Abiksa – instructions for using the medicine, structure, Contraindications

The main active ingredient in Abix is ​​memantine., which acts as a potentially dependent component with an average strength of interaction with chemical. elements and does not act as an NMDA receptor antagonist. Memantine reduces the strength of the effect of glutamate, which in large quantities in the body leads to a failure of neural connections.

Abiksa: indications and dosage

The main indications for the use of Abix are:

Dementia - dementia, a persistent decline in cognitive activity with the loss to one degree or another of previously acquired knowledge and practical skills and the difficulty or impossibility of acquiring new ones.

main cause of dementia - destruction of nerve cells (neurons). When the death of neurons in the brain are formed toxic compound, as well as the process worsens power cells. Less violation of brain activity associated with other independent disease, that complicates the work of the nervous system. On statistics, about 90% deaths occur in the primary with dementia, and 10% – to someone, caused by other diseases (secondary dementia).

Unlike mental retardation (mental retardation), dementia congenital or acquired in infancy, which is an underdevelopment of the psyche, dementia is the breakdown of mental functions, resulting from brain damage:

• often - in youth as a result of addictive behavior
• more often - in old age (senilynaya dementia).

Alzheimer's Disease (from mild to severe) – common neurodegenerative disease, which is currently considered incurable. On statistics, on Alzheimer's accounts for more than 40% of all cases of dementia.

Currently, the exact cause of the development of Alzheimer's disease is unknown. Today, as a possible cause of Alzheimer's disease are considered two theories:

• Amiloidnaja theory of the development of Alzheimer's disease (the cause of Alzheimer's disease is the deposition of beta-amyloid protein in the brain tissue)
• The Tau hypothesis for the development of Alzheimer's disease (the cause of Alzheimer's disease is a violation of the tau protein)

Only a doctor with clinical experience in the treatment of senile dementia can prescribe Abixa. (dementia and Alzheimer's disease).

Important! The course of therapy begins with the presence of an acting guardian or the maintenance of the patient in special institutions around the clock guarding people with neurological problems. Diagnosis of diseases is carried out in accordance with the current recommendations of the Ministry of Health.

Adult. The course of treatment begins with a daily dose 5 mg (1-2 tablets in the morning) during 7 days. To continue, you should prescribe a daily dose 10 mg (by 1-2 tablets 2 once a day) for 14 days and then 15 mg per day (1 tablet in the morning 1-2 pills after lunch) within 21 days.

From the beginning of the 4th week of the course of therapy, you can enter the recommended maintenance daily dose. 20 mg (by 1 tablet 2 once a day). The maximum amount per day is 20 mg. To prevent the occurrence of adverse reactions, the maintenance dose is regulated by the method of gradually increasing the rate by 5 mg per week for the first 3 weeks. Taking pills does not depend on food intake.

Elderly patients. For the elderly (above 65 years) daily rate is 20 mg (2 × 10 mg per day), confirmed by clinical trials.

Impaired renal function. With normal kidney function or with mild kidney dysfunction (creatinine levels in blood plasma within 130 mmol / l) adjustment of the norms of the drug Abiks is not needed.

With moderate renal impairment (creatinine levels in blood plasma 40–60 ml/min/1.73 m2) daily rate is reduced to 10 mg.

There is no information about the use of the drug in patients with severe renal impairment.. Therefore, the dose is adjusted at the discretion of the attending physician..

Abiksa: overdose

The main symptoms of an overdose are:

• anxiety,
• psychosis,
• heteroptics,
• convulsive readiness,
• drowsiness,
• stupor and loss of consciousness.

Treatment of Abix overdose is symptomatic. Standard clinical procedures should be followed to remove the active substance from the body:

• gastric lavage,
• administration of activated charcoal,
• urine acidification reaction methods,
• diurez.

In case of excessive general stimulation of the central nervous system, symptomatic therapeutic measures should be used with caution..

Abiksa: side effects

Conducted clinical studies involving patients with moderate and severe dementia have shown, that the severity of the adverse reaction was not significantly different from the placebo control group. The entire group of side effects refers to mild and moderate severity.. The most common of them are shown in the table..

Also, some side effects of Abiks were measured in percentage equivalent in comparison between control groups., who took this medicine and the group, who received a placebo and are presented in the table below.

Used term by classification WHO ART - WHO terminology of adverse reactions Memantine n=299 Placebo n=288.

Common Side Effects (1-10% or more frequent compared to placebo) for patients, who took memantine and placebo, were introduced:

• hallucinations (2 against 0,7%),
• confusion (1,3 against 0,3%),
• dizziness (1,7 against 1,0%),
• headache (1,7 against 1,4%)
• feeling tired (1 against 0,3%).

Uncommon side effects (0,1-1% or more frequent compared to placebo) We were:

• anxiety,
• increased muscle tone,
• vomiting,
• cystitis(cystitis, caused by microbes, penetrating into the urinary system, causing an inflammatory process)
• increased libido (accelerated recovery of hormones in the body).

There is evidence of epileptic seizures, predominantly in patients, who have previously had a seizure disorder.

In Alzheimer's disease and taking memantine, the following pathological reactions may occur:

• depression,
• suicidal ideas
• suicide.

Abiksa: Contraindications

Abiks should not be taken in case of hypersensitivity to active substances., its constituent.

