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Drug

D0071 | Isoniazid

Molecular Formula C6H7N3O
Molecular Weight 137.14
Structure
State solid
Route of elimination From 50 to 70 percent of a dose of isoniazid is excreted in the urine within 24 hours.
Protein binding Very low (0-10%)
Half life Fast acetylators: 0.5 to 1.6 hours. Slow acetylators: 2 to 5 hours.
Absorption Readily absorbed following oral administration; however, may undergo significant first pass metabolism. Absorption and bioavailability are reduced when isoniazid is administered with food.
Trade names Hydra, Hyzyd, Isovit
Description antibiotic for the treatment of tuberculosis

J

J04AM08 Isoniazid, sulfamethoxazole, trimethoprim and pyridoxine


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM07 Rifampicin, ethambutol and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM06 Rifampicin, pyrazinamide, ethambutol and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM05 Rifampicin, pyrazinamide and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM04 Thioacetazone and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM03 Ethambutol and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM02 Rifampicin and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AM01 Streptomycin and isoniazid


[J04AM] Combinations of drugs for treatment of tuberculosis


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AC51 Isoniazid, combinations


[J04AC] Hydrazides


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

J04AC01 Isoniazid


[J04AC] Hydrazides


[J04A] DRUGS FOR TREATMENT OF TUBERCULOSIS


[J04] ANTIMYCOBACTERIALS


[J] Antiinfectives for systemic use

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL 504.6 µM 30 mins mouse liver mitochondria Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) decrease EC20 36
REDOX CYCLING 278
RESPIRATION 59.8 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. decrease EC20 36
RESPIRATION ND 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. Negative EC20 36
SWELLING > 800 µM 30 mins mouse liver mitochondria swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) increase EC20 36

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 59.8 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. inhibit EC20 36
Succinate dehydrogenase ND 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. Negative EC20 36
Cytochrome c > 400 µM 30 mins mouse liver mitochondria Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) release EC20 36

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 368 companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


H302 (98.37%): Harmful if swallowed [Warning Acute toxicity, oral]


H315 (92.12%): Causes skin irritation [Warning Skin corrosion/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, P302+P352, P321, P330, P332+P313, P362, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Danger

H302: Harmful if swallowed [Warning Acute toxicity, oral]


H361: Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H370: Causes damage to organs [Danger Specific target organ toxicity, single exposure]


H372: Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]


H402: Harmful to aquatic life [Hazardous to the aquatic environment, acute hazard]


H412: Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]


