isosorbide mononitrate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
NO2 - derivatives 1506 16051-77-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • isosorbide mononitrate
  • isosorbide 5-mononitrate
  • isosorbide 5-nitrate
  • monosorbitrate
  • isosorbide-5-mononitrate
for prevention of angina pectoris; structure given in first source; a Russian drug
  • Molecular weight: 191.14
  • Formula: C6H9NO6
  • CLOGP: -2.51
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 93.74
  • ALOGS: -0.53
  • ROTB: 2

Drug dosage:

DoseUnitRoute
40 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.97 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 93 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 1 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 30, 1991 FDA

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
Hypotension 217.68 63.22 63 359 32373 2325290
Toxic epidermal necrolysis 137.91 63.22 28 394 3116 2354547
Respiratory disorder 131.15 63.22 28 394 3976 2353687
Dermatitis exfoliative 116.70 63.22 21 401 1220 2356443
Multiple organ dysfunction syndrome 113.14 63.22 28 394 7613 2350050
Electrolyte imbalance 112.43 63.22 22 400 2015 2355648
Hyperthyroidism 111.79 63.22 22 400 2075 2355588
Bradycardia 110.54 63.22 29 393 9952 2347711
Cholecystitis 110.34 63.22 22 400 2218 2355445
Intentional overdose 106.92 63.22 29 393 11292 2346371
Presyncope 104.27 63.22 23 399 3780 2353883
Subarachnoid haemorrhage 99.65 63.22 20 402 2080 2355583
Colitis microscopic 95.59 63.22 17 405 919 2356744
Diarrhoea 94.89 63.22 44 378 83520 2274143
Dizziness 92.63 63.22 39 383 58626 2299037
Blister 86.11 63.22 22 400 6749 2350914
Restlessness 84.18 63.22 20 402 4543 2353120
Erythema 84.08 63.22 29 393 25130 2332533
Cholelithiasis 79.40 63.22 20 402 5783 2351880
Toxicity to various agents 72.97 63.22 28 394 32726 2324937
Condition aggravated 70.01 63.22 27 395 31952 2325711

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
Hypotension 405.79 49.73 111 317 29543 1716810
Syncope 153.31 49.73 45 383 14124 1732229
Dizziness 100.15 49.73 41 387 34320 1712033
Presyncope 94.92 49.73 22 406 2676 1743677
Wrong patient received product 68.10 49.73 11 417 192 1746161
Angina pectoris 67.44 49.73 19 409 4999 1741354
Acute kidney injury 66.52 49.73 31 397 34913 1711440
Bradycardia 61.31 49.73 21 407 10513 1735840
Dehydration 57.66 49.73 23 405 17635 1728718
Cardiac failure 57.63 49.73 21 407 12581 1733772
Left atrial dilatation 52.02 49.73 9 419 241 1746112
Atrial fibrillation 50.38 49.73 20 408 15091 1731262

Pharmacologic Action:

SourceCodeDescription
ATC C01DA14 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
VASODILATORS USED IN CARDIAC DISEASES
Organic nitrates
FDA EPC N0000175415 Nitrate Vasodilator
FDA Chemical/Ingredient N0000007647 Nitrates
FDA PE N0000009909 Vasodilation
CHEBI has role CHEBI:35620 vasodilator agent
MeSH PA D002317 Cardiovascular Agents
MeSH PA D020030 Nitric Oxide Donors
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Angina pectoris indication 194828000
Angina Pectoris Prevention indication
Chronic heart failure off-label use 48447003
Prevention of Bleeding Esophageal Varices off-label use
Myocardial infarction contraindication 22298006 DOID:5844
Hyperthyroidism contraindication 34486009 DOID:7998
Low blood pressure contraindication 45007003
Injury of head contraindication 82271004
Increased intestinal motility contraindication 102624003
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Anemia contraindication 271737000 DOID:2355
Cerebral hemorrhage contraindication 274100004
Malabsorption States contraindication

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Soluble guanylate cyclase Enzyme ACTIVATOR CHEMBL CHEMBL
Atrial natriuretic peptide receptor 1 Enzyme WOMBAT-PK

External reference:

IDSource
4020224 VUID
N0000179163 NUI
C0064079 UMLSCUI
D00630 KEGG_DRUG
4020224 VANDF
6257 MMSL
28004 RXNORM
d00269 MMSL
4935 MMSL
386854005 SNOMEDCT_US
003639 NDDF
27661 PUBCHEM_CID
CHEBI:6062 CHEBI
CHEMBL1311 ChEMBL_ID
DB01020 DRUGBANK_ID
LX1OH63030 UNII
5177 INN_ID
7052 IUPHAR_LIGAND_ID
C030397 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Isosorbide HUMAN PRESCRIPTION DRUG LABEL 1 0143-2230 TABLET, FILM COATED, EXTENDED RELEASE 30 mg ORAL ANDA 12 sections
Isosorbide HUMAN PRESCRIPTION DRUG LABEL 1 0143-2260 TABLET, FILM COATED, EXTENDED RELEASE 60 mg ORAL ANDA 12 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0228-2620 TABLET 20 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0228-2631 TABLET 10 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-4544 TABLET, FILM COATED, EXTENDED RELEASE 60 mg ORAL ANDA 13 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-4546 TABLET, FILM COATED, EXTENDED RELEASE 30 mg ORAL ANDA 13 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-5549 TABLET 10 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-5550 TABLET 20 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-7756 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 12 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-7757 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 12 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0615-7767 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 12 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0615-7768 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 12 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0615-8043 TABLET 30 mg ORAL ANDA 14 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0615-8044 TABLET 60 mg ORAL ANDA 14 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6449 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6450 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 0904-6451 TABLET, EXTENDED RELEASE 120 mg ORAL ANDA 11 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 10544-243 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 12 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-104 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-105 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
ISOSORBIDE MONONITRATE HUMAN PRESCRIPTION DRUG LABEL 1 13668-106 TABLET, EXTENDED RELEASE 120 mg ORAL ANDA 11 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 21695-575 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 21695-777 TABLET, EXTENDED RELEASE 120 mg ORAL ANDA 11 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 21695-837 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 23155-178 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 23155-519 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections
Isosorbide Mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 23155-628 TABLET, EXTENDED RELEASE 120 mg ORAL ANDA 12 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 43063-313 TABLET, EXTENDED RELEASE 60 mg ORAL ANDA 11 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 43353-917 TABLET, EXTENDED RELEASE 120 mg ORAL ANDA 12 sections
isosorbide mononitrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-0787 TABLET, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections