Galanthamine hydrobromide

The preparation of Galantamine hydrobromide refers to therapeutic agents that actively influence the processes of nerve impulse transmission, stimulating and supporting synaptic acetylcholine neurotransmission in the peripheral nervous system of man. Analogues of this anticholinesterase are Nivalin, Galantamine and Galantamine hydrobromic.

[1], [2], [3]

Indications of the galanthamine hydrobromide

The list of pathologies treated with Galanthamine hydrobromide includes:

• myopathies (hereditary muscle dystrophies, neuromuscular syndromes of neurological diseases);
• myasthenia gravis (muscle weakness);
• neuritis, polyneuritis, radiculitis and radiculoneuritis with loss of sensitivity and motor impairment;
• poliomyelitis (residual events);
• spastic forms of cerebral palsy;
• infantile cerebral palsy and birth paresis of newborns;
• enuresis;
• residual (residual) paresis after cerebrovascular accident, including stroke;
• psychogenic and spinal impotence;
• light and moderate manifestations of neuropsychological conditions with senile dementia (senile dementia) as Alzheimer's.

The use of galanthamine hydrobromide is fully justified in the case of the occurrence of such postoperative neurological syndromes as peripheral paralysis and paresis (including atony of the intestine and bladder).

In addition, Galanthamine hydrobromide is used as an antidote for poisoning (or overdose) parasympatolytic drugs containing atropine and similar substances.

[4], [5], [6],

Release form

Galanthamine hydrobromide is available in the form of 0.25%, 0.5% and 1% solution for injection - in ampoules of 1 ml (in packs of 10 ampoules).

[7]

Pharmacodynamics

The active substance of this drug is a nitrogen-containing natural compound isolated from the bulbs of snowdrop Galantus Woronowi A. Los. - alkaloid galantamine (in the form of hydrobromide).

Galantamine hydrobromide reduces the activity of cholinesterase, an enzyme that participates in the hydrolysis (cleavage) of acetylcholine, a derivative of choline, necessary for the transmission of nerve impulses. Due to the acceleration of the cleavage of acetylcholine in cholinergic synapses, the effect of the cholinesterase enzyme is temporarily blocked. As a result, the content of acetylcholine in neuromuscular synapses increases. This leads to the fact that the excitation of the nerve fiber increases, and the process of transmission of the nerve impulse to the muscle tissues becomes more intense. 

[8], [9], [10], [11]

Pharmacokinetics

After parenteral administration of the preparation Galanthamine hydrobromide under the skin, it is rapidly absorbed into the bloodstream, while binding to plasma proteins is negligible. The drug penetrates the blood-brain barrier.

The therapeutic concentration of the active substance in the blood plasma is observed approximately 25-30 minutes after the injection. Metabolism proceeds gradually, the half-life of products of biological transformation is almost five hours. Metabolites of galantamine hydrobromide are excreted by the kidneys with urine.

[12], [13], [14],

Dosing and administration

The use of Galanthamine hydrobromide is a subcutaneous injection. Dosage is determined by the doctor individually. The standard dose of 1% solution of the drug for adults is 0.25-1 ml once or twice a day. The maximum daily dose is 2 ml of a 1% solution.

The dose for children depends on their age: up to 2 years - 0.1-0.2 ml (0.25% solution), 3-5 years - 0.2-0.4 ml; 7-8 years - 0,3-0,8 ml; 9-13 years - 0.5 ml (0.25% solution). In 14 years and older - 1 ml of a 0.5% solution. The duration of the course of treatment is from 10 to 30 days.

[18], [19], [20], [21], [22]

Use of the galanthamine hydrobromide during pregnancy

When pregnancy is possible in the event that the potential benefit to the mother exceeds the possible risk to the fetus.

Contraindications

The use of galanthamine hydrobromide is contraindicated in angina pectoris and heart failure, a decrease in heart rate (bradycardia), bronchial asthma, epilepsy, and also in the presence of involuntary contractions of limb muscles (hyperkinesis) in patients.

Side effects of the galanthamine hydrobromide

Treatment with the help of this drug, as a rule, does without undesirable side effects.

But individual hypersensitivity to galantamine, as well as its overdose, which have symptoms such as dizziness, slow heartbeat (bradycardia) and impaired salivary gland function (increased salivation and drooling) is possible. In this situation, subcutaneous or intravenous administration of atropine sulfate (1 ml of a 0.1% solution) is recommended.

[15], [16], [17],

Overdose

Symptoms: muscle weakness or fasciculation, severe nausea, vomiting, abdominal cramping, increased salivation, lacrimation, urinary and fecal incontinence, severe sweating, decreased blood pressure, bradycardia, collapse and convulsions. Pronounced muscular weakness in combination with hypersecretion of the mucous membrane of the trachea and bronchospasm can lead to a lethal blockade of the airways.

Postmarketing experience (random intake of 32 mg of the drug): development of bidirectional-spindle ventricular tachycardia, prolongation of the QT interval, ventricular tachycardia with short-term loss of consciousness.

[23]

Storage conditions

Storage conditions: Galanthamine hydrobromide is listed in list A, it should be stored in a dark place at room temperature.

[24], [25],

Shelf life

The shelf life of the drug is indicated on its packaging.

[26], [27], [28], [29]