Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine

Clinical Pharmacokinetics

Volumn 41, Issue 4, 2002, Pages 311-318

  Banfield, Christopher ^a   Gupta, Samir ^a   Marino, Mark ^a   Lim, Josephine ^a   Affrime, Melton ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIHISTAMINIC AGENT; CARRIER PROTEIN; CYTOCHROME P450; DESLORATADINE; FEXOFENADINE; GLYCOPROTEIN P;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG HALF LIFE; DRUG TRANSPORT; ELECTROCARDIOGRAPHY; FEMALE; FOOD DRUG INTERACTION; GRAPEFRUIT JUICE; HUMAN; LIVER METABOLISM; MALE; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

EID: 0036091282     PISSN: 03125963     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003088-200241040-00004     Document Type: Article

References (25)

1. Grapefruit juice-drug interactions
2. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents. Decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins
3. Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein
4. Drug-grapefruit juice interactions
5. OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine
6. P-glycoprotein: A defense mechanism limiting oral bioavailability and CNS accumulation of drugs
7. P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
8. Grapefruit juice selectively inhibits OATP not P-glycoprotein
9. P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans
10. Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells
11. Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist. 1st communication: Receptor selectivity, antihistaminic activity, and antiallergenic effects
12. Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist: 2nd communication: Lack of central nervous system and cardiovascular effects
13. Efficacy and tolerability of once-daily 5mg desloratadine, an H1-receptor antagonist, in patients with seasonal allergic rhinitis: Assessment during the spring and fall allergy seasons
14. Desloratadine: A new, nonsedating, oral antihistamine
15. Once-daily desloratadine improves the signs and symptoms of chronic idiopathic urticaria: A randomized, double-blind, placebo-controlled study
16. Lack of electrocardiographic effects when desloratadine and ketoconazole are coadministered
17. Lack of electrocardiographic interaction between desloratadine and erythromycin
18. Lack of drug interactions between desloratadine and other common medications
19. In vitro characterization of the inhibition profile of loratadine, desloratadine, and 3-OH-desloratadine for five human cytochrome P-450 enzymes
20. Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein
21. Cardiovascular safety of second-generation antihistamines
22. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine
23. Amounts and variation in grapefruit juice of the main components causing grapefruit-drug interaction
24. Citrus juices are potent inhibitors of intestinal OATP but not P-glycoprotein