Pharmacological effects
The role of the nervous system
An analgesic effect: Sinomenine demonstrated positive analgesic effects in experiments with mouse electrical stimulation, hot plate method, and rabbit photothermal stimulation. The dose required for analgesic effect by intracerebral injection is equivalent to 1/2000 of intraperitoneal injection, indicating that the site of analgesia is in the central nervous system; it is combined with propylene morphine and does not appear to antagonize, but instead produces synergy, indicating that it The principle of analgesia is different from that of morphine analgesics. The dose required to produce analgesia is about 10 times that of morphine and has a shorter duration. Continuous use can also produce tolerance, but it is slower than morphine and there is no cross-tolerance with morphine. In combination with promethazine, the effect is enhanced, which is mainly due to the synergy of the central role of the two drugs, and some may also be due to the release of histamine by the promethazine against the sinomenine. When combined, there was no effect on the production and toxicity of sinomenine. Two sedative effects: Sinomenine significantly reduced the spontaneous activity and passive activity of mice, and had no significant effect on the sleep time of barbiturates; it had certain antagonistic effects on strychnine (reduced seizure threshold of strychnine in mice). ) But not against pentamethasine tetrazole. Dogs and monkeys also had significant sedative effects by oral administration of sinomenine 45 to 95 mg/kg. A small dose (5 to 10 mg/kg) prolongs the latency of defensive exercise conditioning in mice and cats. The conditioned reflex partially disappears, and the non-conditioned reflex also disappears in small proportions, indicating that it is primarily for advanced nerve activity. The excitement process has inhibitory effects. Sinomenine also eliminates the irritated reactions induced by electrical stimulation in mice and appears to have a stabilizing effect. Three other effects: sinomenine has an antitussive effect. For mice and cats, the antitussive potency is similar to codeine; for guinea pigs, the potency is only 1/4 that of codeine. Promethazine can strengthen its antitussive effect. In addition, slight emetic effect, no effect on vomiting caused by injection of dehydrated morphine. When rats are given large doses intraperitoneally, there is a certain cooling effect. When the amount of poisoning injected into the rabbit, the body temperature has also declined, but if given repeatedly, can produce tolerance, and body temperature no longer decline. According to reports, it has a local anesthetic effect on rabbit cornea, can be used as a local infiltration anesthetic, but it can also produce tolerance, such as continuous injection, the effect is weakened.
Antihypertensive effect
The total alkaloids of sinomenine have a positive acute hypotensive effect on both anesthetic and non-anesthetized experimental animals (dogs, cats, rabbits, and rats), whether intravenously or intragastrically. The effects are rapid, significant, and long-lasting, but they are administered multiple times in succession. , it produces rapid tolerance. The antihypertensive effect was not related to M-cholinergic nerves or acetylcholine, nor was it due to histamine release. It may be related to its anti-adrenergic and nerve reflex effects. Due to the above-described hypotensive properties, it has no significant therapeutic effect on chronic experimental hypertension in dogs. The acidic extract of Ivy does not affect blood pressure in acute tests in rabbits.
Effect on gastrointestinal activity
Sinomenine often causes mild gastrointestinal adverse reactions to dogs and monkeys; it has inhibitory effects on ex vivo rabbit intestine and guinea pig intestine, and can counteract the deterrence effects of pilocarpine, histamine, acetylcholine, and strontium chloride, but Intravenous sinomenine in dogs and rabbit intestine all caused temporary excitement in the small intestine. This excitatory effect was completely blocked by diphenhydramine and hexahydrocarbamate. Atropine was completely or partially blocked, but both sides were cut off. The vagus nerve does not block. Injection of sinomenine can increase the secretion of gastric juice and its acidity, and no significant change in pepsin activity. Excitatory effects on the gastrointestinal tract are mainly related to histamine release. However, the administration of neotaxine (an antihistamine) failed to suppress the secretion of gastric juice. The acidic extract of sinomenia can stimulate ex vivo rabbit intestines.
Anti-inflammatory effect
Sinomenine has a significant regression effect on formaldehyde and egg white arthritis in rats, and this effect is not observed after the removal of the adrenal gland or pituitary. For normal rats, the content of vitamin C in the adrenal glands can be reduced. After pentobarbital (which inhibits the hypothalamus) anesthesia is lost, the anti-inflammatory action of sinomenine may affect the pituitary through the hypothalamus. Caused by the adrenal system, but not related to the release of histamine. It has a preventive effect on active anaphylactic shock in guinea pigs, but it is worse for dogs. Simultaneously with the antigen, it can inhibit the release of histamine. Trichomonas and Plasmodium also have inhibitory effects.
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