug interactions with grapefruit juice. Clin Pharmacokinet 1997 Aug; 33: 103–21.
Fuhr U. Drug interactions with grapefruit juice. Extent, probable mechanism and clinical relevance. Drug Saf 1998; 18: 251–72.
Bailey DG, Malcolm J, Arnold O, et al. Grapefruit juice-drug interactions. Br J Clin Pharmacol 1998; 46: 101–10.
Lown KS, Bailey DG, Fontana RJ, et al. Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. J Clin Invest 1997; 99: 2545–53.
Soldner A, Christians U, Susanto M, et al. Grapefruit juice activates P-glycoprotein-mediated drug transport. Pharm Res 1999; 16: 478–85.
El-Arini SK, Shiu GK, Skelly JP. An in vitro study of possible food-drug interactions of the controlled-release propranolol products. Int J Pharm 1989; 55: 25–30.
El-Arini SK, Shiu GK, Skelly JP. Theophylline-controlled release preparations and fatty food: in vitro study using the rotating dialysis cell method. Pharm Res 1990; 7: 1134–40.
Williams III RO, Sriwongjanya M, Liu J. An in vitro method to investigate food effects on drug release from film-coated beads. Pharm Dev Technol 1997; 2: 1–9.
Cook CS, Hauswald CL, Grahn AY, et al. Suitability of the dog as an animal model for evaluating theophylline absorption and food effects from different formulations. Int J Pharm 1990; 60: 125–32.
Cook CS, Zhang L, Osis J, et al. Mechanism of compound-and species-specific food effects of structurally related antiarrhythmic drugs, disopyramide and bidisomide. Pharm Res 1998; 15: 429–33.
Semple HA, Tarn YK, Coutts RT. Hydralazine pharmacokinetics and interaction with food: an evaluation of the dog as an animal model. Pharm Res 1990; 7: 274–9.
Shiu GK, LeMarchand A, Sager AO, et al. The beagle dog as an animal model for a bioavailability study of controlled-release theophylline under the influence of food. Pharm Res 1989; 6: 1039–42.
Aoyagi N, Ogata H, Kaniwa N, et al. Gastric emptying of tablets and granules in humans, dogs, pigs, and stomach-emptying controlled rabbits. J Pharm Sci 1992; 81: 1170–4.
Sagara K, Kawata M, Mizuta H, et al. Utility of gastrointestinal physiology regulated-dogs: bioavailability study of a commercial sustained-release dosage form of theophylline. Biol Pharm Bull 1994; 17: 931–4.
Wang B, Semple HA. Inhibition of metoprolol metabolism by amino acids in perfused rat livers: insights into the food effect? Drug Metab Dispos 1997; 25: 287–95.
Lee K-H, Xu G-X, Schoenhard GL, et al. Mechanisms of food effects of structurally related antiarrhythmic drugs, disopyramide and bidisomide in the rat. Pharm Res 1997; 14: 1030–8.
Semple HA, Tam YK, Coutts RT. Computer simulation of the food effect: transient changes in hepatic blood flow and Michaelis-Menten parameters as mediators of hepatic first-pass metabolism and bioavailability of propranolol. Biopharm Drug Dispos 1990; 11: 61–76.
Schaefer HG, Heinig R, Ahr G, et al. Pharmacokinetic-pharmacodynamic modelling as a tool to evaluate the clinical relevance of a drug-food interaction for a nisoldipine controlled-release dosage form. Eur J Clin Pharmacol 1997; 51: 473–80.
Cameron-Smith BD, Collier GR, O’Dea K. Effect of soluble dietary fiber on the viscosity of gastrointestinal contents and the acute glycaemic response in the rat. Br J Nutr 1994; 71: 563–71.
Abernethy DR, Azarnoff DL. Pharmacokinetic investigations in elderly patients: clinical and ethical considerations. Clin Pharmacokinet 1990; 19: 89–93.
Spina E. Pharmacokinetics of antidepressants in the elderly. Biol Psychiatry 1997; 42 Suppl.: 3–4.
Hatlebakk JG, Berstad A. Pharmacokinetic optimization in the treatment of gastro-oesophageal reflux disease. Clin Pharmacokinet 1996 Nov; 31: 386–406.
Samal SC, Ramakrishna BS. Gastrointestinal problems in the elderly. Ind J Med Res 1997; 106: 295–301.
Yuen GJ. Altered pharmacokinetics in the elderly. Clin Geriatr Med 1990; 6: 257–67.
Applied biopharmaceutics and pharmacokinetics. In: Shargel L, Yu ABC, editors. Application of pharmacokinetics in clinical situations. Stamford (CT): Appleton & Lange, 1993: 399–434.
