pharmachologic effect
The medicine has a pronounced sedative effect. Taking it calms aggression, relieves pathological agitation, and normalizes sleep. The active substance blocks alpha adrenergic receptors and dopamine D2 receptors in the brain, reducing nervous tension.
White Azaleptin tablets, penetrating the stomach, quickly dissolve, are absorbed into the blood and begin to work. Maximum fixation in plasma is observed after 2-3 hours. The main substance can accumulate in the body.
Metabolized passing through the liver. It is eliminated from tissues using the kidneys and stomach. The elimination time depends on the dosage.
During treatment, you should not do work that requires concentration or drive a car. Under the influence of pills, a person’s reaction speed decreases.
Analogues of the drug Azaleptin
Clozapine
- Azalepticon
Alemoxan
Closasten
Leponex
Print a list of analogues Clozapine (Clozapine) Antipsychotic drug Granules for the preparation of suspension for oral administration, solution for injection, tablets
An antipsychotic drug (neuroleptic), practically does not cause extrapyramidal disorders, enhances the effect of hypnotics and analgesic drugs. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems. The sedative effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus. It has peripheral and central m-anticholinergic, alpha-adrenergic blocking effects. Does not affect the concentration of prolactin in the blood.
The antipsychotic effect is close to that of aliphatic phenothiazines, but without the “submelancholic tint” and unpleasant subjective sensations, does not have a cataleptogenic effect, and reduces the threshold of convulsive readiness.
Does not affect higher intellectual functions, practically does not cause extrapyramidal disorders.
Indications
Schizophrenia (including resistant to therapy with other neuroleptics and/or intolerance to them), manic states, manic-depressive psychosis, psychomotor agitation in psychopathy, emotional and behavioral disorders (including in children), sleep disorders .
Application and dosage
Orally, after meals, 2-3 times a day. Single dose for adults – 50-200 mg, initial daily dose – 150-300 mg, average daily dose – 200-400 mg. The highest daily dose is 600 mg.
The dose is selected individually, starting with small doses (25 mg) and increasing them by 25-50 mg per day until a therapeutic effect is obtained.
The staged nature of the manifestation of the therapeutic effect should be taken into account: the rapid onset of hypnotic and sedative effects; relief of anxiety, psychomotor agitation and aggressiveness (after 3-6 days); antipsychopathic effect (after 1-2 weeks); effect on symptoms of negativism (after 20-40 days). After achieving a therapeutic effect, they switch to a maintenance course.
Granules from a disposable package are diluted in 5-10 ml of water: a single dose for children 6-8 years old - 5-10 mg, 8-15 years old - 10-20 mg, daily dose for children 6-8 years old - 15-30 mg, 8-15 years – 30-60 mg; it is divided into 2-3 doses; the highest daily dose for children is 100 mg.
Interaction
Increases the effect of sedative and hypnotic drugs, drugs for general anesthesia, narcotic analgesics, MAO inhibitors, antihypertensive drugs, ethanol.
Weakens the effect of levodopa and other dopamine stimulants.
Absorption from the intestine is impaired when taking gel-type antacids and cholestyramine.
In combination with benzodiazepines, an excessive decrease in blood pressure, impaired consciousness, depression or respiratory arrest is possible.
Concomitant use of Li+ drugs increases neurotoxicity (delirium, seizures, extrapyramidal disorders).
Pentetrazole increases the risk of seizures.
Do not use in combination with tricyclic antidepressants, antipsychotic drugs, drugs that damage blood cells (pyrazolone-containing NSAIDs), antidepressants, carbamazepine, Au preparations, thyreostatics and antimalarial drugs.
Caution should be exercised when co-prescribing antiepileptic drugs, anticoagulants, antimicrobial and hypoglycemic drugs (sulfonylurea derivatives). Myelotoxic drugs increase the manifestations of hematotoxicity of the drug
Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.
Contraindications
Before treatment, the list of contraindications should be excluded. The instructions say that the drug is prohibited in the following conditions:
- individual intolerance to the main active ingredient;
- severe damage to the cardiovascular system;
- kidney and liver diseases;
- glaucoma;
- epilepsy;
- hematopoietic dysfunction;
- pathological changes in the prostate gland.
A categorical contraindication is pregnancy, lactation and children under 5 years of age.
