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Drug

D0262 | Diazoxide

Molecular Formula C8H7ClN2O2S
Molecular Weight 230.67
Structure
State solid
Route of elimination Proglycem is extensively bound (more than 90%) to serum proteins, and is excreted in the kidneys.
Protein binding Very high (more than 90%) to serum proteins.
Half life 28 ±8.3 hours in normal adults.
Absorption Readily absorbed following oral administration.
Trade names Proglycem
Description benzothiadiazine derivative; peripheral vasodilator; treat low blood sugar

G

V

C

V03AH01 Diazoxide


[V03AH] Drugs for treatment of hypoglycemia


[V03A] ALL OTHER THERAPEUTIC PRODUCTS


[V03] ALL OTHER THERAPEUTIC PRODUCTS


[V] Various ATC structures

G01AE10 Combinations of sulfonamides


[G01AE] Sulfonamides


[G01A] ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS


[G01] GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS


[G] Genitourinary system and reproductive hormones

C02DA01 Diazoxide


[C02DA] Thiazide derivatives


[C02D] ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON


[C02] ANTIHYPERTENSIVES


[C] Cardiovascular system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
MEMBRANE POTENTIAL > 200 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
RESPIRATION 4.9 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
TRANSPORT OF POTASSIUM EC50= 40mmol/L, saturation by 100mmol/L Primary Culture of Neonatal Rat Cardiac Ventricular Myocytes flow cytometry and quantitative image analysis of cells stained with fluorescent DC indicators. affect 188
SWELLING > 200 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 4.9 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
Glycerol-3-phosphate dehydrogenase, mitochondrial inhibitor 162
Glycerol-3-phosphate dehydrogenase, mitochondrial Homogenates of isolated pancreatic islets; homogenates of whole pancreas, liver, heart, or skeletal muscle The activity of the rnitochondrial glycerol phosphate dehydrogenase was assayed with a timed assay using iodonitrotetrazolium violet as an electron acceptor and in a continuous spectrophotometric assay using dichloroindophenol as an electron acceptor. acceptor. Glycerol phosphate oxidation by islet intact mitochondria was estimated from the tritiated water released from [2- 3H]glycerol phosphate inhibitor 187
mitochondrial KATP chanel (mtKATP) EC50= 40mmol/L, saturation by 100mmol/L Primary Culture of Neonatal Rat Cardiac Ventricular Myocytes flow cytometry and quantitative image analysis of cells stained with fluorescent DC indicators. opener 188
Cytochrome c > 200 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
Danger

Aggregated GHS information provided by 88 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


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


H315 (46.59%): Causes skin irritation [Warning Skin corrosion/irritation]


H319 (46.59%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (45.45%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


H360 (51.14%): May damage fertility or the unborn child [Danger Reproductive toxicity]


H372 (39.77%): Causes damage to organs through prolonged or repeated exposure [Danger Specific target organ toxicity, repeated exposure]


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.


 P201, P202, P260, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P314, P321, P330, P332+P313, P337+P313, P362, P403+P233, 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
mouse LD50 intravenous 228mg/kg (228mg/kg) vascular: bp lowering not characterized in autonomic section Journal of Pharmacology and Experimental Therapeutics. Vol. 136, Pg. 344, 1962.
rat LD50 intraperitoneal 510mg/kg (510mg/kg) Archives Internationales de Pharmacodynamie et de Therapie. Vol. 143, Pg. 446, 1963.
mouse LD50 intraperitoneal 326mg/kg (326mg/kg) vascular: bp lowering not characterized in autonomic section Journal of Pharmacology and Experimental Therapeutics. Vol. 136, Pg. 344, 1962.
rat LD50 oral 980mg/kg (980mg/kg) Archives Internationales de Pharmacodynamie et de Therapie. Vol. 143, Pg. 446, 1963.
mouse LD50 oral 444mg/kg (444mg/kg) vascular: bp lowering not characterized in autonomic section Journal of Pharmacology and Experimental Therapeutics. Vol. 136, Pg. 344, 1962.

