home Audience 12 Galantamine analogues. How to find a cheap analogue of an expensive medicine? Interaction with other drugs

Galantamine analogues. How to find a cheap analogue of an expensive medicine? Interaction with other drugs

Galantamine is available in the form tablets, capsules, solution for injection.

Tablets and capsules are packaged in 10, 14 or 15 pieces in blister packs of 1, 2, 3, 4 or 6 per pack.

Solutions are offered in vials or ampoules.

pharmachologic effect

The drug has anticholinesterase action.

Pharmacodynamics and pharmacokinetics

Galantamine is a reversible anticholinesterase drug. Thanks to its use, cholinergic transmission is improved, enhancing and prolonging the effectiveness of endogenous acetylcholine. At the same time, neuromuscular transmission in the muscles is ensured, and antagonism to curare-like non-depolarizing agents is manifested. Also under the influence of Galantamine increases muscle tone internal organs, the work of the exocrine glands is enhanced. As a result, it decreases , possible occurrence miosis And spasm of accommodation . The active substance quickly penetrates the BBB into the brain, enhancing excitation processes.

The drug is quickly absorbed inside the body. In this case, the therapeutic concentration in the composition is achieved within 30 minutes. The maximum concentration is observed with a single application therapeutic dose, after 2 hours. Galantamine is characterized by a weak connection with plasma proteins. occurs by demethylation, with the formation - epigalantamine And galanthaminone . The drug is excreted mainly in the form of metabolites in urine and a small part in bile.

Indications for use

The drug in the form of capsules and tablets is prescribed for:

Alzheimer's type dementia light and moderate degree gravity.

In addition, tablets are used in the treatment of:

progressive muscle dystrophy, myopathy;
cerebral palsy
, neuritis.

The solution for injection is used in various areas of medicine:

in neurology in the treatment of:

traumatic damage to the nervous system;
cerebral palsy;
diseases spinal cord;
mononeuritis, polyneuritis, polyneuropathy, polyradiculoneuritis;
idiopathic paresis facial nerve;
myopathies;
night

In surgery and anesthesiology the drug is used as an antagonist non-depolarizing muscle relaxants and therapy for postoperative atony Bladder and intestines.

The sensory organs and nervous system may also be affected, which usually manifests itself as: lethargy, changes in taste, behavioral reactions, feeling tired, convulsions, , paranoid reactions and so on.

Other side effects include: chest pain, increased nose bleed, , increased libido, bronchospasms, hypokalemia.

Instructions for use of Galantamine (Method and dosage)

According to the instructions for use of Galantamine, tablets or capsules are prescribed in daily dosage– 5-10 mg taken 3-4 times a day after eating. The duration of therapy can be 4-5 weeks. If high doses are used in treatment, the course may be shortened.

The dosage of the drug in the injection solution depends on the age of the patients. If necessary, the dose may be increased, taking into account individual characteristics sick.

Maximum single dosage for adult patients should not exceed 10 mg and 20 mg per day. Treatment is usually started by taking minimal doses, gradually increasing until they are therapeutically effective. Treatment continues for up to 50 days; after 1-1.5 months, repeat therapy is allowed.

Overdose

In case of overdose, muscle weakness may develop, fasciculations , severe nausea, vomiting, cramping abdominal pain, increased salivation, lacrimation, urinary or fecal incontinence, heavy sweating, pressure reduction, bradycardia, collapse and seizures. Increased muscle weakness, complemented by hypersecretion of the tracheal mucosa and bronchospasm, can cause fatal blockage of the airways.

In this case, treatment is carried out, including gastric lavage, administration of anticholinergic drugs and other symptomatic therapy, taking into account the patient’s condition.

Interaction

It has been established that Galantamine hydrobromide is an antagonist and structural analogues regarding their inhibitory effect on the respiratory center. The drug helps restore neuromuscular conduction after blocking with curare-like drugs with an antidepolarizing effect.

As a result of their intake, the transmission of cholinergic impulses improves and the effect of endogenous acetylcholine is prolonged. In this article we will talk about these medications and the opinions of patients.

Release form, composition

The drug is available in three forms - tablets, capsules and solution for injection.

Round white flat tablets contain active substance- galantamine, and there are different dosages active substance - 4 mg, 8 mg and 12 mg. Auxiliary components are:

Analogs of "Galantamine" have similar composition and similar action.

Shell covering the core active component, consists of hypromellose, Ti dioxide, macrogol (polyethylene glycol), dye-based aluminum varnish.

The drug goes on sale in ten, fifteen, thirty or sixty tablets per pack.

