Refine your search
Collections
Year
A B C D E F G H I J K L M N O P Q R S T U V W X Y Z All
Bhatt, Parloop A.
- Interlinking Between Altered Thyroid State and Development of Insulin Resistance: A Review
Abstract Views :208 |
PDF Views:2
Authors
Affiliations
1 Shri Sarvajanik Pharmacy College, Mehsana-384001, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
1 Shri Sarvajanik Pharmacy College, Mehsana-384001, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
Source
Research Journal of Pharmacology and Pharmacodynamics, Vol 3, No 5 (2011), Pagination: 234-240Abstract
It has long been recognized that thyroid hormones have marked effects on glucose homeostasis. Glucose intolerance is associated with hyperthyroidism and most recently it was shown that hypothyroidism is characterized by insulin resistance (IR). The interaction between thyroid function and insulin sensitivity is an important contributor to diabetic dyslipidemia. Effect of thyroid status on insulin sensitivity is of great interest but despite various studies reveal conflicting data on this subject. Thyroid disorders, including both hypo- and hyperthyroidism, may be associated with IR due to a plethora mechanism like, increased FFA, accumulation of intramyocellular lipids (IMCLs), increase in (Tumor Necrosis Factor)TNF-α, altered peripheral glucose disposal, altered blood flow, impaired GLUT4 translocation, decreased glycogen synthesis, down regulated intracellular glucose catabolism, decreased muscle oxidative capacity and many more contributing factors.Keywords
Insulin Resistance, Hyperthyroidism, Hypothyroidism, Thyroid Hormones.
References
- Rohdenburg GL. Thyroid diabetes. Endocrinol. 4; 1920: 63.
- Melpomeni P et al. Skeletal muscle insulin resistance in endocrine disease J Biomed Biotechnol. 2010.
- Kumar HK et al., Association between thyroid hormones, insulin resistance and metabolic syndrome. Endocrine Abs. 19; 2009: 339.
- Amati F et al., Improvements in insulin sensitivity are blunted by subclinical hypothyroidism. Med Sci Sports Exerc. 41 (2); 2009: 265-269.
- Raboudi N et al. Fasting and postabsorptive hepatic glucose and insulin metabolism in hyperthyroidism. Am J Physiol.; 256 (1); 1989: E159-E166.
- Weinstein SP et al., Regulation of GLUT2 glucose transporter expression in liver by thyroid hormone: evidence for hormonal regulation of the hepatic glucose transport system. Endocrinol. 135; 1994: 649-654.
- Viguerie N et al., Regulation of human adipocyte gene expression by thyroid hormone. J Clin Endocrinol Metab. 87; 2002: 630-634.
- Clement K et al., In vivo regulation of human skeletal muscle gene expression by thyroid hormone. Genome Res. 12; 2002: 281-291.
- D'Arezzo S et al., Rapid nongenomic effects of 3,5,3'-triiodo-
l -thyronine - on the intracellular pH of L-6 myoblasts are mediated by intracellular calcium mobilization and kinase pathways. Endocrinol. 145 (12); 2004: 5694-5703.
- Irrcher I eta l., Thyroid hormone (T3) rapidly activates p38 and AMPK in skeletal muscle in vivo. J Applied Physiol.104 (1); 2008: 178-185.
- Kim SR et al., A hypothesis of synergism: the interrelationship of T3 and insulin to disturbances in metabolic homeostasis. Med Hypotheses. 59 (6); 2002: 660-66.
- Roos A et al., Thyroid function is associated with components of the metabolic syndrome in euthyroid subjects. J Clin Endocrinol Metab. 92 (2); 2007: 491-496.
- Resmini E et al. Secondary diabetes associated with principal endocrinopathies: the impact of new treatment modalities. Acta Diabetol. 46 (2); 2009: 85-95.
- Dimitriadis G et al., Glucose and lipid fluxes in the adipose tissue after meal ingestion in hyperthyroidism. J Clin Endocrinol Metab. 91 (3); 2006: 1112-1118.
- Vinik AI, Pinstone BL, and Hoffenberg R. Studies on raised free fatty acids in hyperthyroidism. Metabolism. 19 (2); 1970: 93-101.
- Griffin ME et al. Free fatty acid-induced insulin resistance is associated with activation of protein kinase C theta and alterations in the insulin signaling cascade. Diabetes. 48 (6); 1999: 1270-1274.
- Frayn KN. Insulin resistance and lipid metabolism. Curr Opin Lipidol. (4); 1993:197-204.
- Steiner G, Morita S, and Vranic M. Resistance to insulin but not to glucagon in lean human hypertriglyceridemics. Diabetes. 29; 1980: 899-905.
- Peppa M et al., Skeletal muscle insulin resistance in endocrine disease. J Biomed Biotechnol. 2010.
- DeFronzo RA et al.,Effects of insulin on peripheral and splanchnic glucose metabolism in noninsulin-dependent (type II) diabetes mellitus. J Clin Invest. 76 (1); 1985: 149-155.
