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Alzepil is a specific and reversible acetylcholinesterase inhibitor that is the predominant type of cholinesterase in the brain. The drug inhibits this enzyme more than 1000 times stronger than butyrylcholinesterase, which is contained mainly outside the central nervous system. After a single dose of the drug in doses of 5 mg or 10 mg, the degree of inhibition of acetylcholinesterase activity, measured in erythrocyte membranes, was 63.6% and 77.3%, respectively. Inhibition of acetylcholinesterase in erythrocytes under the action of donepezil correlates with changes in the ADAS-cog scale (cognitive function assessment scale in Alzheimer's disease). The ability of Alzepil to alter the course of concomitant neurological diseases has not been studied. Thus, the drug cannot be considered to affect the progression of such diseases.
Suction. Cmax Donepezil in plasma after oral administration is reached in about 3-4 hours. Concentration in plasma and AUC increase in proportion to the dose. T1/2 is approximately 70 hours and the systematic use of single doses leads to the achievement of an equilibrium state, which is achieved within 2-3 weeks after the start of therapy. In equilibrium, the concentration of donepezil in plasma and the corresponding pharmacodynamic activity vary slightly during the day. Eating does not affect the absorption of donepezil.
Distribution. Plasma protein binding - 95%. The binding of plasma proteins of the active metabolite, 6-O-desmethyldoneepesil, is unknown. Distribution has not been studied. Donepezil and / or its metabolites may persist in the body for more than 10 days.
Metabolism and excretion. Donepezil is metabolized in the liver by the cytochrome P450 system and is excreted mainly by the kidneys: approximately 57% of the administered dose is found in the urine (17% in unchanged form) and 14.5% in the faecal masses.
After a single dose of 5 mg, the concentration of unchanged donepezil in plasma is 30% of the dose taken, 6-O-desmethyldonepestyl - 11% (the only metabolite with similar activity with donepezil hydrochloride), donepezil-cis-N-oxide - 9%, 5-O-desmethyldonepesyl - 7% and the glucuronic conjugate 5-O-desmethyldoneepesyl - 3%.
Gender, race and smoking do not have a significant effect on plasma plasma level of donepezil.
Increased C may be observed in patients with mild or moderate hepatic impairment.ss donepezil in blood plasma.
Symptomatic treatment of mild or moderate Alzheimer's disease
1 tablet contains:
active substance: donepezil hydrochloride monohydrate (corresponds to donepezil hydrochloride - 5 mg)
Excipients: MCC; low substitution hydroxypropylcellulose (L-HPC B1); magnesium stearate; Opadry Y-1-7000 white (hypromellose; titanium dioxide; macrogol 400)
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Dosage and Administration
For oral inhalation.
Alvesco must be taken for a long period of time daily. The drug is dosed individually. The initial dose should be adjusted depending on the severity of the condition. When the desired clinical effect is achieved, the dose should be reduced to the minimum necessary to control the manifestations of the disease.
Adults, elderly patients and adolescents over 12 years old
Mild to moderate asthma: The recommended daily dose ranges from 160 to 640 mcg; The dose of 640 mcg should be divided into 2 doses per day.
Severe asthma: The dose may be increased to a maximum of 2 × 640 mcg daily.
Improvement of the manifestations of the disease occurs within 24 hours after taking Alvesco. It is assumed that the maximum effect of the treatment - as with other inhaled GCS - is achieved after 2-3 months of use of the drug.
Patients should not stop treatment, even in the absence of asthma symptoms.
Children over 6 years old
The recommended daily dose is 80–160 mcg once or 80 mcg twice a day.
Alvesco can be used with or without spacer. If spacer use is necessary, a spacer is recommended.AeroChamberPlus.
There is no need to adjust the dose for elderly patients or patients with hepatic or renal insufficiency.
Adults and adolescents who constantly take oral GCS
In patients with severe asthma who depend on oral therapy of GCS (for example, prednisone), the dose of Alvesco is 640 mcg twice a day. To transfer patients from oral GCS to Alvesco - patients must be in remission. The dose of Alvesco (640 mcg twice a day) should be applied for 10 days in combination with oral GCS. The dose of oral GCS should then be gradually reduced every week to the lowest possible level, with a decrease in the daily dose of no more than 2.5 mg each time.
