Galantamine - Instructions For Use, Price, Reviews, Analogs, Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Galantamine

Galantamine: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Galantamine

ATX code: N06DA04

Active ingredient: galantamine (Galantamine)

Manufacturer: VIFITECH (Russia); Ozone LLC (Russia); Canonfarma Production, JSC (Russia)

Description and photo updated: 2019-27-08

Prices in pharmacies: from 407 rubles.

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Galantamine is a drug for the treatment of dementia, including Alzheimer's disease.

Release form and composition

• film-coated tablets: round, biconvex, tablets with a dosage of 8 mg have a risk on one side; at the break, two layers stand out: an almost white core and an almost white or white film casing (7, 10, 14, 15, 25, 30 or 50 pieces in blisters, 1–6 or 10 packages in a cardboard box; 10, 20, 30, 40, 50, 56, 60 or 100 pieces in polymer or polyethylene terephthalate cans, 1 can in a cardboard box);
• solution for intravenous (i / v) and subcutaneous (s / c) administration: clear colorless liquid (1 ml in ampoules, in a blister strip packaging 5 ampoules, 2 packs complete with a scarifier or without in a cardboard box).

Each pack also contains instructions for the use of Galantamine.

Composition of 1 tablet:

• active substance: galantamine hydrobromide - 5.126; 10.253 or 15.38 mg (corresponds to the content of galantamine - 4, 8 or 12 mg);
• auxiliary components: aerosil (colloidal silicon dioxide), calcium hydrogen phosphate dihydrate, copovidone (Plasdon Es-630 / Kollidon VA-64), magnesium stearate, primellose (croscarmellose sodium), microcrystalline cellulose;
• film casing: AdvantiaTM Prima 319974RC09 (hydroxypropyl methylcellulose, polyethylene glycol, titanium dioxide, glyceryl caprylocaprate, aluminum varnish based on dyes: brilliant blue, quinoline yellow, indigo carmine).

Composition of 1 ml solution for intravenous and subcutaneous administration:

• active substance: galantamine hydrobromide (in terms of dry matter) - 1 or 5 mg;
• auxiliary component: water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

Galantamine hydrobromide is a selective inhibitor of cerebral acetylcholinesterase, facilitating the conduction of nerve impulses in the area of synapse between muscles and nerve endings. Penetrating well through the blood-brain barrier, it enhances the processes of excitation in the reflexogenic zones of the brain and spinal cord. By stimulating the contraction of skeletal and smooth muscles, it increases its tone, improves the secretion of the glands (digestive, sweat), and helps restore neuromuscular conduction blocked by non-depolarizing muscle relaxants. It causes a spasm of accommodation, miosis, and in case of angle-closure glaucoma, it lowers intraocular pressure.

Pharmacokinetics

Pills

Galantamine after oral administration is rapidly and fully absorbed in the gastrointestinal tract. The absolute bioavailability is high - up to 90%. The therapeutic concentration of the substance is reached in 30 minutes. Achievement of C _max (maximum concentration) after taking 8 mg of galantamine is observed in the period from 60 to 120 minutes and is 1.2 mg / ml.

T _1/2 (half-life) - 5 hours. Equilibrium concentration is established after repeated administration.

It binds weakly to blood proteins. Easily crosses the blood-brain barrier. It is metabolized to an insignificant extent (approximately 10%) in the liver by demethylation.

Excretion occurs mainly in the urine (up to 74%) in the form of metabolites and unchanged substances. Renal clearance is about 100 ml / min.

Plasma concentrations of galantamine may increase in patients with Alzheimer's disease. Also, this indicator increases with moderate to severe impairment of liver / kidney function.

Solution for intravenous and subcutaneous administration

Galantamine is rapidly absorbed after subcutaneous administration. The time to reach a therapeutic concentration in blood plasma is 30 minutes. There was no statistically significant difference in AUC (area under the concentration-time curve) after a single dose of 10 mg administered parenterally or orally. C _max in blood plasma after a single dose of 10 mg administered by any of the two methods is 1.20 mg / ml, the time to reach it is 2 hours.

