Drug

D0286 | Nicorandil

Molecular Formula C8H9N3O4
Molecular Weight 211.17
Structure
State solid
Clearance The total body clearance is approximately 1.15 L/min [A20328].
Volume of distribution After oral (and i.v.) administration of the drug, the apparent volume of distribution is approximately 1.0-1.4 L/kg body weight [A20328].
Route of elimination The main route of elimination is the kidney with more than 60% of the administered dose was eliminated in the urine 24 hours after dosing [L887]. Only approximately 1% of nicorandil is excreted unchanged in the urine, and the remaining compounds are mainly the denitrated metabolite (9%) and its derivatives (e.g. nicotinuric acid 6%, nicotinamide 1%, N-methylnicotinamide < 1% and nicotinic acid < 1%) [L887]. Less than 2% of administered dose is excreted through the biliary system [A20328].
Protein binding Nicorandil is about 25% bound to human albumin and other plasma proteins [A20328].
Half life The elimination half life is approximately 1 hour [A20328].
Absorption Following oral administration, nicorandil is well absorbed from the gastrointestinal tract with the oral bioavailability of 75% with the maximum peak plasma concentration (Cmax) reached within 30-60 minutes. The mean Cmax is Cmax then is approximately 300 ng/ml [A20328]. Steady-state plasma concentrations of nicorandil usually are reached within approximately 96-120 h after twice daily dosing (10 or 20mg) [L887].
Trade names Ikorel
Description vasodilatory drug

C

C01DX16 Nicorandil


[C01DX] Other vasodilators used in cardiac diseases


[C01D] VASODILATORS USED IN CARDIAC DISEASES


[C01] CARDIAC THERAPY


[C] Cardiovascular system


Pictogram Signal Statements Precautionary Statement Codes
Danger

Aggregated GHS information provided by 65 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


Reported as not meeting GHS hazard criteria by 1 of 65 companies. For more detailed information, please visit ECHA C&L website


Of the 6 notification(s) provided by 64 of 65 companies with hazard statement code(s):


H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]


H318 (60.94%): Causes serious eye damage [Danger Serious eye damage/eye irritation]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


P264, P270, P280, P301+P312, P305+P351+P338, P310, P330, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Organism Test type Route Dose (normalized dose) Effect Source
dog LD50 oral 62500ug/kg (62.5mg/kg) Yakkyoku. Pharmacy. Vol. 35, Pg. 1627, 1984.
rat LD50 oral 1220mg/kg (1220mg/kg) Yakkyoku. Pharmacy. Vol. 35, Pg. 1627, 1984.
mouse LD50 intravenous > 560mg/kg (560mg/kg) Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 36, Pg. 425, 1994.
man TDLo oral 195mg/kg/1Y-I (195mg/kg) gastrointestinal: other changes Lancet. Vol. 352, Pg. 1598, 1998.
rat LD50 intravenous 502mg/kg (502mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 19, Pg. 2561, 1991.
mouse LD50 intraperitoneal 214mg/kg (214mg/kg) Yaoxue Tongbao. Bulletin of Pharmacology. Vol. 23, Pg. 182, 1988.
rat LD50 intraperitoneal 1100mg/kg (1100mg/kg) Yakkyoku. Pharmacy. Vol. 35, Pg. 1627, 1984.
rat LD50 subcutaneous 1200mg/kg (1200mg/kg) Yakkyoku. Pharmacy. Vol. 35, Pg. 1627, 1984.
mouse LD50 oral 626mg/kg (626mg/kg) Yaoxue Tongbao. Bulletin of Pharmacology. Vol. 23, Pg. 182, 1988.
dog LDLo intravenous 60mg/kg (60mg/kg) Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 19, Pg. 2561, 1991.
mouse LD50 subcutaneous 1350mg/kg (1350mg/kg) Yakkyoku. Pharmacy. Vol. 35, Pg. 1627, 1984.