Russell TL, Berardi RR, Barnett JL, et al. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. Pharm Res 1993; 10: 187–96.
Mojaverian P, Vlasses PH, Kellner PE, et al. Effects of gender, posture, and age on gastric residence time of an indigestible solid: pharmaceutical considerations. Pharm Res 1988; 5: 639–44.
Russell TL, Berardi RR, Barnett JL, et al. pH-related changes in the absorption of dipyridamole in the elderly. Pharm Res 1994; 11: 136–43.
Divoll M, Greenblatt DJ, Ameer B, et al. Effect of food on acetaminophen absorption in young and elderly subjects. J Clin Pharmacol 1982; 22: 571–6.
Viswanathan CT, Welling PG. Food effects on drug absorption in the elderly. In: Roe DA, editor. Drugs and nutrition in the geriatric patient. New York: Churchill Livingston, 1984: 47–70.
Thomas JA, Burns RA. Important drug-nutrient interactions in the elderly. Drugs Aging 1998; 13: 199–209.
Schumucker DL. Aging and drug disposition: an update. Pharmacol Rev 1985; 37: 133–48.
Welling P. Nutrient effects on drug metabolism and action in the elderly. Drug Nutr Interact 1985; 4: 173–207.
Roberts J, Turner N. Age and diet effects on drug action. Pharmacol Ther 1988; 37: 111–49.
Roe DA. Therapeutic effects of drug-nutrient interactions in the elderly. J Am Diet Assoc 1985; 85: 174–8.
McLeod HL, Evans WE. Pediatric pharmacokinetics and therapeutic drug monitoring. Pediatr Rev 1992; 13: 413–21.
Melander A, Wahlin E, Danielson K, et al. Bioavailability of propylthiouracil: interindividual variation and influence of food intake. Acta Med Scand 1977; 201: 41–4.
Nakamura H, Iwai N. Pharmacokinetic study on oral antibiotics in pediatrics: IIIA. Pharmacokinetic study on cefprozil in pediatrics [in Japanese]. Jpn J Antibiot 1992; 45: 1489–504.
Lafolie P, Bjork O, Hayder S, et al. Variability of 6-mercaptopurine pharmacokinetics during oral maintenance therapy of children with acute leukemia. Med Oncol Tumor Pharmacother 1989; 6: 259–65.
Vaughan LM, Milavetz G, Weinberger MM, et al. Oral bioavailability of slow-release theophylline from unencapsulated beads in preschool children with chronic asthma. Ther Drug Monit 1988; 10: 395–400.
Heimann G, Murgescu J, Bergt U. Influence of food intake on bioavailability of theophylline in premature infants. Eur J Clin Pharmacol 1982; 22: 171–3.
Crom WR. Pharmacokinetics in the child. Environ Health Perspect 1994; 102 Suppl. 11: 111–7.
Atherton JC, Washington N, Bracewell MA, et al. Scintigraphic assessment of the intragastric distribution and gastric emptying of an encapsulated drug: the effect of feeding and of a proton pump inhibitor. Aliment Pharmacol Ther 1994; 8: 489–94.
Yamreudeewong W, Henan NE, Fazio A, et al. Drug-food interactions in clinical practice. J Fam Pract 1995; 40: 376–84.
Berlin I, Lecrubier Y Food and drug interactions with monoamine oxidase inhibitors: how safe are the newer agents? CNS Drugs 1996; 5: 403–13.
Morganroth J, Waldman SA. Improved sensitivity in detecting drug-induced alterations in the PR-interval when measured by a single cardiologist compared to computer analysis. Am J Cardiol 1993; 72: 834–6.
Karbwang J, Na Bangchang K. Clinical pharmacokinetics of halofantrine. Clin Pharmacokinet 1994 Aug; 27: 104–19.
Grant SM, Clissold SP. Itraconazole: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in superficial and systemic mycoses. Drugs 1989; 37: 310–44.
Lake-Bakaar G, Tom W, Lake-Bakaar D, et al. Gastropathy and ketoconazole malabsorption in the acquired immunodeficiency syndrome (AIDS). Ann Intern Med 1988; 109: 471–3.
Salmerón J, Manson JE, Stampfer MJ, et al. Dietary fiber, glycemic load, and the risk of non-insulin-dependent diabetes mellitus in women. JAMA 1997; 277: 472–7.
Pietinen P, Rimm EB, Korhonen P, et al. Intake of dietary fiber and risk of coronary heart disease in a cohort of Finnish men. The Alpha-Tocopherol, Beta-Carotene Cancer Prevention Study. Circulation 1996; 94: 2720–7.
