Rivastigmine (Rivastigminum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

M-, N-holinomimetiki, incl. anticholinesterase agents

Included in the formulation
  • Alzenorm
    solution inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Alzenorm
    capsules inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Excelon®
    solution inwards 
    Novartis Pharma AG     Switzerland
  • Excelon®
    patch through. 
    Novartis Pharma AG     Switzerland
  • Excelon®
    capsules inwards 
    Novartis Pharma AG     Switzerland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.06.D.A   Cholinesterase inhibitors

    N.06.D.A.03   Rivastigmine

    Pharmacodynamics:Selective pseudo-reversible inhibitor of brain acetylcholinesterase of carbamate type (the duration of the blockade of acetylcholinesterase is about 9 hours). Prevents the destruction of acetylcholine, selectively increases the content of acetylcholine in the cerebral cortex and hippocampus, facilitates cholinergic transmission, improves cognitive processes in Alzheimer's disease.
    Pharmacokinetics:

    Fast and complete absorption. F 40%. VD 1,8-2,7 l / kg. The connection with plasma proteins is ~ 40%. Biotransformation in the liver. The half-life period is 1.5 hours.max 1 hour. Elimination by the kidneys, with feces.

    Indications:Weak and moderate dementia of the Alzheimer's type (in the case of suspected or established Alzheimer's disease).
    ICD-10

    V.F00-F09.F00.9 *   Dementia in Alzheimer's disease, unspecified (G30.9 +)

    Contraindications:

    Hypersensitivity to rivastigmine, other carbamate derivatives.

    Carefully:Use with caution in patients with syndrome of weakness of the sinus node or severe arrhythmias, increased risk of erosive and ulcerative gastrointestinal lesions, respiratory diseases (including in the history), with urinary tract obstruction, convulsions. Experience with rivastigmine in patients with bronchial asthma in the exacerbation phase is absent.
    Pregnancy and lactation:

    Studies in humans have not been conducted, teratogenic effects in animals have not been identified. There is no information on the penetration into breast milk. Do not apply.

    Recommendations FDA category B.

    Dosing and Administration:

    The initial dose is 1-1.5 mg 2 times / day. With good tolerability, a single dose can be increased to 3 mg, then to 4.5 and to 6 mg; frequency of admission - 2 times / day; the interval between each dose increase should be at least 2 weeks. In order to achieve the best therapeutic effect, the dose of rivastigmine should be kept at the maximum tolerable level.

    Side effects:

    From the side of the central nervous system: increased fatigue, asthenia, dizziness, headache, agitation, insomnia, impaired orientation, depression, drowsiness.

    From the digestive system: nausea, vomiting, diarrhea, abdominal pain, loss of appetite. Nausea, vomiting, loss of appetite and weight loss were more common in women.

    Other: accidental trauma, upper respiratory tract infection, urinary tract infection, increased sweating, a feeling of malaise, weight loss and tremors.

    Overdose:Symptoms: maximum manifestations of cholinergic action.

    Treatment: antidote - atropine.

    Interaction:

    Anticholinesterase drugs - strengthening or weakening of muscle relaxation.

    NSAIDs - increased gastric secretion, functional disorders of the gastrointestinal tract, bleeding.

    Special instructions:

    There is some evidence of the effectiveness of rivastigmine in vascular cognitive impairment (1 RCT, 136 patients), dementia with Levy bodies (1 CI, 120 patients), and Gottington disease (6 mg / day).

    Rivastigmine at a dose of 6-12 mg / day improves cognitive function and increases activity in patients with moderate Alzheimer's disease (8 RCTs, 3,660 patients), and also improves cognitive function in patients with Parkinson's disease (1 CI, 541 patients).

    Galantamine in a dose of 24 mg 2 times a day, rivastigmine in a dose of 6-12 mg twice a day and donepezil at a dose of 10 mg / day are equally effective in the treatment of moderate Alzheimer's disease. The use of donepezil is accompanied by fewer side effects (13 CI, 7298 patients).

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