Galantamine Canon pills 8mg, 56pcs

Composition

1 tablet contains:

Active ingredients:  

• galantamine hydrobromide, in terms of galantamine-8 mg.

Auxiliary substances:  

• calcium hydrophosphate dihydrate,

• colloidal silicon dioxide (aerosil),

• copovidone (plasdon Es-630 or collidone VA-64),

• magnesium stearate,

• sodium croscarmellose (primellose),

• microcrystalline cellulose.

Shell composition: Advantia Prima 319974RC09 (hydroxypropyl methyl cellulose), macrogol (polyethylene glycol), caprin/caprylic triglyceride (glyceryl caprylocaprate), titanium dioxide, aluminum varnish based on quinoline yellow dye, aluminum varnish based on diamond blue dye, aluminum varnish based on indigo carmine dye.

Pharmacological action

Selective, competitive and reversible acetylcholinesterase inhibitor. It stimulates nicotine receptors and increases the sensitivity of the postsynaptic membrane to acetylcholine. Facilitates excitation in the neuromuscular synapse and restores neuromuscular conduction in cases of its blockade by non-depolarizing muscle relaxants.

Increases the tone of smooth muscles, increases 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 dementia, but does not affect the development of the disease itself.

Pharmacokinetics

The pharmacokinetics of galantamine are linear in the dose range of 4 -16 mg 2 times a day.

Suction

After a single oral dose of 8 mg, galantamine is rapidly absorbed from the gastrointestinal tract (GIT). The maximum concentration (Cmax) in blood plasma is reached after 1.2 hours and is about 43 ng / ml, the area under the concentration-time curve (AUC) is 427 ng x h / ml.

Distribution

Absolute oral bioavailability is 88.5%. Galantamine intake with food slows its absorption (Cmax decreases by 25%), but does not affect the area under the concentration-time curve (AUC). After repeated use of galantamine at a dose of 12 mg 2 times a day, the average concentrations at the end of the course and Cmax in blood plasma vary from 30 ng/ml to 90 ng/ml.

The volume of distribution is 175 ml. The binding of galantamine to plasma proteins is about 18%. In whole blood, galantamine is mainly found in shaped elements (52.7%) and in plasma (39%), while its fraction associated with plasma proteins is only 8.4%.

Metabolism

In vitro studies have shown that the main isoenzymes of the cytochrome P450 system involved in galantamine metabolism are the CYP2D6 isoenzyme, which is associated with the formation of O-demethylgalantamine, and the CYP3A4 isoenzyme, which is associated with the formation of N-oxide galantamine.

The amounts of radioactive substances excreted in the urine and feces did not differ between people with fast and slow metabolism. In the plasma of people with fast and slow metabolism, the main part of radioactive substances consists of unchanged galantamine and its glucuronide.

After a single dose of galantamine, none of the active metabolites (norgalantamine, O-demethylgalantamine, and O-demethylnorgalantamine) is present in the plasma of “fast” and “slow” metabolizers in an unconjugated form. Norgalantamine is detected in the blood plasma of patients after repeated use of galantamine, but its concentration is no more than 10% of the galantamine concentration.

Deduction

Galantamine elimination is bioexponential. The final half-life (T 1/2) is 7-8 hours. Plasma clearance of galantamine is about 200 ml / min. 18-22% of galantamine is excreted unchanged in the urine within 24 hours.

Renal clearance is about 65 ml / min, which is 20-25% of the total plasma clearance. Within 7 days after a single oral dose 3 N-galantamine at a dose of 4 mg 90-97% of radioactivity was excreted in the urine and 2.2-6.3% in the feces.

Pharmacokinetics of individual groups

In patients with Alzheimer’s disease, the concentration of galantamine in the blood plasma is 30% -40% higher than in healthy individuals.

In patients with mild hepatic impairment (Child-Pugh score 5-6), the pharmacokinetic parameters are similar to those in healthy patients. In patients with moderate hepatic impairment (Child-Pugh score 7-9), galantamine AUC and T 1/2 are increased by approximately 30%.

Patients with Alzheimer’s disease with impaired renal function with creatinine clearance of at least 9 ml/min do not need to adjust the dose of galantamine.

Indications

Symptomatic treatment of mild to moderate Alzheimer’s dementia.

Use during pregnancy and lactation

Contraindicated in pregnancy. Breast-feeding should be discontinued for the duration of treatment.

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 hepatic (more than 9 points on the Child – Pugh scale) disorders, mechanical intestinal obstruction, chronic obstructive pulmonary disease, obstructive diseases or recent surgery surgery on the gastrointestinal tract, obstructive diseases or recent surgical treatment of the urinary tract or prostate, children under 18 years of age, pregnancy and lactation. With caution: Light and moderate renal dysfunction or liver; the syndrome of weakness of the sinus node and other supraventricular conduction disorders;

concomitant use of drugs that slow heart rate (digoxin, beta-adrenoblokatora); General anesthesia; ulcer disease of stomach and duodenal ulcers, increased risk of erosive and ulcerative lesions of the gastrointestinal tract; chronic obstructive pulmonary disease (COPD).