- Guo ZK, Jensen MD. Accelerated intramyocellular triglyceride synthesis in skeletal muscle of high-fat-induced obese rats. Intl J Obesity. 27; 2003: 1014-1019.
- Zhou L, Guo ZK. Muscle type-dependent responses to insulin in intramyocellular triglyceride turnover in obese rats. Obes Res. 13; 2005: 2081-2087.
- Okada T et al., Essential role of phosphatidylinositol 3-kinase in insulin-induced glucose transport and antilipolysis in rat adipocytes: studies with a selective inhibitor wortmannin. J Biol Chem. 269; 1994: 3568-3573.
- Coen PM et al., Insulin Resistance Is Associated With Higher Intramyocellular Triglycerides in Type I but Not Type II Myocytes Concomitant With Higher Ceramide Content. Diabetes. 59 (1); 2010: 80-88.
- Summers SA. Ceramides in insulin resistance and lipotoxicity. Prog Lipid Res. 45; 2006: 42-72.
- Mohamed-Ali V, Pinkney JH and Coppack SW. Adipose tissue as an endocrine and paracrine organ. International Journal of Obesity and Related Metabolic Disorders, 22; 1998: 1145-1158.
- Katsuki A et al., Serum levels of tumor necrosis factor-alpha are increased in obese patients with noninsulin-dependent diabetes mellitus. J. Clin. Endocrinol. Metab. 83; 1998: 859-862.
- Fernandez-Real JM et al., Circulating interleukin 6 levels, blood pressure, and insulin sensitivity in apparently healthy men and women. J. Clin. Endocrinol. Metab. 86; 2001: 1154-1159.
- Ahmet K et al., Serum IL-6 and TNF-α in Patients With Thyroid Disorders. Tr. J. of Medical Sciences. 29; 1999: 25-29.
- Hotamisligil GS et al., IRS-1-mediated inhibition of insulin receptor tyrosine kinase activity in TNF-alpha-and obesity-induced insulin resistance. Science. 271; 1996: 665-668.
- Hotamisligil GS, Shargill NS, and Spiegelman, BM. Adipose expression of tumor necrosis factor-alpha: direct role in obesitylinked insulin resistance. Science. 259; 1993: 87-91.
- Sundgren-Andersson AK, Ostlund P and Bartfai T. IL-6 is essential in TNF-alpha-induced fever. Am. J. Physiol. 275; 1998: R2028 - R2034.
- Tsigos C et al., Dose-dependent effects of recombinant human interleukin-6 on glucose regulation. J. Clin. Endocrinol. Metab. 82; 1997: 4167-4170.
- Kanemaki T et al., Interleukin 1β and interleukin 6, but not tumor necrosis factorα, inhibit insulin-stimulated glycogen synthesis in rat hepatocytes. Hepatology. 87; 1998: 1296-1303.
- Senn JJ et al., Interleukin-6 induces cellular insulin resistance in hepatocytes. Diabetes. 51; 2002: 3391-9.
- Rui L et al., Insulin/IGF-1 and TNF-α stimulate phosphorylation of IRS-1 at inhibitory Ser307 via distinct pathways. J Clin Invest. 107 (2); 2001: 181-189.
- Pirola L, Johnston AM, and Van Obberghen E. Modulation of insulin action. Diabetologia. 47 (2); 2004: 170-184.
- Liggett SB, Shah SD, and Cryer PE. Increased fat and skeletal muscle β-adrenergic receptors but unaltered metabolic and hemodynamic sensitivitiy to epinephrine in vivo in experimental human thyrotoxicosis. J Clin Invest. 83 (3); 1989: 803-809.
- Martin WH et al., Skeletal muscle beta-adrenoceptor distribution and responses to isoproterenol in hyperthyroidism. Am J Physiol. 262 (4); 1992: E504-510.
- Chiasson JL, Shikama H, Chu DT, Exton JH. Inhibitory effect of epinephrine on insulin-stimulated glucose uptake by rat skeletal muscle. J Clin Invest. 68; 1981: 706-713.
- Mulder AH et al., Adrenergic receptor stimulation attenuates insulin-stimulated glucose uptake in 3T3-L1 adipocytes by inhibiting GLUT4 translocation. Am J Physiol Endocrinol Metab. 289 (4); 2005: E627-633.
- Lee AD et al., Effects of epinephrine on insulin-stimulated glucose uptake and GLUT-4 phosphorylation in muscle. Am J Physiol Cell Physiol. 273; 1997: C1082-1087.
- Dimitriadis GD, Raptis SA. Thyroid hormone excess and glucose intolerance. Exp Clin Endocrinol Diabetes. 109 (2); 2001: S225-239.
- Bevan S et al. The effects of insulin on transport and metabolism of glucose in skeletal muscle from hyperthyroid and hypothyroid rats. Eur J Clin Invest. 27(6); 1997: 475-83.
