Reminyl 8mg Janssen medicine treats intellectual decline (1 blister x 14 tablets)

Dosage form Box of 1 blister x 14 tablets
Specifications Galantamine

Ingredient

Composition information	Content
Galantamine	8mg

Uses

Indications

Reminyl 8 mg drug is indicated in cases of intellectual dementia caused by mild to moderate alzheimer disease.

Pharmacokic

galantamin, a third -order alkaloid, is a competitive, selective and reversible inhibitor for acetylchininesterase.

In addition, galantamin increases the internal impact of acetylcholin on nicotine receptors, perhaps through cohesion to an alloster position of receptors.

Therefore, an increase in the activity of the Cholinergic system associated with improving cognitive function can be achieved in patients with intellectual dementia caused by Alzheimer.

pharmacokinetic

absorption

After taking a single dose of 8 mg galantamin tablets, the absorption occurs quickly with a plasma peak concentration of 43 ± 13 ng/ml, achieved after 1.2 hours and the average AUC is 427 ± 102 ng. Galantamin's absolute bioavailability is 88.5%. Drinking Galantamin with food will reduce the absorption rate (CMAX decreases by about 25%), but does not affect the level of galantamin absorbed (AUC).

After taking the dose of 12 mg galantamin tablets 2 times/day, the average of the bottom concentration - the vertex of 30 and 90 ng/ml. The pharmacokinetics of galantamin linearly in the dose range from 4 - 16 mg 2 times/day.

Distribution

galantamin has an average distribution (VDSS on average 175 l).

Low plasma protein bonds: 17.7 ± 0.8%. In the blood of all stool, galantamin is mainly distributed to blood cells (52.7%), plasma fluid (39%) while the galantamin part is connected to plasma proteins only 8.4%. The rate of concentration of galantamin in the whole blood compared to plasma is 1.17.

Metabolism

The main metabolic paths are: n-oxidation, n-demethylation, o-demethylation, glucoronid and epimeization. O-Demethyl is much more important in strong metabolic people of CYP2D6.

The level of excretion of the total radioactive activity in urine and feces is no different between strong metabolic and poor metabolic people. In vitro studies have identified that cytochrom P450 2D6 and 3A4 are the main cytochrom p450 isenzyme involved in galantamin metabolism.

In the plasma of strong and poor metabolic people, the form of galantamin is constant and its glucoronids represent the majority of the radioactive activity of the sample. In the plasma of strong specialized people, glucoronid of O-Demethyl-Galantamin is also important.

There is no active metabolites of galantamin (Nor Galantamin, O-Desmethylgalantamin and O-Desmethyl-Norgalantamin) were detected in non-combination forms of strong plasma and poor metabolic people after a single dose.

Norgalantamin may be detected in plasma in patients after use many times, but not exceeding 10% of galantamin concentration.

Elimination

galantamin is a low -level drug (plasma clearance is about 300 ml/minute). Galantamin's excretion by the second -level exponential function, with the semi -discharged time at the end of about 7-8 hours.

7 days after taking a single dose of 4 mg 3h -galantamin, 90 - 97% radioactive activity is found in urine and 2.2 - 6.3% in feces. After intravenous or oral injection, 18-22% of the dose is excreted in the urine in the form of galantamin with constant 24 hours, with the renal clearance of about 65 ml/min, equivalent to 20-25% of the total plasma clearance.

Before taking Reminyl 8mg Janssen medicine treats intellectual decline (1 blister x 14 tablets)

How to use

Reminyl 8 mg is taken orally. Must make sure to drink enough water during treatment.

Should take the remedy capsule reminyl once a day in the morning, preferably during a meal.

Dosage

The recommended starting dose of the release capsules is 8 mg/day for 4 weeks.

The transition from instant release to prolonged release capsules

Patients being treated with instant release reminyl (tablets or oral solution) can be switched to reminl -released capsules by taking the last dose of instant releasing tablets or oral reminyl solution in the evening and starting with the remedy daily release of the next morning. When transferring from Reminyl instant release twice daily to Reminyl capsule released once a day, the total daily dose should be the same.

Maintenance dose

The starting dose is 16 mg once a day and the patient should be maintained at a dose of 16 mg daily for at least 4 weeks.

Increase the maintenance dose of up to 24 mg once a day needs to be considered after there is a proper assessment of clinical benefits and tolerance.

Medication stop

There is no reverse effect after sudden stop treatment (for example, preparing surgery).