In most cases, side effects were mild and did not require discontinuation of the drug Alvesco.
- On the part of the digestive system: sometimes (> 1/1000, <1/100) - nausea, vomiting, unpleasant taste; rarely (> 1/10 000, <1/1000) - abdominal pain, dyspepsia.
- On the part of the respiratory system: sometimes - dyspnea, cough after inhalation, paradoxical bronchospasm.
- From the side of the central nervous system: sometimes - a headache.
- From the side of the cardiovascular system: rarely - heartbeat, arterial hypertension.
- Dermatological reactions: sometimes - eczema and skin rash.
- Allergic reactions: rarely - angioedema, hypersensitivity reactions.
- Local reactions: sometimes - reactions at the site of application, dryness at the site of application.
Other: sometimes - fungal infections of the oral cavity.
Inhaled GCS can cause systemic effects, especially with long-term use in high doses.
Carefully: patients with pulmonary tuberculosis in active or chronic form; patients with bacterial, viral, or fungal infections of the respiratory tract.
According to in vitro data, CYP3A4 is the main enzyme involved in the metabolism of the active metabolite of ciclesonide - M1 (desCiclesonide) in humans.
In studies of drug interactions between ciclesonide and ketoconazole, as a strong inhibitor of CYP3A4, the effect on the active metabolite of desCiclesonide increased by about 3.5 times, whereas no effect on ciclesonide was noted. On this basis, the simultaneous use of potential inhibitors of CYP3A4 and ciclesonide should be avoided.
A study of the interaction of ciclesonide and the substrate CYP3A4 erythromycin showed no interaction between them.
Pregnancy and Lactation
Controlled studies in pregnant women have not been conducted. However, after inhalation of the drug, the concentration of ciclesonide in the blood serum is very low, hence the effect on the embryo and the potential toxicity affecting reproductive function are insignificant. The isolation of ciclesonide or its metabolites through breast milk has not been studied.
Like other inhaled corticosteroids, ciclesonide can be used during pregnancy and lactation as prescribed by a physician, if the expected therapeutic effect exceeds the risk of possible side effects. Newborns from mothers treated with GCS should be monitored by a physician to rule out adrenal hypofunction.
Alvesco is not indicated for the treatment of asthmatic status or other acute episodes of asthma requiring intensive therapeutic measures.
The effect of inhaled corticosteroids with long-term use in children is not fully understood. The physician must constantly monitor the growth of children receiving SCS for a long period. If growth slows down, therapy should be revised to reduce the dose of inhaled corticosteroids. If possible, then to the lowest dose, which is used to maintain constant monitoring of asthma manifestations. Alvesco's dose may be reduced in patients requiring oral GCS.
For patients transferred from oral GCS to Alvesco's inhalation treatment, there may be a decrease in the function of the adrenal cortex for a considerable period of time after the transfer. The possibility of the development of undesirable effects from the use of oral corticosteroids may persist for some time after their cancellation. In such cases it is recommended to monitor the reserve function of the adrenal cortex. The possibility of a residual deterioration of the adrenocortical response in a critical situation (therapeutic or surgical) and in other individual cases that may be caused by a stress reaction, should therefore be taken into account, and therefore the appropriate GCS treatment should be initiated.
In case of insufficiency of adrenocortical response or serious exacerbations, the dose of Alvesco should be increased; if necessary, oral GCS should be used. In case of infection, antibiotics should be used. Paradoxical bronchospasm with increased wheezing and other symptoms of bronchoconstriction that appeared immediately after inhalation should be treated with a fast-acting bronchodilator, which usually leads to quick relief. The patient should be examined, and Alvesco's therapy should be continued only if, after a balanced examination, the expected effect is higher than the possible risk. The relationship between the severity of asthma and the general predisposition to acute bronchial reactions should be taken into account.
Transfer of patients taking oral GCS to Alvesco.
The transfer of patients receiving treatment with oral corticosteroids to Alvesco and their subsequent management needs attention, since recovery of reduced adrenal function caused by prolonged systematic GCS therapy may take some time.
