NICORANDIL

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C8H9N3O4
Molecular Weight	211.1748
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[O-][N+](=O)OCCNC(=O)C1=CC=CN=C1

InChI

InChIKey=LBHIOVVIQHSOQN-UHFFFAOYSA-N

InChI=1S/C8H9N3O4/c12-8(7-2-1-3-9-6-7)10-4-5-15-11(13)14/h1-3,6H,4-5H2,(H,10,12)

HIDE SMILES / InChI

Molecular Formula	C8H9N3O4
Molecular Weight	211.1748
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con105865.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/68020108

Nicorandil is a derivative of the niacinamide that is structurally combined with an organic nitrate. It provides a dual mode of action leading to relaxation of vascular smooth muscle. Nicorandil is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase. Nicorandil has a direct effect on coronary arteries without leading to a steal phenomenon. The overall action improves blood flow to post-stenotic regions and the oxygen balance in the myocardium.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
ATP-sensitive inward rectifier potassium channel 8 9 Target ID: P97794 Gene ID: 16523.0 Gene Symbol: Kcnj8 Target Organism: Mus musculus (Mouse) Sources: http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con105865.pdf	Opener 34
Sodium/calcium exchanger 1 1 Target ID: P23685 Gene ID: 475738.0 Gene Symbol: SLC8A1 Target Organism: Canis lupus familiaris (Dog) (Canis familiaris) Sources: https://www.ncbi.nlm.nih.gov/pubmed/26631169	Activator 1447

Conditions

Condition	Modality	Targets	Highest Phase	Product
Chronic stable angina 10 Sources: http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con105865.pdf	Preventing		Approved 8583	NICORANDIL Approved Use Is used for the prevention and long term treatment of chronic stable angina pectoris; reduction in the risk of acute coronary syndromes in patients with chronic stable angina and at least one of the following risk factors: Previous MI, Previous CABG, CHD on angiography or a positive exercise test together with one of the following: LVH on ECG, left ventricular dysfunction, age ≥ 65, diabetes mellitus (type I or II excluding those on sulphonylureas), hypertension or documented vascular disease. Launch Date 1992
Acute coronary syndrome 33 Sources: http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con105865.pdf	Palliative		Approved 8583	NICORANDIL Approved Use Is used for the prevention and long term treatment of chronic stable angina pectoris; reduction in the risk of acute coronary syndromes in patients with chronic stable angina and at least one of the following risk factors: Previous MI, Previous CABG, CHD on angiography or a positive exercise test together with one of the following: LVH on ECG, left ventricular dysfunction, age ≥ 65, diabetes mellitus (type I or II excluding those on sulphonylureas), hypertension or documented vascular disease. Launch Date 1992

