Nature and flavor

"Handbook of Commonly Used Chinese Herbal Medicines in the North": bitter, pungent, hot, and highly toxic.

Functions and Indications

Activating blood circulation and removing blood stasis, driving wind and removing dampness, relieving pain and reducing swelling. It can be used to treat bruises, rheumatic joint pain, toothache, abdominal pain caused by food accumulation, dysmenorrhea, carbuncles and chilblains in women.

① "Handbook of Commonly Used Chinese Herbal Medicines in the North": Promotes blood circulation, removes blood stasis, and relieves pain. Treat rheumatic joint pain and menstrual pain.

② "Shaanxi Chinese Herbal Medicine": promotes blood circulation and removes blood stasis, removes rheumatism, relieves pain, reduces swelling and poisons, removes putrefaction and promotes muscle growth, stops bleeding, treats bruises, rheumatoid arthritis, waist and leg pain, and strain. Malignant sores and carbuncles, nameless venomous swellings, chilblains, and poisonous snake bites.

Usage and Dosage

External use: grind into powder for application, grind into juice and apply, decoct in water and wash, or grind into powder and put in plaster for application, internal use: decoct in soup, 2 to 3 centimeters; or Grind into powder.

Note

① "Shaanxi Chinese Herbal Medicine": Avoid hot food, cigarettes, and alcohol for two hours after taking the medicine.

② "Selected Chinese Herbal Medicine from Shaanxi, Gansu and Ningxia": Pregnant women should not take it.

Attached Recipe

①Treatment of rheumatic joint pain: an iron rod and a hammer of two to three qian. Grind the powder, add one ounce of white wine, light it with fire, dip it in and wash the affected area, once a day. ("Shaanxi Chinese Herbal Medicine") Two iron rods hammer three centimeters. Decoction in water or grind into powder and drink as a drink. ("Selected Chinese Herbal Medicines from Shaanxi, Gansu and Ningxia Qing")

② To treat toothache: Grind it into powder with an iron rod and hammer, use a toothpick and cotton, soak it in water and then dip five centimeters of the powder into the medicine, apply it to the affected area, but do not swallow it. ("Handbook of Commonly Used Chinese Herbal Medicines in the North")

③Treat lumps and abdominal pain caused by food accumulation: three points for iron rod hammer and two points for araceae. Grind it into powder and sprinkle it on the plaster and stick it on the navel. ("Shaanxi Herbal Medicine")

④ Treatment of scrofula (unbroken): Grind the juice with vinegar with an iron rod and hammer, and apply it to the affected area.

⑤ Treatment of frostbite: Grind the juice with water using an iron rod and hammer, and apply it to the affected area.

⑥ To treat knife wounds: 3 qian each of iron rod hammer and taro qi, 5 fen of borneol, and 1 fen of musk. The drug is made into fine powder and applied externally to the injured area. (The following prescription is from "Shaanxi Chinese Herbal Medicine")

Pharmacological effects

Analgesic effect

The total base of this product has significant analgesic effect. The pain intensity is 43.7 times that of morphine, and its main effective analgesic ingredients are aconitine, 3-acetylaconitine, deoxyaconitine, etc. The effects of aconitine can be found under Aconite and Aconite. 3-acetyl aconitine and deoxyaconitine both have significant nonalgesic activity. The dose ID50 of the subcutaneous injection of deoxyaconitine that inhibits the writhing reaction in mice by the acetic acid writhing method is 0.22±0.06mg/kg, and that of 3-acetylaconitine is 0.13±0.03mg/kg; while the dose measured by the hot plate method The analgesic ED50 of mice with intraperitoneal injection were 0.41±0.10mg/kg and 0.24±0.05mg/kg respectively, and the analgesic therapeutic index was 6.37 and 4.60 respectively.

