Exelon
Exelon
Exelon (Rivastigmine)Pharmacological action
It has been shown, that, slowing down Acetylcholinum destruction, Exelon selectively enlarges its maintenance in a cortex of a brain and a hippocampus, and, thus, promotes improvement of cholinergic nervous transfer. Besides, exist that proof, that acetylcholinesterase inhibition can slow down formation of fragments of the albuminous precursor of the beta amyloid and, thus, to slow down formation of the amyloid plaques which are one of the main pathological signs of an Alzheimer's disease.
Indications
Weakly or moderately expressed dementia (a probable Alzheimer's disease, an Alzheimer's disease).
Dosage regimen
Exelon it is necessary to accept 2 times/sut, during a breakfast and a supper.
The initial dose makes on 1.5 mg 2 times/days
Dose selection. The initial recommended dose - on 1.5 mg 2 times/days If after proprocession a minimum of 2 weeks of treatment becomes perceptible good shipping of this dose, it can be enlarged to 3 mg 2 times/days In case of good shipping of a dose accepted by the patient its probably further augmentation - to 4.5 mg 2 times/sut and even to 6 mg 2 times/sut - with an interval of time not less than 2 weeks after each next step of treatment.
The undesirable phenomena, namely nausea, abdominal pains, depression of appetite or depression of mass the bodies observed during treatment, can decrease after the admission of reception of 1 or several doses of a preparation. If the undesirable phenomena remain, the preparation daily dose should be lowered to the previous dose well transferred by the patient.
The maintenance dose makes from 1.5 to 6 mg 2 times/days For the purpose of achievement of the best therapeutic effect a preparation dose it is necessary to keep at maximum well transferable level.
The maximum daily dose - on 6 mg 2 times/days
Renewal of reception of a preparation after a break. If having rummaged in preparation reception has made some days and more, to renew treatment follows from the least dose. Gradual augmentation of a dose spend in steps as it is described above.
With disturbances of function of kidneys or a liver of changes in a regimen preparation dosage it is not required from patients. The patient with serious disturbances of function of a liver a preparation to prescribe does not follow.
Side effect
It was most often informed on the undesirable phenomena from the alimentary system: a nausea (38 %), vomiting (23 %), basically in dose selection. According to clinical researches the undesirable phenomena from the alimentary system and reduction of mass of a body became perceptible at women is more often.
The undesirable phenomena listed more low have been noted in clinical researches and clinical practice from the moment of Exelon exit on the market.
Contraindications
- A hypersensibility to Rivastigmine, to other derivatives of a carbamate or other components of a preparation.
Exelon is contraindicative to patients with serious disturbances of function of a liver as its application in the given population is not studied.
Pregnancy and lactemia
Safety of Exelon application at pregnancy at the person is not established till now, therefore the preparation can be prescribed at pregnancy only when the expected success of treatment surpasses potential risk for a foetus.
It is not known, whether it is allocated Rivastigminewith thoracal milk. Therefore during preparation application it is necessary to refuse thoracal feeding.
Special indicatings
Exelon , as well as other cholinomimetic agents, it is necessary to apply with care at patients with conductivity disturbances (sinuatrial blockade, AV-blockade).
Cholinergic stimulation can raise hydrochloric acid secretion in a stomach, lead to intensifying of obstruction of urinary ways and an exacerbation of a convulsive syndrome, therefore it is necessary to be careful at Exelon appointment to the patients predisposed to these conditions.
Exelon as well as other cholinomimetics, it should be applied with care at patients with a bronchial asthma or obstructive diseases of respiratory tracts in the anamnesis.
Exelon treatment it is necessary to begin with a dose of 1.5 mg 2 times/sut with the subsequent gradual rising of a dose to the supporting. If treatment interrupts more than for some days, therapy should be renewed from an initial dose (1.5 mg 2 times/sut) for reduction of risk of occurrence of the undesirable phenomena (for example, serious vomiting).
In dose selection the same as and at application of other cholinomimetics, the undesirable phenomena became perceptible during the short period after dose rising. Degree of expression of the undesirable phenomena can decrease in reply to a preparation dose decline. Otherwise Exelon is necessary to cancel.
At application of a preparation for the patients especially sensitive to influence of cholinergic preparations, treatment should be begun with preparation application in a dose of 1 mg 2 times/days
Influence on ability to driving of motor transport and to management of mechanisms
At the patients receiving Exelon , it has not been taped any disturbances of impellent function. Nevertheless ability of the patient with an Alzheimer's disease to drive the car and to control mechanisms it should be estimated by the attending physician regularly.
Overdosage
The casual overdosage of a preparation in most cases was not accompanied by any clinical implications; almost all these patients continued Exelon treatment.
Symptoms: a nausea, vomiting, a diarrhoeia, the expressed rising of a BP, hallucination. Considering vagotonic effect of inhibitors of a cholinesterase on the CARDIAC CONTRACTIONS RATE, it is impossible to exclude occurrence of a bradycardia and-or syncopal conditions. In one case 46 mg of a preparation were accepted; after conservative treatment through 24 h full recover was observed.
At an appreciable overdosage Atropini sulfas which initial dose makes 0.03 mg/kg i.v. can be applied; the subsequent dosage depends on clinical effect. Application of Scopolaminum as an antidote is not recommended.
Medicinal interaction
Rivastigmine is metabolized mainly by hydrolysis with the assistance of esterases. The metabolism of a preparation with the assistance of the basic isoenzymes of cytochrome P450 occurs in the minimum degree. Hence, to expect pharmacokinetic interactions with other medical products metabolized with participation of given enzymes, it is not necessary.
Conditions and periods of storage
Capsules should be stored at temperature not above 30 C. The solution for intake should be stored at temperature not above 30 C in vertical position; to protect from freezing. The preparation should be stored in a place inaccessible to children. A period of validity - 5 years.
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