opium

opium

(compendium)

Another name: diyejia (Tang materia medica), opioid, Furong (compendium), and yapian (suixiju diet).

[source] it is formed from the juice of Papaver poppy fruit. See the article "Poppy" for plant morphology.

[collection] usually, when the fruit is fully grown but not mature, and the pericarp is still green or slightly yellow (at this time, the content of morphine in milk is the highest), use a sharp knife or a special serrated cutter to cut the pericarp lightly (straight or oblique) in the sunny evening, and cut off the milk tube scattered in the pericarp tissue. The white milk exudes into drops from the self cutting seam, and gradually turns from reddish to brown in the air The next morning, each fruit can be scraped 3-4 times. The scraped opium is wrapped in poppy leaves and dried in the dark.

[medicinal materials] opium has different shapes, such as round, cake, brick or irregular shape, brown or black, waxy, with poppy leaves or paper on the outside. It is soft when fresh, but hard when stored for a long time. The odor is special, narcotic, bitter and special.

[chemical constituents] the content of total alkaloids in opium is 10-25%, mainly in the form of maikangate. The main opiate alkaloids produced in Japan are morphine 5-24%, narcotine 4-7%, codeine 0.4-1%, tibagon 0.4-0.8%, papaverine 0.4-0.7%, and narcoryin 0.2-0.5%. In addition, there are codanine, cotanine, cryptopinine, scopolamine, hydrocortisone, lanlengpin, laudanidine, laudanine, laudanine, maikangding, papaverine, neopine, oxidized narcotine, chlorphenamine, chlorphenamine Papaverine, jatrophylline, pseudomorphine, primordine, opium yellow.

Some alkaloids were also found in opium, such as Corydalis skrjabini, d-isoboldine, bicuculline, isocorydalis quatine, hydroxystreptomycin, 7-oxydihydrotibain, corydalis tuber alkaloid, Magnolia alkaloid, Coptis chinensis, berberine, sanguinarine, papaverine, papaverine B, papaverine C, n-methyl-14-o-demethylepivioline, quatraudine and 6-methyl codeine .

Opium also contains maikangning, stigmasterol, cyclomagnolone, cyclomagnolone, cyclomagnolone ester, cyclomagnolone ester, β - sitosterol, mixture of c27-c35 hydrocarbons, cyclomagnolone, cyclomagnosterol, 10-29 alcohol, β - sitosterol-d-glucoside, β - sitosterol-d-glucoside Monopalmitate.

[pharmacological action] opium contains more than 20 kinds of alkaloids, but only morphine, codeine, papaverine and narcotine are commonly used in clinic. The content of other alkaloids is low, which has no effect on the action of opium.

① Analgesic effect

Morphine has significant analgesic effect and high selectivity. During analgesia, not only the patient's consciousness is not affected, but other senses also exist. Its effect on persistent pain (chronic pain) is better than that on intermittent sharp pain. If the dosage is increased, it is also effective for sharp pain. Besides increasing pain threshold, the change of pain response is also an important factor. After using morphine, the pain stimulation was still felt, but the normal reactions such as tension, fear and withdrawal had disappeared, and the patient was "painful but not bitter". If the unpleasant emotions often accompanied with pain are cancelled, the pain will be more tolerable. The analgesic effect of codeine is about 1 / 4 of that of morphine.

② Hypnotic effect

Morphine has hypnotic effect, but sleep is shallow and easy to wake up, can not be regarded as a real hypnotic. Codeine did not cause sleep.

③ Respiratory depression and antitussive effect

Morphine has a highly selective inhibitory effect on the respiratory center. When the dose is lower than the analgesic dose, it can inhibit the respiration. At this time, the respiratory center is less sensitive to CO2, which can be used to treat dyspnea (cardiac asthma). The first manifestation of respiratory depression is the decrease of frequency. At this time, due to the compensatory effect of increasing depth, the ventilation volume has no effect. When intoxicated, because the inhibition deepens and the frequency decreases too much, the depth of respiration increases and cannot be compensated, resulting in severe hypoxia. Respiratory center paralysis is the direct cause of death of morphine poisoning. The effect of codeine on respiratory depression is much less than that of morphine.

Under the action of morphine, the chemoreceptor reactivity of carotid body is increased, which is the result of hypoxia caused by respiratory depression. In morphine poisoning, the maintenance of respiration depends on the stimulation of chemoreceptors by hypoxia. If pure oxygen or high concentration oxygen is inhaled at this time, automatic breathing can be stopped immediately, so artificial respiration should be performed when oxygen is given. Papaverine can act on carotid sinus and aortic body chemoreceptors and slightly stimulate respiration, but it has no significance in treatment.