Side effects

The frequency of side effects is classified according to WHO recommendations: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (

Immune system disorders

Infrequently: hypersensitivity.

Metabolic and nutritional

disorders are common: decreased appetite, anorexia.

Infrequently: dehydration (in rare cases leading to the development of renal failure).

Mental disorders

are common: hallucinations, depression (very rarely with suicide).

Infrequently: visual hallucinations, aggression, agitation.

Nervous system disorders

are common: fainting, dizziness, tremor, headache, drowsiness, lethargy, insomnia, fever.

Infrequently: paresthesia, taste distortion, hypersomnia, seizures (potentially cholinomimetic drugs can cause seizures), cerebrovascular diseases, transient ischemic circulatory disorders.

Very rare: exacerbation of Parkinson’s disease, seizures.

Visual disturbances

Infrequently: blurred visual perception.

Hearing disorders and labyrinth disorders

Infrequently: tinnitus.

Violation of the heart

Often: bradycardia.

Infrequently: supraventricular extrasystole, grade I atrioventricular block, sinus bradycardia, palpitation sensation, arrhythmia acute myocardial infarction, ischemic heart disease, tachycardia.

Vascular disorders

Often: arterial hypertension.

Infrequently: hypotension, hot flashes.

Disorders of the gastrointestinal tract

Very common: vomiting, nausea.

Common: abdominal pain, upper abdominal pain, diarrhea, dyspepsia, stomach discomfort, abdominal discomfort.

Infrequently: urge to vomit.

Very rare: Dysphagia, gastrointestinal bleeding.

Liver and biliary tract disorders

Rare: hepatitis.

Disorders of the skin and subcutaneous tissues

Often: hyperhidrosis.

Rare: skin rash.

Musculoskeletal and connective tissue

disorders are common: muscle spasms.

Infrequently: muscle weakness.

General disorders and disorders at the injection site

Often: increased fatigue, asthenia, malaise, weakness.

Laboratory and instrumental data:

Frequently used: weight loss.

Infrequently: increased activity of “liver” enzymes.

Injuries, intoxications, and manipulation complications

are common: falls, injuries.

Interaction

It is not recommended to combine with other cholinomimetics.

It is an opioid antagonist by its effect on the respiratory center. It exhibits pharmacodynamic antagonism to m-cholinolytics (atropine, homatropine methylbromide, etc. ), ganglioblockers, non-depolarizing muscle relaxants, quinidine, procainamide.

Aminoglycoside antibiotics may reduce the therapeutic effect of galantamine. Galantamine increases neuromuscular blockade during general anesthesia (including when used as a peripheral muscle relaxant suxamethonium). Medications that reduce the heart rate (digoxin, beta-blockers) increase the risk of worsening bradycardia.

Cimetidine may increase the bioavailability of galantamine.

All drugs that also inhibit cytochrome P450 isoenzymes (CYP2D6 and CYP3A4) may increase plasma galantamine concentrations when used concomitantly, resulting in an increased frequency of cholinergic side effects (mainly nausea and vomiting). In this case, depending on the patient’s tolerance to therapy, it may be necessary to reduce the maintenance dose of galantamine.

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.

Increases the depressing effect on the central nervous system of ethanol and sedatives.

How to take, course of use and dosage

Inside, while eating, with water.

Adults

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

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

For Alzheimer’s disease, treatment is recommended to start with taking 4 mg tablets 2 times a day. Within 4 weeks, the daily dose can be gradually increased to 16 mg-1 tablet of 8 mg 2 times a day-in the morning and in the 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 recovery of treatment should begin with the lowest dose and gradually increase it.

Patients with moderate hepatic and renal impairment

The initial dose is 4 mg once a day, which is taken in the morning, for at least 1 week, after which the dose is increased to 4 mg twice a day and taken for 4 weeks.

The total daily dose should not exceed 12 mg.

Overdose

Symptoms: 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 airways.

Treatment: gastric lavage, symptomatic therapy. As an antidote – intravenous use 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.

Special instructions

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 usually experience weight loss. In this regard, it is necessary to monitor the body weight of such patients.

During the treatment period, it is necessary to ensure sufficient fluid intake. Like other cholinomimetics, the drug can cause vagotonic effects from the cardiovascular system (including bradycardia), which should be taken into account in patients with sinus node weakness syndrome and other conduction disorders, as well as when used simultaneously with drugs that reduce heart rate (digoxin or beta-blockers).

When treated with Galantamine, there is a risk of occurrence, and therefore it is necessary to monitor 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 for the treatment of patients with mild cognitive impairment, i. e. with isolated memory impairment that exceeds the expected level for their age and education, but does not meet the criteria for Alzheimer’s disease.

Use in patients with liver function disorders

Contraindicated in severe hepatic impairment. Use caution in patients with mild to moderate hepatic impairment.

Use in patients with impaired renal function

Contraindicated in severe renal impairment. Use caution in patients with mild to moderate renal impairment.

Use in pediatrics

Contraindicated in children under 9 years of age.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, you should refrain from performing work that requires increased concentration of attention and speed of psychomotor reactions, including driving a car.

Composition

Tablet Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Galantamine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Alzheimer ‘s Disease