Reminyl 8mg medicine Janssen treats intellectual decline (4 blisters x 7 tablets)

Dosage form Box of 4 blisters x 7 tablets
Specifications Galantamine

Ingredient

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Composition information	Content
Galantamine	8mg

Uses

Indications

Reminyl® is indicated in the following cases:

Intellectual decline due to mild to medium to moderate level.

Pharmacokic

galantamin, a third -order alkaloid, is a competitive, selective and recovery inhibitor for Acetylcholinesterase. In addition, galantamin increases the internal impact of acetylcholin to nicotine receptors, perhaps through cohesion to the receptor's Alloster position. As a result, it is possible to achieve an increase in the activity of the Cholinergic system associated with improving cognitive function in patients with dementia of Alzheimer.

pharmacokinetic

absorption

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

After taking the dose of 12 mg galantamin tablets twice a day, the peak and the average base in plasma fluctuates between 30 and 90 ng/ml. The pharmacokinetics of galantamin is linearly between 4 - 16 mg 2 times/day.

Distribution

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

Galantamin is low in connection with plasma protein: 17.7 ± 0.8%. In total blood, galantamin is distributed mainly in red blood cells (52.7%), and plasma fluid (39.0%), while the cohesion to the plasma protein is 8.4%. The ratio of total blood concentration compared to the plasma of galantamin is 1.17.

Metabolism

The main metabolic paths are: N - oxidation, n - n - demethylation, o - demethylation, glucuronid and epime. O - Demethyl is much more important in strong metabolic people of CYP2D6. The level of excretion of the total activity marking radioactive in urine and feces is not different from 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 galantamin form is unchanged and its glucuronid form represents most of the radioactive activity of the sample. In the plasma of strong metabolites, Glucuronid of O - Desmethyl - Galantamin is also important.

There is no active metabolites of galantamin (Norgalantamin, O - Desmethyl - Galantamin and O - Desmethyl - Norgalantamin) were discovered in non -combination forms of strong plasma or poor metabolites after a single dose. Norgalantamin may be detected in plasma in patients after multiple doses, but not exceeding 10% of galantamin concentration.

Elimination

galantamin is a low -level liquidity (plasma clearance in approximately 300 ml/minute). Elimination of galantamin by exponential, the last waste time is 7 - 8 hours.

7 days after taking a single dose of 4 mg 3h - galantamin, 90 - 97% of radioactive markers are found in urine and 2.2 - 6.3% in feces. After intravenous injection and oral use, 18-22% of the dose is excreted in the form of galantamin that does not change in urine for 24 hours, with the renal clearance of about 65 ml/min, equivalent to 20-25% of the total plasma clearance.

Before taking Reminyl 8mg medicine Janssen treats intellectual decline (4 blisters x 7 tablets)

How to use

Reminyl is taken orally.

Should take Reminyl tablets 2 times/day, best at breakfast and dinner.

Ensure adequate drinking water during treatment.

Dosage

Starting dose

The recommended starting dose of Reminyl tablets is 4 mg x 2 times/day for 4 weeks.

Transferring from instant release to long -term release capsules.

Patients who are being treated with instant release (tablet or oral solution) can be transferred to the reminl capsule capsules for prolonged release by taking the final dose of instant release tablets or drinking solution in the evening and starting to take Reminyl capsules lasting 1 time/day the next morning. When moving from Reminyl instant release 2 times/day to Reminyl capsule, the release of 1 time/day still keeps the total daily daily dose.

Maintenance dose

The starting dose is 16 mg/day (8 mg x 2 times/day with tablets) and patients should be maintained at a dose of 16 mg/day for at least 4 weeks.

Increase to a maximum maintenance dose of 24 mg/day (12 mg x 2 times/day with tablets) need to be considered after having proper assessments of clinical benefits and tolerance.