Capsules are light pink or white containers containing granules inside white. The additional components are:

The capsules are enclosed in blisters of seven pieces, of which one, two, four, eight or twelve pieces can be contained in one box. Instructions for taking the drug are attached.

The solution for injection is a colorless clear liquid. One milliliter may contain 1 mg or 5 mg of galantamine hydrobromide ( active substance), as well as water for injection and sodium chloride as auxiliary components. The liquid is poured into 1 ml ampoules and placed five in a cell package, which are sold two in a box.

Store the product at temperatures up to 25 ° C in a dry, dark place, out of reach of children.

When is use indicated?

The use of "Galantamine" and analogues is indicated for the following diseases:

myopathy;
muscular dystrophy;
radiculitis and other disorders of the musculoskeletal system;
neuritis accompanied by memory loss;
children's cerebral paralysis;
polio;
dementia;
middle and light weight Alzheimer's disease.

In addition, the solution for injection is used in the treatment of:

pathologies of the spinal cord and brain;
neurological disorders, including idiopathic paresis of the facial nerve;
enuresis;
digestive system;
atony of the bladder;
Guillain-Barre syndrome;
intoxication in case of poisoning with anticholinergic drugs or morphine.

Also this medicine used when iontophoresis is performed for pathologies of the peripheral nervous system or diagnosis of diseases digestive tract.

Medicinal properties of drugs

According to the instructions for use, Galantamine and analogues act on a wide range of diseases. The drugs are released to consumers strictly according to a doctor's prescription.

As a result of taking "Galantomin" and similar drugs:

cholinergic transmission improves;
the influence of endogenous acetylcholine is prolonged;
intramuscular nerve transmission is activated;
the activity of the endocrine secretion glands increases;
antagonism to curare-like substances that have a non-depolarizing effect is manifested;
muscle tone improves.

There is also evidence that after taking medications, it decreases intraocular pressure, but a spasm of accommodation may occur and miosis may develop. The active substance galantamine penetrates into brain cells, as a result of which the nervous excitement.

Pharmacokinetics of drugs

As stated in the instructions, Galantamine and analogues are characterized by rapid and complete absorption into the gastrointestinal tract immediately after ingestion. The tall one says this absolute indicator bioavailability, which reaches 90%.

The therapeutic concentration is achieved within half an hour from the moment of taking the medication due to good absorption. The maximum content in plasma, provided that 8 mg of the active substance is taken, is observed after an hour and a half and is equal to 1.2 mg/ml. The half-life of the substance reaches 5 hours. After repeated administration of drugs with galantamine, an equilibrium concentration value is established.

The active substance can slightly bind to proteins in the blood, easily passing through the blood-brain barrier.

IN small degree(up to 10%) metabolism occurs in the liver through demethylation. Up to 74% of the drug is excreted in the urine in the form of metabolites (galanthaminone and epigalantamine) and partly unchanged.

About 100 ml/min of metabolites pass through the kidneys, the rest is excreted through the intestines.

The plasma concentration of the active substance may increase in people with Alzheimer's disease, as well as in severe and moderate pathologies of the kidneys and liver.

Instructions for use of the tablet form

Taking "Galantamine" and analogues of the drug in tablets is carried out during meals with a sufficient amount of liquid.

For adults, a daily dose of 8-32 mg is prescribed according to the following dosage regimen:

for myasthenia - three times a day;
for Alzheimer's disease - twice a day, starting with 4 mg of the active substance concentration and ending after four weeks with 16 mg (one 8 mg tablet in the evening and in the morning);
for other pathologies, the doctor prescribes the dose and frequency of administration individually.

If the functioning of the kidneys and liver is impaired, start with a dose of 4 mg once a day in the morning for a week. Then the frequency of administration is increased: the same dosage - twice a day for four weeks. It is prohibited to exceed daily norm over 12 mg.

If during therapy the medication is stopped for any reason, then it is resumed again with lowest dose with a gradual increase. The total course duration is usually four to five weeks.

According to the instructions for use, "Galantamine" and analogues of the drug are used for children, starting from the age of nine, for the treatment of cerebral palsy and polio (tablets):

9-11 years - the dose per day is 4-12 mg for two or three doses;
12-15 years - the dose per day is 4-16 mg for two to four doses.

Galantamine capsules are taken orally twice a day - with meals in the morning and in the evening. Experts recommend an initial dosage of 8 mg (4 mg twice a day) for four weeks, then the patient should take a maintenance dose (8 mg twice a day) for a month. The maximum allowed amount of the drug is 24 mg per day, which is prescribed by the doctor after assessment clinical course diseases.