- Weinstein SP, O'Boyle E, and Haber RS. Thyroid hormone increases basal and insulin-stimulated glucose transport in skeletal muscle. The role of GLUT4 glucose transporter expression. Diabetes. 43 (10); 1994: 1185-1189.
- Dimitriadis G et al., Thyroid hormone excess increases basal and insulin-stimulated recruitment of GLUT3 glucose transporters on cell surface. Horm Metab Res. 37 (1); 2005: 15-20.
- Maratou E et al., Studies of insulin resistance in patients with clinical and subclinical hypothyroidism. Eur J Endocrinol. 160(5); 2009: 785-90.
- Dimitriadis G et al., IGF-I increases the recruitment of GLUT4 and GLUT3 glucose transporters on cell surface in hyperthyroidism. Eur J Endocrinol. 158 (3); 2008: 361-366.
- Jenkins RC et al., Association of elevated insulin-like growth factor binding protein-1 with insulin resistance in hyperthyroidism. Clin Endocrinol. 52 (2); 2000: 187-195.
- Dimitriadis G et al., Insulin-stimulated rates of glucose uptake in muscle in hyperthyroidism: the importance of blood flow. J Clin Endocrinol Metab. 93 (6); 2008: 2413-2415.
- Harris PE et al., Forearm muscle metabolism in primary hypothyroidism. Eur J Clin Invest. 23 (9); 1993: 585-588.
- O'Meara NM et al., Alterations in the kinetics of C-peptide and insulin secretion in hyperthyroidism. J Clin Endocrinol Metab. 76 (1); 1993: 79-84.
- Makino M et al., Effect of eicosapentaenoic acid ethyl ester on hypothyroid function. J Endocrinolo. 171 (2); 2001: 259-265.
- Stannard SR, Johnson NA. Insulin resistance and elevated triglyceride in muscle: more important for survival than 'thrifty' genes?. J Physiol. 554 (3); 2004: 595-607.
- Randle PJ et al., The glucose fatty-acid cycle: Its role in insulin sensitivity and the metabolic disturbances of diabetes mellitus. Lancet. 1; 1963: 785-789.
- Roden M et al., Mechanism of free-fatty acid-induced insulin resistance in humans. J Clin Invest. 97; 1996: 2859-2865.
- Krebs M et al., Free fatty acids inhibit the glucose-stimulated increase of intramuscular glucose-6-phosphate concentration in humans. J Clin Endocrinol Metab. 86; 2001: 2153-2160.
- Kraegen EW, Cooney GJ. The role of free fatty acids in muscle insulin resistance. Diabetes Ann. 12; 1999: 141-159.
- Boden J et al., Effects of Acute Changes of Plasma Free Fatty Acids on Intramyocellular Fat Content and Insulin Resistance in Healthy Subjects. Diabetes. 50 (7); 2001: 1612-1627.
- Kayar SR et al., Acute effects of endurance exercise on mitochondrial distribution and skeletal muscle morphology. Eur J Appl Physiol. 54; 1986: 578-584.
- Dagenais GR, Tancredi RG and Zierler KL. Free fatty acid oxidation by forearm muscle at rest, and evidence for an intramuscular lipid pool in the human forearm. J Clin Invest. 58; 1976: 421-431.
- Madden MC et al., 1H NMR spectroscopy can accurately quantitate the lipolysis and oxidation of cardiac triacylglycerols. Biochim Biophys Acta. 1169; 1993: 176-182.
- Vock R et al., Design of the oxygen and substrate pathways. VI. structural basis of intracellular substrate supply to mitochondria in muscle cells. J Exp Biol. 199; 1996: 1689-1697.
- Taylor CR et al., High fat diet improves aerobic performance by building mitochondria. Physiologist. 37; 1994: A84.
- Boden G et al., Effects of fat on insulin-stimulated carbohydrate metabolism in normal men. J Clin Invest. 88; 1991: 960-966.
- Han DH et al., Insulin resistance of muscle glucose transport in rats fed a high-fat diet: a re-evaluation. Diabetes. 46; 1997: 1761-1767.
- Prentki M, Corkey BE. Are the β-cell signaling molecules malonyl-CoA and cytosolic long-chain acyl-CoA implicated in multiple tissue defects of obesity and NIDDM? Diabetes. 45; 1996: 273-283.
- Boden G et al., Mechanisms of fatty-acid induced inhibition of glucose uptake. J Clin Invest. 93; 1994: 2438-2446.
- Momose M et al., Increased cardiac sympathetic activity in patients with hypothyroidism as determined by iodine-123 metaiodobenzylguanidine scintigraphy. Eur J Nucl Med., 24 (9); 1997: 1132-1137.
- Mitrou P et al., Insulin resistance in hyperthyroidism: the role of IL6 and TNF alpha. Eur J Endocrinol. 162 (1); 2010: 121-126.
- Cettour-Rose P et al., Hypothyroidism in rats decreases peripheral glucose utilisation, a defect partially corrected by central leptin infusion. Diabetologia. 48 (4); 2005: 624-633.