C_max

Value	Dose	Analyte	Population
173.59 ng/mL OTHER GOV'T https://mhraproducts4853.blob.core.windows.net/docs/0333728229ac707af08e4320dadca85f6555c479#page=9	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
199.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
502.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
761 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
888.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	24 mg single, intravenous dose: 24 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
63.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	20 μg/kg bw single, intravenous dose: 20 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	28 μg/kg bw single, intravenous dose: 28 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
143 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	39 μg/kg bw single, intravenous dose: 39 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
150 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	54 μg/kg bw single, intravenous dose: 54 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
245 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	74 μg/kg bw single, intravenous dose: 74 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
394 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	103 μg/kg bw single, intravenous dose: 103 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
619 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	144 μg/kg bw single, intravenous dose: 144 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
889 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	200 μg/kg bw single, intravenous dose: 200 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
134.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
271.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	8 mg single, intravenous dose: 8 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
503.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
978.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
738 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	158 mg/kg single, intravenous dose: 158 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1195 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	251 mg/kg single, intravenous dose: 251 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2209 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	398 mg/kg single, intravenous dose: 398 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2303 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	630 mg/kg single, intravenous dose: 630 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
242.77 ng × h/mL OTHER GOV'T https://mhraproducts4853.blob.core.windows.net/docs/0333728229ac707af08e4320dadca85f6555c479#page=9	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
187.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
422 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
766.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
993 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	24 mg single, intravenous dose: 24 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
30.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	20 μg/kg bw single, intravenous dose: 20 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
35.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	28 μg/kg bw single, intravenous dose: 28 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
69.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	39 μg/kg bw single, intravenous dose: 39 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
72.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	54 μg/kg bw single, intravenous dose: 54 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
114 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	74 μg/kg bw single, intravenous dose: 74 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
213 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	103 μg/kg bw single, intravenous dose: 103 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
333 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	144 μg/kg bw single, intravenous dose: 144 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
464 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	200 μg/kg bw single, intravenous dose: 200 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1994.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	35.5 mg 1 times / hour multiple, intravenous dose: 35.5 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2274.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	47.25 mg 1 times / hour multiple, intravenous dose: 47.25 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3549.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	59 mg 1 times / hour multiple, intravenous dose: 59 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
52.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
104 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	8 mg single, intravenous dose: 8 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
207.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
301.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
264 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	158 mg/kg single, intravenous dose: 158 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
424 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	251 mg/kg single, intravenous dose: 251 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
981 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	398 mg/kg single, intravenous dose: 398 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1268 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	630 mg/kg single, intravenous dose: 630 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.51 h OTHER GOV'T https://mhraproducts4853.blob.core.windows.net/docs/0333728229ac707af08e4320dadca85f6555c479#page=9	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.14 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	6 mg single, intravenous dose: 6 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.52 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.17 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=9 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=15	24 mg single, intravenous dose: 24 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	20 μg/kg bw single, intravenous dose: 20 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.74 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	28 μg/kg bw single, intravenous dose: 28 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	39 μg/kg bw single, intravenous dose: 39 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.77 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	54 μg/kg bw single, intravenous dose: 54 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	74 μg/kg bw single, intravenous dose: 74 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	103 μg/kg bw single, intravenous dose: 103 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.76 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	144 μg/kg bw single, intravenous dose: 144 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.73 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=16	200 μg/kg bw single, intravenous dose: 200 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.99 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	35.5 mg 1 times / hour multiple, intravenous dose: 35.5 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.72 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	47.25 mg 1 times / hour multiple, intravenous dose: 47.25 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.01 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=17	59 mg 1 times / hour multiple, intravenous dose: 59 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	NICORANDIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.48 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	8 mg single, intravenous dose: 8 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.18 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	12 mg single, intravenous dose: 12 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.25 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_Q100_1.pdf#page=10 \| https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=19	18 mg single, intravenous dose: 18 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	158 mg/kg single, intravenous dose: 158 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	251 mg/kg single, intravenous dose: 251 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	398 mg/kg single, intravenous dose: 398 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=20	630 mg/kg single, intravenous dose: 630 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered:	NICORANDIL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
75% OTHER https://www.medicines.org.uk/emc/product/9071/smpc#PHARMACOKINETIC_PROPS			NICORANDIL plasma	Homo sapiens
58.5% OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_W104_1.pdf#page=4			NICORANDIL serum	Homo sapiens

Doses

Dose	Population	Adverse events
200 ug/kg/h single, intravenous Studied dose Dose: 200 ug/kg/h Route: intravenous Route: single Dose: 200 ug/kg/h Sources: https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_X103_1.pdf#page=27	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_X103_1.pdf#page=27	Sources: https://www.pmda.go.jp/drugs/2007/P200700050/45004500_20500AMZ00348000_X103_1.pdf#page=27

