How to take Azaleptin
To minimize the risk of low blood pressure, seizures and drowsiness, your doctor should gradually increase the dose of the drug. You should always take Azaleptin exactly as prescribed by your doctor. If you have any doubts, you should consult your doctor or pharmacist.
First of all, it is important not to change the dosage or stop taking Azaleptin without notifying your doctor. Continue taking the drug for as long as your doctor directs. If you are 60 years of age or older, your doctor may start treatment at a lower dosage and increase it gradually because patients in this age group are more likely to develop some unwanted side effects (See "What You Need to Know Before You Use Azaleptin").
If the dosage that you have been prescribed cannot be achieved with this dose, there are other doses of this drug that can be used to achieve the desired dosage of the drug.
Azaleptin tablets can be divided into equal doses.
Treatment of schizophrenia
The recommended starting dose is 12.5 mg (half a 25 mg tablet) once or twice on the first day, then 25 mg once or twice on the second day. Swallow the tablet with water. If this dose is well tolerated, your doctor may gradually increase the dose in increments of 25 to 50 mg over the next 2 to 3 weeks until the dose reaches 300 mg per day. After this, if necessary, the daily dose can be increased further in steps of 50 to 100 mg per half week or, preferably, at weekly intervals.
The recommended daily dose is 200 to 450 mg, divided into several single doses per day. Some people may need a higher dose. The permissible daily dose can be up to 900 mg. Frequent side effects (in particular, seizures) are possible with daily doses of more than 450 mg. Always take the individually determined minimum effective dose of the drug for you. Most people take part of the dose in the morning and another part in the evening. Your doctor will advise you on how to divide the daily dose correctly. If your daily dose is only 200 mg, then you can take it once in the evening. Over a period of time, while you are taking Azaleptin and experiencing positive results, your doctor may lower your dose. It is necessary to take Azaleptin for at least 6 months.
Treatment of severe thinking disorders in patients with Parkinson's disease
The recommended starting dose is 12.5 mg (half a 25 mg tablet) in the evening. Swallow the tablet with water. Your doctor may then gradually increase your dose in 12.5 mg increments, no faster than two steps per week, to a maximum dose of 50 mg by the end of the second week. Dosage increases should be stopped or delayed if you feel weak, dizzy or confused. To avoid these symptoms, blood pressure should be measured during the first weeks of treatment.
The recommended daily dose is 25 to 37.5 mg, taken once in the evening. The dose of 50 mg per day should only be exceeded in exceptional cases. The maximum daily dose is 100 mg. Always take the minimum effective dose of the drug individually selected for you.
If you take more Azaleptin than recommended
If you think you have taken a large number of Azaleptin tablets, or if someone has taken your tablets, you should immediately contact your doctor or seek emergency medical help.
Overdose symptoms include:
Drowsiness, fatigue, loss of energy, loss of consciousness, coma, confusion, hallucinations, agitation, incoherent speech, stiff limbs, tremors, seizures, increased salivation, dilated pupils, blurred vision, low blood pressure, collapse, fast or irregular heartbeat, shallow or difficult breathing.
If you forget to take Azaleptin
If you forget to take your next dose, take it as soon as you remember. If it is time for your next dose, skip the missed dose and take the next dose at the usual recommended time. Do not take a double dose to make up for a missed dose. Contact your doctor as soon as possible if you have not taken Azaleptin for more than 48 hours.
If you stop taking Azaleptin
Do not stop taking Azaleptin without the advice of your doctor, as you may experience withdrawal symptoms. It includes sweating, headache, nausea, vomiting and diarrhea.
If you experience any of the above symptoms, tell your doctor immediately. These symptoms may be followed by more serious side effects if not treated immediately.
Symptoms of the underlying disease may reappear. A gradual dose reduction in 12.5 mg increments over one to two weeks is recommended if treatment needs to be discontinued. Your doctor will tell you how to reduce the daily dose of the drug. If you have to suddenly stop treatment with Azaleptin, you will need to consult your doctor.
If your doctor decides to restart treatment with Azaleptin and the last dose of Azaleptin was taken more than two days ago, the recommended starting dose should be 12.5 mg.
If you have other additional questions related to the use of this drug, consult your doctor or pharmacist.