- Rochon C et al., Response of glucose disposal to hyperinsulinaemia in human hypothyroidism and hyperthyroidism Clin Sci. 104 (1); 2003: 7-15.
- Diaz GB et al., Changes induced by hypothyroidism in insulin secretion and in the properties of islet plasma membranes. Arch Int Physiol Biochim Biophys. 101 (5); 1993: 263-269.
- Mackowiak P et al., The influence of hypo- and hyperthyreosis on insulin receptors and metabolism. Arch Physiol Biochem. 107 (4); 1999: 273-279.
- Duntas LH. Thyroid disease and lipids. Thyroid. 12 (4); 2002: 287-293.
- Howard BV. Insulin resistance and lipid metabolism. Am J Cardiol. 84 (1A); 1999: 28J-32J.
- Sanghvi A et al., Differential suppression of lymphocyte cholesterol synthesis by low density lipoprotein and erythrocyte insulin receptors in normolipidemic subjects. Atherosclerosis. 49 (3); 1983: 307-318.
- Gual P et al., Fatty acid-induced insulin resistance: role of insulin receptor substrate 1 serine phosphorylation in the retroregulation of insulin signalling. Biochem Soc Trans.31(6); 2003: 1152-56.
- P-Glycoprotein - A Unique Transporter Pump
Abstract Views :212 |
PDF Views:2
Authors
Affiliations
1 Shri Sarvajanik Pharmacy College, Mehsana, Gujarat, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
1 Shri Sarvajanik Pharmacy College, Mehsana, Gujarat, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
Source
Research Journal of Pharmacology and Pharmacodynamics, Vol 3, No 5 (2011), Pagination: 241-245Abstract
P-Glycoprotein (P-gp)/MDR1 is the 170-kDa ABC drug transporter protein. It is a member of the ABC(ATP Binding Cassette)super family.It is involved in limiting the harmful exposure of toxins, drugs, and xenobiotics to the body by extruding them into the gastrointestinal tract, bile and urine. Drugs or substrates can cross into the cell membrane by simple diffusion, filtration, or by specialized transport. The first step in drug efflux is drug recognition by P-gp followed by ATP-binding and subsequent hydrolysis. Finally, the generated energy is utilized to efflux substrate outside the cell membrane through central pore. P-gp acts as a rate limiting step during various stages of pharmacokinetic of drug but mainly on the absorption. Different drugs have different impact on P-gp expression. Some drugs are substrate of p-gp while some are inducers or inhibitors of P-gp. Altered P-gp/MDR1 activity due to induction and/or inhibition can cause drug-drug interactions with altered drug pharmacokinetics and response of drug. P-gpmayshow gender basis differences and so drug effect in individuals.References
- Chen J, Raymond K.The role of CYP3A4 and p-glycoprotein in food-drug and herb-drug interactions, Australian pharmacist 2006, 25(9), 732-738.
- Croop JM. P-glycoprotein structure and evolutionary homologies.Cytotechnology 1993,12:1-32.
- Lincke CR, Broeks A, Plasterk RH, Borst P. The expression of two P-glycoprotein (P-gp) genes in transgenic Caenorhabditis elegans is confined to intestinal cells. EMBO J1993, 12, 1615-1620.
- Lin JH.Drug-drug interaction mediated by inhibition and induction of P-glycoprotein.Advanced Drug Delivery Reviews 2003, 55, 53-81.
- Martin C, Berridge G, Higgins CF, Mistry P, Charlton P, Callaghan R. Communication between multiple drug binding sites on P-glycoprotein. Molecular Pharmacology 2000a.58, 624-632.
- Shilling RA, Venter H, Velamakanni S, Bapna A, Woebking B, Shahi S, Van Veen HW. New light on multidrug binding by an ATP-binding-cassette transporter. Trends in Pharmacology Sciences 2006, 27, 195-203.
- Loo TW, Bartlett MC, Clarke DM. Simultaneous binding of two different drugs in the binding pocket of the human multidrug resistance P-glycoprotein. J Biol.Chem. 2003a, 278, 39706-39710.
- Wang RB, Kuo CL, Lien LL, Lien EJ. Structure-activity relationship: Analyses of p-glycoprotein substrates and inhibitors. JClin. Pharm. Ther.2003, 28, 203-228.
- Sonveaux N, Vigano C, Shapiro AB, Ling V, Ruysschaert JM. Ligand-mediated tertiary structure changes of reconstituted P-glycoprotein. J Biol. Chem. 1999, 274, 17649-17654.
- Zhou SF.Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition, Xenobiotica 2008. 38(7-8): 802-832.
- Romsicki Y, Sharom F. The ATPase and ATP-binding functions of P-glycoprotein modulation by interaction with defined phospholipids. Eur J Biochem 1998, 256, 170-178.
- Buxbaum E. Co-operating ATP sites in the multiple drug resistance transporter Mdr1. Eur J Biochem 1999, 265, 54-63.
