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

Stem definition	Drug id	CAS RN
peptides and glycopeptides	2878	107452-89-1

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
12	mcg	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	4.05 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.30 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.50 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.43 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 28, 2004	FDA	JAZZ PHARMS INTL

FDA Adverse Event Reporting System (Female)

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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	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

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FDA Adverse Event Reporting System (Male)

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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	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

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FDA Adverse Event Reporting System (Geriatric)

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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	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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02BG08	NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Other analgesics and antipyretics
CHEBI has role	CHEBI:35481	non-narcotic analgesic
FDA EPC	N0000175697	N-type Calcium Channel Antagonist
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

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

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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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.79	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

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Voltage-dependent N-type calcium channel subunit alpha-1B	Ion channel	Q00975	CAC1B_HUMAN	BLOCKER			UNKNOWN	CHEMBL
Voltage-dependent N-type calcium channel subunit alpha-1B	Ion channel		CAC1B_RAT	BLOCKER	IC50	10.30	IUPHAR
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	Ion channel		CAC1A_RAT	BLOCKER	IC50	6.30	IUPHAR

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External reference:

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ID	Source
008810	NDDF
008811	NDDF
16135415	PUBCHEM_CID
19115	MMSL
4024901	VUID
4024901	VANDF
416293004	SNOMEDCT_US
416512006	SNOMEDCT_US
425344003	SNOMEDCT_US
486126	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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