Anti-inflammatory effect

The total base of this product, as well as aconitine, 3-acetylaconitine, and deoxyaconitine all have significant anti-inflammatory activity. Total alkali 0.15 mg/kg, aconitine and 3-acetyl aconitine 0.05 mg/kg have significant inhibitory effects on egg white and formaldehyde-induced plantar swelling in rats, but have no significant effect on cotton ball granulation tissue hyperplasia. Deoxyaconitine also has a significant inhibitory effect on a variety of acute exudative edematous inflammations. Intraperitoneal or subcutaneous injection of 0.2 mg/kg can significantly inhibit the swelling of rat soles caused by carrageenan, formaldehyde, etc., and inhibit Hyperpermeability of capillaries in rat skin caused by histamine or abdominal cavity of mice caused by acetic acid. 0.8 mg/kg can also inhibit ear inflammation in mice caused by croton oil, but it has no effect on croton oil granuloma or cotton ball tissue. There was no obvious effect on proliferation. For carrageenan-induced plantar edema in rats, the ED50 of intraperitoneal injection of deoxyaconitine is 0.42±0.06mg/kg, and the therapeutic index is 6.38, while the ED50 of 3-acetylaconitine measured by the same method is 0.12± 0.02mg/kg, the therapeutic index is 5.92.

Local anesthetic effect

This product's total alkali, aconitine, and 3-acetyl aconitine all have significant local anesthetic effects, and are effective when injected intramuscularly or intradermally. The local anesthetic strength of total base is 14 times that of procaine hydrochloride and 159 times that of procaine hydrochloride.

Antipyretic effect

Intraperitoneal injection of 3-acetylaconitine 0.04mg/kg or deoxyaconitine 0.24mg/kg into rabbits with fever caused by typhoid vaccine has significant antipyretic effect. The thermal effect starts 30 minutes after injection and lasts for more than 3 hours.

Arrhythmogenic effects

Similar to aconitine, 3-acetylaconitine and deoxyaconitine also have arrhythmogenic effects, but intravenous injection in mice induces cardiac rhythm. The dosage of abnormality is higher than that of aconitine, 3-acetyl aconitine is 2.85 times that of aconitine, and deoxyaconitine is 7.2 times that of aconitine, and the induction success rate is also much lower. And the respiratory depression is only 38% that of aconitine. The arrhythmia-inducing dose of 3-acetyl aconitine in rats by intravenous injection is 0.097 mg/kg. 6. In vivo process The blood drug time curve of 3-acetylaconitine conforms to the open three-compartment model. Among the various tissues, the gallbladder has the highest content, followed by liver, kidney and lung. Small amounts of drugs can cross the placenta and enter the fetus. After intravenous injection, it is mainly excreted in the urine, most of which are excreted in the form of metabolites, and some are excreted in the form of original substances.

Toxicity

The LD50 of 3-acetyl aconitine in mice by gavage, subcutaneous injection, intraperitoneal injection, and intravenous injection were 2.5 mg/kg, 0.7 mg/kg, and intravenous injection respectively. 0.47mg/kg, the absolute lethal dose of intravenous injection in rats was 0.41mg/kg; another report showed that intraperitoneal injection in rats was 0.71±0.17mg/kg, and that in mice was 1.10±0.12mg/kg; there was also a report of oral administration of mice , the LD50 of subcutaneous injection, intraperitoneal injection and intravenous injection are 3.09mg/kg, 0.70mg/kg, 0.58-0.62mg/kg and 0.40mg/kg respectively. In rats, the LD50 of intragastric injection, subcutaneous injection and intraperitoneal injection is 2.30mg/kg. , 0.49mg/kg and 0.31mg/kg. Symptoms of poisoning include salivation, increased tear secretion, vomiting-like reactions within 5-15 minutes, ataxia, limb weakness, crawling and lying, slow breathing, etc., paroxysmal convulsions before death, and suffocation within more than 15 hours. die. The safe dose for intravenous injection into rabbits is 10 μg/kg, for anesthetized dogs it is 10 μg/kg, for intramuscular injection into rabbits it is 20 μg/kg, and for awake dogs it is 22 μg/kg. Increasing the dose may cause salivation, respiratory depression, arrhythmia, decreased blood pressure, etc. The lethal dose of intravenous injection into rabbits was 30 μg/kg and no death was found. 3-Acetylaconitine has accumulation properties, and its toxicity increases with continuous administration. The subacute toxicity of 3-acetyl aconitine in rats, rabbits, and dogs mainly damages the myocardium, causing myocardial cell degeneration, mild damage to liver cells, and blocking the development of sperm cells in some rats. However, no teratogenicity has been found in mice and rabbits. effect, but has some embryotoxicity. Atropine and atropine plus artificial respiration have obvious rescuing effects on acetyl-aconitine poisoning. The LD50 of intraperitoneal injection of deoxyaconitine was 2.61±0.30mg/kg in mice and 2.68±0.75mg/kg in rats.