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加兰他敏 加兰他敏
【又名】尼瓦林，强肌宁Galanthamine, Nivalin, Lycoremine
【作用与用法】
其抗胆碱酯酶作用较弱，易透过血脑屏障，故中枢作用较强，可用于重症肌无力。口服10mg/次，3次/日。但疗效不如新斯的明。
用于小儿麻痹后遗症，口服剂量同上，常采用肌肉注射。每次0.05-0.1mg/kg，每日1次，一疗程2-6周。如疗效欠佳，应停用。此外也可用于儿童脑型麻痹，多发性神经炎，脊神经根炎及外伤性感觉运动障碍。副作用同新斯的明。
【剂型】
片剂：5mg
针剂：1mg 2.5mg 5mg/ml
其他名称】：尼互林 强肌片
主要成分：
性状：针剂,片剂。
功能主治】：用于重症肌无力、进行性肌营养不良、脊髓灰质炎后遗症、儿童脑型麻痹、因神经系统疾患所致感觉或运动障碍、多发性神经炎等。
用法及用量】1.肌注或皮下注射：每次2.5-10ｍｇ，小儿每次每千克体重0.05-0.1ｍｇ，１日１次，１疗程2-６周。2.口服：每次10ｍｇ，１日３次。小儿每日每千克体重0.5-１ｍｇ，分３次服。
不良反应和注意】：超量时，可有流涎心动过缓、头晕、腹痛等不良反应。
生产厂家】
是否医保用药：非医保
是否非处方药：处方
其它：过敏病人应减量。为避免过敏反应发生，剂量一般应由小逐渐增大。癫痫、运动亢进、支气管哮喘、心绞痛、心动过缓者忌用。
加兰他敏
1、从石蒜粗提物中分离高纯度加兰他敏的方法
2、分离加兰他敏的方法
3、一种加兰他敏全合成的新方法
可以用与AD的治疗,是AD治疗目前临床上的首选药
[药品名]氢溴酸加兰他敏
[英文名]Galanthamini Hydrobtomidum
[别名]强肌片、尼瓦林、Nivalin。
[分子式]C17H21O3N·HBr
[性状]为白色结晶性粉末；无臭，味苦。溶于水，微溶于乙醇，不溶于氯仿、乙醚。
[作用与用途]
有抑制胆碱酯酶作用，易于通过血脑屏障进入脑组织，对中枢神经作用较强。与毒扁豆碱、新斯的明、吡啶斯的明比较，其治疗范围广，毒性小，毒罩碱样作用微弱短暂。
主用于重症肌无力、脊髓灰白质炎静止期和后遗症，也用于儿童脑性麻痹、多发性神经炎、脊神经根炎及由于神经系统疾病或外伤所引起的感觉运动障碍等。
[用法与用量]
口服：每次10mg，每日3次；小儿每日O．5-lmg／kg，分3次。
皮下或肌注：每次2．5—10mg，每日1次；小儿每次O．05—0．1mg／kg，每日1次。对脊髓灰白质炎静止期及后遗症可连续用药40-50天，隔30—45天后开始第二个疗程。
[注意事项]
1．应用时宜由小剂量开始逐渐增大，一般20-40天为1疗程或视病人情况而定。如用1—2疗程无效者，应停止使用。
2，癫痫、运动机能亢进、心绞痛、心动过缓及支气管哮喘等患者禁用。
3．偶有过敏或过量时，出现心动过缓、眩晕、流涎及腹痛等。可用阿托品对抗。
[贮藏]
避光，密闭保存。
[制剂]
片剂：每片5mg；
注射剂：每支1ml：1mg、1ml：2．5rng、1ml：5Mg。
COMPOSITION:
Galantamine hydrobromide — 0.10%, 0.25%, 0.50% and 1% solution in in ampoules of 1 ml; 1% injection solution in vials of 5 ml (multidose package); 1% solution collyriurm in vials of 10 ml; and tablets of 1, 5 and 10 mg.
 ACTION
Nivalin, isolated from Galanthus nivalis var. gracilis (snowdrop), is an alkaloid with anticholinesterase action – inhibits the activity of cholinesterase, stabilizes acetylcholine, exhibits cholinomitetic effect. It facilitates the transmission of nerve impulses in the region of the neuromuscular synapses and the synapses of the central and vegetative nervous system. It increases the intensity of the reflex centers of the spinal cord, medulla oblongata and cerebral cortex, i.e. influences all links of the reflex arc: receptors, reflex centers, vegetative ganglia and neuromuscular junctions. Increases the tonus, intensifies its influence upon smooth and striated musculature and influences favorably the glands secretion. Nivalin exerts anticurare effect only towards the non-depolarizing muscle relaxants (those of the pachicurare group with concurrent action – d-tubocurarine, galamine, etc.) and shows potentiating influence in regard to the depolarizing muscle relaxants (succinylcholine, etc.). Its action is antagonistic to morphine and its structural analogs, mainly inhibits their influence on the respiratory center. On instilling Nivalin collyrium in the conjunctival sac, it causes contraction of the pupil and decreases the raised intraocular tension. The preparation does not bring about abruptly expressed spasm of accommodation.
EFFECT: Pharmacologic properties - near to the Physostigmine and Neostigmine. It acts as a powerful reversible inhibitor of the cholinesterine and increases the sensibility of the receptors to the acetylcholine. It facilitates the conduction of the ebullience of the neuromuscular synapses and recuperates the neuromuscular conduction, when blocked by not-depolarizing neural muscular blockers. The Nivalin penetrates through the hematoencephalic barrier, facilitates the conduction of the CNS—impulses and enhances the excitation processes. It enhances the tonicity of the smooth musculature and enhances the secretion of the alimentary and perspiration glands, induces eye pupil contraction. It acts as antagonist towards the suppressing influence on the respiratory centre of the morphine and of its structural analogues. An oral form of Nivalin, suitable to be applied for children having affect on the central nervous system, as a result of generic traumas, infections etc. and as supporting therapeutics in durable treatment of children and adults in the intervals of the injection courses - for myasthenia, progressive muscle atrophy etc.
