Article: Sevelamer

Sevelamer
Systematic (IUPAC) name
poly(allylamine- co-N,N'-diallyl-1,3-diamino-2-hydroxypropane)
Identifiers
CAS number	52757-95-6
ATC code	V03AE02
PubChem	3085017
DrugBank	APRD01226
Chemical data
Formula	[(C3H7N)a+b.(C9H17N2O)c]m where a+b:c = 9:1
Mol. weight	variable
Pharmacokinetic data
Bioavailability	nil
Metabolism	nil
Half life	n/a
Excretion	faecal 100%
Therapeutic considerations
Pregnancy cat.	B3 (Australia)
Legal status	Schedule 4 (Australia)
Routes	oral

Sevelamer (rINN) (IPA: [sɛˈvɛləmir]) is a phosphate binding drug used to prevent hyperphosphataemia in patients with chronic renal failure. When taken with meals, sevelamer binds to dietary phosphate and prevents its absorption. It is marketed by Genzyme under the trade name Renagel.

Chemistry and pharmacology

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

Indications

Sevelamer is indicated for the management of hyperphosphataemia in adult patients with stage 4 and 5 chronic renal failure (end stage renal disease).

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, diarrhoea, flatulence, and/or constipation.