Promethazine Hydrochloride Powder CAS 58-33-3

Promethazine hydrochloride powder, chemical formula C17H21ClN2S, CAS 58-33-3, molecular weight 320.88g/mol. It is a white or grayish white powder or granular substance, almost odorless, with a bitter taste. There is also a certain degree of instability under light, oxidation, or thermal conditions, which gradually turns blue when left in air for a long time. This is due to its oxidation in the air. It can undergo various chemical reactions with other compounds, such as diazotization reactions, substitution reactions, etc. It is highly soluble in water and also soluble in ethanol (96%) and dichloromethane. This good solubility allows for easy mixing with other substances in the pharmaceutical industry to produce various formulations. In addition, its solubility also provides convenience for its use in chemical experiments and industrial production. It also has certain application value in the field of scientific research. Due to its ability to block H1 receptors in tissues such as smooth muscle and capillary walls, it can be used to study the mechanism of action of histamine in living organisms. In addition, it can also be used as an experimental tool to study the metabolic process and pharmacodynamics of drugs in living organisms.

Promethazine hydrochloride powder is a commonly used diphenhydramine antihistamine drug, which is widely used in the fields of medical treatment, health care and agriculture. It has various pharmacological effects such as sedative, anti-allergic, anti-emetic and antipyretic. Each use of Promethazine hydrochloride will be introduced in detail.

1. Antihistamine effect:

 

Promethazine hydrochloride is an H1 receptor antagonist that inhibits histamine release and activation of histamine receptors. In the body, histamine is mainly released by macrophages and mast cells, causing allergic reactions. Promethazine hydrochloride prevents histamine from binding to its receptors, reducing the occurrence of histamine-related symptoms, such as nasal congestion, runny nose, itchy skin, and hives.

2. Sedative and sleeping effects:

 

Promethazine hydrochloride has sedative and hypnotic effects and can be used as a sedative or hypnotizer. It works by interfering with signaling between neurons in the central nervous system (CNS), inhibiting activity and thus achieving sedative and relaxing effects. At the same time, Promethazine hydrochloride can also improve sleep quality, shorten the time to fall asleep, reduce nighttime waking and increase sleep time.

3. Anti-nausea and vomiting effect:

 

Promethazine hydrochloride can also inhibit dopamine receptors, histamine receptors and acetylcholine receptors in the central nervous system (CNS) and intestines, thereby reducing the occurrence of nausea and vomiting. Its anti-emetic effect is mainly regulated by affecting the chemoreceptor trigger area and the motility function of the digestive tract, so that nausea and vomiting can be effectively controlled. Therefore, Promethazine hydrochloride is often used in the treatment of nausea and vomiting symptoms before surgery and during radiation therapy.

4. Antipyretic and analgesic effects:

 

Promethazine hydrochloride can prevent the synthesis and release of PGE2 and other inflammatory mediators, thereby relieving fever and pain symptoms. The drug can effectively relieve mild to moderate pain, such as headache, toothache, joint pain, menstrual pain, etc., and can also be used for antipyretic treatment of fever.

5. Respiratory system drugs:

 

Promethazine hydrochloride can also be used in the treatment of chronic obstructive airway disease (COPD), bronchitis, asthma and other respiratory diseases. It has anti-inflammatory and bronchodilatory properties, which can reduce dyspnea, bronchospasm, and other symptoms related to the respiratory system.

6. As an oxytocin accelerator:

 

In recent years, some studies have shown that Promethazine hydrochloride can promote uterine contraction and fetal descent during pregnancy, and has the effect of oxytocin accelerator. It can inhibit the activity of the sympathetic nervous system, thereby reducing changes in physiological indicators such as heart rate and blood pressure, and ensuring the safety of the mother and fetus. However, Promethazine hydrochloride is limited to use only under the supervision of a physician.

In conclusion, Promethazine Hydrochloride Powder is a multifunctional drug widely used in clinical, health care and agricultural fields. Although the drug has many therapeutic effects, it also has certain side effects and contraindications, and should be used reasonably under the guidance of a doctor.

Promethazine Hydrochloride Powder is a diphenhydramine-type antihistamine drug with various pharmacological effects such as sedative, antiallergic, antiemetic and antipyretic. It is widely used in fields such as medical treatment, health care and agriculture. In order to meet the needs of Promethazine hydrochloride in different fields, it is necessary to develop a variety of synthetic methods.

