Sevelamer
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| General | |||||||||
| Surname | Sevelamer | ||||||||
| other names |
IUPAC : Poly (allylamine- co - N , N ′ -diallyl- 1,3-diamino-2-hydroxypropane) |
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| CAS number | 52757-95-6 | ||||||||
| PubChem | 3085017 | ||||||||
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| DrugBank | DB00658 | ||||||||
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| Mechanism of action |
Binding of phosphate, excretion of the non-absorbable complex |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||
Sevelamer ( rINN ) ( IPA : [sɛˈvɛləmə, -mər, -mir] ) is a drug from the group of phosphate binders that is used in dialysis patients with excess phosphate in the blood ( hyperphosphatemia ) to bind phosphate from food.
Sevelamer is available in two salt forms:
- Sevelamer hydrochloride (Renagel ® )
- Sevelamer carbonate (e.g. Renvela ® )
In addition to the original product Renvela ® , several generic drugs are available for sevelamer carbonate .
pharmacology
Pharmacodynamics
Sevelamer is a metal-free phosphate binder. The cross-linked polymer contains numerous amino groups that are each separated from the polymer backbone by a carbon atom and are protonated in the stomach. These, now positively charged, protonated amines bind negatively charged ions such as. B. phosphate in the intestine from food. Sevelamer prevents its absorption by binding phosphate in the gastrointestinal tract and reduces the serum phosphate level.
Pharmacokinetics
Due to its macromolecular structure, sevelamer is not absorbed from the gastrointestinal tract. This was confirmed by an absorption study in healthy volunteers .
Dosage form
In Germany, film-coated tablets and powder for the preparation of an oral suspension are commercially available.
application areas
Sevelamer is indicated for the treatment of hyperphosphatemia in adult patients on hemodialysis or peritoneal dialysis .
Sevelamer is also indicated for the treatment of hyperphosphatemia in non-hemodialytic adult patients with chronic renal insufficiency and serum phosphate levels ≥ 1.78 mmol / L.
Sevelamer should be used as part of a combined therapy that includes calcium supplements and vitamin D compounds to control renal bone diseases.
Contraindications
Sevelamer must not be used in case of hypersensitivity to the active substance, hypophosphataemia or intestinal obstruction .
Side effects
The safety of sevelamer (both as carbonate and hydrochloride) has been investigated in numerous clinical studies involving a total of 969 hemodialysis patients (724 with sevelamer hydrochloride and 245 with sevelamer carbonate) and treatment durations of between 4 and 50 weeks. Including 97 peritoneal dialysis patients (sevelamer hydrochloride) with a treatment duration of 12 weeks and 128 patients with chronic renal insufficiency (79 with sevelamer hydrochloride and 49 with sevelamer carbonate) with a treatment duration between 8 and 12 weeks who were not treated with hemodialysis.
The most common side effects affect the gastrointestinal tract and are mild to moderate in severity:
- Very common (≥1 / 10): nausea, vomiting, upper abdominal pain, constipation
- Common (≥1 / 100, <1/10): diarrhea , dyspepsia , flatulence, abdominal pain
Media sclerosis
A special form of hardening of the arteries is medial sclerosis , in which the middle wall layer of the arteries calcifies due to the deposition of calcium compounds. The development of this disease is promoted, among other things, by renal insufficiency. If patients with renal insufficiency are treated with calcium-based phosphate binders, this can further promote the development and progression of media sclerosis. Sevelamer as a metal-free phosphate binder offers a lower-risk alternative and slows down the progression of coronary and aortic calcification.
Hydrochloride or carbonate
Sevelamer hydrochloride (Renagel®) is the predecessor preparation to Sevelamer carbonate (Renvela®). The only chemical difference between the two active ingredients is their salt form. In contrast to the hydrochloride, the carbonate also acts as a carbonate buffer, through which the acid-base balance of the body can be kept within the target range more easily. This also ensures better gastrointestinal tolerance.
Trade names
- Sevelamer hydrochloride: Renagel®
- Sevelamer carbonate: Renvela®, Sevemed, numerous generics
Web links
- Renvela (English)
- Public Assessment Report (EPAR) of the European Medicines Agency (EMA) for: Sevelamer
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ Manufacturer website Renagel.com (English)
- ↑ a b Red List Online, as of March 2010.
- ↑ a b AGES-PharmMed, as of March 2010.
- ↑ AM comp. d. Switzerland, as of March 2010.
- ↑ Manufacturer website Renvela.com (English)
- ↑ a b search for sevelamer | Yellow list. In: www.gelbe-liste.de. Retrieved June 2, 2016 .
- ↑ a b c d e Technical information Renvela 800 mg film-coated tablets ( Memento from April 29, 2014 in the Internet Archive ) (PDF; 67 kB), as of December 2011.
- ↑ a b c d e Technical information Renvela 2.4 g powder ( Memento from April 29, 2014 in the Internet Archive ) (PDF; 68 kB), as of December 2011.
- ↑ GM Chertow, SK Burke, P. Raggi et al: Sevelamer Attenuates the Progression of Coronary and Aortic Calcification in Hemodialysis Patients. In: Kidney Int . 2002; 62, pp. 245-252.