In the event of a break in therapy, which lasted several days, begin taking the initial dose again, after which it is gradually increased to the previous values. For moderate or mild forms of liver pathology, the basic dosage should be no more than 4 mg once a day in the morning for seven days. This is followed by a gradual increase to 4 mg twice a day for a monthly course. In this case, the maximum daily dose cannot be set above 16 mg.

Instructions for using injections

The amount of solution for injection depends on the age of the patient and is determined by the attending physician. For use in adults, the maximum single dose is 10 mg, the daily dose is 20 mg. In children aged one year - 0.25 mg once a day, at sixteen years - 10 mg once a day.

Subcutaneous and intravenous administration up to two times a day as usual and up to three times at higher dosages. Treatment should begin with a minimum amount and continue with gradual increase to the required volume.

The course of injections lasts one and a half months, then a break of the same duration and a new cycle, if prescribed by the treatment regimen. In total, the doctor can prescribe three courses of injections.

Precautions and contraindications

According to the instructions for use of Galantamine and analogues, therapy with these drugs is not permitted for the following diseases:

obstructive pulmonary diseases;
pathological disorders in the functioning of the liver and kidneys;
atrioventricular block;
intestinal obstruction;
epilepsy;
hypertension;
arterial hypertension;
ailments of the digestive system and operations on its organs;
hyperkinetic syndrome;
bronchial asthma;
surgery on the prostate or urinary tract;
diseases of cardio-vascular system(angina pectoris, bradycardia);
increased sensitivity (allergic reaction) on the components of the drug;
pregnancy and breastfeeding;
childhood up to nine years old.

Galantamine and analogues (photos of the drugs are presented in the article) are used with great caution:

for moderate and mild pathologies of the kidneys and liver;
with existing ulcers of the digestive tract or risks of their occurrence;
during general anesthesia;
for weakness syndrome sinus node;
in the presence of supraventricular conduction disorders.

The injection solution is not used to treat children under one year of age.

Interaction with other means

There are the following restrictions on the use of medications in this group with other drugs:

“Galantamine” and analogues (synonyms) are strictly prohibited from being taken simultaneously with other cholinomimetics.
Do not use simultaneously with medications that slow the heart.
Cimetidine increases the bioavailability of galantamine.
Antibiotics of the aminoglycoside group reduce the therapeutic effect of drugs.
Isoenzymes of the cytochrome system in symbiosis with galantamine can cause vomiting and nausea.
"Erythromycin", "Zidovudine", "Ketoconazole" reduce the absorption of the active substance.
"Galantamine" and analogues enhance the effect sedatives and ethanol.
Aminoglycolides reduce the effectiveness of the described drugs.
Concomitant use with paroxetine and ketaconazole increases the concentration of galantamine by thirty percent.

Side effects and overdose

According to reviews and instructions for use of “Galantamine” and analogues, the following may appear during therapy: side symptoms:

From the heart and blood vessels: swelling, surges in blood pressure, tachycardia, the occurrence of orthostatic collapse and atrial fibrillation, bradycardia, ischemia, myocardial infarction.
From the digestive tract: vomiting, nausea, abdominal pain, diarrhea and flatulence, dyspepsia and gastritis, hepatitis, lack of appetite.
From the muscular and musculoskeletal system: weakness, spasms.
From the urinary tract: renal colic, enuresis, hematuria, infections, lack of urination.
From the nervous system and sensory organs: hallucinations, tremors, convulsions, lethargy and fatigue, changes in taste, depression and apathy, dizziness, paranoid behavior.
Other: painful symptoms in the sternum, fever, bronchospasms, hypokalemia, dehydration, nosebleeds, excessive sweating, tinnitus, visual impairment.

When side effects treatment is stopped.

A drug Galantamine- anticholinesterase agent
Selective, competitive and reversible acetylcholinesterase inhibitor. Stimulates nicotinic receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine. Facilitates the conduction of excitation at the neuromuscular synapse and restores neuromuscular conduction in cases of its blockade by muscle relaxants of a non-depolarizing type of action. Increases smooth muscle tone, enhances the secretion of 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 has no effect on the development of the disease itself.

Pharmacokinetics

After oral administration, it is quickly and completely absorbed from the gastrointestinal tract. Absolute bioavailability is high - up to 90%. Therapeutic concentration is achieved 30 minutes after administration. The maximum plasma concentration after taking 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 doses, an equilibrium concentration is established.
Slightly binds to blood proteins. Easily passes through the blood-brain barrier. To a small extent (about 10%) is metabolized in the liver by demethylation.
It is excreted (in unchanged form and in the form of metabolites), mainly in the urine (up to 74%). Renal clearance is approximately 100 ml/min. In patients with Alzheimer's disease, plasma concentrations of galantamine may be increased. With moderate and severe impairment of liver and kidney function, plasma concentrations of galantamine increase.

