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ziconotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peptides and glycopeptides | 2878 | 107452-89-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Ziconotide binds to N-type calcium channels located on the primary nociceptive (A-delta and C) afferent nerves in the superficial layers (Rexed laminae I and II) of the dorsal horn in the spinal cord. Although the mechanism of action of ziconotide has not been established in humans, results in animals suggest that its binding blocks N-type calcium channels, which leads to a blockade of excitatory neurotransmitter release from the primary afferent nerve terminals and antinociception.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 12 | mcg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.43 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 4.05 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.50 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.30 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 28, 2004 | FDA | JAZZ PHARMS INTL |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Device issue | 139.09 | 33.90 | 41 | 1555 | 29496 | 90597355 |
| Hallucination, auditory | 96.74 | 33.90 | 27 | 1569 | 15948 | 90610903 |
| Confusional state | 78.34 | 33.90 | 60 | 1536 | 386145 | 90240706 |
| Mental status changes | 62.44 | 33.90 | 25 | 1571 | 44654 | 90582197 |
| Nystagmus | 56.74 | 33.90 | 15 | 1581 | 7212 | 90619639 |
| Drug withdrawal syndrome | 54.17 | 33.90 | 20 | 1576 | 28703 | 90598148 |
| Hallucination | 44.01 | 33.90 | 22 | 1574 | 65937 | 90560914 |
| Psychotic disorder | 35.21 | 33.90 | 15 | 1581 | 31215 | 90595636 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Device issue | 149.52 | 35.22 | 42 | 1380 | 13467 | 42606446 |
| Confusional state | 84.25 | 35.22 | 58 | 1364 | 167539 | 42452374 |
| Hallucination | 68.94 | 35.22 | 35 | 1387 | 57472 | 42562441 |
| Hallucination, auditory | 62.09 | 35.22 | 22 | 1400 | 14842 | 42605071 |
| Drug withdrawal syndrome | 47.36 | 35.22 | 20 | 1402 | 21529 | 42598384 |
| Vasoplegia syndrome | 37.39 | 35.22 | 10 | 1412 | 2645 | 42617268 |
| Complication associated with device | 36.10 | 35.22 | 12 | 1410 | 6669 | 42613244 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Device issue | 244.17 | 33.81 | 71 | 2681 | 34464 | 110552083 |
| Confusional state | 141.25 | 33.81 | 106 | 2646 | 468574 | 110117973 |
| Hallucination, auditory | 117.11 | 33.81 | 38 | 2714 | 26359 | 110560188 |
| Drug withdrawal syndrome | 96.14 | 33.81 | 36 | 2716 | 38018 | 110548529 |
| Hallucination | 93.33 | 33.81 | 47 | 2705 | 101385 | 110485162 |
| Mental status changes | 81.11 | 33.81 | 39 | 2713 | 76083 | 110510464 |
| Psychotic disorder | 53.93 | 33.81 | 26 | 2726 | 50911 | 110535636 |
| Nystagmus | 48.61 | 33.81 | 16 | 2736 | 11561 | 110574986 |
| Hallucination, visual | 44.30 | 33.81 | 21 | 2731 | 39584 | 110546963 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02BG08 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Other analgesics and antipyretics |
| FDA MoA | N0000020069 | N-Calcium Channel Receptor Antagonists |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018696 | Neuroprotective Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| FDA EPC | N0000175697 | N-type Calcium Channel Antagonist |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
N02BG Other analgesics and antipyretics 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain in spine | indication | 48926009 | |
| Severe pain | indication | 76948002 | |
| Chronic pain | indication | 82423001 | |
| Chronic Pain with Opioid Tolerance | indication | ||
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Psychotic disorder | contraindication | 69322001 | |
| Increased Creatine Phosphokinase | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.79 | acidic |
| pKa2 | 9.65 | acidic |
| pKa3 | 12.24 | acidic |
| pKa4 | 12.4 | acidic |
| pKa5 | 12.58 | acidic |
| pKa6 | 12.87 | acidic |
| pKa7 | 12.94 | acidic |
| pKa8 | 13.0 | acidic |
| pKa9 | 13.12 | acidic |
| pKa10 | 13.22 | acidic |
| pKa11 | 13.3 | acidic |
| pKa12 | 13.5 | acidic |
| pKa13 | 13.6 | acidic |
| pKa14 | 13.61 | acidic |
| pKa15 | 13.84 | acidic |
| pKa16 | 13.96 | acidic |
| pKa17 | 14.0 | acidic |
| pKa18 | 11.5 | Basic |
| pKa19 | 11.17 | Basic |
| pKa20 | 10.92 | Basic |
| pKa21 | 10.69 | Basic |
| pKa22 | 10.39 | Basic |
| pKa23 | 10.01 | Basic |
| pKa24 | 6.94 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-dependent N-type calcium channel subunit alpha-1B | Ion channel | BLOCKER | UNKNOWN | CHEMBL | |||||
| Voltage-dependent N-type calcium channel subunit alpha-1B | Ion channel | BLOCKER | IC50 | 10.30 | IUPHAR | ||||
| Voltage-dependent P/Q-type calcium channel subunit alpha-1A | Ion channel | BLOCKER | IC50 | 6.30 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4024901 | VUID |
| N0000171594 | NUI |
| D06363 | KEGG_DRUG |
| 914454-03-8 | SECONDARY_CAS_RN |
| 4024901 | VANDF |
| C0211011 | UMLSCUI |
| CHEBI:142406 | CHEBI |
| CHEMBL4594214 | ChEMBL_ID |
| CHEMBL1795072 | ChEMBL_ID |
| DB06283 | DRUGBANK_ID |
| C078452 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2536 | IUPHAR_LIGAND_ID |
| 7694 | INN_ID |
| 7I64C51O16 | UNII |
| 16135415 | PUBCHEM_CID |
| 486126 | RXNORM |
| 19115 | MMSL |
| 64067 | MMSL |
| d05424 | MMSL |
| 008810 | NDDF |
| 008811 | NDDF |
| 416293004 | SNOMEDCT_US |
| 416512006 | SNOMEDCT_US |
| 425344003 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PRIALT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70720-720 | INJECTION, SOLUTION | 100 ug | INTRATHECAL | NDA | 28 sections |
| PRIALT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70720-722 | INJECTION, SOLUTION | 100 ug | INTRATHECAL | NDA | 28 sections |
| PRIALT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70720-723 | INJECTION, SOLUTION | 25 ug | INTRATHECAL | NDA | 28 sections |