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Home > Products >  Haloperidol

Haloperidol CAS NO.52-86-8

  • Min.Order: 1 Metric Ton
  • Payment Terms: T/T,
  • Product Details

Keywords

  • Haloperidol
  • 52-86-8

Quick Details

  • ProName: Haloperidol
  • CasNo: 52-86-8
  • Appearance: white powder
  • DeliveryTime: 3 days after payment
  • PackAge: 25kg/plastic drum,200Kg/iron drum
  • Port: Shanghai, Shenzhen, Guangzhou, Hongkon...
  • ProductionCapacity: 1 Metric Ton/Day
  • Purity: 99%
  • Storage: Keep in cool and dry place, away from ...
  • LimitNum: 1 Metric Ton
  • Related Substances: <0.1%
  • Residue on Ignition: <0.1%
  • Heavy Metal: <0.002%
  • Valid Period: 2 years

Superiority

 

  • 【Density】
  • 1.3 g/cm3 (20 C)
  • 【Melting Point】
  • 152 °C
  • 【Boiling Point】
  • 529
  • 【Flash Point】
  • 274
  • 【Solubilities】
  • 14 mg/L
  • 【Color/Form】
  • white
  • 【Stability】
  • Stable at normal temperature and pressure.
  • 【Storage temp】
  • Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.
  • 【Spectral properties】
  • UV max (9:1 0.1M HCl:methanol): 247,221 nm (Epsilon: 13300, 15000)
    Intense mass spectral peaks: 123 m/z, 189 m/z, 224 m/z, 237 m/z, 375 m/z
    MASS: 42411 (NIST/EPA/MSDC Mass Spectral Database, 1990 Version)
    UV: 2315 (Absorption Spectra in the UV and Visible Region, Academic Press, NY)
  • 【Computed Properties】
  • Molecular Weight:375.864223 [g/mol]
    Molecular Formula:C21H23ClFNO2
    XLogP3:3.2
    H-Bond Donor:1
    H-Bond Acceptor:4
    Rotatable Bond Count:6
    Tautomer Count:2
    Exact Mass:375.140135
    MonoIsotopic Mass:375.140135
    Topological Polar Surface Area:40.5
    Heavy Atom Count:26
    Formal Charge:0
    Complexity:451
    Isotope Atom Count:0
    Defined Atom Stereocenter Count:0
    Undefined Atom Stereocenter Count:0
    Defined Bond Stereocenter Count:0
    Undefined Bond Stereocenter Count:0
    Covalently-Bonded Unit Count:1
    Feature 3D Acceptor Count:2
    Feature 3D Donor Count:1
    Feature 3D Cation Count:1
    Feature 3D Ring Count:3
    Effective Rotor Count:7.2
    Conformer Sampling RMSD:0.8
    CID Conformer Count:487

Safety and Handling

  • 【Hazard Codes】
  • T:Toxic;
  • 【Risk Statements】
  • R60;R61;R25;R36/37/38;R43
  • 【Safety Statements 】
  • S53;S26;S36/37/39;S45
  • 【HazardClass】
  • 6.1(b)
  • 【PackingGroup 】
  • III
  • 【Transport】
  • UN 2811
  • 【Formulations/Preparations】
  • Oral tablet - 0.5, 1, 2, 5, 10, 20 mg, Haldol (scored), (Ortho-McNeil)
    Haloperidol Decanoate: Parenteral: Injection for IM use only: 50, 100 mg (haloperidol) per mL, Haldol Decanoate (with benzyl alcohol 1.2% in sesame oil), (Ortho-McNeil), also promoted by Scios Nova), Haloperidol Decanoate Injection (with benzyl alcohol 1.2% in sesame oil), (American Pharmaceutical Partners, Apotex, Bedford, GensiaSicor). /Haloperidol decanoate/
    Haloperidol Lactate: Oral solution: 2 mg (haloperidol) per mL, Haldol Concentrate (with methylparaben), (Ortho-McNeil), Haloperidol Intensol (with parabens and propylene glycol), (Roxane). Parenteral injection: 5 mg (haloperidol) per mL, Haldol (with parabens), (Ortho-McNeil). /Haloperidol lactate/
  • 【Exposure Standards and Regulations】
  • The Approved Drug Products with Therapeutic Equivalence Evaluations List identifies currently marketed prescription drug products, incl haloperidol, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act.
  • 【Octanol/Water Partition Coefficient】
  • log Kow = 4.30
  • 【Disposal Methods】
  • SRP: The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

 

Details

 

