| Primary information |
|---|
| ThPP ID | Th1100 |
| Therapeutic Peptide/Protein Name | Pramlintide |
| Sequence | KCNTATCATQRLANFLVHSSNNFGPILPPTNVGSNTY view full sequnce in fasta |
| Functional Classification | Ia |
| Molecular Weight | 3949.3896 |
| Chemical Formula | C171H267N51O53S2 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | Approximately 48 minutes |
| Description | New adjunct treatment for type I and type II diabetes. It is developed by Amylin Pharmaceuticals. It is derived from amylin, a hormone released after meal, in a pattern similar to insulin. Diabetic patients are also deficient in amylin. |
| Indication/Disease | For the treatment of type 1 and type 2 diabetes mellitus as an adjunct to preprandial insulin therapy in patients without adequate glycemic control of insulin therapy. |
| Pharmacodynamics | Pramlintide is a synthetic analog of amylin, a glucoregulatory hormone that is synthesized by pancreatic β-cells and released into the bloodstream, in a similar pattern as insulin, after a meal. Like insulin, amylin is deficient in individuals with diabetes. It is provided as an acetate salt. Pramlintide is a 37-amino acid polypeptide that differs structurally from human amylin by the replacement of alanine, serine, and serine at positions 25, 28, and 29 respectively with proline. |
| Mechanism of Action | Pramlintide is an amlyinomimetic, a functional analog of the naturally occurring pancreatic hormone amylin. Amylin has activity in a number of gastrointestinal and glucodynamic systems, and by mimicking its activity, pramlintide acts to improve glycemic control through modulation of the rate of gastric emptying, prevention of post-prandial rise in glucagon levels, and by increasing sensations of satiety, thereby reducing caloric intake and potentiating weight loss. There appears to be at least three distinct receptor complexes that bind with high affinity to amylin. All three complexes contain the calcitonin receptor at the core, plus one of three Receptor activity-modifying proteins, RAMP1, RAMP2, or RAMP3. |
| Toxicity | N.A. |
| Metabolism | Metabolized primarily by the kidneys. |
| Absorption | The absolute bioavailability of a single subcutaneous dose of pramlintide is approximately 30 to 40%. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | N.A. |
| Patents Number | US5686411 |
| Date of Issue | 17/03/03 |
| Date of Expiry | 17/03/23 |
| Drug Interaction | N.A. |
| Target | Calcitonin receptor,Receptor activity-modifying protein 1,Receptor activity-modifying protein 2,Receptor activity-modifying protein 3 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Symlin |
| Company | Amylin Pharmaceuticals (now a wholly owned subsidiary of AstraZeneca) |
| Brand Discription | SYMLIN (pramlintide acetate) injection is an anti-diabetic medication for use in patients with diabetes treated with insulin. Pramlintide is a synthetic analog of human amylin, a naturally occurring neuroendocrine hormone synthesized by pancreatic beta cells that contributes to glucose control during the postprandial period. Pramlintide is provided as an acetate salt of the synthetic 37-amino acid polypeptide, which differs in amino acid sequence from human amylin by replacement with proline at positions 25 (alanine), 28 (serine), and 29 (serine). The structural formula of pramlintide acetate is shown below: Lys-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gln-Arg-Leu-Ala-Asn-Phe-Leu-Val-His-Ser-Ser-AsnAsn-Phe-Gly-Pro-Ile-Leu-Pro-Pro-Thr-Asn-Val-Gly-Ser-Asn-Thr-Tyr-NH2 acetate (salt) with a disulfide bridge between the two Cys residues. Pramlintide acetate is a white powder that has a molecular formula of C171H267N51O53S2• × C2H4O2 (3 ≤ × ≤ 8); the molecular weight is 3949.4. Pramlintide acetate is soluble in water. |
| Prescribed for | SYMLIN is indicated as an adjunctive treatment in patients with type 1 or type 2 diabetes who use mealtime insulin therapy and who have failed to achieve desired glucose control despite optimal insulin therapy. |
| Chemical Name | N.A. |
| Formulation | The disposable multidose SymlinPen pen-injector contains 1000 mcg/mL of pramlintide (as acetate). The formulation contains 2.25 mg/mL of metacresol as a preservative, D-mannitol as a tonicity modifier, acetic acid, sodium acetate as pH modifiers, and water for injection. SYMLIN has a pH of approximately 4.0 |
| Physcial Appearnce | Clear, isotonic, sterile solution for subcutaneous administration |
| Route of Administration | Subcutaneous |
| Recommended Dosage | Reduce mealtime insulin doses by 50%, then initiate SYMLIN at 15 mcg subcutaneously, injecting immediately prior to each major meal. Increase the SYMLIN dose to the next increment (30, 45, or 60 mcg) when no clinically significant nausea has occurred for at least 3 days. If significant nausea persists at the 45 or 60 mcg dose level, the SYMLIN dose should be decreased to 30 mcg. If the 30 mcg dose is not tolerated, discontinuation of SYMLIN therapy should be considered. |
| Contraindication | N.A. |
| Side Effects | Nausea, Anorexia, Vomiting, Arthralgia, Fatigue, Allergic Reaction, Dizziness |
| Useful Link | http://www.symlin.com/ http://www.rxlist.com/symlin-drug.htm http://www.drugs.com/pro/symlin.html http://diabetes.emedtv.com/symlin/symlin.html |
| PubMed ID | 18998755, 17619527, 16330288, 12841822 |
| 3-D Structure | Th1100 (View) or (Download) |