- Ambudkar SV, Dey S, Hrycyna. Biochemical, cellular and pharmacological aspects of multidrug transporter. Annu Rev Pharmacol Toxicol 1999, 39,361-98.
- Ueda K, Taguchi Y, Morishima M. How does P-glycoprotein recognize its substrates? Semin Cancer Biol 1997.8, 151-9.
- Tandon V, Kapoor B.Bano G, Gupta S, Gillani Z, Gupta S, Kour D.P-glycoprotein: pharmacological relevance. Indian J Pharmacol 2006, 38(1),13-24.
- Van Veen HW, Higgins CF,Konings WN. Molecular basis of multidrug transport by ATP-binding cassette transporters: a proposed two-cylinder engine model, J. Mol. Microbiol. Biotechnol 2001, 3, 185-192.
- Sauna ZE, Ambudkar SV. Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein. ProcNatlAcadSci 2000, 97, 2515-20.
- Mark FR, Alhaji BK, Richard C, Christopher FH, Robert CF. Three-dimensional structures of the mammalian multidrug resistance P-glycoprotein demonstrates major conformational changes in the transmembrane domains upon nucleotide binding. J BiolChem 2003, 278, 8294-99.
- Loo TW, Clarke DM. Do drug substrates enter the common drug-binding pocket of P-glycoprotein through "gates"? Biochem Biophys Res Commun 2005, 329, 419-22.
- Varma MVS, Perumal OP,Panchagnula R. Functional role of P-glycoprotein in limiting peroral drug absorption: optimizing drug delivery.Current Opinion in Chemical Biology 2006, 10, 367-373.
- Cortes-Selva F, Munoz-Martinez F, Ilias A, Jimenez AI, Varadi A, Gamarro F, et al. Functional expression of a multidrug P-glycoprotein transporter of Leishmania. BiochemBiophys Res Commun 2005, 329, 502-7.
- Hayashi M, Tomita M, Awzu S.Transcellular and paracellular contribution to transport processes in the colorectal route. Adv. Drug Deliv. Rev. 1997, 28, 191-204.
- Hunter J, Hirst BH. Intestinal secretion of drugs. The role of P-glycoprotein and related drug efflux systems in limiting oral dru absorption. Adv. Drug Del. Rev.1997, 25, 129-157.
- Evers R, Kool M, Van Deemter L, Janssen H, Calafat J, Oomen LCJM, Paulusma CC, Oude Elferink, RPJ, Baas F, Schinkel AH, Borst P. Drug export activity of the human canalicular multispecific organic anion transporter in polarised kidney MDCK cells expressing cMOAT (MRP2) cDNA. J. Clin. Invest. 1998, 101, 1310-1319.
- Fromm MF, Kauffman HM, Fritz P, Burk O, Kroemer HK, Warzok RW, Eichelbaum,M, Siegmund W, Schrenk D. The effect of rifampin treatment on intestinal expression of human MRP transporters. Am. J. Pathol. 2000, 157, 1575-1580.
- Watkins PB. Drug metabolism by cytochromes P450 in the liver and small bowel. Gastrointest. Pharmacol. 1992, 21, 511-526.
- Seelig A. A general pattern for substrate recognition by P-glycoprotein. Eur. J. Biochem. 1998, 251, 252-261.
- Seelig A, Landwojtowicz E. Structure-activity relationship of P-glycoprotein substrates and modifiers. Eur. J.Pharm. Sci.2000, 12, 31-40.
- Bain L, McLachlan J, LeBlanc G. Structure-activity relationships for xenobiotic transport substrates and inhibitory ligands of P-glycoprotein. Environmental Health Perspectives 1997, 105, 812-818.
- Wang RB, Kuo CL, Lien LL, Lien EJ. Structure-activity relationship: Analyses of p-glycoprotein substrates and inhibitors. J. Clin. Pharm. Thera. 2003, 28, 203-228.
- Raub TJ. P-glycoprotein recognition of substrates and circumvention through rational drug design. Mol.Pharmacol.2006, 3, 3-25.
- Machado CG, Calado RT,Garcia AB, Falcao RP.Age-related changes of the multidrug resistance P-glycoprotein function in normal human peripheral blood T lymphocytes, Br J. Med. Boil. Research 2003, 36, 1653-1657.
- Lesliea EM, Deeleyb RG, Coleb PC. Multidrug resistance proteins: role of P-glycoprotein, MRP1, MRP2, and BCRP (ABCG2) in tissue defense. Toxicol. Appl. Pharmacol. 2005, 204, 216-237.
- Dean M.The human ATP-binding cassette (ABC) transporter superfamily. National Center for Biotechnology Information (NCBI) 2002, National library of Medicine, Bethesda, MD, USA.
- Shiraga K, Sakaguchi K, Senoh T, Ohta T.Modulation of doxorubicin sensitivity by cyclosporine A in hepatocellular carcinoma cells and their doxorubicin-resistant sublines. J. Gastroenterol. Hepatol.2001, 16, 460-466.
