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  • Exelon
    / Novartis


    Active Ingredient
    Rivastigmine 1.5, 3, 4.5 , 6 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Hard Capsules

    28 X 1.5 mg

    partial basket chart 85368 5117

    Hard Capsules

    28 X 3 mg

    partial basket chart 85369 5118

    Hard Capsules

    28 X 4.5 mg

    partial basket chart 30604 5201

    Hard Capsules

    28 X 6 mg

    partial basket chart 30605 5202

    Related information


    Dosage

    Administration: Exelon hard capsules should be administered twice a day, with morning and evening meals.
    Initial dose: 1.5 mg twice a day. Patients known to be particularly sensitive to the effects of cholinergic drugs should be started at a dose of 1 mg twice a day.
    Dose titration: The starting dose is 1.5 mg twice a day. If this dose is well tolerated after a minimum of two weeks of treatment, the dose may be increased to 3 mg twice a day. Subsequent increases to 4.5 mg and then 6 mg twice a day should also be based on good tolerability of the current dose and may be considered after a minimum of two weeks’ treatment at that dose level.  If adverse effects (e.g. nausea, vomiting, abdominal pain or loss of appetite) or weight decrease are observed during treatment, these may respond to omitting one or more doses. If adverse effects persist, the daily dose should be reduced to the previous well-tolerated dose.
    Maintenance dose: 1.5 mg to 6 mg twice a day; to achieve maximum therapeutic benefit patients should be maintained on their highest well-tolerated dose.
    Recommended maximum daily dose: 6 mg twice a day.
    Re-initiation of therapy: The incidence and severity of adverse events are generally increased with higher doses. If treatment is interrupted for longer than several days, treatment should be re-initiated with 1.5 mg twice daily and titrated as described above.
    Special population
    Paediatric patients:
    Children and adolescents (age below 18 years):The use of Exelon in children has not been studied and is therefore not recommended.
    Renal impairment or hepatic impairment: No dose adjustment is necessary in patients with renal or hepatic impairment. However, due to increased exposure in moderate renal and mild to moderate hepatic impairment, dosing recommendations to titrate according to individual tolerability should be closely followed as patients with clinically significant renal or hepatic impairment might experience more adverse events. Patients with severe liver impairment have not been studied, however, Exelon capsules may be used in this patient population provided close monitoring is exercised.


    Indications

    Treatment of patients with mild to moderately severe dementia of the Alzheimer type, also termed probable Alzheimer’s Disease or Alzheimer’s Disease. Symptomatic treatment of mild to moderately severe Alzheimer’s dementia. Symptomatic treatment of mild to moderately severe dementia associated with Parkinson’s disease.


    Contra-Indications

    The use of Exelon is contraindicated in patients with: Known hypersensitivity to rivastigmine, to other carbamate derivatives or to the excipients of the formulation. Previous history of application site reactions suggestive of allergic contact dermatitis with rivastigmine transdermal patch.


    Special Precautions

    Treatment should always be started at a dose of 1.5 mg twice daily and titrated to the patient’s maintenance dose. If treatment is interrupted for longer than several days, treatment should be re-initiated with the lowest daily dose to reduce the possibility of adverse reactions (e.g. severe vomiting). Gastrointestinal disorders such as nausea, vomiting and diarrhoea may occur when initiating treatment and/or increasing the dose. They may respond to a dose reduction. In other cases, use of Exelon has been discontinued. Patients who show signs or symptoms of dehydration resulting from prolonged vomiting or diarrhoea can be managed with iv fluids and dose reduction or discontinuation if recognized and treated promptly. Dehydration can be associated with serious outcomes. Patients with Alzheimer’s disease may lose weight whilst taking cholinesterase inhibitors, including rivastigmine. The patient’s weight should be monitored during therapy with Exelon. Patients with body weight below 50 kg may experience more adverse events and may be more likely to discontinue due to adverse events. As with other cholinomimetics, care must be taken when using Exelon in patients with sick sinus syndrome or conduction defects (sino-atrial block, atrio-ventricular block). Cholinergic stimulation may cause increased gastric acid secretion and may exacerbate urinary obstruction and seizures. Caution is recommended in treating patients predisposed to such conditions. Like other cholinomimetics, Exelon should be used with caution in patients with a history of asthma or obstructive pulmonary disease. Like other cholinomimetics, rivastigmine may exacerbate extrapyramidal symptoms. In patients with dementia associated with Parkinson’s disease who were treated with Exelon capsules, worsening of parkinsonian symptoms, particularly tremor, has been observed.
    Skin reactions: In patients who develop application site reactions suggestive of allergic contact dermatitis to Exelon Patch and who still require rivastigmine, treatment should be switched to oral rivastigmine only after negative allergy testing and under close medical supervision. It is possible that some patients sensitized to rivastigmine by exposure to rivastigmine patch may not be able to take rivastigmine in any form. Allergic contact dermatitis should be suspected if application site reactions spread beyond the patch size, if there is evidence of a more intense local reaction (e.g. increasing erythema, edema, papules, vesicles) and if symptoms do not significantly improve within 48 hours after patch removal. In these cases, treatment should be discontinued. There have been isolated post-marketing reports of patients experiencing disseminated skin hypersensitivity reactions when administered rivastigmine irrespective of the route of administration (oral, transdermal). In these cases, treatment should be discontinued. Patients and caregivers should be instructed accordingly.
    Special population: Patients with clinically significant renal or hepatic impairment may experience more adverse events. Dosing recommendations to titrate according to individual tolerability should be closely followed . Patients with severe liver impairment have not been studied, however, Exelon capsules may be used in this patient population provided close monitoring is exercised.
    Driving and using machines: Alzheimer’s and Parkinson’sdisease dementia may cause gradual impairment of driving performance or compromise the ability to use machinery. Rivastigmine may induce dizziness and somnolence, mainly when initiating treatment or increasing the dose.Therefore, in patients with dementia treated with Exelon, the ability to continue driving or operating complex machines should be routinely evaluated by the treating physician.


