納菲制藥
Nasal-Phyto
Butorphin tartrate nasal spray
Author : admin Time : 2019-11-28Click :
Butorphanol tartrate is an agonist-antagonist mixed opioid receptor agonist. It has a lower affinity to u-type opioid receptors and can also stimulate k opioid receptors. Interaction with the above-mentioned central nervous system (CNS) receptors can produce most of the pharmacological effects including analgesic butorphine tartrate; in addition to the analgesic effects, the central effects include the suppression of spontaneous respiratory activity, cough, emetic, Pupil dilation and sedation. Exciting k-opioid receptors can cause unpleasant psychiatric-like effects in some patients. Butorphanol tartrate can change the resistance and volume of cardiac blood vessels (nerves), bronchomotor tension, gastrointestinal secretion, and bladder sphincter activity through non-CNS action mechanisms.
No teratogenic effect was observed in the teratogenicity test in mice, rats and rabbits. However, the incidence of stillbirths was higher in rats given subcutaneous injection of butorphanol tartrate 1mg / kg (5.9mg / ㎡) than in the control group. When rabbits were orally administered 30 mg / kg (360 mg / ㎡) and 60 mg / kg (720 mg / ㎡), the loss rate after implantation increased. Full and tightly controlled studies have not been conducted on pregnant women before 37 weeks of pregnancy, so they should only be used during pregnancy if the potential benefits of this product outweigh the potential danger to the fetus. In the case of giving this product once or multiple times, taking other analgesics or sedatives, and premature delivery within 2 hours before delivery, it may cause respiratory depression or apnea in infants, but clinical reports of this adverse reaction Rarely. A study of 119 patients found that intramuscular injection of butorphanol tartrate 1 mg before childbirth resulted in treatment-related temporary positive spin wave-like fetal heart rate (for 10-90 minutes), so it should be used with caution when the fetal heart rate is abnormal. This product. This product can be secreted by breast milk, but the intake of infants may not have significant clinical significance (muscular injection of butorphin tartrate 2 mg / time, 4 times / d, breast milk concentration is about 4ug / L). Although there is no clinical experience with nasal administration in lactating women, it is believed that the levels of butorphin tartrate in breast milk will be similar to those when administered intramuscularly.
According to foreign literature reports, after taking 1 mg of butorphanol tartrate nasal spray, the peak blood concentration was reached within 30 to 60 minutes, with an average peak concentration of 0.9 to 1.04 ng / ml. Butorphanol tartrate nasal spray has an absolute bioavailability of 60 to 70%. When applied to patients with allergic rhinitis, its bioavailability will not change. The use of this product in patients using nasal vasoconstriction drugs can slow the absorption rate of this product, but the total absorption will not change. The distribution capacity of butorphanol tartrate ranges from 305 to 901 liters, the total clearance rate is 2 liters / hour to 154 liters / hour, the serum protein binding rate is 80%, and it is present in a concentration range of not more than 7ng / ml Concentration dependence. The drug can penetrate the blood-brain barrier, the placental barrier, and enter milk. It is mainly metabolized in the liver and the main metabolite is hydroxylated butorphinol. Most of the drug's metabolites (70-80%) are excreted through urine, and a small amount is excreted from feces.
The half-life of elderly patients using butorphanol tartrate nasal spray is significantly longer than that of younger patients. In patients with renal failure (creatinine clearance <30ml / min), the elimination half-life of this drug is nearly twice that of normal people, and the overall drug clearance rate is half that of normal people. The drug is used in patients with liver dysfunction, and its clearance half-life is three times that of normal people, and the overall drug clearance rate is half of normal people.
No teratogenic effect was observed in the teratogenicity test in mice, rats and rabbits. However, the incidence of stillbirths was higher in rats given subcutaneous injection of butorphanol tartrate 1mg / kg (5.9mg / ㎡) than in the control group. When rabbits were orally administered 30 mg / kg (360 mg / ㎡) and 60 mg / kg (720 mg / ㎡), the loss rate after implantation increased. Full and tightly controlled studies have not been conducted on pregnant women before 37 weeks of pregnancy, so they should only be used during pregnancy if the potential benefits of this product outweigh the potential danger to the fetus. In the case of giving this product once or multiple times, taking other analgesics or sedatives, and premature delivery within 2 hours before delivery, it may cause respiratory depression or apnea in infants, but clinical reports of this adverse reaction Rarely. A study of 119 patients found that intramuscular injection of butorphanol tartrate 1 mg before childbirth resulted in treatment-related temporary positive spin wave-like fetal heart rate (for 10-90 minutes), so it should be used with caution when the fetal heart rate is abnormal. This product. This product can be secreted by breast milk, but the intake of infants may not have significant clinical significance (muscular injection of butorphin tartrate 2 mg / time, 4 times / d, breast milk concentration is about 4ug / L). Although there is no clinical experience with nasal administration in lactating women, it is believed that the levels of butorphin tartrate in breast milk will be similar to those when administered intramuscularly.
According to foreign literature reports, after taking 1 mg of butorphanol tartrate nasal spray, the peak blood concentration was reached within 30 to 60 minutes, with an average peak concentration of 0.9 to 1.04 ng / ml. Butorphanol tartrate nasal spray has an absolute bioavailability of 60 to 70%. When applied to patients with allergic rhinitis, its bioavailability will not change. The use of this product in patients using nasal vasoconstriction drugs can slow the absorption rate of this product, but the total absorption will not change. The distribution capacity of butorphanol tartrate ranges from 305 to 901 liters, the total clearance rate is 2 liters / hour to 154 liters / hour, the serum protein binding rate is 80%, and it is present in a concentration range of not more than 7ng / ml Concentration dependence. The drug can penetrate the blood-brain barrier, the placental barrier, and enter milk. It is mainly metabolized in the liver and the main metabolite is hydroxylated butorphinol. Most of the drug's metabolites (70-80%) are excreted through urine, and a small amount is excreted from feces.
The half-life of elderly patients using butorphanol tartrate nasal spray is significantly longer than that of younger patients. In patients with renal failure (creatinine clearance <30ml / min), the elimination half-life of this drug is nearly twice that of normal people, and the overall drug clearance rate is half that of normal people. The drug is used in patients with liver dysfunction, and its clearance half-life is three times that of normal people, and the overall drug clearance rate is half of normal people.
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