The half-life of galantamine is 10 minutes. This value is longer in comparison with the value of the indicator for neostigmine methyl sulfate and pyridostigmine bromide (0.54-3.5 and 5.0-6.6 minutes, respectively), so it begins to act later than other cholinesterase inhibitors.

V _d (volume of distribution) of the substance - 175 l, binding to plasma proteins - no more than 18%; approximately 53% of galantamine is in the blood cells.

T _{1/2 is} two _- phase and takes 7 to 8 hours.

Galantamine metabolism does not differ in intensity, it occurs with the participation of cytochrome P450 isoenzymes (CYP2D6 and CYP3A4 isoenzymes), mainly by N- and O-demethylation (about 5-6% of the dose), as well as glucuronidation, epimerization and N-oxidation. The main metabolites found in urine and plasma are galantaminone and epigalanthamine.

Excretion of 90–97% of galantamine occurs by the kidneys (unchanged - from 18 to 22%) through glomerular filtration, by the intestines - 2.2–6.3%, with bile - approximately 0.2%. Renal clearance is in the range from 65 to 100 ml / min (20-25% of plasma clearance), this value is close to inulin clearance.

In Alzheimer's disease, the plasma concentration of galantamine exceeds the value of this indicator in healthy volunteers by 30-40%. Moderate hepatic impairment slows down the elimination of galantamine by about 25%. Moderate chronic renal failure (with creatinine clearance from 52 to 104 ml / min) increases its plasma concentration by 38%, in severe disorders (in patients with creatinine clearance of 9-51 ml / min) - by 67%.

Indications for use

Pills

• dementia of the Alzheimer's type in mild to moderate stage;
• poliomyelitis, developing immediately after the end of the febrile period, in the recovery period or in the period of residual phenomena;
• progressive muscular dystrophy, myasthenia gravis, infantile cerebral palsy, radiculitis, neuritis, myopathy.

Solution

Diseases of the central and peripheral nervous system:

• neuritis, polyneuropathy, polyneuritis, other diseases of the peripheral nervous system;
• muscle atrophy, flaccid paralysis, myoclonic convulsions as a result of damage to the anterior horns of the spinal cord after myelitis, poliomyelitis, spinal muscular atrophy;
• cerebral palsy after a stroke, spastic forms of cerebral palsy (cerebral palsy);
• disorders of neuromuscular transmission (myasthenia gravis).

In surgery and anesthesiology, Galantamine solution is used as an antagonist of non-depolarizing muscle relaxants, as well as for the treatment of postoperative paresis of the small intestine and urinary bladder.

In physiotherapy of neurological diseases of the peripheral nervous system, the drug is used for iontophoresis, and in toxicology - in case of poisoning with cholinesterase inhibitors (as an antidote).

Contraindications

Absolute contraindications:

• bradycardia;
• atrioventricular (AV) block;
• hyperkinesis;
• bronchial asthma;
• arterial hypertension;
• chronic heart failure (CHF) - for pills;
• severe heart failure III – IV group according to the classification of the New York Heart Association (NYHA) - for solution;
• angina pectoris;
• epilepsy;
• severe renal impairment with creatinine clearance (CC) <9 ml / min;
• severe liver dysfunction on the Child - Pugh scale> 9 points;
• chronic obstructive pulmonary disease (COPD);
• mechanical intestinal obstruction, recent surgery or obstructive diseases of the gastrointestinal tract (GIT) - for tablets;
• mechanical violations of the patency of the urinary tract - for solution;
• recently undergone surgery or obstructive diseases of the prostate, urinary tract;
• the period of pregnancy and breastfeeding;
• children's age: for tablets - up to 9 years, for solution - up to 1 year;
• individual hypersensitivity to any component of the drug.