Children

The use of reminyl for children is not recommended. There is no data on the use of reminyl for children.

kidney failure

Agriculture and galantamin in plasma may increase in patients with average renal failure (clearinin clearance = 52 - 104 ml/min) to severe (creatinine clearance = 9 - 51 ml/min).

No dose adjustment for patients with creatinine clearance> 9 ml /min.

The use of reminyl for patients with creatinn clearance below 9 ml/minute is not recommended because there is no enough data.

Hepatic failure

Agriculture galantamin in plasma has increased in patients with medium to severe liver or kidney failure.

In patients with average liver failure (Child-Pugh 7-September), based on the pharmacokinetic model, should start at a dose of 8 mg a day in at least 1 week, preferably in the morning. After that, patients should continue with 8 mg once daily with capsules released for at least 4 weeks. In these patients, the total daily dose should not exceed 16 mg.

The use of Reminyl for patients with severe liver failure (Child-Pugh scales> 9), not recommended.

Simultaneous treatment

It is necessary to consider reducing the dose in patients treated with strong CYP2D6 or CYP3A4 inhibitors.

Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.

What to do when overdose?

Symptoms and signs

Galantamin significant overdose and symptoms may occur similarly to the overdose of other cholin -like drugs.

These effects often affect the central nervous system, sympathetic system and nerve connectivity.

In addition to muscle weakness and local muscle vibration, some or all the manifestations of the cholinergic attack can onset: intense nausea, vomiting, gastrointestinal spasms, salivation, tearing, urination, defecation, sweating, slow heartbeat, hypotension, falling and convulsions. Increasing muscle weakness, along with hyperactivity and bronchospasm can lead to life -threatening.

There are post -torsion reports (Torsade de Pointes), extending the QT interval, slow heart rate, ventricular tachycardia and short -term eyes related to the overdose of Galantamin due to unintentional. In one case the dose is known, 8 tablets of 4 mg (total 32 mg) have been taken in a day.

Two more cases due to accidental 32 mg (nausea, vomiting and dry mouth: nausea, vomiting and chest pain under the breastbone) and a case of 40 mg oral (nausea) must be hospitalized for a period of time to monitor and recover completely.

A patient, who has been prescribed 24 mg/day and has a history of hallucinations for two years ago, took the wrong 24 mg twice a day for 34 days and developed an illusion that needs hospitalization.

Another patient was prescribed 16 mg/day oral solution, accidentally taking 160 mg (40 ml) that had sweating, vomiting, slow rhythm and almost fainted an hour later, needed to be hospitalized for treatment.

Symptoms of this patient have been resolved within 24 hours.

Treatment

Normal support measures should be used in all cases of overdose. For severe cases, anti -cholinergic drugs such as atropin are used as antidote to drugs that are similar to cholin. The starting dose should be 0.5 -1 mg intravenously, the next dose based on clinical response.

Due to the continuous overdose control strategies, contact the toxic control center to get the latest recommendations for over -treatment methods.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

Side Effects

When using Reminyl 8 mg, you may experience unwanted effects (ADR).

Common, ADR> 1/100

Metabolism and nutrition: Reduce appetite.

Mental system: depression, hallucinations

Muscle and connective tissue system: muscle spasm.

Metabolism and nutrition: dehydration. Khan.

Hepatitis system: Hepatitis.

Skin and subcutaneous tissue: Steven syndrome - Johnson, acute pustules, diverse roses.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Warnings

Contraindicated

Reminyl 8 mg drug is contraindicated in the following cases:

Do not use Reminyl for patients who have been hypersensitively to galantamin hydrobromid or any excipients of the drug.

Precautions when using

The mental dementia is different from the intellectual dementia of Alzheimer's disease

Reminyl is indicated for dementia treatment due to mild to moderate alzheimer disease. The benefits of reminyl in patients dementia in other bodies or other mental decline have not been proven.

Serious skin reactions

Serious skin reactions (Stevens-Johnson syndrome and acute pustules) have been reported in patients using Reminyl. Patients should be notified of signs of serious skin reactions and stop using Reminyl when the first signal of the skin rash appears.

Monitoring weight

Patients with Alzheimer's disease lost weight. The treatment of these patients with cholinesterase inhibitors, including galantamin, is related to weight loss. Therefore, it is necessary to monitor the patient seriously during treatment.

