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    Bile Acid Sequestrants

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    Febrian Isharyadi
    1. Bile acid sequestrants work by binding to negatively charged bile acids in the intestine, forming insoluble complexes that are excreted in feces. This increases the conversion of cholesterol into bile acids and raises HDL levels while lowering LDL. 2. Common side effects include constipation, nausea, indigestion and flatulence due to gastrointestinal disturbances. Long term use may cause osteoporosis, hypertriglyceridemia, and vitamin/mineral deficiencies. 3. Fibrates are a class of drugs that lower triglycerides and modestly lower LDL while moderately raising HDL levels. They work by stimulating lipolysis, increasing fatty acid uptake in the liver, enhancing LDL cat

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    Bile Acid Sequestrants

    Uploaded by

    Febrian Isharyadi
    92 views4 pages
    1. Bile acid sequestrants work by binding to negatively charged bile acids in the intestine, forming insoluble complexes that are excreted in feces. This increases the conversion of cholesterol into bile acids and raises HDL levels while lowering LDL. 2. Common side effects include constipation, nausea, indigestion and flatulence due to gastrointestinal disturbances. Long term use may cause osteoporosis, hypertriglyceridemia, and vitamin/mineral deficiencies. 3. Fibrates are a class of drugs that lower triglycerides and modestly lower LDL while moderately raising HDL levels. They work by stimulating lipolysis, increasing fatty acid uptake in the liver, enhancing LDL cat

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    1. Bile acid sequestrants work by binding to negatively charged bile acids in the intestine, forming insoluble complexes that are excreted in feces. This increases the conversion of cholesterol into bile acids and raises HDL levels while lowering LDL. 2. Common side effects include constipation, nausea, indigestion and flatulence due to gastrointestinal disturbances. Long term use may cause osteoporosis, hypertriglyceridemia, and vitamin/mineral deficiencies. 3. Fibrates are a class of drugs that lower triglycerides and modestly lower LDL while moderately raising HDL levels. They work by stimulating lipolysis, increasing fatty acid uptake in the liver, enhancing LDL cat

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    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    92 views4 pages

    Bile Acid Sequestrants

    Uploaded by

    Febrian Isharyadi
    1. Bile acid sequestrants work by binding to negatively charged bile acids in the intestine, forming insoluble complexes that are excreted in feces. This increases the conversion of cholesterol into bile acids and raises HDL levels while lowering LDL. 2. Common side effects include constipation, nausea, indigestion and flatulence due to gastrointestinal disturbances. Long term use may cause osteoporosis, hypertriglyceridemia, and vitamin/mineral deficiencies. 3. Fibrates are a class of drugs that lower triglycerides and modestly lower LDL while moderately raising HDL levels. They work by stimulating lipolysis, increasing fatty acid uptake in the liver, enhancing LDL cat

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    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    of 4

