What Is Dexmedetomidine?
Dexmedetomidine is also known as Dexmedetomidine Hydrochloride; Dexmedetomidine Hydrochloride; Precedex. This product is soluble in water and easily soluble in methanol and absolute ethanol. It is almost insoluble in anhydrous ether and 0.1mol / l hydrochloric acid solution. Molecular formula: C13H16N2, molecular weight: 200.28000. Dexmedetomidine is an effective 2-adrenergic receptor agonist with an 8-fold higher affinity for 2-adrenergic receptor than clonidine. Calm. [1-3]
- Drug Name
- Dexmedetomidine
- Alias
- Dexmedetomidine hydrochloride
- Foreign name
- Dexmedetomidine
- Whether prescription drugs
- prescription
- Dosage
- See below for details
- Adverse reactions
- Hypotension, nausea, bradycardia, etc.
- Main medication contraindications
- People who are allergic to this medicine, pregnant, lactating women
- Dosage form
- Injection
- Athletes use with caution
- Use with caution
- Whether to include health insurance
- Not included
- Drug type
- chemical
- CAS number
- 113775-47-6
- Molecular formula
- C13H16N2
- Molecular weight
- 200.28000
- Dexmedetomidine is also known as Dexmedetomidine Hydrochloride; Dexmedetomidine Hydrochloride; Precedex. This product is soluble in water and easily soluble in methanol and absolute ethanol. It is almost insoluble in anhydrous ether and 0.1mol / l hydrochloric acid solution. Molecular formula: C13H16N2, molecular weight: 200.28000. Dexmedetomidine is an effective 2-adrenergic receptor agonist with an 8-fold higher affinity for 2-adrenergic receptor than clonidine. Calm. [1-3]
Dexmedetomidine Basic Information
- Chinese name dexmedetomidine
- English name: dexmedetomidine
- English alias: Dexmedetomidine; 5-[(1S) -1- (2,3-dimethylphenyl) ethyl] -1H-imidazole; Dexmedetomidina; (S) -medetomidine; Dexmedetomidinum;
- CAS number: 113775-47-6 [1]
- Molecular formula: C13H16N2
- Molecular weight: 200.28000 [1]
- Chemical Structure:
- Exact mass: 200.13100
- PSA: 28.68000
- LogP: 3.17830 [1]
Dexmedetomidine physical and chemical properties
- Density: 1.053g / cm 3
- Boiling point: 381.9ºC at 760mmHg
- Flash point: 191.3ºC
- Refractive index: 1.569
- Vapor pressure: 1.08E-05mmHg at 25 ° C [1]
Dexmedetomidine Safety Information
- Customs code: 2933290090 [1]
Dexmedetomidine customs data
- China Customs Code: 2933290090
- Summary: 2933290090. Other compounds containing non-fused imidazole rings. VAT rate: 17.0%. Rebate rate: 13.0%. Regulatory conditions: None. MFN tariff: 6.5%. Ordinary tariff: 20.0%
- Declaration elements: product name, ingredient content, use, please indicate the appearance of 6-caprolactam, please indicate the appearance, date of contract [1]
Overview of dexmedetomidine drug information
Dexmedetomidine drug name
- Chinese name dexmedetomidine
- English name: Dexmedetomidine
- Alias: Dexmedetomidine hydrochloride; Dexmedetomidine Hydrochloride; Precedex [2]
Dexmedetomidine classification
- Neurological Drugs> Sedatives & Hypnotics> Others [2]
Dexmedetomidine
- Injection [2]
Dexmedetomidine pharmacological effects
- Dexmedetomidine is a relatively selective 2-adrenergic receptor agonist with sedative effects. Selective effects on 2-adrenergic receptors can be seen when dexmedetomidine is slowly infused in animals at 10 to 300 g / kg, but at higher doses (1000 g / kg), slow intravenous infusion or rapid intravenous injection Both drugs have effects on 1 and 2-receptors. [2]
Dexmedetomidine Pharmacokinetics
- Dexmedetomidine is rapidly absorbed after subcutaneous injection or intramuscular injection, and the peak time is 1h. After intravenous infusion of dexmedetomidine, the distribution half-life is about 6min and the steady-state distribution volume is about 118L. After dexmedetomidine is extensively metabolized in the body, the metabolites are mainly excreted in the urine. The elimination half-life is about 2h, and the elimination period is about 39L / h. [2]
Dexmedetomidine indication
- Dexmedetomidine is suitable for sedation during tracheal intubation and mechanical ventilation in patients undergoing general anesthesia. [2]
Dexmedetomidine contraindications
- 1. Disable allergy to dexmedetomidine. [2]
- 2. Pregnant and lactating women, with caution in patients with advanced heart block. [2]
Dexmedetomidine precautions
- 1. Patients should be continuously monitored at the time of dexmedetomidine infusion.
