基本情報
- 標準SMILES
CC(CN1c2ccccc2Sc2ccccc21)N(C)C.Cl- InChIKey
XXPDBLUZJRXNNZ-UHFFFAOYSA-N- 分子式
- C17H20N2S.ClH
- 平均分子量
- 320.9 g/mol
- 単同位体質量
- 320.11139735
概要
Promethazine hydrochloride is an odorless white to faint yellow crystalline powder. Bitter taste. A 10% solution in water has a pH of 3.5-5.0. (NTP, 1992)
名称と識別子
- 優先名称
- Promethazine Hydrochloride
- IUPAC
- N,N-dimethyl-1-phenothiazin-10-ylpropan-2-amine;hydrochloride
名称と別名
名称をさらに表示
データベース識別子
- CAS
58-33-3- PubChem CID
- 6014
- DTXSID
DTXSID3021192- ChEMBL
CHEMBL1200750- ChEBI
CHEBI:8462- UNII
- R61ZEH7I1I
- EC Number
- 200-375-2
物性
構造計算による物性
- 極性表面積
- 31.8 Ų
- 水素結合供与体数
- 1
- 水素結合受容体数
- 3
- 回転可能結合数
- 3
- 重原子数
- 21
- 形式電荷
- 0
- 複雑度
- 298
実験および物理化学的性質
Human Drugs
Breast Feeding; Lactation; Milk, Human; Antiemetics; Antipruritics; Phenothiazines
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
安全と法規制
GHS分類
GHS Classification
This chemical does not meet GHS hazard criteria for 0.7% (1 of 142) of reports.
Danger
H302 (92.3%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P264+P265, P270, P271, P272, P273, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P305+P354+P338, P317, P319, P321, P330, P332+P317, P333+P317, P337+P317, P362+P364, P391, P403+P233, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 142 reports by companies from 19 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
危険有害性情報
Health Hazards
SYMPTOMS: Symptoms of exposure to this compound include excitement, sleepiness, convulsions and rigidity. Other symptoms include leukopenia, agranulocytosis, drowsiness, confusion and stupor. Acute transitory myopia may occur. Central nervous system effects may also occur. It may cause an increase in blood pressure, mild hypotension, jaundice, extra-pyramidal reactions and photosensitivity. It may also cause dizziness, central nervous system depression, vomiting, local anesthesia, abdominal pain, diarrhea and dryness of the mouth, throat and nose. Symptoms of exposure to this type of compound include muscular weakness, tachycardia, nausea, sedation, tinnitus, lassitude, incoordination, fatigue, blurred vision, diplopia, euphoria, nervousness, insomnia, tremors, loss of appetite, epigastric distress, constipation, cough, urinary retention or frequency, dysuria, palpitation, headache, tightness of the chest, tingling, heaviness and weakness of the hands, allergic dermatitis, fever, hemolytic anemia (rare), fixed and dilated pupils, and flushing. In children, exposure can cause hallucinations, excitement, ataxia, incoordination, athetosis and convulsions.
Reactivity Profile
PROMETHAZINE HYDROCHLORIDE is sensitive to light. In aqueous solution, it is degraded by heat and light (more rapidly in air or oxygen). Incompatible with alkalis and alkaline solutions such as those of aminophylline, soluble barbiturates and phenytoin sodium. Iron(III) and copper(III) accelerate the degradation (NTP, 1992).
安全と保護具
First Aid
EYES: First check the victim for contact lenses and remove if present. Flush victim's eyes with water or normal saline solution for 20 to 30 minutes while simultaneously calling a hospital or poison control center. Do not put any ointments, oils, or medication in the victim's eyes without specific instructions from a physician. If symptoms (such as redness or irritation) develop, immediately transport the victim to a hospital.
Nonfire Spill Response
SMALL SPILLS AND LEAKAGE: If you spill this chemical, you should dampen the solid spill material with water, then transfer the dampened material to a suitable container. Use absorbent paper dampened with water to pick up any remaining material. Seal your contaminated clothing and the absorbent paper in a vapor-tight plastic bag for eventual disposal. Wash all contaminated surfaces with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned.
Personal Protective Equipment (PPE)
RECOMMENDED RESPIRATOR: Where the neat test chemical is weighed and diluted, wear a NIOSH-approved half face respirator equipped with an organic vapor/acid gas cartridge (specific for organic vapors, HCl, acid gas and SO2) with a dust/mist filter.
毒性情報
Toxicity Summary
Like other H1-antagonists, promethazine competes with free histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. The relief of nausea appears to be related to central anticholinergic actions and may implicate activity on the medullary chemoreceptor trigger zone.
Signs and Symptoms
Symptoms of overdose include mild depression of the central nervous system and cardiovascular system to profound hypotension, respiratory depression, unconsciousness, and sudden death. Other reported reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar reflexes (Babinski reflex).
Carcinogen Classification
Promethazine Hydrochloride
TR-425: Toxicology and Carcinogenesis Studies of Promethazine Hydrochloride (CASRN 58-33-3) in F344/N Rats and B6C3F1 Mice (Gavage Studies) (1993 )
12/01/92
No Evidence
No Evidence
No Evidence
Drug Induced Liver Injury
Drug Induced Liver Injury Rank (DILIrank 2.0)
Promethazine hydrochloride
vLess-DILI-concern
5
Adverse reactions
DOI:10.1016/j.drudis.2016.02.015
化学と産業
薬理情報
FDA Pharmacological Classification
PROMETHAZINE HCI
Phenothiazine [EPC]; Phenothiazines [CS]
PROMETHAZINE HCL
Phenothiazines [CS]; Phenothiazine [EPC]
PROMETHAZINE HYDROCHLORIDE
Phenothiazines [CS]; Phenothiazine [EPC]
MeSH Pharmacological Classification
Agents, usually topical, that relieve itching (pruritus).
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475)
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