Treatment
Symptom-based therapy consists of eliminating the victim’s complaints:
- pain in the stomach - painkillers and antispasmodics: No-shpa, Drotaverine, Papaverine, Spazgan, Revalgin, Spazmalgon, Novigan, etc.,
- nausea and vomiting – Smecta, Neosmectin, Bifiform,
- heartburn - Almagel, Rennie, Phosphalugel, Gastal, Gaviscon,
- excessive excitement, muscle cramps - extract of valerian, motherwort (in tablets!), other sedatives.
Monitoring the state of the cardiovascular system is ensured by an ECG, and restoration of water-salt balance is ensured by drinking plenty of fluids.
It is necessary to monitor the patient’s health for a week in order to early identify possible complications of an overdose of Azaleptin.
Side effects
The medicine should be used only under the constant supervision of a doctor. Its use may cause side effects.
- A dangerous complication is granulocytopenia. In this condition, agranulocytosis develops. In humans, the level of leukocytes in the blood critically decreases. As a result, susceptibility to fungal and viral infections increases.
- Other side effects include aplastic anemia. Under the influence of the drug, the functioning of the hematopoietic system is disrupted, threatening death to the patient.
At the recommended dosage, the drug is well tolerated. In some cases there are:
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- sleep disorders;
- headache;
- confusion;
- blood pressure surges;
- dizziness;
- tachycardia;
- bowel dysfunction;
- dry mouth or increased salivation.
The genitourinary system may be affected: there are complaints of pain when urinating, frequent urge to go to the toilet, decreased potency.
Azaleptin
Azaleptin belongs to the group of antipsychotic drugs, neuroleptics.
Release form and composition
The only form of release of the drug is tablets of 25 and 100 mg. The tablets are packaged either in contour cells of 10 pieces each, or in light-protective glass jars of 50 pieces. Both forms of release are located in cardboard boxes. One box contains 1 bank or 5 contour cells.
Each Azaleptin tablet contains clozapine (azaleptin) in an amount of 25 or 100 mg. Auxiliary additives are: lactose monohydrate or milk sugar - 0.101/0.11 g (in tablets containing clozapine 25 mg and 100 mg, respectively), calcium stearate - 0.0015 and 0.0025 g, potato starch - 0.0225 and 0.375 g.
According to the instructions for Azaleptin, treatment with the drug is advisable for disorders of the nervous system listed below:
- For schizophrenia in acute or chronic form;
- In manic states;
- For manic-depressive psychosis;
- With psychomotor agitation arising against the background of psychopathy;
- For behavioral and emotional disorders, including in pediatric patients;
- For sleep disorders of various origins.
Side effects of Azaleptin
The instructions for Azaleptin list possible negative reactions to the drug, which should be read before starting treatment:
- Headache, akathisia, agitation, drowsiness, confusion, insomnia, extrapyramidal disorders (which include hypokinesia, tremor, akinesia, muscle rigidity), depression, restless sleep, NMS, tardive dyskinesia, epileptic seizures;
- Arterial hypotension, tachycardia, arterial hypertension, orthostatic hypotension and dizziness against its background;
- Nausea, heartburn, hypersalivation, dry mouth, vomiting;
- Increased sweating, sudden increase in body weight;
- Leukopenia, eosinophilia, thrombocytopenia, granulocytopenia;
- Accommodation disorders, constipation, dry mouth, urination problems;
- Decreased potency.
Analogues of Azaleptin
The instructions for Azaleptin indicate the following analogues of the drug:
- Clozapine;
- Closasten;
- Azaleprol;
- Leponex.
Terms and conditions of storage
Azaleptin is a potent drug and should be kept away from children. The shelf life of the drug is 5 years from the date of release. It is necessary to choose a storage place protected from light, where the temperature does not rise above 30 °C.
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Instructions
The doctor prescribes the dosage individually based on the patient’s clinical picture. The drug should be taken 2-3 times a day after meals, with plenty of liquid.
For adults
A single dosage ranges from 25 to 200 mg. To avoid side effects, doctors often increase it gradually, starting with a minimal amount.
A lethal dose is considered to be taking more than 600 mg of the drug per day. You need to be careful during treatment and not increase the use of pills uncontrollably.
- For insomnia, excessive excitability and other sleep disorders, it is recommended to drink 25-50 mg of the drug twice a day.
- Relief of anxiety symptoms is observed on days 3-6. A person's nervous tension decreases, anxiety disappears, and sleep normalizes.
- To consolidate the therapeutic effect, it is necessary to continue taking the antipsychotic for 1-2 weeks.
For children
Azaleptin is rarely used in pediatrics. Its use is allowed for serious mental disorders in children over 5 years of age. Therapy is required to eliminate symptoms:
- manic-depressive syndrome;
- schizophrenia;
- behavioral and emotional disorders.
