Neuroleptic Ketilept: indications, instructions for use, reviews

Methods of using this drug and dosage

Reviews about the drug in question, Ketilept, indicate that it is prescribed only by a doctor. All information provided below is for informational purposes only.

Basically, Ketilept is prescribed to be taken 2 times a day, regardless of food intake. For adults, this medication should be taken according to the following table:

• first day - 50 mg;
• second day - 100 mg;
• third day - 200 mg;
• fourth day - 300 mg.

On the fifth and subsequent days, the daily norm is 300 mg.

The psychiatrist's reviews of the drug "Ketilept" confirm that the clinical response and individual tolerance of each patient are taken into account. Therefore, the dose can be adjusted both up and down, while the daily rate should not exceed 800 mg per day.

In cases where the patient is in stable remission, the attending physician prescribes the lowest dosage. In such cases, patients are periodically examined to determine the need for maintenance therapy with this medication.

If medical therapy was previously completely canceled, and there is a need to urgently resume it, then the daily dose is selected based on the break time.

For example, if only one week has passed since the date of discontinuation, Ketilept continues to be used in the same dosage as before discontinuation of the drug.

If more than one week and one day have passed since the date of cancellation, then the medicine is started according to the initial selection of therapy.

If the patient has a weakened condition or is predisposed to hypertension, then this drug is prescribed at a minimum dose, and the general condition of such a patient must be monitored. In the case when a person has renal or liver failure, this medication is started at 25 mg per day, increasing the dosage daily until the required dose is reached.

General information about the drug

Ketilept is an atypical antipsychotic drug used for various mental disorders of inorganic nature.
Due to its affinity for various brain receptors, it is indispensable in psychiatric practice. The drug belongs to the group of antipsychotics, its international nonproprietary name is quetiapine. Ketilept is used in the field of psychiatry in patients with severe mental pathologies that require correction.

Release forms and prices for the drug, average in Russia

Release form: film-coated tablets (25, 100 and 200 mg). The average price for a package of 60 tablets of 100 mg is 1,500 rubles, for 200 mg - 2,800 rubles. Prices for Ketilept in different pharmacies are shown in the table:

What side effects may occur after taking it?

Reviews of the drug Ketilept indicate that the most common side effects are the following:

• drowsiness;
• dizziness;
• dry mouth;
• development of asthenia;
• constipation;
• tachycardia;
• development of hypotension.

It is worth noting that the above symptoms appear quite rarely. However, it is strictly forbidden to take this medication on your own. It is important to understand that patients use this medication only under the supervision of the attending physician.

What are the contraindications to the use of this product?

Reviews of the drug "Ketilept" confirm that the use of this drug is not recommended in the following situations:

• during pregnancy;
• during breastfeeding;
• patients under 14 years of age;
• with hypersensitivity to one of the components that make up the medication.

Also, this drug is prescribed with caution to patients who have liver failure and may experience seizures. This drug is not recommended for the elderly, but if there is an urgent need to take it, then use is carried out under the strict supervision of a doctor.

pharmachologic effect

The active component of the drug causes an antipsychotic effect without increasing the accumulation of prolactin in the blood plasma.
The drug is quite effective in the treatment of schizophrenia. The therapeutic effect of the drug lasts for twelve hours after taking it. The active substance of the drug (quetiapine) has an antagonistic effect on the neurotransmitter receptors of the central nervous system.

Ketilept affects histamine receptors, resulting in drowsiness. Due to the effect on alpha-1 adrenergic receptors, arterial orthostatic hypotension occurs.

Use during pregnancy and lactation

Reviews from a psychiatrist about the drug Ketilept confirm that to date its safety and effectiveness during pregnancy have not been established. Therefore, in the vast majority of cases, the use of such a drug is not recommended.

But at the same time, in some cases, the appointment of such a drug is still possible, but only in a situation where the benefit to the expectant mother will outweigh the possible risk to the child. As for the period of breastfeeding, it is currently not precisely established whether the active ingredient quetialin enters the milk or not. Therefore, if there is an urgent need to take this drug, breastfeeding should be stopped immediately.

