Efficacy and function of sinomenine
Effects on the heart
Sinomenine can significantly reduce myocardial contractility, heart rate, diastolic pressure, left ventricular systolic pressure, cardiac index, peripheral vascular resistance and cardiac output in anesthetized dogs.
Hypotensive effect
Sinomenine has a rapid and powerful antihypertensive effect, and it is not easy to produce rapid tolerance after repeated use. No matter what route of administration is adopted, it has a positive acute hypotensive effect on anesthetized or non-anesthetized animals. However, repeated application of sinomenine is prone to rapid tolerance.
Anti-arrhythmia effect
Sinomenine has obvious antagonistic effects on arrhythmia in rats and guinea pigs caused by aconitine and ouabain, ventricular fibrillation in rats caused by calcium chloride, arrhythmia in rabbits caused by chloroform-epinephrine and heart rate increase caused by isoproterenol, which can improve the abnormal electrocardiogram in rats caused by pituitrin, prevent the damage to the heart caused by ischemia-reperfusion and also have obvious antagonistic effects on ischemic arrhythmia.
anti-inflammatory action
Sinomenine tablets can significantly inhibit adjuvant arthritis in rats, paw swelling and agar granuloma formation in rats caused by carrageenan, antagonize the increase of vascular permeability caused by 5-HT, and significantly inhibit the writhing reaction in mice caused by acetic acid. Intraperitoneal injection can significantly reduce the content of PGE in the inflammatory exudate of rats' feet, inhibit the synthesis of M inflammatory substances PGE2 and leukotriene C4, and reduce the content of vitamin C in rats' adrenal glands, but the anti-inflammatory effect disappears after bilateral adrenalectomy or pituitary resection. Sinomenine extract can also inhibit platelet aggregation induced by platelet activating factor in rabbits. It can obviously reduce the whole blood viscosity and improve the deformability of red blood cells in experimental arthritis rats, and the effect is more obvious with the increase of dose, but it has no obvious effect on plasma viscosity. In addition, it can prevent neutrophil aggregation caused by complement activation and improve inflammatory symptoms.
Effect on gastrointestinal tract
Sinomenine can increase gastric acid secretion and has an exciting effect on sinomenine in rabbit intestine in vivo, which is related to its promotion of histamine release.
Release histamine
Sinomenine is one of the strongest histamine releasing agents in plants. Intravenous injection of sinomenine in dogs can increase the content of histamine in plasma, lower blood pressure, increase portal vein pressure and promote lymphogenesis. Can be inhibited by antihistamines.
Effects on nervous system
Sinomenine can obviously increase the pain threshold of mice, and can also cooperate with and enhance the sedative and hypnotic effects of pentobarbital sodium. Sinomenine can reduce the spontaneous activity of mice, prolong the sleep time of cyclohexylbarbital sodium, inhibit the electrical stimulation response of mice, lower the convulsion threshold of strychnine, and have obvious effect on exercise conditioned reflex.
abirritation
Hot plate method in mice, electrothermal method in rabbits and photothermal method all prove that sinomenine has obvious analgesic effect. Its action intensity is about * * * l/2.5— 1/l0, and its duration is short. Continuous drug use can also produce tolerance, but it is slower than * * *, and the drug resistance disappears after a few days of drug withdrawal. Monkeys were injected with sinomenine subcutaneously for a long time, and there was no abnormal reaction after observing 172 hours, indicating that they were not addicted. The chemical structure of sinomenine is similar to that of morphine, but its mode of action is different from that of morphine, because propylene * * * does not antagonize its analgesic effect, but shows synergistic effect, and there is no cross-resistance with * * * *. It was once thought that the analgesic effect of sinomenine was related to histamine release. In addition, it has obvious synergistic effect with antihistamines such as diphenhydramine and promethazine. Therefore, its analgesic effect has nothing to do with histamine release.