1. Mannich reaction method:

The Mannich reaction method is a commonly used synthesis method of Promethazine hydrochloride. It replaces acetophenone as the starting material, and undergoes steps such as Mannich reaction, Schiff alkalization reaction, and oxidative cracking to finally obtain the Promethazine hydrochloride product.

The Mannich reaction is to react a carbonyl compound, an amine and an active methyl compound under certain conditions to generate a compound containing an N-Mannich carbon amine bond. In the Mannich reaction, acetophenone, formaldehyde, and isopropylamine react to form N-isopropyl-N-phenylacetylformamide (IPAF).

The Schiff alkalization reaction is to react IPAF and aniline under certain conditions to generate N-isopropyl-N-phenylacetylaniline (IPAA). Finally, IPAA undergoes an oxidative cleavage reaction to generate Promethazine hydrochloride.

The method has the advantages of easy availability of reaction raw materials, fewer synthesis steps, mild reaction conditions and high yield, and is suitable for large-scale industrial production. However, the products generated in the Mannich reaction process need to be separated and purified, and the operation is cumbersome. At the same time, IPAF is prone to moisture and has poor stability, which will affect the yield and quality.

2. Catechol oxidation method:

Catechol oxidation method is a commonly used synthesis method of Promethazine hydrochloride. It uses catechol to catalyze the oxidation of phenethylamine as a starting material, and under the action of an oxidizing agent, α-ethyl-o-quinone pyridine (α -ethyl-1,2-benzanthraquinone imine, EBQI), and then through alkali imitation reduction, acidification and other steps to finally obtain the Promethazine hydrochloride product.

In the catechol oxidation method, phenethylamine reacts with catechol to generate α-phenyl-o-quinone pyridine, and then the reaction temperature and time are controlled by the action of an oxidant to obtain EBQI.

EBQI undergoes alkali imitation reduction reaction to generate N-ethyl-o-phenylium phenethylamine (N-ethylbenzamidine, NEBA). Subsequent acidic addition produces Promethazine hydrochloride.

3. Urea method:

The urea method is a synthetic method of Promethazine hydrochloride first reported by Russian scientist Valery Nemykin in the 1950s. It uses aniline and dimethyl carbonate as raw materials, undergoes steps such as urea condensation reaction, epoxy compound cracking, hydrochloric acid acidification, etc., to finally obtain the Promethazine hydrochloride product.

In the urea method, under the joint action of urea and sodium hydroxide, aniline and dimethyl carbonate undergo condensation reaction under reflux conditions to generate N-phenyl-N'-(2-methylcarboethoxy )-urea (N-phenyl-N'-(2-methylcarbonylethoxy)urea, PMEU).

PMEU undergoes cleavage reaction of epoxy compounds to generate N-(2-methylcarbonylethoxy)-N-phenyl-1,2-dihydropyridine (N-(2-methylcarbonylethoxy)-N-phenyl-1 ,2-dihydroxy-1,2-dihydroquinoline, PMQ), followed by acid addition reaction to generate Promethazine hydrochloride.

This method has the advantages of easy-to-obtain raw materials, simple operation, and high yield, but due to the use of toxic dimethyl carbonate, safety protection needs to be paid attention to; at the same time, the synthesis of some intermediate PMQ is relatively difficult, which will affect the yield of Promethazine Hydrochloride Powder and quality.

Promethazine Hydrochloride Powder (promethazine hydrochloride) is a commonly used diphenhydramine antihistamine drug, which is widely used in the fields of medical treatment, health care and agriculture. The drug has multiple pharmacological effects such as sedative, anti-allergic, anti-emetic and antipyretic. Although Promethazine hydrochloride is widely used in clinical treatment, it still has some side effects and potential safety risks. For this reason, this article will discuss the safety of Promethazine hydrochloride in detail.

Safety Risks and Contraindications

In addition to side effects, Promethazine hydrochloride has other potential safety risks and contraindications.

(1) drug dependence

Promethazine Hydrochloride Powder can cause dependence, which means that patients need to continue using the drug to stay on track. Also, overuse of this drug may cause withdrawal syndrome.

(2) Depression of the central nervous system

Promethazine hydrochloride has some depressant effects on the central nervous system (CNS), especially when used in high doses. Therefore, individuals should pay attention to work that requires attention, such as driving and operating machinery, when using Promethazine hydrochloride.

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