Mechanism of action

The exact algorithm for the functioning of this medicine is unknown. In conventional tests, the active substance of the drug has antipsychotic activity.

Quetiapine provokes a selective decrease in the functioning of mesolimbic dopaminergic nerve cells. With prolonged use of this drug, no increase in prolactin saturation in the blood plasma is observed. The highest effectiveness of Ketilept is observed when used twice a day.

The active component acts as a powerful paralyzer of serotonin nerve endings and is very similar to histamine and a-1 adrenergic receptors. The antipsychotic and rare extrapyramidal effects of the drug are due to a special combination of antagonistic effects on receptors.

Special instructions for the drug "Ketilept"

Application (reviews also confirm this) should be careful for the following diseases:

• heart diseases;
• seizures;
• tardive dyskinesia;
• neuroleptic malignant syndrome;
• sudden withdrawal reaction;
• for lactose intolerance.

All this is confirmed by patient reviews about the drug Ketilept. If a person suffers from heart disease or vascular defects of the brain, then this drug is prescribed with caution and in a minimal dose. The fact is that Ketilept can provoke orthostatic hypotension, which can manifest itself at the initial stage of treatment. As a rule, this problem occurs in elderly people, so they should start taking the drug strictly under the supervision of their doctor.

To date, there have been no cases of a person experiencing seizures after taking this medication. But this drug, as well as other antipsychotic drugs, can provoke such a reaction. Therefore, it is necessary to start taking this medication with extreme caution.

This is also described in detail in the instructions for the drug "Ketilept".

Reviews also indicate that it can provoke tardive dyskinesia if used for a long time. Therefore, if such an unpleasant symptom makes itself felt, you should immediately contact your doctor to adjust the dose taken downward or to completely discontinue the drug.

Instructions for use KETILEPT®

Since quetiapine has several indications for use, its safety profile should be considered in relation to each patient's diagnosis and dosage of the drug.

Children and adolescents aged 10 to 18 years

Quetiapine is not recommended for children and adolescents under 18 years of age due to the lack of data supporting the use of quetiapine in this age group. In clinical studies with quetiapine, it was found that in addition to the known safety profile established in adults (see section Side effects), some side effects occurred with a higher frequency in children and adolescents compared to adult patients (increased appetite, increased prolactin levels serum, vomiting, rhinitis and syncope), and some side effects have variable significance in children and adolescents (eg, extrapyramidal symptoms and irritability), and one side effect has not previously been observed in clinical trials in adults (increased blood pressure).

Changes in thyroid function test results have also been observed in children and adolescents.

In addition, studies examining the effects of long-term use of quetiapine on growth and development did not exceed 26 weeks. The effect of long-term use of quetiapine on cognitive function and behavior is also unknown.

In placebo-controlled studies in children and adolescents with schizophrenia or manic bipolar disorder, quetiapine was shown to increase the incidence of extrapyramidal symptoms (EPS) compared with placebo (see Adverse Reactions section).

Suicide, suicidal ideation, or worsening clinical condition

Depression in bipolar disorder is associated with an increased risk of suicidal ideation, self-harm, and suicide risk. This risk persists until significant remission occurs. Since improvement may not occur during the first weeks, and possibly for a longer period, patients should be carefully monitored until improvement occurs. Clinical experience also suggests that suicide risk may increase early in the course of improvement.

In addition, clinicians should consider the possible risk of suicide following sudden discontinuation of quetiapine due to known risk factors for the disease being treated with quetiapine.

Other psychiatric disorders for which quetiapine is prescribed may also increase the risk of suicide. Moreover, these disorders may be comorbid with a major depressive episode. Therefore, the same precautions should be taken when treating patients with other psychiatric disorders as when treating patients with a major depressive episode.

Patients with a history of suicidal ideation or behavior, as well as those with significant suicidal ideation before treatment, are at increased risk for suicidal ideation and suicide attempts and should therefore be closely monitored during treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with psychiatric disorders found an increased risk of suicidal behavior when comparing groups of patients receiving antidepressants compared with placebo in patients aged <25 years.

