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Questions And Answer

• Physical and Chemical Properties

  Galanthamine，White or slightly yellow crystalline powder. Odorless, bitter taste. Melting point 127~129 ℃, [α] D20-118.8 ° (ethanol). Soluble in ethanol, acetone, chloroform, insoluble in benzene, ether and water. After reaction with ammonium molybdate solution, water bath, evaporate, sulfuric acid is added ，it turns to blue-green. Use bulbs of Lycoris squamigera Maxim as raw material, under different acidity ， extract and refine repeatedly with ethanol and chloroform to obtain the product . It belongs to anti-cholinesterase drugs.It is used for sequelae of infantile paralysis and myasthenia gravis. Medicinal use is its hydrobromide. ;

• Alkaloids

  Galanthamine is alkaloid which is extracted from Amaryllidaceae plants Lycoris squamigera Maxim or Lycoris aurea,it is a reversible anti-cholinesterase drug, it is easy for it to go through the blood brain barrier into the brain tissue ,its effect on central nervous system is stronger, it can improve neuromuscular conduction , compared with physostigmine, neostigmine , pyridostigmine , it has wide range of treatment, and low toxicity, muscarinic effects are weak and short-lived. Clinically Galanthamine is used not only for the treatment of myasthenia gravis, polio sequelae resting, but also for children with cerebral palsy, multiple neuritis, radiculitis and sensorimotor disorders caused by nervous system disease or trauma . ;

• Alzheimer's disease drugs

  Alzheimer's disease (AD) is a primary degenerative disease of the central nervous system, and it is more common in the elderly or pre-senile dementia ,it has a latent onset, course of disease is progressive. AD patients account for 55% of patients with dementia. The prevalence rate is 5% to 8%, the prevalence increases with the increase of age . Cause is unknown.
  Cholinergic deficiency plays an important role in the pathogenesis of Alzheimer's disease. Cholinergic system is necessary to maintain the human short-term memory and attention, the cholinergic system dysfunction is associated with certain neuropsychiatric symptoms and behaviors occurring in patients . Cholinesterase inhibitors by inhibiting the degradation of acetylcholine increase the amount of acetylcholine. New evidence suggests that long-term use of cholinesterase inhibitors not only improves cognitive and behavioral disorders, but also may affect the function and survival of neurons. In the current treatment of Alzheimer's disease, cholinesterase inhibitor occupies an important position. Cholinesterase inhibitors have been approved for the treatment of mild to moderate Alzheimer's, such as tetrahydro-amino acridine (tacrine), donepezil (trade name: Aricept), rivaroxaban neostigmine (trade name: Exelon), galanthamine, huperzine.
  Galanthamine is the second generation of AchE inhibitors. It sas a dual mechanism of action, which can better stimulate and inhibit AchE, it can increase brain levels of acetylcholine, slow brain cell function loss process. It can significantly improve mild to moderate AD patients' cognitive function, maintain their daily living skills. After oral ,plasma peak time is 2h, T1/2 is 5~6h. It has quick absorption and well tolerance, its improving cognitive effects are stronger than Brooklyn . Oral doses of each 10mg, 3 times a day.
  The above information is edited by the chemicalbook of Tian Ye. ;

• Clinical application

  Galanthamine hydrobromide is used for myasthenia gravis, muscular dystrophy, polio sequelae, children cerebral palsy, sensory or motor disorders caused by neurological disorders , multiple neuritis. The oral dosage form of the drug can be used for memory impairment, mild to moderate Alzheimer's disease.
  Oral: it is used for myasthenia gravis, muscular dystrophy, multiple peripheral neuropathy treatment: 1 10mg per time, tid. Children 0.5~1mg/(kg · d), 3 times.
  It is used for Alzheimer's disease: initial dose of 1 4mg, bid, for four weeks; maintenance dose of 8mg per time, bid, at least for four weeks; maximum maintenance dose of 1 times 12mg, bid.
  Intramuscular or subcutaneous injection: 2.5~10mg/d, children each 0.05~0.1mg/kg, qd, 1 course is 2 to 6 weeks. Poliomyelitis continuous medication 40~50d, the general course of treatment is 20~40d, the start of the second compartment is 30~45d after treatment. After 1 to 2 courses ,if the condition has not been improved, patients should stop the medication. If it is effective ,3 courses can be used. Application of the dose should be small to large, in order to reduce adverse reactions. ;

• Adverse reactions

  Overdose can lead to bradycardia, dizziness, salivation, and abdominal pain. Atropine confrontation can be used. ;

• Precautions

  1. epilepsy, mechanical obstruction, angina pectoris, bradycardia and bronchial asthma patients are disabled.
  2. Applications should start from small dose, then it is gradually increased, generally 20 to 40 days for treatment is a course,according to the condition . If one or two courses of treatment are ineffective, it should be suspended.
  3. patients with a history of peptic ulcer or using with non-steroidal anti-inflammatory drugs, moderate liver and kidney damage patients, severe heart disease patients should use with caution. ;

• Hazardous characteristics

  Galanthamine has a reversible effect on cholinesterase , its pharmacological and toxicological effects are similar to physostigmine and neostigmine , but it has less effect, and its toxicity is also low. Mouse oral LD50 18.7mg/kg; intraperitoneal injection LD506.42mg/kg; intravenous LD505.2mg/kg~8.0mg/kg. ;

• Uses

  It is used for neurological diseases and trauma-induced movement disorders, multiple neuritis, ramitis and so on. ;

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