Sedative action
Sinomenine significantly reduced spontaneous and passive activities of mice, but had no significant effect on sleep time of mice. It has a certain antagonistic effect on strychnine, reducing the onset threshold of strychnine in mice, but it cannot antagonize pentylenetetrazol. Dogs and monkeys taking sinomenine 45-90 mg/kg orally also have significant sedative effect. Low dose of * * * 5 ~10 mg/kg * * can prolong the latency of conditioned reflex in mice and cats, and the conditioned reflex part disappears, and then the unconditioned reflex part disappears. It shows that it can inhibit the exciting process of higher-order nerve activities, and sinomenine can also eliminate the "anger" reaction caused by electric mice, which seems to have a * * * effect.
Antitussive effect
Sinomenine has antitussive effect, and its antitussive effect is similar to codeine in ***S02 method in mice and * * * * electric nerve method in cats. For guinea pigs, the effect of S02 method is only 1/4 of codeine. Promethazine can enhance its antitussive effect.
The taboo of ivy
Traditional document Compendium of Materia Medica: non-toxic. It also says, "The whole body itches after taking it, which is unacceptable."
Toxicological test 1, LD50, LD50 of mice fed with sinomenine decoction was 580 mg/kg 5 mg/kg. 2. Toxic reaction: dogs and monkeys took 45mg/kg and 95mg/kg orally, respectively, which showed sedation and mild gastrointestinal reaction. Subacute toxicity test: there is no change in liver and renal function. Because of the rapid drug resistance, the toxicity is obviously reduced after continuous medication. It shows that the toxicity is relatively small.
Clinical observation shows no toxicity. There is no uncomfortable reaction after the conventional dose of water decoction. There is no obvious adverse reaction after long-term use. Overdose has adverse reactions such as nausea, pantothenic acid, stomachache and rash. It can be used equally with stomach drugs and antiallergic drugs to reduce adverse reactions. Clinical use of sinomenine tablets, some patients have allergic dermatitis, stomach pain and leukopenia and other adverse reactions.
Taboo: Use with caution for those with spleen and stomach deficiency and cold.
Medicinal value of sinomenine
1, treating rheumatic joint pain
Ivy roots are three or two, and self-defense is one or two. Fu Rui, put in a bottle of wine and boil it. * * * "Outline" quoted "Puji Fang" * * * Caulis Sinomenii and Caulis Sargentodoxae each 65438±05g, decocted in water, and taken in moderation with wine; Or sinomenine 30-60g, Cinnamomum cassia twig 3g for upper limb pain and Achyranthes bidentata 6g for lower limb pain, decocted with appropriate amount of yellow wine water and taken after meals. * * * Zhejiang medicinal flora * * *
2. Cure all the wind
Pick vines in February and March, no matter how much, put them in the kettle, simmer for seven days and nights, become paste, and put them in porcelain bottles. When using, prepare three or five combs to measure the actual situation of people. After taking a teaspoon of wine, pat the patient's palm, and then the whole body will itch, so it is urgent to comb. To relieve itching, drinking cold water will relieve it. Take shelter from the wind for a few days. * * * Lakeside Set Simplified Formula Qingteng Cream * * *
3. Treat joint pain.
The roots or stems and leaves of Aristolochia angustifolia are appropriate, and the decoction often washes the sore spot. * * * Guizhou folk medicine * * *
4, edema, beriberi
This product can dredge channels and promote diuresis, and can be used alone to treat Shanghai syndrome. For edema, it can also be used with Atractylodes macrocephala. Treating wet swelling of beriberi with syndrome of Evodia rutaecarpa and papaya.
5, diuresis
Sinomenine promotes diuresis, purges lower energizer, and causes blood to be damp and hot. It can be used for treating rheumatic edema, beriberi, rheumatic joint pain, mouth-eye deviation, carbuncle swelling and malignant sores. Records of Medicinal Plants in Tianmu Mountain, Zhejiang Province
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