Indications for use

Indications for use of the drug Galantamine are:
- mild or moderate Alzheimer's type dementia;
- poliomyelitis (immediately after the cessation of the febrile period, as well as during recovery period and period residual effects);
- myasthenia gravis, progressive muscular dystrophy, cerebral palsy, neuritis, radiculitis, myopathy.

Mode of application

Galantamine tablets take orally, during meals, with water.
Adults:
The daily dose is 8-32 mg, divided into 2-4 doses.
For myasthenia gravis, the daily dose is divided into 3 doses.
For Alzheimer's disease, treatment is recommended to begin with taking 4 mg tablets
2 times a day. Over the course of 4 weeks, the daily dose can be gradually increased to 16 mg - 1 tablet. 8 mg 2 times a day - morning and evening. During treatment with the drug, it is necessary to ensure that a sufficient amount of fluid is taken. If during treatment it is necessary to stop taking the drug, then reinstatement of treatment should begin with the lowest dose and gradually increase it.
For patients with moderately severe impairment of liver and kidney function:
The initial dose is 4 mg 1 time per day, 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 old)
Treatment of polio, cerebral palsy:
from 9 to 11 years of age, the daily dose is 4-12 mg, divided into 2-3 doses;
from 12 to 15 years of age, the daily dose is 4-16 mg, divided into 2-4 doses.

Side effects

From the cardiovascular system: decrease or increase in blood pressure, orthostatic collapse, heart failure, edema, atrioventricular block, atrial flutter or fibrillation, prolongation
QT interval, ventricular and supraventricular tachycardia, supraventricular extrasystole, hot flashes, bradycardia, ischemia or myocardial infarction.
From 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 esophageal mucosa , bleeding from the upper and lower sections gastrointestinal tract.
From the musculoskeletal system: muscle spasms, muscle weakness, fever.
Laboratory findings: increased liver enzymes, anemia, hypokalemia, increased sugar levels or alkaline phosphatase in blood.
Hematological: thrombocytopenia, purpura.
From the urinary system: urinary incontinence, hematuria, frequent urination, infections urinary tract, urinary retention, calculosis, renal colic.
From the nervous system: often tremor, syncope, lethargy, taste perversion, visual and auditory hallucinations, behavioral reactions including agitation/aggression; transient disorder cerebral circulation or stroke; headache, dizziness, convulsions, muscle spasms, paresthesia, ataxia, hypo- or hyperkinesis, apraxia, aphasia, anorexia, drowsiness, insomnia.
From the senses: rhinitis, nosebleeds, visual disturbances, spasm of accommodation, infrequently - tinnitus.
From the mental side: depression (very rarely with suicide), apathy, paranoid reactions, increased libido, delirium.
General: chest pain, increased sweating, weight loss, feeling tired, dehydration (in in rare cases- with development renal failure), bronchospasm.

Contraindications

Contraindications to the use of the drug Galantamine are: 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 hepatic (more than 9 points on the Child-Pugh scale) disorders; 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 urinary tract or prostate; children under 9 years of age; pregnancy and lactation period.
With caution: mild and moderate impairment kidney or liver function; sick sinus syndrome and other supraventricular conduction disorders; simultaneous administration drugs that slow down the heart rate (digoxin, beta-blockers); general anesthesia; peptic ulcer stomach and duodenum, increased risk development erosive and ulcerative lesions gastrointestinal tract.

Pregnancy

Taking pills is contraindicated Galantamine during pregnancy. Breastfeeding should be stopped during treatment.

Interaction with other drugs

Not recommended Galantamine combine with other cholinomimetics.
It is an opioid antagonist in its effect on the respiratory center.
Shows pharmacodynamic antagonism to m-anticholinergics (atropine, homatropine methyl bromide, etc.), ganglion blockers, non-depolarizing muscle relaxants, quinine, procainamide.
Aminoglycoside antibiotics may reduce the therapeutic effect of galantamine.
Galantamine enhances neuromuscular blockade during general anesthesia (including when suxamethonium is used as a peripheral muscle relaxant).
Medicines that reduce heart rate (digoxin, beta-blockers) risk worsening bradycardia.
Cimetidine may increase the bioavailability of galantamine.
All drugs that inhibit isoenzymes of the cytochrome P450 system (CYP2D6 and CYP3A4) may increase plasma concentrations of galantamine when used concomitantly, which may result in an increased incidence of cholinergic reactions. side effects(mainly nausea and vomiting). In this case, depending on the tolerability of therapy by a 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 prescribe simultaneously with ketoconazole, zidovudine, erythromycin.
Strengthens the inhibitory effect on the central nervous system ethanol and sedatives.