Patients taking systemic corticosteroids for a long period of time or at a high dose may experience suppression of adrenal function. The adrenal function in these patients should be monitored regularly, and the dose of systemic corticosteroids should be reduced gradually. After approximately one week, gradual elimination of systemic corticosteroids with a reduction in their daily dose of 1 mg of prednisolone or its equivalent can be started. For a maintenance dose of prednisone over 10 mg daily, it may be prudent to take larger dose reductions during weekly intervals.
Some patients may feel unwell during drug withdrawal, despite maintaining or even improving respiratory function. They must be examined for adrenocortical insufficiency.
When transferring patients from taking systemic corticosteroids to inhalation therapy, allergic reactions may occur (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs.These allergies should be treated symptomatically with antihistamines and / or topical agents, including topical GCS.
Influence on the ability to drive a car or perform work that requires increased speed of physical and mental reactions. There is no data on the effect of the drug on the ability to drive vehicles and mechanisms.
Symptoms: Inhalation use of a single dose of 2880 mcg of ciclesonide in healthy volunteers was well tolerated. The possibility of acute toxic effects following an overdose of inhaled ciclesonide is low. May increase the dryness of the mucous membrane of the mouth and pharynx, sensations of irritation or sore throat, dysphonia.
Treatment: after acute overdose, the need for specific treatment is absent.
Symptoms: After prolonged administration of 1280 mcg of ciclesonide, no clinical signs of adrenal suppression were observed. However, if the excess of the recommended dose continues for an extremely long period of time, some degree of suppression of the adrenal glands cannot be excluded.
Treatment: It is recommended to control the function of the adrenal glands.
- Brand name: Alvesco
- Active ingredient: Ciclesonide
- Dosage form: Aerosol for inhalation dosed.
- Manufacturer: Takeda GmbH
- Country of Origin: Japan
- Pharmacotherapy for people with Alzheimer's disease: a Markov-cycle evaluation of five years' therapy using donepezil
- Donepezil for dementia with Lewy bodies: a case study
- Sustained cognitive improvement following treatment of Alzheimer's disease with donepezil
- Donepezil for the treatment of psychosis in dementia with Lewy bodies
- Donepezil for behavioural disorders associated with Lewy bodies: a case series
- Did knowledge, opinions, background, and health authority advice influence early prescribing of the novel Alzheimer's disease drug donepezil in general practice?—National postal survey
- Donepezil in Alzheimer's disease: eighteen month results from Southampton Memory Clinic
- Better cognitive and psychopathologic response to donepezil in patients prospectively diagnosed as dementia with Lewy bodies: a preliminary study
- Use of donepezil for the treatment of mild – moderate Alzheimer's disease: an audit of the assessment and treatment of patients in routine clinical practice
- Improvement in sundowning in dementia with Lewy bodies after treatment with donepezil
- Carers' assessment of patients on donepezil—how reliable?
- Donepezil hydrochloride: A treatment drug for Alzheimer’s disease
- Limited donepezil inhibition of acetylcholinesterase measured with positron emission tomography in living Alzheimer cerebral cortex
- Donepezil for Huntington's disease
- Donepezil for the treatment of language deficits in adults with Down syndrome: A preliminary 24-week open trial
- Donepezil effects on language in children with Down syndrome: Results of the first 22-week pilot clinical trial
- Preliminary study of the safety and efficacy of donepezil hydrochloride in children with Down syndrome: A clinical report series
- The efficacy, safety, and tolerability of donepezil for the treatment of young adults with Down syndrome
- Donepezil for treatment of cognitive dysfunction in children with Down syndrome aged 10–17
- Variability of AChE, BChE, and ChAT genes in the late-onset form of Alzheimer's disease and relationships with response to treatment with Donepezil and Rivastigmine
- A rapid and specific approach for direct measurement of donepezil concentration in human plasma by LC-MS/MS employing solid-phase extraction
- A rapid and specific approach for direct measurement of donepezil concentration in human plasma by LC-MS/MS employing solid-phase extraction
- A rapid and sensitive LC-MS/MS method for quantification of donepezil and its active metabolite, 6-o-desmethyl donepezil in human plasma and its pharmacokinetic application
- Interaction study of aspirin or clopidogrel on pharmacokinetics of donepezil hydrochloride in rats by HPLC-fluorescence detection