In the early stages of treatment, as well as after changing the dose of the drug, patients, especially those at risk, should be closely monitored.

Patients (and caregivers) should be warned to monitor for clinical worsening, suicidal behavior or ideation, or unusual changes in behavior, and to seek medical attention if these symptoms occur.

In shorter-term, placebo-controlled clinical trials of patients with major depressive episode due to bipolar disorder, an increased risk of suicide-related events was observed in young adult patients <25 years of age receiving quetiapine compared with those receiving placebo (3.0% vs 0). % respectively).

Misuse and Abuse

There have been reports of misuse or abuse. Caution should be exercised when prescribing quetiapine to patients with a history of alcoholism or drug abuse.

Risk of developing metabolic disorders

Based on the observed risk of worsening the metabolic profile in clinical studies, including changes in body weight, changes in lipids and blood glucose (hyperglycemia), metabolic parameters should be monitored at the start of treatment, and changes in these parameters should be monitored regularly as treatment progresses. Deterioration of these parameters should be adjusted based on clinical need (see section Side effects).

Extrapyramidal symptoms

In placebo-controlled clinical trials in adult patients, an increased incidence of extrapyramidal symptoms (EPS) was found compared with placebo in patients treated for major depressive episodes in bipolar disorders (see sections Side effects and Pharmacological effects).

The use of quetiapine has been associated with the development of akathisia with a subjectively unpleasant or depressing restlessness, a need to move, often accompanied by an inability to stand or sit quietly. These symptoms are more likely to develop during the first weeks of treatment. In patients with these symptoms, increasing the dose may harm them.

Tardive dyskinesia

If signs and symptoms of tardive dyskinesia develop, dose reduction or discontinuation of Ketilept® should be considered. Symptoms of tardive dyskinesia may worsen or appear for the first time when treatment is stopped (see Side effects section).

Drowsiness and dizziness

An association has been found between the use of quetiapine and drowsiness or related symptoms (eg, sedation) (see Adverse Reactions section). In clinical studies involving patients with bipolar depression, these symptoms developed during the first three days of treatment, and their intensity was generally mild or moderate. Patients with bipolar disorder who develop severe, severe sleepiness may need more frequent contact with their doctor for at least 2 weeks after the onset of sleepiness.

Orthostatic hypotension

Quetiapine may cause orthostatic hypotension and associated dizziness (see section Side effects), especially at the initial stage of dose selection; it occurs more often in older patients than in younger patients. This may increase the risk of accidental falls, especially in older patients, compared to younger ones. For patients with cardiovascular disease, a dose reduction or slower individual dose titration is recommended. Therefore, patients are advised to exercise caution before determining the effect of the drug on their body.

Cardiovascular diseases

Ketilept® should be used with caution in patients with known cardiovascular disease, cerebrovascular disease, or other conditions predisposing to hypotension. Quetiapine may cause orthostatic hypotension, especially during the initial dose titration period, so a dose reduction or slower dose titration should be considered. Slower dose titration is recommended in patients with cardiovascular disease.

Sleep apnea syndrome

Sleep apnea syndrome has been observed in patients receiving quetiapine. Quetiapine should be administered with caution to patients taking other medicinal products that inhibit the central nervous system and who currently have or have had a history of sleep apnea (eg, weight gain/obesity, male patients).

Epileptic seizures

In controlled clinical trials, no differences were found in the frequency of epileptic seizures in patients receiving quetiapine or placebo. There are no data on the frequency of seizures in patients with a history of seizures. As with other antipsychotic drugs, caution should be exercised when treating patients with a history of epileptic seizures (see Side Effects section).

Neuroleptic malignant syndrome (NMS)

Neuroleptic malignant syndrome can occur during treatment with antipsychotic drugs, including quetiapine (see section Side effects). Its clinical manifestations include fever, changes in mental status, muscle rigidity, instability of autonomic functions (inconsistent heart rate and blood pressure, sweating, arrhythmia), as well as increased levels of creatine phosphokinase. In such cases, Ketilpet® should be discontinued and appropriate drug therapy should be prescribed.