 P201, P202, P260, P264, P270, P273, P281, P301+P312, P307+P311, P308+P313, P314, P321, P330, P405, 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
rabbit LD50 intramuscular 155mg/kg (155mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
guinea pig LD50 oral 255mg/kg (255mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
mouse LD50 intraperitoneal 100mg/kg (100mg/kg) National Technical Information Service. Vol. AD277-689,
rabbit LD50 subcutaneous 135mg/kg (135mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
cat LD50 intraperitoneal 325mg/kg (325mg/kg) Klinische Wochenscrift. Vol. 30, Pg. 959, 1952.
mouse LD50 intravenous 149mg/kg (149mg/kg) behavioral: convulsions or effect on seizure threshold Journal of Pharmacology and Experimental Therapeutics. Vol. 122, Pg. 110, 1958.
man LDLo oral 116mg/kg (116mg/kg) Journal of Analytical Toxicology. Vol. 16, Pg. 57, 1992.
rat LD50 intravenous 365mg/kg (365mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 26, Pg. 409, 1976.
mouse LD50 oral 133mg/kg (133mg/kg) American Review of Tuberculosis. Vol. 65, Pg. 376, 1952.
man TDLo oral 430mg/kg (430mg/kg) Neurology. Vol. 20, Pg. 299, 1970.
rat LD50 oral 1250mg/kg (1250mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 26, Pg. 409, 1976.
dog LD50 oral 50mg/kg (50mg/kg) American Review of Tuberculosis. Vol. 65, Pg. 392, 1952.
rat LD50 intramuscular 400mg/kg (400mg/kg) behavioral: convulsions or effect on seizure threshold Therapie. Vol. 8, Pg. 62, 1953.
guinea pig LD50 intravenous 220mg/kg (220mg/kg) gastrointestinal: "hypermotility, diarrhea" Archiv fuer Toxikologie. Vol. 22, Pg. 80, 1966.
infant TDLo oral 91mg/kg (91mg/kg) Pediatrics. Vol. 95, Pg. 700, 1995.
women TDLo oral 12mg/kg/2D-I (12mg/kg) Neurology. Vol. 34, Pg. 703, 1984.
rabbit LD50 intraperitoneal 147mg/kg (147mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
child TDLo oral 125mg/kg (125mg/kg) Annals of Emergency Medicine. Vol. 17, Pg. 73, 1988.
rat LD50 intraperitoneal 335mg/kg (335mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
rabbit LD50 intravenous 94mg/kg (94mg/kg) behavioral: convulsions or effect on seizure threshold American Review of Tuberculosis. Vol. 65, Pg. 376, 1952.
women TDLo oral 90200ug/kg/7D (90.2mg/kg) Pediatrics. Vol. 97, Pg. 782, 1996.
guinea pig LD50 subcutaneous 195mg/kg (195mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
human LDLo oral 100mg/kg (100mg/kg) peripheral nerve and sensation: structural change in nerve or sheath American Review of Respiratory Disease. Vol. 105, Pg. 206, 1972.
mouse LD50 subcutaneous 125mg/kg (125mg/kg) behavioral: convulsions or effect on seizure threshold Yakugaku Zasshi. Journal of Pharmacy. Vol. 81, Pg. 1225, 1961.
rat LD50 subcutaneous 329mg/kg (329mg/kg) Journal of Pharmacology and Experimental Therapeutics. Vol. 119, Pg. 444, 1957.
rabbit LD50 oral 250mg/kg (250mg/kg) Arzneimittel-Forschung. Drug Research. Vol. 12, Pg. 22, 1962.
women TDLo oral 99300ug/kg (99.3mg/kg) Pediatrics. Vol. 95, Pg. 700, 1995.
rabbit LD50 intracrebral > 12mg/kg (12mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
child TDLo oral 3600mg/kg/43W (3600mg/kg) Canadian Medical Association Journal. Vol. 148, Pg. 49, 1993.
child TDLo oral 195mg/kg (195mg/kg) Japanese Journal of Toxicology. Vol. 12, Pg. 225, 1999.
guinea pig LD50 intraperitoneal 195mg/kg (195mg/kg) Klinische Wochenscrift. Vol. 30, Pg. 959, 1952.
mouse LD50 intramuscular 137mg/kg (137mg/kg) American Review of Tuberculosis. Vol. 65, Pg. 376, 1952.
man TDLo oral 100mg/kg/3W-C (100mg/kg) American Review of Respiratory Disease. Vol. 106, Pg. 849, 1972.
man LDLo oral 523mg/kg/17W- (523mg/kg) JAMA, Journal of the American Medical Association. Vol. 176, Pg. 877, 1961.
guinea pig LD50 intramuscular 255mg/kg (255mg/kg) Schweizerische Zeitschrift fuer Tuberkulose und Pneumonologie. Vol. 9, Pg. 226, 1952.
women TDLo oral 11250mg/kg (11250mg/kg) Anaesthesia. Vol. 47, Pg. 781, 1992.
man TDLo oral 39mg/kg/9D-I (39mg/kg) skin and appendages (skin): "dermatitis, other: after systemic exposure" Southern Medical Journal. Vol. 75, Pg. 81, 1982.