Cases of caution

As well as other cholin -like drugs, need to be cautious when using Reminyl in the following cases:

Cardiovascular: Due to pharmacological effects, cholin -acting drugs may have the effects of the sympathetic nerve force on the heart rate (for example: slow heart rate). This may be especially important for patients with "sinus node impairment syndrome" or there are types of ventricular disorders on ventricular or in people who are simultaneously using drugs that reduce their heart rate such as digoxin and beta receptor inhibitors. In clinical trials, the use of Reminyl is related to fainting and danger when it is related to the province's heart rate very slowly. However, clinical studies show that Reminyl does not increase the frequency of ulcer or gastrointestinal bleeding (compared to placebo). Reminyl should not be used for patients with gastrointestinal obstruction or patients who are recovering after the gastrointestinal tract surgery. The seizures can also be a manifestation of Alzheimer's disease.

Safety in patients with mild cognitive loss (MCI)

Reminyl is not indicated for patients with mild cognitive impairment (MCI), for example, those who have signs of memory impairment than expected than their age and knowledge, but do not satisfy the criteria of Alzheimer's disease.

The MCI research objects in two verified tests, for two years, does not satisfy the initial dual effectiveness.

Although the mortality rate in two low treatment groups, other deaths were first recorded in random objects using galantamin than fake, the rate of serious adverse events is the same between the two treatment groups.

Death due to many unpredictable causes in the elderly population group. When including data obtained from a large number of patients who have stopped treatment before the end of the double time, there is no evidence of increasing the risk of death in those treated with Reminyl during this time.

Objects in the placebo group stopped treatment before death than the galantamin group, could be the cause of the difference in the death of the initial recognition.

The ability to drive and operate machinery

Alzheimer's disease can gradually reduce the ability to drive and operate machinery. Moreover, like other Cholin drugs, Reminyl can cause adverse reactions (such as dizziness and sleep), which affects the ability to drive and operate machinery, especially in the first weeks after starting treatment

Pregnancy

There has been no research to use Reminyl in pregnant women. Only use Reminyl during pregnancy when the benefits of the drug gives mothers more important than the risk to the fetus.

Breastfeeding period

Reminyl is not known whether or not to be excreted through breast milk or not and no research in nursing women. Therefore, women who are drinking reminyl should not breastfeed.

Drug interaction

Pharmacological interactions

Due to the mechanism of action, galantamin should not be used simultaneously with other cholin -like drugs. Galantamin oppose the effect of anti -cholinergic drugs. Usually in drug -like drugs, pharmacological interaction can occur with medications significantly reducing heart rate (for example, digoxin and beta receptor inhibitors). Galantamin, as a cholin -like drug, can have a strong impact on Succinylcholin muscle relaxation during anesthesia.

Dynamic interactions

galantamin metabolizes through many roads and is discharged through the kidneys.

Based on in vitro studies, found that two yeasts mainly participated in the metabolism of galantamin, CYP2D6 and CYP3A4.

Galantamin's absorption is not reduced when the excretion of gastric acid is inhibited.

Other drugs influenced the metabolism of galantamin

Strong inhibitors CYP2D6 and CYP3A4 have increased (AUC) of galantamin.

Many dosage studies have shown that when taken with ketoconazole and paroxetin, Galantamin's AUC AUC increased in order of 30% and 40%. When taken with Erythromycin - another CYP3A4 enamel inhibitor - the AUC of Galantamin only increased by about 10%. Pharmacokinetic analysis on the population group with alzheimer disease shows that galantamin's clearance decreases by about 25 - 33% when it is taken with amitriptylin, fluoxetin, fluvoxamine, paroxetin and quinidine, which are CYP2D6 enamel inhibitors.

Therefore, in the beginning of treatment with strong inhibitors CYP2D6 and CYP3A4, the patient may increase the frequency of cholinergic side effects, mainly nausea and vomiting. In such cases, it is necessary to focus on tolerance to consider reducing the maintenance dose of galantamin.

Memantin, a N-methyl-D-Aspartat receptor antagonist (NMDA), at a dose of 10 mg/day for 2 days, followed by a dose of 10 mg 2 times a day for 12 days, there is no effect on the kinetic effect of Galantamin 16 mg/day in the constant state.

The effect of galantamin on the metabolism of other drugs

Galantamin treatment dose (12 mg x 2 times/day) does not affect the dynamic of digoxin and warfarin. Galantamin does not affect the effect of prolonging prothrombin caused by warfarin.

In vitro studies show that the potential for inhibition of galantamin for the main types of cytochrom P450 enamel in humans are very low.

Storage

Store at a temperature not exceeding 30 ° C.

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