Clinical trials about the Lappaconitine Hydrobromide Injection
Lappaconitine is a two terpene alkaloid which extracted from the root of Aconi tum sinomonatum). It is commonly used its hydrobromic acid salt in che clinical, which is a Non addiction analgesics, with strong analgesic action. This product also has local anesthesia, cooling, antipyretic and anti-inflammatory swelling. This product is no addiction, no teratogenic tire effect on animal test, also won't happen accumulation of lead poisoning. This product analgesic effect onset time is 20 ~ 30 minutes, analgesic time is 2 ~ 22 hours. The analgesic action is mainly through the prevent voltage dependence sodium channel, inhibiting presynaptic membrane on norepinephrine reuptake of, restrain the afferent fibers substance P release, thus giving full play to the analgesic effect.
. ●Ⅰ．Strength analgesia
★ Lappaconitine hydrobromide postoperative intravenous analgesia clinical curative effect observation.
Option period esophageal cancer surgery patients 45 cases, ASA Ⅰ - Ⅲ level, random divided into A, B, C three groups, each group of 15 cases. All of the patients without previous history of chronic pain, and also have no long-term use of sedation analgesic history, age, weight, operation type, operation time were no statistically significant differences. Intraoperative anesthetic stable and smooth operation. In the top 30 min before complete surgery, B, C two groups of patients were slow intravenous Lappaconitine 4 ~ 6 mg, and at the same time, venous connection analgesia pump, injection speed 2 m1 / h, group B analgesia pump liquid medicine for lappaconitine 0.3 mg/kg. 2 d, C group of analgesia pump liquid medicine for lappaconitine 0.35 mg/kg. 2 d, two groups of all use 0.9% brine dilution to 100 m1. A group as control group, according to the patient's postoperative pain, VAS score 5 points or more muscle injection for butyl bromide 50 to 100 mg analgesia. The situation is as follows (table is abbreviated).
Adverse reaction: Postoperative analgesia in during A group 2 (13.3%) nausea,
but not vomiting; And B, C two groups, no patient nausea, vomiting appear. Nausea and vomiting incidence was significantly lower than in group A (P < 0.01). In addition A group of four people appear hyperhidrosis (26.7%); Group B two people appear hyperhidrosis (13.3%); C group 3 people appear hyperhidrosis (20%). Three groups of comparison between no significant difference (P > 0.05). Three groups were all did not appear respiratory depression, low blood pressure and other adverse reaction.
Conclusion: 1. Lappaconitine analgesic efficiency of the high and low dose and is closely related to increase with the dose and analgesic effect improved, the two days lappaconitine dosage 0.35 mg/kg, already can achieve thoracic open-chest surgery patients postoperative analgesia effective basic requirements. 2.
Lappaconitine for postoperative analgesia, analgesic effect exactly, small side effects, it is worth clinical application.
★Lappaconitine and dolantin used for liver cancer pain curative effect contrast
Guangdong province EnPingShi people's hospital application lappaconitine Hydrobromide liver cancer pain treatment of 17 cases and application of dolantin treatment of 11 cases. 28 cases were selected from the hospital from January 1991 to December 1993 hospital patients, the clinical manifestation, laboratory examination, B ultrasound, CT examination which conform to the liver cancer diagnosis (primary), and all have liver area persistent intense pain. Randomly divided into lappaconitine treatment group (referred to as treatment group) and dolantin treatment group (referred to as the control group). Patient sex, age, weight, etc were no statistically significant differences.
1. Therapeutic method
The treatment group: 8 mg lappaconitine hydrobromide injection soluble in sodium chloride injection 500 ml of static drop, once a day, when necessary, + 1 times; Control group: muscle note dolantin 50 mg (failed increased to 100 mg), 3 times a day. Two groups are not added with other painkillers.
2. Curative effect judgment
Remarkable effect：Relieve Pain. Effect：Reducing pain can bear. Invalid： Pain no change or reduce the duration of time not more than half an hour.
3. treatment outcome
3.1 1 weeks treatment
The treatment group effect is remarkable in 7 patients (41.18%), effective 8 cases (47.16%), the total effective rate was 88.24%. Invalid 2 cases (11.76%); Control
group effect is remarkable 6 patients (54.55%), effective 4 cases (36.36%), with the total effective rate of 9 o. 91%, invalid 1 cases (9.09%). Two groups of curative effect comparison has no significant difference (P > 0.05).