Stop treatment

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

Special subjects

Children

Do not use Reminyl for children. There is no data on the use of reminyl for children.

kidney failure

Increasing galantamin concentration may be increased in patients with average renal function. (Creatinin clearance = 52 - 104 ml/min) to severe (creatinine clearance = 9 - 51 ml/min).

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

Do not use reminyl for patients with creatinine clearance below 9 ml/min because there is no enough data.

Hepatic failure

Plasma galantamin concentrations can increase in patients with average to severe liver function, in patients with average liver function impairment (Child - PUGH point from 7-9), based on the pharmacokinetic model, the starting dose for tablets is 4 mg x 1 time/day for at least 1 week, best in the morning. After that, the patient may switch to a dose of 4 mg of tablets x 2 times/day for at least 4 weeks, in these patients, the total dose should not exceed 16 mg daily.

Do not use Reminylcho patients with severe liver function (Child - Pugh> 9).

Simultaneous treatment

It is necessary to consider reducing the dose in patients treated with strong CYP2D6 or CYP3A4 inhibitors (see the interaction of the drug with other drugs and other types of interactions - other drugs that affect the metabolism of galantamin).

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's symptoms and overdose may occur similarly to the overdose of other cholinergic stimulants. These effects often affect the central nervous system, sympathetic and neurotransmitter nervous system. In addition to muscle weakness or local muscle vibration, some or all the manifestations of a cholinergic attack may appear: intense nausea, vomiting, gastrointestinal spasm, increased salivation, watery, urination, defecation, sweating, slow heartbeat, hypotension, collapse and convulsions. Increasing muscle weakness, along with hyperactivity and bronchospasm can lead to life -threatening.

There have been after -sales reports of the peak, extending QT, slow heart rate, ventricular tachycardia and short consciousness related to the overdose of Galantamin due to unintentional. In a case of knowing the dose of use, 8 4 mg tablets (total 32 mg) were taken in a day.

Two more cases due to accidental taken 32 mg (nausea, vomiting, and dry mouth; nausea, vomiting, and chest pain under the breastbone) and a case of 40 mg (vomiting) lead to hospitalization for a short time to observe completely recovery. A patient, has been prescribed 24 mg/day and has a history of hallucinations for more than 2 years, has been taken at 24 mg/twice a day for 34 days and the progressive illusion needs to be hospitalized. Another patient, prescribed 16 mg/day oral solution, accidentally taken 160 mg (40 ml), sweating, vomiting, slow heartbeat 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 for cholinergic stimulants. The starting dose should be 0.5 - 1 mg intravenously, the next dose based on clinical response.

should contact the toxic control center to get the latest information about the overdose management by the current overdose control strategies.

What to do when forgetting 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®, you may experience unwanted effects (ADR).

The following adverse reactions are reported during the use of drugs in the market.

Common: ≥ 1/100 and

Mental disorders: hallucinations.

Pentecology: Hypertension.

Uncommon: ≥ 1/1000 and

The immune system disorder: Hypersensitivity.

Mental disorders: Virtual, virtual bar.

Nervous system disorders: convulsions.

Disorders of ears and mesmerizing: Tinnitus.

Rare: ≥ 1/10000 and

Heart disorders: Bock completely.

Hepatitis: Hepatitis.

Unknown: It is impossible to estimate from available data

Disorders on the skin and subcutaneous tissue: Steven syndrome - Johnson, Excavaded pus disease, diverse roses.

Instructions on how to handle ADR

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

Before using the drug you need to read the instructions carefully and refer to the information below.

Contraindicated

Reminyl® drug contraindicated in the following cases:

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

Caution when using

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

Reminyl is expected to treat intellectual dementia 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 (see unwanted effects). Patients should be notified of signs of serious skin reactions and stop using Reminyl when the first signs appear on the skin.

Monitoring weight

Patient Alzheimer lost weight. Treatment with cholinesterase inhibitors, including galantamin, is related to weight loss in these patients.

