Universal reference book for medicines
Product name: REMINYL В® (REMINYL В® )

Active ingredient: galantamine

Type: Selective inhibitor of brain acetylcholinesterase.
The drug for Alzheimer's disease
Manufacturer: JOHNSON & JOHNSON (Russia) manufactured by JANSSEN-CILAG (Italy)
Composition, form of production and packaging
The tablets covered with a film cover of
white or almost white color, round, biconcave, on one side an engraving "JANSSEN", on another - "G4".

1 tab.

galanthamine hydrobromide 5.127 mg,

which corresponds to the content of galanthamine 4 mg

[PRING] lactose monohydrate, microcrystalline cellulose (premix in the ratio of 75% and 25% respectively);
crospovidone, magnesium stearate, silicon dioxide colloidal anhydrous.
The composition of the tablet shell: hypromellose 2910 (viscosity 5 mPa.s), propylene glycol, titanium dioxide (E171), talc, iron oxide yellow (E172).

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
The tablets covered with a film cover of pink color, round, biconcave, on one side an engraving "JANSSEN", on another - "G8".

1 tab.

galanthamine hydrobromide 10.254 mg,

which corresponds to the content of galantamine 8 mg

[PRING] lactose monohydrate, microcrystalline cellulose (premix in the ratio of 75% and 25% respectively);
crospovidone, magnesium stearate, silicon dioxide colloidal anhydrous.
The composition of the tablet shell: hypromellose 2910 (viscosity 5 mPa.s), propylene glycol, titanium dioxide (E171), talc, iron oxide red (E172).

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
The tablets covered with a film cover of orange-brown color, round, biconcave, on one side an engraving "JANSSEN", on another - "G12".

1 tab.

galantamine hydrobromide 15.38 mg,

which corresponds to the content of galantamine 12 mg

[PRING] lactose monohydrate, microcrystalline cellulose (premix in the ratio of 75% and 25% respectively);
crospovidone, magnesium stearate, silicon dioxide colloidal anhydrous.
The composition of the tablet coating: hypromellose (viscosity 5 mPa.s), propylene glycol, titanium dioxide (E171), talc, iron oxide red (E172), orange-yellow S (E110) dye.

14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Selective competitive and reversible inhibitor of acetylcholinesterase, is a tertiary alkaloid.
Increases the effect of acetylcholine on n-cholinergic receptors, apparently due to binding to the allosteric portion of the receptor.
By increasing the activity of the cholinergic system, it can improve cognitive function in patients with Alzheimer's dementia.

PHARMACOKINETICS

Suction

After a single oral dose of 8 mg is rapidly absorbed from the digestive tract.
C max is achieved in 1.2 h and is 43 В± 13 ng / ml, the average AUC is 427 В± 102 ng h / ml.Absolute bioavailability of galantamine when ingested is 88.5%. The intake of galantamine with food slows its absorption (C max decreases by 25%), but does not affect the amount of absorbed drug (AUC).
The pharmacokinetics of galantamine is linear in the dose range 4-16 mg 2 times / day.

Distribution

After repeated administration of galantamine at a dose of 12 mg 2 times / day, the average concentrations at the end of the course and C max in the plasma ranged from 30 ng / ml to 90 ng / ml.

In the equilibrium state, V d is 175 liters.

The degree of galantamine binding to plasma proteins is small and amounts to 17.7 В± 0.8%.
In the whole blood, galantamine is predominantly in shaped elements (52.7%) and in plasma (39%), whereas its fraction bound to plasma proteins is only 8.4%. The ratio of blood / plasma galantamine concentrations is 1.17.
Metabolism

After a single administration of galantamine, none of its active metabolites (norgalanthamn, O-demethyl-galantamine and O-demethyl-norhalanthamine) were present in the plasma of "fast" and "slow" metabolizers in unconjugated form.
Norgalantamine was detected in the plasma of patients after repeated administration of galantamine, but its amount was no more than 10% of the levels of galantamine.
Excretion

Elimination of galantamine is bi-exponential.
The final T 1/2 is approximately 7-8 hours.
The clearance from plasma is about 300 ml / min.

Within 7 days after a single oral intake of 4 mg of 3 H-galantamine, 90-97% of the radioactivity was excreted in the urine and 2.2-6.3% - with feces.
After intravenous administration and oral administration, 18-22% of the dose was excreted as unchanged galantamine in urine for 24 hours, the renal clearance was about 65 ml / min, which is 20-25% of the total clearance from the plasma.
Pharmacokinetics in special clinical cases

The results of clinical trials have demonstrated that in patients with Alzheimer's disease the concentration of galantamine in blood plasma is 30-40% higher than in young healthy individuals.

