Galantamine pills 8mg №56

Trade name: galantamine

International non-proprietary name of the drug: galantamine

Dosage Form: film coated tablets

Composition: 1 tablet, film coated, contains:

active substance - galantamine hydrobromide 5,127 mg, 10.254 mg and 15.380 mg in terms of galantamine 4.00 mg, 8.00 mg and 12.00 mg;

Excipients — Calcium hydrogen phosphate dihydrate, colloidal silicon dioxide (aerosil), copovidone (plasdone Es – 630 or collidon VA – 64), Magnesium stearate, croscarmellose sodium (primelloza), microcrystalline cellulose;

film coating composition - Advantia^Tm Prima 319974RC09 [hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol), caprin / caprylic triglyceride (glyceryl caprylocaprate), titanium dioxide, aluminum lacquer based on quinoline yellow, aluminum lacquer on the basis of the dye, green, blue, orange, lacquer, green, blue, green, white, green, blue, green, white, green, blue, green, white, blue, green, white, green, blue, green, blue, green, blue, green, blue, green, white

Description

The pills covered with a film cover of blue color, round, biconvex, on a cross-section - white color.

Pharmacotherapeutic group: Anticholinesterase agent

Pharmacological properties

Pharmacodynamics

Selective, competitive and reversible acetylcholinesterase inhibitor. Stimulates nicotinic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine. Facilitates the conduct of excitation in the neuromuscular synapse and restores the neuromuscular conduction in cases of its blockade with muscle relaxants of non-depolarizing type of action. Increases the tone of smooth muscles, increases the secretion of the digestive and sweat glands, causes miosis. By increasing the activity of the cholinergic system, galantamine improves cognitive function in patients with Alzheimer's-type dementia, but does not affect the development of the disease itself.

Pharmacokinetics

After ingestion is rapidly and completely absorbed in the gastrointestinal tract. Absolute bioavailability is high - up to 90%. Therapeutic concentration is reached 30 minutes after administration. The maximum plasma concentration after administration in a dose of 8 mg is observed at the 2nd hour and is 1.2 mg / ml.

The half-life is 5 hours.After repeated intake, equilibrium concentration is established.

It is slightly bound to blood proteins. Easily passes through the hemato-encephalic barrier. To a small extent (about 10%) is metabolized in the liver by demethylation.

Excreted (in unchanged form and form of metabolites), mainly with urine (up to 74%). Renal clearance is approximately 100 ml / min. In patients with Alzheimer's disease, the plasma concentration of galantamine may increase. In moderate and severe hepatic and renal dysfunction, plasma concentrations of galantamine increase.

Indications

- dementia of Alzheimer's type of mild or moderate degree;

- poliomyelitis (immediately after the cessation of the febrile period, as well as during the recovery period and the period of residual effects);

- myasthenia gravis, progressive muscular dystrophy, cerebral palsy, neuritis, sciatica, myopathy.

Contraindications

hypersensitivity to any of the components of the drug; bronchial asthma; bradycardia; atrioventricular block;

arterial hypertension, angina pectoris; chronic heart failure; epilepsy; hyperkinesis;

severe renal (creatinine clearance - less than 9 ml / min) and liver (more than 9 points on the Child-Pugh scale) violations; mechanical intestinal obstruction; chronic obstructive pulmonary disease; obstructive diseases or recent surgery on the organs of the gastrointestinal tract;

obstructive disease or recent surgery for urinary tract or prostate gland; children up to 9 years; pregnancy and lactation.

Carefully:

mild to moderate renal or hepatic impairment;

sick sinus syndrome and other supraventricular conduction disorders;

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

Dosage and administration

Inside, while eating, drinking water.

Adults:

The daily dose is 8-32 mg, divided into 2-4 doses.

With myasthenia gravis, the daily dose is divided into 3 doses.

With Alzheimer's disease, it is recommended to start treatment with 4 mg tablets.
2 times a day. Within 4 weeks, the daily dose can be gradually increased to 16 mg - by
1 tab. on 8 mg 2 times a day - in the morning and in the evening. During treatment with a drug, it is necessary to ensure that enough liquid is taken up. If during treatment it is necessary to stop taking the drug, then the restoration of treatment should be started at the lowest dose and gradually increased.

Patients with moderately impaired liver and kidney function:

Initial dose - 4 mg 1 time per day, which is taken in the morning, for at least
1 week, after which the dose is increased to 4 mg 2 times a day and taken for
4 weeks.

The total daily dose should not exceed 12 mg.

Children (from 9 years)

Treatment of poliomyelitis, cerebral palsy:

from 9 to 11 years, the daily dose is 4–12 mg divided into 2–3 doses;

From 12 to 15 years, the daily dose is 4–16 mg divided into 2–4 doses.

