Sevelamer

Sevelamer
Clinical data
Trade names Renagel, Renvela
AHFS/Drugs.com Monograph
MedlinePlus a601248
Pregnancy
category
Routes of
administration
oral
ATC code V03AE02 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability nil
Metabolism nil
Biological half-life n/a
Excretion faecal 100%
Identifiers
CAS Number 52757-95-6 YesY
PubChem (CID) 3085017
DrugBank DB00658 N
ChemSpider 2341997 N
UNII 941N5DUU5C N
KEGG D08512 YesY
ChEMBL CHEMBL1201492 N
ECHA InfoCard 100.207.865
Chemical and physical data
Formula [(C3H7N)a+b.(C9H17N2O)c]m
where a+b:c = 9:1
Molar mass variable
 NYesY (what is this?)  (verify)

Sevelamer (rINN) (/sɛˈvɛləmər/ or /sɛˈvɛləmɪər/) 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. Sevelamer was invented and developed by GelTex Pharmaceuticals. Sevelamer is currently marketed by Sanofi under the trade names Renagel (sevelamer hydrochloride) and Renvela (sevelamer carbonate).

Chemistry and pharmacology

Sevelamer consists of polyallylamine that is crosslinked with epichlorohydrin.[1] 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.

Clinical use

Indications

Sevelamer is indicated for the management of hyperphosphataemia in adult patients with stage 4 and 5 chronic kidney disease on hemodialysis.

Contraindications

Sevelamer therapy is contraindicated in hypophosphataemia or bowel obstruction.

Adverse effects

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

Sevelamer can significantly reduce serum uric acid.[2] This reduction has no known detrimental effect and several beneficial effects, including reducing hyperuricemia, uric acid nephrolithiasis, and gout.

References

  1. (1) Rosenbaum, D. P.; Mandeville, W. H.; Pitruzzello, M.; Goldberg, D. I. Nephrology Dialysis Transplantation Effect of RenaGel A , a Non-Absorbable , Cross-Linked , Polymeric Phosphate Binder , on Urinary Phosphorus Excretion in Rats. 1997, 961–964.
  2. 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.
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