- 2. Dexmedetomidine cannot be combined with blood or plasma through the same intravenous catheter.
- 3. Patients with obvious cardiovascular dysfunction need to take resuscitation measures in advance. [2]
- 4. The continuous infusion of dexmedetomidine should not exceed 24h. [2]
Dexmedetomidine for pregnant and lactating women
- Sufficiently good clinical studies have not been conducted in pregnant women. Dexmedetomidine can be used in pregnant women only if the potential benefits outweigh the potential risks to the fetus. [3] The safety of this product for pregnant women and pregnant women has not been studied. Therefore, this product is not recommended for cesarean section during labor and delivery.
It is unknown whether this product is secreted into human milk. Radioactive isotopes of dexmedetomidine were secreted in breast milk after being administered subcutaneously to nursing female rats. Because many drugs are secreted in human milk, lactating women should use this product with caution. [2-3]
Dexmedetomidine for children
- The safety and effectiveness of this product in children under 18 years of age are unknown. Therefore, this product is not recommended for these people. [3]
Dexmedetomidine for the elderly
- Dexmedetomidine is known to be excreted mainly through the kidney, and the drug is at greater risk for adverse reactions in patients with impaired renal function. Older patients have reduced renal function, so doses should be carefully selected for older patients, and monitoring of renal function may be useful. In foreign clinical studies, there were 729 patients aged 65 or older and 200 patients aged 75 or older in the intensive care sedation test. In patients over 65 years of age, the incidence of bradycardia and hypotension was higher after administration of this product. Therefore, patients over 65 years of age should consider reducing the dose when using this product. A total of 131 patients were 65 years of age and 47 patients were 75 years of age in the clinical trial of procedure sedation. The incidence of hypotension was 72% at age 65 or older, 74% at age 75 or older, and 47% at age 65 or older. Therefore, patients over 65 years of age should reduce the loading dose when using this product. It is recommended that the infusion should be 0.5 g / kg for more than 10 minutes. [2-3]
Dexmedetomidine adverse reactions
- Dexmedetomidine is well tolerated, and common adverse reactions include hypotension, nausea, bradycardia, tissue hypoxia, and atrial fibrillation. [2]
Dexmedetomidine Dosage
- Adult dose: It is formulated into a concentration of 4ug / ml slowly and intravenously at a dose of 1ug / kg, and the infusion time exceeds 10 minutes. This product must be diluted with 0.9% sodium chloride solution to a concentration of 4ug / ml before administration. 2ml of this product can be taken out and added to 48ml of 0.9% sodium chloride injection to form a total 50ml solution. Gently shake to make uniform mixing. [2]
Dexmedetomidine interactions with other drugs
- 1. Dexmedetomidine combined with anesthetics, sedatives, hypnotics, and opioids (such as sevoflurane, isoflurane, propofol, alfentanil, midazolam) may improve efficacy. [2]
- Dexmedetomidine does not affect the neuromuscular blockade of rocuronium bromide. [2]
Dexmedetomidine Toxicology Study
- Genotoxicity
- Dexmedetomidine Ames test, mammalian cell positive gene mutation test results were negative; rat S9 metabolic activation in vitro human lymphocyte chromosome aberration test, NMRI mice in vivo micronucleus test were positive, but The results of chromosomal aberration tests on human lymphocytes in vitro and micronuclei in CD-1 mice with or without human S9 metabolic activation were negative. [3]
- Reproductive toxicity
- Male or female rats have been administered subcutaneous injections of dexmedetomidine at doses of up to 54 g / kg daily from 10 and 3 weeks before mating, respectively (based on g / m, which is lower than the maximum recommended human intravenous injection dose). ) No effect on fertility.
Rats received subcutaneous injections of dexmedetomidine at a dose of up to 200 g / kg on the 5th to 16th days of pregnancy, and rabbits received subcutaneous injections of 96 g / kg on the 6th to 18th day of pregnancy without teratogenic effects. According to the calculation of g / m, the rat dose is equivalent to twice the maximum recommended human intravenous injection dose; according to the plasma drug AUC value, the rabbit exposure is similar to that at the maximum recommended human intravenous injection dose. Fetal toxicity was seen at a dose of 200 g / kg in rats, with increased loss after implantation and reduced number of surviving pups. The non-affected dose is 20 g / kg (based on g / m, which is lower than the maximum recommended human intravenous dose). [3] Rats were given dexmedetomidine subcutaneously from day 16 of pregnancy to lactation, resulting in a dose of 8, 32 g / kg (based on g / m, which is lower than the maximum recommended human intravenous injection dose) The pups lost weight. The pups in the 32 g / kg dose group showed retarded motor function. 32g / kg dose group F2 generation also showed embryo and fetal toxicity. The above toxicity was not seen at a dose of 2 g / kg.
Radiolabeled dexmedetomidine was administered subcutaneously in pregnant rats, and placental transport was visible. [3]