Search for dissertations about: "p-glycoprotein and cyp3a4"

Showing result 1 - 5 of 11 swedish dissertations containing the words p-glycoprotein and cyp3a4.

2. 1. Intestinal Permeability and Presystemic Extraction of Fexofenadine and R/S-verapamil

   Author : Christer Tannergren; Hans Lennernäs; Dirk KF Meijer; Uppsala universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Biopharmacy; Bioavailability; Fexofenadine; Verapamil; P-glycoprotein; CYP3A4; OATP; Enantioselective; Permeability; Caco-2; Intestinal perfusion; Biofarmaci; Biopharmacy; Biofarmaci;

   Abstract : The main objective of this thesis was to investigate the in vivo relevance of membrane transporters and cytochrome P450 (CYP) 3A4-mediated metabolism in the intestine and liver for the bioavailability of drugs in humans after oral administration.In the first part of the thesis, the main transport mechanisms involved in the intestinal absorption and bioavailability were investigated for fexofenadine, a minimally metabolized drug, which is a substrate for P-glycoprotein (P-gp) and members of organic anion transporting polypeptide (OATP) family. READ MORE

4. 2. Clinical studies of CYP3A4 and P-glycoprotein

   Author : Erik Sparve; Karolinska Institutet; Karolinska Institutet; []
   Keywords : ;

   Abstract : In the field of pharmacokinetics, cytochrome P450 enzymes have been extensively studied. The CYP450 enzyme with the most drug substrates is CYP3A4, but despite its significance, administration of a specific substrate to subjects is required to determine its activity, by measuring the metabolic ratio. READ MORE

5. 3. Pharmacogenetic Studies of Paclitaxel in Ovarian Cancer : focus on interindividual differences in pharmacodynamics and pharmacokinetics

   Author : Henrik Green; Curt Peterson; Peter Söderkvist; Per Rosenberg; Håkan Melhus; Linköpings universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; pharmacogenetics; paclitaxel; LC MS; Taxol; ovarian cancer; pharmacokinetics; CYP2C8; CYP3A4; ABCB1; äggstockscancer; paklitaxel; Clinical pharmacology; Klinisk farmakologi;

   Abstract : Ovarian cancer is one of the most common female cancer diseases in the world today and in Sweden more than 800 new cases are diagnosed every year. The standard treatment consists of chemotherapy with paclitaxel in combination with carboplatin after initial cytoreductive surgery. READ MORE

6. 4. Drug Transport and Metabolism in Rat and Human Intestine

   Author : Sofia Berggren; Hans Lennernäs; Janet Hoogstraate; Patrick Augustijns; Uppsala universitet; []
   Keywords : Biopharmacy; Ussing chamber; microsome; single-pass perfusion; human; rat; intestine; permeability; efflux; P-glycoprotein; metabolism; cytochrome P450; ropivacaine; lidocaine; bupivacaine; Biofarmaci; PPX;

   Abstract : One of the aims of this thesis was to investigate the involvement of efflux proteins, such as the P-glycoprotein (Pgp), in the drug transport in different regions of the rat and the human intestine. The intestinal extrusion of intracellularly formed CYP3A4 metabolites, including whether this extrusion might be mediated by Pgp, was also studied. READ MORE

7. 5. Intestinal barriers to oral drug absorption: Cytochrome P450 3A and ABC-transport proteins

   Author : Helena Engman; Per Artursson; Hans Lenernäs; Heyo K Kroemer; Uppsala universitet; []
   Keywords : MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Pharmaceutics; oral drug delivery; bioavailability; human jejunum; Caco-2; ABC-transporter; P-glycoprotein; CYP3A; Galenisk farmaci; Pharmaceutics; Galenisk farmaci;

   Abstract : The subject of this thesis was to study two intestinal barriers to oral drug bioavailability, drug efflux proteins of the ABC-transporter family, and in particular ABCB1/P-glycoprotein (Pgp), and the drug metabolizing enzyme cytochrome P450 (CYP) 3A4. At the onset of this thesis, similarities between CYP3A4 and Pgp in terms of their tissue distribution and gene regulation, along with overlapping substrate specificities, had generated the hypothesis that CYP3A4 and Pgp may have a complementary function and thus form a coordinated intestinal barrier to drug absorption and gut wall metabolism. READ MORE