Exelon Transdermal therapist sist 9.5 mg/24h N30 (Novartis)

Exelon Transdermal therapist sist 9.5 mg/24h N30 (Novartis)

Exelon is a selective inhibitor of brain acetyl- and butyrylcholinesterase used to treat Alzheimer's disease and dementia in Parkinson's disease. Rivastigmine slows down the destruction of the neurotransmitter acetylcholine produced by functionally intact neurons. At the same time, rivastigmine selectively increases the content of acetylcholine in the cerebral cortex and hippocampus, and thus helps to improve cholinergic nerve transmission. Exelon may have a positive effect on cognitive decline associated with acetylcholine deficiency, in particular in dementia associated with Alzheimer's disease and Parkinson's disease. In addition, there is evidence that inhibition of cholinesterases can slow down the formation of fragments of the amyloid-beta precursor protein involved in amyloidogenesis, and thus slow down the formation of amyloid plaques, which are one of the main pathological hallmarks of Alzheimer's disease. Rivastigmine interacts with the target enzyme with the formation of a covalent bond, which leads to temporary inactivation of the enzyme. In young healthy men, after taking Exelon 3 mg, cerebrospinal fluid (CSF) acetylcholinesterase activity has been shown to decrease by approximately 40% during the first 1.5 hours. After reaching the maximum inhibitory effect, enzyme activity returns to its original level after approximately 9 hours. It has been shown that butyrylcholinesterase activity in the CSF of young healthy volunteers is inhibited reversibly and is restored to its original level after 3-6 hours. In patients with Alzheimer's disease, the inhibition of acetylcholinesterase activity in the CSF by rivastigmine is dose-dependent over the dose range studied (up to the highest dose of 6 mg twice daily). Inhibition of butyrylcholinesterase is also dose-dependent: a dose of 6 mg 2 times a day causes a decrease in enzyme activity by more than 60% compared to the original. This effect of Exelon persisted for 12 months of therapy (the maximum period studied). Statistically significant correlations have been shown between the degree of inhibition of both CSF enzymes by rivastigmine and changes in cognitive function in patients with Alzheimer's disease; Moreover, it is the inhibition of butyrylcholinesterase in the CSF that reliably and consistently correlates with improved results of tests of memory, attention and reaction speed. The effectiveness of Exelon therapy for Alzheimer's disease has been shown in patients with mild to moderate dementia (10-24 points on the Mini Mental State Examination, MMSE). According to clinical studies, Exelon therapy leads to a significant improvement in cognitive functions (attention, memory, speech, etc.), functional status and activity in everyday life, as well as a decrease in the severity of the disease and the severity of mental and behavioral manifestations (such as agitation, tearfulness, illusions, hallucinations, etc.). Studies have shown that the effect of Exelon therapy is observed approximately at week 12 and persists for 6 months of therapy, while during the control period in the group of patients receiving placebo, a deterioration in the corresponding indicators was observed. In dementia associated with Parkinson's disease, the effectiveness of Exelon was demonstrated in a placebo-controlled study lasting 24 weeks in patients with mild to moderate dementia (MMSE score 10 - 24). Patients receiving Exelon showed a statistically significant improvement in cognitive functions (attention, memory, speech, etc.), while in patients receiving placebo, similar indicators worsened.

Exelon, 9.5 mg/day, transdermal therapeutic system, 30 pcs.

Transdermal.

Therapy with the drug should only be carried out under the supervision of a physician experienced in treating patients with dementia and under the supervision of persons caring for the patients. Patients and their caregivers should be instructed by competent healthcare professionals about the use of the drug.

The amount of rivastigmine contained and released depending on the dosage of TTS Exelon® is presented in the table.

Table

Mild or moderate dementia of the Alzheimer's type

Initial dose and selection of the recommended effective dose.

Treatment with the drug should begin with the use of TTC Exelon® 4.6 mg/day once a day.

After a minimum of 4 weeks of treatment, if well tolerated, the dose of the drug should be increased to the recommended effective dose by using TTC Exelon® 9.5 mg/day, which can be used as long as the therapeutic effect remains.

Increasing the dose.