  • Acute coronary syndrome

  • Arteriospasm coronary

  • Myocardial infarction

  • Myocardial ischaemia

  • 2-(Nicotinamido)ethyl nitrat 2-(Pyridine-3-carboxamido)ethyl Nitrate 2-(nicotinamido)ethyl nitrate
    2-(pyridin-3-ylcarbonylamino)ethyl nitrate 2-(pyridine-3-carbonylamino)ethyl nitrate 2-Nicotinamidethyl Nitrate
    2-Nicotinamidoethyl nitrate 2-[(3-pyridinylcarbonyl)amino]ethyl nitrate 2-[(PYRIDIN-3-YLCARBONYL)AMINO]ETHYL NITRATE
    2-[(Pyridine-3-carbonyl)amino]ethyl nitrate 260456HAM0 3-PYRIDINECARBOXAMIDE, N-[2-(NITROOXY)ETHYL]-
    3-Pyridinecarboxamide, N-(2-(nitrooxy)ethyl)- 3-Pyridinecarboxamide, N-(2-(nitroxy)ethyl)- 65141-46-0
    A834984 AB0013362 AB00639978-08
    AB00639978-09 AB00639978_10 AB00639978_11
    AB04467 AB2000397 AC-4690
    AKOS001589705 AKOS015855406 AKOS025149378
    API0003563 ARONIS24318 Adancor
    Aprior BBC/474 BCP09434
    BDBM50247908 BG0267 BRD-K97752965-001-01-6
    BRN 0481451 C13280 CAS-65141-46-0
    CCG-101045 CHEBI:31905 CHEMBL284906
    CPD000466365 CS-2383 D01810
    DB09220 DSSTox_CID_25692 DSSTox_GSID_45692
    DSSTox_RID_81064 DTXSID8045692 Dancor
    EINECS 265-514-1 F0005-2298 FT-0602677
    GTPL2411 H924 HMS2051N16
    HMS2089L12 HMS2095E14 HMS2232A06
    HMS3268L19 HMS3371N18 HMS3393N16
    HMS3413G17 HMS3655P05 HMS3677G17
    HMS3712E14 HS-0049 HY-B0341
    Ikorel Ikorel;Dancor;Nikoran;Aprior;Nitorubin;Sigmart J10427
    KS-00000UH3 KS-0000478H LBHIOVVIQHSOQN-UHFFFAOYSA-N
    LS-130673 MCULE-6145684901 MFCD00186520
    MLS000759488 MLS001424162 MLS002222323
    MLS006010701 N-(2-Hydroxyethyl)nicotinamide nitrate N-(2-Hydroxyethyl)nicotinamide nitrate (ester)
    N-[2-(NITROOXY)ETHYL]-3-PYRIDINECARBOXAMIDE N-[2-(Nitrooxy)ethyl]pyridine-3-carboxamide N-[2-(nitrooxy)ethyl]-3-pyridylcarboxamide
    N0837 NC00295 NCGC00025357-01
    NCGC00025357-02 NCGC00025357-04 NICORANDIL
    Nicorandil (Ikorel) Nicorandil (JP17/USAN/INN) Nicorandil [USAN:BAN:INN:JAN]
    Nicorandil [USAN:INN:BAN:JAN] Nicorandil(Ikorel) Nicorandilum
    Nicorandilum [INN-Latin] Nikoran Nitorubin
    PERISALOL Q862989 RP-46417
    SAM001246701 SBB080749 SC-12673
    SCHEMBL34547 SG 75 SG-75
    SMR000466365 SR-01000597534 SR-01000597534-1
    SR-01000597534-5 ST45054164 STL445540
    SW197675-3 Sigmart Sigmart (TN)
    Tox21_110968 Tox21_110968_1 UNII-260456HAM0
    ZINC1533102 ZX-AFC001332 ZX-AS004678
    n-(2-hydroxyethyl)nicotinamide nitrate ester nitric acid 2-[[oxo(3-pyridinyl)methyl]amino]ethyl ester s1971

    DrugBank Name Nicorandil
    DrugBank DB09220
    CAS Number 65141-45-9, 65141-46-0
    PubChem Compound 47528
    KEGG Compound ID C13280
    KEGG Drug D01810
    PubChem.Substance 310265127
    ChEBI 31905
    PharmGKB PA166184081
    ChemSpider 43240
    Wikipedia Nicorandil