  • Diabetes mellitus

  • Extrapulmonary tuberculosis

  • Hodgkin's disease

  • Hodgkin's disease lymphocyte depletion type stage unspecified

  • Hodgkin's disease lymphocyte predominance type stage unspecified

  • Immunodeficiency

  • Induration

  • Infection

  • Leukaemia

  • Low income

  • Malabsorption

  • Malnutrition

  • Neoplasm malignant

  • Peptic ulcer

  • Renal failure chronic

  • Silicosis

  • Skin test positive

  • Ulcer

  • Weight decreased

    • 101033-EP2272832A1 101033-EP2272972A1 101033-EP2272973A1
    101033-EP2277872A1 101033-EP2295053A1 101033-EP2298776A1
    101033-EP2301544A1 10319-EP2272972A1 10319-EP2272973A1
    10319-EP2274983A1 10319-EP2275102A1 10319-EP2275401A1
    10319-EP2277872A1 10319-EP2280000A1 10319-EP2280012A2
    10319-EP2281563A1 10319-EP2289510A1 10319-EP2289876A1
    10319-EP2295407A1 10319-EP2295411A1 10319-EP2295416A2
    10319-EP2295433A2 10319-EP2298312A1 10319-EP2298736A1
    10319-EP2298747A1 10319-EP2298748A2 10319-EP2301536A1
    10319-EP2301538A1 10319-EP2301924A1 10319-EP2305640A2
    10319-EP2305642A2 10319-EP2305808A1 10319-EP2308852A1
    10319-EP2311455A1 10319-EP2311824A1 10319-EP2311830A1
    10319-EP2314584A1 10319-EP2316452A1 10319-EP2316459A1
    10319-EP2380872A1 4-(Hydrazinocarbonyl)pyridine 4-Pyridinecarbonylhydrazine
    4-Pyridinecarboxylic acid hydrazide 4-Pyridinecarboxylic acid, hydrazide 4-Pyridinecarboxylic hydrazide
    4-Pyridylcarbonyl hydrazide 4-Pyridylcarbonylhydrazide 4-pyridinecarbohydrazide
    4-pyridinecarbohydrazide(Isoniazid) 40687-EP2298761A1 40687-EP2311830A1
    5015 R.P 5015 R.P. 5015 RP
    54-85-3 AB00052025 AB00052025-20
    AB00052025-21 AB00052025_22 AB00052025_23
    AB00052025_24 AB00052025_25 AB1009474
    ACMC-209ljq AE-641/02310003 AI3-23936
    AK-46317 AKOS000119062 ANW-32196
    ARONIS25141 AZT + Isoniazid Abdizide
    Andrazide Anidrasona Antimicina
    Antituberkulosum Armacide Armazid
    Armazide Atcotibine Azuren
    BB 0240534 BBL008409 BCP13791
    BDBM50336507 BIDD:GT0140 BP 5015
    BPBio1_000025 BPBio1_001322 BRD-K87202646-001-26-8
    BSPBio_000021 BSPBio_002204 Bacillin
    Biomol-NT_000288 C07054 C6H7N3O
    CAS-54-85-3 CCG-39710 CCRIS 351
    CHEBI:6030 CHEMBL64 CPD000059082
    CS-2371 Cedin Cedin (Aerosol)
    Cemidon Chemiazid Chemidon
    Continazine Cortinazine Cotinazin
    Cotinizin D00346 DB00951
    DSSTox_CID_755 DSSTox_GSID_20755 DSSTox_RID_75771
    DTXSID8020755 Defonin Dibutin
    Diforin Dinacrin Ditubin
    DivK1c_000070 Dow-Isoniazid EINECS 200-214-6
    Ebidene Epitope ID:141801 Eralon
    Ertuban Eutizon Evalon
    F0391-0007 FRS-3 FSR 3
    FSR-3 FT-0627424 Fetefu
    Fimalene GINK HIA
    HMS1568B03 HMS1920H09 HMS2089I16
    HMS2091N19 HMS2095B03 HMS2234G04
    HMS3259E19 HMS3373O01 HMS3655L03
    HMS3712B03 HMS500D12 HSDB 1647
    HY-B0329 Hid rasonil Hidranizil
    Hidrasonil Hidrulta Hidrun
    Hycozid Hydra Hydrazid
    Hydrazide Hyozid Hyzyd
    I.A.I I.A.I. I0138
    IDI1_000070 INH INH
    INHd20 ISONICOTINIC ACID HYDRAZIDE(ISONIAZIDE) Ido-tebin
    Idrazide dell'acido isonicotinico Idrazide dell'acido isonicotinico [Italian] Idrazil
    In-73 InChI=1/C6H7N3O/c7-9-6(10)5-1-3-8-4-2-5/h1-4H,7H2,(H,9,10 Inah
    Inh-Burgthal Inizid Iscotin
    Isidrina Ismazide Isobicina
    Isocid Isocidene Isocotin
    Isohydrazide Isokin Isolyn
    Isonerit Isonex Isoniacid
    Isoniazid (JP17/USP/INN) Isoniazid (Tubizid) Isoniazid SA
    Isoniazid [INN:BAN:JAN] Isoniazid [USP:INN:BAN:JAN] Isoniazid daily for 9 months
    Isoniazid(Tubizid) Isoniazid, European Pharmacopoeia (EP) Reference Standard Isoniazid, Pharmaceutical??Secondary??Standard;??Certified??Reference??Material
    Isoniazid, United States Pharmacopeia (USP) Reference Standard Isoniazid, Vetec(TM) reagent grade, 98% Isoniazid, analytical standard, >=99% (TLC)
    Isoniazid, certified reference material, TraceCERT(R) Isoniazida Isoniazida [INN-Spanish]
