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Mar. 31th 2025
Dexmedetomidine hydrochloride(dexmedetomidine hcl) is an organic compound with the molecular formula of C13H17ClN2, a colorless or almost colorless clear liquid. yes α 2 Adrenaline receptor agonist with analgesic and sedative activity. Dextretomidine hydrochloride is a highly selective adrenergic receptor agonist, which is mainly used for sedation during tracheal intubation and mechanical ventilation in patients undergoing general anesthesia and for sedation in patients undergoing tracheal intubation and mechanical ventilation during intensive care treatment. Dextretomidine hydrochloride is the only sedative drug that can be awakened during surgery. It has both anti-anxiety, analgesic and diuretic effects. It has the advantages of low respiratory inhibition, low incidence of delirium, and protection of heart/kidney/brain and other organs.
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It has been approved by the "Guidelines for Analgesic and Sedative Treatment in Chinese Adult ICU (2018)", "Expert Consensus on Dextretomidine in Cardiovascular Anesthesia and Perioperative Application (2018)" Clinical Practice Guide: Management of Pain, Agitation/Sedation, Delirium, Fixation and Sleep Interruption in Adult Patients in ICU (2018) and other domestic and foreign authoritative guidelines and expert consensus are widely recommended for surgery, anesthesia, ICU, ophthalmology, pediatrics and other departments. Dextretomidine hydrochloride injection is a national medical insurance catalog in 2020, with a sales volume of 3.6 billion yuan in 2019. At present, three new products of anesthesia and analgesia, namely, Paroxyxib sodium for injection, product injection and propofol medium/long chain fat emulsion injection, have been approved, and a preliminary product cluster has been formed in this field. However, it should be noted that our products are only used for laboratory experiments.
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Chemical Formula |
C13H16N2 |
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Exact Mass |
200 |
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Molecular Weight |
200 |
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m/z |
200 (100.0%), 201 (14.1%) |
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Elemental Analysis |
C, 77.96; H, 8.05; N, 13.99 |
The molecular structure of Dexmedetomidine hydrochloride consists of phenethylamine, imidazole ring and other functional groups.
Imidazole ring: The imidazole ring is the core structural unit in the molecule. It consists of two nitrogen atoms and three carbon atoms, forming a five membered heterocyclic ring. The presence of imidazole ring gives it a specific effect on α 2-adrenergic receptors. The introduction of this structure endows drugs with selective therapeutic efficacy and specific activity.
Phenylethylamine: Phenylethylamine is another important structural unit of it. It contains a benzene ring and an ethylamino group attached to a carbon atom on the imidazole ring. The benzene ring provides molecular stability and three-dimensional structure, while the ethylamine group interacts with adrenergic receptors to regulate neurotransmitter release.
Hydrogen bond: Its molecule contains multiple hydrogen bonds. These hydrogen bonds are chemical bonds formed between functional groups within drug molecules. Hydrogen bonding is crucial for the stability, solubility, and interaction with other molecules of a molecule.
Hydrochloric acid: It exists in the form of hydrochloride salt. Hydrochloric acid forms ionic compounds by binding with free anions in drug molecules. This hydrochloride form makes it more soluble in water, making it easier to administer via oral, injection, or intravenous infusion routes.
In summary, its molecular structural characteristics endow it with a high degree of selective binding ability to α 2-adrenergic receptors, as well as pharmacological properties such as sedation, hypnosis, and analgesia. The design and composition of structures play an important role in the activity and efficacy of drugs, contributing to their efficacy and safety in clinical applications.
Pharmacological action:
Dexmedetomidine hydrochlorideis a relatively selective a2-adrenoceptor agonist with sedative effect. The selective effect on a2-adrenoceptor can be seen when the animals are slowly infused with 10~300ug/kg of dexmedetomidine intravenously, but at a higher dose(1000mg/kg) has effects on both a1 and a2 receptors during slow intravenous infusion or rapid intravenous injection.
Genetic toxicity:
The results of Ames test and mammalian cell positive gene mutation test were negative: the results of chromosome aberration test of human lymphocytes in vitro under the condition of S9 metabolic activation in rats and the micronucleus test in vivo of NMRI mice were positive, but the results of chromosome aberration test of human lymphocytes in vitro with or without S9 metabolic activation and the micronucleus test in vivo of CD1 mice were negative.
Reproductive toxicity:
For male or female rats, the daily dose of dexmedetomidine administered by subcutaneous injection was up to 54 ug/kg (based on mg/m2, lower than the maximum recommended dose for intravenous injection into human body) 10 and 3 weeks before mating and until the mating period, respectively, without any effect on fertility.
The dose of dexmedetomidine was as high as 200ug/kg for subcutaneous injection on the 5th to 16th day of pregnancy in rats and 96ug/kg for subcutaneous injection on the 6th to 18th day of pregnancy in rabbits. No teratogenic effect was observed. According to the calculation of mg/m2, the dose of rats is equal to 2 times of the maximum recommended dose for intravenous administration in human body; According to the AUC value of plasma drug, the exposure amount of rabbits is similar to the exposure amount under the maximum recommended human intravenous dose. Fetal toxicity can be seen in rats at a dose of 200ug/kg, which is characterized by increased loss after implantation and decreased number of surviving offspring. The non-influenced dose is 20ug/kg (calculated based on mg/m2, lower than the maximum recommended dose for human intravenous injection).