Can be used if the child is haunted by thoughts of suicide or suffers from unmotivated aggression. The course of treatment must be carried out under the supervision of medical personnel and parents. The dosage is selected individually.
During pregnancy and lactation
The active substance included in Azaleptin can negatively affect the fetus, so pregnant women should not use the tablets. The components of the medicine pass into breast milk. If there is a need for treatment during lactation, breastfeeding should be discontinued.
Indications
This antipsychotic has a pronounced and rapid sedative effect. There are many mental and neurotic disorders that can be treated with Azaleptin. Indications for use of the drug are as follows:
- Acute and chronic schizophrenia, accompanied by psychotic symptoms.
- Bipolar disorder is a disease in which periods of unnaturally elevated mood and increased activity alternate with phases of depression and loss of energy.
- Manic states in various mental illnesses These are pathologies characterized by causeless fun, unreasonable optimism, excessive talkativeness, hyperactivity and sleep disorders.
- Increased nervous excitability and excessive emotionality in children.
- Insomnia due to neurotic disorders.
It is important to remember that this drug is strictly prescription and self-medication in this case is absolutely unacceptable. Only a doctor can prescribe the potent antipsychotic "Azaleptin"
Psychiatrists often use this medication in cases where the patient has developed tolerance to other antipsychotic drugs.
Overdose
Exceeding the recommended dose provokes intoxication of the body and poisoning. They appear:
- nausea;
- vomiting;
- headaches;
- excessive sleepiness;
- confusion.
In severe cases, a person experiences breathing difficulties, epilepsy attacks, and tachycardia. If the patient is not provided with medical care, coma and death may occur.
In case of overdose, you should urgently call an ambulance. The patient is advised to lavage the stomach, take adsorbents and drugs to support the respiratory and cardiac systems .
How to take the drug
Azaleptin is recommended to be taken after meals. The dosage of the drug is determined by the attending physician. Typically, therapy is started with a small amount of the drug: from 25 mg to 50 mg per day. Then, if necessary, the dosage is gradually increased by approximately 25 - 50 mg daily. A maximum of 600 mg of antipsychotic medication per day is allowed.
After the patient feels better, they are transferred to maintenance doses of 25 mg to 150 mg per day. Elderly patients are prescribed reduced dosages of the drug.
You should not suddenly stop taking Azaleptin. Otherwise, withdrawal syndrome may develop, especially if the drug was taken for a long time and in large doses. This condition is characterized by anxiety, insomnia, and exacerbation of signs of mental illness. Therefore, antipsychotics are discontinued gradually, gradually reducing the daily dose.
Interaction with other tools
Azaleptin interacts with medications. To exclude complications, it is necessary to tell the doctor about all the medications used by the patient.
- The medicine should not be taken simultaneously with substances that depress the central nervous system. These include haloperidol, caffeine, narcotics, and tranquilizers. They increase the risk of side effects, causing shortness of breath and difficulty breathing.
- Clozapine enhances the effect of sleeping pills, so when taken together, you must scrupulously follow your doctor's prescriptions.
- The use of Azaleptin together with valproic acid and Risperidone disrupts the metabolism of the main active substance and increases its concentration in the blood.
- Combination with lithium carbonate threatens deterioration of mental stability, convulsions and headaches.
What does Azaleptin help with?
The main indications for prescribing Azaleptin are the following conditions/diseases:
- Bipolar disorder;
- Schizophrenia is a disease characterized by decomposition of thinking;
- When psychoses alternate between manic and depressive phases with periods of well-being, these are diseases accompanied by unreasonable anxiety, anxiety, anger, absent-mindedness and fun, accompanied by sleep disorders;
- The body’s resistance to other psychotropic drugs or their individual intolerance;
- Manic states - pronounced optimism, excessively good mood, caused by diseases of the central nervous system or psychoses;
- The drug is also prescribed for children with excessive emotionality and severe behavioral disorders.
The drug is indispensable for those suffering from schizophrenia, depressive psychoses and sleep disorders, especially in cases where other medications do not bring the desired effect. Although you feel better after the first dose, you should not self-medicate.
Directions for use and doses
The drug Azaleptin ® should be used only if, before treatment, the number of leukocytes and the absolute number of neutrophils are within normal limits, i.e. leukocyte count ≥3.5·10 9 /l, and absolute neutrophil count ≥2·10 9 /l. In addition, when using the drug, it is necessary to be able to regularly determine the number of leukocytes and the absolute number of neutrophils: weekly for the first 18 weeks, then at least once every 4 weeks throughout the course of treatment, as well as 4 weeks after the end of treatment.
