ziconotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 2878 107452-89-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ziconotide
  • prialt
  • omega-Conopeptide MVIIA (Conus)
  • ziconotide acetate
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.
  • Molecular weight: 2639.14
  • Formula: C102H172N36O32S7
  • CLOGP:
  • LIPINSKI: 3
  • HAC: 68
  • HDO: 42
  • TPSA: 1133.84
  • ALOGS: -3.05
  • ROTB: 38

Drug dosage:

DoseUnitRoute
12 mcg P

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Dec. 28, 2004 FDA JAZZ PHARMS INTL

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device issue 134.48 33.18 41 1516 23740 63463725
Hallucination, auditory 89.32 33.18 26 1531 12798 63474667
Confusional state 79.94 33.18 57 1500 236323 63251142
Nystagmus 54.05 33.18 15 1542 6205 63481260
Mental status changes 50.92 33.18 23 1534 39576 63447889
Hallucination 46.68 33.18 24 1533 54793 63432672
Drug withdrawal syndrome 42.08 33.18 18 1539 27176 63460289
Psychotic disorder 36.45 33.18 16 1541 25696 63461769

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device issue 155.23 35.70 42 1363 9735 34945791
Confusional state 80.06 35.70 57 1348 144103 34811423
Hallucination, auditory 66.71 35.70 23 1382 11894 34943632
Hallucination 52.56 35.70 30 1375 51468 34904058
Drug withdrawal syndrome 45.38 35.70 20 1385 19814 34935712
Complication associated with device 39.12 35.70 13 1392 5993 34949533
Vasoplegia syndrome 39.09 35.70 10 1395 1846 34953680
Psychotic disorder 38.37 35.70 19 1386 24433 34931093

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device issue 240.82 32.27 71 2582 27037 79714698
Confusional state 139.02 32.27 101 2552 317896 79423839
Hallucination, auditory 111.36 32.27 37 2616 20656 79721079
Drug withdrawal syndrome 82.36 32.27 34 2619 34684 79707051
Hallucination 76.82 32.27 43 2610 85702 79656033
Mental status changes 69.43 32.27 37 2616 66922 79674813
Psychotic disorder 60.89 32.27 29 2624 41373 79700362
Nystagmus 46.50 32.27 16 2637 9888 79731847
Hallucination, visual 42.31 32.27 21 2632 32708 79709027
Vasoplegia syndrome 34.30 32.27 10 2643 3620 79738115
Urinary retention 34.03 32.27 22 2631 56608 79685127
Aggression 33.62 32.27 21 2632 50937 79690798
Burning sensation 33.33 32.27 22 2631 58610 79683125

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02BG08 NERVOUS SYSTEM
ANALGESICS
OTHER ANALGESICS AND ANTIPYRETICS
Other analgesics and antipyretics
FDA MoA N0000020069 N-Calcium Channel Receptor Antagonists
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018696 Neuroprotective Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D020011 Protective Agents
MeSH PA D018689 Sensory System Agents
FDA EPC N0000175697 N-type Calcium Channel Antagonist
CHEBI has role CHEBI:35481 non-narcotic analgesic

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MCG/1ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
100MCG/1ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
100MCG/1ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
100MCG/1ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
100MCG/1ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
200MCG/2ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
200MCG/2ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
200MCG/2ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
200MCG/2ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
200MCG/2ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
500MCG/20ML (25MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
500MCG/20ML (25MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/20ML (25MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
500MCG/20ML (25MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/20ML (25MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
500MCG/5ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
500MCG/5ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/5ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
500MCG/5ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/5ML (100MCG/ML) PRIALT TERSERA N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
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
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-720 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 28 sections
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-722 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 28 sections
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-723 INJECTION, SOLUTION 25 ug INTRATHECAL NDA 28 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-720 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-720 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-720 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-722 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-722 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-722 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-723 INJECTION, SOLUTION 25 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-723 INJECTION, SOLUTION 25 ug INTRATHECAL NDA 30 sections
PRIALT HUMAN PRESCRIPTION DRUG LABEL 1 70720-723 INJECTION, SOLUTION 25 ug INTRATHECAL NDA 30 sections