Scopolamine is an organic substance with chemical formula CseventeenHtwenty-oneNOfour, a tropane alkaloid, which exists in solanaceous plants.In 1892, E. Schmidt was first separated from scopolamine.The effect is similar to atropine. Its mydriasis and inhibition of gland secretion are stronger than atropine. It has an exciting effect on the respiratory center, but has a significant inhibitory effect on the cerebral cortex. In addition, it has the effects of expanding capillaries, improving microcirculation, and resisting seasickness and carsickness.
Chinese name
Scopolamine[2]
Foreign name
Scopolamine[1][5]
chemical formula
CseventeenHtwenty-oneNOfour[1]
molecular weight
three hundred and three point three five three[2]
CAS login number
51-34-3[2]
EINECS login number
200-090-3
Melting point
59 ℃[2]
Boiling point
460.3 ℃
Water solubility
high
Density
1.31 g/cm³
Flash point
232.2 ℃
Application
Inhibition of gland secretion
Security description
S25；S45
Hazard symbol
R26/27/28[2]
Hazard description
Highly toxic
Chinese Pinyin
dōng làng dàng jiǎn
PSA
sixty-two point three zero zero zero zero
Precision quality
three hundred and three point one four seven zero zero
Storage conditions: low temperature, ventilated and dry in the warehouse
security information
Hazard category code: R26/27/28
Safety instructions: S25;S45
Dangerous goods sign: T+[2]
Molecular structure data
1. Molar refractive index: 80.44
2. Molar volume (cmthree/mol）：230.9
3. Isotonic specific volume (90.2K): 632.8
4. Surface tension (dyne/cm): 56.3
5. Polarization (10-24cmthree）：31.89
Drug description
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Main purpose
Scopolamine is an alkaloid with the strongest pharmacological effect in belladonna, which can be used to blockparasympathetic, can also be used asCentral nervous system inhibitor。Its action is similar to belladonnaine, but its action is stronger and shorter.Its hydrobromide is generally used clinically, which can be used for anesthesia, analgesia, cough, asthma, motion sickness, and also for controlling rigidity and tremor of Parkinson's disease.
survey
Scopolamine (French, English: Scopolamine, German: Scopolamine), also known as L-fairy amine, is a kind of scopolamine alkaloid drug, which has the effect of muscarinic receptor antagonist.Scopolamine acts as aCompetitive antagonistPlay its role;Therefore, it is classified as anticholinergic drugs and anti muscarinic drugs.It is a drug of hyoscyamane alkaloids manufactured artificially under the action of muscarinic receptor antagonists.The drugs mainly come from solanaceous plants, such as henna, mandala, etc.Although the drug is highly toxic, it has even been used as a crime;There is even another name of "devil's breath", but in fact, because of its nature as an acetylcholine inhibitor, it can be used as a legal medical application in very small doses;For example, postauricular patches for carsickness, postoperative nauseaIrritable bowel syndromeGastrointestinal spasm, renal or biliary tract spasm and administration before operation to reduce respiratory tract secretion.
pharmacological action
This product is a tertiary amine anti muscarine drug.Its action is generally similar to atropine, and has effects on the central and surrounding areas.It has a stronger inhibitory effect on saliva secretion than atropine, and usually slows the heart rate rather than accelerates it, especially in small doses.Its effect on the central nervous system is different from that of atropine, which can inhibit the cerebral cortex and produce lethargy and amnesia.The inhibitory effect on eye smooth muscle and gland secretion is stronger than atropine.This product is a peripheral anticholinergic drug. In addition to its antispasmodic effect on smooth muscle, it can also block the ganglia and neuromuscular junction, with a weak effect on the central nervous system.The eye function is similar to atropine. Its mydriasis, paralysis regulation and secretion inhibition are twice as strong as atropine, but the duration is short.Contrary to atropine stimulating the brain, this product shows significant sedative effect.
The peripheral effect of scopolamine is similar to that of atropine. It has a stronger inhibitory effect on the secretion of salivary glands, bronchi and sweat glands than atropine. It has a faster effect on mydriasis and paralysis regulation than atropine, but the effect disappears faster and has a weaker effect on the smooth muscle of heart, intestines and bronchi.It also has the effect of relieving vasospasm and improving microcirculation.It has obvious inhibitory effect on the central nervous system at the general therapeutic dose.Hypnotic effect can be produced in large doses.In large doses, central excitatory symptoms such as excitement, restlessness, hallucination or delirium may occur, but they will soon fall asleep.The greater the dose (0.08mg/kg intravenous injection), the more significant the cortical inhibition.If combined with chlorpromazine, paralysis may occur quickly.Scopolamine has stronger respiratory excitation, anti motion and anti paralysis effects than atropine.