Description of the drug AZALEPTIN
When used simultaneously with drugs that have a depressant effect on the central nervous system (including benzodiazepine derivatives), ethanol-containing drugs, ethanol, the severity and frequency of manifestations of the inhibitory effect on the central nervous system and increased depression of the respiratory center increase.
When used simultaneously with drugs that cause arterial hypotension, additive hypotensive effects are possible.
When used simultaneously with drugs that cause myelosuppression, the inhibitory effect on bone marrow hematopoiesis may be enhanced; with anticholinergic drugs - the anticholinergic effect may be enhanced.
When used simultaneously with digoxin or with drugs characterized by high protein binding (including heparin, warfarin, phenytoin), their concentrations in the blood plasma may increase, and clozapine may also be displaced by these drugs from the sites of its protein binding.
When used simultaneously with valproic acid, a change in the concentration of clozapine in the blood plasma is possible, while clinical manifestations of the interaction were practically absent.
When used simultaneously with carbamazepine, the concentration of clozapine in the blood plasma decreases. Cases of severe pancytopenia and neuroleptic malignant syndrome have been described.
When used simultaneously with caffeine, the concentration of clozapine in the blood plasma increases and the incidence of side effects may increase.
When used simultaneously with lithium carbonate, myoclonus, convulsions, neuroleptic malignant syndrome, delirium, and psychosis are possible.
When used simultaneously with risperidone, an increase in the concentration of clozapine in the blood plasma is possible, apparently due to a competitive effect on the CYP2D6 isoenzyme, which leads to inhibition of the metabolism of clozapine. When quickly replacing clozapine with risperidone, dystonia may develop.
Rifampicin may increase the rate of metabolism of clozapine by inducing the isoenzymes CYP1A2 and CYP3A.
When used simultaneously with phenytoin, a decrease in the concentration of clozapine in the blood plasma is possible; with fluoxetine, paroxetine, sertraline, fluvoxamine, it is possible to increase the concentration of clozapine in the blood plasma, which in some patients is accompanied by toxicity. This effect is especially pronounced when clozapine is used concomitantly with fluvoxamine.
When used simultaneously with ciprofloxacin, it is possible to increase the concentration of clozapine in the blood plasma.
Azaleptin and its side effects
Clozapine, sold in Russia most often under the brand name Azaleptin, is an atypical antipsychotic. In fact, azaleptin may cause side effects, some of which are serious and potentially fatal. Common side effects of azaleptine include: constipation, night sweats, drooling, muscle rigidity, sedation, tremor, orthostatic hypotension, hyperglycemia, weight gain. The risk of extrapyramidal symptoms, such as tardive dyskinesia, is lower than with classical antipsychotics (typical antipsychotics); this may be due to the anticholinergic effects of clozapine. Extrapyramidal symptoms may be somewhat less severe after the patient switches from another antipsychotic to clozapine.
Azaleptin is rare, but still dangerous in relation to the development of agranulocytosis while taking it. Agranulocytosis occurs in about 1% of people who take clozapine during the first few months of treatment, and the risk of developing it is highest in about the first three months of treatment and decreases significantly thereafter, to less than 0.01% after a year. In the context of the trials, potentially dangerous low white blood cell counts appear to be more common in children and adolescents and in older adults than in young or middle-aged adults.)
Myocarditis is a sometimes fatal side effect of clozapine that usually develops within the first month of treatment. The first manifestations of the disease are fever, which may be accompanied by symptoms associated with an infection of the upper respiratory tract, gastrointestinal tract, or urinary tract. Monitoring guidelines recommend testing CRP (c-reactive protein) and troponin at baseline and every other week and every week for the first four weeks after starting azaleptin (clozapine) treatment and monitoring patients. Signs of heart failure are less common and may develop in parallel with the rise in troponin.
Another grossly underappreciated and potentially life-threatening side effect is decreased gastrointestinal contractions, which may manifest as severe constipation, intestinal obstruction, acute megacolon, ischemia, or necrosis. Colonic hypomotility has been shown to occur in up to 80% of people taking azaleptin when gastrointestinal function is objectively measured with radiopaque markers. The gastrointestinal wasting expected from clozapine now carries the risk of a higher mortality rate than the more well-known side effect of agranulocytosis. Monitoring bowel function and preferential use of laxatives in all patients treated with clozapine have been shown to improve colonic transit time and reduce the serious effects of azaleptine therapy.