For long-term treatment, if the patient has therapeutic efficacy, it is recommended to use TTC Exelon® 9.5 mg/day. If the drug is well tolerated and after at least 6 months of treatment with TTS Exelon® 9.5 mg/day, the attending physician, if necessary to achieve an additional therapeutic effect, can increase the dose to 13.3 mg/day in patients who, despite the use of TTS Exelon® 9.5 mg/day, there is a significant impairment of cognitive functions (for example, deterioration in results on the Mini-Mental Status Assessment) and/or deterioration in functional status (based on the subjective assessment of the physician).

Severe dementia of the Alzheimer's type

Initial dose and selection of the recommended effective dose.

Treatment with the drug should begin with the use of TTC Exelon® 4.6 mg/day once a day. The dose of the drug should be sequentially increased, first to 9.5 mg/day, and then to an effective dose of 13.3 mg/day. Each dose increase is possible only after a minimum of 4 weeks of treatment and if the previous dose is well tolerated. Doses above 13.3 mg/day do not provide a significant benefit, but increase the incidence of side effects.

Interruption of treatment

The clinical effect of therapy with Exelon® TTC should be regularly assessed. If there is no clinical effect from therapy when using optimal doses of TTC Exelon®, it is necessary to discontinue drug therapy.

Treatment with the drug should be temporarily discontinued if adverse events (AEs) from the digestive system occur and/or existing extrapyramidal symptoms (including tremor) worsen until they resolve. If the break in the use of the drug was no more than 3 days, you can resume taking the drug at the same dose. In case of a longer withdrawal period, treatment should be resumed with the initial dose (TTS Exelon® 4.6 mg/day).

Patients treated with rivastigmine in the form of capsules or oral solution can switch to TTC Exelon® treatment as follows:

- in patients receiving oral therapy with rivastigmine at a dose of ≤6 mg/day, treatment should begin with the use of TTS Exelon® 4.6 mg/day;

- in patients receiving oral therapy with rivastigmine at a stable and well-tolerated dose of 9 mg/day, treatment can begin immediately with the use of TTS Exelon® 9.5 mg/day. But if oral therapy was not stable and well tolerated, it is recommended to start switching to the transdermal form with a dose of 4.6 mg/day;

- in patients receiving oral therapy with rivastigmine at a dose of 12 mg/day, treatment can begin immediately with the use of TTS Exelon® 9.5 mg/day.

After 4 weeks of treatment, at a minimum, if well tolerated, the dose of TTC Exelon® 4.6 mg/day should be increased to the recommended effective dose by using TTC Exelon® 9.5 mg/day.

Treatment with TTC Exelon® is recommended to begin the day after the last oral dose of rivastigmine.

Special patient groups

Patients weighing less than 50 kg.

Patients weighing less than 50 kg were more likely to develop AEs and discontinuation of therapy, so when increasing the dose in this group of patients, use extreme caution, carefully titrate the dose and monitor for the development of AEs (eg, excessive nausea or vomiting), and consider the possibility of reducing the dose of the drug by using TTS Exelon® 4.6 mg/day in the event of the development of such AEs. Particular care should be taken when titrating the dose above the recommended effective dose of TTC Exelon® 9.5 mg/day.

Liver dysfunction.

No adjustment is required to the TTC Exelon® dosage regimen. However, due to the increased exposure of rivastigmine observed when rivastigmine was taken orally in patients with mild to moderate hepatic impairment, it is recommended that the dose of rivastigmine be carefully titrated to individual tolerance in these patients.

The use of TTS Exelon® in patients with severe liver dysfunction has not been studied. Particular care should be taken when titrating the dose in patients in this category.

In patients with clinically significant liver dysfunction, a more frequent development of dose-dependent adverse events may be observed, and therefore in patients in this category the possibility of using TTC Exelon® 4.6 mg / day should be considered as the initial and maximum dose.

Renal dysfunction.

No adjustment is required to the TTC Exelon® dosage regimen. However, due to the increased exposure of rivastigmine observed when oral rivastigmine was taken in patients with mild to moderate renal impairment, it is recommended that the dose of rivastigmine be carefully titrated to individual tolerance in these patients. In patients with clinically significant renal impairment, a more frequent development of dose-dependent adverse events may be observed, and therefore in patients in this category the possibility of using TTC Exelon® 4.6 mg / day should be considered as the initial and maximum dose.

Children.

The use of rivastigmine in children has not been studied and is therefore not recommended for use in children.

Instructions for use

Attention!