Relative contraindications (the drug is used with caution):

• tablets: for mild and moderate renal / liver dysfunction, sick sinus syndrome (SSS) and other supraventricular conduction disorders, concomitant use with drugs that slow down the heart rate (HR), for example, β-blockers, digoxin, with general anesthesia, peptic ulcer of the stomach and duodenal ulcer, an increased risk of developing erosive and ulcerative lesions of the gastrointestinal tract;
• solution: for renal / hepatic failure, urinary disorders, surgical interventions using general anesthesia.

Galantamine, instructions for use: method and dosage

Pills

The tablets are taken orally during meals with water.

The recommended daily dose for adult patients: 8-32 mg taken in 2-4 divided doses. When treating myasthenia gravis, it is recommended to divide the daily dose into 3 doses.

Treatment of Alzheimer's disease is recommended to begin with taking 4 mg tablets 2 times a day (morning and evening). For 4 weeks, the dose can be gradually increased to 16 mg per day: 1 tablet at a dose of 8 mg 2 times a day.

Patients taking pills should provide the body with a sufficient amount of fluid. If it is necessary to interrupt the course, the restoration of therapy begins with the lowest dose, increasing it gradually.

With moderate renal / hepatic impairment, the initial dose of galantamine is 4 mg; the pill is taken 1 time per day, in the morning, for at least a week, then the dose is increased to 4 mg 2 times a day and taken for four weeks. The maximum daily dose for this category of patients is ≤ 12 mg.

Recommended doses for the treatment of polio and cerebral palsy in children over 9 years old:

• 9-11 years: daily dose - 4-12 mg in 2-3 doses;
• 12-15 years: daily dose - 4-16 mg in 2-4 doses.

Solution

Galantamine solution is intended for intravenous and subcutaneous administration.

The dose and duration of the course of therapy is determined by the doctor depending on the severity of the symptoms of the disease and the individual response of the patient.

For the treatment of diseases of the central and peripheral nervous system, Galantamine in the form of a solution is used for a short time, only when there is no possibility of taking the drug inside. As soon as the patient's condition permits, he is transferred to oral administration of galantamine.

The recommended dosage regimen for adult patients: the dose is determined at the rate of 0.03-0.28 mg / kg. Treatment is started with minimum doses, which are increased gradually. The initial daily dose is 2.5 mg, its increase can be carried out gradually, every 3-4 days by 2.5 mg. The maximum daily dose of 20 mg is divided into 2–3 doses in equal amounts, but not more than 10 mg of galantamine per administration.

For children, the drug is administered subcutaneously, the daily dose is determined for children 1–2 years old at the rate of 0.02–0.08 mg / kg, over 3 years old - 0.03–0.28 mg / kg:

• 1-2 years - 0.25-1 mg;
• 3-5 years - 0.5-5 mg;
• 6-8 years old - 0.75-7.5 mg;
• 9-11 years old - 1-10 mg;
• 12-15 years old - 1.25-12.5 mg;
• > 15 years - 1.25-15 mg.

Recommended doses of galantamine in surgery, anesthesiology, toxicology:

• overdose with peripheral non-depolarizing muscle relaxants: 10–20 mg per day intravenously;
• postoperative paresis of the gastrointestinal tract and bladder: in doses determined according to age, distributed over 2-3 s / c or i / v injections per day;
• physiotherapeutic procedures: 2.5–5 mg is administered by iontophoresis at an electric current of 1–2 mA for 10 minutes. The duration of the course is 10-15 days.