The dose of the drug should be selected individually. The minimum effective dose should be used in each patient. In order to minimize the risk of hypotension, seizures and sedation, the dose should be selected with caution, dividing the daily dose into several doses.
In patients receiving medications that interact with Azaleptin ® (such as benzodiazepines or SSRIs), adequate dosage adjustment of the drug is necessary.
Transition from previous treatment with antipsychotics to therapy with Azaleptin ® .
It is not recommended to use the drug Azaleptin ® in combination with other antipsychotics. In the event that treatment with Azaleptin ® needs to be started in a patient already taking an antipsychotic by mouth, the dose reduction or discontinuation of the previous drug should be done gradually. Based on clinical data, the attending physician should determine the need to discontinue taking another antipsychotic before starting therapy with Azaleptin ® .
Treatment-resistant schizophrenia
On the first day, use 1 tablet. 25 mg 1 time per day. If it is necessary to start treatment with a dosage of 12.5 mg (1/2 tablet of 25 mg) 1 or 2 times a day, scored tablets containing clozapine 25 mg should be used for dosing accuracy; on the second day - 1 or 2 tablets. drug 25 mg. Subsequently, if well tolerated, the dose of the drug can be slowly increased by 25–50 mg so that within 2–3 weeks a daily dose of no more than 300 mg is reached. Then, if necessary, the daily dose can be increased by 50-100 mg every 3-4 days or, preferably, every 7 days.
In most patients, the onset of the antipsychotic effect of the drug should be expected when using a daily dose of Azaleptin ® 300–450 mg (in several doses). Some patients may benefit from a lower dose; others may require doses up to 600 mg/day. The daily dose can be divided into separate doses unevenly, taking most of it before bedtime.
To achieve the full therapeutic effect, some patients require a higher dose of the drug. In this case, it is advisable to gradually increase the dose (by no more than 100 mg each time) until a maximum dose of 900 mg/day is reached. The possibility of a more frequent development of side effects (in particular, the appearance of seizures) should be taken into account when using a dose exceeding 450 mg / day.
After achieving the maximum therapeutic effect, lower maintenance doses may be used. The dose of the drug should be reduced slowly and with caution. Maintenance treatment should continue for at least 6 months. If the daily dose of the drug does not exceed 200 mg, you can switch to a single evening dose of the drug.
Azaleptin, how to quit. can you help me get off azaleptin?
In general, I take Azaleptin 50 mg before bed and that’s all! As soon as I start to get off it, I don’t sleep at night, but I feel great and my mood is better! physical activity is better! ENDURANCE! but then before the second night after stopping azaleptin I start to feel tension in my body and without running or fast walking it is very noticeable. In short, I stopped taking azaleptin and didn’t sleep that night - it seemed normal) but then I decided to sleep anyway and not spend the second night without sleep, I lay down and couldn’t get rid of my thoughts! both positive and negative thoughts kept me awake! there is a feeling that the origin seems to need rest, but the brain does not allow it to rest... constant thoughts that I have heard and know from life criticize me or give advice or call me names, for example, “go to sleep,” and another thought “NO! Are you too weak to sleep?? " then " find yourself a girl! "" Fuck you, you need this!..." "Don't listen to anyone! " "Let's stop playing with your mind))) " "How can I stop! I've already tried it! thoughts don't go away! " "Well, you're a loser... ahahah" "Fuck you! “(this is me) I was diagnosed with “psychosis” but for some reason I suspect that I just have a strong neurosis! after all, after I more or less managed to fall asleep, I SHARPLY wake up from FEAR (either from thoughts or from a dream that had just begun) and I twitch very strongly!! I'm twitching very hard!.. until I more or less understand that the situation is not what I thought... I'm afraid to go back to the psychiatric hospital! I don’t trust the doctor because it seems to me that he will deceive me and make the wrong diagnosis just for his own benefit! I don’t hear voices and I don’t have glitches!... it’s just that my brain itself generates such thoughts because of which I can’t decide what to do in real time... and also... it seems to me that my attention does not support multitasking... BUT I’m very I focus well on ONE task while I don’t complete others!... and my reaction speed is FAST... I thought it was because of the ANDROENES that I injected while doing sports... it also happens that from caffeine (tea and coffee0 I get so worked up that I It seems like I’m going to lose consciousness or my heart is going to stop... when in the evening I look out the window and see that it’s dark there, I immediately have thoughts like (wow... it’s time for crime, beatings, robberies and murders) the world is somehow perceived negatively without