Biomedical Effects and Toxicity

  • 【Biological Activity】
  • Dopamine antagonist with selectivity for D 2 -like receptors (K i values are 1.2, ~ 7, 2.3, ~ 80 and ~ 100 nM for D 2 , D 3 , D 4 , D 1 and D 5 receptors respectively). Subtype-selective NMDA antagonist.
  • 【Pharmacological Action】
  • - Drugs used in the treatment of movement disorders. Most of these act centrally on dopaminergic or cholinergic systems. Among the most important clinically are those used for the treatment of Parkinson disease (ANTIPARKINSON AGENTS) and those for the tardive dyskinesias.
    - Drugs used to prevent NAUSEA or VOMITING.
    - Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.
    - Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
  • 【Therapeutic Uses】
  • Anti-Dyskinesia Agents; Antiemetics; Antipsychotic Agents, Butyrophenone; Dopamine Antagonists
    Haloperidol is indicated for the management of the manifestations of acute and chronic psychotic disorders including schizophrenia, manic states, and drug-induced psychoses, such as steroid psychosis. It may also be useful in the management of aggressive and agitated patients, including patients with organic mental syndrome or mental retardation. Haloperidol decanoate, a long-acting parenteral from, is intended for maintenance use in the management of patients requiring prolonged parenteral therapy, as in chronic schizophrenia. /Included in US product labeling/
    Haloperidol is effective in the treatment of children with severe behavior problems of apparently unprovoked, combative, explosive hyperexcitability. It is also effective in the short-term treatment of hyperactivity in children who show excessive motor activity with accompanying conduct disorders such as aggressiveness, impulsiveness, easy frustration, short attention span, and/or rapid mood fluctuations. In these two groups of children, haloperidol should be tried only in patients who fail to respond to psychotherapy or other non-neuroleptic medication. /Included in US product labeling/
    Haloperidol is used to control tics and vocalizations of Tourette's syndrome in children and adults. /Included in US product labeling/
    Haloperidol has been used to reduce abnormal behaviors, such as withdrawal, stereotypy, abnormal abject relationships, fidgetiness, hyperactivity, negativism, angry affect, and labile affect, and may improve learning, in some patients with autism. /NOT included in US product labeling/
    Because of its strong extrapyramidal effects, haloperidol is used to reduce disabling choreiform movements in Huntington's disease. /NOT included in US product labeling/
    Haloperidol is used as a second-line agent to control nausea and vomiting associated with antineoplastic therapy and surgery. /NOT included in US product labeling/
    Three severely agitated patients in ICU did not respond to conventional therapy with opiates, benzodiazepines, and intermittent intravenous doses of haloperidol. In each case, control was achieved rapidly after initiation and titration of a continuous haloperidol infusion. Two patients had a history of schizophrenia. No adverse effects attributable to therapy were identified. Haloperidol is often used in the ICU for control of severe agitation, even in patients without a psychiatric history. It usually is given by bolus intravenous injection, sometimes in high doses (> 5 mg), even though that is not approved by the Food and Drug Administration. Intravenous haloperidol is generally well tolerated, but multiform ventricular tachycardia has been reported. Experience with continuous haloperidol infusions is growing, and it appears to be an effective method for control of severe agitation or delirium. In our experience and in other limited published data, adverse effects are rare, but prolongation of the QT interval has occurred and multiform ventricular tachycardia is likely a risk. In selected patients, a continuous infusion of haloperidol may be a useful alternative for control of agitation and delirium. Close monitoring for QT prolongation or rhythm disturbances is mandatory. [Seneff MG, Mathews RA; Ann Pharmacother 29 (7-8): 690-3 (1995)]
  • 【Biomedical Effects and Toxicity】
  • Haloperidol is well absorbed from the gastrointestinal tract but first-pass hepatic metabolism decreases oral bioavailability to 40 to 75%. Serum concentration peaks 0.5 to 4 hours after an oral dose.
    The apparent volume of distribution is about 20 L/kg, consistent with the high lipophilicity of the drug. Haloperidol circulates in blood bound predominantly (90-94%) to plasma proteins.
    Following administration of haloperidol in animals, the drug is distributed mainly into the liver, with lower concentrations being distributed into the brain, lung, kidneys, spleen, and heart. ... Haloperidol is about 92% bound to plasma proteins.

Environmental Fate and Exposure Potential

  • 【Environmental Fate/Exposure Summary】
  • TERRESTRIAL FATE: Based on a classification scheme(1), an estimated Koc value of 5,200(SRC), determined from a log Kow of 4.30(2) and a regression-derived equation(3), indicates that haloperidol is expected to be immobile in soil(SRC). Volatilization of haloperidol from moist soil surfaces is not expected to be an important fate process(SRC) given an estimated Henry's Law constant of 2.3X10-14 atm-cu m/mole(SRC), using a fragment constant estimation method(4). Haloperidol is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 4.8X10-11 mm Hg(SRC), determined from a fragment constant method(5).
    AQUATIC FATE: Based on a classification scheme(1), an estimated Koc value of 5,200(SRC), determined from a log Kow of 4.3(2) and a regression-derived equation(3), indicates that haloperidol is expected to adsorb to suspended solids and sediment(SRC). Volatilization from water surfaces is not expected(3) based upon an estimated Henry's Law constant of 2.3X10-14 atm-cu m/mole(SRC), developed using a fragment constant estimation method(4). The pKa of haloperidol is 8.66(5), indicating that this compound will exist primarily in the protonated form in the environment and cations generally adsorb more strongly to organic carbon and clay than their neutral counterparts(6). According to a classification scheme(7), an estimated BCF of 59(SRC), from its log Kow(2) and a regression-derived equation(8), suggests the potential for bioconcentration in aquatic organisms is moderate(SRC).
    ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), haloperidol, which has estimated vapor pressure of 4.8X10-11 mm Hg at 25 deg C(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase haloperidol may be removed from the air by wet and dry deposition(SRC).

 

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