Pharmacokinetics
This product is absorbed rapidly from gastrointestinal tract after oral administration.It is almost completely metabolized in the liver, and only a small part of it is discharged with the urine.It can penetrate the blood cerebrospinal fluid barrier and the placenta.The transdermal preparation of this product is also easy to absorb.Its t1/2 is 2.9h, and its distribution volume is 1.7L/kg.0.5% solution of this product can produce maximum mydriasis for 20 minutes, lasting for 90 minutes, and recover the level of the eyes in 3 to 7 days.The maximum ciliary muscle paralysis occurred in 40 minutes, lasted for about 90 minutes, and gradually recovered after 72 hours.0.5~1h after the injection of scopolamine, the plasma volume was about 0.5% of the total amount introduced, and the concentration dropped rapidly after reaching the peak, t1/2 was 1.35h.Its distribution in the body is relatively high in the brain, liver and lung. Its concentration gradually increases from a few minutes to 30 minutes after administration, and maintains a certain concentration for 2-3 hours. Its effect on the brain is large and lasting, with the peak at about 2 hours, indicating that it can successfully pass the blood cerebrospinal fluid barrier.After injection of the drug, the urine output in 30 minutes has reached 27.15% of the total amount of introduction, 49.5% in 1 hour, 75.88% in 2 hours, and 92.8% in 48 hours.
Dosage form
1. Tablets: 0.2mg, 0.3mg;
2. Injection: 0.3mg (1mL), 0.5mg (1mL);
3. Eye ointment: 0.15%, 0.5%, 1%;
4. Eye drops: 0.25% ～ 1% (5mL).
5. Patch: 1.5mg.
indication
1. It is used for pre anesthesia administration, motion sickness and Parkinson's disease.
2. Mitigationsmooth muscle spasm (especially the gastrointestinal tract) and dilate the pupils.
3. Rescue organophosphorus pesticide poisoning.
4. Mainly used for patients with atropine allergy, but also for mild patientsIridocyclitis。
Prohibited for glaucoma, prostatic hypertrophymyasthenia gravisSevere heart disease, organic pyloric stenosis, gastrointestinal obstructive diseaseReflux esophagitis、Ulcerative colitisorToxic megacolonpatient.The poisoned can be rescued and treated symptomatically with cholinergic drugs.
Usage and dosage
1. Take 0.3mg orally 0.5 h before departure. If necessary, take it once every 6 hours. Take it three times at most within 24 h.Children aged 4-10 years can be given 75-150 μ g, and children aged>10 years can be given 150-300 μ g.Scopolamine can also prevent motion sickness through transdermal preparation. This preparation can be applied behind the ear, and 1mg can be used within 3 days.The paste shall be applied 5~6h before departure.This paste can also be used for adults to prevent postoperative nausea and vomiting.
2. Scopolamine can also be administered subcutaneously, intramuscularly or intravenously: for vomiting, 0.3-0.6 mg can be administered each time.Intravenous injection should be diluted with water for injection.
3. Scopolamine 0.2~0.6 mg is often combined with subcutaneous or intramuscular injection of opioid total alkaloids as a drug before general anesthesia (30~60 min before anesthesia induction).
4. Scopolamine 0.25%~1% solution or eye ointment solution can play the role of mydriasis and cycloplegia.It takes effect later than atropine and lasts for 3 to 7 days.
5. Bronchial asthma and asthmatic bronchitis: 0.3-0.5mg intravenous injection each time, repeated several hours later if necessary, and once a day thereafter.
matters needing attention
1.（1）PhysostigmineIt can relieve the poisoning reaction of belladonnas and can be used as an antidote.(2) Diazepam phenobarbitalPhenobarbital sodiumIt can antagonize the central excitatory effect of scopolamine and can be used for the treatment of scopolamine drug poisoning.(3) Copper sulfate 0.3~0.5g, dissolved in 100~250mL water, can be used as an emetic for oral belladonna poisoning.Do not use ipecac or apomorphine to induce vomiting.
