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Wikipedia

Sevelamer

April 11, 2024

Sevelamer (rINN) is a phosphate binding medication used to treat hyperphosphatemia in patients with chronic kidney disease. When taken with meals, it binds to dietary phosphate and prevents its absorption. Sevelamer was invented and developed by GelTex Pharmaceuticals. Sevelamer is marketed by Sanofi under the brand names Renagel (sevelamer hydrochloride) and Renvela (sevelamer carbonate).

Sevelamer
Clinical data
Pronunciation(/sɛˈvɛləmər/ or /sɛˈvɛləmɪər/)
Trade namesRenagel, Renvela
AHFS/Drugs.comMonograph
MedlinePlusa601248
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability0%
ExcretionFeces 100%
Identifiers
  • poly(allylamine-
    co-N,N'-diallyl-1,3-diamino-2-hydroxypropane)
CAS Number
  • 52757-95-6 Y
PubChem CID
  • 3085017
DrugBank
  • DB00658 N
ChemSpider
  • 2341997 N
UNII
  • 941N5DUU5C
KEGG
  • D08512 Y
  • as HCl: D01983
ChEMBL
  • ChEMBL1201492 N
CompTox Dashboard (EPA)
  • DTXSID80872282
Chemical and physical data
Formula[(C3H7N)a+b.(C9H17N2O)c]m
where a+b:c = 9:1
Molar massvariable
 NY (what is this?)  (verify)

Chemistry and pharmacology edit

Sevelamer consists of polyallylamine that is crosslinked with epichlorohydrin.[2] 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 phosphate ions through ionic and hydrogen bonding.[citation needed]

Medical uses edit

Sevelamer is used in the management of hyperphosphatemia in adult patients with stage 4 and 5 chronic kidney disease (CKD) on hemodialysis. Its efficacy at lowering phosphate levels is similar to that of calcium acetate, but without the accompanying risk of hypercalcemia and arterial calcification.[3][4] In patients with CKD, it has also been shown to reduce LDL and cholesterol.[5]

Contraindications edit

Sevelamer therapy is contraindicated in hypophosphatemia or bowel obstruction.[6] In hypophosphatemia, sevelamer could exacerbate the condition by further lowering phosphate levels in the blood, which could be fatal.[7]

Adverse effects edit

Common adverse drug reactions (ADRs) associated with the use of sevelamer include: nausea and vomiting, constipation, diarrhea, stomach pain, heartburn, gas.[8]

Other effects edit

Sevelamer can significantly reduce serum uric acid.[9] This reduction has no known detrimental effect and may be helpful in patients with gout.

Sevelamer is able to sequester advanced glycation end products (AGEs) in the gut, preventing their absorption into the blood. AGEs contribute to oxidative stress, which can damage cells (like beta cells, which produce insulin in the pancreas). As Vlassara and Uribarri explain in a 2014 review on AGEs, this may explain why sevelamer, but not calcium carbonate (a phosphate binder that does not sequester AGEs), has been shown to lower AGEs in the blood, as well as oxidative stress and inflammatory markers.[10]