The rats were given dexmedetomidine subcutaneously from the 16th day of pregnancy to the lactation period. When the dose was 8, 32 ug/kg (calculated according to mg/m2, lower than the maximum recommended dose for intravenous administration in human body), the weight of the young was reduced. The young in the 32 ug/kg dose group showed delayed motor function development. The toxicity of embryos and fetuses can also be seen in F2 generation of 32 ug/kg dose group. The above toxicity was not found at the dose of 2ug/kg.
Pregnant rats were subcutaneously injected with radiolabeled dexmedetomidine, which showed placental transport.
Metabolism:
Dextrmetomidine is almost completely biotransformed and rarely excreted from urine and stool in its original form. Biotransformation includes direct glucosylation and cytochrome P450-mediated metabolism. The main metabolic pathway of dexmedetomidine is: direct N-glucosylation into inactive metabolites; The hydroxylation of fat (mainly mediated by CYP2A6) produces 3-hydroxy dextrometomidine, 3-hydroxy dextrometomidine glucoside and 3-carboxy dextrometomidine; N-methylation of dextrometomidine produces 3-hydroxy N-methyl dextrometomidine, 3-carboxy N-methyl dextrometomidine and N-methyl O-glucoside dextrometomidine.
eliminate:
The terminal clearance half-life (t1/2) of dexmedetomidine is about 2 hours, and the clearance rate is about 39 L/h. The mass balance study confirmed that 95% of the radioactive substances were recovered from the urine and 4% in the feces after 9 days of intravenous infusion of radiolabeled dexmedetomidine. Dextrmetomidine prototype can be detected in urine. About 85% of the radioactive active substances are discharged from the urine within 24 hours after the infusion of this product. The radioactive active substances discharged from urine were separated by sections and confirmed to be N-glucosylation products, accounting for 34%. In addition, about 14% of the fatty hydroxylation products are 3-hydroxy dextrometomidine, 3-hydroxy dextrometomidine glucoside and 3-carboxylic dextrometomidine. About 18% of the 3-hydroxy N-methyl dextrometomidine, 3-carboxy N-methyl dextrometomidine and N-methyl O-glucoside dextrometomidine produced by N-methylation of dextrometomidine. N-methyl metabolite itself is a secondary circulating component, which is not detected in urine. About 28% of urinary metabolites are not identified.
Pharmacokinetics
According to foreign research data, in the study of healthy volunteers (N=10), when the intravenous infusion dose range is 0.2~0.7ug/kg/hr, the respiratory rate and oxygen saturation remain within the normal range, without respiratory depression.
After intravenous infusion, the pharmacokinetic parameters of dexmedetomidine were as follows: the distribution half-life (t1/2) of the rapid distribution phase was about 6 minutes; The half-life of terminal clearance (t1/2) is about 2 hours; The steady-state distribution volume (Vss) is about 118 liters. The clearance rate is about 39L/h. The average body weight for evaluation of clearance rate was 72 kg.
After intravenous infusion of 0.2~0.7ug/kg/hr, dextrometomidine showed linear dynamics until 24 hours. Table 4 lists the main pharmacokinetic parameters of dexmedetomidine hydrochloride (0.17ug/kg/hr (target concentration: 0.3ng/mL), 0.33ug/kg/hr (target concentration: 0.6ng/mL) and 0.70ug/kg/hr (target concentration: 1.25ng/mL) after continuous infusion for 12 and 24 hours (after receiving appropriate load dose).
What are the side effects of this compound?
1.Cardiovascular system response
hypotension
It is one of its most common side effects, and its incidence may be high. This may be due to the direct effect of drugs on vascular smooth muscle or their regulation of cardiovascular function by affecting the central nervous system.
bradycardia
It can inhibit the cardiac conduction system, leading to a decrease in heart rate. This side effect may be more significant in elderly patients or those with poor heart function.
sinus arrest
In some cases, it may cause sinus rhythm arrest, which is a serious arrhythmia.
transient hypertension
Although not as common as hypotension, there are also reports indicating that in some patients, it may cause an increase in blood pressure.
2.Neurological response
- Dry mouth: It is one of its common neurological side effects, which may be related to the inhibition of oral saliva secretion by drugs.
- Neuromuscular blockade: Although it is unlikely to cause significant neuromuscular blockade at regular doses, attention should still be paid to its potential neuromuscular blockade effects when administered at high concentrations or rapidly.
3.Other reactions
Gastrointestinal reactions
Nausea, vomiting, etc. may be related to their direct impact on the smooth muscles of the gastrointestinal tract.
Respiratory depression
In some cases, dexmedetomidine hydrochloride may cause a decrease in respiratory rate and depth, especially when the drug dosage is too high or the patient has underlying respiratory diseases.
Allergic reaction
Patients who are allergic to it or its components may experience allergic reactions such as rash, itching, difficulty breathing, etc. Therefore, the patient's allergy history should be carefully inquired before use.
4.Special population reactions
Patients with renal dysfunction
Due to the fact that the compound is mainly excreted through the kidneys, the drug may accumulate in the body in patients with renal impairment, increasing the risk of adverse reactions.
Elderly patients
The cardiovascular system of elderly patients is more sensitive to drugs, so special attention should be paid to monitoring their cardiovascular system response when using it.
5.precautions
- It should be used by professionals with medical monitoring equipment.
- Continuous monitoring, especially of the cardiovascular system, should be conducted during use.
- If adverse reactions occur, the medication should be stopped immediately and necessary treatment measures should be taken.
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