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

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	1909	55985-32-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nicardipine (+/-)-Nicardipine perpidine nicardipine hydrochloride nicardipine HCl	A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. Molecular weight: 479.53 Formula: C26H29N3O6 CLOGP: 5.23 LIPINSKI: 1 HAC: 9 HDO: 1 TPSA: 111.01 ALOGS: -5.29 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nicardipine
(+/-)-Nicardipine
perpidine
nicardipine hydrochloride
nicardipine HCl

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.

Molecular weight: 479.53
Formula: C26H29N3O6
CLOGP: 5.23
LIPINSKI: 1
HAC: 9
HDO: 1
TPSA: 111.01
ALOGS: -5.29
ROTB: 11

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
90	mg	O
90	mg	P

ADMET properties:

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Property	Value	Reference
S (Water solubility)	7.90 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	4.10 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	23 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	11 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 21, 1988	FDA	CHIESI USA INC

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
Premature delivery	172.76	24.01	78	6808	30203	63451933
Acute kidney injury	140.29	24.01	157	6729	263258	63218878
Cerebral vasoconstriction	138.66	24.01	31	6855	1177	63480959
Hyponatraemia	127.86	24.01	102	6784	111798	63370338
Eosinophilia	106.09	24.01	51	6835	22705	63459431
Posterior reversible encephalopathy syndrome	99.88	24.01	45	6841	17300	63464836
Hyperkalaemia	97.33	24.01	65	6821	54138	63427998
Hepatocellular injury	94.31	24.01	50	6836	27331	63454805
Acute motor-sensory axonal neuropathy	83.82	24.01	16	6870	273	63481863
Hypotension	81.11	24.01	122	6764	272482	63209654

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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
Cerebral vasoconstriction	107.21	21.17	20	4812	231	34951868
Blood lactic acid	88.83	21.17	18	4814	328	34951771
Foetal disorder	83.47	21.17	20	4812	806	34951293
Premature baby	81.47	21.17	44	4788	19589	34932510
Neutropenia neonatal	75.89	21.17	18	4814	694	34951405
Acute kidney injury	66.37	21.17	136	4696	304852	34647247
Eosinophilia	64.67	21.17	42	4790	26180	34925919
Low birth weight baby	63.99	21.17	28	4804	7877	34944222
Ureteric compression	62.67	21.17	13	4819	267	34951832
Cerebral haemorrhage	58.21	21.17	44	4788	34893	34917206

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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
Cerebral vasoconstriction	230.24	19.92	51	11163	1419	79731755
Acute kidney injury	183.64	19.92	289	10925	519115	79214059
Eosinophilia	162.95	19.92	93	11121	45252	79687922
Cerebral haemorrhage	120.73	19.92	84	11130	57589	79675585
Hyperkalaemia	104.67	19.92	103	11111	114295	79618879
Rash maculo-papular	102.02	19.92	75	11139	56003	79677171
Hepatocellular injury	98.85	19.92	69	11145	47524	79685650
Cholestasis	97.75	19.92	71	11143	52038	79681136
Hyponatraemia	92.03	19.92	119	11095	177729	79555445
Premature delivery	89.30	19.92	50	11164	23417	79709757

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C08CA04	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38215	calcium channel blockers
CHEBI has role	CHEBI:88230	autophagy inhibitors
CHEBI has role	CHEBI:176497	geroprotectors
FDA CS	M0006414	Dihydropyridines
FDA EPC	N0000175421	Dihydropyridine Calcium Channel Blocker
FDA MoA	N0000000069	Calcium Channel Antagonists
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors

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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
Hypertensive disorder	indication	38341003	DOID:10763
Angina pectoris	indication	194828000
Prinzmetal angina	off-label use	87343002
Raynaud's phenomenon	off-label use	266261006
Portal hypertension	contraindication	34742003	DOID:10762
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003
Chronic idiopathic constipation	contraindication	82934008
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.02	Basic
pKa2	2.37	Basic

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
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	DISCN	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF

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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-gated L-type calcium channel	Ion channel	Q01668 Q13936	CAC1D_HUMAN CAC1C_HUMAN	BLOCKER			CHEMBL	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.32	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.49	CHEMBL
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN				WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.78	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	6.55	WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN		Ki	5.55	WOMBAT-PK
Malate dehydrogenase cytoplasmic	Enzyme	P40925	MDHC_HUMAN		IC50	4.30	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.38	WOMBAT-PK
Beta-lactamase	Enzyme		AMPC_ECOLI		IC50	4.70	CHEMBL

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External reference:

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ID	Source
000712	NDDF
004518	NDDF
108526002	SNOMEDCT_US
108527006	SNOMEDCT_US
2278	MMSL
235230	RXNORM
2559	IUPHAR_LIGAND_ID
372502001	SNOMEDCT_US
4019350	VANDF
4019858	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cardene IV	HUMAN PRESCRIPTION DRUG LABEL	1	10122-313	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	23 sections
Cardene IV	HUMAN PRESCRIPTION DRUG LABEL	1	10122-314	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	23 sections
Cardene IV	HUMAN PRESCRIPTION DRUG LABEL	1	10122-325	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	NDA	23 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-009	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	24 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-009	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	24 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-009	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	24 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-009	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	24 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-016	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	NDA	24 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9542	INJECTION	2.50 mg	INTRAVENOUS	NDA	26 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9542	INJECTION	2.50 mg	INTRAVENOUS	NDA	26 sections

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