References edit

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2015". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  2. ^ Ramsdell R (June 1999). "Renagel: a new and different phosphate binder". review. ANNA Journal. 26 (3): 346–7. PMID 10633608.
  3. ^ Burke SK (September 2000). "Renagel: reducing serum phosphorus in haemodialysis patients". review. Hospital Medicine. 61 (9): 622–7. doi:10.12968/hosp.2000.61.9.1419. PMID 11048603.
  4. ^ Habbous S, Przech S, Acedillo R, Sarma S, Garg AX, Martin J (January 2017). "The efficacy and safety of sevelamer and lanthanum versus calcium-containing and iron-based binders in treating hyperphosphatemia in patients with chronic kidney disease: a systematic review and meta-analysis". review. Nephrology, Dialysis, Transplantation. 32 (1): 111–125. doi:10.1093/ndt/gfw312. PMID 27651467.
  5. ^ Patel L, Bernard LM, Elder GJ (February 2016). "Sevelamer Versus Calcium-Based Binders for Treatment of Hyperphosphatemia in CKD: A Meta-Analysis of Randomized Controlled Trials". review. Clinical Journal of the American Society of Nephrology. 11 (2): 232–44. doi:10.2215/CJN.06800615. PMC 4741042. PMID 26668024.
  6. ^ Yuste, Claudia (2017). "Gastrointestinal complications induced by sevelamer crystals". Clinical Kidney Journal. 10 (4): 539–544. doi:10.1093/ckj/sfx013. PMC 5570024. PMID 28852493.
  7. ^ Emmett M (September 2004). "A comparison of clinically useful phosphorus binders for patients with chronic kidney failure". review. Kidney International Supplements. 66 (90): S25–32. doi:10.1111/j.1523-1755.2004.09005.x. PMID 15296504.
  8. ^ "Sevelamer". MedlinePlus.
  9. ^ Locatelli F, Del Vecchio L (May 2015). "Cardiovascular mortality in chronic kidney disease patients: potential mechanisms and possibilities of inhibition by resin-based phosphate binders". review. Expert Review of Cardiovascular Therapy. 13 (5): 489–99. doi:10.1586/14779072.2015.1029456. PMID 25804298. S2CID 32586527.
  10. ^ Vlassara H, Uribarri J (January 2014). "Advanced glycation end products (AGE) and diabetes: cause, effect, or both?". review. Current Diabetes Reports. 14 (1): 453. doi:10.1007/s11892-013-0453-1. PMC 3903318. PMID 24292971.

External links edit

  • "Sevelamer". Drug Information Portal. U.S. National Library of Medicine.
  • "Sevelamer hydrochloride". Drug Information Portal. U.S. National Library of Medicine.
  • "Sevelamer carbonate". Drug Information Portal. U.S. National Library of Medicine.