Side effects

Pills

• cardiovascular system: increase or decrease in blood pressure (BP), heart failure, atrial flutter / atrial fibrillation, orthostatic collapse, edema, atrioventricular (AV) block, lengthening of the QT interval, ventricular and supraventricular tachycardia, hot flashes, suprajsticular ischemia / myocardial infarction;
• digestive system: bloating, gastrointestinal discomfort, abdominal pain, dyspepsia, anorexia, nausea / vomiting, diarrhea, gastritis, dry mouth / increased salivation, dysphagia, diverticulitis, duodenitis, gastroenteritis, hepatitis, upper esophageal mucosal perforation and lower gastrointestinal tract;
• musculoskeletal system: myasthenia gravis, muscle spasms, fever;
• urinary system: hematuria, urinary incontinence, frequent urination, urinary retention, urinary tract infections, renal colic, calculus;
• nervous system: often - syncope, tremors, lethargy, auditory and visual hallucinations, taste perversion, behavioral reactions (including agitation / aggression), transient cerebrovascular accident / stroke, dizziness, headache, muscle spasms, convulsions, paresthesia, apraxia, ataxia, aphasia, hypo- or hyperkinesis, anorexia, drowsiness / insomnia;
• sense organs: rhinitis, epistaxis, accommodation spasm, visual impairment, tinnitus;
• psyche: apathy, increased libido, paranoid states, delirium, depression (in extremely rare cases before suicide);
• laboratory parameters: anemia, hypokalemia, increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), increased blood levels of alkaline phosphatase or sugar;
• hematological pathologies: thrombocytopenia, purpura;
• general reactions: chest pain, hyperhidrosis, weight loss, dehydration (in rare cases, before the development of renal failure), fatigue, bronchospasm.

Solution

• cardiovascular system: AV block, increase or decrease in blood pressure, bradycardia, angina pectoris, palpitations, prolongation of the QT interval;
• nervous system: headache, dizziness, insomnia / drowsiness, tremors;
• sense organs: epistaxis, accommodation spasm, visual impairment, tinnitus, rhinitis;
• Gastrointestinal tract: abdominal pain, nausea / vomiting, increased salivation, increased intestinal peristalsis, diarrhea;
• reactions to stimulation of cholinergic receptors: pronounced nicotinic or muscarinic (to a lesser extent) actions characteristic of cholinesterase inhibitors;
• hypersensitivity reactions: rash, itching, urticaria, rhinitis; possible acute allergic reactions up to anaphylactic shock with loss of consciousness;
• other reactions: hyperhidrosis, muscle spasms, loss of appetite, weight loss.

The presence of these or other side effects and their aggravation should be reported to the doctor. When m-cholinomimetic reactions increase, the daily dose must be reduced or interrupted for 2-3 days, and then continued with lower doses.

Overdose

Symptoms of a galantamine overdose are: colic (cramps) in the abdomen, increased salivation, nausea / vomiting, diarrhea, lacrimation, urinary and fecal incontinence, hyperhidrosis, decreased blood pressure, bradycardia, prolonged QT interval, bronchospasm, myasthenia gravis, and in more severe cases, convulsions … The consequence of severe muscle weakness in combination with bronchospasm and hypersecretion of the tracheal mucosa can be a complete blockage of the airways.

Therapy of the condition is symptomatic, including control of the respiratory function and the cardiovascular system. As an antidote, it is recommended to administer atropine intravenously in an initial dose of 0.5–1 mg, then the dose of atropine is determined depending on the response to therapy and the patient's condition.

special instructions

The use of acetylcholinesterase inhibitors is accompanied by a decrease in body weight, especially this should be taken into account in the treatment of patients with Alzheimer's disease, regularly monitoring their weight.

Patients taking Galantamine require adequate fluid intake.

The vagotonic effect of galantamine, as well as other cholinomimetics, on the sinoatrial node, can cause bradycardia and AV block. This should be taken into account in patients with SSS, other conduction disorders and while using the drug with drugs that lower heart rate (digoxin, β-blockers). According to post-registration observations, patients without cardiac pathologies also had a slowing of the heart rate, therefore, all patients using galantamine are at risk of intracardiac conduction disturbances.

Due to the risk of syncope, it is necessary to monitor blood pressure more often, especially when taking high doses of the drug (from 40 mg galantamine per day or more). To prevent such adverse reactions at the beginning of therapy, the dose of the drug must be selected very carefully. The effectiveness of galantamine in patients with other types of dementia and memory impairment has not been established.

Cholinomimetics are capable of increasing gastric secretion, which requires constant monitoring of patients at risk of gastrointestinal ulcers and gastrointestinal bleeding. Also, taking cholinomimetics can cause impaired urine flow.