Overdose

Overdose symptoms Galantamine: depression of consciousness (up to coma), convulsions, increased severity of side effects, severe muscle weakness in combination with hypersecretion of the glands of the tracheal mucosa and bronchospasm can lead to fatal blockage of the respiratory tract.
Treatment: gastric lavage, symptomatic therapy. As an antidote - intravenous administration 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.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Release form

Galantamine - film-coated tablets, 4 mg, 8 mg and 12 mg.
7, 10, 15 or 30 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
1, 2, 4, 8 blister packs of 7 tablets each or 1, 3, 6 blister packs of 10 tablets each or 1, 2, 4 blister packs of 15 tablets each or 1, 2, 3 blister packs of 15 tablets each 30 tablets along with instructions for use are placed in a cardboard pack.

Compound

1 film-coated tablet Galantamine contains the 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 (plasdon Es-630 or collidon VA-64), magnesium stearate, croscarmellose sodium (primellose), microcrystalline cellulose.
Film shell composition: AdvantiaTM Prima 319974RC09 [hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol), caprin/caprylic triglyceride (glyceryl caprylocaprate), titanium dioxide, quinoline yellow dye-based aluminum varnish, brilliant blue dye-based aluminum varnish, aluminum varnish based on indigo carmine dye.

Additionally

During the treatment period, you should refrain from performing work that requires increased concentration and speed of psychomotor reactions, including driving.
Treatment with acetylcholinesterase inhibitors is accompanied by a decrease in body weight. This is especially important to keep in mind when treating patients with Alzheimer's disease, who typically experience weight loss. In this regard, it is necessary to monitor body weight in such patients.
During the treatment period, it is necessary to ensure sufficient fluid intake.
Like other cholinomimetics, the drug can cause vagotonic effects on the cardiovascular system (including bradycardia), which must be taken into account in patients with sick sinus syndrome and other conduction disorders, as well as when used simultaneously with drugs that reduce heart rate (digoxin or beta blockers).
During treatment Galantamine There is a risk of syncope and therefore needs to be monitored more frequently arterial pressure, especially when taking the drug for more high 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 effectiveness of the drug 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 weak 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.

Main settings

Name:	GALANTAMINE
ATX code:	N06DA04 -

Gross formula

C17H21NO3

Pharmacological group of the substance Galantamine

Nosological classification (ICD-10)

CAS code

357-70-0

Characteristics of the substance Galantamine

Hydrobromide of an alkaloid isolated from snowdrop tubers Voronov (Galanthus Woronowii A. Los.), amaryllis family (Amaryllidaceae). Also found in other species of the snowdrop genus Galanthus. White fine-crystalline powder with a bitter taste. Slightly soluble in water, practically insoluble in ethyl alcohol.

Pharmacology

pharmachologic effect- anticholinesterase.

Reversibly inhibits acetylcholinesterase, enhances and prolongs the action of endogenous acetylcholine. Facilitates the conduction of impulses in cholinergic, incl. neuromuscular, synapses, enhances excitation processes in reflex zones spinal and brain. Increases the tone of smooth and skeletal muscles, stimulates the secretion of digestive and sweat glands. Causes miosis and spasm of accommodation, lowers intraocular pressure in closed-angle glaucoma. When injected into the conjunctival sac, it may cause temporary swelling of the conjunctiva. Penetrates the BBB, enhances excitation processes in the central nervous system. When used in complex therapy spastic forms cerebral palsy improves neuromuscular conduction, increases muscle contractility, and has a positive effect on mnestic functions. Due to increased activity of the cholinergic system, it can improve cognitive function in patients with Alzheimer's type dementia.

