isoniazid Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1497 54-85-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • isoniazid
  • 4-Pyridinecarboxylic hydrazide
  • armazid
  • isoniazide
  • isonicotinohydrazide
Antibacterial agent used primarily as a tuberculostatic. It remains the treatment of choice for tuberculosis.
  • Molecular weight: 137.14
  • Formula: C6H7N3O
  • CLOGP: -0.67
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 68.01
  • ALOGS: -0.59
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 153 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 7 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 72.92 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.82 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 7.40 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) 1 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 29, 1952 FDA SANDOZ

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
Drug reaction with eosinophilia and systemic symptoms 867.99 54.48 184 1790 5334 2350777
Acute hepatic failure 576.94 54.48 116 1858 2526 2353585
Drug-induced liver injury 521.07 54.48 113 1861 3586 2352525
Pyrexia 457.83 54.48 185 1789 53523 2302588
Drug resistance 447.91 54.48 94 1880 2530 2353581
Paradoxical drug reaction 432.25 54.48 70 1904 403 2355708
Jaundice 419.23 54.48 102 1872 5406 2350705
Hepatotoxicity 415.94 54.48 93 1881 3388 2352723
Hepatitis 355.65 54.48 92 1882 6245 2349866
Tuberculosis 276.74 54.48 60 1914 1875 2354236
Alanine aminotransferase increased 271.16 54.48 89 1885 13943 2342168
Aspartate aminotransferase increased 255.76 54.48 83 1891 12529 2343582
Vomiting 231.92 54.48 127 1847 71475 2284636
Tuberculoma of central nervous system 216.67 54.48 29 1945 24 2356087
Pulmonary tuberculosis 199.32 54.48 40 1934 845 2355266
Drug interaction 191.27 54.48 84 1890 29079 2327032
Exposure during pregnancy 179.52 54.48 77 1897 25142 2330969
Hepatic encephalopathy 175.54 54.48 40 1934 1567 2354544
Transaminases increased 173.99 54.48 49 1925 4538 2351573
Eosinophilia 165.57 54.48 43 1931 2927 2353184
Disseminated tuberculosis 160.73 54.48 31 1943 528 2355583
Nausea 154.04 54.48 116 1858 112073 2244038
Immune reconstitution inflammatory syndrome associated tuberculosis 153.06 54.48 21 1953 25 2356086
Lymphadenopathy 146.32 54.48 45 1929 5653 2350458
Hepatic failure 142.15 54.48 44 1930 5645 2350466
Hepatic function abnormal 139.18 54.48 44 1930 6048 2350063
Rash maculo-papular 136.91 54.48 40 1934 4212 2351899
Liver injury 136.22 54.48 35 1939 2279 2353832
Generalised tonic-clonic seizure 136.11 54.48 42 1932 5330 2350781
Encephalopathy 129.81 54.48 39 1935 4522 2351589
Hepatic enzyme increased 122.37 54.48 45 1929 9757 2346354
Toxicity to various agents 121.77 54.48 64 1910 32690 2323421
Coagulopathy 119.01 54.48 33 1941 2876 2353235
Liver function test abnormal 118.50 54.48 41 1933 7449 2348662
Condition aggravated 117.48 54.48 62 1912 31917 2324194
Pruritus 110.22 54.48 66 1908 43274 2312837
Rash 109.88 54.48 74 1900 59484 2296627
Hepatocellular injury 108.18 54.48 33 1941 4022 2352089
Cerebellar ataxia 108.10 54.48 19 1955 187 2355924
Seizure 94.20 54.48 49 1925 24417 2331694
Anaemia 93.62 54.48 55 1919 34737 2321374
Immune reconstitution inflammatory syndrome 88.97 54.48 22 1952 1222 2354889
Headache 88.07 54.48 73 1901 80106 2276005
Thrombocytopenia 84.32 54.48 42 1932 19089 2337022
Abdominal pain 83.77 54.48 51 1923 34323 2321788
Blood bilirubin increased 79.63 54.48 28 1946 5317 2350794
Meningitis tuberculous 77.40 54.48 13 1961 95 2356016
Neurotoxicity 77.24 54.48 22 1952 2108 2354003
Liver transplant 77.07 54.48 17 1957 570 2355541
Neuropathy peripheral 74.81 54.48 33 1941 11399 2344712
Metabolic acidosis 72.78 54.48 27 1947 5971 2350140
Liver disorder 71.02 54.48 27 1947 6387 2349724
Blood alkaline phosphatase increased 70.49 54.48 27 1947 6518 2349593
Tuberculosis of central nervous system 70.11 54.48 11 1963 49 2356062
Rhabdomyolysis 69.86 54.48 27 1947 6677 2349434
Gamma-glutamyltransferase increased 67.34 54.48 25 1949 5537 2350574
Intentional overdose 65.53 54.48 30 1944 11291 2344820
Peritoneal tuberculosis 62.31 54.48 11 1963 111 2356000
Cholestasis 61.22 54.48 21 1953 3700 2352411
Multiple-drug resistance 60.87 54.48 12 1962 229 2355882
Face oedema 60.00 54.48 21 1953 3927 2352184
Malaise 59.57 54.48 50 1924 55535 2300576
Drug ineffective 58.76 54.48 65 1909 101559 2254552
Maternal exposure during pregnancy 57.76 54.48 30 1944 14833 2341278
Abdominal pain upper 56.86 54.48 34 1940 22066 2334045
Pancreatitis acute 56.66 54.48 20 1954 3833 2352278
Glomerulonephritis minimal lesion 55.12 54.48 9 1965 54 2356057

