Atypical neuroleptic of Inveg in the therapy of schizophrenia and schizoaffective disorder

Invega( Paliperidone) belongs to the group of atypical antipsychotics. Use a medication for the therapy of schizophrenia and schizoaffective disorder.

The drug is an altered molecule of its precursor to risperidone, in contrast to which Invega has fewer side effects, as well as better quality and stability of therapy.

In the liver, risperidone is converted into the active substance paliperidone, the molecules of which bind to serotoninergic 5 - HT and dopaminergic D - 2 receptors of the brain structures, providing an antipsychotic effect. If the patient has a history of liver failure, then complications and adverse reactions are possible.

The drug is available in tablets with a dosage of 3, 6, 9 and 12 mg.

Pharmacological profile

The molecule of paliperidone has one additional hydroxyl group in comparison with risperidone. Because of this, the liver is not capable of metabolizing the drug, most of the medication is excreted by the kidneys.

Due to this effect, Invega practically does not interact with drugs metabolized in the liver. The drug is safe to prescribe to patients who have mild or moderate severity of the liver.

An additional positive point is that Invega gives a faster therapeutic effect, and there is no need for a gradual increase in dosage.

In the manufacture of a medicine, the principle of osmotic release of the active substance is used. Osmotic pressure contributes to the release of medication at a certain rate.

The capsule has a core consisting of three levels. It is surrounded by a semipermeable membrane and a membrane. Two core layers contain the main component of the drug and additional substances.

In the third, ejection layer, there are osmotic structures. On the layers containing the medicine, there are 2 holes. Through them, the active substance is gradually released within a day.

In the stomach and intestines, the drug coating dissolves. The membrane is impregnated with water, which then penetrates into the core. Its hydrophilic polymers swell and form a gel that contains the drug. Subsequently, the gel is squeezed through these openings.

Insoluble constituent capsules are excreted with feces. Therefore, in the feces, you can notice the secretive pill. This is normal.

A stable level of the drug in the blood is formed about 5 days after the start of treatment and from this point on it has a stable therapeutic effect.

Indications and contraindications for the use of

Invego are used for the following purposes:

• for the long-term treatment of various forms of schizophrenia and relief of the exacerbations of this disease;
• has been successfully used to treat schizoaffective conditions.
• in the treatment of bipolar disorder.

Contraindications for use are as follows:

• intolerance of the active ingredient of a medicament or any other substance in its composition;
• Acute psychomotor agitation with anxiety, affective disorder, delirium.

Rules for taking and dosage

The drug is taken in the morning. The time of reception is not related to eating. It is necessary to swallow a whole capsule, you can not violate the integrity of the pill!

When the dose is selected, the weight of a person is taken into account. For people weighing up to 50 kg, the dosage of the drug is usually not more than 6 mg / day. For patients weighing 50 - 70 kg, the average dose of the drug is 9 mg.

For people of average weight who have not previously taken antipsychotics, or if they used this group of drugs during treatment for exacerbation of schizophrenia( duration not more than 2 months), treatment should be started at 6 mg / day.

Patients with a mass above 85 kg, as well as people who had a therapeutic effect in the past only from taking high doses of antipsychotics, should start taking with 9 mg.

Sometimes, in patients weighing more than 70 kg, the "working" dose is 12 mg.

Almost always individually selected dosage of the drug does not need a subsequent increase. The medication is effective for the therapy of schizophrenia during an exacerbation and as a supporting treatment.

With proper therapy, the full anti-productive effect of the antipsychotic medication is manifested by 4 to 6 weeks from the start of the admission, and the anti-deficiency effect by 8 to 12 months of continuous treatment.

That is, with a good tolerability of the drug, even after exiting the area of ​​exacerbation, the dose can not be reduced.

The reason for reducing dosage is the occurrence and persistence of more than 7 days of adverse events, such as:

• dizziness;
• drowsiness;
• mild diarrheal disorders.

In case of intolerance or in case of severe complications, the medicine is immediately canceled. But such situations are quite rare.

The question of a possible replacement of the remedy, if there are no serious side effects, should be placed no earlier than 3 to 4 weeks.from the start of therapy.

Clinical effect of

Paliperidone significantly reduces both positive manifestations of schizophrenia( delirium, thinking disorders, hallucinations), and negative symptoms( affect flattening, emotional closure, spontaneity disorder).

Of particular importance is the reduction of negative symptoms - this, as a rule, can not be achieved with the treatment of typical antipsychotic drugs. They usually eliminate only positive symptoms. There is an improvement in night sleep in the absence of sleepiness during the day.

Does not produce insomnia, anxiety. When using medicament there are no manifestations of agitation.

The drug has a more pronounced sedative effect. However, the inhibition and lethargy, characteristic of sedative antipsychotics, is absent.

Cases of overdose

When the dose is exceeded, the pharmacological properties of the drug increase.

Often there is a syndrome of prolonged QT interval with the development of a life-threatening arrhythmia.

Malignant neuroleptic syndrome develops, which is the cause of acute poisoning and lethal cases.

It occurs in approximately 0.1% of patients who are on inpatient treatment and receive antipsychotics.

Neuroleptic syndrome is manifested by four clinical signs:

• increased muscle tone;
• hyperthermia;
• mental disorders;
• is a vegetative "storm".

Conscious overdose for suicide

Another cause of acute poisoning is not the medical use of the drug by patients with a view to suicide.

Suicide is a serious danger for patients with schizophrenia. Among such patients mortality from accidents, physical illnesses and suicide is high, in comparison with ordinary people, as well as patients suffering from other mental disorders.