After a single oral administration 8 mg is quickly absorbed from the gastrointestinal tract, bioavailability is about 90%. Food intake slows down absorption (Cmax decreases by 25%), but does not affect the completeness of absorption (AUC). Tmax is reached after 1.2 hours. The pharmacokinetics of galantamine is linear in the dose range of 4-16 mg 2 times a day. Plasma protein binding - 18%. In whole blood, galantamine is found predominantly in shaped elements(52.7%). The blood/plasma concentration ratio of galantamine is 1.2. Plasma clearance is about 300 ml/min, volume of distribution is 175 l. The main metabolic pathways are N-oxidation, N- and O-demethylation, glucuronidation and epimerization. In people with active metabolism of substrates CYP2D6 the most important metabolic pathway is O-demethylation. The main isoenzymes of the cytochrome P450 system involved in the metabolism of galantamine are CYP2D6 and CYP3A 4. In the plasma of people with fast and slow metabolizers, the main part is unchanged galantamine and its glucuronide. O-desmethylgalantamine glucuronide is also found in the plasma of fast metabolizers. Elimination is biphasic, the final half-life is 7-8 hours. Renal clearance is 65 ml/min (20-25% of plasma clearance). Excreted in urine (90-97%, of which 18-22% unchanged within 24) and feces (2.2-6.3%). After a single dose of galantamine in the plasma of fast and slow metabolizers, none of the active metabolites (norgalantamine, O-demethylgalantamine and O-demethylnorgalantamine) were detected in unconjugated form. Norgalantamine is detected in the plasma of patients after repeated doses of galantamine (not more than 10% of the concentration of galantamine). In patients with Alzheimer's disease, the concentration of galantamine in the blood plasma is 30-40% higher than in young people healthy people. With moderate liver failure(7-9 points on the Child-Pugh scale) AUC and T 1/2 increase by 30%. With moderate chronic renal failure (creatinine clearance 52-104 ml/min), the plasma concentration of galantamine increases by 38%, with severe chronic renal failure (creatinine clearance - 9-51 ml/min) - by 67%.

Application of the substance Galantamine

Extended release capsules: Alzheimer's type dementia of mild or moderate severity, incl. With chronic disorders cerebral circulation.

Pills: Alzheimer's type dementia of mild or moderate severity; poliomyelitis (immediately after the cessation of the febrile period, as well as in the recovery period and the period of residual effects); myasthenia gravis, progressive muscular dystrophy, myopathy; cerebral palsy; neuritis; radiculitis.

Injection: in neurology - traumatic injuries nervous system, cerebral palsy, spinal cord diseases (myelitis, poliomyelitis, polio form tick-borne encephalitis), mononeuritis, polyneuritis, polyneuropathy, polyradiculoneuritis, Guillain-Barré syndrome, idiopathic facial nerve paresis, myopathy, bedwetting. In anesthesiology and surgery: as an antagonist of non-depolarizing muscle relaxants and for the treatment of postoperative atony of the intestines and bladder. In physiotherapy: in the form of iontophoresis for diseases of the peripheral nervous system. In toxicology: intoxication with anticholinergic drugs, morphine and its analogues. In radiology: to improve the quality of diagnostics of the digestive system, incl. gallbladder.

Contraindications

Hypersensitivity, epilepsy, hyperkinesis, bronchial asthma, angina pectoris, bradycardia, chronic heart failure, AV block, arterial hypertension, chronic obstructive pulmonary disease, mechanical intestinal obstruction, obstructive diseases or recently undergone surgery on the gastrointestinal tract, obstructive diseases or recently undergone surgery intervention on the urinary tract or prostate gland, renal failure (creatinine clearance less than 9 ml/min), severe liver dysfunction (more than 9 points on the Child-Pugh scale), children under 1 year of age (for solution), up to 9 years (for tablets).

Restrictions on use

General anesthesia, sick sinus syndrome, simultaneous use of drugs that slow down the heart rate (digoxin, beta-blockers), mild to moderate dysfunction of the liver and/or kidneys; for oral forms (optional): peptic ulcer of the stomach and duodenum; for tablets (additionally): gluten enteropathy (due to the presence of wheat starch in the drug), lactose deficiency, galactosemia, glucose-galactose malabsorption syndrome (the drug contains lactose).

Use during pregnancy and breastfeeding

During pregnancy it is possible if potential benefit for mother exceeds possible risk for the fetus.

Women receiving galantamine should avoid breastfeeding(it is unknown whether galantamine is excreted from breast milk).

Side effects of the substance Galantamine

From the cardiovascular system and blood (hematopoiesis, hemostasis): decrease or increase in blood pressure, orthostatic collapse, heart failure, edema, AV block, atrial flutter or fibrillation, prolongation of the QT interval, ventricular and supraventricular tachycardia, supraventricular extrasystole, flushing, bradycardia, myocardial ischemia or infarction, thrombocytopenia, purpura, anemia.

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

From the musculoskeletal system: muscle spasms, muscle weakness.

From the outside genitourinary system: urinary incontinence, hematuria, frequent urination, urinary tract infections, urinary retention, calculosis, renal colic.