PubMed

Title	Date	PubMed
Nicorandil prevents epinephrine-induced arrhythmias in halothane-anesthetized rats by nitric oxide-dependent mechanism.	2002-12	12444492
The effects of vasodilators on the relaxation of guinea-pig aorta during acute recoil.	2002-12	12419556
Nicorandil reduced coronary events in stable angina.	2002-11-07	12418823
[Fast-disintegration oral tablets having sustained release property].	2002-11	12440156
Nicorandil and leukocyte activation.	2002-11	12409977
Infarct size limitation by nicorandil: roles of mitochondrial K(ATP) channels, sarcolemmal K(ATP) channels, and protein kinase C.	2002-10-16	12392845
K(ATP) channel opening is an endogenous mechanism of protection against the no-reflow phenomenon but its function is compromised by hypercholesterolemia.	2002-10-02	12383584
Nicorandil ameliorates posttransplant dysfunction in cardiac allografts harvested from non-heart-beating donors.	2002-10	12428383
[A case of intraoperative repeated coronary artery spasm with ST-segment depression].	2002-10	12428317
Nicorandil infusion leads to good recovery from ischemia of left ventricular regional work in comparison with nitroglycerin.	2002-10	12381090
Long-term administration of nicorandil abolishes ischemic and pharmacologic preconditioning of the human myocardium: role of mitochondrial adenosine triphosphate-dependent potassium channels.	2002-10	12324733
Opening of the adenosine triphosphate-sensitive potassium channel attenuates cardiac remodeling induced by long-term inhibition of nitric oxide synthesis: role of 70-kDa S6 kinase and extracellular signal-regulated kinase.	2002-09-04	12225728
Nicorandil-induced preconditioning as evidenced by troponin T measurements after coronary angioplasty in patients with stable angina pectoris.	2002-09	12452302
Left ventricular remodeling after infarction: sequential MR imaging with oral nicorandil therapy in rat model.	2002-09	12202722
Antiapoptotic effect of nicorandil mediated by mitochondrial atp-sensitive potassium channels in cultured cardiac myocytes.	2002-08-21	12204514
Nicorandil associated anal ulceration.	2002-08-17	12241662
Triggers of ventricular tachyarrhythmias and therapeutic effects of nicorandil in canine models of LQT2 and LQT3 syndromes.	2002-08-07	12142125
Inhibition of human and pig ureter motility in vitro and in vivo by the K(+) channel openers PKF 217-744b and nicorandil.	2002-08	12130728
Nicorandil improves myocardial high-energy phosphates in postinfarction porcine hearts.	2002-08	12099993
Original method for nicorandil synthesis.	2002-07-03	12092148
[Microanalysis of tryptophan metabolites and suppressor factor of delayed-type hypersensitivity in mice].	2002-07	12136639
Nicorandil preserves mitochondrial function during ischemia in perfused rat heart.	2002-06-20	12098593
Effect of potassium-channel openers on the release of endothelium-derived hyperpolarizing factor in porcine coronary arteries stored in cold hyperkalemic solution.	2002-06	12139122
Highly protective effects of chronic oral administration of nicorandil on the heart of ageing rats.	2002-05-16	12010190
[Adenosine production and its role in protection against ischemic and reperfusion injury of the myocardium].	2002-05	12061138
Promises kept and broken: new pharmaceuticals.	2002-05	12032574
Opening of K(ATP) channel attenuates the increase in QT dispersion produced by the first balloon inflation during coronary angioplasty.	2002-05	12030342
Blood pool contrast-enhanced MRI detects suppression of microvascular permeability in early postinfarction reperfusion after nicorandil therapy.	2002-05	11979568
ATP-sensitive potassium channels and endogenous adenosine are involved in spinal antinociception produced by locus coeruleus stimulation.	2002-04-25	11973594
Effect of nicorandil on coronary events in patients with stable angina: the Impact Of Nicorandil in Angina (IONA) randomised trial.	2002-04-13	11965271
The IONA study: preparing the myocardium for ischaemia?	2002-04-13	11965265
Noninvasive assessment of the effects of nicorandil on left ventricular volumes and function in reperfused myocardial infarction.	2002-04	12062364
Nicorandil inhibits degranulation and TNF-alpha release from RBL-2H3 cells.	2002-04	12058954
Pharmacological modulation of K(ATP) channels.	2002-04	12023875
Effect of ischemic preconditioning and mitochondrial KATP channel openers on chronic left ventricular remodeling in the ischemic-reperfused rat heart.	2002-04	11954959
Nicorandil enhances myocardial tolerance to ischemia without progressive collateral recruitment during coronary angioplasty.	2002-04	11954943
Angina, diabetes and SUR.	2002-03	11993445
Selective mitochondrial K(ATP) channel activation results in antiarrhythmic effect during experimental myocardial ischemia/reperfusion in anesthetized rabbits.	2002-02-22	11890905
Interactions of sildenafil with various coronary vasodilators in isolated porcine coronary artery.	2002-02-22	11890904
[Anesthetic management of MIDCAB with high dose diltiazem].	2002-02	11889788
Vasorelaxant properties of isolated human radial arteries: comparison with internal mammary arteries.	2002-02	11849657
Effects of nicorandil on myocardial function and metabolism in the post-ischaemic reperfused heart with or without inhalation anaesthetics.	2002-01	11903068
[Protective effect of nicorandil (ATP-sensitive potassium channel opener) on ischemic rabbit spinal cord].	2002-01	11868374
Synergistic effect of nicorandil and amlodipine on mitochondrial function during isoproterenol-induced myocardial infarction in rats.	2002-01	11829124
Clinical trials update: The Heart Protection Study, IONA, CARISA, ENRICHD, ACUTE, ALIVE, MADIT II and REMATCH. Impact Of Nicorandil on Angina. Combination Assessment of Ranolazine In Stable Angina. ENhancing Recovery In Coronary Heart Disease patients. Assessment of Cardioversion Using Transoesophageal Echocardiography. AzimiLide post-Infarct surVival Evaluation. Randomised Evaluation of Mechanical Assistance for Treatment of Chronic Heart failure.	2002-01	11812672
Arrhythmogenic peroxynitrite-induced alterations in mammalian heart contractility and its prevention with quercetin-filled liposomes.	2002	12271156
Formulation optimization and stability study of transdermal therapeutic system of nicorandil.	2002	12229264
[Mouth ulcers in patients receiving tacrolimus].	2001-12	11908135
Safety of oral nicorandil before coronary artery bypass graft surgery.	2001-12	11878685
Involvement of potassium channels in spinal antinociceptions induced by fentanyl, clonidine and bethanechol in rats.	2001-12	11829146