    Bile acid sequestrants

    Bile acid synthesis is the main pathway of


    cholesterolcatabolism in the liver; it has been
    estimated that about 500 mg of cholesterolis
    converted daily into bile acids in the adult
    humanliver. Bile acids are secreted into the intestine
    and have an important role in facilitating the
    absorption of fats from food31.
    Bile acid sequestrants include
    cholestyramine, colestipol, colestimide,and
    colesevelam. Cholestyramine and colestipol are the
    two bile acid sequestrants currently available.
    Cholestyramineis a quaternary amine composed
    of styrene and divinylbenzenepolymers.
    Colestipolis a copolymer of diethylenetriamine and
    1-chloro-2,3-epoxypropane32.
    Mechanism of action
    Bile acid sequestrants are positively
    charged resins that bind to the negatively charged
    bile acids in the intestine to form a large insoluble
    complex that not absorbed and so excreted in the
    feces. Excretion is increased up to tenfold when
    resins are given, resulting in greater conversion of
    cholesterol to bile acids. Furthermore bile acid
    sequestrants increase HDL levels33. Side effects
    Bile acid sequestrants are rarely used as
    initial therapy because of poor patient tolerance.
    Gastrointestinal disturbances are the most common
    complaints of the bile acid sequestrants include
    constipation, nausea, indigestion,bloating and
    flatulence34.
    On long-term therapybile acid
    sequestering agents may cause osteoporosis due
    to calcium loss. They may aggravate
    hypertriglyceridemia by an unknown mechanism.
    Some vitamins minerals deficiencymay occur32.
    Fibric acid derivatives(Fibrates)
    Fibrates include clofibrate, gemfibrozil,
    fenofibrate, and bezafibrate, areawidely used class
    of antihyperlipidemic agents, results in a significant
    reduction in plasmatriglycerides and a modest
    reduction in LDL cholesterol. HDL cholesterol level
    increases moderately. Angiographictrials results
    showed that fibrates play an important role in
    slowing the progression of coronaryatherosclerosis
    and decrease the incidence of coronary artery
    disease.
    Mechanism of action
    Data from studies in rodents and in
    humans imply fourmain mechanisms of fibrates:
    Stimulation of lipoprotein lipolysis.
    Fibrates function primarily as ligands for the nuclear transcription receptor, PPAR-. They
    increased the expression of lipoprotein lipase, apo,
    and down-regulate apo C-III, an inhibitor of lipolysis.
    Fibrates also increase the level of HDL cholesterol
    by increasing the expression of apo AI andapo AII35.
    Increase hepatic fatty acid (FA) uptake and
    reduction of hepatic triglyceride production.
    Fibrates enhance the production of fatty
    acid transport protein and acyl-CoA synthetase,
    which contribute to the increase uptake of fatty acid
    by the liver and as a result in a lower availability of
    fatty acids for triglyceride production36.
    Increase removal of LDL particles.
    Fibrate, appears to enhance LDL
    catabolism via the receptor-mediated pathway; LDL
    particles became larger and more lipid rich and
    therefore had more affinity for receptors. Fibrates
    also inhibits the formation of slowly metabolized,
    potentially atherogenic LDL particles37.
    Increase in HDL production and stimulation of
    reverse cholesterol transport.
    Fibrates increase apo A-I production in the
    liver which leads to the observed elevation in
    plasma levels of apo A4 and HDL-cholesteroland
    a more effective reverse cholesterol transport38.

    A. bilimbi adalah tanaman obat penting yang digunakan dalam pengobatan tradisional untuk
    pengobatan berbagai penyakit dan dalam menjaga kesehatan dan kesejahteraan yang baik.
    Penelitian farmakologi ekstensif yang dilakukan selama bertahun-tahun telah membuktikan
    pangkalan ilmiah untuk penggunaan terapeutik daun dan buah A. bilimbi dalam pengobatan
    beberapa penyakit termasuk diabetes mellitus, hipertensi dan infeksi mikroba. Berbeda dengan
    beberapa penelitian farmakologis, beberapa studi fitokimia awal telah dilaporkan pada tanaman
    ini dan senyawa yang diidentifikasi sejauh ini terutama adalah minyak volatil, asam lemak dan
    hidrokarbon rantai panjang dengan nilai obat yang lemah. Meskipun manfaat penggunaan A.
    bilimbi dalam pengobatan gratis dan kegiatan farmakologi terbukti secara ilmiah, ada
    kekurangan informasi tentang senyawa bioaktif yang ada di tanaman ini. Mengingat profil
    farmakologi yang menarik, ada kebutuhan mendesak untuk mengidentifikasi dan mengisolasi
    konstituen bioaktif dari tanaman ini yang bertanggung jawab untuk berbagai kegiatan biologis.
    Isolasi dan karakterisasi senyawa bioaktif dari bagian yang berbeda dari A. bilimbi akan
    memberikan wawasan ke dalam tindakan mekanisme biokimia tanaman ini. Pengetahuan
    tentang konstituen bioaktif akan memberikan dasar untuk mengembangkan obat baru dari
    tanaman baik sebagai senyawa murni atau ekstrak standar menggunakan teknologi canggih dan
    canggih. Senyawa murni yang menunjukkan efek farmakologi yang berbeda juga dapat berfungsi
    sebagai petunjuk untuk pengembangan obat di masa depan.
    Katekin.
    Hal ini sesuai dengan yang dikemukakan Gunawijaya (1996) cit Ekawati (2007) bahwa katekin adalah
    antioksidan kuat dengan kemampuan untuk membersihkan radikal bebas yang bersumber dari oksigen
    termasuk OH reaktif. Katekin sebagai antioksidan memiliki banyak fungsi. Menurut Diaz et al. (1997),
    antioksidan berperan melindungi LDL terhadap oksidasi. Selain itu, menurut Langseth (1995),
    antioksidan melindungi sel dari Reactive Oxygen Species (ROS) atau spesies radikal lainnya melalui
    mekanisme scavenger radikal-oksigen seperti enzim katalase, superoksida dismutase dan glutation
    peroksidase. Suyatna dan Handoko (1995) mengemukakan, katekin dapat menurunkan kadar kolesterol,
    LDL dan trigliserida. Mekanisme penurunan tersebut adalah dengan cara meningkatkan aktivitas
    lipoprotein lipase, sehingga katabolisme lipoprotein kaya trigliserida seperti VLDL (Very Low Density
    Lipoprotein) dan IDL (Intermediet Density Lipoprotein) meningkat. Kadar kolesterol HDL (High Density
    Lipoprotein) meningkat secara tidak langsung akibat menurunnya kadar trigliserida VLDL. Efek
    penurunan kolesterol LDL diduga berhubungan dengan meningkatnya bersihan VLDL dan IDL
    dalam hati sehingga produksi LDL menurun. Sitompul (2003) menambahkan, antioksidan melalui
    mekanismenya dapat menghambat dan mencegah kerusakan LDL karena oksidasi, yang akhirnya dapat
    menurunkan kadar kolesterol dalam darah
    1

