Expiration date: 05/2025

Pharmachologic effect:

Galantamine - a selective, competitive and reversible inhibitor of acetylcholinesterase. It stimulates nicotinic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine. It facilitates the conduction of excitation in the neuromuscular junction, and restores neuromuscular conductivity in the case of its non-depolarizing muscle relaxants blockade action type. It increases smooth muscle tone, increases the secretion of digestive and sweat glands, causing cramps. By increasing the activity of the cholinergic system, galantamine improve cognitive function in patients with dementia of Alzheimer's type, but does not affect the development of the disease.

Testimony

• dementia of the Alzheimer type mild or moderate degree
  
• polio (immediately after the cessation of the febrile period, and the recovery period and the period of residual effects)
  
• myasthenia gravis, progressive muscular dystrophy, cerebral palsy, neuritis, sciatica, myopathy.
  

Contraindications

• hypersensitivity to any component of the drug, asthma, bradycardia, atrioventricular block,
  
• hypertension, angina, congestive heart failure, epilepsy, hyperkinesis,
  
• severe renal (creatinine clearance - less than 9 ml / min) and liver (more than 9 points on a scale Child-Pugh) disorders, mechanical intestinal obstruction, chronic obstructive pulmonary disease, obstructive pulmonary disease or recent myocardial surgery on the gastrointestinal tract organs,
  
• obstructive disease or recent myocardial surgical treatment of urinary tract or prostate, children up to 9 years, pregnancy and lactation.
  

Carefully:

light to moderate impaired renal or hepatic function,

sick sinus syndrome or other supraventricular conduction abnormalities,

concomitant use of drugs that slow the heart rate (digoxin, beta-adrenoblokotory), general anesthesia, gastric ulcer and duodenal ulcers, increased risk of erosive and ulcerative lesions of the gastrointestinal tract.

Dosing and Administration

Inside, during a meal, washed down with water. Adults: daily dose is 8-32 mg divided into 2-4 reception. In myasthenia gravis daily dose divided into 3 admission. Children (9 years old): the treatment of polio, cerebral palsy: from 9 to 11 years of daily dose - 4-12 mg, divided into 2-3 doses, from 12 to 15 years, the daily dose is - 4-16 mg divided by 2-4 reception.

Side effects

Since the cardiovascular system: reduction or increase in blood pressure, orthostatic collapse, heart failure, edema, atrioventricular block, atrial flutter or atrial fibrillation, the elongation

QT-interval, ventricular and supraventricular tachycardia, supraventricular arrhythmias, "tides", bradycardia, myocardial ischemia or infarction.

From the digestive system: abdominal distension, dyspepsia, gastrointestinal discomfort, anorexia, diarrhea, abdominal pain, nausea, vomiting, gastritis, dysphagia, dry mouth, increased salivation, diverticulitis, gastroenteritis, duodenitis, hepatitis, perforation of the esophageal mucosa , bleeding from the upper and lower gastrointestinal tract.

From the musculoskeletal system: muscle cramps, muscle weakness, fever.

Laboratory indicators: increase in liver enzymes, anemia, hypokalemia, increased blood sugar, or alkaline phosphatase in the blood.

Hematologic: thrombocytopenia purpura.

From the urinary system: urinary incontinence, hematuria, urinary frequency, urinary tract infection, urinary retention, kalkulez, renal colic.

From the nervous system: often tremor, syncope, lethargy, dysgeusia, visual and auditory hallucinations, behavioral reactions, including agitation / aggression, transient ischemic attack or stroke, headache, dizziness, convulsions, muscle cramps, paresthesias, ataxia, hypo - or hyperkinesis, apraxia, aphasia, anorexia, somnolence, insomnia.

From the senses: rhinitis, epistaxis, visual disturbances, spasm of accommodation, rarely - ringing in the ears.

On the part of the psyche, depression (very rarely - a suicide), apathy, paranoid reactions, increased libido, and delirium.

Common: chest pain, excessive sweating, weight loss, fatigue, dehydration (in rare cases - with the development of renal failure), bronchospasm.

Special instructions

During the period of treatment should refrain from doing jobs that require high concentration and psychomotor speed reactions, including driving.

Treatment of acetylcholinesterase inhibitors is accompanied by a decrease in body weight. Especially it should be borne in mind when treating patients with Alzheimer's disease, which usually occurs weight loss. In this regard, care should be taken of the body weight in these patients.

In the period of treatment is necessary to ensure adequate fluid intake.

Like other cholinomimetics, the drug can cause side effects vagotonic cardiovascular system (including bradycardia), which should be considered in patients with sick sinus syndrome and other disorders of conduction, and while the use of drugs that reduce heart rate (digoxin or beta-adrenoblokotory).

Galantamine in the treatment there is a risk of occurrence of syncope, and therefore the need to monitor blood pressure frequently, especially when taking the drug at higher doses (40 mg daily dose). In order to prevent such side effects is necessary to select the dose carefully in the beginning of treatment.

Efficacy in patients with other types of dementia and memory impairment has not been established.

The drug is not intended for the treatment of patients with mild cognitive impairment, ie, with isolated memory impairment, higher than the expected level for their age and education, but does not meet the criteria for Alzheimer's disease.

Drug interactions

Do not combine with other holinomimetikami.

It is the antagonist of opioid effects on the respiratory center.

Shows pharmacodynamic antagonism m-anticholinergic (atropine, homatropine methyl bromide, etc.), Ganglionic, non-depolarizing muscle relaxants, quinine, procainamide.

Aminoglycoside antibiotics may reduce the therapeutic effect of galantamine.

Galantamine enhances neuromuscular blockade during general anesthesia (including when used as a peripheral muscle relaxant suxamethonium).

Drugs that reduce the heart rate (digoxin, beta-adrenoblokotory), - the risk of worsening bradycardia.

Cimetidine may increase the bioavailability of galantamine.

All drugs that inhibit both isozymes of cytochrome P450 (CYP2D6 and CYP3A4), can increase the plasma concentration of galantamine while their application, whereby the frequency can be increased cholinergic side-effects (mainly nausea and vomiting). In this case, depending on the particular patient tolerance therapy may need to decrease maintenance dose of galanthamine.

Inhibitors of CYP2D6 isoenzyme (amitriptyline, fluoxetine, fluvoxamine, paroxetine, quinidine), galantamine clearance is lower by 25-30%. For this reason, it is not recommended concurrently with ketoconazole, zidovudine, erythromycin.

Do dampening effect on the central nervous system of ethanol and sedatives.

Overdose

Symptoms: depression of consciousness (even coma), convulsions, increased severity of side effects, severe muscle weakness, combined with hypersecretion of the glands of the mucous membrane of the trachea and bronchospasm, may lead to lethal blockade of the respiratory tract.

Treatment: gastric lavage, symptomatic therapy. As an antidote - in / atropine in doses of 0.5-1 mg. Subsequent doses of atropine determined depending on the therapeutic response and the condition of the patient.

Storage conditions

In a dry, dark place at a temperature no higher than 25 ° C. Keep out of the reach of children.