2. Others: for motion sickness, preventive medicine has good effect, anddiphenhydramineCombined use can increase the curative effect.In order to avoid systemic absorption during ophthalmic administration, finger pressure can be applied to the lacrimal sac for 2-3 minutes after instillation.The depth of anterior chamber should be estimated before administration to avoid inducingAngle closure glaucoma。When used in ophthalmology, its toxic reaction rate is higher than other anticholinergic drugs.Therefore, it should not be used as the first choice drug.Avoid driving or engaging in dangerous activities during medication.
3. In case of allergic reaction, the drug should be stopped in time.
4. Avoid nerves and blood vessels during injection.If it is necessary to inject repeatedly, it should be injected alternately from left to right instead of at the same site.
Adverse reactions
1. Tachycardia is a common adverse reaction, especially when the dosage is large.There are also reports of hypotension.
twocentral nervous system: When used in large doses, it can cause dizziness, restlessness, tremor, fatigue and difficulty in movement.Transdermal administration can also cause drowsiness, restlessness, memory impairment, hallucination and confusion.Children are more likely to have disorientation, irritability, confusion, hallucination and tremor than adults.There are reports of coma, high fever and convulsion.
3. Digestive system: dry mouth, constipation.
4. Urinary/reproductive system: it can cause dysuria and urinary retention, especially for elderly patients.
5. Eyes: long-term use of eye preparations can cause local irritation, namely conjunctivitis, vascular congestion, edema andEczematous dermatitis。In addition, hallucinations can also occur.It has the function of mydriasis and can cause blurred vision and photophobia.At higher doses, ciliary paralysis may also occur.Drug administration through skin may cause dry, red or itchy eyes, and may also causeAcute angle closure glaucoma。Occasionally, the pupil size and esotropia are caused.
6. Skin: skin adhesive can cause skin rash, erythemaContact dermatitisEtc.
7. Withdrawal symptoms: some patients have withdrawal symptoms after discontinuing scopolamine skin paste, including dizziness, nausea, vomiting, headache and balance disorder.These withdrawal symptoms are more common in patients who have been taking drugs for more than 3 days.Occasionally, psychosis is caused by drug administration through skin.
Drug response
one
Physostigmine, an aphrodisiac, can relieve the poisoning reaction of belladonnas and can be used as an antidote.
two
Amphetamine and scopolamine have synergistic central excitatory effect.
three
Tolazoline and scopolamine have synergistic effect.
four
Diazepam phenobarbital sodium can antagonize the central excitatory effect of scopolamine and can be used for the treatment of scopolamine drug poisoning.
five
Belladonna drugs can delay and reduce the absorption of antipyretic and analgesic drugs, and reduce the antipyretic effect.
six
Hyoscyams have a pressor effect and can reduce the efficacy of antihypertensive drugs.
seven
Belladonna drugs slow gastric emptying and increase digitalis drug absorption. Long term combined use of the two drugs is likely to cause cardiac glycoside poisoning.
eight
Alkaline solution can make belladonna alkaloids hydrolysis invalid.
nine
Dilute hydrochloric acid and belladonna mixture have incompatibility and antagonistic effect, and should not be taken at the same time.
ten
Copper sulfate can be used as an emetic for oral belladonna poisoning.
eleven
When used together with atropine to treat organophosphorus pesticide poisoning, it can play a synergistic role, but the adverse reactions also increase, so attention should be paid to adjusting the dosage.
twelve
Combined with general anesthetics, it can reduce the secretion of respiratory tract and saliva, prevent inhalation pneumonia, and prevent laryngeal edema and bronchospasm.
Expert comments
According to the clinical observation of curative effect, the drug has similar effect with atropine. Its mydriasis and gland inhibition effect is stronger than atropine, and it has an exciting effect on the respiratory center, but has a significant inhibitory effect on the cerebral cortex. In addition, it has the effects of expanding capillaries, improving microcirculation, and resisting seasickness and carsickness.Scopolamine is an alkaloid extracted from plants of Solanaceae, such as goldenrod, belladonna and scopolamine.When used in ophthalmology, scopolamine has a higher incidence of toxic reactions than other anticholinergic drugs, so it should not be used as the first choice.The mechanism of action of scopolamine is similar to that of atropine. It has obvious bronchiectasis effect, can reduce the secretion of airway mucus, and reduce obstruction, which is beneficial to the patency of airway. Scopolamine has various effects. It also has obvious effects on improving microcirculation, and can relieve vasospasm, which is beneficial toRespiratory inflammationImprovement and recovery.