The pharmacokinetic parameters of galantamine in patients with mild violations of the liver function (5-6 points on the Child-Pugh scale) were similar to those of healthy individuals.
In patients with moderate impaired liver function (7-9 on the Child-Pugh scale), AUC and T 1/2 of galantamine were increased by approximately 30%.
Population pharmacokinetic study and analysis using a number of models have shown that in patients with Alzheimer's disease and renal dysfunction with QC at least 9 mL / min, the dose of galantamine should not be adjusted.

INDICATIONS

- dementia of the Alzheimer's type of mild or moderate degree, incl.
with concomitant deficiency of cerebral circulation.
DOSING MODE

Reminol should be taken 2 times / day, preferably during morning and evening meals.

The initial dose is 8 mg / day (4 mg 2 times / day), it should be taken within 4 weeks.

The maintenance dose is 16 mg / day (8 mg 2 times / day), it should also be taken at least 4 weeks.
The question of increasing the maintenance dose to the maximum recommended 24 mg / day (12 mg / day) should be addressed after a comprehensive assessment of the clinical situation, in particular, the effect achieved and tolerability.
With moderate violations of the liver function, the initial dose should be 4 mg 1 time / day, it should be taken in the morning for at least 1 week.
After that, patients can take 4 mg 2 times / day for at least 4 weeks.
If renal dysfunction (KK> 9 ml / min) dose of Remineral is not necessary to correct.

With the simultaneous administration of strong inhibitors of isoenzymes CYP2D6 or CYP3A4, it may be necessary to reduce the dose of Reminil.

SIDE EFFECT

On the part of the digestive system: during clinical trials, nausea, vomiting, abdominal pain, indigestion, anorexia were often observed (? 5% or with a frequency of twice the frequency in patients receiving placebo).
Nausea, vomiting and anorexia were more common in women.
From the side of the central nervous system: in clinical trials, often (? 5% or with a frequency of twice the frequency in patients receiving placebo), weakness, dizziness, headache, drowsiness;
also reported (? 5% or frequency of occurrence in patients receiving placebo) confusion, sudden falls, insomnia; rarely - a tremor, fainting.
Other: often - weight loss, trauma, rhinitis, urinary tract infections;
rarely - severe bradycardia.
CONTRAINDICATIONS

- severe renal dysfunction (CC <9 ml / min);

- pronounced impaired liver function (> 9 on the Child-Pugh scale);

- Hypersensitivity to galantamine or other components of the drug.

PREGNANCY AND LACTATION

Reminol can be prescribed during pregnancy only in those cases when the potential benefit of treatment for the mother exceeds the possible risk to the fetus.

If you need to use the drug during lactation, breastfeeding should be discontinued.

APPLICATION FOR FUNCTIONS OF THE LIVER

The drug is contraindicated for use in severe disorders of kidney function (QC less than 9 ml / min).
If renal dysfunction (KK> 9 ml / min) dose of Remineral is not necessary to correct.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

The drug is contraindicated for use in severe violations of the liver (more than 9 points on the scale Child-Pugh).
With moderate violations of the liver function, theinitial dose should be 4 mg 1 time / day, it should be taken in the morning for at least 1 week. After this, patients can take 4 mg 2 times / day for at least 4 weeks

APPLICATION FOR CHILDREN

Reminil is not recommended for children.
Data on the efficacy and safety of Reminil in pediatric practice are not available.
SPECIAL INSTRUCTIONS