PHARMACOKINETICS
The Nivalin is resorbed very quickly. The therapeutic plasma concentrations are reached 25-30 minutes after the peroral application and are maintained up to five hours.
INDICATIONS
Poliomyelitis – immediately after the fall of temperature, as well as in the recuperative and residual period; neuritis (especially in facial neuritis), radiculitis, radiculoneurities, polyneuritis, spastic pareses and paralyses and other sequelae of lesions of vascular, inflammatory, toxic and traumatic origin (cerebral apoplexy, meningitis, meningoencephalitis, myelitis, etc.; myopathies – myasthenia gravis pseudoparalytice, progressive muscular atrophy; consequences of diseases of the cerebrum vessels; motional and sensory violations, connected with diseases and traumatic damages of the nervous system; as anticurare means in anesthesiology; diseases with decreased tone of the smooth musculature of the urinary bladder and the gastrointestinal tract. As antidote, in morphine poisoning; in ophthalmology – mainly pronary glaucoma (better results are achieved in its congestive form, especially in acute stage); secondary glaucoma (favorable results are achieved only in separate cases).
CONTRAINDICATIONS
Bronchial asthma, bradycardia, stenocardia, cardiac decompensation, epilepsy, hyperkinesias.
APPLICATION AND DOSAGE
Nivalin is applied subcutaneously:
- For adults: 2.5 – 25 mg daily
- For children, according to age as follows:
- From 1 to 2 years of age: 0.25 – 1 mg (= 0.1 – 0.4 ml of 2.5% solution)
- From 3 to 5 years of age: 0.5 – 5 mg (= 0.2 – 2 ml of 2.5% solution)
- From 6 to 8 years of age: 0.75 – 7.5 mg (= 0.3 – 3 ml of 2.5% solution)
- From 9 to 11 years of age: 1 – 10 mg (= 0.4 – 4 ml of 2.5% solution)
- From 12 to 15 years of age: 1.25 – 12.5 mg (= 0.5 – 5 ml of 2.5% solution)
The indicated doses may in some cases be exceeded, but strictly individually, depending on the tolerance to the preparation and to the severity and duration of the disease. That optimum dose (not always the maximum one) should be determined, which leads to the best therapeutic effect. The tolerance to Nivalin in infancy is great.
The maximum dose for adults may in some cases be applied to bigger children.
The treatment should always begin with the smallest dose, which is gradually increased. When higher curative doses are reached, they are divided into 2 – 3 separate administrations. The course of treatment lasts 50 – 60 days. After an interval of 1 t 1.5 months the therapeutic course may be repeated 2 – 3 times. It is recommended to combine Nivalin treatment with physiotherapeutic procedures (massage, therapeutic exercise, etc.), which should be conducted 1 to 1 ½ hours after Nivalin injection. As anticurare means Nivalin is applied intravenously in the following dosage:
- For adults: 10 – 40 mg (2 – 8 tablets of 5 mg) daily
- For children:
- From 1 to 2 years of age: 0.5 – 3 mg (1/2 to 3 tablets of 1 mg) daily
- From 3 to 5 years of age: 1.25 – 7.5 mg (1/4 to 1 ½ tablets of 5 mg) daily
- From 6 to 8 years of age: 5 – 12.5 mg (1 – 2 ½ tablets of 5 mg) daily
- From 9 to 11 years of age: 5 – 15 mg (1 – 3 tablets of 5 mg) daily
- From 12 to 15 years of age: 5 – 25 mg (1 – 5 tablets of 5 mg) daily
The daily dose is divided into 2 – 3 portions, while in the first 4 – 5 days the minimum initial dose is applied two times daily – in the morning and at noon after meal; in case of myasthenia gravis, the dosage is dividied into 3 portions – morning, noon and at the end of the day. Then the daily dose is increased to the optimal one. This indicated doses may in some cases be exceeded, depending on the tolerance of the preparation and the received effect of the treatment. The tablets should be taken 1 hour after meal. The course of treatment should last 50 – 60 days. The treatment of patients with myasthenia should be carried out strictly individually. After the optimum trating effect is reached, it is recommended to decrease the daily dose so that the minimum dose should be found, which maintains the therapeutic effect. Some days the patient may not take the preparation. In light cases, only tablets are administered; in severe cases, in the intervals between the treatment with injections, the tablets are used.
In ophthalmology – Glaucoma 1 – 2 drops of the collyrium in the eye twice or three times a day in the interparoxysmal period. In the acute period – a continual Nivalin bath on the eye. May be applied in combination with pilocarpine.
SIDE EFFECTS
Increased salivation, perspiration, nausea, vomiting, dizziness, rarely bradycardia. The dose is tehn reduced to the one, which does not cause side effecs, or the treatment is discontinued for 2 – 3 days after which lower doses are applied. If necessary as antidote may be used atropine, or ganglioplegics and myorelaxants. In collyrium – insignificant reddening of the conjunctiva and feeling of light itching may occur.
PACKING
Boxes of 10 and 100 ampoules of 0.10, 0.25, 0.50 and 1% solution of 1 ml; and 1% solution – 5 ml for intravenous application.
Package with 20 and 50 tablets of 1, 5 and 10 mg.
Vials of 10 ml solution – 1% collyrium. |