To predict the likelihood of suicide in individuals with schizophrenia is difficult. This can happen both during inpatient treatment and on an outpatient basis.

Irregular intake of the drug or complete rejection of it leads to an exacerbation of the disease. This increases the possibility of suicide using the same medication.

Overdose treatment is symptomatic. There is no antidote.

In case of severe symptoms, treatment takes place in the intensive care unit. Conducted:

• intubation to ensure respiratory function;
• oxygenation;
• rinsing of the stomach, intestines;
• detoxification therapy;
• ECG monitoring, treatment of heart rhythm disturbances;
• therapy of collapse, hypotension;
• is administered m-cholinergic blockers for extrapyramidal disorders.

Adverse reactions

Invega is much less common than its predecessor risperidone causes drowsiness, dyspepsia, dizziness.

Dry mouth, tremors, headaches, increased pressure, orthostatic pressure drop, increased QT interval - occur at a frequency of less than 5%.Tachycardia is much more common.

Extrapyramidal effects from the drug( akathisia, hypersalivation, rigidity, hypokinesia, acute dystonia) depend on the dose.

When using up to 6 mg of medication, adverse events occur at the same frequency as with placebo( up to 13%).

When taking 9-12 mg / day, about 26% of patients have side effects. The severity of extrapyramidal symptoms is small.

The possibility of their occurrence increases in patients:

• with severe cerebral insufficiency;
• in people who had long been taking typical antipsychotics.

The most vivid extrapyramidal disorders are expressed in the first three days of treatment. They decrease in 1-3 months, and then completely pass.

Other adverse events:

• memory impairment, decreased speed of thinking and reaction to external stimuli, etc.;
• cerebrovascular deficit.

Risk:

• worsening carbohydrate metabolism;
• is an extension of the QT interval on a cardiogram, which is manifested by severe arrhythmia leading to death.

Weight gain of patients occurs within 2 months of treatment, an average of 700 grams. A significant weight gain( more than 7% of the initial weight) is rare and is associated with the dosage of the drug. To curb weight gain, there is no need to prescribe higher doses.

People who are prone to obesity are additionally prescribed diet and exercise.

An increase in prolactin levels in the blood is detected in 67% of patients by the end of the 2nd week of treatment with paliperidone. Then this indicator remains on the same level. Possible manifestations of hyperprolactinaemia:

• discharge from the nipples;
• termination of menstruation;
• gynecomastia;
• sexual dysfunction, etc.

But they appear only in 2% of patients who use the drug. This advantageously distinguishes it from risperidone and other classical antipsychotics.

Special instructions

Inveg tablets practically do not change their shape when passing the stomach and intestines. Therefore, they can not be taken:

• patients with significant narrowing of any of the digestive tract;
• to patients with impaired swallowing.

Such people occasionally may have a violation of the patency of the stomach or intestines, associated with the use of undeformable drugs.

Combination with alcohol

Care must be taken during treatment with alcohol, because the drug acts directly on the brain. It is better not to drink alcohol.

Assignments for impaired renal and hepatic function

Drug dose is reduced with moderate and severe renal impairment. With moderate and moderate severity of liver function, dosage should not be changed.

Interaction with other drugs

Before starting treatment and one week after the start of therapy, it is necessary to register a cardiogram to exclude the expansion of the QT interval.

It is not recommended to use the medication for psychosis therapy against the background of dementia because of the danger of cerebrovascular complications.

Because of possible impairment of brain activity, metabolic disorders and QT interval expansion, it is not recommended to combine Invega with:

• tricyclic antidepressants;
• with quetiapine;
• in-blockers.

Pregnancy and lactation

Paliperidone is not prescribed to women while breastfeeding and pregnant.

In exceptional cases, the drug is prescribed to pregnant women if the benefit to the mother is more harmful to the fetus.

Admission of children

Assign for the treatment of schizophrenia with 12 years. In adolescents, the starting dose is 3 mg in the morning. Some can increase the dose to 6 - 12 mg.

Practical experience of using

The opinion of practicing doctors and reviews of patients who took Invega's medicine for a long time.

From the psychiatric practice of

The doctor appointed Invega to a 25-year-old patient who was hospitalized for the third time. When taking classical neuroleptics, the productive symptomatology did not stop.

The patient remained indifferent. The drug is prescribed at 6 mg / day. After 2 weeks, the patient began to change. He woke up emotions, began to communicate, be included in the work processes, lost "apathy to everything that is happening", there was a potential for action.

Other case. ..

Three patients taking haloperidol for a long time were transferred to Paliperidone. At patients at change of a preparation mental processes have improved, social activity has increased.

All three had an exacerbation within 3 months, which required hospitalization. The dose of the drug was increased to 12 mg. The timing of the release of their course of therapy is the same as on Haloperidol.

Viewpoint of the patients themselves

Cost and analogues

The price of one pack of medicine of Invega for 28 tablets lies in the area of ​​6634 - 10198 rubles, depending on the pharmacy.

Store the drug in an inaccessible place for children. Temperature 15 - 30 degrees Celsius. Shelf life - 24 months. Let go in pharmacies, according to the prescription.

Molecular analogues of Invega preparation containing paliperidone in the composition do not exist now.

In the market there is only an original preparation produced by Jansen-Silag, the USA in two forms:

• tablets for daily intake of 3, 6, 9 and 12 mg;
• Xseplion - suspension B - M 50, 100, 150 mg, syringe number 1.