In patients with Alzheimer's disease, weight loss is observed.
The use of acetylcholinesterase inhibitors, including Reminil, may also be accompanied by a decrease in body weight. Therefore, during treatment with Remineral it is necessary to monitor changes in body weight of patients.
Like other cholinomimetics, Reminil should be used with caution in cardiovascular diseases, because
due to its pharmacological action holinomimetiki can cause vagotonic effects from the heart (for example, bradycardia). With special care, the drug should be given to patients with SSSU and other supraventricular conduction disorders, as well as to patients who simultaneously receive drugs that reduce heart rate such as digoxin or beta-blockers.
In patients with an increased risk of developing erosive-ulcerative gastrointestinal lesions, for example having a history of peptic ulcer, it is necessary to monitor the patient's condition for the purpose of early detection of the corresponding symptoms.
It should be noted that during clinical trials in patients who received Reminil, there was no increase in the incidence of peptic ulcers and bleeding from the digestive tract compared to patients receiving placebo. Reminil is not recommended for use in patients with gastrointestinal obstruction, as well as in patients who have recently had an operation on the digestive system.
It is believed that holinomimetiki have a certain ability to cause generalized convulsions.
It should be remembered, however, that convulsive activity may be a manifestation of Alzheimer's disease itself. In clinical trials, there was no increase in the frequency of seizures in patients taking Reminil, compared with patients receiving placebo.
With caution appoint Reminil to patients with severe bronchial asthma or chronic obstructive pulmonary disease due to the cholinomimetic activity of the drug.

Reminil is not recommended for patients with obstruction of the urinary tract, as well as for people who have recently undergone an operation on the bladder.

After the abrupt withdrawal of Reminil (for example, when preparing for surgery), there is no aggravation of symptoms.

Most of the undesirable side effects occur against the background of a gradual increase in the dose of Reminil.
Nausea and vomiting (the most common phenomena) in most cases lasted less than 1 week and only occurred once. In such cases, antiemetic drugs and abundant drinking can be used.
Use in Pediatrics

Reminil is not recommended for children.
Data on the efficacy and safety of Reminil in pediatric practice are not available.
Impact on the ability to drive vehicles and manage mechanisms

Alzheimer's disease can worsen the ability to drive and work with machinery.
In addition, against the background of the use of Reminil, especially in the first weeks of its use, there may be drowsiness and dizziness, which also violate the ability to concentrate and negatively affect the driving and handling of machinery.
OVERDOSE

Symptoms: There may be muscle weakness, fasciculation, some or all of the symptoms of the cholinergic crisis (severe nausea, vomiting, abdominal cramping, increased salivation, lacrimation, urinary and fecal incontinence, severe sweating, bradycardia, hypotension, collapse, convulsions).
The expressed muscular weakness in a combination to a hypersecretion of a mucosa of a trachea and a bronchospasm can lead to a lethal outcome.
Treatment: if necessary, conduct symptomatic and supportive therapy.
In severe cases, atropine is administered as the antidote IV, the initial dose is 0.5-1 mg, the frequency of administration and the amount of subsequent doses depend on the dynamics of the clinical state of the patient.
DRUG INTERACTION

With simultaneous use, Reminil enhances the effect of other cholinomimetics, so this combination is not recommended.

Galantamine is an antagonist of anticholinergic drugs.

With the simultaneous use of Reminil enhances the effect of drugs that reduce heart rate (eg, digoxin and beta-blockers).

Being holinomimetikom, Reminil can strengthen the neuromuscular blockade caused by the action of peripheral muscle relaxants depolarizing type (for example, suksametonium) during anesthesia.

Pharmacokinetic interactions

In vitro studies have shown that the main role in the metabolism of galantamine is played by the isozymes CYP2D6 and CYP3A4.

Drugs that are potent inhibitors of CYP2D6 and CYP3A4 isoenzymes can increase the galactamine AUC.
Pharmacokinetic studies with repeated administration of drugs showed that the AUC of galantamine is increased by 30 and 40% with simultaneous application of it to ketoconazole and paroxetine, respectively. When used concomitantly with erythromycin, which is also an inhibitor of the CYP3A4 isoenzyme, the galactamine AUC increases by only about 10%. Pharmacokinetic studies in patients with Alzheimer's disease showed that the clearance of galantamine decreased by about 25-33% with the simultaneous use of this drug with known inhibitors of the isoenzyme CYP2D6, such as amitriptyline, fluoxetine, fluvoxamine, paroxetine or quinidine.
Thus, at the beginning of treatment with strong inhibitors of CYP2D6 and CYP3A4 isozymes, the incidence of adverse reactions associated with cholinomimetic activity, mainly nausea and vomiting, may increase.
In these situations, depending on the tolerability of therapy by a particular patient, a reduction in the maintenance dose of Reminil may be necessary.
The suppression of secretion of gastric juice does not impair the absorption of galantamine.

Therapeutic doses of galantamine (12 mg 2 times / day) did not affect the kinetics of digoxin and warfarin.
Galantamine did not affect the increase in prothrombin time caused by warfarin.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of 15 В° to 30 В° C.
Shelf life - 2 years.
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