Composition, form of production and packaging
Tablets, film-coated 1 tab.
galantamine 4 mg
- "- 8 mg
- "- 12 mg
10 pieces. - packings of cellular contour (1) - packs cardboard.
14 pcs. - packings cellular planimetric (2) - packs cardboard.
14 pcs. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (6) - packs cardboard.
15 pcs. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Selective, competitive and reversible inhibitor of acetylcholinesterase. Stimulates nicotinic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine. It facilitates the conduction of excitation in the neuromuscular synapse and restores neuromuscular conduction in cases of its blockade with muscle relaxants of a nondepolarizing action type. Increases the tone of smooth muscles, increases the secretion of digestive and sweat glands, causes miosis. Increasing the activity of the cholinergic system, galantamine improves cognitive function in patients with Alzheimer's dementia, but does not affect the development of the disease itself.
PHARMACOKINETICS
After oral administration, it is quickly and completely absorbed into the digestive tract. Absolute bioavailability is high - up to 90%. Therapeutic concentration is achieved after 30 minutes after administration. C max after taking in a dose of 8 mg is observed at the 2 nd hour and is 1.2 mg / ml.
T 1/2 - 5 hours. After repeated intake, the equilibrium concentration is established.
To a small extent binds to blood proteins. Easily passes through the hemato-encephalic barrier. To an insignificant extent (about 10%) is metabolized in the liver by demethylation.
It is excreted (unchanged and the form of metabolites), mainly with urine (up to 74%). Kidney clearance is approximately 100 ml / min.
In patients with Alzheimer's disease, the plasma concentration of galantamine can increase. With moderate and severe violations of the liver and kidney plasma concentrations of galantamine are increased.
INDICATIONS
- Alzheimer's dementia of mild to moderate degree;
- poliomyelitis (immediately after the termination of the febrile period, as well as in the recovery period and the period of residual events);
- Myasthenia gravis, progressive muscular dystrophy, cerebral palsy, neuritis, radiculitis, myopathy.
DOSING MODE
Inside, with food, washing with water.
Adults:
The daily dose is 8-32 mg, divided into 2-4 admission.
In myasthenia gravis, the daily dose is divided into 3 divided doses.
In Alzheimer's disease, it is recommended to start treatment with taking 4 mg tablets twice a day. Within 4 weeks the daily dose can be gradually increased to 16 mg - 1 tablet, 8 mg 2 times / day - morning and evening. During treatment with the drug must ensure the intake of a sufficient amount of fluid. If, during treatment, it is necessary to stop taking the drug, then the restoration of treatment should begin with the lowest dose and gradually increase it.
Patients with moderately severe impairment of liver and kidney function:
The initial dose is 4 mg 1 time / day, which is taken in the morning, for at least 1 week, after which the dose is increased to 4 mg 2 times / day and taken within 4 weeks.
The total daily dose should not exceed 12 mg.
Children (from 9 years old):
Treatment of poliomyelitis, cerebral palsy:
from 9 to 11 years - a daily dose of 4-12 mg, divided into 2-3 doses;
from 12 to 15 years - the daily dose is 4-16 mg, divided into 2-4 admission.
SIDE EFFECT
From the cardiovascular system: a decrease or increase in blood pressure, orthostatic collapse, heart failure, edema, atrioventricular block, flutter or atrial fibrillation, prolongation of the QT interval, ventricular and supraventricular tachycardia, supraventricular extrasystole, "hot flashes", bradycardia, ischemia or infarction myocardium.
On the part of the digestive system: bloating, dyspepsia, gastrointestinal discomfort, anorexia, diarrhea, abdominal pain, nausea, vomiting, gastritis, dysphagia, dry mouth, increased salivation, diverticulitis, gastroenteritis, duodenitis, hepatitis, perforation of the esophagus mucosa , bleeding from the upper and lower divisions of the gastrointestinal tract.
From the musculoskeletal system: muscle spasms, muscle weakness, fever.
Laboratory indicators: increased activity of hepatic enzymes, anemia, hypokalemia, increased levels of sugar or alkaline phosphatase in the blood.
Hematologic: thrombocytopenia, purpura.
From the urinary system: urinary incontinence, hematuria, frequent urination, urinary tract infections, urinary retention, calculosis, renal colic.
From the nervous system: often tremor, syncope, inhibition, taste distortion, visual and auditory hallucinations, behavioral reactions, including agitation / aggression;transient impairment of cerebral circulation or stroke; headache, dizziness, convulsions, muscle spasms, paresthesia, ataxia, hypo- or hyperkinesis, apraxia, aphasia, anorexia, drowsiness, insomnia.
From the sense organs: rhinitis, epistaxis, visual impairment, accommodation spasm, infrequently - tinnitus.
