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CAS NO.25332-39-2
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C19H23Cl2N5O |
| Molar Mass | 408.32 |
| Melting Point | 223-226 C |
| Boling Point | 528.5°C at 760 mmHg |
| Flash Point | 9℃ |
| Water Solubility | Soluble at 25mg/ml in methanol. Also soluble in 0.1M HCl or DMSO. Insoluble in water/n |
| Solubility | DMSO 1 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Vapor Presure | 2.94E-11mmHg at 25°C |
| Appearance | powder |
| Color | off-white |
| PH | pH (10g/l, 25℃) : 3.9～4.5 |
| Storage Condition | 2-8°C |
| MDL | MFCD00079603 |
| Use | Used as an antidepressant |
| antidepressants | trazodone hydrochloride is a triazolopyridine antidepressant, it is mainly used for the treatment of various types of depression and anxiety disorders accompanied by depressive symptoms, as well as mood disorders after withdrawal of drug addicts. This product is a phenylpiperazine propyl derivative which is chemically unrelated to tricyclic or tetracyclic antidepressants. It has no monoamine oxidase inhibition or amphetamine-like characteristics, and almost no anticholinergic effect. The exact mechanism of its antidepressant for the human body has not been fully elucidated, but it is generally believed that in the therapeutic dose, its antidepressant pharmacological effect is selective inhibition of 5-hydroxytryptamine (5-HT) reabsorption, and may have a weak role in preventing norepinephrine reabsorption, but has no effect on dopamine, histamine and acetylcholine, and does not inhibit the activity of monoamine oxidase (MAO) in the brain. Trazodone hydrochloride also potentiates behavioral changes induced by serotonin, the precursor of 5-HT, and its antidepressant effect is similar to that of tricyclic and monoamine oxidase inhibitors (MAOI), but the cardiovascular system toxicity is small, more suitable for elderly or patients with cardiovascular disease. It is well absorbed after oral administration, and the peak of plasma concentration occurs about 1 hour after taking it on an empty stomach and 2 hours after taking it with food. Elimination of trazodone hydrochloride in two phases, consisting of an initial phase (T1/2 for 6h) and a subsequent slow phase (T1/2 for 5-9 h), because the clearance of trazodone hydrochloride in the body varies greatly, some patients may accumulate in the plasma after taking it. This product also has a central sedative effect and a slight muscle relaxation effect, but no anti-spasm and central excitement. This product can cause blood pressure drop, years of clinical experience, the cardiac toxicity is a growing concern, the role of dose-related. |
| pharmacokinetics | trazodone hydrochloride is well absorbed after oral administration in humans and is not selectively and centrally distributed to any tissue, the plasma protein binding rate was 85% ~ 95%. When this product is taken immediately after a meal, food may increase the absorption of the drug, reduce the maximum blood concentration and extend the time to reach the highest concentration. When taken orally on an empty stomach, the maximum blood concentration is achieved over approximately one hour, whereas it takes approximately two hours to take it with or after a meal. Trazodone hydrochloride is mainly extensively metabolized by microsomal enzymes of the liver. Both the product and its metabolites easily penetrate the blood-cerebrospinal fluid barrier, but a very small amount passes through the placental barrier, and the metabolites are finally excreted by the kidney. The excretion of this product is divided into two stages, including the initial phase (half-life of 3 to 6 hours) and the second phase (Half-Life of 5 to 9 hours), and is not affected by food. Because the goods in vivo clearance rate of individual differences, so for some patients trazodone hydrochloride may be accumulated in the plasma. This product can be excreted through the milk. |
| trazodone | trazodone is a triazopyridine antidepressant that acts similarly to tricyclics and MAOI, clinical can be used for the treatment of depression, refractory depression patients by other antidepressants ineffective treatment, with this product is often effective. Can also be used for the treatment of anxiety, more suitable for the treatment of senile depression or associated with heart disease patients. The mechanism of action is to selectively block the reuptake of 5-HT and weakly prevent the reuptake of norepinephrine, but has no effect on dopamine, histamine and acetylcholine, also does not inhibit the activity of MAO in the brain, less toxic to the cardiovascular system, more suitable for elderly or associated with cardiovascular disease in patients with depression. This product also has a central sedative, mild muscle relaxation, but no anti-spasm and central excitation. No effect on the heart, but can cause a drop in blood pressure and dose-related. It is well absorbed after oral administration, and the peak of plasma concentration occurs about 1 hour after taking trazodone hydrochloride on an empty stomach, and 2 hours after taking the same food. After absorption, it is distributed in the liver and kidney, metabolized by the liver, and the metabolites still have obvious activity. Easily passes the blood-cerebrospinal fluid barrier, but rarely passes the placental barrier. The metabolites are finally excreted by the kidneys. Rarely excreted in the original form. Renal impairment also does not affect its excretion. t1/2 is 4.1h. Elimination of trazodone hydrochloride in two phases, consisting of an initial phase (T1/2 for 6h) and a subsequent slow phase (T1/2 for 5-9H), because the clearance of trazodone hydrochloride in the body varies greatly, some patients may accumulate in the plasma after taking it. |