From the nervous system and sensory organs: tremor, syncope, lethargy, taste perversion, visual and auditory hallucinations, behavioral reactions, including agitation/aggression; transient cerebrovascular accident or stroke; feeling of fatigue, headache, dizziness, drowsiness, insomnia, convulsions, muscle spasms, paresthesia, ataxia, hypo- or hyperkinesis, depression (very rarely with suicide), apathy, paranoid reactions, delirium, apraxia, aphasia, visual impairment (spasm accommodation), tinnitus (uncommon).

Others: chest pain, increased sweating, fever, weight loss, nosebleeds, rhinitis, dehydration (in rare cases with the development of renal failure), bronchospasm, increased libido, hypokalemia, increased blood sugar or alkaline phosphatase levels.

Interaction

It is an antagonist of morphine and its structural analogues in relation to the inhibitory effect on the respiratory center. Restores neuromuscular conduction blocked by curare-like drugs with antidepolarizing action (tubocurarine, etc.). Enhances the effect of depolarizing muscle relaxants (Ditilin). Anticholinergic drugs (atropine, etc.) eliminate the peripheral muscarinic-like effects of galantamine, curare-like substances and ganglion blockers are nicotine-like.

Aminoglycosides may reduce the therapeutic effect of galantamine. Medicines that reduce heart rate (digoxin, beta-blockers) are at risk of worsening bradycardia. Cimetidine may increase the bioavailability of galantamine.

Isoenzyme inhibitors CYP2D6 and CYP3A4 cytochrome P450 may increase the AUC of galantamine when administered concomitantly. The AUC of galantamine increases by 30 and 40% when administered concomitantly with ketoconazole and paroxetine, respectively. When used simultaneously with erythromycin, the AUC of galantamine increases by 10%. Isoenzyme inhibitors CYP2D6(amitriptyline, fluoxetine, fluvoxamine, paroxetine, quinidine) reduce the clearance of galantamine by 25-33%. Galantamine enhances the inhibitory effect of ethanol and sedatives on the central nervous system.

Galantamine is a medicine intended to treat Alzheimer's disease and dementia. The drug eliminates the blood-brain barrier, improves the stimulating effect in the reflexogenic zones of the brain of the head and back.

The drug galantamine, instructions for use of which are always attached to it, maintains the functioning of skeletal and smooth muscles in an active state, increases its tone, normalizes the secretion of glands, promotes good conductivity of the neuromuscular system, reduces eye pressure.

In contact with

The main components of the medicine and its creator

The manufacturer of the pharmaceutical product “Galantamine” is the Russian pharmacological company CJSC “Canonpharma Production”.

The key active component of this pharmaceutical product stands active substance galantamine hydrobromide.

Auxiliary ingredients included in the presented product: aerosil, calcium, hydrogen phosphate dihydrate, copovidone, magnesium stearite, primellose, cellulose consisting of microcrystals.

The outside of the tablet is covered with a film-like shell, which also consists of several components:

AdventiaTM Prima 319974RC09,
titanium dioxide,
macrogol,
caprylic triglyceride,
aluminum varnish.

Release forms

The presented medicine is available in three types:

Long-acting capsules. Drug dosage: 8 mg, 16 mg, 24 mg.
Tablets in the following dosages: 4 mg, 8 mg, 12 mg. The packages contain 10, 15, 28, 30, 56 and 60 tablets. External part The tablets are coated with a special film coating;
Injection. The drug can be purchased in dosages: 1 mg – 10 ml ampoule 10 pieces; 5 mg -2 ml ampoule 10 pieces.

Mechanism of action

The presented drug has its own mechanism of action on the human body. A reversible cholinesterase inhibitor improves the perception of nerve impulses in the area of neuromuscular synapses, increases excitation processes in the reflex zones of the brain of the head and back, quickly destroys the blood-brain barrier, improves tone and actively stimulates smooth and skeletal muscles to contract, promotes normal secretion of digestive and sweat glands. Galantamine is well absorbed after subcutaneous administration drug.

Important! The content of the required amount of drug in the blood plasma required for therapy is achieved after half an hour.

A single use of the drug with a dosage of 10 milligrams leads to maximum concentration in blood plasma equal to 1.20 milligrams.

This result is observed after a couple of hours. The distribution period of Galantamine is 10 minutes.

When administering the drug parenterally, this period increases, unlike other drugs such as neostigmine, methyl sulfate and pyridostigmine.

For this reason, it begins to act much later than other inhibitors. The half-life of galantamine is 8 hours. 97% of the drug is excreted by the kidneys, 2.8% by the intestines and 0.2% by bile.

