Pramlintide
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| Image:Pramlintide sequence.svg | |
| Pramlintide
| |
| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C171H269N51O53S2 |
| Mol. mass | 3951.41 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 30 to 40% |
| Protein binding | Approximately 60% |
| Metabolism | Renal |
| Half life | Approximately 48 minutes |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
C(US) |
| Legal status | |
| Routes | Subcutaneous |
Pramlintide acetate (Symlin) is a relatively new adjunct treatment for diabetes (both type 1 and 2), developed by Amylin Pharmaceuticals.
Contents |
Pharmacology
It is derived from amylin, a hormone that is released into the bloodstream, in a similar pattern as insulin, after a meal.[1] Like insulin, amylin is deficient in individuals with diabetes.
By substituting for amylin, pramlintide aids in the absorption of glucose by slowing gastric emptying, promoting satiety, and inhibiting inappropriate secretion of glucagon, a catabolic hormone that opposes the effects of insulin and amylin.
Approval
Symlin has been approved for use by the FDA by type 1 and type 2 diabetics who use insulin.[1] Symlin results in weight loss, allows patients to use less insulin, lowers average blood sugar levels, and substantially reduces what otherwise would be a large unhealthy rise in blood sugar that occurs in diabetics right after eating. Symlin is the only drug approved by the FDA to lower blood sugar in type 1 diabetics since insulin's discovery in the early 1920s.
Design and structure
Since native human amylin is highly amyloidogenic and potentially toxic, the strategy for designing pramlintide was to substitute residues from rat amylin, which is not amyloidogenic (but would presumably retain clinical activity). Proline residues are known to be structure-breaking residues, so these were directly grafted into the human sequence. The glutamine residue was also substituted with an asparagine, probably because glutamines are generally considered to be amyloid-promoting.
Amino acid sequences:
Pramlintide: KCNTATCATNRLANFLVHSSNNFGPILPPTNVGSNTY-(NH2)
Amylin: KCNTATCATQRLANFLVHSSNNFGAILSSTNVGSNTY-(NH2)
Rat amylin: KCNTATCATQRLANFLVRSSNNFGPVLPPTNVGSNTY-(NH2)
Pramlintide (positively charged) is delivered as an acetate salt.
References
External links
- www.symlin.com - product website
- www.amylin.com - Symlin page on the Amylin Pharmaceuticals website
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
