Generic Name: Dihydroetorphine Hydrochloride Sublingual Tablets English Name: Dihydroetorphine Hydrochloride Sublingual Tablets Chinese Pinyin: Yansuan Eeqinaituofei Shexia Pian 17-Methyl-7α[(S )-1-hydroxy-1-methylbutyl] -6,14-Bridged ethylidene-6,7,8,14-tetrahydropapaverine hydrochloride. Molecular Formula: C25H35NO4・HCl Molecular Weight: 449.98 【Properties】This product is white tablets. Pharmacology and Toxicology] This product is a highly effective analgesic, is a pure agonist of opioid receptor, and the affinity with μ, δ, κ receptors are much greater than that of morphine, especially the affinity for μ receptors is thousands of times greater than that of δ and κ. The quantitative effect relationship of its analgesic effect is linear like that of morphine, and the strength of its pharmacological activity is 6,000 to 10,000 times stronger than that of morphine. Therefore, the safety factor (i.e., therapeutic index) is larger than that of morphine, and the potential for physical dependence is significantly lighter than that of morphine. In monkeys chronically given dihydroetorphine, the withdrawal symptoms produced are significantly milder than those of morphine, whether the drug is abruptly stopped or the antagonist enalaporphine is injected subcutaneously to induce addiction. The potential for psychiatric dependence was studied in rats by autoinjection, which also showed less severe results than morphine, and phase I clinical trials showed no euphoria in subjects, but rather dizziness, nausea, vomiting, and malaise at higher doses. The traditional concept of opioid agonists is that the stronger the analgesic effect, the more pronounced the euphoria and the greater the addiction. The analgesic dosage of dihydroetorphine is the smallest, the analgesic effect is the strongest, but no euphoria reaction, so its potential for addiction is small. phase II clinical trials and the promotion of more than 3,000 times the results of the trial show that the analgesic effect of this product, the total effective rate of 99.6%. Dihydroetorphine also has sedative and antispasmodic central effect. The inhibition of respiration is relatively milder than that of morphine, and respiratory depression rarely occurs at the prescribed analgesic dose (0.83%), but can be markedly inhibited when overdosed. If administered intravenously, respiratory depression is evident at doses greater than 0.4 μg/kg and respiratory management is required. Long-term use is also associated with the development of tolerance and dependence. The main deficiency of this product is the short effective time of analgesia. Toxicology: Acute toxicity LD50 (mg/kg): subcutaneous, mice 82 ± 17. rabbits, 0.047 ± 0.016 (morphine is 436 ± 70.533). [1] 【Pharmacokinetics】 This product is poorly absorbed orally, ED50 is as high as 123(98~153)μg/kg, sublingual absorption is fast, after 10~15min pain can be significantly reduced, the dose is only equivalent to oral 1/30. due to the extremely small dosage, there is no drug testing method for human pharmacokinetic studies. Indications】This product is suitable for all kinds of severe pain relief, such as traumatic pain, post-surgical pain, acute abdominal pain, dysmenorrhea, advanced cancer pain, including the use of morphine, pethidine is ineffective in severe pain. Usage and dosage] Sublingualization. Common dosage, 20~40μg each time, repeat administration after 3~4h as needed. Extreme dose, 60μg each time, 180μg a day, generally should not be used continuously for more than 1 week, advanced cancer patients with long-term application of the product to produce tolerance, as needed, the appropriate increase in the dose, the maximum can be used up to 100μg each time, 400μg a day, when the use of large doses should be in accordance with the doctor’s advice. Adverse reactions] When this product is used in various pain cases, there are generally no significant adverse reactions under the therapeutic dose, a few patients may experience dizziness, nausea, vomiting, fatigue, sweating, and bedridden patients are less reactive than active patients. These reactions may resolve spontaneously without any treatment. Occasionally, respiratory depression is seen. No morphine-like constipating effects have been observed. Occasionally the respiratory slowdown to about 10 times per minute, with respiratory excitatory drug niclosamide can be corrected, can also be corrected with oxygen. Contraindications] This product is contraindicated in traumatic brain injury, delirium or pulmonary insufficiency. Hepatic and renal insufficiency should be used with caution or reduce the dosage. Non-intense pain such as toothache, headache, rheumatic pain, hemorrhoidal pain or small traumatic pain in local tissues should not be used. Precautions] 1, this product is a national special management of narcotic drugs, must strictly comply with the national regulations on the management of narcotic drugs, hospitals and hospital rooms of the storage of drugs must be locked, the color of the prescription should be differentiated from the prescription of other drugs. Custodians at all levels should abide by the handover system and should not be negligent.2. It can be addictive, and is lighter than morphine.3. It can only be contained under the tongue, and should not be swallowed, otherwise it will affect the pain-relieving effect.4. The State Ministry of Health stipulates that it should not be used as a substitute for the detoxification treatment of heroin addiction.5. It has little effect on the function of the circulatory system in the general dosage, and there can be a transient drop in blood pressure when the dosage is too large. Pregnant women and lactating women] is not clear. [For children] Prohibited for infants, young children, immature newborns. Elderly patients: Use with caution. Drug interactions] Not known. Overdose] No toxic reaction has occurred when used within the prescribed dose, but in overdose of non-medical advice or improper use, acute poisoning can occur, mainly manifested as respiratory arrest, coma, etc., and can be quickly rescued with allylmorphine or naloxone. Storage] Keep in a sealed place with light shielding. Expiry date: 4 years.