- Chaudhary P, Roninson I. Induction of multidrug resistance in human cells by transient exposure to different chemotherapeutic drugs. J. Natl. Caner. Inst.1993, 85, 632-639.
- Schuetz EG, Furuya KN,Schuetz JD. "Interindividual Variation in Expression of P-Glycoprotein in Normal Human Liver and Secondary Hepatic Neoplasms," Journal of Pharmacology and ExperimentalTherapeutics 1995, 275(2), 1011-1018.
- Wolbold R, Klein K, Burk O, et al. "Sex is a Major Determinant of CYP3A4 Expression in Human Liver," Hepatology, 2003, 8(4), 978-988.
- Rabbaa L, Dautrey S, Colas-Linhart N, et al. "Intestinal Elimination of Ofloxacin Enantiomers in the Rat: Evidence of a Carrier-Mediated Process," Antimicrobial Agents and Chemotherapy 1996, 40(9), 2126-2130.
- Aminimanizani A, Beringer P, Jelliffe R.Comparative Pharmacokinetics and Pharmacodynamics of the Newer Fluoroquinolone Antibacterials.Clinical Pharmacokinetics 2001, 40(3), 169-187.
- Carrasco-Portugal MC, Flores-Murrieta FJ. Gender Differences in the Pharmacokinetics of Oral Drugs.Pharmacology and Pharmacy, 2011, 2, 31-41.
- Benet LZ, Cummins CL. The drug efflux: Metabolism alliance-Biochemical aspects. Adv Drug Deliv Rev 2001, 50, S3-S11.
- Van Asperen J,Schinkel AH, Beijnen JH, et al. Altered pharmacokinetics of vinblastine in MDR lA P-glycoprotein deficient mice. J Natl Cancer Inst 1996, 88, 994-999.
- Benet LZ, Cummins CL, Wu CY. Unmasking the dynamic interplay between efflux transporters and metabolic enzymes. Int J Pharm 2004, 277, 3-9.
- VanAsperen J, van Tellingen O, Tijssen F, et al. Increased accumulation of doxorubicin and doxorubicinol in cardiac tissue of mice lacking mdr la P-glycoprotein. Br J Cancer 1999, 79, 108-113.
- VanAsperen J, van Tellingen O, Schinkel AH, et al: Comparative pharmacokinetics of vinblastine after a 96-hour continuous infusion in wild type mice and mice lacking mdr la P-glycoprotein. J Pharmacol Exp Ther 1999, 289, 329-333.
- Schuetz EG, Furuya KN, Scheutz JD.Interindividual variation in expression of P-Glycoprotein in normal human liver and secondary hepatic neoplasms. J Pharmacol Exp Ther 1995, 275, 1011-1018.
- Cummins CL, Wu C, Benet LZ. Sex-related differences in the clearance of cytochrome P450 3A4 substrates may be caused by P-glycoprotein. Clin Pharmacol Ther 2002, 72, 474-489.
- Yokogawa K, Takahashi M, Tamai I, et al. P-glycoprotein dependent disposition kinetics of tacrolimus: Studies in mdr la knockout mice. Pharm Res 1999, 16, 1213-1218.
- Meyers PA, Schwartz CL, Krailo M, et al. Gender Differences in p-Glycoprotein: Drug Toxicity and Response, J Clin Oncol 2005, 23, 2004-2011.
- Chiou WL, Chung SM, Wu, Ta C: Potential role of P-Glycoprotein in affecting hepatic metabolism of drugs. Pharm Res 2000, 17, 903-905.
- Singh S, Parulekar W, Murray N, et al: Influence of sex on toxicity and treatment outcome in small-cell lung cancer. J Clin Oncol 2005, 23, 850-856.
- Kando JC, Yonkers KA, Cole JO. "Gender as a Risk Factor for Adverse Events to Medications," Drugs1995, 50(1), 1-6.
- Warrington JS, Greenblatt DJ, and Moltke LL. The Effect of Age on P-Glycoprotein Expression and Function in the Fischer-344 Rat. The journal of pharmacology and experimental therapeutics 2004, 309(2):730-736.
- Larsen UL, Olesen LH, Nyvold CG, Eriksen J, Jakobsen P, oestergaard M, Autrup H and Andersen V. Human intestinal P-glycoprotein activity estimated by the model substrate digoxin. Scand J Clin Lab Invest 2007, 67, 123-134.
- Bauer M, Karch R, Neumann F, Abrahiml A, Kletter K, Mueller M, Langer O. Decreased blood-brain barrier P-glycoprotein function with aging. J Nucl Med. 2009, 50 (2), 606.