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
Paradoxical drug reaction 846.08 47.91 137 2097 364 1744183
Drug-induced liver injury 832.89 47.91 181 2053 3056 1741491
Drug reaction with eosinophilia and systemic symptoms 659.60 47.91 163 2071 4907 1739640
Jaundice 655.25 47.91 168 2066 5894 1738653
Hepatotoxicity 581.49 47.91 134 2100 2950 1741597
Drug resistance 429.71 47.91 106 2128 3124 1741423
Tuberculosis 377.29 47.91 86 2148 1780 1742767
Pyrexia 359.54 47.91 181 2053 46219 1698328
Hepatitis 271.97 47.91 81 2153 4874 1739673
Hepatic failure 241.34 47.91 77 2157 5826 1738721
Tuberculoma of central nervous system 228.34 47.91 33 2201 23 1744524
Alanine aminotransferase increased 228.04 47.91 89 2145 12189 1732358
Liver function test abnormal 214.83 47.91 70 2164 5656 1738891
Immune reconstitution inflammatory syndrome 206.28 47.91 51 2183 1498 1743049
Immune system disorder 204.01 47.91 45 2189 790 1743757
Pulmonary tuberculosis 182.53 47.91 43 2191 1023 1743524
Hepatic function abnormal 173.70 47.91 63 2171 7011 1737536
Acute hepatic failure 168.66 47.91 46 2188 1997 1742550
Aspartate aminotransferase increased 164.91 47.91 68 2166 10688 1733859
Skin disorder 161.44 47.91 45 2189 2119 1742428
Vomiting 159.38 47.91 100 2134 38215 1706332
Hepatic enzyme increased 144.14 47.91 54 2180 6567 1737980
Condition aggravated 140.57 47.91 75 2159 21075 1723472
Meningitis tuberculous 131.63 47.91 22 2212 73 1744474
Nausea 119.80 47.91 94 2140 51102 1693445
Serpiginous choroiditis 119.11 47.91 16 2218 0 1744547
Rash maculo-papular 105.97 47.91 37 2197 3666 1740881
Drug interaction 101.12 47.91 67 2167 27891 1716656
Decreased appetite 100.60 47.91 63 2171 23808 1720739
Eosinophilia 99.99 47.91 35 2199 3492 1741055
Disseminated tuberculosis 98.77 47.91 23 2211 517 1744030
Metabolic acidosis 92.35 47.91 37 2197 5365 1739182
Encephalopathy 92.03 47.91 35 2199 4417 1740130
Hepatitis toxic 91.85 47.91 21 2213 434 1744113
Anaemia 90.86 47.91 64 2170 29393 1715154
Liver disorder 90.84 47.91 37 2197 5599 1738948
Blood bilirubin increased 90.72 47.91 38 2196 6172 1738375
Rash 90.16 47.91 71 2163 38622 1705925
Acute kidney injury 89.86 47.91 68 2166 34876 1709671
Hepatitis fulminant 87.39 47.91 22 2212 692 1743855
Liver injury 86.86 47.91 27 2207 1855 1742692
Transaminases increased 85.32 47.91 32 2202 3885 1740662
Hepatic encephalopathy 81.63 47.91 27 2207 2265 1742282
Lymphadenopathy 80.21 47.91 31 2203 4083 1740464
Hepatocellular injury 79.96 47.91 29 2205 3202 1741345
Neuropathy peripheral 79.18 47.91 39 2195 9214 1735333
Drug eruption 78.95 47.91 28 2206 2898 1741649
Coma 78.64 47.91 36 2198 7226 1737321
Optic neuritis 75.64 47.91 20 2214 766 1743781
Toxicity to various agents 75.47 47.91 57 2177 29084 1715463
Hydrocephalus 73.13 47.91 20 2214 872 1743675
Generalised tonic-clonic seizure 70.12 47.91 28 2206 4018 1740529
Immune reconstitution inflammatory syndrome associated tuberculosis 68.54 47.91 11 2223 26 1744521
Tubulointerstitial nephritis 67.45 47.91 25 2209 2933 1741614
Thrombocytopenia 67.34 47.91 47 2187 21202 1723345
Demodicidosis 66.55 47.91 10 2224 12 1744535
Multiple-drug resistance 66.29 47.91 15 2219 295 1744252
Pruritus 65.85 47.91 48 2186 23174 1721373
Bilirubin conjugated increased 57.32 47.91 15 2219 551 1743996
Seizure 55.09 47.91 41 2193 20400 1724147
Hepatic necrosis 53.32 47.91 15 2219 726 1743821
Peritoneal tuberculosis 51.73 47.91 10 2224 87 1744460
Rhabdomyolysis 50.96 47.91 31 2203 11059 1733488
Papule 50.90 47.91 14 2220 623 1743924
Blindness 50.69 47.91 20 2214 2776 1741771
Granuloma 48.84 47.91 13 2221 510 1744037
Tuberculous pleurisy 48.80 47.91 10 2224 120 1744427
Erythema 48.70 47.91 33 2201 14155 1730392