When is it effective?

The presented drug is used in the treatment various diseases. Galantamine has the following indications for use:

Alzheimer's disease to a moderate stage;
polio;
muscle dystrophy;
spastic paralysis;
vascular inflammatory disorders;
stroke;
meningitis;
myasthenia gravis;
decrease in intraocular pressure;
radiculitis;
neuritis;
myopathy.

Important! It is recommended to treat the disease with this pharmacological product only after consultation with a qualified doctor.

Contraindications for use

Galantamine – strong in its action pharmacological product, having a number contraindications:

bronchial type asthma, bronchitis;
heart disease;
disorders of the kidneys and liver;
intestinal obstruction;
diseases of the respiratory system;
pathologies of the gastrointestinal tract that arose after surgery;
age limit - up to 9 years;
increased sensitivity;
time period of bearing a child and feeding;
taking multiple medications at the same time;
peptic ulcers (intestinal ulcers, stomach ulcers, erosion).

Important! You should not use Galantamine if you have one of the following diseases.

Side effects

In case of improper use drugs or ignoring contraindications, the drug can cause a number of side effects in various systems human body.

Cardiovascular

In the cardiovascular system may appear following problems associated with drug use:

Digestive

Also, during use of the medicine, you may experience the following diseases related to the digestive system:

bloating of the abdominal area;
exhaustion of the body;
dry mouth;
intestinal problems;
excessive salivation;
gastritis;
liver problems;
discomfort of the gastrointestinal system.

Musculoskeletal

Taking the drug can cause the following pathologies:

weakness and muscle spasms;
fever;
anemia.

Urinary

Incorrect use of funds traditional medicine, can lead to a series negative consequences, related to the urinary system human body:

urinary incontinence;
hematuria;
frequent urination;
infectious diseases of the urinary system;
colic in the kidney area.

Nervous

Many medications negatively affect the nervous system of the human body. Galantamine is no exception. Side effects pharmaceutical products related to the nervous system:

Important! Strict adherence to instructions can allow a person to avoid side effects.

Mode of application

We offer a recipe for preparing the product for use. This medicine is taken orally during meals, washed down with a sufficient amount of running water. Dosage for adults and children is presented in the table.

It is necessary to start the treatment process with a small dosage, gradually bringing it to the recommended level. The tablets should be taken strictly according to the prescription issued by the doctor. Only in this case can positive results be achieved.

Analogs

The drug Galantamine has its own analogues.

These drugs have similar properties and can be used to treat similar diseases.

Analogues can be direct, when the active substance is absolutely identical to the original, and indirect, when some substances in the composition may differ from the control pharmaceutical drug.

Their main difference is the dosage of the medicine and its country of manufacture. The highest quality and well-known of them are presented in the table.

Name of the drug	Dosage, mg	Manufacturer country	Purpose
Nivalin	10-40 mg	Bulgaria	Poliomyelitis, myopathy, neuritis, radiculitis, cerebral palsy, Alzheimer's disease
Reminyl	4-24 mg	Italy	Chronic circulatory disorders in the brain, Alzheimer's disease
Neuromidin	5-20 mg	Latvia	Poliomyelitis, myopathy, neuritis, radiculitis, cerebral palsy, Alzheimer's disease, central nervous system diseases.
Prozerin	0.5-15 mg	Ukraine	Atrophy optic nerve, muscle paralysis, intestinal atony, meningitis, encephalitis.
Kalimin	60 mg	Germany	Intestinal atony, muscle weakness, kidney disease
Physistigmine	0.5 – 1 mg	USA, Russia	Attacks of glaucoma, neuromuscular diseases, atony of the intestines and urinary system.
Arisept	5-10 mg	USA	Alzheimer's disease.

What determines the quality of treatment?

It is not recommended to perform work that requires increased concentration, since the medicine blocks this body function.
It is necessary to monitor your body weight, because the presented drug leads to a sharp decrease in weight. And in diseases of the Alzheimer's type, normal weight is of great importance.
Need to keep an eye on drinking plenty of fluids. Galantamine absorbs all moisture entering the human body.
It is necessary to control blood pressure, which will constantly decrease and increase. It will be quite difficult to normalize it.
The drug is not intended for the treatment of patients with mild cognitive memory impairment.

Galantamine - all about the drug

Conclusion

Galantamine – domestic drug, which has an active positive impact on the cardiovascular, nervous, urinary, digestive, musculoskeletal system human body. The medication must be used according to a doctor's prescription to avoid side effects.