    Pengaruh pemberian sari belimbing wuluh


    (Averrhoa bilimbi L.) terhadap kadar kolesterol
    total wanita dewasa
    Alkhamees OA. 2013. Protective effects of vitamin-P and vitamin-C on hypercholesterolemia -
    induced oxidative hepatic damage and lipid profile changes in female rats: A comparative
    study. J Appl Pharm Sci. 3(4) : 99–105.
    Prakoso Z. 2006. Pengaruh pemberian vitamin C terhadap kadar LDL dan HDL kolesterol serum
    tikus wistar jantan hiperlipidemia setelah perlakuan jus lidah buaya [Artikel Penelitian].
    Semarang (ID) : Universitas Diponegoro.
    Moses T, Papadopoulou KK, Osbourn A. 2014. Metabolic and functional diversity of saponins,
    biosynthetic intermediates and semi-synthetic derivatives. Critical reviews in
    biochemistry and molecular biology, 49(6) : 439-462.
    Percival SS, Turner RE. 2001. Applications of herbs to functional foods. Di dalam Wildman
    REC (Ed.). Handbook of Nutraceuticals and Functional Foods. Washington DC (US) :
    CRC Press. p. 393−406.
    Sheehy T, Morrissey A. 1998. Functional foods: Prospects and perspectives. Di dalam Henry
    CJK, Heppell NJ (Ed). Nutritional Aspects of Food and Processing and Ingredients.
    Maryland (US) : Chapman & Hall. Aspen Publishers Inc. p. 45−65.
    Radhika S, Smila KH, Muthezhilan R. 2011. Antidiabetic and hypolipidemic activity of Punica
    granatum Linn on alloxan induced rats. World J.med. Scie. 6(4): 178-182.
    Ranti GC, Fatimawali, Wehantouw F. 2013. Uji efektivitas ekstrak flavonoid dan steroid dari
    gedi (Abelmoschus manihot) sebagai anti obesitan dan hipolipidemik pada tikus putih
    jantan galur wistar. Jurnal Ilmiah Farmasi UNSRAT. 2 (2).
    Sukandar EY, Andrajati R, Sigit JI, Kusnandar. 2008. ISO Farmakoterapi. Jakarta (ID) : ISFI
    (Ikatan Sarjana Farmasi Indonesia). p. 111-117.
    Mahley RW, Bersot TP. 2012. Terapi obat untuk hiperkolesterolemia dan dislipidemia.
    Di dalam Hardman JG, Limbird LE (Ed). Goodman & Gilman Dasar Farmakologi Terapi
    Ed 10 Vol. 2. Jakarta (ID) : EGC
    Furi PR, Wahyuni AS. 2011. Pengaruh ekstrak etanol jamur lingzhi (Ganoderma lucidum)
    terhadap HDL (high density lipoprotein) level in dislipidemic rats. Pharmacon. (12)1.

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