セベラマー
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/08/11 12:25:43」(JST)
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Sevelamer
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Systematic (IUPAC) name |
poly(allylamine-
co-N,N'-diallyl-1,3-diamino-2-hydroxypropane) |
Clinical data |
Trade names |
Renagel |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a601248 |
Pregnancy cat. |
B3 (Australia), C (US) |
Legal status |
Schedule 4 (Australia), Rx only (US) |
Routes |
oral |
Pharmacokinetic data |
Bioavailability |
nil |
Metabolism |
nil |
Half-life |
n/a |
Excretion |
faecal 100% |
Identifiers |
CAS number |
52757-95-6 Y |
ATC code |
V03AE02 |
PubChem |
CID 3085017 |
DrugBank |
DB00658 |
ChemSpider |
2341997 N |
UNII |
941N5DUU5C N |
KEGG |
D08512 Y |
ChEMBL |
CHEMBL1201492 N |
Chemical data |
Formula |
[(C3H7N)a+b.(C9H17N2O)c]m
where a+b:c = 9:1 |
Mol. mass |
variable |
N (what is this?) (verify)
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Sevelamer (rINN) (// or //) is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease. When taken with meals, it binds to dietary phosphate and prevents its absorption. It is marketed by Genzyme (now Sanofi-Aventis) under the trade names Renagel (sevelamer hydrochloride) and Renvela (sevelamer carbonate).
Contents
- 1 Chemistry and pharmacology
- 2 Clinical use
- 2.1 Indications
- 2.2 Contraindications
- 2.3 Adverse effects
- 2.4 Other effects
- 3 External links
- 4 References
Chemistry and pharmacology[edit source | edit]
Sevelamer is a copolymer of 2-(chloromethyl)oxirane (epichlorohydrin) and prop-2-en-1-amine. The marketed form sevelamer hydrochloride is a partial hydrochloride salt being present as approximately 40% amine hydrochloride and 60% sevelamer base. The amine groups of sevelamer become partially protonated in the intestine and interact with phosphorus molecules through ionic and hydrogen bonding.
Clinical use[edit source | edit]
Indications[edit source | edit]
Sevelamer is indicated for the management of hyperphosphataemia in adult patients with stage 4 and 5 chronic kidney disease on hemodialysis.
Contraindications[edit source | edit]
Sevelamer therapy is contraindicated in hypophosphataemia or bowel obstruction.
Adverse effects[edit source | edit]
Common adverse drug reactions (ADRs) associated with the use of sevelamer include: hypotension, hypertension, nausea and vomiting, dyspepsia, diarrhea, flatulence, and/or constipation.
Other effects[edit source | edit]
Sevelamer can significantly reduce serum uric acid.[1] This reduction has no known detrimental effect and several beneficial effects, including reducing hyperuricemia, uric acid nephrolithiasis, and gout.
External links[edit source | edit]
- Sevelamer - medlineplus.org
- Renagel - genzyme.com
- Renvela - genzyme.com
References[edit source | edit]
- ^ Garg JP, Chasan-Taber S, Blair A, et al. (January 2005). "Effects of sevelamer and calcium-based phosphate binders on uric acid concentrations in patients undergoing hemodialysis: a randomized clinical trial". Arthritis and rheumatism 52 (1): 290–5. doi:10.1002/art.20781. PMID 15641045.
Drugs for treatment of hyperkalemia and hyperphosphatemia (V03AE)
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Potassium binders |
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Phosphate binders |
- Aluminium hydroxide
- Calcium acetate
- Calcium acetate/magnesium carbonate
- Calcium carbonate
- Lanthanum carbonate
- Sevelamer
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mt, k, c/g/r/p/y/i, f/h/s/l/o/e, a/u, n, m
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k, cgrp/y/i, f/h/s/l/o/e, au, n, m, epon
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m (A16/C10), i (k, c/g/r/p/y/i, f/h/s/o/e, a/u, n, m)
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UpToDate Contents
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English Journal
- Optimal phosphate control: still an unmet need in chronic kidney disease patients.