3.2 3 weeks treatment
The treatment group effect is remarkable in 5 patients (39.41%), effective 9 cases (53.94%), the total effective rate 92.35%, invalid in 3 patients (17.65%);
Control group effective 2 cases (18.18%), 9 cases failed (81.83%), two groups of comparisons have a significant difference (P < 0.01). The treatment group have 12 cases (70.59%), the long-term drugs are effective; Control group invalid cases will dose increased to 100 mg, effective time also can only lasts 1 ~ 2 h. After occurrence curative effect time and hold time: treatment group is in commonly 10 min or so, hold time 5 ~ 6 h more than control group in 5 min inside, maintain 2 ~ 5h.
4. Summary: Application of lappaconitine hydrobromide to therapy liver cancer
patient’s liver area pain have got better analgesic effect
Compared with dolantin, 1, 2 weeks curative effect approximation, but the third week dolantin’s curative effect down significantly. Two groups of comparisons have significantly difference (P < 0.01). Conclusin: dolantin is easy to produce resistance, and easy to addiction; Lappaconitine’s curative effect is stable, not easy the creation bears the medicine, also don't addiction, non-toxic side effects, and Lappaconitine not only has the analgesic action, and there are local anesthesia, cooling, antipyretic and swelling effect of malignant tumor and other stubborn pain curative effect is distinct.
★After cesarean section vein, lappaconitine hydrobromide controlled analgesia
effect and the influence of prolactin
Shanxi medical university second affiliated hospital of 29 cases of option forward underwent cesarean section pregnant women, random divided into analgesia group (n = l4) and the control group (n = l5). Analgesic group in cesarean section, using PCIA give Lappaconitine Hydrobromide, continuous dose of 0.4 mg/h, PCA dose of 0.1 mg, analgesic time 40 h. With radioimmunoassay measuring plasma PRL concentration, visual analogue scale (VAS) evaluation method of analgesic effect, postoperative pain control group when muscle pethidine injection. Clinical verification confirmed: after cesarean section using Lappaconitine PCIA, analgesic effect exact safety, which has no effect on the newborn babies sleep time, lactation time and behavioral. In addition, puerpera’s PRL secretion increase, colostrum advance, which can promote lactation.
● ⅡOther pharmacological action
Lappaconitine also has significant anti-inflammatory detumescence, local anesthetic effect local anesthesia, cooling, antipyretic and enhancing immunity function. This for surgery incision healing and preventing damage of sexual stimulation upload has good effect. This product can be used as surgery analgesics, also can improve the patient's systemic symptom, improve the body's immune index, and the curative effect stability, not easy the creation bears the medicine, no song horse variety side effects(Calm, dry mouth, sweating, nausea, vomiting, headaches and nonspecific central nervous system symptoms such as dizziness and other adverse reaction),Side effects are less and mild. This product and morphine collaborative enhance analgesic action, the clinical both share reduce morphine consumption, reduce such as morphine analgesia drug side effects, improve the analgesic effects are help, can be used as the preferred drug cancer pain.
● Ⅲ Instruction of Lappaconitine Hydrobromide Injection
【Drug Names】Lappaconitine Hydrobromide Injection
【Character】Colorless transparent liquid
【Pharmacology and toxicology】This product is a Non addiction analgesics, with strong analgesic action. It also has local anesthesia, cooling, antipyretic and
anti-inflammatory swelling. Compared with pethidine, it has the same analgesic effect, although onset time is a bit slow, but which can maintain a long time. Its analgesic action is seven times than antipyretic analgesics aminopyrine. This product is no addiction, no teratogenic tire effect on animal test, also won't happen accumulation of lead poisoning. Acute toxicity test results: rats through the mouth LD50 to 20 mg/kg; Mice celiac injection LD50 to 9.1 mg/kg, intravenous LD50 to 6.9 mg/kg.
【Adaptation disease】For more than a moderate pain
【Usage and Dosage】Intramuscular injection:4mg/per time,1～2times/per day,Or as directed by a physician
Intravenous: 4～8mg/per day, Soluble in glucose's chloride injection 500 ml of static drop.
【Untoward effect】Individual patients experienced urticaria, flustered, bosom is
frowsty, giddy, etc., after discontinuation of quickly disappear.
【Matters need attention】This product poisoning early performance is electrocardiogram (ecg) changes (reversible).
【UN Specification Packaging】 2ml :4mg, Ampoule packaging，5 Branch/box.
【Expiry date】 Two years.