Severe neutropenia and agranulocytosis

Severe neutropenia (neutrophil count <0.5 x 109/L) was observed in clinical studies with quetiapine. Most cases of severe neutropenia developed within several months of starting treatment with quetiapine. There is no obvious dose dependence of this effect. Based on post-marketing experience, some cases have been fatal. Possible risk factors for the development of neutropenia include a history of low white blood cell count or neutropenia caused by other drugs. If the neutrophil count decreases to <1.0 x 109/L, quetiapine should be discontinued. Patients should be monitored for signs and symptoms of infection and neutrophil levels monitored until they exceed 1.5 x 109/L (see Side Effects and Pharmacological Actions).

The possibility of developing neutropenia should be considered in patients with infection or fever, especially in the absence of predisposing factors, which requires appropriate treatment. Patients should be informed to report signs/symptoms of agranulocyotosis/infection (fever, weakness, lethargy, or sore throat). In such patients, it is necessary to immediately determine the number of leukocytes and the absolute number of neutrophils, especially in the absence of predisposing factors.

Anticholinergic (muscarinergic effects)

Norquetiapine, the active metabolite of quetiapine, has moderate to strong affinity for various muscarinic receptor subtypes. This predetermines the possibility of developing anticholinergic side effects when using quetiapine in recommended doses, when used together with other drugs that have anticholinergic properties, as well as in overdose. Quetiapine should be used with caution in patients concomitantly receiving other drugs with anticholinergic properties. Quetiapine should also be prescribed with caution to patients who have or have previously had urinary retention, clinically significant prostatic hypertrophy, intestinal obstruction or similar conditions, increased intraocular pressure or angle-closure glaucoma (see sections Drug interactions, Side effects, Overdose and Pharmacological effects).

Interactions

(see also section Drug interactions)

The use of quetiapine concomitantly with a strong hepatic enzyme inducer, such as carbamazepine or phenytoin, significantly reduces the plasma concentrations of quetiapine, which may affect the effectiveness of treatment with this drug. In patients receiving a liver enzyme inducer, treatment with Quetiapine should only be initiated if the physician determines that the benefits of quetiapine outweigh the risk of discontinuing the liver enzyme inducer. It is important that any change in inducer dosage be gradual and, if necessary, replaced with a non-inducer drug such as sodium valproate.

Body mass

Weight gain has been observed in patients receiving quetiapine; changes in body weight should be monitored and adjusted as a clinically important change, in accordance with available guidelines for the use of antipsychotic drugs (see sections Side effects and Pharmacological effects).

Hyperglycemia

Hyperglycemia or exacerbation of pre-existing diabetes, sometimes accompanied by the development of ketoacidosis or coma, sometimes fatal, have been described in rare cases (see section Side effects). In some cases, this was preceded by an increase in body weight, which can be considered as a predisposing factor. Appropriate clinical monitoring is recommended in accordance with available guidelines for the use of antipsychotic drugs. Patients receiving antipsychotic drugs, including quetiapine, should be monitored for the development of signs and symptoms of hyperglycemia (polydipsia, polyuria, polyphagia and weakness), and patients with diabetes, as well as patients at risk of developing diabetes mellitus, should be regularly monitored for worsening glycemic control. control.

Lipids

Increases in triglycerides, LDL and total cholesterol, as well as decreases in HDL cholesterol, were observed in clinical studies with quetiapine (see Side Effects section). Changes in lipid levels should be monitored and corrected as clinically significant.

QT prolongation

In clinical trials in which the drug was used in accordance with the instructions for medical use, the use of quetiapine was not associated with persistent prolongation of the QT interval. However, in post-registration studies, prolongation of the QT interval was observed in therapeutic doses (see section Side effects) and in overdose (see section Overdose). Just as when prescribing other antipsychotic drugs, caution should be exercised when prescribing quetiapine to patients with cardiovascular diseases, when combining quetiapine with drugs that increase the QT interval (including other antipsychotic drugs), especially in elderly patients, patients with congenital long QT syndrome, heart failure, cardiac hypertrophy, hypokalemia, hypomagnesemia and in patients with a family history of QT interval prolongation.