- Significance of Estrogen in Acute Coronary Syndrome
Abstract Views :215 |
PDF Views:0
Authors
Affiliations
1 Shri Sarvajanik Pharmacy College, Mehsana-384001, Gujarat, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
4 Care Institute of Medical Sciences, Ahmedabad, IN
1 Shri Sarvajanik Pharmacy College, Mehsana-384001, Gujarat, IN
2 Shri Sarvajanik Pharmacy College, Mehsana, IN
3 L. M. College of Pharmacy, Ahmedabad, IN
4 Care Institute of Medical Sciences, Ahmedabad, IN
Source
Research Journal of Pharmacology and Pharmacodynamics, Vol 3, No 4 (2011), Pagination: 210-214Abstract
Estrogen, a cardioprotective agent, potentiates acetylcholine-induced increase in coronary blood flow, decreases coronary endothelin-1 levels, reduces ischemia, enhances fibrinolysis, shifts markers of coagulation toward hypercoagulability, and increases blood levels of matrix metalloproteinase-9, involved in plaque disruption and inflammatory markers like interleukin-6 and C-reactive protein. Rates of cardiovascular disease in women tend to rise during menopause, when estrogen level decreases. Hormone replacement therapy (HRT) provides exogenous estrogen to encounter the deficiency of estrogen into body, which demonstrates favorable cardioprotective effects, if initiated few years within the onset of menopause. However, use of HRT is controversial in preventing progression of the diseases at the later stages; since it cannot repair the damage already occurred. The therapy reduces the progression rate of atherosclerosis in post-menopausal women, who are not suffering from cardiovascular disease. However, in patients with cardiovascular disease or risk factors, estrogen therapy enhances cardiac events.Keywords
Estrogen, Hormone Replacement Therapy, Cardiovascular Disease, Menopause.References
- Pifarre R, Scanlon P, editors. Evidence-based management of the acute coronary syndrome. Philadelphia: Hanley and Belfus, Inc; 2001.
- La Vecchia C. Sex hormones and cardiovascular risk. Hum Reprod.7; 1992:162-7.
- Li Xiang-Ping, Zhou Yan, Zhao Shui-Ping, Gao Mei, Zhou Qichang, Li Yan-Sheng. Effect of endogenous estrogen on endothelial function in women with coronary heart disease and its mechanism. Clinica Chimica Acta. 339; 2004: 183-8.
- Rossouw JE. Hormones, genetic factors, and gender differences in cardiovascular disease. Cardiovasc Res. 53; 2002: 550.
- Baker L, Meldrum KK, Wang M, Sankula R, Vanam R, Raiesdana A, et al. The Role of Estrogen in Cardiovascular Disease. Journal of Surgical Research.115; 2003: 325-44.
- Williams JK, Adams MR, Klopfenstein HS. Estrogen modulates responses of atherosclerotic coronary arteries. Circulation. 81; 1990: 1680-7.
- Herrington DM, Braden GA, Williams JK, Morgan TM. Endothelial-dependent coronary vasomotor responsiveness in postmenopausal women with and without estrogen replacement therapy. Am J Cardiol. 73; 1994: 951-2.
- Barrett-Connor E, Grady D. Hormone replacement therapy, heart disease, and other considerations. Annu Rev Public Health. 19; 1998: 55 - 72.
- Grady D, Herrington D, Bittner V, et al for the HERS Research Group. Cardiovascular disease outcomes during 6.8 years of hormone therapy: Heart and Estrogen/Progestin Replacement Study follow-up (HERS II). J Am Med Assoc. 288; 2002:49-57.
- Li Xiang-Ping, Zhou Yan, Zhao Shui-Ping, Gao Mei, Zhou Qichang, Li Yan-Sheng. Effect of endogenous estrogen on inhibition of human vascular smooth muscle cell proliferation by estrogens. Mol. Cell. Endocrinol. 219; 2004: 17-26.
- Simpson ER, et al. Aromatase expression in health and disease. Recent Prog. Horm. Res. 199, 52, 185-213.
- Bruch, H.R. et al. Androstenedione metabolism in cultured human osteoblastlike cells. J. Clin. Endocrinol. Metab. 75; 1992: 101-5.
- Bayard F, et al. Oestrogen biosynthesis, oestrogen metabolism and functional oestrogen receptors in bovine aortic endothelial cells. Ciba Found. Symp. 191; 1995: 122-32.
- Sasano H, et al. Aromatase and sex steroid receptors in human vena cava. Endocr. J. 46; 1999: 233-42.
- Naftolin F, et al. The formation of estrogens by central neuroendocrine tissues. Recent Prog. Horm. Res. 31; 1975: 295-319.
- Liao JK. Endothelium and acute coronary syndromes. Clinical Chemistry. 44, 8(B); 1998: 1799-1808.
- Green S, Walter P, Kumar V, Krust A, Bornert JM, Argos P, Chambon P. Human oestrogen receptor cDNA: sequence, expression and homology to v-erb-A. Nature. 320; 1986: 134-9.
- Flouriot G, Brand H, Denger S, Metivier R, Kos M, Reid G, Sonntag-Buck V, Gannon F. Identification of a newisoform of the human estrogen receptor alpha (hER-α) that is encoded by distinct transcripts and that is able to repress hER-α activation function 1. EMBO J. 19; 2000: 4688-700.
- Mendelsohn ME, Karas RH. The protective effects of estrogen on the cardiovascular system. N Engl J Med. 340; 1999: 1801-11.