Morphine also has a strong antitussive effect, mainly due to the inhibition of cough center. For example, 2-4 mg of morphine can produce significant antitussive effect, while 5-15 mg of morphine is required for analgesia. Codeine is the most commonly used antitussive drug because its antitussive effect is not as strong as that of morphine, but it is satisfactory enough without many disadvantages of morphine (strong addiction, easy constipation, inhibition of breathing, etc.). Narcotine has the same antitussive effect as codeine, but it has no other central inhibitory effect, does not produce mental or physical dependence, does not inhibit breathing, and has the effect of stimulating breathing in large quantities in animals.

④ Effects on cardiovascular system

The therapeutic dose had no effect on the blood pressure, heart rate and rhythm of patients in supine position, and had no significant effect on the vascular motor center. But postural hypotension may occur. Morphine can relax the peripheral blood vessels and release histamine. The combination of morphine and phenothiazines has a synergistic effect on respiratory depression and may cause hypotension. It is necessary to pay attention to the reports of death caused by morphine in patients with cor pulmonale.

Papaverine can relax all kinds of smooth muscle, especially the large artery smooth muscle (including coronary artery, cerebral artery, peripheral artery and pulmonary artery). When there is spasm, the relaxation effect is more significant. It can be used for peripheral artery or pulmonary embolism. It can dilate coronary artery and increase coronary flow for a long time in dogs, but it is not enough to prevent angina pectoris because of its positive muscle strength and lower systolic blood pressure. High dose can inhibit myocardial conduction and prolong refractory period. The treatment dose has no significant effect on ECG. High dose can prevent cardiac fibrillation caused by chloroform epinephrine.

Nacotine also inhibited smooth muscle and myocardium, but these effects did not appear at the antitussive dose.

⑤ Effects on digestive tract and other smooth muscle organs

Morphine can cause constipation, mainly due to the gastrointestinal tract and its sphincter tension increase, coupled with the reduction of digestive secretion and constipation will be slow, so that the gastrointestinal contents forward movement is greatly delayed. The treatment dose of morphine increased the biliary tract pressure significantly, and the patient felt uncomfortable in the upper abdomen, even biliary colic. Morphine can make sphincter of Oddi constrict and prevent emptying, so it can increase the pressure in the tube. Codeine's inhibitory effect on intestinal peristalsis is much weaker than that of morphine, and it is not easy to cause constipation.

Although a large amount of morphine can constrict the bronchus, it rarely occurs in the treatment dose. There are reports of death caused by morphine during the occurrence of bronchial asthma, so morphine is forbidden.

Papaverine can inhibit intestinal smooth muscle, but the effect is very weak, and it can not eliminate the bile duct spasm caused by morphine, and it has no effect on the asthma (human) caused by methacholine.

Morphine also has a significant effect on mydriasis, which can be used as one of the diagnostic criteria for morphine poisoning.

⑥ Others

Repeated application of morphine can produce tolerance, but only the central inhibitory effect can be tolerated, such as analgesia, hypnosis, respiratory inhibition, etc., while its excitatory effect and its effect on pupil and smooth muscle can not be tolerated. Therefore, people with morphine addiction are often constipated and their pupils shrink. Generally, the tolerance is produced after 2-3 weeks of continuous administration. The tolerance disappeared within a few days to two weeks after drug withdrawal. If it is used again, the second tolerance is faster. For those addicts who have acquired tolerance, the dosage can be 20-200 times of that of common treatment, even 5 grams per day without poisoning. Tolerance is probably due to the decreased sensitivity of some nerve tissues to morphine.

Those who take morphine continuously for more than 2 weeks can become morphine patients, and sometimes they can become addicted after taking morphine for several days. After addiction, the patient will appear euphoria (euphoria is a kind of emotional change, the patient is in a special "happy" state, carefree, and indifferent to the mental and physical pain. This special "happy" state is an important cause of addiction. In the euphoria of morphine, the ability of correct judgment and reasoning still exists. At the same time, the critical attitude to his personal behavior and behavior is completely preserved, and his motor function is also barrier free. His performance is like loneliness and indulge in fantasy. If you don't get morphine at that time, you will have severe withdrawal symptoms 5 to 8 hours later. Addicts are very depressed and excited, and their degree can reach paroxysmal crying and shouting, constantly begging for morphine. Even yawning and sneezing, tears, cold sweat. Diarrhea and vomiting can also occur. I can't sleep. After 2-3 days, most of the symptoms subsided. Sometimes there are cycle collapse and loss of consciousness. If enough morphine was given, all withdrawal symptoms disappeared immediately. Abstinence treatment of morphine addiction is difficult and easy to relapse.

The euphoria and addiction of codeine are very low. Papaverine and narcotine are not addictive.

[toxicity] the adverse reactions of morphine were headache, dizziness, nausea, vomiting, constipation, urgency and dysuria, sweating, biliary colic, etc., but the most dangerous was respiratory depression. Acute morphine

Chinese PinYin : Ya Pian