Pharmacologic Action:

SourceCodeDescription
ATC J04AC01 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Hydrazides
ATC J04AC51 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Hydrazides
ATC J04AM01 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM02 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM04 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM05 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM06 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM07 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
ATC J04AM08 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIMYCOBACTERIALS
DRUGS FOR TREATMENT OF TUBERCULOSIS
Combinations of drugs for treatment of tuberculosis
CHEBI has role CHEBI:88188 drug allergen
CHEBI has role CHEBI:33231 antitubercular agent
FDA EPC N0000175483 Antimycobacterial
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000963 Antimetabolites
MeSH PA D000995 Antitubercular Agents
MeSH PA D054872 Fatty Acid Synthesis Inhibitors
MeSH PA D000960 Hypolipidemic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Inactive tuberculosis indication 11999007
Acute tuberculosis indication 25629007
Pulmonary tuberculosis indication 154283005 DOID:2957
Tuberculosis of meninges off-label use 58437007
Atypical mycobacterial infection off-label use 111812000
Nutritional disorder contraindication 2492009 DOID:374
Alcoholism contraindication 7200002
Jaundice contraindication 18165001
Acute hepatitis contraindication 37871000
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Diabetes mellitus contraindication 73211009 DOID:9351
Gout contraindication 90560007 DOID:13189
Anemia due to enzyme deficiency contraindication 111577008
Acute hepatic failure contraindication 197270009
Disease of liver contraindication 235856003 DOID:409
Diabetic - poor control contraindication 268519009
Peripheral nerve disease contraindication 302226006
Porphyria contraindication 418470004
Diabetic peripheral neuropathy contraindication 424736006
Slow acetylator due to N-acetyltransferase enzyme variant contraindication 425079005
Prolonged-Severe Nausea and Vomiting contraindication
Chronic Hepatic Disease contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.98 acidic
pKa2 3.79 Basic
pKa3 1.94 Basic