  • Adenoma benign

  • Blood insulin increased

  • Blood pressure increased

  • Cardiac failure congestive

  • Cerebral haemorrhage

  • Diabetes mellitus

  • Haemoglobin

  • Haemorrhage

  • Hyperinsulinism

  • Hyperplasia

  • Hypertensive crisis

  • Hypertensive encephalopathy

  • Hypoglycaemia

  • Hypotension

  • Malignant hypertension

  • Nephritis

  • Renal failure

  • Renal impairment

  • Vascular resistance systemic

    • 2270-EP2281815A1 2270-EP2295550A2 2270-EP2301933A1
    2270-EP2308838A1 2270-EP2311827A1 2H-1,2, 4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide
    2H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide 2H-1,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide 3-methyl-7-chloro-1,2,4-benzothiadiazine 1,1-dioxide
    32273-EP2281815A1 32273-EP2298415A1 32273-EP2301933A1
    32273-EP2305640A2 32273-EP2311827A1 364-98-7
    364D987 4H-1,2,4-Benzothiadiazine, 7-chloro-3-methyl-, 1,1-dioxide 7-Chloro-3-methyl-1lambda~4~,2,4-benzothiadiazin-1-ol 1-oxide
    7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine1,1-dioxide 7-Chloro-3-methyl-2H-1,4-benzothiadiazine 1,1-dioxide
    7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido 7-Cloro-3-metil-2H-1,2,4-benzotiodiazina-1,1-diossido [Italian] 7-chloranyl-3-methyl-4H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide
    7-chloro-3-methyl-1,2,4-benzothiadiazine,1,1-dioxide 7-chloro-3-methyl-2H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide 7-chloro-3-methyl-2H-1?^{6},2,4-benzothiadiazine 1,1-dioxide
    7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine 1,1-dioxide 7-chloro-3-methyl-4H-1$l^{6},2,4-benzothiadiazine-1,1-dione 7-chloro-3-methyl-4H-1|E?,2,4-benzothiadiazine-1,1-dione
    7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide 7-chloro-3-methyl-4h-1,2,4-benzothiadiazine 1,1-dioxide A823275
    ACM364987 ACN-054388 AKOS015896340
    AKOS024458715 AOB5782 Aroglycem
    B6526 BCP26107 BDBM50237612
    BDBM86248 BG0437 BPBio1_000016
    BRD-K73109821-001-05-2 BRD-K73109821-001-10-2 BSPBio_000014
    BSPBio_001307 BSPBio_002290 Bio1_000036
    Bio1_000525 Bio1_001014 Bio2_000027
    Bio2_000507 C-13401 C06949
    C8H7ClN2O2S CAS-364-98-7 CAS_364-98-7
    CBiol_001750 CC-26456 CCG-101062
    CCG-204497 CHEBI:4495 CHEMBL1518123
    CHEMBL181 CPD000058392 CS-4745
    D 9035 D00294 D5402
    DB-048966 DB01119 DSSTox_CID_2914
    DSSTox_GSID_22914 DSSTox_RID_76786 DTXSID7022914
    Diazossido Diazossido [DCIT] Diazossido [Italian]
    Diazoxide (JAN/USP/INN) Diazoxide [USAN:INN:BAN] Diazoxide [USAN:USP:INN:BAN:JAN]
    Diazoxide, European Pharmacopoeia (EP) Reference Standard Diazoxide, United States Pharmacopeia (USP) Reference Standard Diazoxido
    Diazoxido [INN-Spanish] Diazoxidum Diazoxidum [INN-Latin]
    Dizoxide EINECS 206-668-1 EN300-122611
    EU-0100404 Eudemine Eudemine injection
    Eudimine FCH1327708 FT-0603087
    GDLBFKVLRPITMI-UHFFFAOYSA-N GTPL2409 HMS1361B09
    HMS1568A16 HMS1791B09 HMS1922L22
    HMS1989B09 HMS2051P20 HMS2089L04
    HMS2093N12 HMS2095A16 HMS2234B23
    HMS3261A10 HMS3267I11 HMS3371L13
    HMS3393P20 HMS3402B09 HMS3411L18
    HMS3675L18 HMS3712A16 HY-B1140
    Hyperstat Hyperstat (TN) Hypertonalum
    IDI1_033777 KBio2_000027 KBio2_002595
    KBio2_005163 KBio3_000053 KBio3_000054
    KBio3_001510 KBioGR_000027 KBioGR_001776
    KBioSS_000027 KC-115 KS-000010A1
    KS-1444 LP00404 LS-40410
    Lopac-D-9035 Lopac0_000404 MCULE-5031397425
    MFCD00078578 MLS000028459 MLS001076071
    MLS001424164 Mutabase NC00312
    NCGC00015380-01 NCGC00015380-02 NCGC00015380-03
    NCGC00015380-04 NCGC00015380-05 NCGC00015380-06
    NCGC00015380-07 NCGC00015380-08 NCGC00015380-09
    NCGC00015380-10 NCGC00015380-11 NCGC00015380-12
    NCGC00015380-13 NCGC00022882-03 NCGC00024907-01
    NCGC00024907-02 NCGC00024907-03 NCGC00024907-04
    NCGC00024907-05 NCGC00024907-06 NCGC00024907-07
    NCGC00024907-08 NCGC00261089-01 NSC 64198
    NSC 76130 NSC-64198 NSC-759574
    NSC-76130 NSC64198 NSC759574
    NSC76130 NSC_3019 O5CB12L4FN
    Opera_ID_608 Pharmakon1600-02300206 Prestwick0_000087
    Prestwick1_000087 Prestwick2_000087 Prestwick3_000087
    Prestwick_163 Proglicem Proglycem
    Q420009 SAM001246872 SC-83321
    SCHEMBL41254 SMR000058392 SPBio_001953
    SPECTRUM2300206 SR-01000075314 SR-01000075314-1
    SR-01000075314-3 SR-01000075314-4 SR-01000075314-6
    SRG 95213 SRG-95213 Sch 6783
    Sch-6783 Spectrum3_000735 Spectrum4_001248
    Tocris-0964 Tox21_110132 Tox21_110132_1
    Tox21_500404 UNII-O5CB12L4FN VU0239714-6
    Z3125 ZINC3872277 diazoxide
    s4630

    DrugBank Name Diazoxide
    DrugBank DB01119
    CAS Number 1098065-76-9, 1329613-88-8, 1432063-51-8, 364-98-7
    PubChem Compound 3019
    KEGG Compound ID C06949
    KEGG Drug D00294
    PubChem.Substance 46508027
    ChEBI 4495
    PharmGKB PA449285
    ChemSpider 2911
    BindingDB 86248.0
    TTD DAP000956
    Wikipedia Diazoxide
    HET 20J
    DPD 9557