Trowell HC. Ischaemic heart disease, atheroma and fibrinolysis. In: Burkitt DP, Trowell HC, editors. Refined carbohydrate food and disease. London: Academic Press, 1975.
Holt S, Heading RC, Carter DC, et al. Effect of gel fiber on gastric emptying and absorption of glucose and paracetamol. Lancet 1979; I: 636–9.
Jenkins DJ A, Wolever TMS, Leeds AR, et al. Dietary fibers, fiber analogues, and glucose tolerance: importance of viscosity. BMJ 1978; 1: 1392–4.
Pilch SM, editor. Physiological effects and health consequences of dietary fiber. Bethesda (MD): Life Sciences Research Office, FASEB, 1987.
Van der Meer R, Lapré JA, Govers MJAP, et al. Mechanisms of the intestinal effects of dietary fats and milk products on colon carcinogenesis. Cancer Lett 1997; 114: 75–83.
Hollman PCH, van Trijp JMP, Buysman MNCP, et al. Relative bioavailability of the antioxidant flavonoid quercetin from various foods in man. FEBS Lett 1997; 418: 152–6.
Hollman PCH, van Trijp JMP, Mengelers MJB, et al. Bioavailability of the dietary antioxidant flavonol quercetin in man. Cancer Lett 1997; 114: 139–40.
Dai R, Jacobson KA, Robinson RC, et al. Differential effects of flavonoids on testosterone-metabolizing cytochrome P450s. Life Sci 1997; 61: 75–80.
Barnes S, Sfakianos J, Coward L, et al. Soy isoflavonoids and cancer prevention: underlying biochemical and pharmacological issues. Adv Exp Med Biol 1996; 401: 87–100.
Kurlandsky LE, Bennink MR, Webb PM, et al. The absorption and effect of dietary supplementation with omega-3 fatty acids on serum leukotriene B4 in patients with cystic fibrosis. Pediatr Pulmonol 1994; 18: 211–7.
Kempster PA, Wahlqvist ML. Dietary factors in the management of Parkinson’s disease. Nutr Rev 1994; 52: 51–8.
Astarloa R, Mena MA, Sanchez V, et al. Clinical and pharmacokinetic effects of a diet rich in insoluble fiber on Parkinson disease. Clin Neuropharmacol 1992; 15: 375–80.
Chisholm A, Sutherland W, Ball M. The effect of dietary fat content on plasma noncholesterol sterol concentrations in patients with familial hypercholesterolemia treated with simvastatin. Metabolism 1994; 43: 310–4.
National Cholesterol Education Program. Second report of the expert panel on detection, evaluation, and treatment of high cholesterol in adults (Adult Treatment Panel). Circulation 1994; 89: 1333–445.
Wright N, Scott BB. Dietary treatment of active Crohn’s disease. BMJ 1997; 314: 454–5.
Introduction: semi-solid formulations for oral drug delivery. In: Robinson JR, editor. Semi-solid formulations and oral absorption enhancement. Sanit Rémy de Provence: Bulletin Technique Gattefossé 1996 Jun: 11–3.
Technical Dossier: Gelucire®. Pharmaceutical excipients for oral semi-solid formulations, 2nd ed. Westwood (NJ): Gattefossé Corporation, 1996 Oct.
Bioavailability enhancers for oral liquid and capsule formulations. Westwood (NJ): Gattefossé Corporation, 1997.
Lenaerts V, Moussa I, Dumoulin Y, et al. Cross-linked high amylose starch for controlled release of drugs: recent advances. J Control Rel 1998; 53: 225–34.
Gauthier I, Malone M. Drug-food interactions in hospitalised patients: methods of prevention. Drug Saf 1998; 18: 383–93.
Holdiness MR. Clinical pharmacokinetics of N-acetylcysteine. Clin Pharmacokinet 1991 Feb; 20: 123–34.
Belluzi A, Brignola C, Campieri M, et al. Effect of an entericcoated fish-oil preparation on relapses in Crohn’s disease. N Engl J Med 1996; 334: 1557–60.
Steinijans VW, Hauschke D, Jonkman JHG. Controversies in bioequivalence studies. Clin Pharmacokinet 1992; 22: 247–53.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Singh, B.N. Effects of Food on Clinical Pharmacokinetics. Clin Pharmacokinet 37, 213–255 (1999). https://doi.org/10.2165/00003088-199937030-00003
Published:
Issue Date:
DOI: https://doi.org/10.2165/00003088-199937030-00003