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
Cytochrome P450 3A4 Enzyme IC50 5.31 WOMBAT-PK
Cytochrome P450 3A5 Enzyme IC50 4.96 WOMBAT-PK
Enoyl-[acyl-carrier-protein] reductase [NADH] Enzyme INHIBITOR WOMBAT-PK CHEMBL
Catalase-peroxidase Enzyme WOMBAT-PK
Dihydrofolate reductase Enzyme Ki 9 CHEMBL

External reference:

IDSource
D007538 MESH_DESCRIPTOR_UI
4017505 VUID
N0000145890 NUI
C0022209 UMLSCUI
D00346 KEGG_DRUG
81335000 SNOMEDCT_US
2955 MMSL
387472004 SNOMEDCT_US
4929 MMSL
d00101 MMSL
4017505 VANDF
6038 RXNORM
002844 NDDF
3767 PUBCHEM_CID
CHEBI:6030 CHEBI
CHEMBL64 ChEMBL_ID
DB00951 DRUGBANK_ID
V83O1VOZ8L UNII
4188 INN_ID
ISZ PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rifamate HUMAN PRESCRIPTION DRUG LABEL 2 0068-0509 CAPSULE 150 mg ORAL ANDA 13 sections
Rifater HUMAN PRESCRIPTION DRUG LABEL 3 0088-0576 TABLET, SUGAR COATED 50 mg ORAL NDA 14 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0185-4350 TABLET 300 mg ORAL NDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0185-4351 TABLET 100 mg ORAL NDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0440-1655 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0440-7655 TABLET 300 mg ORAL ANDA 14 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0527-1109 TABLET 300 mg ORAL ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0555-0066 TABLET 100 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0555-0071 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 0781-3056 INJECTION, SOLUTION 100 mg INTRAMUSCULAR ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 10135-584 TABLET 300 mg ORAL ANDA 14 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 10544-087 TABLET 300 mg ORAL ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 10544-121 TABLET 300 mg ORAL ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 10544-218 TABLET 300 mg ORAL ANDA 14 sections
ISONIAZID HUMAN PRESCRIPTION DRUG LABEL 1 16590-984 TABLET 300 mg ORAL ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 21695-627 TABLET 300 mg ORAL ANDA 14 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 43063-463 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 46287-009 SOLUTION 50 mg ORAL ANDA 14 sections
isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 46672-597 SYRUP 50 mg ORAL ANDA 13 sections
isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 46672-865 TABLET 100 mg ORAL ANDA 13 sections
isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 46672-866 TABLET 300 mg ORAL ANDA 13 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 50090-0370 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 50090-0410 TABLET 100 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 51079-083 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 51655-391 TABLET 300 mg ORAL ANDA 10 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 52959-145 TABLET 300 mg ORAL ANDA 14 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 53002-2920 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 53808-1041 TABLET 300 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 54868-2304 TABLET 100 mg ORAL ANDA 12 sections
Isoniazid HUMAN PRESCRIPTION DRUG LABEL 1 54868-2416 TABLET 300 mg ORAL ANDA 12 sections