Cardiomyopathy and myocarditis

In clinical studies and with the use of quetiapine in the post-registration period, there have been reports of the development of cardiomyopathy and myocarditis, however, a causal relationship with quetiapine has not been established. The appropriateness of treatment with quetiapine in patients with cardiomyopathy and myocarditis should be analyzed.

Sudden withdrawal reactions

Acute withdrawal symptoms, including insomnia, nausea, vomiting, headache, diarrhea, dizziness, and irritability, have been described after abrupt discontinuation of high-dose antipsychotic medications. Therefore, if it is necessary to stop taking the drug, it is recommended to gradually reduce the dose over one to two weeks (see section Side effects).

Elderly patients with dementia-related psychosis

Quetiapine is not approved for use in patients with psychosis associated with dementia.

An approximately 3-fold increase in the risk of adverse cerebrovascular events was observed in randomized placebo-controlled trials in populations with dementia with the use of some atypical antipsychotics. The mechanism for this increased risk is unknown. An increased risk cannot be excluded also with the use of other antipsychotics or in other patient populations. In placebo-controlled studies using quetiapine, the incidence of cerebrovascular adverse events per 100 patient-years in the quetiapine group was not greater than that in the placebo group. Quetiapine should be used with caution in patients with risk factors for stroke.

A meta-analysis of atypical antipsychotics found that older patients with dementia-related psychosis had an increased risk of death compared with placebo.

However, in two 10-week placebo-controlled studies of quetiapine in the same patient population (n=710; mean age 85 years, range 56-99 years), mortality in the quetiapine group was 5.5% versus 3.2% in the placebo group. In these studies, patients died from many causes that would be expected in this population. These data do not allow us to establish a causal relationship between quetiapine use and death in elderly patients with dementia.

Dysphagia

Dysphagia (see Side Effects section) and aspiration have been observed during treatment with quetiapine. Ketilept® should be used with caution in patients at risk of developing aspiration pneumonia.

Constipation and intestinal obstruction

Constipation is a risk factor for intestinal obstruction. There have been reports of constipation and intestinal obstruction while taking quetiapine (see section Side effects). Deaths have been reported in patients at increased risk of intestinal obstruction, including those concomitantly receiving drugs that inhibit intestinal motility, who did not inform the doctor about the development of constipation. Patients with intestinal obstruction require close monitoring and emergency medical attention.

Venous thromboembolism

Cases of venous thromboembolism (VTE) have been observed during treatment with antipsychotic drugs. Due to the fact that patients receiving antipsychotic drugs had acquired risk factors for VTE, all possible risk factors for VTE should be identified before and during treatment with Ketilept® and preventive measures should be taken.

Pancreatitis

Pancreatitis has been observed both in clinical studies and in post-marketing experience. Despite the fact that in the post-registration period, risk factors were not identified in all cases, many patients had factors against which pancreatitis could develop:

• increased triglyceride levels (see section Special instructions), gallstones and alcohol consumption.

Additional Information

There are limited data on the use of quetiapine in combination with divalproex or lithium for moderate to severe episodes of mania. However, combination therapy was well tolerated (see sections Side effects and Pharmacological effects). These data revealed an additive effect at week 3.

Ketilept® contains lactose monohydrate

Since Ketilept® contains lactose monohydrate, this drug should not be prescribed to patients with rare hereditary disorders of galactose tolerance, hereditary lactose deficiency or glucose-galactose malabsorption syndrome.

Preclinical safety studies

In a series of in vitro

and
in vivo
no signs of genotoxicity were detected. The following abnormalities have not yet been confirmed in long-term clinical trials in laboratory animals at exposure levels achievable in clinical settings:

Pigment deposition in the thyroid gland was observed in rats. In marmoset monkeys, follicular cell hypertrophy of the thyroid gland, a decrease in plasma T3 levels, a decrease in hemoglobin levels and the number of erythrocytes and leukocytes were found. Cases of lens opacities and cataracts have been reported in dogs.

Given all these data, the benefit of quetiapine treatment must be weighed against the safety risk to the patient.

Impact on the ability to drive vehicles and operate machinery

Due to its effect on the central nervous system, Ketilept® may reduce the level of wakefulness of patients. Therefore, in the first stages of treatment, for an individually determined period of time, patients should be advised to refrain from driving vehicles and working with dangerous mechanisms. In the future, the degree of restrictions should be set for each patient individually.

Signs of neuroleptic syndrome

Often, during medical therapy, a person is diagnosed with neuroleptic malignant syndrome. It can be identified by the following symptoms:

• hyperthermia;
• changes in mental status;
• the appearance of muscle rigidity;
• instability of the nervous system.

If such signs are detected, then you should immediately stop using Ketilept and, accordingly, carry out medical therapy to eliminate this defect.

If a person experiences a sudden withdrawal reaction, they will experience the following symptoms:

• signs of acute withdrawal;
• severe nausea;
• gagging;
• insomnia.

It is worth emphasizing that such a reaction of the body occurs in very rare cases. It mainly manifests itself if the antipsychotic drug is abruptly stopped. In this case, a mental disorder is added to all the signs described above. In order to avoid this effect, the patient should gradually reduce the dosage of the drug used and only then completely abandon it.

If a person has lactose intolerance, then this medication is replaced with an analogue. The fact is that the shell that covers the tablets is created with the addition of lactose. Therefore, the drug is not recommended for use. But if it is not possible to switch to an analogue, then the use of such tablets is started extremely carefully, monitoring the manifestation of side effects.

Overdose

As the instructions for use indicate for the drug “Ketilept” (reviews also confirm this), to date there have been cases of overdose, which are expressed in the following symptoms:

• decrease in blood pressure;
• increased heart rate;
• drowsiness;
• manifestation of apathy;
• in rare cases, coma may occur.

If this drug is combined with other antipsychotic medications, fainting and swelling of the entire body may occur.

At the moment, there are no special antidotes that can neutralize an overdose. Therefore, therapeutic therapy is aimed at normalizing the activity of the cardiovascular system, as well as restoring respiratory function. For these purposes, the patient is provided with ventilation and oxygenation.

A prerequisite is complete observation of the victim until his complete recovery.

Reviews after using this medication

There are a lot of reviews for the drug "Ketilept". For depression, it is prescribed quite often.

And the overwhelming majority of reviews about this medication are positive. A very good and effective drug, people who started taking this drug got rid of panic attacks that they had suffered from for a long time. And the main advantage of this medication is that there are practically no side effects. The conclusion suggests itself: Ketilept is an effective antipsychotic medication.

Often people come to the appointment who show signs of schizophrenia. In this case, the drug Ketilept is recommended, since its active substance has a sedative effect. As for side effects, with many years of practice in prescribing this drug, such negative effects were extremely rare. Therefore, when diagnosed with schizophrenia, only this medication is clearly prescribed.

Pharmacokinetics of the drug

When taken internally, the active ingredient is quickly absorbed from the gastrointestinal tract. The ability to bind to plasma proteins is 83%. The active component undergoes a complete metabolization process in the liver. The main metabolites of the drug do not have clear pharmacological dynamics.

The half-life is approximately seven hours. 73% of quetiapine is excreted in urine, 21% in feces. About 5% of the active component cannot be metabolized and is released in its original form.

The rate of plasma clearance from the drug in elderly patients is 40-50% less than in patients aged eighteen to sixty years. In the presence of clinical renal impairment, the plasma clearance rate is approximately 25% less than in healthy patients.

What do experts say about this medication?

Reviews from doctors about the drug “Ketilept” confirm that when prescribing this drug, the patient has to get used to it for a very long time, but the result of such torment is worth it. After using the medicine, all mood swings disappear. And most importantly, apathy towards the world around us disappears.

Initially, the doctor prescribes taking this medication 300 mg per day. As soon as the course of treatment begins, the patient experiences lethargy and constant drowsiness. But gradually these side effects go away, and in return a long-awaited feeling of calm and self-confidence appears.