- Miller AP, Xing D, Feng W, Fintel M, Chen YF, Oparil S. Aged rats lose vasoprotective and anti-inflammatory actions of estrogen in injured arteries. Menopause. 14; 2007: 251-60.
- Nakamura Y, Suzuki T, Miki Y, Tazawa C, Senzaki K, Moriya T, et al. Estrogen receptors in atherosclerotic human aorta:
- Grady D, Rubin SM, Petitti DB, Fox CS, Black D, Ettinger B, Ernster VL, Cummings SR. Hormone therapy to prevent disease and prolong life in postmenopausal women. Ann. Intern. Med. 117; 1992: 1016-37.
- Caulin-Glaser T, Watson CA, Pardi R, Bender JR. Effects of 17β-estradiol on cytokine-induced endothelial cell adhesion molecule expression. J. Clin. Invest. 98; 1996: 36-42.
- Mendelsohn ME, Karas RH. The protective effects of estrogen on the cardiovascular system. N. Engl. J. Med. 340; 1999: 1801-11.
- Hayashi T, Yamada K, Esaki T, et al. Estrogen increases endothelial nitric oxide by a receptor mediated system. Biochem Biophys Res Commun. 214; 1995: 847-55.
- Hayashi T, Esaki T, Sumi D, et al. Modulating role of estradiol on arginase II expression in hyperlipidemic rabbits as an atheroprotective mechanism. ProcNatlAcadSci U S A. 103; 2006: 10485-90.
- Razmara A, Sunday L, Stirone C, Wang XB, Krause DN, Duckles SP, Procaccio V. Mitochondrial effects of estrogen are mediated by estrogen receptor alpha in brain endothelial cells. J. Pharmacol. Exp. Ther. 325; 2008: 782-90.
- Rosano GMC, Webb CM, Chierchia S, et al. Natural progesterone, but not medroxyprogesterone acetate, enhances the beneficial effect of estrogen on exercise-induced myocardial ischemia in postmenopausal women. J Am CollCardiol. 36; 2000: 2154-9.
- Rosano GMC, Caixeta AM, Chierchia S, et al. Short-term antiischemic effect of 17-estradiol in postmenopausal women with coronary artery disease. Circulation. 96; 1997: 2837-41
- Guetta V, Quyyumi AA, Prasad A, Panza JA, Waclawiw M, Cannon RO. The role of nitric oxide in coronary vascular effects of estrogen in postmenopausal women. Circulation. 96; 1997: 2795-801.
- Webb CM, Ghatei MA, McNeill JG, Collins P. 17-Estradiol decreases endothelin-1 levels in the coronary circulation of postmenopausal women with coronary artery disease. Circulation. 102; 2000: 1617-22.
- Vehkavaara S, Silveira A, Hakala-Ala-Pietilla T, et al. Effects of oral and transdermal estrogen replacement therapy on markers of coagulation, fibrinolysis, inflammation and serum lipids and lipoproteins in postmenopausal women. Thromb Haemost. 85; 2001: 619-25.
- Zanger D, Yang BK, Ardans J, et al. Divergent effects of hormone therapy on serum markers of inflammation in postmenopausal women with coronary artery disease on appropriate medical management. J Am CollCardiol. 36; 2000: 1797-802.
- Falk E. Pathogenesis of atherosclerosis. J Am CollCardiol. 47(8); 2006: C7-12.
- Kannel WB. The Framingham Study: historical insight on the impact of cardiovascular risk factors in men versus women. J Gend Specif Med. 5; 2002: 27-37.
- Clarkson TB. Estrogen effects on arteries vary with stage of reproductive life and extent of subclinical atherosclerosis progression. Menopause. 14; 2007: 373-84.
- Hulley S, Grady D, Bush T, Furberg C, Herrington D, Riggs B, Vittinghoff E. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart diseasein postmenopausal women. Heart and Estrogen/progestin Replacement Study (HERS) Research Group. JAMA. 280; 1998: 605.
- MacLennan AH. Hormone replacement therapy: a 2008 perspective. Obstetrics, Gynaecology and Reproductive Medicine. 19(1); 2008: 13-8.
- Tackett AH, Bailey AL, Foody JM, Carolynpperson-Hansen JM, Ohman EM, Hochman JS, et al. Hormone Replacement Therapy among Postmenopausal Women Presenting with Acute endothelial function in women with coronary heart disease and its mechanism. Clinica Chimica Acta. 339; 2004: 183-8.
- Antonicelli R, Olivieri F, Morichi V, Urbani E, Mais M. Prevention of cardiovascular events in early menopause: A possible role for hormone replacement therapy. International Journal of Cardiology. 130; 2008: 140-6.
- Post WS, Goldschmidt-Clermont PJ, Wilhide CC, et al. Methylation of the estrogen receptor gene is associated with aging and atherosclerosis in the cardiovascular system. Cardiovasc Res. 43; 1999: 985-91.