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NIVALIN, GALAMTAMINE AN ALKALOID WITH ANTICHOLINESTERASE ACTIVITY !
About Nivalin Galanthamine hydrobromide!
Primary and long-term treatment of mild and moderate dementia. Diseases of the peripheral nervous system - neuritis..
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.
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.
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.
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.
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).
Bronchial asthma, bradycardia, stenocardia, cardiac decompensation, epilepsy, hyperkinesias.
Application and dosage
Nivalin is applied subcutaneously:
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:
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.
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.
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.
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