Adverse Effects

Cardiovascular: decrease or increase in blood pressure, orthostatic collapse, heart failure, edema, atrioventricular block, atrial flutter or atrial fibrillation, lengthening
QT-interval, ventricular and supraventricular tachycardia, supraventricular premature beats, tides, bradycardia, ischemia, or myocardial 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, mucosal perforation, gastroenteritis, duodenitis, hepatitis; lower gastrointestinal tract.

Musculoskeletal system: muscle cramps, muscle weakness, fever.

Laboratory values: increased liver enzymes, anemia, hypokalemia, increased blood sugar or alkaline phosphatase.

Hematologic: thrombocytopenia, purpura.

Urogenital: urinary incontinence, hematuria, frequent urination, urinary tract infections, urinary retention, calculus, renal colic.

Nervous system: often tremor, syncope, lethargy, taste perversion, visual and auditory hallucinations, behavioral responses, including agitation / aggression; transient cerebrovascular accident or stroke; headache, dizziness, convulsions, muscle spasms, paresthesia, ataxia, hypo- or hyperkinesis, apraxia, aphasia, anorexia, drowsiness, insomnia.

From the senses: rhinitis, nosebleeds, visual disturbances, accommodation spasm, infrequently - tinnitus.

From the psyche: depression (very rarely with suicide), apathy, paranoid reactions, increased libido, delirium.

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

Overdosage

Symptoms: depression of consciousness (up to coma), convulsions, increased severity of side effects, severe muscle weakness combined with hypersecretion of the glands of the tracheal mucosa and bronchospasm can lead to a fatal blockade of the respiratory tract.

Treatment: gastric lavage, symptomatic therapy. As an antidote - in / in the introduction 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.

Use during pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Interaction with other drugs

It is not recommended to combine with other cholinomimetics.

It is an opioid antagonist of action on the respiratory center.
Shows pharmacodynamic antagonism to m-anticholinergics (atropine, gomatropine methyl bromide, etc.), ganglioblokatoram, non-depolarizing muscle relaxants, quinine, procainamide.

Aminoglycoside antibiotics can reduce the therapeutic effect of galantamine.
Galantamine increases neuromuscular blockade during general anesthesia (including suxamethonia when used as a peripheral muscle relaxant).

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

Cimetidine may increase the bioavailability of galantamine.

All drugs that inhibit and isoenzymes of the cytochrome P450 system (CYP2D6 and CYP3A4) can increase plasma concentrations of galantamine while their simultaneous use, as a result of which the frequency of cholinergic side effects (mainly nausea and vomiting) may increase. In this case, depending on the tolerance of therapy by the particular patient, a reduction in the maintenance dose of galantamine may be necessary.

Inhibitors of the CYP2D6 isoenzyme (amitriptyline, Fluoxetine, fluvoxamine, paroxetine, quinidine) reduce the clearance of galantamine by 25–30%. For this reason, it is not recommended to administer simultaneously with Ketoconazole, zidovudine, Erythromycin .
Strengthens the inhibitory effect on the central nervous system of ethanol and sedatives.

special instructions

During the period of treatment should refrain from performing work requiring increased concentration of attention and speed of psychomotor reactions, including driving.
Treatment with acetylcholinesterase inhibitors is accompanied by a decrease in body weight. This is especially necessary to keep in mind when treating patients with Alzheimer's disease, who usually experience weight loss. In this regard, it is necessary to monitor the weight of the body in such patients.

During treatment it is necessary to ensure adequate fluid intake.
Like other cholinomimetics, the drug can cause vagotonic effects on the part of the cardiovascular system (including bradycardia), which must be taken into account in patients with sick sinus syndrome and other conduction disorders, as well as simultaneous use with drugs that reduce heart rate (digoxin or beta-blockers).

When treating Galantamine there is a risk of syncope, and therefore it is necessary to control blood pressure more often, especially when taking the drug in 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 treatment.
The efficacy of the drug in patients with other types of dementia and memory impairment has not been established.

The drug is not intended to treat patients with mild cognitive impairment, i.e. with isolated memory impairment exceeding the expected level for their age and education, but not meeting the criteria for Alzheimer's disease.

Release form

Tablets, film coated, 4 mg, 8 mg and 12 mg.

On 7, 10, 15 or 30 pills in a blister strip packaging from a film of polyvinyl chloride and aluminum foil printed lacquered.

1, 2, 4, 8 blister packs of 7 pills or 1, 3, 6 blister packs of 10 pills or 1, 2, 4 blister packs of 15 pills or 1, 2, 3 blister packs 30 pills together with instructions for use are placed in a pack of cardboard.

Storage conditions: In a dry, dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.