- Locatelli F, Del Vecchio L.Author information Alessandro Manzoni Hospital, Department of Nephrology, Dialysis and Renal Transplant , Via dell'Eremo 9/11 23900 Lecco , Italy f.locatelli@ospedale.lecco.it.AbstractReduction of phosphate levels has traditionally been considered a mainstay treatment for patients with chronic kidney disease (CKD). Unfortunately, the treatment of hyperphosphatemia is far from being satisfactory. Available phosphate binders have limited efficacy, forcing the consumption of many tablets in order to achieve mild-to-moderate effect or low tolerability. Moreover, even if calcium-free phosphate binders, such as sevelamer and lanthanum carbonate, decrease serum phosphate levels without affecting serum calcium concentration, they do not significantly reduce circulating parathyroid hormone (PTH). The higher phosphate-binding efficacy of lanthanum carbonate should be balanced with the accumulation in bones and the lack of pleiotropic effects on lipid metabolism and inflammation. However, the fact that lanthanum carbonate seems to decrease the rate of development of vascular calcifications more or less similar to sevelamer suggests that phosphate control could actually be the key factor to improve patient outcome. New iron-based phosphate binders are undergoing clinical development. In addition to phosphate binding, they can be useful to treat anemia, and are undergoing Phase II clinical development for this indication. This could be of clinical importance particularly in CKD patients not on dialysis, avoiding the need for extra oral iron administration, and favoring compliance. In conclusion, the control of phosphate retention should still be considered an unmet medical need for CKD patients.
- Expert opinion on pharmacotherapy.Expert Opin Pharmacother.2014 Feb;15(3):307-9. doi: 10.1517/14656566.2014.860446. Epub 2013 Nov 27.
- Reduction of phosphate levels has traditionally been considered a mainstay treatment for patients with chronic kidney disease (CKD). Unfortunately, the treatment of hyperphosphatemia is far from being satisfactory. Available phosphate binders have limited efficacy, forcing the consumption of many ta
- PMID 24283572
- Phosphate management in chronic kidney disease.
- Bhan I.Author information Division of Nephrology, Department of Medicine, Massachusetts General Hospital, Boston, Massachusetts, USA.AbstractPURPOSE OF REVIEW: The review focuses on the rationale and evidence behind management strategies for hyperphosphatemia in patients with chronic kidney disease (CKD).
- Current opinion in nephrology and hypertension.Curr Opin Nephrol Hypertens.2014 Jan 16. [Epub ahead of print]
- PURPOSE OF REVIEW: The review focuses on the rationale and evidence behind management strategies for hyperphosphatemia in patients with chronic kidney disease (CKD).RECENT FINDINGS: Optimal management of phosphate in CKD remains an area of uncertainty, but multiple studies now point to a clinical be
- PMID 24445424
- Toward Individualized Cholesterol-Lowering Treatment in End-Stage Renal Disease.
- Silbernagel G1, Baumgartner I2, Wanner C3, März W4.Author information 1Department of Angiology, Swiss Cardiovascular Center, Inselspital, University of Bern, Bern, Switzerland; Division of Endocrinology, Diabetology, Nephrology, Vascular Disease, and Clinical Chemistry, Department of Internal Medicine, University of Tübingen, Tübingen, Germany. Electronic address: guenther.silbernagel@insel.ch.2Department of Angiology, Swiss Cardiovascular Center, Inselspital, University of Bern, Bern, Switzerland.3Division of Nephrology, Department of Medicine, University of Würzburg, Würzburg, Germany.4Medical Clinic V (Nephrology, Hypertensiology, Endocrinology, Diabetology, and Rheumatology), Mannheim Medical Faculty, University of Heidelberg, Mannheim, Germany; Synlab Academy, Synlab Services GmbH, Mannheim, Germany; Clinical Institute of Medical and Chemical Laboratory Diagnostics, Medical University of Graz, Graz, Austria.AbstractThere is broad evidence that lowering low-density lipoprotein (LDL) cholesterol will reduce cardiovascular risk. However, in patients on maintenance hemodialysis treatment, lowering LDL cholesterol is not as effective in preventing cardiovascular complications as in the general population. Cholesterol is either endogenously synthesized or absorbed from the intestine. It has been suggested that the benefit of using statins to prevent atherosclerotic complications is less pronounced in people with high absorption of cholesterol. Recent data indicate that patients on hemodialysis have high absorption of cholesterol. Therefore, these patients may benefit from dietary counseling to reduce cholesterol intake, from functional foods containing plant sterols and stanols, and from drugs that interfere with intestinal absorption of sterols (i.e., ezetimibe, bile acid resins, and sevelamer). This review discusses cholesterol homeostasis and the perspective of personalized treatment of hypercholesterolemia in hemodialysis.
- Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation.J Ren Nutr.2014 Jan 10. pii: S1051-2276(13)00208-2. doi: 10.1053/j.jrn.2013.11.001. [Epub ahead of print]
- There is broad evidence that lowering low-density lipoprotein (LDL) cholesterol will reduce cardiovascular risk. However, in patients on maintenance hemodialysis treatment, lowering LDL cholesterol is not as effective in preventing cardiovascular complications as in the general population. Cholester
- PMID 24418266
Japanese Journal
- 透析患者における血清終末糖化産物(AGEs)濃度 : セベラマー塩酸塩投与の効果
- 村本 弘昭,北田 欽也,武藤 寿生 [他],竹内 正義
- 日本透析医学会雑誌 = Journal of Japanese Society for Dialysis Therapy 44(10), 1015-1021, 2011-10-28
- 終末糖化産物(AGEs)は糖尿病や尿毒症において生成が促進され,血管合併症の発現に深く関与していると考えられている.今回われわれはリン吸着薬であるセベラマー塩酸塩によるAGEsの吸着除去効果につき検討した.3か月以上安定して週3回の血液透析を施行している患者9例を対象に,炭酸カルシウムから徐々にセベラマー塩酸塩に変更し,最終的に全例にセベラマー塩酸塩4.5g/日,1例に炭酸カルシウム1.5g/日を …
- NAID 10029861729
- 高カルシウム血症からサルコイドーシスの診断に至った維持透析患者の1例
- 越智 文美,若井 幸子,中山 一誠 [他],安井 由紀子,加賀 俊江,雫 淳一,阿部 恭知,遠藤 真理子,小倉 三津雄,新田 孝作
- 日本透析医学会雑誌 = Journal of Japanese Society for Dialysis Therapy 44(7), 649-654, 2011-07-28
- 維持透析療法において,透析患者の高Ca血症は骨ミネラル代謝異常の一部であり,高頻度に認められる.また,それにより血管石灰化,ひいては,心血管イベントをひき起こす.透析患者における高Ca血症の原因として,Ca製剤の過剰投与,活性化ビタミンDの過剰投与,高度の二次性副甲状腺機能亢進症などを第一に考え治療を行った.しかし,これらの治療に抵抗性の高Ca血症を呈し,精査を行い,サルコイドーシスの診断に至った …
- NAID 10029407330
- 透析施設におけるMBD管理を中心とした診療方針調査の集計結果報告 : 透析MBDアウトカム研究より
- 横山 啓太郎,福原 俊一,深川 雅史 [他],秋澤 忠男,黒川 清
- 日本透析医学会雑誌 = Journal of Japanese Society for Dialysis Therapy 44(6), 557-566, 2011-06-28
- 透析MBD(mineral and bone disorders)アウトカム研究は日本全国の大規模透析施設が参加した,二次性副甲状腺機能亢進症(SHPT)を合併する血液透析患者を対象とした多施設共同の前向き観察研究である(2008年1月~2011年1月).本研究では,施設の診療方針がSHPT患者のアウトカムに及ぼす影響を検討項目のひとつとしており,研究開始時および終了時に診療方針調査 …
- NAID 10029407163
Related Links
- Sevelamer (rINN) is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease. When taken with meals, it binds to dietary phosphate and prevents its absorption. It is marketed by Genzyme now ...
Related Pictures
★リンクテーブル★
[★]
- 英
- sevelamer
- 商
- レナジェル、フォスブロック、セベラマー塩酸塩
- 化
- 塩酸セベラマー sevelamer hydrochloride
- 関
- 高リン血症
[★]
セベラマー、塩酸セベラマー