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pramlintide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peptides and glycopeptides | 2236 | 151126-32-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pramlintide is an analog of human amylin. Amylin is colocated with insulin in secretory granules and cosecreted with insulin by pancreatic beta cells in response to food intake. Amylin and insulin show similar fasting and postprandial patterns in healthy individuals. In patients with type 1 and type 2 diabetes, there is reduced secretion from pancreatic beta cells of both insulin and amylin in response to food. Amylin affects the rate of postprandial glucose appearance through a variety of mechanisms, as determined by nonclinical studies. Amylin slows gastric emptying (i.e., the rate at which food is released from the stomach to the small intestine) without altering the overall absorption of nutrients. In addition, amylin suppresses glucagon secretion (not normalized by insulin alone), which leads to suppression of endogenous glucose output from the liver. Amylin also regulates food intake due to centrally-mediated modulation of appetite. In human studies, pramlintide, acting as an amylin analog, slows gastric emptying, reduces the postprandial rise in plasma glucagon, and modulates satiety leading to decreased caloric intake.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.00 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.41 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.40 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.60 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 16, 2005 | FDA | ASTRAZENECA AB |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BX05 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Other blood glucose lowering drugs, excl. insulins |
| FDA MoA | N0000020064 | Amylin Agonists |
| MeSH PA | D007004 | Hypoglycemic Agents |
| FDA EPC | N0000177910 | Amylin Analog |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:74518 | anti-obesity agent |
Related Drugs by ATC class:
A10BX Other blood glucose lowering drugs, excl. insulins 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Type 1 Diabetes Mellitus Treatment Adjunct | indication | ||
| Type 2 Diabetes Mellitus Treatment Adjunct | indication | ||
| Gastroparesis | contraindication | 235675006 | |
| Hypoglycemic disorder | contraindication | 237630007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.88 | acidic |
| pKa2 | 11.69 | acidic |
| pKa3 | 11.79 | acidic |
| pKa4 | 12.17 | acidic |
| pKa5 | 12.18 | acidic |
| pKa6 | 12.38 | acidic |
| pKa7 | 12.45 | acidic |
| pKa8 | 12.6 | acidic |
| pKa9 | 12.65 | acidic |
| pKa10 | 12.75 | acidic |
| pKa11 | 12.85 | acidic |
| pKa12 | 12.9 | acidic |
| pKa13 | 12.95 | acidic |
| pKa14 | 13.08 | acidic |
| pKa15 | 13.09 | acidic |
| pKa16 | 13.24 | acidic |
| pKa17 | 13.33 | acidic |
| pKa18 | 13.39 | acidic |
| pKa19 | 13.43 | acidic |
| pKa20 | 13.5 | acidic |
| pKa21 | 13.65 | acidic |
| pKa22 | 13.7 | acidic |
| pKa23 | 13.72 | acidic |
| pKa24 | 13.8 | acidic |
| pKa25 | 13.93 | acidic |
| pKa26 | 11.0 | Basic |
| pKa27 | 10.4 | Basic |
| pKa28 | 7.28 | Basic |
| pKa29 | 6.56 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Amylin receptor AMY2 | GPCR | AGONIST | EC50 | 8.64 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Amylin receptor AMY1 | GPCR | AGONIST | EC50 | 9.45 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Amylin receptor AMY3 | GPCR | AGONIST | EC50 | 9.05 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D05594 | KEGG_DRUG |
| 196078-30-5 | SECONDARY_CAS_RN |
| 4024910 | VANDF |
| C0537551 | UMLSCUI |
| CHEMBL2103758 | ChEMBL_ID |
| CHEMBL3833353 | ChEMBL_ID |
| DB01278 | DRUGBANK_ID |
| C105254 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7482 | IUPHAR_LIGAND_ID |
| 7448 | INN_ID |
| D3FM8FA78T | UNII |
| 70691388 | PUBCHEM_CID |
| 139953 | RXNORM |
| 19568 | MMSL |
| 19801 | MMSL |
| 66996 | MMSL |
| d05488 | MMSL |
| 010717 | NDDF |
| 010718 | NDDF |
| 416392006 | SNOMEDCT_US |
| 416425000 | SNOMEDCT_US |
| 427360000 | SNOMEDCT_US |
| CHEBI:135922 | CHEBI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SymlinPen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-6615 | INJECTION | 1000 ug | SUBCUTANEOUS | NDA | 29 sections |
| SymlinPen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0310-6627 | INJECTION | 1000 ug | SUBCUTANEOUS | NDA | 29 sections |