Promethazine Hydrochloride

HCID 6014CAS 58-33-3

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

PROMETHAZINE HYDROCHLORIDE58-33-3Promethazine HclRemsedPromethaconPrometheganDiprasineFellozineGanphenPlletiaPrometh FortisPrometh Plain
名称をさらに表示
Mymethazine FortisAnergan 25KinetosinPromantinePhencenPrimineDormePromethazine chloride

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

実験および物理化学的性質

Solubilitygreater than or equal to 100 mg/mL at 72 °F (NTP, 1992)
Human Drugs · 3 件

Breast Feeding; Lactation; Milk, Human; Antiemetics; Antipruritics; Phenothiazines

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Melting Point446 to 450 °F (decomposes) (NTP, 1992)
Physical DescriptionPromethazine 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)
Collision Cross Section162.7 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

安全と法規制

GHS分類

GHS Classification · 5 件

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

Regulatory Information10H-Phenothiazine-10-ethanamine, N,N,.alpha.-trimethyl-, monohydrochloride: Does not have an individual approval but may be used under an appropriate group standard
Other Safety InformationIMAP assessments - 10H-Phenothiazine-10-ethanamine, N,N,.alpha.-trimethyl-, monohydrochloride: Environment tier I assessment
Fire HazardsFlash point data for this chemical are not available; however, it is probably combustible. (NTP, 1992)
Health Hazards · 1 件

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.

Reactive GroupAmines, Phosphines, and Pyridines
Reactivity Profile · 1 件

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

Fire FightingFires involving this material can be controlled with a dry chemical, carbon dioxide or Halon extinguisher. (NTP, 1992)
First Aid · 1 件

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 · 1 件

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) · 1 件

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

Exposure RoutesOn average, 88% of a promethazine dose is absorbed after oral administration; however, the absolute bioavailability is only 25% because of first-pass clearance.
Toxicity Summary · 1 件

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 · 1 件

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 · 6 件

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 · 6 件

Drug Induced Liver Injury Rank (DILIrank 2.0)

Promethazine hydrochloride

vLess-DILI-concern

5

Adverse reactions

DOI:10.1016/j.drudis.2016.02.015

Effects During Pregnancy and Lactation◉ Summary of Use during Lactation

化学と産業

薬理情報

Metabolism/MetabolitesHepatic Route of Elimination: Promethazine hydrochloride is metabolized in the liver, with the sulfoxides of promethazine and N-desmethylpromethazine being the predominant metabolites appearing in the urine. Half Life: 16-19 hours
FDA Pharmacological Classification · 6 件

PROMETHAZINE HCI

Phenothiazine [EPC]; Phenothiazines [CS]

PROMETHAZINE HCL

Phenothiazines [CS]; Phenothiazine [EPC]

PROMETHAZINE HYDROCHLORIDE

Phenothiazines [CS]; Phenothiazine [EPC]

MeSH Pharmacological Classification · 3 件

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)

用途と製造

UsesFor the treatment of allergic disorders, and nausea/vomiting.
General Manufacturing Information10H-Phenothiazine-10-ethanamine, N,N,.alpha.-trimethyl-, hydrochloride (1:1): INACTIVE

関連反応

2 件

関連ノート

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