positivity... and in every person I see only the bad (well, almost) all the time I look for the negative in a person so that I know what I can get to the bottom of... and feeling not from the whole world sometimes I have such a thought (HE’S not like everyone else, he knows too much) that it’s like we won’t even talk to people they see my basis of thinking and despise me, in short, it all the time seems that no one likes me... it feels like now I know the world as truly as possible... I used to work out in the gym, I was eager to pump up... but now... it feels like just to laugh) ))... under azaleptin I don’t love anyone, but at least they love me (girls from contacts) and without alaleptin this is the thought - a girl: he loves me and I will move away from him and let him run after me and try to get me) ahahahaha... more there is such a thought “I shouldn’t leave the house and get fucked, no one should know that I’m a beast, otherwise modern society will devour me or try to humiliate me, one will be afraid of me, then he will tell about me to a more frostbitten type and he will want to make sure that I remain either humiliated or he’ll kill you” - that’s a crazy thought.. hahahah in short I CAN’T RELAX after stopping Azaleptin.. I’m tense and anxious all the time) I can of course compensate for this with positivity, but in the end I’ll be exhausted but I won’t be calm anyway... the world used to seem colorful to me! but now something is wrong... what a gloomy world... all attacks on me are taken to heart...
Storage conditions and periods
The medicine should be stored for no more than 3 years out of the reach of children, since Azaleptin poisoning is very dangerous. The temperature in the room should be maintained at 15-30 °C.
Azaleptin - tips and recommendations on News4Health.ru
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General information about the drug
The drug has been known on the market for more than 25 years and is the most effective among other antipsychotics. The medicine belongs to the class of drugs with antipsychotic and sedative effects.
Drug group, INN, scope of application
The drug is classified as an atypical antipsychotic. INN of the drug is Clozapine. Azaleptin has been successfully used in psychiatric and neurological practice since the end of the 20th century and continues to be valued by specialists due to its wide spectrum of antipsychotic action, which makes it stand out among its analogues.
Release forms, prices and composition of Azaleptin
Azaleptin can be purchased in pharmacies in the form of round green tablets; the price of the drug depends on the dosage.
The main substance of the drug is clozapine. Its dosage in one tablet is 25 mg and 100 mg. You can purchase in quantities of 50 pieces in a plastic or glass jar. Additional substances included in the composition include potato starch (0.02 and 0.03 g), calcium stearate (0.001 and 0.002 g), lactose monohydrate (0.101 and 0.11 g).
Pharmacodynamics and pharmacokinetics
The structure of the drug is similar to benzodiazepines and tricyclic antidepressants. It belongs to a number of atypical neuroleptics due to the minimal amount of extrapyramidal dysfunctions that occur.
It has not only a sedative and antipsychotic effect, but also inhibits manic and depressive activity, and also belongs to the group of drugs with a hypnotic effect, and also potentiates the effect of analgesics and hypnotics.
The actions of the substance are manifested by blocking dopamine, serotonin, muscarinic, histamine and adrenergic receptors. The absence of extrapyramidal disorders is directly related to the blocking of dopamine D2 receptors in the mesocortical region of the brain. The effect on GABA receptors provokes a muscle relaxant effect.
General information about the drug
Taking the medicine does not affect intellectual functions. The effect of taking Azaleptin appears gradually. First, a hypnotic and sedative effect occurs, then anxiety and increased excitability go away, and the antipsychotic effect and negativism appear at the end of treatment, after a month and a half.
The drug is well adsorbed in the digestive system. The maximum amount of the main substance appears in the blood 2-3 hours after administration, and a stable concentration level appears after the 10th day of treatment. The medicine binds to blood proteins by 90-95%. The distribution and accumulation of the substance in the body occurs very quickly. In the liver it breaks down into metabolic products and is excreted in bile and urine. Complete elimination from the body is observed 8 hours after administration.
Chemical structure and metabolism
In terms of its chemical structure, it is a tricyclic compound that has elements of similarity to tricyclic antidepressants and partially to benzodiazepine tranquilizers. The first metabolite in the chain of biotransformation of clozapine in the liver is norclozapine (N-desmethylclozapine), which has all the same pharmacological properties as the parent compound. One of the metabolites of norclozapine in the body is benzodiazepine, which is partly responsible for the strong anti-anxiety activity of clozapine.