Colestilan

Colestilan

Colestilan
Systematic (IUPAC) name
2-(chloromethyl)oxirane 2-methyl-1H-imidazole copolymer
Clinical data
Trade names BindRen
AHFS/Drugs.com
Pregnancy
category
  • B
Legal status
  • (Prescription only)
Routes of
administration
Oral
Pharmacokinetic data
Bioavailability Not absorbed
Protein binding NA
Metabolism Not absorbed
Excretion Gut
Identifiers
CAS Registry Number  YesY
ATC code V03
PubChem CID:
KEGG  YesY
ChEMBL  N
Chemical data
Formula (C4H5ClN2)m(C3H6O)n
 N   

Colestilan (INN, trade name BindRen) is a medication that acts as a phosphate binder[1] and bile acid sequestrant.[2]

Clinical use

Colestilan is used for the treatment of hyperphosphataemia (too high phosphate concentrations in the blood serum) in patients undergoing dialysis, including peritoneal dialysis.[1][3]

Contraindications

Colestilan is contraindicated in patients with bowel obstruction.[3]

Interactions

The substance can inhibit the resorption of other drugs, as well as fat soluble vitamins (A, D, E, K) and folate, from the gut.[1] Resulting lower blood levels can be clinically problematic with immunosuppressant and antiepileptic drugs.[3]

Adverse effects

Adverse effects include gastrointestinal problems such as constipation, as well as vitamin and calcium deficiency. Vitamin K deficiency sometimes causes gastrointestinal bleeding.[1][3]

Chemistry and mechanism of action

Colestilan is a cross-linked copolymer of 2-methylimidazole and epichlorohydrin and works as an anion exchanger resin with affinity to phosphate, bile acid anions and urate. It binds these anions in the gut and removes them from the enterohepatic circulation. Colestilan is not absorbed from the gut, but is excreted together with the bound anions.[1]

2-methyl-1H-imidazole (left) and epichlorohydrin (right)

References

  1. ^ a b c d e
  2. ^
  3. ^ a b c d