Patents

Sample Use Guides

In Vivo Use Guide

The recommended starting dose is 10 mg nicorandil twice daily, although 5 mg twice daily may be employed in patients particulary susceptible to headache.

Route of Administration: Oral

In Vitro Use Guide

Nicorandil relaxes coronary vascular smooth muscle by stimulating guanylyl cyclase and increasing cyclic GMP (cGMP) levels as well as by a second mechanism resulting in activation of K+ channels and hyperpolarization. The relative contributions of either mechanism to the overall response in bovine circular strips of coronary arteries by simultaneously measuring changes in length and in cGMP levels through radioimmunoassay were studied. Blockade by 10 microM methylene blue of the cGMP increases in strips precontracted by 1 microM of the thromboxane A2 analogue U46619 reduced nicorandil-induced relaxation to 30-50%, and there were no significant changes in cGMP levels. Suppression of the hyperpolarizing component of nicorandil by 80.4 mM K+ or 1 microM glibenclamide in precontracted strips reduced nicorandil relaxation to 50% (K+) or shifted the dose response to the right by a factor of two (glibenclamide) without alteration of increases in cGMP. A quantitative separation of both mechanisms of action was obtained by comparing the correlation between increases in cGMP and relaxation under conditions of inhibited versus noninhibited hyperpolarization. The results indicate that cGMP contributes to the total relaxing effect of nicorandil by 30-40% at low concentrations and 80-90% at high concentrations of nicorandil.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:35:48 GMT 2025` Edited by `admin` on `Mon Mar 31 17:35:48 GMT 2025`
Record UNII	260456HAM0
Record Status	`Validated (UNII)`
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Name

Type

Language

SIGMART

Preferred Name

English

NICORANDIL

Official Name

English

NICORANDIL [USAN]

Common Name

English

NICORANDIL [MART.]

Common Name

English

NICORANDIL [EP MONOGRAPH]

Common Name

English

3-PYRIDINECARBOXAMIDE, N-(2-(NITROXY)ETHYL)-

Common Name

English

Nicorandil [WHO-DD]

Common Name

English

N-(2-Hydroxyethyl)nicotinamide nitrate (ester)

Common Name

English

nicorandil [INN]

Common Name

English

SG-75

Code

English

NICORANDIL [MI]

Common Name

English

NICORANDIL [JAN]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QC01DX16