From the side of the psyche: depression (very rarely - with suicide), apathy, paranoid reactions, increased libido, delirium.
Common: chest pain, excessive sweating, weight loss, fatigue, dehydration (in rare cases - with the development of kidney failure), bronchospasm.
CONTRAINDICATIONS
- bronchial asthma;
bradycardia;
- atrioventricular block;
- arterial hypertension;
- angina pectoris;
- Chronic heart failure;
- epilepsy;
- hyperkinesis;
- severe renal (creatinine clearance less than 9 ml / min) and hepatic (more than 9 points: according to the Child-Pugh scale);
- mechanical intestinal obstruction;
- chronic obstructive pulmonary disease;
- Obstructive diseases or recent surgery on the organs of the gastrointestinal tract;
- Obstructive diseases or recent surgical treatment of the urinary tract or prostate;
- children's age till 9 years;
- pregnancy and lactation;
- hypersensitivity to any of the components of the drug.
With caution :
- mild and moderate impairment of kidney or liver function;
- syndrome of sinus node weakness and other supraventricular conduction disorders;
- simultaneous reception of drugs slowing the heart rate (digoxin, beta-blockers);
- general anesthesia;
- peptic ulcer of the stomach and duodenum, increased risk of development of erosive and ulcerative lesions of the gastrointestinal tract.
PREGNANCY AND LACTATION
Contraindicated in pregnancy. For the duration of treatment, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal dysfunction. With caution for mild to moderate renal dysfunction
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function. With caution in light and moderate violations of liver function
APPLICATION FOR CHILDREN
Contraindicated in children younger than 9 years.
SPECIAL INSTRUCTIONS
Treatment with inhibitors of acetylcholinesterase is accompanied by a decrease in body weight. Especially it is necessary to bear in mind in the treatment of patients with Alzheimer's disease, who usually have weight loss. In this regard, it is necessary to monitor the body weight of such patients.
During the treatment period, sufficient fluid intake should be ensured. Like other holinomimetics, the drug can cause vagotonic effects on the part of the cardiovascular system (including bradycardia), which must be taken into account in patients with sinus node weakness syndrome and other conduction disorders, as well as with simultaneous use with drugs that reduce heart rate (digoxin or beta-adrenergic blockers).
In the treatment of Galantamine, there is a risk of syncope, in connection with which it is necessary to control blood pressure more often, especially when taking the drug at higher doses (40 mg daily dose). In order to prevent such side effects, it is necessary to carefully select the dose of the drug at the beginning of the treatment.The effectiveness of the drug in patients with other types of dementia and memory impairment is not established.
The drug is not intended for the treatment of patients with mild cognitive impairment, i.e. with isolated memory impairment exceeding the expected level for their age and education, but not satisfying the criteria of Alzheimer's disease.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, one should refrain from performing work that requires an increased concentration of attention and speed of psychomotor reactions, including driving.
OVERDOSE
Symptoms: depression of consciousness (up to coma), seizures, increased severity of side effects, severe muscle weakness in combination with hypersecretion of the glands of the mucous membrane of the trachea and bronchospasm can lead to lethal blockade of the airways.
Treatment: gastric lavage, symptomatic therapy. As an antidote - iv injection of atropine in doses of 0.5-1 mg. Subsequent doses of atropine are determined depending on the therapeutic response and the patient's condition.
DRUG INTERACTION
It is not recommended to combine with other holinomimetics.
It is an opioid antagonist by action on the respiratory center. It exhibits pharmacodynamic antagonism to m-cholinolytics (atropine, gomatropine methyl bromide, etc.), ganglion blockers, nondepolarizing muscle relaxants, quinine, procainamide.
Aminoglycoside antibiotics can reduce the therapeutic effect of galantamine. Galantamine increases neuromuscular blockade during general anesthesia (including when used as a peripheral muscle relaxant suksametoniya). Drugs that reduce the heart rate (digoxin, beta-adrenoblocker) increase the risk of aggravation of bradycardia. Cimetidine may increase the bioavailability of galantamine.
All drugs that inhibit cytochrome P450 system isoenzymes (CYP2D6 and CYP3A4) can increase plasma concentrations of galantamine while simultaneously using them, which may increase the incidence of cholinergic side effects (mainly nausea and vomiting). In this case, depending on the tolerability of therapy by a specific patient, a reduction in the maintenance dose of galantamine may be necessary.
Inhibitors of the isoenzyme CYP2D6 (amitriptyline, fluoxetine, fluvoxamine, paroxetine, quinidine) reduce the clearance of galantamine by 25-30%. For this reason, it is not recommended to appoint simultaneously with ketoconazole, zidovudine, erythromycin. Increases the inhibitory effect on the central nervous system of ethanol and sedatives.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
In a dry, protected from light place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 2 years. Do not use after the expiration date.