During the period of Galantamine therapy, it is unacceptable to take ethanol and sedatives.

Influence on the ability to drive vehicles and complex mechanisms

Since galantamine can cause dizziness, drowsiness, visual impairment, during treatment, you should refrain from performing types of work that require speed of psychomotor reactions and increased concentration of attention, including from driving.

Application during pregnancy and lactation

Galantamine is not prescribed during pregnancy / lactation.

Pediatric use

It is contraindicated to use Galantamine tablets for children under 9 years of age. The solution is not prescribed for the treatment of children under the age of 1 year.

With impaired renal function

• severe renal dysfunction (in patients with CC <9 ml / min): therapy is contraindicated;
• mild to moderate renal impairment: Galantamine is administered under medical supervision.

For violations of liver function

• severe liver dysfunction (Child-Pugh scale> 9 points): therapy is contraindicated;
• mild to moderate liver dysfunction: Galantamine is administered under medical supervision.

Drug interactions

• opioids (morphine and its structural analogs): galantamine is their antagonist in terms of action on the respiratory center;
• m-anticholinergics (atropine, homatropine, methyl bromide, etc.), ganglion blockers, non-depolarizing muscle relaxants, quinine, procainamide: galantamine exhibits pharmacodynamic antagonism towards them;
• aminoglycoside antibiotics (amikacin, gentamicin): may reduce the therapeutic effect of galantamine;
• drugs for general anesthesia (including suxamethonium as a peripheral muscle relaxant): galantamine enhances neuromuscular blockade during anesthesia;
• drugs that reduce heart rate (digoxin, β-blockers): increase the likelihood of worsening bradycardia;
• cimetidine: an increase in the bioavailability of galantamine is possible;
• drugs that inhibit isoenzymes of the cytochrome P _{450 system} (CYP2D6 and CYP3A4): an increase in plasma concentrations of galantamine is possible with a further increase in the frequency of cholinergic side effects (mainly nausea and vomiting), which may require a decrease in the maintenance dose of galantamine;
• ethanol and sedatives: galantamine enhances their depressant effect on the central nervous system.

Galantamine is not recommended to be combined with other cholinomimetics.

Analogs

Galantamine analogues are: Galantamine-Teva, Galnora-SR, Nivalin, Reminil.

Terms and conditions of storage

Keep out of the reach of children.

Store in a place out of the reach of light, keep the tablets from moisture, storage temperature up to 25 ° C.

Shelf life: tablets - 2 years, solution - 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Galantamine

According to reviews, Galantamine is often used in clinical practice, especially for the treatment of Alzheimer's disease in elderly patients. Therapy is not effective in all cases. They indicate the development of side effects and the need to correct the regimen.

Price for Galantamine in pharmacies

The approximate price for Galantamine is: 4 mg tablets (14 pcs.) - 397-617 rubles, 8 mg tablets (56 pcs.) - 2138-2153 rubles, injection solution 1 mg / ml (10 ampoules of 1 ml) - 1298-1568 rubles.

Galantamine: prices in online pharmacies

Drug name Price Pharmacy

Galantamine Canon 4 mg film-coated tablets 14 pcs. 407 r Buy

Galantamine Canon tablets p.o. 4mg 14 pcs. 430 RUB Buy

Galantamine Canon 8 mg film-coated tablets 56 pcs. 1055 RUB Buy

Galantamine 12 mg film-coated tablets 56 pcs. 2396 RUB Buy

Galantamine Canon tablets p.o. 8mg 56 pcs. 2477 RUB Buy

Galantamine Canon 12 mg film-coated tablets 56 pcs. RUB 2780 Buy

Galantamine Canon tablets p.o. 12mg 56 pcs. 2808 RUB Buy

Galantamine 12 mg film-coated tablets 56 pcs. 2885 RUB Buy

Galantamine 8 mg film-coated tablets 56 pcs. RUB 2939 Buy

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!