Manifestations of Alzheimer's disease from moderate to severe often leads to a decrease in concentration when driving vehicles and to a violation of the ability to work with heavy mechanisms and complex equipment..

Besides, the substance memantine has little effect on the patient's thought process, therefore, the patient should be aware of the possible complications while driving, sophisticated equipment and extreme sports.

Abiksa: interactions with other drugs and alcohol

Abiksa should not be taken in combination with NMDA antagonists., such as:

• amantadin,
• ketamine,
• dextromethorphan and others.

The listed substances have an effect on the same receptors, that the active substance of Abix is ​​memantine. Therefore, adverse reactions of the CNS (eg, risk of developing pharmacotoxic psychosis) may be increased or increased with concomitant use.

Data on side effects have also been recorded with the combined use of memantine and phenytoin..

Also, due to the similarity of the mechanism of action of NMDA antagonists, a strong effect from drugs is possible.:

• levodopa,
• dopamine receptor agonists,
• anticholinergics.

During a parallel course of taking Abix barbiturates and antipsychotics, the effect of the latter decreases..

Dose adjustment is necessary due to the combined effect of Abix and drugs such as:

• antispasmodic drugs,
• dantrolene,
• ʙaklofen.

Preparations, that use the same cation transport system in the kidneys, that memantine increases the risk of too high plasma concentrations of substances:

• cimetidine,
• ranitidine,
• prokaynamyd,
• quinidine,
• quinones,
• nicotine.

The reaction of memantine with hydrochlorothiazide was also noted.. This reaction leads to a decrease in the effect of the drug based on hydrochlorothiazide in medicinal products..

Abiksa: use during pregnancy or lactation

Accurate information on the effect of memantine on the fetus during pregnancy has not been found.. Animal clinical studies have shown, that the active substance of Abix in human norms has an effect on the intrauterine development of the fetus and can slow down its growth. This gives grounds, for, to talk about the negative effect of the drug during pregnancy for a woman and without extreme necessity it should not be prescribed.

No studies have been conducted on the penetration of the components of the drug into milk., however, accumulation of the substance in the fatty layer is possible. Therefore, during lactation, taking Abix is ​​also undesirable..

Abiksa: pharmachologic effect

Specialists studying the causes of the development of dementia of the neurodegenerative type, the main factor is the dysfunction of glutamatergic neurotransmission, especially for NMDA(N-methyl-D-aspartate)-receptors.

The active substance of the drug Abiks is dependent on the chemical potential and, by interaction with other substances, cannot act as an antagonist of NMDA receptors. Memantine effectively reduces the effects of glutamate, which, at high levels in the blood, leads to disruption of neuronal connections.

The positive effect of taking Abix in Alzheimer's disease (mild-severe degree) within six months:

• normalization and improvement of general indicators of the body and its functions,
• stabilization of cognitive operations.

The active substance of Abix - memantine - is absolutely bioavailable on 100%. The time to maximum concentration (Tmax) in plasma from 3 to 8 hours. Absorption of the drug is not associated with food intake..

Abiksa: pharmacokinetics

Abix's drug has a linear property within the normal range of 10–40 mg. Standard dose 20 mg maintains a stable plasma level of memantine in the range of 70–150 ng/mL (0,5–1 μmol) depending on the individual patient.

When prescribing memantine at a daily dose of 5–30 mg, the ratio of the drug content in cerebrospinal fluid and blood plasma is equal to 0,52. About 45% memantine binds to plasma proteins. In the human body about 80% memantine circulates unchanged, the main metabolite N-3,5-dimethyl-gludanthan does not have NMDA antagonistic activity.

Involvement of cytochrome P450 in in vitro metabolism was not revealed. Memantine is eliminated predominantly by the kidneys according to a mono-exponential curve, T1 / 2 - 60–100 h, total ground clearance 170 mL/min per 1.73 m2. The renal pharmacokinetics of memantine also includes tubular reabsorption.. The rate of renal elimination of memantine under conditions of alkaline urine may decrease by 7–9 times.. Alkalinization of urine can occur as a result of a change in diet, eg, when replacing a meat-rich diet with a vegetarian one, or due to frequent use of antacids. In elderly volunteers with normal or reduced kidney function (creatinine clearance 50–100 ml/min/1.73 m2) observed a stable correlation between creatinine clearance and total renal clearance of memantine. The effect of impaired liver function on the pharmacokinetics of memantine has not been studied.. Since metabolites do not have antagonistic activity to NMDA structures, clinically significant changes in pharmacokinetics in mild to moderate hepatic dysfunction are not noted. Pharmacodynamic and pharmacokinetic relationship: when using memantine at a dose 20 mg/day, the level of concentration in the cerebrospinal fluid corresponds to the value of Ki (pressure constant) for memantine, what is 0,5 µmol in the human frontal cortex.

Abiksa: composition and properties

Structure
memantine hydrochloride 10 mg.

Product form

By 14 tablets in blister packs, by 2 blister pack in carton. Released by prescription.

Storage conditions

Does not require special storage conditions. Shelf life 4 year. Keep out of the reach of children.

Abiksa: general information

• Sales form: over-the-counter
• Current in-about: Memantine
• Manufacturer: Lundbeck X. A/C, Denmark
• Farm. Group: Preparations, used in dementia