    Side Effects

    The most commonly reported adverse drug reactions are gastrointestinal including nausea (38%) and vomiting (23%), especially during titration. Female patients in clinical studies were found to be more susceptible to gastrointestinal adverse drug reactions and weight loss. Additional reported adverse drug reactions were:
    Very common: Dizziness, diarrhoea, loss of appetite.
    Common: Agitation, confusion, anxiety, Headache, somnolence, tremor, Abdominal pain and dyspepsia, Hyperhydrosis, Fatigue and asthenia, malaise, Weight loss.
    For full details see prescribing information.


    Drug interactions

    Rivastigmine is metabolised mainly through hydrolysis by esterases. Minimal metabolism occurs via the major cytochrome P450 isoenzymes. Thus, no pharmacokinetic interactions are anticipated with other drugs metabolised by these enzymes.
    No pharmacokinetic interaction was observed between oral rivastigmine and digoxin, warfarin, diazepam or fluoxetine in studies in healthy volunteers. The increase in prothrombin time induced by warfarin is not affected by administration of rivastigmine. No untoward effects on cardiac conduction were observed following concomitant administration of digoxin and rivastigmine. Concomitant administration of rivastigmine with commonly prescribed medications, such as antacids, antiemetics, antidiabetics, centrally acting antihypertensives, beta-blockers, calcium channel blockers, inotropic drugs, antianginals, non-steroidal anti-inflammatory drugs, oestrogens, analgesics, benzodiazepines and antihistamines, was not associated with an alteration in the kinetics of rivastigmine, or an increased risk of clinically relevant untoward effects. In view of its pharmacodynamic effects, rivastigmine should not be given concomitantly with other cholinomimetic drugs and might interfere with the activity of anticholinergic medications. As a cholinesterase inhibitor, rivastigmine may exaggerate the effects of succinylcholine-type muscle relaxants during anaesthesia.
    For full details see prescribing information.


    Pregnancy and Lactation

    Pregnancy: In animal studies, rivastigmine was not teratogenic. However, the safety of Exelon in human pregnancy has not been established, and it should only be given to pregnant women if the potential benefit outweighs the potential risk for the foetus.
    Lactation: In animals, rivastigmine and/or metabolites were transferred to the milk. It is not known if Exelon is excreted into human milk, and patients on Exelon should therefore not breast-feed.
    For full details see prescribing information.


    Overdose

    Symptoms: Most cases of accidental overdose have not been associated with any clinical signs or symptoms and almost all of the patients concerned continued Exelon treatment. Where symptoms have occurred, they have included nausea, vomiting, diarrhoea, hypertension and hallucinations. Due to the known vagotonic effect of cholinesterase inhibitors on heart rate, bradycardia and/or syncope may also occur. Ingestion of 46 mg occurred in one case; following conservative management the patient fully recovered within 24 hours.
    Treatment: As rivastigmine has a plasma half-life of about 1 hour and a duration of acetylcholinesterase inhibition of about 9 hours, it is recommended that in cases of asymptomatic overdose no further dose of Exelon should be administered for the next 24 hours. In overdose accompanied by severe nausea and vomiting, the use of antiemetics should be considered. Symptomatic treatment for other adverse events should be given as necessary. In massive overdose, atropine can be used. An initial dose of 0.03 mg/kg i.v. atropine sulfate is recommended, with subsequent doses based on clinical response. Use of scopolamine as an antidote is not recommended.
    For full details see prescribing information.


    Important notes

    Storage: Do not store above 30°C.


    Manufacturer
    Novartis Farmaceutica S.A., Spain
    Licence holder
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