| Toxicology | (1) Acute toxicity The dose of trazodone hydrochloride LD50 in mice was 610mg/kg, the rats were 8.6 mg/kg and the rabbits were 560mg/kg. Lethal dose can cause animals Dyspnea, salivation, collapse, spasm and other symptoms. (2) Long-term toxicity dog oral dose 10mg/(kg). d)~ 30mg/(kg.d) and monkeys oral dose 20~80mg/(kg.d) the one-year study showed no organ toxicity caused by trazodone hydrochloride, but some female dogs in the high dose group experienced convulsions and death. (3) reproductive toxicity in rats and rabbits in the second trimester oral administration of 15~450mg/(kg). d), except at 450mg/(kg.d) No teratogenic effect was found in the presence of stillbirth; 10-300mg/kg was administered before and after mating in male and female rats. Human), female rats in pregnancy and lactation to continue administration, in addition to the high dose group in the delivery of the baby slightly light body weight, fertility, mating ability, pregnancy and postpartum no side effects; rats were administered 10-300mg/(kg) during the last 6-7 days of pregnancy and throughout the lactation period. d), as a result, it was found that there were no adverse effects on pregnancy, survival of pups and feeding of pups by mothers, except that the pups at the time of delivery and at the age of 21 days were slightly lighter. (4) carcinogenicity A test in which a daily dose of 300mg/Kg was orally administered to rats for 18 months showed no carcinogenicity. |
| dosage | the dose should be started from the low dose, gradually increasing the dose and observing the treatment response. When lethargy occurs, most of the daily dose should be assigned to bedtime or reduced. The symptoms were relieved within the first week of taking the drug, and the better antidepressant effect appeared within two weeks. Usually, it takes two to four weeks to get the best effect. An initial adult dose of 50 to 100mg(1 to 2 tablets) per day is recommended in divided doses, followed by an increase of 50mg(1 tablet) every two to four days. Outpatient general daily 200mg(4 tablets) is appropriate, divided into doses. Hospitalized patients with severe dose may be larger. The maximum dose should not exceed 400mg(8 tablets) per day in divided doses. The maintenance dose for long-term use should be maintained at the lowest dose. Once there is sufficient efficacy, it can be gradually reduced. It is generally recommended that the course of treatment should last for several months after the onset of action. |
| adverse reactions | the common adverse reactions were drowsiness, fatigue, dizziness, Head Pain, Sleep Initiation and Maintenance Disorders, Nervousness and tremor; as well as blurred vision, dry mouth, constipation. Rare orthostatic hypotension (with a meal at the same time medication can reduce), tachycardia, Nausea, Vomit and abdominal discomfort. Very few patients have musculoskeletal pain and dreams. Clinical studies have reported that some adverse reactions may be related to the use of trazodone hydrochloride: akathisia, allergic reactions, anemia, flatulence, abnormal urination, sexual dysfunction and abnormal menstruation. But it is seen in a very small number of patients. |
| overdose | this product and other drugs (ethanol, ethanol-chloral hydrate-diazepam, amobarbital, when used in combination with diazepam or methyl propamide), the overdose of trazodone hydrochloride can cause death. The most serious adverse reactions of overdose alone are priapism, respiratory arrest, seizures and ECG abnormalities. The most common adverse events were drowsiness and Vomit. Overdose causes an increase in the incidence and extent of various adverse reactions. there is currently no specific antidote. Hypotension and excessive sedation should be treated according to clinical routine. In case of excessive use of this product, gastric lavage should be carried out. Taking diuretics can promote drug excretion. |
| drug interaction | 1. In patients treated with trazodone hydrochloride, plasma levels of digoxin or phenytoin may be increased if digoxin or phenytoin is concomitantly administered. 2. This product may enhance the role of alcohol, barbiturates and other central nervous system inhibitors. 3. The interaction between this product and MAOI is not clear recently. If the product is taken immediately after stopping the drug or at the same time with it, trazodone hydrochloride should be started at a low dose until the clinical curative effect is produced. 4. When trazodone hydrochloride is used in combination with antihypertensive drugs, it is necessary to reduce the dose of antihypertensive drugs. |
CAS:
25332-39-2
MF:
C19H23Cl2N5O
MW:
408.32
EINECS:
246-855-5
MDL No.:
MFCD00079603
Melting point:
223-226 C
Flash point:
9℃
storage temp.
2-8°C
solubility
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 23.3 mg/mL
form
powder
color
off-white
PH
pH (10g/l, 25℃) : 3.9～4.5
Water Solubility
Soluble at 25mg/ml in methanol. Also soluble in 0.1M HCl or DMSO. Insoluble in water /n
InChIKey
OHHDIOKRWWOXMT-UHFFFAOYSA-N
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.