Only one Exelon® TTS can be used at a time. Each subsequent Exelon® TTS should be glued only after the previous one has been removed. TTC Exelon® must not be cut or divided into parts, or damaged in any way. TTC Exelon® should be pressed firmly with the palm of your hand at the attachment site for at least 30 s.

Place of attachment of TTS Exelon®:

— TTC Exelon® is applied to clean, dry, intact skin with minimal hair;

- do not use creams, lotions, oils, powders and other skin care products in the area where the drug is attached to prevent it from coming off;

— TTC Exelon® should not be applied to red, rash-covered, irritated or damaged skin;

— only one Exelon® TTC per day should be applied to only one of the body areas: left or right shoulder, upper chest left or right (should not be applied to the breast area), upper back left or right, lower back left or right.

Every 24 hours, the previous Exelon® TTS should be removed before applying one new Exelon® TTS.

To avoid skin irritation, each subsequent Exelon® TTS should be glued to a different area of ​​the skin (possibly within the same anatomical area). For example, if the Exelon® TTC was attached to the lumbar area on the right, then next time it is necessary to place the system on the left.

To minimize the risk of skin irritation, TTS can only be applied to the same area of ​​skin at intervals of 2 weeks.

How to attach the Exelon® TTC:

— carefully remove the previous Exelon® TTS;

— remove the drug from the sealed bag immediately before use by cutting or tearing the bag along the dotted line or groove;

— you should carefully remove the protective film protecting the adhesive side of the Exelon® TTS without touching the surface;

— immediately after removing the protective film, stick TTC Exelon® onto the skin of the upper or lower half of the back, shoulder or chest;

— after attaching the TTS to the skin, it is necessary to remove the top protective layer on the other side of the TTS;

— TTC Exelon® should be pressed firmly with the palm of your hand at the attachment site for at least 30 s. Make sure that the system fits snugly against the skin, especially around the edges;

— if necessary, after gluing, it is recommended to write the date of attachment (for example, the day of the week) on the TTS with a thin ballpoint pen.

TTC Exelon® must be worn constantly and replaced with a new one after 24 hours.

TTC Exelon® is a thin, opaque, plastic patch for gluing to the skin.

You should not remove the Exelon® TTC from the sealed bag and do not remove the previous Exelon® TTC if you do not plan to glue a new one.

The drug should be used immediately after removal from the sealed package.

Attaching the TTS to different areas of the skin allows you to select the most comfortable areas of the body, where the system will not come into contact with tight-fitting clothing.

How to remove TTC Exelon®:

— you should carefully bend one of the corners and slowly and carefully remove the TTS;

- If there is glue residue on the skin, lightly moisten the area with warm water and a mild soap solution or baby oil to remove any glue residue. Do not use alcohol or other liquid solvents (including nail polish remover);

- You must wash your hands thoroughly with soap and water after attaching or removing the Exelon® TTC. In case of eye contact or eye redness following attachment or removal of Exelon® TTC, immediately flush eyes with plenty of water and seek medical attention if symptoms persist.

How to dispose of used Exelon® TTS:

— bend the used TTS in half and connect the adhesive parts together;

— place the used Exelon® TTC in the bag. The bag containing used TTS should be thrown away out of the reach of children. After disposing of the drug, you must wash your hands with soap.

Conditions for wearing TTC Exelon® (water procedures, prolonged stay near heat sources):

— TTC Exelon® does not come off during water procedures (shower, bath, swimming pool). During water procedures, you need to make sure that the system fits tightly to the skin, especially at the edges;

— patients using TTS Exelon® should not stay near any external heat sources (excessive solar radiation, saunas, solariums) for a long time.

What to do if TTS Exelon® comes off:

If the Exelon® TTC has become unstuck, it must be replaced with a new TTC by the end of the day. The next day, attach the new Exelon® TTS as usual.

When using more than one Exelon® TTS at the same time:

You should immediately remove all TTS from the skin and inform your doctor about the incident. The patient may require medical attention. In some cases, with an overdose, nausea, vomiting, diarrhea, increased blood pressure, and hallucinations were noted. Bradycardia and/or fainting may also occur. If the patient forgot to apply the next TTS at the usual time, it should be applied immediately. The next TTS can be used the next day at the usual time. You should not apply two TTCs to make up for a missed dose.