Although clozapine is a muscarinic antagonist of the M1, M2, M3, and M5 receptors, azaleptin is also a full agonist of the M4 receptor. Because M4 is highly expressed in the salivary gland, its M4 agonist activity is thought to be responsible for hypersalivation.
Side effects of azaleptin on the central nervous system are varied and include: drowsiness, dizziness, headache, tremor, fainting, sleep disturbance, depression, anxiety, seizures, fatigue. There are also nightmares here. Like other antipsychotics, clozapine is rarely associated with neuroleptic malignant syndrome.
While taking azaleptin, leukopenia, neutropenia, suppression of bone marrow activity, dementia, and hypotension may occur.
. Treatment with azaleptin should begin with a small dose and slowly, ideally, once a week increasing it, under the control of determining the concentration of azaleptin (clozapine) in the blood. In our practice, we quite often encountered very high concentrations of clozapine in the blood at seemingly fairly low doses of azaleptin.
Many male patients complain of cessation of ejaculation as a side effect of clozapine, although this side effect is rarely described in official medication guides.
Abrupt cessation of taking azaleptin can lead to cholinergic effects (rebound effect), impaired motor activity, and decompensation with signs of psychosis. It is recommended that patients, family members and caregivers be aware of the symptoms and risks of abruptly stopping clozapine. When discontinuing clozapine, a gradual dose reduction is recommended to reduce the intensity of withdrawal effects.
Azaleptin tablets 25 mg 50 pcs. in St. Petersburg
Agranulocytosis.
Because of the significant risk of agranulocytosis, a potentially life-threatening complication (see Side Effects), clozapine should only be used in patients with schizophrenia who are resistant to previous therapy, i.e.
who have no effect from the use of classical antipsychotics or are intolerant to them. Before starting treatment with clozapine, it is necessary to ensure that white blood counts are normal. During the treatment period, it is necessary to regularly determine the number of leukocytes and, preferably, the absolute number of neutrophils (weekly for the first 18 weeks, then at least once a month throughout the course and 1 month after the end of treatment). If granulocytopenia occurs, treatment is stopped immediately. Epileptic seizures
(see "Side effects"). Clozapine lowers the seizure threshold in a dose-dependent manner and may cause myoclonic muscle contractions or generalized seizures. The occurrence of these symptoms is more likely with a rapid increase in the dose of the drug and in patients with epilepsy. In this case, the dose should be reduced and anticonvulsant therapy adjusted if necessary.
Myocarditis.
Analysis of a database of post-marketing reports suggests that the use of clozapine is associated with an increased risk of fatal myocarditis, especially in the first month of treatment. In patients with suspected myocarditis, clozapine treatment should be discontinued immediately.
Other adverse cardiovascular and respiratory effects
(see "Side effects"). Orthostatic hypotension with or without syncope may occur during treatment with clozapine. Rarely, collapse can be quite severe and may be accompanied by respiratory arrest and/or cardiac arrest. Orthostatic hypotension is usually noted during the initial dose titration due to rapid dose increases. Caution is warranted in patients who have taken benzodiazepines or other psychotropic drugs because they have experienced collapse, respiratory arrest, and cardiac arrest during initial treatment.
Increased mortality in older patients with dementia-associated psychosis
. Elderly patients with dementia-related psychosis are at increased risk of mortality when treated with antipsychotic drugs. An analysis of 17 placebo-controlled trials (lasting 10 weeks) in patients taking atypical antipsychotics found a risk of drug-related mortality that was 1.65 times greater than that in the placebo group. Over the course of a typical 10-week controlled study, the percentage of deaths associated with the drug was 4.5, compared with 2.6 in the placebo group. Although the causes of death varied, most deaths appeared to be related to either cardiovascular (heart failure, sudden death) or infectious (pneumonia) complications. Observational studies indicate that mortality may be increased with both atypical antipsychotics and traditional antipsychotics. How much of the increase in mortality in observational studies can be attributed to the effects of antipsychotics and how much to the condition of the patients themselves remains unclear. However, clozapine is not approved for the treatment of psychosis in patients with dementia.