Need to monitor patients with treatment during treatment.

Cases of caution

As well as other cholinergic stimulants, Reminyl should be cautious when used in the following cases:

Cardiovascular disease: Due to pharmacological effects, the cholinergic stimulants may have the effects of increased sympathetic nerve tone on the heart rate including slow heart rate and all types of atrial atrial block block (see unwanted effects). This may be especially important for patients with "sinus node impairment syndrome" or there are types of conduction disorders on ventricular or in people who are simultaneously using a significant heart rate reduction such as digoxin and beta receptor inhibitors. In clinical studies, the use of Reminyl has been related to fainting and rarely related to very slow heart rate. However, clinical studies show that Reminyl does not increase the frequency of ulcer and gastrointestinal bleeding compared to placebo. Reminyl should not be used for patients with pathologies that cause gastrointestinal obstruction or patients who are recovering after the gastrointestinal tract surgery. The seizures can also be an expression of Alzheimer's disease.

Safety in patients with mild cognitive decline (MCI) Reminyl is not indicated for those who have a mild cognitive impairment (MCI), that is, those who have been shown to be a more severe memory decline inappropriate than their age and knowledge, but do not satisfy the criteria of Alzheimer's disease.

The ability to drive and operate machinery

Alzheimer's disease can gradually reduce the ability to drive and operate machinery. Moreover, like other Cholinergic stimulants, Reminyl can cause adverse reactions (such as dizziness and sleep), which can affect the ability to drive and operate machinery, especially in the first week of treatment.

Pregnancy

There has been no research to use Reminyl in pregnant women. Only use reminyl during pregnancy when the effect is outstanding potential risk to the fetus.

Breastfeeding period

clear whether reminyl treatment is excreted through breast milk or not and no research in breastfeeding women. Therefore, women who are drinking reminyl should not breastfeed.

Drug interaction

Mobile interactions

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

Based on in vitro studies, found two enzymes mainly involved 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 can increase the AUC of Galantamin.

Dermatological pharmacokinetic studies show that when taken with ketoconazole and paroxetin, Galantamin's AUC AUC increases in order of 30% and 40%. When taken with Erythromycin, another CYP3A4 inhibitor, Galantamin's AUC only increased by about 10%. Pharmacokinetic analysis (PK) in the group of Alzheimer patients shows that galantamin's clearance decreases by about 25 - 33% when taken with amitriptylin, fluoxetin, fluvoxamine, paroxetin and quinidine, known as CYP2D6 inhibitors.

Therefore, during the beginning of treatment with strong CYP2D6 or CYP3A4 inhibitors, the patient may increase the frequency of cholinergic -style side effects, mainly nausea and vomiting. In such cases, it is necessary to rely on tolerance and consider reducing the maintenance dose of galantamin. (See dosage and usage - Special object).

Memantin, a receptor -resistant - methyl - d - aspartat (NMDA), at 10 mg/day for 2 days, followed by a dose of 10 mg x 2 times/day for 12 days without impact on pharmacokinetics of Galantamin 16 mg/day in a stable state.

Galantamin's image to metabolism of other drugs

Galantamin treatment dose (12 mg x 2 times/day) does not affect the pharmacokinetics of Digoxin and Warfarin. Galantamin does not affect the long -lasting effect prothrombin of warfarin.

In vitro studies have shown the potential for inhibition of galantamin for the main types of cytochrom P450 in humans are very low.

Pharmacological interactions

Due to the mechanism of action, galantamin should not be used simultaneously with other cholinergic stimulants. Galantamin oppose the effect of anti -cholinergic drugs. Usually in the cholinergic stimulants, pharmacological interaction can occur with significant reduced heart rate (for example: digoxin and beta receptor inhibitors). Galantamin, as a cholinergic stimulant, can have a strong impact on the sucinylcholin muscle relaxation during anesthesia.

Storage

Store at temperatures not exceeding 30 ° C.

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