    Isoniazide Isoniazidum Isoniazidum [INN-Latin]
    Isonicazide Isonicid Isonico
    Isonicotan Isonicotil Isonicotinhydrazid
    Isonicotinic acid hydrazide Isonicotinic acid hydrazide Isonicotinic acid hydrazide (Isoniazid)
    Isonicotinic acid hydrazide(Isoniazid) Isonicotinic acid hydrazide, 99% Isonicotinic hydrazide
    Isonicotinic hydrazide Isonicotinohydrazide Isonicotinoyl hydrazide
    Isonicotinoylhydrazine Isonicotinsaeurehydrazid Isonicotinsaeurehydrazid [German]
    Isonicotinyl hydrazide Isonicotinylhydrazide Isonicotinylhydrazine
    Isonide Isonidrin Isonikazid
    Isonilex Isonin Isonindon
    Isonirit Isoniton Isonizida
    Isonizide Isotamine Isotebe
    Isotebezid Isotinyl Isozid
    Isozide Isozyd KBio1_000070
    KBio2_001333 KBio2_003901 KBio2_006469
    KBio3_001424 KBioGR_000423 KBioSS_001333
    KS-00000JHE KS-0000471R KSC-27-048
    KUC109571N L 1945 LANIZID
    LS-205 Laniazid Laniazid (TN)
    Laniozid MCULE-6324947959 MFCD00006426
    MFCD00006426 (97%) MLS000069444 MLS001055327
    Mayambutol Mybasan NC00513
    NCGC00016244-01 NCGC00016244-02 NCGC00016244-03
    NCGC00016244-04 NCGC00016244-05 NCGC00016244-06
    NCGC00016244-07 NCGC00016244-08 NCGC00016244-09
    NCGC00016244-10 NCGC00016244-11 NCGC00016244-12
    NCGC00016244-14 NCGC00016244-15 NCGC00022648-03
    NCGC00022648-04 NCGC00022648-05 NCGC00022648-06
    NCGC00022648-07 NCGC00254094-01 NCGC00258919-01
    NINDS_000070 NIZ NSC 9659
    NSC-757078 NSC-9659 NSC757078
    NSC9659 Neo-Tizide Neoteben
    Neoxin Neumandin Nevin
    Niadrin Nicazide Nicetal
    Nicizina Niconyl Nicotibina
    Nicotibine Nicotisan Nicozide
    Nidaton Nidrazid Nikozid
    Niplen Nitadon Niteban
    Nitebannsc 9659 Nydrazid Nyscozid
    Opera_ID_454 Oprea1_396155 PS-4129
    Pelazid Percin Pharmakon1600-01500355
    Phthisen Preparation 6424 Prestwick0_000161
    Prestwick1_000161 Prestwick2_000161 Prestwick3_000161
    Prestwick_578 Pycazide Pyreazid
    Pyricidin Pyridicin Pyrizidin
    Q423169 QRXWMOHMRWLFEY-UHFFFAOYSA-N RP 5015
    RP-5015 RTR-019381 RU-EF-Tb
    RY-EF-Tb Raumanon Razide
    Retozide Rifater (Salt/Mix) Rimicid
    Rimifon Rimiphone Rimitsid
    Robiselin Robisellin Roxifen
    SAM002554904 SBB004195 SBI-0051419.P003
    SC-12623 SCHEMBL228 SCHEMBL2998929
    SMR000059082 SPBio_000094 SPBio_001942
    SPECTRUM1500355 SR-01000003025 SR-01000003025-2
    SR-01000003025-3 ST078858 ST24025094
    STK086288 STR00210 SW196752-3
    SY010614 Sanohidrazina Sauterazid
    Sauterzid Soniazid,(S) Spectrum2_000107
    Spectrum3_000472 Spectrum4_000022 Spectrum5_000876
    Spectrum_000853 Stanozide T7976
    TB-Phlogin TB-Razide TB-Vis
    TR-019381 Tebecid Tebenic
    Tebexin Tebilon Tebos
    Teebaconin Tekazin Tibazide
    Tibemid Tibiazide Tibinide
    Tibison Tibivis Tibizide
    Tibusan Tisin Tisiodrazida
    Tizide Tox21_113640 Tox21_113640_1
    Tox21_201367 Tox21_300193 Tubazid
    Tubazide Tubeco Tubecotubercid
    Tuberian Tubicon Tubilysin
    Tubizid Tubomel Tyvid
    UNII-V83O1VOZ8L UPCMLD0ENAT5791176:001 Unicocyde
    Unicozyde Usaf cb-2 V83O1VOZ8L
    Vazadrine Vederon WLN: T6NJ DVMZ
    Z58981801 ZINC1590 Zidafimia
    Zinadon Zonazide [(4-Pyridinylcarbonyl)oxy]hydrazine
    bacillen bp 5 015 component of Niadox (Salt/Mix)
    isoco tin isoniazid isoniazid (inh)
    isonicotinate hydrazide isonicotinhydrazide isonicotinic acid hydrazid
    isonicotinic acid hydrazone isonicotinicacid hydrazide isonicotinoylhydrazide
    isozid e nidra zid pyridine-4-carbohydrazide
    pyridine-4-carboxylic acid hydrazide rimif on s1937
    tebemid tubercid

    DrugBank Name Isoniazid
    DrugBank DB00951
    CAS Number 2066-89-9, 54-85-3
    PubChem Compound 3767
    KEGG Compound ID C07054
    KEGG Drug D00346
    PubChem.Substance 46506039
    ChEBI 6030
    PharmGKB PA450112
    ChemSpider 3635
    BindingDB 50336507.0
    TTD DAP000011
    Wikipedia Isoniazid
    HET NIZ
    DPD 6618

    1. Dykens et al. (2007)