April 11, 2024
sevelamer, rinn, phosphate, binding, medication, used, treat, hyperphosphatemia, patients, with, chronic, kidney, disease, when, taken, with, meals, binds, dietary, phosphate, prevents, absorption, invented, developed, geltex, pharmaceuticals, marketed, sanofi. Sevelamer rINN is a phosphate binding medication used to treat hyperphosphatemia in patients with chronic kidney disease When taken with meals it binds to dietary phosphate and prevents its absorption Sevelamer was invented and developed by GelTex Pharmaceuticals Sevelamer is marketed by Sanofi under the brand names Renagel sevelamer hydrochloride and Renvela sevelamer carbonate SevelamerClinical dataPronunciation s ɛ ˈ v ɛ l em er or s ɛ ˈ v ɛ l em ɪer Trade namesRenagel RenvelaAHFS Drugs comMonographMedlinePlusa601248License dataEU EMA by INN US DailyMed SevelamerPregnancycategoryAU B3Routes ofadministrationBy mouthATC codeV03AE02 WHO Legal statusLegal statusAU S4 Prescription only 1 US only EU Rx onlyPharmacokinetic dataBioavailability0 ExcretionFeces 100 IdentifiersIUPAC name poly allylamine co N N diallyl 1 3 diamino 2 hydroxypropane CAS Number52757 95 6 YPubChem CID3085017DrugBankDB00658 NChemSpider2341997 NUNII941N5DUU5CKEGGD08512 Yas HCl D01983ChEMBLChEMBL1201492 NCompTox Dashboard EPA DTXSID80872282Chemical and physical dataFormula C3H7N a b C9H17N2O c mwhere a b c 9 1Molar massvariable N Y what is this verify Contents 1 Chemistry and pharmacology 2 Medical uses 3 Contraindications 4 Adverse effects 5 Other effects 6 References 7 External linksChemistry and pharmacology editSevelamer consists of polyallylamine that is crosslinked with epichlorohydrin 2 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 phosphate ions through ionic and hydrogen bonding citation needed Medical uses editSevelamer is used in the management of hyperphosphatemia in adult patients with stage 4 and 5 chronic kidney disease CKD on hemodialysis Its efficacy at lowering phosphate levels is similar to that of calcium acetate but without the accompanying risk of hypercalcemia and arterial calcification 3 4 In patients with CKD it has also been shown to reduce LDL and cholesterol 5 Contraindications editSevelamer therapy is contraindicated in hypophosphatemia or bowel obstruction 6 In hypophosphatemia sevelamer could exacerbate the condition by further lowering phosphate levels in the blood which could be fatal 7 Adverse effects editCommon adverse drug reactions ADRs associated with the use of sevelamer include nausea and vomiting constipation diarrhea stomach pain heartburn gas 8 Other effects editSevelamer can significantly reduce serum uric acid 9 This reduction has no known detrimental effect and may be helpful in patients with gout Sevelamer is able to sequester advanced glycation end products AGEs in the gut preventing their absorption into the blood AGEs contribute to oxidative stress which can damage cells like beta cells which produce insulin in the pancreas As Vlassara and Uribarri explain in a 2014 review on AGEs this may explain why sevelamer but not calcium carbonate a phosphate binder that does not sequester AGEs has been shown to lower AGEs in the blood as well as oxidative stress and inflammatory markers 10 References edit Prescription medicines registration of new chemical entities in Australia 2015 Therapeutic Goods Administration TGA 21 June 2022 Retrieved 10 April 2023 Ramsdell R June 1999 Renagel a new and different phosphate binder review ANNA Journal 26 3 346 7 PMID 10633608 Burke SK September 2000 Renagel reducing serum phosphorus in haemodialysis patients review Hospital Medicine 61 9 622 7 doi 10 12968 hosp 2000 61 9 1419 PMID 11048603 Habbous S Przech S Acedillo R Sarma S Garg AX Martin J January 2017 The efficacy and safety of sevelamer and lanthanum versus calcium containing and iron based binders in treating hyperphosphatemia in patients with chronic kidney disease a systematic review and meta analysis review Nephrology Dialysis Transplantation 32 1 111 125 doi 10 1093 ndt gfw312 PMID 27651467 Patel L Bernard LM Elder GJ February 2016 Sevelamer Versus Calcium Based Binders for Treatment of Hyperphosphatemia in CKD A Meta Analysis of Randomized Controlled Trials review Clinical Journal of the American Society of Nephrology 11 2 232 44 doi 10 2215 CJN 06800615 PMC 4741042 PMID 26668024 Yuste Claudia 2017 Gastrointestinal complications induced by sevelamer crystals Clinical Kidney Journal 10 4 539 544 doi 10 1093 ckj sfx013 PMC 5570024 PMID 28852493 Emmett M September 2004 A comparison of clinically useful phosphorus binders for patients with chronic kidney failure review Kidney International Supplements 66 90 S25 32 doi 10 1111 j 1523 1755 2004 09005 x PMID 15296504 Sevelamer MedlinePlus Locatelli F Del Vecchio L May 2015 Cardiovascular mortality in chronic kidney disease patients potential mechanisms and possibilities of inhibition by resin based phosphate binders review Expert Review of Cardiovascular Therapy 13 5 489 99 doi 10 1586 14779072 2015 1029456 PMID 25804298 S2CID 32586527 Vlassara H Uribarri J January 2014 Advanced glycation end products AGE and diabetes cause effect or both review Current Diabetes Reports 14 1 453 doi 10 1007 s11892 013 0453 1 PMC 3903318 PMID 24292971 External links edit Sevelamer Drug Information Portal U S National Library of Medicine Sevelamer hydrochloride Drug Information Portal U S National Library of Medicine Sevelamer carbonate Drug Information Portal U S National Library of Medicine Portal nbsp Medicine Retrieved from https en wikipedia org w index php title Sevelamer amp oldid 1177388085, wikipedia, wiki, book, books, library,

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